ES2183905T3 - Inhibidores de metaloproteasa de matriz. - Google Patents

Inhibidores de metaloproteasa de matriz.

Info

Publication number
ES2183905T3
ES2183905T3 ES96119780T ES96119780T ES2183905T3 ES 2183905 T3 ES2183905 T3 ES 2183905T3 ES 96119780 T ES96119780 T ES 96119780T ES 96119780 T ES96119780 T ES 96119780T ES 2183905 T3 ES2183905 T3 ES 2183905T3
Authority
ES
Spain
Prior art keywords
sup
heteroarilo
hydrogen
cycalalkyl
arilo
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Lifetime
Application number
ES96119780T
Other languages
English (en)
Inventor
Steven Lee Bender
Chris Allen Broka
Jeffrey Allen Campbell
Arlindo Lucas Castelhano
Lawrence Emerson Fisher
Robert Than Hendricks
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
F Hoffmann La Roche AG
Agouron Pharmaceuticals LLC
Original Assignee
F Hoffmann La Roche AG
Agouron Pharmaceuticals LLC
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=27358753&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=ES2183905(T3) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by F Hoffmann La Roche AG, Agouron Pharmaceuticals LLC filed Critical F Hoffmann La Roche AG
Application granted granted Critical
Publication of ES2183905T3 publication Critical patent/ES2183905T3/es
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/62Oxygen or sulfur atoms
    • C07D213/63One oxygen atom
    • C07D213/64One oxygen atom attached in position 2 or 6
    • C07D213/6432-Phenoxypyridines; Derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/02Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • 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
    • A61P37/00Drugs for immunological or allergic disorders
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D211/54Sulfur atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D309/00Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
    • C07D309/02Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C07D309/08Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • 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
    • C07D401/06Heterocyclic 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 linked by a carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D407/00Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/02Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings
    • C07D407/12Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms 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)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Pain & Pain Management (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pulmonology (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Pyridine Compounds (AREA)
  • Heterocyclic Compounds Containing Sulfur Atoms (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Furan Compounds (AREA)
  • Pyrane Compounds (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)

Abstract

COMPUESTOS DE FORMULA: DONDE: N ES 0,1 O 2; Y ES HIDROXI O XONH-, DONDE X ES HIDROGENO O ALQUILO INFERIOR; R{SUP,1}ES HIDROGENO O ALQUILO INFERIOR; R{SUP,2}ES HIDROGENO, ALQUILO INFERIOR, HETEROALQUILO, ARILO, ARALQUILO, ARILHETEROALQUILO, CICLOALQUILO, CICLOALQUILALQUILO, HETEROARILO, HETEROARALQUILO, HETEROARILHETEROALQUILO, HETEROCICLO, HETEROCICLO-ALQUILO INFERIOR, HETEROCICLOHETEROALQUILO INFERIOR, O -NR{SUP,6}R{SUP,7}, DONDE: R{SUP,6} ES HIDROGENO, ALQUILO INFERIOR, CICLOALQUILO O CICLOALQUILALQUILO, ARILO, HETEROARILO Y HETEROARALQUILO; R{SUP,7} ES HIDROGENO, ALQUILO INFERIOR, CICLOALQUIL O CICLOALQUILALQUILO, ARILO, ARALQUILO, HETEROARILO, HETEROARALQUILO, -C(O)R{SUP,8}, -C(O)NR{SUP,8}R{SUP,9}, SO{SUB,2}NR{SUP,8}R{SUP,9}, -SO{SUB,2}R{SUP,10}, ARILOXICARBONILO, O ALCOXICARBONILO; O R{SUP,6} Y R{SUP,7} JUNTO CON EL ATOMO DE NITROGENO AL CUAL ESTAN UNIDOS, REPRESENTAN UN GRUPO HETEROCICLICO; DONDE R{SUP,8} Y R{SUP,9} SON INDEPENDIENTEMENTE HIDROGENO, ALQUILO INFERIOR, CICLOALQUILO, CICLOALQUILALQUILO, ARILO, ARALQUILO, HETEROARILO, O HETEROALQUILO; Y R{SUP,10} ES ALQUILO INFERIOR, CICLOALQUILO, CICLOALQUILALQUILO, ARILO, ARALQUILO, HETEROARILO, HETEROARALQUILO, HETEROARILO, O HETEROCICLO; O R{SUP,1} Y R{SUP,2} JUNTO CON EL ATOMO DE CARBONO AL QUE ESTAN UNIDOS, REPRESENTAN UN GRUPO CICLOALQUILO O HETEROCICLICO; R{SUP,3} ES HIDROGENO, ALQUILO INFERIOR, CICLOALQUILO, CICLOALQUILALQUILO, ARILO, ARALQUILO, HETEROARILO, , HETEROARALQUILO, HETEROALQUILO O ALCOXI INFERIOR; R{SUP,4} ES HIDROGENO, ALQUILO INFERIOR, CICLOALQUILO O CICLOALQUILALQUILO; O R{SUP,2} Y R{SUP,3} JUNTO CON LOS CARBONOS A LOS QUE ESTAN UNIDOS, REPRESENTAN UN GRUPO CICLOALQUILO O HETEROCICLICO; O R{SUP,3} Y R{SUP,4} JUNTO CON EL CARBONO AL QUE ESTAN UNIDOS, REPRESENTAN UN GRUPO CICLOALQUILO O HETEROCICLICO; Y R{SUP,5} ES ALQUILO INFERIOR, CICLOALQUILO, CICLOALQUILALQUILO, ARILO, ARALQUILO, HETEROARILO, O HETEROARALQUILO. SE DESCRIBEN ASIMISMO LAS SALES O ESTERES FARMACEUTICAMENTE ACEPTABLES DE LOS CITADOS COMPUESTOS, QUE PRESENTAN PROPIEDADES FARMACOLOGICAS UTILES, ESPECIALMENTE PARA UTILIZACION COMO INHIBIDORES DE METALOPROTEASAS DE LA MATRIZ, EN PARTICULAR DE LAS COLAGENASAS INTERSTICIALES.
