MA30208B1 - Derives de pyrimidine utilises en tant qu'inhibiteurs de kinase pi -3 - Google Patents

Derives de pyrimidine utilises en tant qu'inhibiteurs de kinase pi -3

Info

Publication number
MA30208B1
MA30208B1 MA31157A MA31157A MA30208B1 MA 30208 B1 MA30208 B1 MA 30208B1 MA 31157 A MA31157 A MA 31157A MA 31157 A MA31157 A MA 31157A MA 30208 B1 MA30208 B1 MA 30208B1
Authority
MA
Morocco
Prior art keywords
kinase inhibitors
pyrimidine derivatives
alone
pharmaceutically acceptable
combination
Prior art date
Application number
MA31157A
Other languages
English (en)
Inventor
Matthew Burger
Zhi-Jie Ni
Sabina Pecchi
Gordana Atallah
Sarah Bartulis
Kelly Frazier
Aaron Smith
Joelle Verhagen
Yanchen Zhang
Allan Wagman
Simon Ng
Keith Pfister
Daniel Poon
Alicia Louie
Teresa Pick
Paul Barsanti
Edwin Iwanowicz
Wendy Fantl
Thomas Hendrickson
Mark Knapp
Hanne Meritt
Charles Voliva
Marion Wiesmann
Xiahua Xin
Original Assignee
Hanne Meritt
Charles Voliva
Marion Wiesmann
Xiahua Xin
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=37951939&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=MA30208(B1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Hanne Meritt, Charles Voliva, Marion Wiesmann, Xiahua Xin filed Critical Hanne Meritt
Publication of MA30208B1 publication Critical patent/MA30208B1/fr

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

La présente invention concerne des composés (I) inhibiteurs de phosphatidylinositol 3-kinase (PI), leurs sels pharmaceutiquement acceptables et des promédicaments de ceux-ci ; des compositions des nouveaux composés, soit seuls soit en association avec au moins un agent thérapeutique supplémentaire, avec un excipient pharmaceutiquement acceptable ; et des utilisations des nouveaux composés, soit seuls soit en association avec au moins un agent thérapeutique supplémentaire dans la prophylaxie ou le traitement de maladies prolifératives caractérisées par l'activité anormale de facteurs de croissance, de protéines sérine/thréonine kinases et des phospholipides kinases.
MA31157A 2006-01-20 2008-08-06 Derives de pyrimidine utilises en tant qu'inhibiteurs de kinase pi -3 MA30208B1 (fr)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US76078906P 2006-01-20 2006-01-20

Publications (1)

Publication Number Publication Date
MA30208B1 true MA30208B1 (fr) 2009-02-02

Family

ID=37951939

Family Applications (1)

Application Number Title Priority Date Filing Date
MA31157A MA30208B1 (fr) 2006-01-20 2008-08-06 Derives de pyrimidine utilises en tant qu'inhibiteurs de kinase pi -3

Country Status (40)

Country Link
US (2) US8217035B2 (fr)
EP (2) EP2261223B1 (fr)
JP (1) JP5161110B2 (fr)
KR (1) KR101353829B1 (fr)
CN (1) CN101389622B (fr)
AR (2) AR059087A1 (fr)
AT (1) ATE478064T1 (fr)
AU (1) AU2007206048B2 (fr)
BR (1) BRPI0707189B1 (fr)
CA (1) CA2636993C (fr)
CR (1) CR10163A (fr)
CY (1) CY1111091T1 (fr)
DE (1) DE602007008529D1 (fr)
DK (2) DK1984350T3 (fr)
EA (1) EA018083B1 (fr)
EC (1) ECSP088630A (fr)
ES (2) ES2427624T3 (fr)
GE (1) GEP20115147B (fr)
GT (1) GT200800143A (fr)
HN (1) HN2008001144A (fr)
HR (2) HRP20100603T1 (fr)
IL (1) IL192763A (fr)
JO (1) JO2660B1 (fr)
MA (1) MA30208B1 (fr)
ME (2) MEP3908A (fr)
MY (1) MY144233A (fr)
NO (1) NO342183B1 (fr)
NZ (1) NZ569771A (fr)
PE (1) PE20071322A1 (fr)
PL (2) PL1984350T3 (fr)
PT (2) PT1984350E (fr)
RS (2) RS52928B (fr)
SI (2) SI1984350T1 (fr)
SM (1) SMP200800048B (fr)
SV (1) SV2008002984A (fr)
TN (1) TNSN08305A1 (fr)
TW (2) TW201315723A (fr)
UA (1) UA96284C2 (fr)
WO (1) WO2007084786A1 (fr)
ZA (1) ZA200806017B (fr)