ES96119780T 1995-12-20 1996-12-10 Inhibidores de metaloproteasa de matriz. Expired - Lifetime ES2183905T3 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US893995P 1995-12-20 1995-12-20
US2243996P 1996-08-07 1996-08-07
US3209696P 1996-12-04 1996-12-04

Publications (1)

Publication Number Publication Date
ES2183905T3 true ES2183905T3 (es) 2003-04-01

Family

ID=27358753

Family Applications (1)

Application Number Title Priority Date Filing Date
ES96119780T Expired - Lifetime ES2183905T3 (es) 1995-12-20 1996-12-10 Inhibidores de metaloproteasa de matriz.

Country Status (29)

Country Link
US (1) US5932595A (es)
EP (1) EP0780386B1 (es)
JP (1) JP2921673B2 (es)
KR (1) KR100240536B1 (es)
CN (1) CN1177821C (es)
AT (1) ATE225343T1 (es)
AU (1) AU700725B2 (es)
BR (1) BR9606134A (es)
CO (1) CO4790091A1 (es)
CY (1) CY2414B1 (es)
CZ (1) CZ291478B6 (es)
DE (1) DE69624081T2 (es)
DK (1) DK0780386T3 (es)
ES (1) ES2183905T3 (es)
HR (1) HRP960612B1 (es)
HU (1) HU225696B1 (es)
IL (1) IL119843A (es)
MX (1) MX9606709A (es)
MY (1) MY117574A (es)
NO (1) NO314845B1 (es)
NZ (1) NZ299941A (es)
PE (1) PE30298A1 (es)
PL (1) PL198032B1 (es)
PT (1) PT780386E (es)
RS (1) RS49781B (es)
RU (1) RU2175316C2 (es)
SG (1) SG76490A1 (es)
TR (1) TR199601032A2 (es)
UY (1) UY24409A1 (es)

Families Citing this family (385)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2238306A1 (en) * 1995-12-08 1997-06-12 Agouron Pharmaceuticals, Inc. Metalloproteinase inhibitors, pharmaceutical compositions containing them and their pharmaceutical uses, and methods and intermediates useful for their preparation
US6500948B1 (en) 1995-12-08 2002-12-31 Agouron Pharmaceuticals, Inc. Metalloproteinase inhibitors-compositions, uses preparation and intermediates thereof
JP4358908B2 (ja) * 1996-01-02 2009-11-04 アヴェンティス ファーマシューティカルズ インコーポレイテッド 置換(アリール、ヘテロアリール、アリールメチル又はヘテロアリールメチル)ヒドロキサム酸化合物
KR20000022532A (ko) * 1996-06-27 2000-04-25 오노 야꾸힝 고교 가부시키가이샤 아릴(설파이드, 설폭시드 및 설폰)유도체 및 이를 활성 성분으로 함유하는 약물
EP0818442A3 (en) * 1996-07-12 1998-12-30 Pfizer Inc. Cyclic sulphone derivatives as inhibitors of metalloproteinases and of the production of tumour necrosis factor
DE69729007T2 (de) * 1996-08-07 2005-04-07 Darwin Discovery Ltd., Slough Hydroxamsäure- und carbonsäure-derivate mit mmp und tnf hemmender wirkung
US6566384B1 (en) 1996-08-07 2003-05-20 Darwin Discovery Ltd. Hydroxamic and carboxylic acid derivatives having MMP and TNF inhibitory activity
EP0923561B1 (en) * 1996-08-28 2002-10-23 The Procter & Gamble Company Heterocyclic metalloprotease inhibitors
WO1998013340A1 (en) 1996-09-27 1998-04-02 Pharmacia & Upjohn Company β-SULFONYL HYDROXAMIC ACIDS AS MATRIX METALLOPROTEINASES INHIBITORS
CZ298022B6 (cs) 1996-10-15 2007-05-30 G. D. Searle & Co. Použití inhibitoru cyklooxygenázy-2 pro výrobu léciva pro lécení a prevenci neoplazie
US6228869B1 (en) 1996-10-16 2001-05-08 American Cyanamid Company Ortho-sulfonamido bicyclic hydroxamic acids as matrix metalloproteinase and TACE inhibitors
US6548524B2 (en) 1996-10-16 2003-04-15 American Cyanamid Company Preparation and use of ortho-sulfonamido bicyclic heteroaryl hydroxamic acids as matrix metalloproteinase and TACE inhibitors
US5977408A (en) * 1996-10-16 1999-11-02 American Cyanamid Company Preparation and use of β-sulfonamido hydroxamic acids as matrix metalloproteinase and TACE inhibitors
US5929097A (en) * 1996-10-16 1999-07-27 American Cyanamid Company Preparation and use of ortho-sulfonamido aryl hydroxamic acids as matrix metalloproteinase and tace inhibitors
US5962481A (en) * 1996-10-16 1999-10-05 American Cyanamid Company Preparation and use of ortho-sulfonamido heteroaryl hydroxamic acids as matrix metalloproteinase and tace inhibitors
WO1998030566A1 (en) * 1997-01-06 1998-07-16 Pfizer Inc. Cyclic sulfone derivatives
EP0960096B1 (en) * 1997-01-22 2005-04-06 Aventis Pharmaceuticals Inc. Substituted beta-thiocarboxylic acids
ID22849A (id) * 1997-01-23 1999-12-09 Hoffmann La Roche Penghambat-penghambat sulmafida-metaloprotease
ZA98376B (en) * 1997-01-23 1998-07-23 Hoffmann La Roche Sulfamide-metalloprotease inhibitors
JP2000507975A (ja) * 1997-02-07 2000-06-27 ファイザー・インク N−ヒドロキシ−β−スルホニルプロピオンアミド誘導体類及びそれらのマトリックスメタロプロテイナーゼ阻害薬としての使用
US6696449B2 (en) 1997-03-04 2004-02-24 Pharmacia Corporation Sulfonyl aryl hydroxamates and their use as matrix metalloprotease inhibitors
US6362183B1 (en) 1997-03-04 2002-03-26 G. D. Searle & Company Aromatic sulfonyl alpha-hydroxy hydroxamic acid compounds
WO1998039315A1 (en) * 1997-03-04 1998-09-11 Monsanto Company Aromatic sulfonyl alpha-cycloamino hydroxamic acid compounds
US6476027B1 (en) * 1997-03-04 2002-11-05 Monsanto Company N-hydroxy 4-sulfonyl butanamide compounds
US6794511B2 (en) 1997-03-04 2004-09-21 G. D. Searle Sulfonyl aryl or heteroaryl hydroxamic acid compounds
US7115632B1 (en) 1999-05-12 2006-10-03 G. D. Searle & Co. Sulfonyl aryl or heteroaryl hydroxamic acid compounds
US6380258B2 (en) * 1997-03-04 2002-04-30 G. D. Searle, L.L.C. Sulfonyl divalent aryl or heteroaryl hydroxamic acid compounds
US5985900A (en) * 1997-04-01 1999-11-16 Agouron Pharmaceuticals, Inc. Metalloproteinase inhibitors, pharmaceutical compositions containing them and their pharmaceutical uses
US6300514B1 (en) 1997-06-25 2001-10-09 Ono Pharmaceutical Co., Ltd. Aryl (sulfide, sulfoxide and sulfone) derivatives and drugs containing the same as the active ingredient
AU7937298A (en) 1997-07-08 1999-02-08 Ono Pharmaceutical Co. Ltd. Amino acid derivatives
US6235786B1 (en) 1997-08-06 2001-05-22 Abbott Laboratories Reverse hydroxamate inhibitors of matrix metalloproteinases
US6294573B1 (en) 1997-08-06 2001-09-25 Abbott Laboratories Reverse hydroxamate inhibitors of matrix metalloproteinases
US6130220A (en) * 1997-10-16 2000-10-10 Syntex (Usa) Inc. Sulfamide-metalloprotease inhibitors
JPH11199512A (ja) * 1997-10-24 1999-07-27 Pfizer Prod Inc 変形性関節症および他のmmp媒介疾患の治療のためのmmp−13選択的阻害剤の使用
DE69811111T2 (de) * 1997-11-12 2003-07-24 Darwin Discovery Ltd., Cambridge Hydroxamsäure- und carbonsäurederivate mit mmp und tnf hemmender wirkung
US20010039287A1 (en) 1997-11-14 2001-11-08 Thomas E Barta Aromatic sulfone hydroxamic acid metalloprotease inhibitor
EP1042290A1 (en) * 1997-11-14 2000-10-11 G.D. SEARLE & CO. Aromatic sulfone hydroxamic acid metalloprotease inhibitor
US6750228B1 (en) 1997-11-14 2004-06-15 Pharmacia Corporation Aromatic sulfone hydroxamic acid metalloprotease inhibitor
IL135586A0 (en) 1997-11-21 2001-05-20 Upjohn Co α-HYDROXY, -AMINO, AND HALO DERIVATIVES OF β-SULFONYL HYDROXAMIC ACIDS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME
GB9725782D0 (en) * 1997-12-05 1998-02-04 Pfizer Ltd Therapeutic agents
GB9801690D0 (en) * 1998-01-27 1998-03-25 Pfizer Ltd Therapeutic agents
PL200418B1 (pl) * 1998-01-30 2009-01-30 Darwin Discovery Ltd Pochodna N-hydroksyformamidu, zawierający ją środek farmaceutyczny i jej zastosowanie
US6680338B2 (en) * 1998-02-06 2004-01-20 Darwin Discovery Ltd. Hydroxamic and carboxylic acid derivatives
CN1290260A (zh) * 1998-02-06 2001-04-04 达尔文发现有限公司 异羟肟酸和羧酸衍生物
PA8469401A1 (es) * 1998-04-10 2000-05-24 Pfizer Prod Inc Derivados biciclicos del acido hidroxamico
EP1077974A1 (en) 1998-05-14 2001-02-28 Du Pont Pharmaceuticals Company Substituted aryl hydroxamic acids as metalloproteinase inhibitors