Families Citing this family (365)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JO2660B1 (en) 2006-01-20 2012-06-17 نوفارتيس ايه جي Pi-3 inhibitors and methods of use
TW200808739A (en) 2006-04-06 2008-02-16 Novartis Vaccines & Diagnostic Quinazolines for PDK1 inhibition
MX2009002046A (es) 2006-08-24 2009-03-06 Astrazeneca Ab Derivados de morfolino pirimidina utiles en el tratamiento de trastornos proliferativos.
WO2008070740A1 (fr) 2006-12-07 2008-06-12 F.Hoffmann-La Roche Ag Composés inhibant la phosphoinositide 3 kinase et procédés d'utilisation
WO2008098058A1 (fr) * 2007-02-06 2008-08-14 Novartis Ag Inhibiteurs de la pi3-kinase et procédés de leur utilisation
JP5676249B2 (ja) * 2007-04-20 2015-02-25 プロビオドルグ エージー グルタミニルシクラーゼ阻害剤としてのアミノピリジン誘導体
CA2687931C (fr) 2007-05-31 2016-05-24 Boehringer Ingelheim International Gmbh Antagonistes des recepteurs ccr2 et utilisations de ceux-ci
CN101809002B (zh) 2007-07-09 2013-03-27 阿斯利康(瑞典)有限公司 用于与mtor激酶和/或pi3k相关的疾病中的吗啉代嘧啶衍生物
WO2009017838A2 (fr) * 2007-08-01 2009-02-05 Exelixis, Inc. Combinaisons d'inhibiteurs jak-2 et d'autres agents
US20100311736A1 (en) * 2007-10-22 2010-12-09 Glaxosmithkline Llc Pyridosulfonamide derivatives as p13 kinase inhibitors
WO2009066084A1 (fr) * 2007-11-21 2009-05-28 F. Hoffmann-La Roche Ag 2-morpholinopyrimidines et leur utilisation en tant qu'inhibiteurs de kinase pi3
WO2009093981A1 (fr) * 2008-01-23 2009-07-30 S Bio Pte Ltd Composés de triazine comme inhibiteurs de la kinase
MX2010009743A (es) 2008-03-05 2010-09-28 Novartis Ag Uso de derivados de pirimidina para el tratamiento de las enfermedades dependientes de los receptores del factor de crecimiento epidermico (egfr) o de enfermedades que hayan adquirido resistencia a los agentes que se dirigen a los miembros de la fami
BRPI0909082A2 (pt) * 2008-03-26 2019-02-26 Novartis Ag imidazoquinolinas e derivados de pirimidina como moduladores potentes de processos angiogênicos acionados por vegf
AU2012203914C1 (en) * 2008-03-26 2013-11-28 Novartis Ag 5imidazoquinolines and pyrimidine derivatives as potent modulators of VEGF-driven angiogenic processes
EP2276750A2 (fr) * 2008-03-27 2011-01-26 Auckland Uniservices Limited Pyrimidines et triazines substituées, et leur utilisation en thérapie anticancéreuse
US9273077B2 (en) 2008-05-21 2016-03-01 Ariad Pharmaceuticals, Inc. Phosphorus derivatives as kinase inhibitors
PT2300013T (pt) 2008-05-21 2017-10-31 Ariad Pharma Inc Derivados de fósforo como inibidores de cinases
EP2310391A1 (fr) * 2008-06-27 2011-04-20 S*BIO Pte Ltd Purines substituées par la pyrazine
KR20110028651A (ko) * 2008-07-11 2011-03-21 노파르티스 아게 (a) 포스포이노시타이드 3-키나제 억제제 및 (b) ras/raf/mek 경로의 조절제의 조합물
PE20110196A1 (es) * 2008-07-29 2011-04-03 Boehringer Ingelheim Int 5-alquinil-pirimidinas
WO2010030967A1 (fr) * 2008-09-12 2010-03-18 Wyeth Llc 4-aryloxyquinolin-2(1h)-ones utiles en tant qu'inhibiteurs de la kinase mtor et de la kinase pi3, devant servir en tant qu'agents anticancéreux
EP2617414A3 (fr) * 2008-10-01 2013-11-06 Novartis AG Antagonisme lissé pour le traitement de troubles liés à la voie Hedgehog
TWI378933B (en) 2008-10-14 2012-12-11 Daiichi Sankyo Co Ltd Morpholinopurine derivatives
MX2011004585A (es) * 2008-10-31 2011-06-01 Novartis Ag Combinacion de un inhibidor de fosfatidilinositol-3-cinasa (p13k) y un inhibidor de mtor.
US8653098B2 (en) * 2008-11-20 2014-02-18 Genentech, Inc. Pyrazolopyridine PI3K inhibitor compounds and methods of use
HUE025547T2 (en) 2008-12-19 2016-02-29 Boehringer Ingelheim Int Cyclic pyrimidine-4-carboxamides as CCR2 receptor antagonists for the treatment of inflammation, asthma and COPD
KR20110123253A (ko) 2009-03-05 2011-11-14 다이이찌 산쿄 가부시키가이샤 피리딘 유도체
SG174527A1 (en) 2009-03-27 2011-11-28 Pathway Therapeutics Inc Pyrimidinyl and 1,3,5-triazinyl benzimidazole sulfonamides and their use in cancer therapy
CA2754343A1 (fr) * 2009-04-09 2010-10-14 Oncothyreon, Inc. Methodes et compositions d'inhibiteurs de pi3 kinase utilisees dans le traitement des fibroses
UY32582A (es) 2009-04-28 2010-11-30 Amgen Inc Inhibidores de fosfoinositida 3 cinasa y/u objetivo mamífero
CN102958518A (zh) * 2009-05-15 2013-03-06 诺瓦提斯公司 磷脂酰肌醇3-激酶抑制剂和抗糖尿病化合物的组合
CN102459272B (zh) * 2009-05-27 2014-08-06 健泰科生物技术公司 对P110δ具有选择性的为PI3K抑制剂的二环嘧啶化合物和使用方法
US8486939B2 (en) 2009-07-07 2013-07-16 Pathway Therapeutics Inc. Pyrimidinyl and 1,3,5-triazinyl benzimidazoles and their use in cancer therapy
US20120065166A1 (en) * 2009-08-12 2012-03-15 Virginia Espina Bone Modulators And Methods Therewith
CN101993416B (zh) * 2009-08-27 2013-09-11 中国科学院上海药物研究所 喹啉类化合物、其制备方法、包含该化合物的药物组合物及该化合物的用途
EP2475375A4 (fr) * 2009-09-09 2013-02-20 Avila Therapeutics Inc Inhibiteurs de pi3 kinase et leurs utilisations
NZ599290A (en) 2009-10-16 2014-10-31 Melinta Therapeutics Inc Antimicrobial compounds and methods of making and using the same
MX2012004341A (es) 2009-10-16 2012-10-05 Rib X Pharmaceuticals Inc Compuestos antimicrobianos y metodos para fabricar y utilizar los mismos.
ES2674275T3 (es) 2009-12-17 2018-06-28 Centrexion Therapeutics Corporation Antagonistas del receptor CCR2 y usos de los mismos
GB201004200D0 (en) 2010-03-15 2010-04-28 Univ Basel Spirocyclic compounds and their use as therapeutic agents and diagnostic probes
WO2011141477A1 (fr) 2010-05-12 2011-11-17 Boehringer Ingelheim International Gmbh Nouveaux antagonistes du récepteur ccr2, leur procédé de production et leur utilisation en tant que médicaments
EP2569298B1 (fr) 2010-05-12 2015-11-25 Boehringer Ingelheim International GmbH Nouveaux antagonistes du récepteur ccr2, son procédé de production et utilisation associée en tant que médicaments
WO2011144501A1 (fr) 2010-05-17 2011-11-24 Boehringer Ingelheim International Gmbh Antagonistes du récepteur ccr2 et leurs utilisations
EP2576542B1 (fr) 2010-05-25 2015-04-22 Boehringer Ingelheim International GmbH Dérivés d'amide cycliques d'acides pyridazine-3-carboxyliques utiles dans le traitement de maladies respiratoires, liées à des douleurs, liées au système immunitaire et cardiovasculaires
EP2576538B1 (fr) 2010-06-01 2015-10-28 Boehringer Ingelheim International GmbH Nouveaux antagonistes de CCR2
SA111320519B1 (ar) 2010-06-11 2014-07-02 Astrazeneca Ab مركبات بيريميدينيل للاستخدام كمثبطات atr
CN103209955A (zh) 2010-09-07 2013-07-17 第一三共株式会社 制备安息香酸酯的方法
EP2621908A2 (fr) * 2010-10-01 2013-08-07 Novartis AG Procédé de fabrication de dérivés de pyrimidine
BR112013008816A2 (pt) * 2010-10-14 2016-06-28 Ariad Pharma Inc método de tratamento de câncer direcionado ao egfr resistente à erlotinibe ou gefitinibe, ou uso de um sal farmacêuticamente aceito em um indivíduo
KR20130101111A (ko) * 2010-11-12 2013-09-12 바이엘 인텔렉쳐 프로퍼티 게엠베하 프로프-2-엔-1-아민으로부터 2,2-디플루오로에틸아민의 제조방법
WO2012065021A1 (fr) 2010-11-12 2012-05-18 Board Of Regents, The University Of Texas System Polythérapie à la dexaméthasone
AU2011346567A1 (en) * 2010-12-21 2013-07-25 Novartis Ag Bi-heteroaryl compounds as Vps34 inhibitors
WO2012109423A1 (fr) 2011-02-11 2012-08-16 Dana-Farber Cancer Institute, Inc. Procédé d'inhibition de cellules tumorales d'hamartome
CZ305457B6 (cs) 2011-02-28 2015-09-30 Ústav organické chemie a biochemie, Akademie věd ČR v. v. i. Pyrimidinové sloučeniny inhibující tvorbu oxidu dusnatého a prostaglandinu E2, způsob výroby a použití
ES2608967T3 (es) 2011-03-28 2017-04-17 Mei Pharma, Inc. (Aralquilamino sustituido en alfa y heteroarilalquilamino)pirimidinil y 1,3,5-triazinil benzimidazoles, composiciones farmacéuticas que los contienen, y estos compuestos para usar en el tratamiento de enfermedades proliferativas
US9834518B2 (en) 2011-05-04 2017-12-05 Ariad Pharmaceuticals, Inc. Compounds for inhibiting cell proliferation in EGFR-driven cancers
CN103635189B (zh) * 2011-07-01 2016-05-04 诺华股份有限公司 用于治疗癌症的含有cdk4/6抑制剂和pi3k抑制剂的联合治疗
EP2731941B1 (fr) 2011-07-15 2019-05-08 Boehringer Ingelheim International GmbH Antagonistes ccr2, nouveaux et sélectifs
EP2734205B1 (fr) 2011-07-21 2018-03-21 Tolero Pharmaceuticals, Inc. Inhibiteurs de protéine kinase hétérocycliques
CN103764144B (zh) 2011-08-31 2016-07-20 诺华股份有限公司 Pi3k抑制剂与mek抑制剂的协同组合
JP2014527542A (ja) * 2011-09-01 2014-10-16 ノバルティス アーゲー 骨がんの治療に使用するためまたは原発がん細胞の骨への転移性播種を予防するためのpi3k阻害剤
KR20140069235A (ko) 2011-09-27 2014-06-09 노파르티스 아게 돌연변이체 idh의 억제제로서의 3-피리미딘-4-일-옥사졸리딘-2-온
WO2013049581A1 (fr) * 2011-09-30 2013-04-04 Beth Israel Deaconess Medical Center Inc. Compositions et méthodes de traitement de maladies de prolifération