EP0967201A1 (en) * 1998-05-20 1999-12-29 Roche Diagnostics GmbH Pharmaceutical agents containing sulfonamids as matrix metalloproteinase inhibitors
AU4692399A (en) 1998-06-17 2000-01-05 Du Pont Pharmaceuticals Company Cyclic hydroxamic acids as metalloproteinase inhibitors
EP1357109B1 (en) 1998-06-18 2008-07-23 F. Hoffmann-La Roche Ag Process for aryl alkyl sulfide
TWI245035B (en) 1998-06-26 2005-12-11 Ono Pharmaceutical Co Amino acid derivatives and a pharmaceutical composition comprising the derivatives
KR100633349B1 (ko) 1998-07-14 2006-10-16 오노 야꾸힝 고교 가부시키가이샤 아미노산 유도체 및 이들을 유효 성분으로서 함유하는 약제
NZ511423A (en) 1998-11-12 2003-01-31 Darwin Discovery Ltd Hydroxamic and carboxylic acid derivatives having MMP and TNF inhibitory activity
US20040122011A1 (en) * 1998-12-23 2004-06-24 Pharmacia Corporation Method of using a COX-2 inhibitor and a TACE inhibitors as a combination therapy
US6753337B2 (en) 1999-01-27 2004-06-22 Wyeth Holdings Corporation Alkynyl containing hydroxamic acid compounds as matrix metalloproteinase/tace inhibitors
CO5150194A1 (es) * 1999-01-27 2002-04-29 Abbott Lab Inhibidores hidroxamato inversos de las metalopreteinasas matriciales
BR0007784A (pt) * 1999-01-27 2002-02-05 American Cyanamid Co Composto, método para inibir mudanças patológicas mediadas pela enzima que converte o tnf-alfa (tace) em um mamìfero, composição farmacêutica, e, processo para preparar um composto
US6800646B1 (en) 1999-02-08 2004-10-05 Pharmacia Corporation Sulfamato hydroxamic acid metalloprotease inhibitor
AP2001002240A0 (en) 1999-02-08 2001-09-30 Searle & Co Sufamato hydroxamic acid metalloprotease inhibitor.
US6583299B1 (en) * 1999-05-20 2003-06-24 G.D. Searle & Co. α-amino-β-sulfonyl hydroxamic acid compounds
US6511993B1 (en) 1999-06-03 2003-01-28 Kevin Neil Dack Metalloprotease inhibitors
GB9912961D0 (en) * 1999-06-03 1999-08-04 Pfizer Ltd Metalloprotease inhibitors
US6869951B1 (en) 1999-07-16 2005-03-22 Pharmacia Corporation Method of changing conformation of a matrix metalloproteinase
US7632645B1 (en) 1999-08-16 2009-12-15 Max-Planck-Gesellschaft Zur Forderung Der Wissenschaften E.V. EGF receptor transactivation by G-protein-coupled receptors requires metalloproteinase cleavage of proHB-EGF
AU779298B2 (en) * 1999-08-16 2005-01-13 Max-Planck-Gesellschaft Zur Forderung Der Wissenschaften E.V. Use of proteinase inhibitor in order to inhibit the cleavage of growth factor precursor
UA74803C2 (uk) 1999-11-11 2006-02-15 Осі Фармасьютікалз, Інк. Стійкий поліморф гідрохлориду n-(3-етинілфеніл)-6,7-біс(2-метоксіетокси)-4-хіназолінаміну, спосіб його одержання (варіанти) та фармацевтичне застосування
JP2003528072A (ja) 2000-03-17 2003-09-24 ブリストル−マイヤーズ スクイブ ファーマ カンパニー マトリックスメタロプロテアーゼおよびTNF−αの阻害剤としての環状β−アミノ酸誘導体
JP2003528097A (ja) 2000-03-17 2003-09-24 ブリストル−マイヤーズ スクイブ ファーマ カンパニー マトリックスメタロプロテアーゼおよびTNF−α阻害剤としてのβ−アミノ酸誘導体
EP1138680A1 (en) * 2000-03-29 2001-10-04 Pfizer Products Inc. Gem substituted sulfonyl hydroxamic acids as MMP inhibitors
US6683093B2 (en) 2000-05-12 2004-01-27 Pharmacia Corporation Aromatic sulfone hydroxamic acids and their use as protease inhibitors
EP1292576A1 (en) 2000-05-15 2003-03-19 Darwin Discovery Limited Hydroxamic and carboxylic acid derivatives having mmp and tnf inhibitory activity
AU5652001A (en) * 2000-05-15 2001-11-26 Darwin Discovery Limited Hydroxamic and carboxylic acid derivatives having mmp and tnf inhibitory activity
US6927216B2 (en) 2000-10-03 2005-08-09 Bristol-Myers Squibb Pharma Company Cyclic sulfonyl compounds as inhibitors of metalloproteases
BRPI0116728B1 (pt) 2001-01-05 2018-10-30 Pfizer Inc. anticorpos para receptor de fator de crescimento i semelhante à insulina
US6642255B2 (en) 2001-01-11 2003-11-04 Bristol-Myers Squibb Pharma Company 1,2,-Disubstituted cyclic inhibitors of matrix metalloproteases and TNF-alpha
US6825215B2 (en) 2001-01-11 2004-11-30 Bristol-Myers Squibb Pharma Company 1,1-disubstituted cyclic inhibitors of matrix metalloproteases and TNF-α
AU2002258507A1 (en) 2001-03-15 2002-10-03 Bristol-Myers Squibb Company Spiro-cyclic beta-amino acid derivatives as inhibitors of matrix metalloproteinases and tnf-alpha converting enzyme (tage)
CN1764655A (zh) 2001-05-11 2006-04-26 法马西亚公司 芳族砜异羟肟酸酯及其作为蛋白酶抑制剂的用途
AU2002345792A1 (en) 2001-06-21 2003-01-08 Pfizer Inc. Thienopyridine and thienopyrimidine anticancer agents
US6683078B2 (en) 2001-07-19 2004-01-27 Pharmacia Corporation Use of sulfonyl aryl or heteroaryl hydroxamic acids and derivatives thereof as aggrecanase inhibitors
AR039067A1 (es) 2001-11-09 2005-02-09 Pfizer Prod Inc Anticuerpos para cd40
PE20030701A1 (es) 2001-12-20 2003-08-21 Schering Corp Compuestos para el tratamiento de trastornos inflamatorios
US7504537B2 (en) * 2001-12-27 2009-03-17 Dainippon Sumitomo Pharma Co., Ltd. Hydroxamic acid derivative and MMP inhibitor containing the same as active ingredient
US7006585B2 (en) * 2001-12-31 2006-02-28 Texas Instruments Incorporated Recovering data encoded in serial communication channels
SG2013013339A (en) 2002-03-13 2014-12-30 Array Biopharma Inc N3 alkylated benzimidazole derivatives as mek inhibitors
US20050209278A1 (en) * 2002-04-25 2005-09-22 Mcdonald Joseph J Piperidinyl- and piperazinyl-sulfonylmethyl hydroxamic acids and their use as protease inhibitors
MXPA04010555A (es) 2002-04-25 2005-02-17 Pharmacia Corp Acidos piperidinil- y piperazinil-sulfonilmetil hidroxamicos y su uso como inhibidores de proteasa.
UA77303C2 (en) 2002-06-14 2006-11-15 Pfizer Derivatives of thienopyridines substituted by benzocondensed heteroarylamide useful as therapeutic agents, pharmaceutical compositions and methods for their use
MXPA05000171A (es) * 2002-06-25 2005-04-08 Pharmacia Corp Acido arilsulfonilhidroxamico y derivados de amida y su uso como inhibidores de la proteasa.
WO2004056806A1 (en) 2002-12-19 2004-07-08 Pfizer Inc. 2-(1h-indazol-6-ylamino)-benzamide compounds as protein kinases inhibitors useful for the treatment of ophtalmic diseases
EP2181704B1 (en) 2002-12-30 2015-05-06 Angiotech International Ag Drug delivery from rapid gelling polymer composition
CA2517256C (en) 2003-02-26 2013-04-30 Sugen, Inc. Aminoheteroaryl compounds as protein kinase inhibitors
ES2433440T3 (es) 2003-04-04 2013-12-11 Yeda Research And Development Co. Ltd. Anticuerpos contra MMP2 o MMP9 y composiciones farmacéuticas que contienen los mismos útiles para inhibir la actividad de dichas metaloproteínas
US7008953B2 (en) 2003-07-30 2006-03-07 Agouron Pharmaceuticals, Inc. 3, 5 Disubstituted indazole compounds, pharmaceutical compositions, and methods for mediating or inhibiting cell proliferation
HN2004000285A (es) 2003-08-04 2006-04-27 Pfizer Prod Inc ANTICUERPOS DIRIGIDOS A c-MET
AR045563A1 (es) 2003-09-10 2005-11-02 Warner Lambert Co Anticuerpos dirigidos a m-csf
GB0325836D0 (en) * 2003-11-05 2003-12-10 Celltech R&D Ltd Biological products
CA2546353A1 (en) 2003-11-19 2005-06-09 Array Biopharma Inc. Bicyclic inhibitors of mek and methods of use thereof
ATE473967T1 (de) * 2003-11-26 2010-07-15 Pfizer Prod Inc Aminopyrazolderivate als gsk-3-inhibitoren
MXPA06010974A (es) 2004-03-22 2007-04-23 Southern Res Inst Inhibidores nopeptidos de metaloproteinasas de matriz.