KR20140096035A (ko) * 2011-10-28 2014-08-04 노파르티스 아게 위장 기질 종양을 치료하는 방법
EP2780017A1 (fr) * 2011-11-15 2014-09-24 Novartis AG Combinaison d'un inhibiteur de la phosphoinositide 3-kinase et d'un modulateur de la voie janus kinase 2 - transducteur de signal et activateur de transcription 5
UY34632A (es) * 2012-02-24 2013-05-31 Novartis Ag Compuestos de oxazolidin- 2- ona y usos de los mismos
JP6378171B2 (ja) 2012-04-24 2018-08-22 バーテックス ファーマシューティカルズ インコーポレイテッドVertex Pharmaceuticals Incorporated Dna−pk阻害剤
US20150166591A1 (en) 2012-05-05 2015-06-18 Ariad Pharmaceuticals, Inc. Methods and compositions for raf kinase mediated diseases
KR20150009540A (ko) * 2012-05-16 2015-01-26 노파르티스 아게 Pi-3 키나제 억제제에 대한 투여 요법
JP6301316B2 (ja) 2012-05-23 2018-03-28 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft 内胚葉細胞および肝実質細胞の組成物ならびにそれらの細胞を入手および使用する方法
RU2014154009A (ru) 2012-06-06 2016-08-10 Новартис Аг Комбинация ингибитора 17-альфа-гидроксилазы (с17,20-лиазы) и специфического ингибитора pi-3k для лечения онкологического заболевания
WO2013192367A1 (fr) 2012-06-22 2013-12-27 Novartis Ag Traitement d'une tumeur neuroendocrine
EP2869818A1 (fr) 2012-07-06 2015-05-13 Novartis AG Combinaison d'un inhibiteur de phosphoinositide 3-kinase et d'un inhibiteur de l'interaction il-8/cxcr
WO2014016849A2 (fr) 2012-07-23 2014-01-30 Sphaera Pharma Pvt. Ltd. Nouveaux composés de triazine
HK1211476A1 (en) * 2012-08-16 2016-05-27 Novartis Ag Combination of pi3k inhibitor and c-met inhibitor
CN102952086B (zh) * 2012-09-28 2013-08-28 天津科创医药中间体技术生产力促进有限公司 一种2-吗啉基取代嘧啶类化合物的制备方法
DK2909181T3 (da) 2012-10-16 2017-11-20 Tolero Pharmaceuticals Inc PKM2-modulatorer og fremgangsmåder til anvendelse deraf
PL2912030T3 (pl) * 2012-10-23 2017-02-28 Novartis Ag Ulepszony sposób wytwarzania 5-(2,6-di-4-morfolinylo-4-pirymidynylo)-4- trifluorometylopirydyno-2-aminy
US9296733B2 (en) * 2012-11-12 2016-03-29 Novartis Ag Oxazolidin-2-one-pyrimidine derivative and use thereof for the treatment of conditions, diseases and disorders dependent upon PI3 kinases
JP6322200B2 (ja) 2012-11-16 2018-05-09 メルク・シャープ・アンド・ドーム・コーポレーションMerck Sharp & Dohme Corp. ヒトホスファチジルイノシトール3−キナーゼデルタのプリン阻害剤
WO2014093230A2 (fr) * 2012-12-10 2014-06-19 Merck Patent Gmbh Compositions et procédés de fabrication de composés pyrimidine et pyridine ayant une activité inhibitrice de btk
EP2742940B1 (fr) 2012-12-13 2017-07-26 IP Gesellschaft für Management mbH Sel de fumarate de (R)-3-(6-(4-methylphenyl)-pyridin-3-yloxy)-l-aza-bicyclo-[2.2.2]octane destinés à être administrés une fois par jour, deux fois par jour ou trois fois par jour
WO2014090147A1 (fr) * 2012-12-14 2014-06-19 上海恒瑞医药有限公司 Dérivés de pyrimidine et leurs sels, leur procédé de préparation et leur utilisation pharmaceutique
DK2958943T3 (da) 2013-02-20 2019-12-09 Univ Pennsylvania Behandling af cancer ved anvendelse af humaniseret anti-EGFRvIII kimær antigenreceptor
GB201303109D0 (en) * 2013-02-21 2013-04-10 Domainex Ltd Novel pyrimidine compounds
ES2634020T3 (es) 2013-03-06 2017-09-26 Novartis Ag Formulaciones de compuestos orgánicos
SI3527563T1 (sl) 2013-03-12 2022-01-31 Vertex Pharmaceuticals Incorporated Inhibitorji DNA-PK
US9498532B2 (en) 2013-03-13 2016-11-22 Novartis Ag Antibody drug conjugates
MX394360B (es) 2013-03-14 2025-03-24 Sumitomo Pharma Oncology Inc Inhibidores de jak2 y alk2 y metodos para su uso.
EP2970240B1 (fr) 2013-03-14 2018-01-10 Novartis AG 3-pyrimidin-4-yl-oxazolidin-2-ones comme inhibiteurs d'idh mutante
US9242969B2 (en) 2013-03-14 2016-01-26 Novartis Ag Biaryl amide compounds as kinase inhibitors
NZ710929A (en) 2013-03-15 2018-02-23 Novartis Ag Antibody drug conjugates
UA118846C2 (uk) * 2013-03-21 2019-03-25 Новартіс Аг Комбінована терапія
US9611283B1 (en) 2013-04-10 2017-04-04 Ariad Pharmaceuticals, Inc. Methods for inhibiting cell proliferation in ALK-driven cancers
CA2907912A1 (fr) * 2013-05-01 2014-11-06 F. Hoffmann-La Roche Ag Pyrimidines a substitution heterocycloalkyle liees a c et leurs utilisations
PH12019502378A1 (en) 2013-05-01 2022-05-11 Hoffmann La Roche Biheteroaryl compounds and uses thereof
LT2994126T (lt) * 2013-05-07 2018-09-25 Novartis Ag Pi3 kinazės inhibitoriaus derinys su paklitakseliu, skirtas panaudoti galvos ir kaklo vėžio gydymui arba prevencijai
RU2015156221A (ru) 2013-06-11 2017-07-17 Новартис Аг Фармацевтические комбинация ингибитора pi3k и средства, дестабилизирующего микротрубочки
KR20160020502A (ko) 2013-06-18 2016-02-23 노파르티스 아게 제약 조합물
JP2016527305A (ja) 2013-08-08 2016-09-08 ノバルティス アーゲー Pimキナーゼ阻害剤の組合せ
KR102529049B1 (ko) 2013-08-14 2023-05-08 노파르티스 아게 암의 치료를 위한 조합 요법
WO2015022657A1 (fr) 2013-08-16 2015-02-19 Novartis Ag Combinaisons pharmaceutiques
CA2923214A1 (fr) 2013-09-09 2015-03-12 Melinta Therapeutics, Inc. Composes antimicrobiens et procedes de fabrication et d'utilisation de ces composes
EP3038623A4 (fr) 2013-09-09 2017-04-19 Melinta Therapeutics, Inc. Composés antimicrobiens et procédés de fabrication et méthodes d'utilisation de ceux-ci
CN103483345B (zh) * 2013-09-25 2016-07-06 中山大学 Pi3k激酶抑制剂、包含其的药物组合物及其应用
US10570204B2 (en) 2013-09-26 2020-02-25 The Medical College Of Wisconsin, Inc. Methods for treating hematologic cancers
RU2675270C2 (ru) 2013-10-17 2018-12-18 Вертекс Фармасьютикалз Инкорпорейтед Сокристаллы и содержащие их фармацевтические композиции
BR112016012141A2 (pt) 2014-01-15 2017-08-08 Novartis Ag "combinações farmacêuticas, uso das mesmas, e embalagem comercial"
SG10201900002QA (en) 2014-01-24 2019-02-27 Dana Farber Cancer Institue Inc Antibody molecules to pd-1 and uses thereof
EP3099717B1 (fr) 2014-01-31 2019-03-27 Novartis AG Molécules d'anticorps anti-tim-3 et leurs utilisations
WO2015131080A1 (fr) 2014-02-28 2015-09-03 Nimbus Lakshmi, Inc. Inhibiteurs de tyk2 et leurs utilisations
US20150259420A1 (en) 2014-03-14 2015-09-17 Novartis Ag Antibody molecules to lag-3 and uses thereof
RU2688665C2 (ru) 2014-04-22 2019-05-22 Университет Базель Новый способ получения производных триазина, пиримидина и пиридина
WO2016001789A1 (fr) * 2014-06-30 2016-01-07 Pfizer Inc. Dérivés de pyrimidine en tant qu'inhibiteurs de pi3k destinés à être utilisés dans le traitement du cancer
WO2016001341A1 (fr) * 2014-07-03 2016-01-07 F. Hoffmann-La Roche Ag Composés sulfonylaminopyridine, compositions et procédés d'utilisation associés
US10786578B2 (en) 2014-08-05 2020-09-29 Novartis Ag CKIT antibody drug conjugates
EP4578865A3 (fr) 2014-08-12 2025-07-30 Monash University Promédicaments dirigeant la lymphe
KR20170040249A (ko) 2014-08-12 2017-04-12 노파르티스 아게 항-cdh6 항체 약물 접합체
CN105330699B (zh) * 2014-08-13 2018-12-04 山东汇睿迪生物技术有限公司 一种含磷吡啶并[2,3-d]嘧啶-7-酮类化合物或其药学上可接受的盐、药物组合物及其应用
CN104151256B (zh) * 2014-08-14 2016-08-24 西安交通大学 二取代苯甲酰胺类化合物及其合成方法和应用
ES2771926T3 (es) 2014-09-13 2020-07-07 Novartis Ag Terapias de combinación
CN105461714B (zh) * 2014-09-29 2017-11-28 山东轩竹医药科技有限公司 并环类pi3k抑制剂
AU2015327868A1 (en) 2014-10-03 2017-04-20 Novartis Ag Combination therapies
MA41044A (fr) 2014-10-08 2017-08-15 Novartis Ag Compositions et procédés d'utilisation pour une réponse immunitaire accrue et traitement contre le cancer
TWI716362B (zh) 2014-10-14 2021-01-21 瑞士商諾華公司 針對pd-l1之抗體分子及其用途
JP6882978B2 (ja) 2014-10-29 2021-06-02 バイスクルアールディー・リミテッド Mt1−mmpに特異的な二環性ペプチドリガンド
MA40933A (fr) * 2014-11-11 2017-09-19 Piqur Therapeutics Ag Difluorométhyl-aminopyridines et difluorométhyl-aminopyrimidines
WO2016075670A1 (fr) 2014-11-14 2016-05-19 Novartis Ag Conjugués anticorps-médicament
CN105085476B (zh) * 2014-11-24 2018-03-09 苏州晶云药物科技有限公司 5‑[2,6‑二(4‑吗啉基)‑4‑嘧啶基]‑4‑(三氟甲基)‑2‑吡啶胺二盐酸盐的晶型及其制备方法
US10689459B2 (en) * 2014-12-12 2020-06-23 Novartis Ag Treatment of breast cancer brain metastases
AU2015366357B2 (en) * 2014-12-17 2018-07-19 Shanghai Haiyan Pharmaceutical Technology Co. Ltd. 2-morpholin-4,6-disubstituted pyrimidine derivative, and preparation method and pharmaceutical use thereof
WO2016100882A1 (fr) 2014-12-19 2016-06-23 Novartis Ag Polythérapies
CA2969090C (fr) 2014-12-23 2023-05-02 Novartis Ag Composes triazolopyrimidine et leurs utilisations
CN105832741A (zh) * 2015-01-16 2016-08-10 复旦大学 Pi3k抑制剂与紫杉醇的药物组合物及其在制备抗肿瘤药物中的应用
EP3262049B1 (fr) 2015-02-27 2022-07-20 Nimbus Lakshmi, Inc. Inhibiteurs de tyk2 et leurs utilisations
BR112017018198A2 (pt) 2015-02-27 2018-04-10 Curtana Pharmaceuticals Inc inibição da atividade de olig2