US20050277897A1 (en) * 2004-06-14 2005-12-15 Ghannoum Ziad R Handpiece tip
KR20070036130A (ko) 2004-07-16 2007-04-02 화이자 프로덕츠 인코포레이티드 항-아이지에프-1알 항체를 사용하는 비-혈액학적악성종양에 대한 조합 치료
BR122020017756B1 (pt) 2004-08-26 2022-02-15 Pfizer Inc Uso de compostos de aminoeteroarila enantiomericamente puros na preparação de um medicamento para o tratamento de crescimento celular anormal em um mamífero
MY146381A (en) 2004-12-22 2012-08-15 Amgen Inc Compositions and methods relating relating to anti-igf-1 receptor antibodies
US8436190B2 (en) 2005-01-14 2013-05-07 Cephalon, Inc. Bendamustine pharmaceutical compositions
US7429667B2 (en) 2005-01-20 2008-09-30 Ardea Biosciences, Inc. Phenylamino isothiazole carboxamidines as MEK inhibitors
GB0505756D0 (en) * 2005-03-21 2005-04-27 Mars Uk Ltd Method
JP4173909B1 (ja) 2005-04-28 2008-10-29 ファイザー・リミテッド アミノ酸誘導体
SG177981A1 (en) 2005-05-18 2012-02-28 Array Biopharma Inc 4-(phenylamino)-6-oxo-1, 6-dihydropyridazine-3-carboxamide derivatives as mek inhibitors for the treatment of hyperproliferative diseases
US8101799B2 (en) 2005-07-21 2012-01-24 Ardea Biosciences Derivatives of N-(arylamino) sulfonamides as inhibitors of MEK
AU2006292278B2 (en) 2005-09-20 2012-03-08 Osi Pharmaceuticals, Inc. Biological markers predictive of anti-cancer response to insulin-like growth factor-1 receptor kinase inhibitors
US7842836B2 (en) 2006-04-11 2010-11-30 Ardea Biosciences N-aryl-N'alkyl sulfamides as MEK inhibitors
MX2008013097A (es) 2006-04-18 2008-10-27 Ardea Biosciences Inc Piridona sulfonamidas y piridona sulfamidas como inhibidores de metiletilcetona.
ATE509956T1 (de) * 2006-06-08 2011-06-15 Helmholtz Zentrum Muenchen Spezifische proteaseinhibitoren und ihre verwendung in der krebstherapie
KR20090025367A (ko) 2006-06-28 2009-03-10 가부시키가이샤산와카가쿠켄큐쇼 신규 6-5계 이환식 복소환 유도체 및 그 의약용도
EP2121626A1 (en) 2006-12-15 2009-11-25 Pfizer Products Inc. Benzimidazole derivatives
MX2009007661A (es) 2007-01-19 2009-12-14 Ardea Biosciences Inc Inhibidores de mek.
KR20090113908A (ko) 2007-02-23 2009-11-02 예다 리서치 앤드 디벨럽먼트 캄파니 리미티드 금속단백질 활성 억제용 항체 및 이를 함유하는 약학적 조성물
PT2144604E (pt) * 2007-02-28 2011-10-19 Conatus Pharmaceuticals Inc Métodos para o tratamento da hepatite c viral crónica utilizando ro-113-0830
WO2008106167A1 (en) * 2007-02-28 2008-09-04 Conatus Pharmaceuticals, Inc. Combination therapy comprising matrix metalloproteinase inhibitors and caspase inhibitors for the treatment of liver diseases
BRPI0810411B8 (pt) 2007-04-18 2021-05-25 Pfizer Prod Inc derivados de sulfonil amida para o tratamento de crescimento celular anormal, seu sos, bem como composição farmacêutica
UA99731C2 (ru) 2007-07-30 2012-09-25 Ардеа Биосайенсис, Инк Кристаллические полиморфные формы n-(ариламино)сульфонамидов как ингибиторы мэк, композиция (варианты) и применение
AU2008343065B2 (en) 2007-12-19 2012-04-05 Genentech, Inc. 5-anilinoimidazopyridines and methods of use
NZ586575A (en) 2007-12-21 2012-03-30 Genentech Inc Azaindolizines and methods of use
EP3613743B1 (en) 2008-01-04 2022-03-16 Intellikine, LLC Processes for the preparation of 1h-pyrazolo[3,4-d]pyrimidin-4-amine derivatives
US8193182B2 (en) 2008-01-04 2012-06-05 Intellikine, Inc. Substituted isoquinolin-1(2H)-ones, and methods of use thereof
US8637542B2 (en) 2008-03-14 2014-01-28 Intellikine, Inc. Kinase inhibitors and methods of use
AR072777A1 (es) 2008-03-26 2010-09-22 Cephalon Inc Formas solidas de clorhidrato de bendamustina
CA2756690C (en) 2008-03-28 2016-08-16 Hale Biopharma Ventures, Llc Administration of benzodiazepine compositions
JP5788316B2 (ja) 2008-07-08 2015-09-30 インテリカイン, エルエルシー キナーゼインヒビターおよび使用方法
RU2503681C2 (ru) * 2008-09-30 2014-01-10 Эйсай Ар Энд Ди Менеджмент Ко., Лтд. Новое конденсированное производное аминодигидротиазина
US8476410B2 (en) 2008-10-16 2013-07-02 University of Pittsburgh—of the Commonwealth System of Higher Education Fully human antibodies to high molecular weight-melanoma associated antigen and uses thereof
US8476431B2 (en) 2008-11-03 2013-07-02 Itellikine LLC Benzoxazole kinase inhibitors and methods of use
CN102365021B (zh) 2009-02-05 2015-07-15 伊缪诺金公司 新型苯并二氮杂*衍生物
US20100204221A1 (en) 2009-02-09 2010-08-12 Hariprasad Vankayalapati Pyrrolopyrimidinyl axl kinase inhibitors
WO2010099139A2 (en) 2009-02-25 2010-09-02 Osi Pharmaceuticals, Inc. Combination anti-cancer therapy