HK1248603A1 (zh) 2015-03-10 2018-10-19 Aduro Biotech, Inc. 用於活化"干扰素基因的刺激剂"依懒性信号传导的组合物和方法
HK1249758A1 (zh) 2015-03-11 2018-11-09 Melinta Therapeutics, Inc. 抗微生物化合物及其制备和使用方法
US9481665B2 (en) * 2015-03-13 2016-11-01 Yong Xu Process for preparing PI3K inhibitor buparsilib
EP3273959A1 (fr) * 2015-03-25 2018-01-31 Novartis Ag Combinaisons pharmaceutiques
RU2017134379A (ru) 2015-03-25 2019-04-03 Новартис Аг Формилированные n-гетероциклические производные в качестве ингибиторов fgfr4
EP3310813A1 (fr) 2015-06-17 2018-04-25 Novartis AG Conjugués anticorps-médicament
WO2017004134A1 (fr) 2015-06-29 2017-01-05 Nimbus Iris, Inc. Inhibiteurs d'irak et leurs utilisations
MX383744B (es) 2015-07-02 2025-03-14 Centrexion Therapeutics Corp Citrato de (4-((3r,4r)-3-metoxitetrahidro-piran-4-ilamino)piperidin-1-il) (5-metil-6-(((2r, 6s)-6-(p-tolil)tetrahidro-2h-piran-2-il) metilamino) pirimidin-4-il) metanona.
WO2017009751A1 (fr) * 2015-07-15 2017-01-19 Pfizer Inc. Dérivés de pyrimidine
EP3878465A1 (fr) 2015-07-29 2021-09-15 Novartis AG Polythérapies comprenant des molécules d'anticorps tim-3
US20180222982A1 (en) 2015-07-29 2018-08-09 Novartis Ag Combination therapies comprising antibody molecules to pd-1
DK3317301T3 (da) 2015-07-29 2021-06-28 Immutep Sas Kombinationsterapier omfattende antistofmolekyler mod lag-3
RU2020142739A (ru) 2015-08-28 2021-01-15 Новартис Аг Ингибиторы mdm2 и их комбинации
CN105001151B (zh) * 2015-08-28 2017-07-14 苏州明锐医药科技有限公司 布帕尼西中间体及其制备方法
EP4327809A3 (fr) 2015-09-02 2024-04-17 Takeda Pharmaceutical Company Limited Inhibiteurs de tyk2 et leurs utilisations
CA2997106C (fr) 2015-09-08 2024-06-04 Monash University Promedicaments ciblant la lymphe
US10683308B2 (en) 2015-09-11 2020-06-16 Navitor Pharmaceuticals, Inc. Rapamycin analogs and uses thereof
HUE061437T2 (hu) 2015-10-23 2023-06-28 Navitor Pharm Inc A Sestrin-GATOR2 kölcsönhatás modulátorai és ezek alkalmazásai
TN2018000112A1 (en) 2015-10-29 2019-10-04 Novartis Ag Antibody conjugates comprising toll-like receptor agonist
US20180280370A1 (en) 2015-11-02 2018-10-04 Novartis Ag Dosage regimen for a phosphatidylinositol 3-kinase inhibitor
EP3370768B9 (fr) 2015-11-03 2022-03-16 Janssen Biotech, Inc. Anticorps se liant spécifiquement à pd-1 et leurs utilisations
JP2018535997A (ja) 2015-12-03 2018-12-06 ノバルティス アーゲー ctDNAにPIK3CA変異を有するために事前選択された患者におけるPI3K阻害剤を用いた癌の処置
US11370792B2 (en) 2015-12-14 2022-06-28 Raze Therapeutics, Inc. Caffeine inhibitors of MTHFD2 and uses thereof
CN106883185B (zh) * 2015-12-15 2021-07-09 重庆博腾制药科技股份有限公司 一种4-氯-2-三氟甲基嘧啶的制备方法
WO2017106656A1 (fr) 2015-12-17 2017-06-22 Novartis Ag Molécules d'anticorps anti-pd-1 et leurs utilisations
EP4234552A3 (fr) 2016-03-09 2023-10-18 Raze Therapeutics, Inc. Inhibiteurs de la 3-phosphoglycérate déshydrogénase et leurs utilisations
LT3426243T (lt) 2016-03-09 2021-08-10 Raze Therapeutics, Inc. 3-fosfogliceratdehidrogenazės inhibitoriai ir jų panaudojimas
US11337969B2 (en) 2016-04-08 2022-05-24 X4 Pharmaceuticals, Inc. Methods for treating cancer
EP3231799A1 (fr) * 2016-04-14 2017-10-18 Universität Basel Dérivés de 4-(azétidin-1-yl)pyrimidine ayant une activité anti-mitotique et antiproliférative
US11098047B2 (en) 2016-05-06 2021-08-24 BioVersys AG Antimicrobials and methods of making and using same
MX2018014167A (es) 2016-05-18 2019-08-16 Piqur Therapeutics Ag Tratamiento de lesiones de la piel.
ES2863250T3 (es) * 2016-05-18 2021-10-11 Torqur Ag Tratamiento de trastornos neurológicos
US10544137B2 (en) 2016-06-02 2020-01-28 Shanghai Haiyan Pharmaceutical Technology Co., Ltd. PI3K inhibitor, and pharmaceutically acceptable salt, polycrystalline form, and application thereof
WO2017221092A1 (fr) 2016-06-20 2017-12-28 Novartis Ag Composés de triazolopyridine et leurs utilisations
WO2017221100A1 (fr) 2016-06-20 2017-12-28 Novartis Ag Composés d'imidazopyrimidine utiles pour le traitement du cancer
JP7042812B2 (ja) 2016-06-20 2022-03-28 ノバルティス アーゲー トリアゾロピリミジン化合物の結晶形態
ES2870920T3 (es) 2016-06-21 2021-10-28 X4 Pharmaceuticals Inc Inhibidores de CXCR4 y usos de los mismos
WO2017223243A1 (fr) 2016-06-21 2017-12-28 X4 Pharmaceuticals, Inc. Inhibiteurs de cxcr4 et leurs utilisations
CN109640988A (zh) 2016-06-21 2019-04-16 X4 制药有限公司 Cxcr4抑制剂及其用途
WO2018009466A1 (fr) 2016-07-05 2018-01-11 Aduro Biotech, Inc. Composés dinucléotidiques cycliques d'acide nucléique bloqué et leurs utilisations
CN106905294A (zh) * 2016-07-08 2017-06-30 苏州科睿思制药有限公司 5‑[2,6‑二(4‑吗啉基)‑4‑嘧啶基]‑4‑(三氟甲基)‑2‑吡啶胺的晶型及其制备方法
RU2758669C2 (ru) 2016-09-27 2021-11-01 Вертекс Фармасьютикалз Инкорпорейтед Способ лечения рака с применением сочетания днк-поражающих агентов и ингибиторов днк-пк
EP4089116A1 (fr) 2016-09-27 2022-11-16 Cero Therapeutics, Inc. Molécules de récepteurs d'engloutissement chimériques
EP3848370B1 (fr) 2016-10-14 2025-05-07 Takeda Pharmaceutical Company Limited Inhibiteurs de tyk2 et leurs utilisations
EP3528816A4 (fr) 2016-10-21 2020-04-08 Nimbus Lakshmi, Inc. Inhibiteurs de tyk2 et leurs utilisations
WO2018089499A1 (fr) 2016-11-08 2018-05-17 Navitor Pharmaceuticals, Inc. Inhibiteurs de la phényl amino pipéridine mtorc et leurs utilisations
WO2018092064A1 (fr) 2016-11-18 2018-05-24 Novartis Ag Combinaisons d'inhibiteurs de mdm2 et d'inhibiteurs de bcl-xl
EP4035659A1 (fr) 2016-11-29 2022-08-03 PureTech LYT, Inc. Exosomes destinés à l'administration d'agents thérapeutiques
US11091451B2 (en) 2016-12-05 2021-08-17 Raze Therapeutics, Inc. SHMT inhibitors and uses thereof
WO2018115203A1 (fr) 2016-12-23 2018-06-28 Bicyclerd Limited Dérivés peptidiques ayant de nouvelles structures de liaison
EP3565638B8 (fr) 2017-01-06 2024-04-10 BicycleRD Limited Conjugué bicyclique pour traiter le cancer
JOP20190187A1 (ar) 2017-02-03 2019-08-01 Novartis Ag مترافقات عقار جسم مضاد لـ ccr7
WO2018163051A1 (fr) 2017-03-06 2018-09-13 Novartis Ag Méthodes de traitement du cancer à expression d'ubb réduite
JP7160824B2 (ja) 2017-03-08 2022-10-25 ニンバス ラクシュミ, インコーポレイテッド Tyk2阻害剤、使用およびその製造のための方法
EP3375778A1 (fr) 2017-03-14 2018-09-19 Artax Biopharma Inc. Dérivés d'aryl-pipéridine
EP3375784A1 (fr) 2017-03-14 2018-09-19 Artax Biopharma Inc. Dérivés d'aza-dihydro-acridone
GB201705263D0 (en) * 2017-03-31 2017-05-17 Probiodrug Ag Novel inhibitors
WO2018185618A1 (fr) 2017-04-03 2018-10-11 Novartis Ag Conjugués de médicament-anticorps anti-cdh6 et combinaisons d'anticorps anti-gitr et méthodes de traitement
WO2018191146A1 (fr) 2017-04-10 2018-10-18 Navitor Pharmaceuticals, Inc. Inhibiteurs de rheb à base d'hétéroaryle et leurs utilisations
US10912750B2 (en) 2017-04-26 2021-02-09 Navitor Pharmaceuticals, Inc. Modulators of Sestrin-GATOR2 interaction and uses thereof
WO2018197893A1 (fr) 2017-04-27 2018-11-01 Bicycletx Limited Ligands peptidiques bicycliques et leurs utilisations
UY37695A (es) 2017-04-28 2018-11-30 Novartis Ag Compuesto dinucleótido cíclico bis 2’-5’-rr-(3’f-a)(3’f-a) y usos del mismo
US11304953B2 (en) 2017-05-23 2022-04-19 Mei Pharma, Inc. Combination therapy
WO2018215937A1 (fr) 2017-05-24 2018-11-29 Novartis Ag Protéines à greffe de cytokine-anticorps anti-interleukine-7 et procédés d'utilisation dans le traitement du cancer
EP3630162A1 (fr) 2017-05-24 2020-04-08 Novartis AG Protéines greffées anticorps-cytokine et méthodes d'utilisation
BR112019024556A2 (pt) 2017-05-24 2020-06-23 Novartis Ag Proteínas enxertadas com citocina de anticorpo e métodos para uso no tratamento de câncer
CN118307674A (zh) 2017-06-22 2024-07-09 诺华股份有限公司 针对cd73的抗体分子及其用途
WO2018237173A1 (fr) 2017-06-22 2018-12-27 Novartis Ag Molécules d'anticorps dirigées contre cd73 et utilisations correspondantes
JP7301757B2 (ja) 2017-06-26 2023-07-03 バイスクルアールディー・リミテッド 検出可能部分を持つ二環式ペプチドリガンドおよびその使用
KR102717819B1 (ko) 2017-07-28 2024-10-14 다케다 야쿠힌 고교 가부시키가이샤 Tyk2 억제제 및 이의 용도
CN111183147B (zh) 2017-08-04 2024-07-05 拜斯科技术开发有限公司 Cd137特异性的双环肽配体
KR20200041358A (ko) 2017-08-14 2020-04-21 메이 파마, 아이엔씨. 병용 요법
WO2019034866A1 (fr) 2017-08-14 2019-02-21 Bicyclerd Limited Conjugués ligands peptidiques bicycliques et leurs utilisations
WO2019034868A1 (fr) 2017-08-14 2019-02-21 Bicyclerd Limited Conjugués peptide bicyclique-ligand ppr-a et leurs utilisations
JP7290627B2 (ja) * 2017-08-17 2023-06-13 ボード オブ レジェンツ,ザ ユニバーシティ オブ テキサス システム Atrキナーゼの複素環式阻害剤
US11883497B2 (en) 2017-08-29 2024-01-30 Puretech Lyt, Inc. Lymphatic system-directing lipid prodrugs
EP3675838A4 (fr) 2017-08-29 2021-04-21 PureTech LYT, Inc. Promédicaments lipidiques orientant vers le système lymphatique
AU2018329925B2 (en) 2017-09-08 2025-05-29 F. Hoffmann-La Roche Ag Diagnostic and therapeutic methods for cancer
MX2020003190A (es) 2017-09-22 2020-11-11 Kymera Therapeutics Inc Degradadores de proteinas y usos de los mismos.
WO2019060693A1 (fr) 2017-09-22 2019-03-28 Kymera Therapeutics, Inc. Ligands crbn et utilisations de ces derniers
EP3688032B1 (fr) 2017-09-26 2025-11-05 Cero Therapeutics Holdings, Inc. Molécules de récepteur d'engloutissement chimérique et méthodes d'utilisation
CN109651341A (zh) * 2017-10-11 2019-04-19 上海医药工业研究院 二吗啉氰基嘧(吡)啶类衍生物及作为抗肿瘤药物应用
US11351156B2 (en) 2017-10-13 2022-06-07 Inserm Combination treatment of pancreatic cancer
SG11202004589SA (en) 2017-11-23 2020-06-29 Piqur Therapeutics Ag Treatment of skin disorders
EP3713963A1 (fr) 2017-11-23 2020-09-30 INSERM (Institut National de la Santé et de la Recherche Médicale) Nouveau marqueur permettant de prédire la sensibilité à des inhibiteurs de pi3k
TWI825046B (zh) 2017-12-19 2023-12-11 英商拜西可泰克斯有限公司 Epha2特用之雙環胜肽配位基
US11608345B1 (en) 2017-12-19 2023-03-21 Puretech Lyt, Inc. Lipid prodrugs of rapamycin and its analogs and uses thereof
US11304954B2 (en) 2017-12-19 2022-04-19 Puretech Lyt, Inc. Lipid prodrugs of mycophenolic acid and uses thereof
GB201721265D0 (en) 2017-12-19 2018-01-31 Bicyclerd Ltd Bicyclic peptide ligands specific for EphA2
EP3727362A4 (fr) 2017-12-19 2021-10-06 PureTech LYT, Inc. Promédicaments lipidiques d'acide mycophénolique et leurs utilisations
BR112020012651A2 (pt) 2017-12-22 2020-12-01 Ravenna Pharmaceuticals, Inc. compostos derivados de aril-bipiridina amina como inibidores da fosfatidilinositol fosfato quinase, composição farmacêutica compreendendo os mesmos e usos terapêuticos dos ditos compostos
EP3728228A1 (fr) 2017-12-22 2020-10-28 Ravenna Pharmaceuticals, Inc. Dérivés d'aminopyridine utilisés en tant qu'inhibiteurs de la phosphatidylinositol phosphate kinase
IL315310A (en) 2017-12-26 2024-10-01 Kymera Therapeutics Inc Irak degraders and uses thereof
WO2019140380A1 (fr) 2018-01-12 2019-07-18 Kymera Therapeutics, Inc. Agents de dégradation de protéines et utilisations associées
WO2019140387A1 (fr) 2018-01-12 2019-07-18 Kymera Therapeutics, Inc. Ligands crbn et leurs utilisations
US12398209B2 (en) 2018-01-22 2025-08-26 Janssen Biotech, Inc. Methods of treating cancers with antagonistic anti-PD-1 antibodies
KR20200116481A (ko) 2018-01-29 2020-10-12 메르크 파텐트 게엠베하 Gcn2 억제제 및 이의 용도
EP3746071A4 (fr) 2018-01-29 2021-09-01 Merck Patent GmbH Inhibiteurs de gcn2 et leurs utilisations
JP2021514953A (ja) 2018-02-23 2021-06-17 バイスクルテクス・リミテッド 多量体二環式ペプチドリガンド
KR20260028873A (ko) 2018-02-27 2026-03-04 아텍스 바이오파마 인코포레이티드 Tcr-nck 상호 작용의 억제제로서의 크로멘 유도체
JP7444781B2 (ja) 2018-03-28 2024-03-06 セロ・セラピューティクス・インコーポレイテッド 細胞免疫療法組成物およびその使用
WO2019191334A1 (fr) 2018-03-28 2019-10-03 Cero Therapeutics, Inc. Récepteurs tim4 chimériques et leurs utilisations
RU2020135106A (ru) 2018-03-28 2022-04-29 Серо Терапьютикс, Инк. Векторы экспрессии для химерных рецепторов поглощения, генетически модифицированные клетки-хозяева и их применения
CN112533602A (zh) 2018-04-05 2021-03-19 大日本住友制药肿瘤公司 Axl激酶抑制剂及其用途
BR112020019732A2 (pt) * 2018-04-06 2021-02-17 Nippon Soda Co., Ltd. composto, formulações para controlar organismos nocivos e para controlar ou exterminar endoparasitas, e, formulações inseticida ou acaricida e nematicida.
ES3032793T3 (en) 2018-04-10 2025-07-24 Neuropore Therapies Inc Tri-substituted aryl and heteroaryl derivatives as modulators of pi3-kinase and autophagy pathways
CN112533917B (zh) 2018-04-10 2024-06-21 神经孔疗法股份有限公司 作为vps34的抑制剂的吗啉衍生物
ES2969982T3 (es) 2018-04-24 2024-05-23 Vertex Pharma Compuestos de pteridinona y usos de los mismos
ES2919572T3 (es) 2018-04-24 2022-07-27 Merck Patent Gmbh Compuestos antiproliferación y usos de los mismos
AR126019A1 (es) 2018-05-30 2023-09-06 Novartis Ag Anticuerpos frente a entpd2, terapias de combinación y métodos de uso de los anticuerpos y las terapias de combinación
US20210214459A1 (en) 2018-05-31 2021-07-15 Novartis Ag Antibody molecules to cd73 and uses thereof
IL314362A (en) 2018-06-15 2024-09-01 Janssen Pharmaceutica Nv Rapamycin analogs and their uses
CN108864067B (zh) * 2018-06-20 2020-05-12 郑州大学 一种2-炔丙巯基-5-氰基嘧啶类衍生物及其制备方法和应用
IL279489B2 (en) 2018-06-22 2025-10-01 Bicycletx Ltd Bicyclic peptide ligands specific for nectin-4, a drug conjugate containing the peptide ligands and a pharmaceutical composition containing the drug conjugate
GB201810316D0 (en) 2018-06-22 2018-08-08 Bicyclerd Ltd Peptide ligands for binding to EphA2
WO2020010227A1 (fr) 2018-07-06 2020-01-09 Kymera Therapeutics, Inc. Agents de dégradation de protéines et leurs utilisations
US11292792B2 (en) 2018-07-06 2022-04-05 Kymera Therapeutics, Inc. Tricyclic CRBN ligands and uses thereof
MX2021000977A (es) 2018-07-26 2021-04-12 Sumitomo Pharma Oncology Inc Metodos para tratar enfermedades asociadas con expresion anormal de receptor de activina a tipo 1 (acvr1) e inhibidores de acvr1 para uso en los mismos.
CN118666832A (zh) 2018-08-17 2024-09-20 诺华股份有限公司 作为smarca2/brm atp酶抑制剂的脲化合物和组合物
US10548889B1 (en) 2018-08-31 2020-02-04 X4 Pharmaceuticals, Inc. Compositions of CXCR4 inhibitors and methods of preparation and use
US12030875B2 (en) 2018-09-07 2024-07-09 PIC Therapeutics, Inc. EIF4E inhibitors and uses thereof
JP7619951B2 (ja) 2018-10-15 2025-01-22 武田薬品工業株式会社 Tyk2阻害剤およびその使用
WO2020084305A1 (fr) 2018-10-23 2020-04-30 Bicycletx Limited Ligands peptidiques bicycliques et leurs utilisations
CN113164414A (zh) 2018-10-24 2021-07-23 纳维托制药有限公司 多晶型化合物和其用途
EP3873532A1 (fr) 2018-10-31 2021-09-08 Novartis AG Conjugué médicament-anticorps anti-dc-sign
JP7623943B2 (ja) 2018-11-30 2025-01-29 カイメラ セラピューティクス, インコーポレイテッド Irak分解剤およびそれらの使用
JP7530360B2 (ja) 2018-11-30 2024-08-07 武田薬品工業株式会社 Tyk2阻害剤およびその使用
GB201820288D0 (en) 2018-12-13 2019-01-30 Bicycle Tx Ltd Bicycle peptide ligaands specific for MT1-MMP
GB201820325D0 (en) 2018-12-13 2019-01-30 Bicyclerd Ltd Bicyclic peptide ligands specific for psma
GB201820295D0 (en) 2018-12-13 2019-01-30 Bicyclerd Ltd Bicyclic peptide ligands specific for MT1-MMP
WO2020124397A1 (fr) 2018-12-19 2020-06-25 Inventisbio Shanghai Ltd. Inhibiteurs de kinase src c-terminale
EP3670659A1 (fr) 2018-12-20 2020-06-24 Abivax Biomarqueurs et leurs utilisations dans le traitement d'infections virales, d'inflammations ou du cancer
JP7607564B2 (ja) 2018-12-21 2024-12-27 ノバルティス アーゲー Pmel17に対する抗体及びその結合体
US12551567B2 (en) 2018-12-21 2026-02-17 Bicyclerd Limited Bicyclic peptide ligands specific for PD-L1
JP2022514618A (ja) 2018-12-21 2022-02-14 バイスクルテクス・リミテッド Pd-l1に特異的な二環式ペプチドリガンド
JPWO2020130125A1 (ja) 2018-12-21 2021-11-04 第一三共株式会社 抗体−薬物コンジュゲートとキナーゼ阻害剤の組み合わせ
CN109705033B (zh) * 2019-01-22 2021-03-30 杭州壹瑞医药科技有限公司 N-杂芳基磺酰胺类衍生物及制备和应用
CN109651297B (zh) * 2019-01-22 2022-05-27 杭州壹瑞医药科技有限公司 一种n-苄基-n-芳基磺酰胺类衍生物及制备和应用
CN120865208A (zh) 2019-01-23 2025-10-31 武田药品工业株式会社 Tyk2抑制剂和其用途
NZ778055A (en) 2019-02-12 2025-11-28 Sumitomo Pharma America Inc Formulations comprising heterocyclic protein kinase inhibitors
WO2020165600A1 (fr) 2019-02-14 2020-08-20 Bicycletx Limited Conjugués peptide-ligand bicyclique et leurs utilisations
CA3133460A1 (fr) 2019-03-22 2020-10-01 Sumitomo Dainippon Pharma Oncology, Inc. Compositions comprenant des modulateurs de pkm2 et methodes de traitement les utilisant
US20220184222A1 (en) 2019-04-02 2022-06-16 Bicycletx Limited Bicycle toxin conjugates and uses thereof
TWI875749B (zh) 2019-04-05 2025-03-11 美商凱麥拉醫療公司 Stat降解劑及其用途
WO2020243423A1 (fr) 2019-05-31 2020-12-03 Ikena Oncology, Inc. Inhibiteurs de tead et leurs utilisations
WO2020251972A1 (fr) 2019-06-10 2020-12-17 Kymera Therapeutics, Inc. Agents de dégradation de smarca et leurs utilisations
TW202112767A (zh) 2019-06-17 2021-04-01 美商佩特拉製藥公司 作為磷脂酸肌醇磷酸激酶抑制劑之胺基吡啶衍生物
BR112021026517A2 (pt) 2019-06-28 2022-05-10 Kymera Therapeutics Inc Degradadores de irak e usos dos mesmos
WO2021001431A1 (fr) 2019-07-02 2021-01-07 INSERM (Institut National de la Santé et de la Recherche Médicale) Utilisation d'inhibiteurs sélectifs de pi3ka pour traiter une maladie métastatique chez des patients souffrant de cancer du pancréas
WO2021001427A1 (fr) 2019-07-02 2021-01-07 INSERM (Institut National de la Santé et de la Recherche Médicale) Procédés de traitement prophylactique du cancer chez des patients souffrant de pancréatite