US20110171124A1 (en) 2009-02-26 2011-07-14 Osi Pharmaceuticals, Inc. In situ methods for monitoring the EMT status of tumor cells in vivo
EP2401614A1 (en) 2009-02-27 2012-01-04 OSI Pharmaceuticals, LLC Methods for the identification of agents that inhibit mesenchymal-like tumor cells or their formation
WO2010099138A2 (en) 2009-02-27 2010-09-02 Osi Pharmaceuticals, Inc. Methods for the identification of agents that inhibit mesenchymal-like tumor cells or their formation
US20100222381A1 (en) 2009-02-27 2010-09-02 Hariprasad Vankayalapati Cyclopentathiophene/cyclohexathiophene DNA methyltransferase inhibitors
JP2012519282A (ja) 2009-02-27 2012-08-23 オーエスアイ・ファーマシューティカルズ,エルエルシー 間葉様腫瘍細胞またはその生成を阻害する薬剤を同定するための方法
CN106478496A (zh) 2009-03-27 2017-03-08 阿迪生物科学公司 作为mek抑制剂的二氢吡啶磺酰胺和二氢吡啶硫酰胺
EP2427195B1 (en) 2009-05-07 2019-05-01 Intellikine, LLC Heterocyclic compounds and uses thereof
WO2011014726A1 (en) 2009-07-31 2011-02-03 Osi Pharmaceuticals, Inc. Mtor inhibitor and angiogenesis inhibitor combination therapy
PE20121148A1 (es) 2009-08-17 2012-09-07 Intellikine Llc Compuestos heterociclicos y usos de los mismos
CA2772194A1 (en) 2009-09-01 2011-03-10 Pfizer Inc. Benzimidazole derivatives
CN102666512B (zh) 2009-10-13 2014-11-26 奥斯特姆医疗公司 对疾病治疗有用的mek抑制剂
WO2011049625A1 (en) 2009-10-20 2011-04-28 Mansour Samadpour Method for aflatoxin screening of products
PH12012500901A1 (en) 2009-11-05 2016-08-05 Rhizen Pharmaceuticals Sa Novel benzopyran kinase modulators
TW201129384A (en) 2010-02-10 2011-09-01 Immunogen Inc CD20 antibodies and uses thereof
EP2534153B2 (en) 2010-02-12 2024-05-22 Pfizer Inc. Salts and polymorphs of 8-fluoro-2-{4-[(methylamino}methyl]phenyl}-1,3,4,5-tetrahydro-6h-azepino[5,4,3-cd]indol-6-one
CA2783665A1 (en) 2010-03-03 2011-09-09 OSI Pharmaceuticals, LLC Biological markers predictive of anti-cancer response to insulin-like growth factor-1 receptor kinase inhibitors
CA2783656A1 (en) 2010-03-03 2011-09-09 OSI Pharmaceuticals, LLC Biological markers predictive of anti-cancer response to insulin-like growth factor-1 receptor kinase inhibitors
JP5960688B2 (ja) 2010-05-17 2016-08-02 インコゼン セラピューティクス プライベート リミテッド プロテインキナーゼ調節物質としての新規3,5−二置換−3h−[1,2,3]トリアゾロ[4,5−b]ピリジン化合物
CA2799579A1 (en) 2010-05-21 2011-11-24 Intellikine, Inc. Chemical compounds, compositions and methods for kinase modulation
ES2611479T3 (es) 2010-06-16 2017-05-09 University Of Pittsburgh- Of The Commonwealth System Of Higher Education Anticuerpos contra endoplasmina y su uso
JP5802756B2 (ja) 2010-10-20 2015-11-04 ファイザー・インク スムーズンド受容体モジュレーターとしてのピリジン−2−誘導体
JP2013545749A (ja) 2010-11-10 2013-12-26 インフィニティー ファーマシューティカルズ, インコーポレイテッド 複素環化合物及びその使用
WO2012080050A1 (en) * 2010-12-14 2012-06-21 F. Hoffmann-La Roche Ag Solid forms of a phenoxybenzenesulfonyl compound
TWI674262B (zh) 2011-01-10 2019-10-11 美商英菲尼提製藥股份有限公司 製備異喹啉酮之方法及異喹啉酮之固體形式
CA2825894C (en) 2011-02-02 2021-11-30 Amgen Inc. Prognosis of cancer using a circulating biomarker
JP6049642B2 (ja) 2011-02-15 2016-12-21 イミュノジェン・インコーポレーテッド 複合体の調製方法
US20120214830A1 (en) 2011-02-22 2012-08-23 OSI Pharmaceuticals, LLC Biological markers predictive of anti-cancer response to insulin-like growth factor-1 receptor kinase inhibitors in hepatocellular carcinoma
WO2012116237A2 (en) 2011-02-23 2012-08-30 Intellikine, Llc Heterocyclic compounds and uses thereof
EP2681209B1 (en) * 2011-03-02 2018-05-09 Aquilus Pharmaceuticals, Inc Compounds and methods for the treatment of pain and other disorders
US9150644B2 (en) 2011-04-12 2015-10-06 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Human monoclonal antibodies that bind insulin-like growth factor (IGF) I and II
DK2699598T3 (en) 2011-04-19 2019-04-23 Pfizer COMBINATIONS OF ANTI-4-1BB ANTIBODIES AND ADCC-INducing ANTIBODIES FOR TREATMENT OF CANCER
EP2702173A1 (en) 2011-04-25 2014-03-05 OSI Pharmaceuticals, LLC Use of emt gene signatures in cancer drug discovery, diagnostics, and treatment
HRP20190128T1 (hr) 2011-05-04 2019-03-08 Rhizen Pharmaceuticals S.A. Novi spojevi kao modulatori protein kinaza
EP4085899A1 (en) 2011-06-14 2022-11-09 Neurelis, Inc. Administration of benzodiazepine
WO2013012915A1 (en) 2011-07-19 2013-01-24 Infinity Pharmaceuticals Inc. Heterocyclic compounds and uses thereof
MX2014000648A (es) 2011-07-19 2014-09-25 Infinity Pharmaceuticals Inc Compuestos heterociclicos y sus usos.