WO2021001426A1 (fr) 2019-07-02 2021-01-07 INSERM (Institut National de la Santé et de la Recherche Médicale) Utilisation d'une imagerie d'élasticité ultrarapide pour la détection de cancers du pancréas
JP2022539208A (ja) 2019-07-03 2022-09-07 スミトモ ファーマ オンコロジー, インコーポレイテッド チロシンキナーゼ非受容体1(tnk1)阻害剤およびその使用
WO2021011868A1 (fr) 2019-07-17 2021-01-21 Kymera Therapeutics, Inc. Agents de dégradation d'irak et leurs utilisations
TWI860386B (zh) 2019-07-30 2024-11-01 英商拜西可泰克斯有限公司 異質雙環肽複合物
JP7842684B2 (ja) 2019-09-11 2026-04-08 ビンシア・バイオサイエンシーズ・インコーポレイテッド Usp30阻害剤及びその使用
CN114945366B (zh) 2019-09-13 2025-01-07 林伯士萨顿公司 Hpk1拮抗剂和其用途
US20220348651A1 (en) 2019-09-18 2022-11-03 Novartis Ag Entpd2 antibodies, combination therapies, and methods of using the antibodies and combination therapies
DK4034535T3 (da) 2019-09-26 2026-04-07 Novartis Ag Aza-quinolinforbindelser og anvendelser deraf
WO2021067875A1 (fr) 2019-10-03 2021-04-08 Cero Therapeutics, Inc. Récepteurs tim4 chimériques et leurs utilisations
CA3156436A1 (fr) 2019-11-01 2021-05-06 Steven LEVENTER Methodes de traitement a l'aide d'un modulateur de mtorc1
KR20220128345A (ko) 2019-12-05 2022-09-20 아나쿠리아 테라퓨틱스, 인코포레이티드 라파마이신 유사체 및 이의 용도
US12551564B2 (en) 2019-12-10 2026-02-17 Kymera Therapeutics, Inc. IRAK degraders and uses thereof
WO2021127283A2 (fr) 2019-12-17 2021-06-24 Kymera Therapeutics, Inc. Agents de dégradation d'irak et leurs utilisations
WO2021127190A1 (fr) 2019-12-17 2021-06-24 Kymera Therapeutics, Inc. Agents de dégradation d'irak et leurs utilisations
WO2021133917A1 (fr) 2019-12-23 2021-07-01 Kymera Therapeutics, Inc. Inhibiteurs de smarca et leurs utilisations
BR112022012410A2 (pt) 2019-12-23 2022-08-30 Kymera Therapeutics Inc Degradadores smarca e usos dos mesmos
CN115348864A (zh) 2020-02-05 2022-11-15 纯技术Lyt股份有限公司 神经甾体的脂质前药
CN115151534B (zh) * 2020-02-14 2024-02-06 南京药石科技股份有限公司 白细胞介素-1受体相关激酶(irak)/fms样受体酪氨酸激酶(flt3)的抑制剂、其药物产品及其方法
AU2021230289A1 (en) 2020-03-03 2022-09-29 PIC Therapeutics, Inc. eIF4E inhibitors and uses thereof
US12528785B2 (en) 2020-03-19 2026-01-20 Kymera Therapeutics, Inc. MDM2 degraders and uses thereof
CN115397818A (zh) * 2020-03-27 2022-11-25 东亚St株式会社 氨基嘧啶衍生物及其作为芳烃受体调节剂的应用
US20230181756A1 (en) 2020-04-30 2023-06-15 Novartis Ag Ccr7 antibody drug conjugates for treating cancer
WO2021247897A1 (fr) 2020-06-03 2021-12-09 Kymera Therapeutics, Inc. Agents de dégradation d'irak deutérés et leurs utilisations
TW202210483A (zh) 2020-06-03 2022-03-16 美商凱麥拉醫療公司 Irak降解劑之結晶型
KR20210158019A (ko) 2020-06-23 2021-12-30 주식회사 온코빅스 포스파티딜이노시톨 3-키나제(pi3k) 억제제로써 pten 과오종 증후군에 의한 종양 세포의 성장 또는 증식을 억제하는데 유용한 신규한 피리미딘 유도체 및 이의 약제학적으로 허용가능한 염, 및 이를 유효성분으로 함유하는 약제학적 조성물
IL300248A (en) 2020-08-03 2023-03-01 Bicycletx Ltd peptide-based linkers
AR123185A1 (es) 2020-08-10 2022-11-09 Novartis Ag Compuestos y composiciones para inhibir ezh2
WO2022036287A1 (fr) 2020-08-14 2022-02-17 Cero Therapeutics, Inc. Récepteurs chimériques anti-cd72 et utilisations de ceux-ci
WO2022036285A1 (fr) 2020-08-14 2022-02-17 Cero Therapeutics, Inc. Compositions et méthodes de traitement du cancer à l'aide de récepteurs tim chimériques en association avec des inhibiteurs de la poly(adp-ribose)polymérase
WO2022036265A1 (fr) 2020-08-14 2022-02-17 Cero Therapeutics, Inc. Récepteurs chimériques tim et leurs utilisations
WO2022038158A1 (fr) 2020-08-17 2022-02-24 Bicycletx Limited Conjugués "bicycle" spécifiques de la nectine-4 et leurs utilisations
WO2022043556A1 (fr) 2020-08-31 2022-03-03 Novartis Ag Composition pharmaceutique stable
US20230321285A1 (en) 2020-08-31 2023-10-12 Advanced Accelerator Applications International Sa Method of treating psma-expressing cancers
US20230338587A1 (en) 2020-08-31 2023-10-26 Advanced Accelerator Applications International Sa Method of treating psma-expressing cancers
US12331046B2 (en) 2020-10-23 2025-06-17 Nimbus Clotho, Inc. CTPS1 inhibitors and uses thereof
TWI877433B (zh) 2020-11-30 2025-03-21 大陸商杭州阿諾生物醫藥科技有限公司 用於治療pik3ca突變癌症的組合療法
WO2022120353A1 (fr) 2020-12-02 2022-06-09 Ikena Oncology, Inc. Inhibiteurs de tead et leurs utilisations
EP4255895A1 (fr) 2020-12-02 2023-10-11 Ikena Oncology, Inc. Inhibiteurs de tead et utilisations associées
EP4259144A4 (fr) 2020-12-09 2025-08-20 Kymera Therapeutics Inc Agents de dégradation de smarca et leurs utilisations
TW202237119A (zh) 2020-12-10 2022-10-01 美商住友製藥腫瘤公司 Alk﹘5抑制劑和彼之用途
PH12023500015A1 (en) 2020-12-30 2024-03-11 Kymera Therapeutics Inc Irak degraders and uses thereof
JP2024506858A (ja) 2021-02-02 2024-02-15 リミナル・バイオサイエンシーズ・リミテッド Gpr84アンタゴニストおよびその使用
EP4288427A1 (fr) 2021-02-02 2023-12-13 Liminal Biosciences Limited Antagonistes de gpr84 et leurs utilisations
CN117120090A (zh) 2021-02-12 2023-11-24 林伯士萨顿公司 Hpk1拮抗剂和其用途
CN116867494A (zh) 2021-02-15 2023-10-10 凯麦拉医疗公司 Irak4降解剂和其用途
WO2022174268A1 (fr) 2021-02-15 2022-08-18 Kymera Therapeutics, Inc. Agents de dégradation d'irak4 et leurs utilisations
AU2022227021A1 (en) 2021-02-26 2023-09-21 Kelonia Therapeutics, Inc. Lymphocyte targeted lentiviral vectors
EP4301756A4 (fr) 2021-03-05 2025-02-26 Nimbus Saturn, Inc. Antagonistes de hpk1 et leurs utilisations
WO2022194248A1 (fr) * 2021-03-18 2022-09-22 苏州国匡医药科技有限公司 Agent de dégradation à petites molécules ctla-4 et son utilisation
WO2022213062A1 (fr) 2021-03-29 2022-10-06 Nimbus Saturn, Inc. Antagonistes de hpk1 et leurs utilisations
AU2022256074A1 (en) 2021-04-09 2023-11-02 Nimbus Clio, Inc. Cbl-b modulators and uses thereof
EP4323356A1 (fr) 2021-04-13 2024-02-21 Nuvalent, Inc. Hétérocycles amino-substitués pour le traitement de cancers avec des mutations egfr
CA3235132A1 (fr) 2021-04-16 2022-10-20 Novartis Ag Conjugues anticorps-medicament et leurs procedes de fabrication
JP2024514879A (ja) 2021-04-16 2024-04-03 イケナ オンコロジー, インコーポレイテッド Mek阻害剤及びその使用
AU2022271290A1 (en) 2021-05-07 2023-11-23 Kymera Therapeutics, Inc. Cdk2 degraders and uses thereof
JP2024529474A (ja) 2021-07-28 2024-08-06 セロ・セラピューティクス・インコーポレイテッド キメラTim4受容体およびその使用
US12157732B2 (en) 2021-08-25 2024-12-03 PIC Therapeutics, Inc. eIF4E inhibitors and uses thereof
JP2024534127A (ja) 2021-08-25 2024-09-18 ピク セラピューティクス, インコーポレイテッド eIF4E阻害剤及びその使用
US12187744B2 (en) 2021-10-29 2025-01-07 Kymera Therapeutics, Inc. IRAK4 degraders and synthesis thereof
EP4444309A4 (fr) * 2021-12-08 2026-03-04 Kineta Inc Pyrimidines et leurs procédés d'utilisation
WO2023114984A1 (fr) 2021-12-17 2023-06-22 Ikena Oncology, Inc. Inhibiteurs de tead et leurs utilisations
EP4472967A4 (fr) 2022-01-31 2026-04-15 Kymera Therapeutics Inc Agents de dégradation d'irak et leurs utilisations
CN114213340B (zh) 2022-02-22 2022-06-07 北京蓝晶微生物科技有限公司 2,4-二氨基嘧啶氧化物的制备方法
CN114591326B (zh) * 2022-02-28 2024-02-27 上海筛杰生物医药有限公司 Cct-251921的中间体及其制备方法
WO2023173053A1 (fr) 2022-03-10 2023-09-14 Ikena Oncology, Inc. Inhibiteurs de mek et leurs utilisations
WO2023173057A1 (fr) 2022-03-10 2023-09-14 Ikena Oncology, Inc. Inhibiteurs de mek et leurs utilisations
WO2023211889A1 (fr) 2022-04-25 2023-11-02 Ikena Oncology, Inc. Composés polymorphes et leurs utilisations
IL316768A (en) 2022-05-25 2025-01-01 Ikena Oncology Inc MEK inhibitors and their uses
CN117186072B (zh) * 2022-06-01 2026-03-27 安驰达生物医药技术(广州)有限公司 一种抑制磷脂酰肌醇-3-激酶γ亚型活性的化合物及其制备方法与应用
JP2025527247A (ja) 2022-08-02 2025-08-20 リミナル・バイオサイエンシーズ・リミテッド アリール-トリアゾリル及び関連するgpr84アンタゴニストならびにそれらの使用
IL318575A (en) 2022-08-02 2025-03-01 Liminal Biosciences Ltd HETEROARYL CARBOXAMIDE AND GPR84-RELATED ANTAGONISTS AND USES THEREOF
CN120051456A (zh) 2022-08-02 2025-05-27 里米诺生物科学有限公司 取代的吡啶酮gpr84拮抗剂及其用途
US20240208961A1 (en) 2022-11-22 2024-06-27 PIC Therapeutics, Inc. Eif4e inhibitors and uses thereof
IL321486A (en) 2023-06-23 2025-08-01 Kymera Therapeutics Inc Iraqi joints and their uses
WO2025027560A1 (fr) * 2023-08-01 2025-02-06 Fondazione Istituto Italiano Di Tecnologia Nouveaux inhibiteurs de rhoj/cdc42 développés pour le traitement du cancer, de tumeurs bénignes, de troubles rétiniens, de troubles vasculaires et de cardiomyopathies
WO2025062372A1 (fr) 2023-09-21 2025-03-27 Takeda Pharmaceutical Company Limited Inhibiteurs de tyk2 destinés à être utilisés dans le traitement d'une maladie inflammatoire de l'intestin
PY2501648A (es) 2024-01-12 2025-10-31 Syngenta Crop Protection Ag Nuevos compuestos de carboxamida
WO2026008750A1 (fr) 2024-07-05 2026-01-08 Syngenta Crop Protection Ag Nouveaux composés carboxamides

Family Cites Families (121)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB581334A (en) 1943-09-29 1946-10-09 Francis Henry Swinden Curd New pyrimidine compounds
AT340933B (de) 1973-08-20 1978-01-10 Thomae Gmbh Dr K Verfahren zur herstellung neuer pyrimidinderivate und ihrer saureadditionssalze
DE2341925A1 (de) 1973-08-20 1975-03-06 Thomae Gmbh Dr K Neue pyrimidinderivate und verfahren zu ihrer herstellung
JPS6041077B2 (ja) 1976-09-06 1985-09-13 喜徳 喜谷 1,2‐ジアミノシクロヘキサン異性体のシス白金(2)錯体
US4323581A (en) 1978-07-31 1982-04-06 Johnson & Johnson Method of treating carcinogenesis
US4329726A (en) * 1978-12-01 1982-05-11 Raychem Corporation Circuit protection devices comprising PTC elements
IL73534A (en) 1983-11-18 1990-12-23 Riker Laboratories Inc 1h-imidazo(4,5-c)quinoline-4-amines,their preparation and pharmaceutical compositions containing certain such compounds
DE3752123T2 (de) 1987-03-09 1998-05-14 Kyowa Hakko Kogyo Kk Derivate des physiologisch aktiven mittels k-252
US4994386A (en) 1987-07-13 1991-02-19 Pharmacia Diagnostics, Inc. Production of HBLV virus in the HSB-2 cell line
US4904768A (en) 1987-08-04 1990-02-27 Bristol-Myers Company Epipodophyllotoxin glucoside 4'-phosphate derivatives
WO1989007105A1 (fr) 1988-02-04 1989-08-10 Kyowa Hakko Kogyo Co., Ltd. Derives de staurosporine
US4929726A (en) 1988-02-09 1990-05-29 Georgia State University Foundation, Inc. Novel diazines and their method of preparation
US5238944A (en) 1988-12-15 1993-08-24 Riker Laboratories, Inc. Topical formulations and transdermal delivery systems containing 1-isobutyl-1H-imidazo[4,5-c]quinolin-4-amine
US4929624A (en) 1989-03-23 1990-05-29 Minnesota Mining And Manufacturing Company Olefinic 1H-imidazo(4,5-c)quinolin-4-amines
GB9012311D0 (en) 1990-06-01 1990-07-18 Wellcome Found Pharmacologically active cns compounds
US5389640A (en) 1991-03-01 1995-02-14 Minnesota Mining And Manufacturing Company 1-substituted, 2-substituted 1H-imidazo[4,5-c]quinolin-4-amines
US6410010B1 (en) 1992-10-13 2002-06-25 Board Of Regents, The University Of Texas System Recombinant P53 adenovirus compositions
US5451700A (en) 1991-06-11 1995-09-19 Ciba-Geigy Corporation Amidino compounds, their manufacture and methods of treatment
US5268376A (en) 1991-09-04 1993-12-07 Minnesota Mining And Manufacturing Company 1-substituted 1H-imidazo[4,5-c]quinolin-4-amines
WO1993007153A1 (fr) 1991-10-10 1993-04-15 Schering Corporation Derives de staurosporine 4'-(n-substituee-n-oxydee)
US5266575A (en) 1991-11-06 1993-11-30 Minnesota Mining And Manufacturing Company 2-ethyl 1H-imidazo[4,5-ciquinolin-4-amines
WO1993008809A1 (fr) 1991-11-08 1993-05-13 The University Of Southern California Compositions contenant des composes k-252 et destinees a potentialiser l'activite de la neurotrophine
AU661533B2 (en) 1992-01-20 1995-07-27 Astrazeneca Ab Quinazoline derivatives
US5948898A (en) 1992-03-16 1999-09-07 Isis Pharmaceuticals, Inc. Methoxyethoxy oligonucleotides for modulation of protein kinase C expression
US5621100A (en) 1992-07-24 1997-04-15 Cephalon, Inc. K-252a derivatives for treatment of neurological disorders
US5756494A (en) 1992-07-24 1998-05-26 Cephalon, Inc. Protein kinase inhibitors for treatment of neurological disorders
ES2225824T3 (es) 1992-08-31 2005-03-16 Ludwig Institute For Cancer Research Nonapeptido aislado derivado del gen mage-3 y presentado por hla-a1, y sus usos.
DE69331228T4 (de) 1992-09-21 2002-09-05 Kyowa Hakko Kogyo Co., Ltd. Heilmittel für thrombozytopenia
BR9207175A (pt) 1992-10-28 1995-12-12 Genentech Inc Composição contendo antagonista de fator de crescimento de célula endotelial vascular sequência aminoácida de anticorpo monoclonal polipeptídeo e método de tratamento de tumor em mamífero
US5395937A (en) 1993-01-29 1995-03-07 Minnesota Mining And Manufacturing Company Process for preparing quinoline amines
EP0708772B1 (fr) 1993-07-15 2000-08-23 Minnesota Mining And Manufacturing Company IMIDAZO [4,5-c]PYRIDIN-4-AMINES
US5352784A (en) 1993-07-15 1994-10-04 Minnesota Mining And Manufacturing Company Fused cycloalkylimidazopyridines
US5478932A (en) 1993-12-02 1995-12-26 The Board Of Trustees Of The University Of Illinois Ecteinascidins
ES2236702T3 (es) 1993-12-23 2005-07-16 Eli Lilly And Company Inhibidores de la proteina quinasa c.
US5587459A (en) 1994-08-19 1996-12-24 Regents Of The University Of Minnesota Immunoconjugates comprising tyrosine kinase inhibitors
US6083903A (en) 1994-10-28 2000-07-04 Leukosite, Inc. Boronic ester and acid compounds, synthesis and uses
US5482936A (en) 1995-01-12 1996-01-09 Minnesota Mining And Manufacturing Company Imidazo[4,5-C]quinoline amines
MX9707453A (es) 1995-03-30 1997-12-31 Pfizer Derivados de quinazolina.
AU692090B2 (en) 1995-04-13 1998-05-28 Taiho Pharmaceutical Co., Ltd. Novel 4,6-diarylpyrimidine derivatives and salts thereof
GB9508538D0 (en) 1995-04-27 1995-06-14 Zeneca Ltd Quinazoline derivatives
US6331555B1 (en) 1995-06-01 2001-12-18 University Of California Treatment of platelet derived growth factor related disorders such as cancers
US5747498A (en) 1996-05-28 1998-05-05 Pfizer Inc. Alkynyl and azido-substituted 4-anilinoquinazolines
US5880141A (en) 1995-06-07 1999-03-09 Sugen, Inc. Benzylidene-Z-indoline compounds for the treatment of disease
AU6888196A (en) 1995-08-11 1997-03-12 Yale University Glycosylated indolocarbazole synthesis
FR2741881B1 (fr) 1995-12-01 1999-07-30 Centre Nat Rech Scient Nouveaux derives de purine possedant notamment des prorietes anti-proliferatives et leurs applications biologiques
DE69620445T2 (de) 1995-12-08 2002-12-12 Janssen Pharmaceutica N.V., Beerse (imidazol-5-yl)methyl-2-chinolinoderivate als farnesyl protein transferase inhibitoren
KR100447918B1 (ko) 1996-07-25 2005-09-28 동아제약주식회사 대장을포함한위장관보호작용을갖는플라본및플라바논화합물
CA2262776C (fr) 1996-08-02 2005-03-08 Genesense Technologies, Inc. Sequences antisens et antitumorales dirigees conte les constituants r1 et r2 de la ribonucleotide reductase
JP3734907B2 (ja) 1996-12-19 2006-01-11 富士写真フイルム株式会社 現像処理方法
CO4950519A1 (es) 1997-02-13 2000-09-01 Novartis Ag Ftalazinas, preparaciones farmaceuticas que las comprenden y proceso para su preparacion
US6126965A (en) 1997-03-21 2000-10-03 Georgetown University School Of Medicine Liposomes containing oligonucleotides
AU744986B2 (en) 1997-07-12 2002-03-07 Cancer Research Technology Limited Cyclin dependent kinase inhibiting purine derivatives
KR100563514B1 (ko) 1997-07-24 2006-03-27 젠야쿠코교가부시키가이샤 헤테로고리 화합물 및 이를 유효성분으로 하는 항종양제
US6166037A (en) 1997-08-28 2000-12-26 Merck & Co., Inc. Pyrrolidine and piperidine modulators of chemokine receptor activity
US6150362A (en) 1997-12-12 2000-11-21 Henkin; Jack Triazine angiogenesis inhibitors
RS49779B (sr) 1998-01-12 2008-06-05 Glaxo Group Limited, Biciklična heteroaromatična jedinjenja kao inhibitori protein tirozin kinaze
SI0930302T1 (en) 1998-01-16 2003-10-31 F. Hoffmann-La Roche Ag Benzosulfone derivatives
EA005032B1 (ru) 1998-05-29 2004-10-28 Сьюджен, Инк. Пирролзамещенные 2-индолиноны (варианты), фармацевтическая композиция (варианты), способ модулирования каталитической активности протеинкиназы, способ лечения или профилактики нарушения в организме, связанного с протеинкиназой
KR100581199B1 (ko) 1998-06-19 2006-05-17 카이론 코포레이션 글리코겐 신타제 키나제 3의 억제제
US7045519B2 (en) 1998-06-19 2006-05-16 Chiron Corporation Inhibitors of glycogen synthase kinase 3
US20030083242A1 (en) 1998-11-06 2003-05-01 Alphonse Galdes Methods and compositions for treating or preventing peripheral neuropathies
AU768201B2 (en) 1999-01-22 2003-12-04 Amgen, Inc. Kinase inhibitors
US6495558B1 (en) 1999-01-22 2002-12-17 Amgen Inc. Kinase inhibitors
GB9913083D0 (en) 1999-06-04 1999-08-04 Novartis Ag Organic compounds
HK1039330B (en) 1999-05-04 2005-12-09 Schering Corporation Piperidine derivatives useful as ccr5 antagonists
CA2371583C (fr) 1999-05-04 2005-09-13 Schering Corporation Derives de piperazine faisant office d'antagonistes ccr5
CA2376596C (fr) 1999-06-25 2009-10-06 Genentech, Inc. Anticorps anti-erbb2 humanises et traitement a l'aide de ces anticorps
JP2003503351A (ja) 1999-06-30 2003-01-28 メルク エンド カムパニー インコーポレーテッド Srcキナーゼ阻害化合物
WO2001000214A1 (fr) 1999-06-30 2001-01-04 Merck & Co., Inc. Composes inhibiteurs de la kinase src
AU5636900A (en) 1999-06-30 2001-01-31 Merck & Co., Inc. Src kinase inhibitor compounds
EP1201668A4 (fr) 1999-07-13 2003-05-21 Kyowa Hakko Kogyo Kk Derives de staurosporine
ATE250053T1 (de) 1999-07-15 2003-10-15 Pharmacopeia Inc Bradikinin b1 rezeptor antagonisten
CZ301689B6 (cs) 1999-11-05 2010-05-26 Astrazeneca Ab Derivát chinazolinu a farmaceutický prostredek, který ho obsahuje
SI1255752T1 (sl) 2000-02-15 2007-12-31 Pharmacia & Upjohn Co Llc S pirolom substituirani zaviralci 2-indolinon protein kinaza
EP1274705A1 (fr) 2000-03-29 2003-01-15 Cyclacel Limited 4-heteroaryle-pyrimidines substituees en 2 et leur utilisation dans le traitement de troubles proliferants
PT1274718E (pt) 2000-04-12 2007-01-31 Genaera Corp Processo para a preparação de esteróis 7. alfa-hidroxi 3- aminosubstítuidos utilizando intermediários com um grupo 7. alfa-hidroxilo desprotegido
CN1186324C (zh) 2000-04-27 2005-01-26 山之内制药株式会社 稠合杂芳基衍生物
NZ522217A (en) 2000-04-28 2004-04-30 Tanabe Seiyaku Co Cyclic compounds
AU2001268711A1 (en) 2000-06-23 2002-01-08 Bristol-Myers Squibb Pharma Company Heteroaryl-phenyl substituted factor xa inhibitors
PL204958B1 (pl) 2000-06-30 2010-02-26 Glaxo Group Ltd Ditosylany związków chinazolinowych, środek farmaceutyczny i zastosowanie tych związków
AU2001295026B2 (en) 2000-09-06 2008-04-03 Novartis Vaccines And Diagnostics, Inc. Inhibitors of glycogen synthase kinase 3
CZ304344B6 (cs) 2000-09-11 2014-03-19 Novartis Vaccines & Diagnostics, Inc. Chinolinonový derivát a jeho použití a farmaceutický prostředek s obsahem tohoto derivátu
EP1317450B1 (fr) 2000-09-15 2006-11-22 Vertex Pharmaceuticals Incorporated Composes de pyrazole utiles comme inhibiteurs de proteine kinase
US6677450B2 (en) 2000-10-06 2004-01-13 Bristol-Myers Squibb Company Topoisomerase inhibitors
SE0004053D0 (sv) 2000-11-06 2000-11-06 Astrazeneca Ab N-type calcium channel antagonists for the treatment of pain
NZ526472A (en) 2000-12-21 2004-04-30 Vertex Pharma Pyrazole compounds useful as protein kinase inhibitors
WO2002057423A2 (fr) 2001-01-16 2002-07-25 Regeneron Pharmaceuticals, Inc. Isolement de cellules exprimant des protéines sécrétées
WO2002062826A1 (fr) 2001-02-07 2002-08-15 Vadim Viktorovich Novikov Procede de fabrication des peptides
WO2002062766A2 (fr) 2001-02-07 2002-08-15 Millennium Pharmaceuticals, Inc. Composes de liaison au recepteur de la melanocortine-4 et procedes d'utilisation de tels composes
EP1395561A1 (fr) 2001-05-25 2004-03-10 Boehringer Ingelheim Pharmaceuticals Inc. Composes de carbamate et d'oxamide inhibant la production de cytokine
JP2005500294A (ja) 2001-06-19 2005-01-06 ブリストル−マイヤーズ スクイブ カンパニー ホスホジエステラーゼ7に対するピリミジン阻害剤
US20040186172A1 (en) 2001-07-02 2004-09-23 Houssam Ibrahim Oxaliplatin active substance with a very low content of oxalic acid
US6603000B2 (en) 2001-07-11 2003-08-05 Boehringer Ingelheim Pharmaceuticals, Inc. Synthesis for heteroarylamine compounds
KR100484504B1 (ko) 2001-09-18 2005-04-20 학교법인 포항공과대학교 쿠커비투릴 유도체를 주인 분자로서 포함하고 있는 내포화합물 및 이를 포함한 약제학적 조성물
WO2003030909A1 (fr) 2001-09-25 2003-04-17 Bayer Pharmaceuticals Corporation 2- et 4-aminopyrimidines n-substituees par un noyau bicyclique utilisees comme inhibiteurs de kinases dans le traitement du cancer
US20030134846A1 (en) 2001-10-09 2003-07-17 Schering Corporation Treatment of trypanosoma brucei with farnesyl protein transferase inhibitors
WO2003077902A1 (fr) 2002-02-19 2003-09-25 Xenoport, Inc. Procede de synthese de promedicaments a partir de derives de 1-acyl-alkyl et compositions correspondantes
DE60327999D1 (de) 2002-03-15 2009-07-30 Vertex Pharma Azolylaminoazine als inhibitoren von proteinkinasen
AU2003218215A1 (en) 2002-03-15 2003-09-29 Vertex Pharmaceuticals, Inc. Azolylaminoazines as inhibitors of protein kinases
EP1485100B1 (fr) 2002-03-15 2010-05-05 Vertex Pharmaceuticals Incorporated Azinylaminoazoles utilises comme inhibiteurs de proteine kinases
WO2003078423A1 (fr) 2002-03-15 2003-09-25 Vertex Pharmaceuticals, Inc. Compositions s'utilisant comme inhibiteurs de proteine kinases
NZ535985A (en) 2002-03-29 2007-04-27 Chiron Corp Substituted benzazoles and use thereof as RAF kinase inhibitors
US6900342B2 (en) 2002-05-10 2005-05-31 Dabur India Limited Anticancer taxanes such as paclitaxel, docetaxel and their structural analogs, and a method for the preparation thereof
US6727272B1 (en) 2002-07-15 2004-04-27 Unitech Pharmaceuticals, Inc. Leflunomide analogs for treating rheumatoid arthritis
US7148342B2 (en) 2002-07-24 2006-12-12 The Trustees Of The University Of Pennyslvania Compositions and methods for sirna inhibition of angiogenesis
EP1562605A4 (fr) 2002-10-08 2006-07-12 Massachusetts Inst Technology Composes pour la modulation du transport du cholesterol
US7423148B2 (en) * 2002-11-21 2008-09-09 Chiron Corporation Small molecule PI 3-kinase inhibitors and methods of their use
CA2511646A1 (fr) 2002-12-27 2004-07-22 Chiron Corporation Thiosemicarbazones antiviraux et immunostimulants
ES2391770T3 (es) 2003-01-21 2012-11-29 Novartis Vaccines And Diagnostics, Inc. Uso de compuestos de triptantrina para la potenciación inmune
WO2004084824A2 (fr) 2003-03-24 2004-10-07 Merck & Co., Inc. Heterocycles a 6 elements a substitution biaryle en tant que bloqueurs des canaux sodiques
US7893096B2 (en) 2003-03-28 2011-02-22 Novartis Vaccines And Diagnostics, Inc. Use of small molecule compounds for immunopotentiation
US20050014753A1 (en) 2003-04-04 2005-01-20 Irm Llc Novel compounds and compositions as protein kinase inhibitors
JP2007523875A (ja) 2003-07-15 2007-08-23 ニューロジェン・コーポレーション バニロイド受容体リガンドとしての置換ピリミジン−4−イルアミン類縁体
CA2531619A1 (fr) 2003-07-16 2005-01-27 Neurogen Corporation Analogues de biaryl piperazinyl-pyridine
AR045944A1 (es) * 2003-09-24 2005-11-16 Novartis Ag Derivados de isoquinolina 1.4-disustituidas
GB0415365D0 (en) * 2004-07-09 2004-08-11 Astrazeneca Ab Pyrimidine derivatives
GB0415364D0 (en) 2004-07-09 2004-08-11 Astrazeneca Ab Pyrimidine derivatives
JP2009523161A (ja) 2006-01-11 2009-06-18 アストラゼネカ アクチボラグ モルホリノピリミジン誘導体と療法におけるその使用
JO2660B1 (en) 2006-01-20 2012-06-17 نوفارتيس ايه جي Pi-3 inhibitors and methods of use
WO2008098058A1 (fr) 2007-02-06 2008-08-14 Novartis Ag Inhibiteurs de la pi3-kinase et procédés de leur utilisation
WO2012109423A1 (fr) 2011-02-11 2012-08-16 Dana-Farber Cancer Institute, Inc. Procédé d'inhibition de cellules tumorales d'hamartome

Also Published As

Publication number Publication date
AR112118A2 (es) 2019-09-25
CA2636993C (fr) 2014-02-25
EP1984350A1 (fr) 2008-10-29
EA018083B1 (ru) 2013-05-30
PE20071322A1 (es) 2008-01-27
SI1984350T1 (sl) 2010-12-31
US20100249126A1 (en) 2010-09-30
EA200801680A1 (ru) 2008-12-30
TW200808786A (en) 2008-02-16
IL192763A (en) 2013-04-30
KR20080096776A (ko) 2008-11-03
HK1122031A1 (en) 2009-05-08
GT200800143A (es) 2009-06-11
JO2660B1 (en) 2012-06-17
CN101389622A (zh) 2009-03-18
US20120225859A1 (en) 2012-09-06
AU2007206048A1 (en) 2007-07-26
HRP20130796T1 (en) 2013-09-30
MEP3908A (xx) 2010-02-10
ECSP088630A (es) 2008-08-29
PL1984350T3 (pl) 2011-02-28
HRP20100603T1 (hr) 2010-12-31
PL2261223T3 (pl) 2013-12-31
JP2009527464A (ja) 2009-07-30
NO20083389L (no) 2008-09-19
TNSN08305A1 (en) 2009-12-29
TW201315723A (zh) 2013-04-16
NZ569771A (en) 2011-07-29
SMAP200800048A (it) 2008-08-13
EP2261223A1 (fr) 2010-12-15
DE602007008529D1 (de) 2010-09-30
PT2261223E (pt) 2013-09-16
IL192763A0 (en) 2009-02-11
SV2008002984A (es) 2010-08-17
BRPI0707189A8 (pt) 2018-01-02
US8217035B2 (en) 2012-07-10
PT1984350E (pt) 2010-11-11
RS51548B (sr) 2011-06-30
BRPI0707189A2 (pt) 2011-04-26
CR10163A (es) 2008-09-17
ATE478064T1 (de) 2010-09-15
ZA200806017B (en) 2009-12-30
EP2261223B1 (fr) 2013-06-12
JP5161110B2 (ja) 2013-03-13
WO2007084786A1 (fr) 2007-07-26
KR101353829B1 (ko) 2014-01-21
GEP20115147B (en) 2011-01-25
EP1984350B1 (fr) 2010-08-18
ME00012B (fr) 2010-02-10
AR059087A1 (es) 2008-03-12
CA2636993A1 (fr) 2007-07-26
ES2427624T3 (es) 2013-10-31
SI2261223T1 (sl) 2013-10-30
NO342183B1 (no) 2018-04-09
SMP200800048B (it) 2009-07-14
AU2007206048B2 (en) 2011-04-21
CN101389622B (zh) 2013-04-17
RS52928B (sr) 2014-02-28
HN2008001144A (es) 2011-04-08
US8563549B2 (en) 2013-10-22
DK1984350T3 (da) 2010-11-15
BRPI0707189B1 (pt) 2021-12-21
DK2261223T3 (da) 2013-09-23
CY1111091T1 (el) 2015-06-11
MY144233A (en) 2011-08-15
UA96284C2 (ru) 2011-10-25
ES2351172T3 (es) 2011-02-01
TWI385170B (zh) 2013-02-11

Similar Documents

Publication Publication Date Title
MA30208B1 (fr) Derives de pyrimidine utilises en tant qu'inhibiteurs de kinase pi -3
NO20070917L (no) Imidazotriaziner som protein-kinaseinhibitorer
NO20075113L (no) Proteinkinaseinhibitorer
CL2007003821A1 (es) Compuestos derivados de isoquinolina o isoquinolinona sustituidos con cicloalquilamina; composicion farmaceutica; y su uso para tratar y/o prevenir enfermedades asociadas con la rho-quinasa y/o la fosforilacion mediada por la rho-quinasa de la cadena ligera de miosina, tales como hipertension, retinopatia, glaucoma, alzheimer, sida entre otras.
MX2007013216A (es) Derivados de amida substituida como inhibidores de la proteina de cinasa.
EA200900152A1 (ru) Ингибиторы пирролотриазинкиназы
MX2009004716A (es) Compuestos y composiciones en la forma de inhibidores de quinasa de proteina.
MA30952B1 (fr) Cyclopenta [d] pyrimidines utiles en tant qu'inhibiteurs de la proteine kinase akt
MX2010010525A (es) Inhibidores de metaloproteasa de matriz basados en aril-sulfonamida.
MA32070B1 (fr) Dérivés hétérocycliques réunis par fusion et procédés d'utilisation associés
TN2014000420A1 (fr) Derives d'indole et d'indazole qui activent la mpk
MA31903B1 (fr) Derives de thiazole utilises comme inhibiteur de la pi 3 kinase
UA99141C2 (ru) Замещенные производные индазола, активные в качестве ингибиторов киназы
MA33119B1 (fr) Derives de benzofuranyle utilises comme inhibiteurs de la glucokinase
NO20062136L (no) Imidazopyrazintyrosin-kinaseinhibitorer
NO20082508L (no) Aminopyrimidiner anvendelige som kinaseinhibitorer
EP2178869A4 (fr) Composés d'indole en tant qu'inhibiteurs de nécrose cellulaire
MX2008010397A (es) Inhibidores de pi-3 quinasa y metodos para su uso.
CY1110969T1 (el) 5-υποκατεστημενα-2-φαινυλαμινο-βενζαμιδια ως αναστολεiς μεκ
ATE456565T1 (de) Pyridin- und pyrazinderivate als mnk- kinaseinhibitoren
UA103321C2 (ru) Производные тиенопиридона как активаторы amp-активированной протеинкиназы (амрк)
NO20090723L (no) Kondenserte heterosykliske derivater og fremgangsmater for anvendelse
UY31027A1 (es) Derivados de tetrahidroindol y tetrahidroindazol
DE602007001463D1 (de) Pyrimidin-, chinazolin-, pteridin- und triazinderivate
CR7882A (es) Compuestos 2-(1H-Indazol-6-ilamino-benzamidas como inhibidores proteinquinasas utiles para el tratamiento de enfermedades oftalmicas