EP2734205B1 (en) 2011-07-21 2018-03-21 Tolero Pharmaceuticals, Inc. Heterocyclic protein kinase inhibitors
KR20140075693A (ko) 2011-08-29 2014-06-19 인피니티 파마슈티칼스, 인코포레이티드 헤테로사이클릭 화합물 및 그의 용도
KR20140059246A (ko) 2011-09-22 2014-05-15 화이자 인코포레이티드 피롤로피리미딘 및 퓨린 유도체
WO2013049332A1 (en) 2011-09-29 2013-04-04 Infinity Pharmaceuticals, Inc. Inhibitors of monoacylglycerol lipase and methods of their use
CA2848842C (en) 2011-10-04 2020-09-29 King's College London Ige anti -hmw-maa antibody
RU2014114015A (ru) 2011-11-08 2015-12-20 Пфайзер Инк. Способы лечения воспалительных расстройств с использованием антител против m-csf
WO2013126617A1 (en) 2012-02-22 2013-08-29 The Regents Of The University Of Colorado, A Body Corporate Bouvardin derivatives and therapeutic uses thereof
US9452215B2 (en) 2012-02-22 2016-09-27 The Regents Of The University Of Colorado Bourvadin derivatives and therapeutic uses thereof
EP2831073B1 (en) 2012-03-30 2020-12-09 Rhizen Pharmaceuticals S.A. Novel 3,5-disubstitued-3h-imidazo[4,5-b]pyridine and 3,5- disubstitued -3h-[1,2,3]triazolo[4,5-b]pyridine compounds as modulators of c-met protein kinases
WO2013152252A1 (en) 2012-04-06 2013-10-10 OSI Pharmaceuticals, LLC Combination anti-cancer therapy
US8940742B2 (en) 2012-04-10 2015-01-27 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
PL2859017T3 (pl) 2012-06-08 2019-07-31 Sutro Biopharma, Inc. Przeciwciała zawierające swoiste dla miejsca, niewystępujące naturalnie reszty aminokwasowe, sposoby ich wytwarzania i sposoby ich zastosowania
WO2014004639A1 (en) 2012-06-26 2014-01-03 Sutro Biopharma, Inc. Modified fc proteins comprising site-specific non-natural amino acid residues, conjugates of the same, methods of their preparation and methods of their use
HK1211208A1 (zh) 2012-08-22 2016-05-20 Immunogen, Inc. 細胞毒性苯並二氮呯衍生物
HRP20220455T1 (hr) 2012-08-31 2022-05-27 Sutro Biopharma, Inc. Modificirane aminokiseline koje sadrže azid grupu
DK2909181T3 (da) 2012-10-16 2017-11-20 Tolero Pharmaceuticals Inc PKM2-modulatorer og fremgangsmåder til anvendelse deraf
EP2914296B2 (en) 2012-11-01 2021-09-29 Infinity Pharmaceuticals, Inc. Treatment of cancers using pi3 kinase isoform modulators
GB201302755D0 (en) 2013-02-15 2013-04-03 Mars Inc Horse supplement
WO2014134486A2 (en) 2013-02-28 2014-09-04 Immunogen, Inc. Conjugates comprising cell-binding agents and cytotoxic agents
JP6494533B2 (ja) 2013-02-28 2019-04-03 イミュノジェン・インコーポレーテッド 細胞結合剤及び細胞毒性剤としてのマイタンシノイドを含む複合体
MX394360B (es) 2013-03-14 2025-03-24 Sumitomo Pharma Oncology Inc Inhibidores de jak2 y alk2 y metodos para su uso.
UY35464A (es) 2013-03-15 2014-10-31 Araxes Pharma Llc Inhibidores covalentes de kras g12c.
US9745319B2 (en) 2013-03-15 2017-08-29 Araxes Pharma Llc Irreversible covalent inhibitors of the GTPase K-Ras G12C
EP2968340A4 (en) 2013-03-15 2016-08-10 Intellikine Llc COMBINING KINASE INHIBITORS AND USES THEREOF
JP6473133B2 (ja) 2013-03-15 2019-02-20 アラクセス ファーマ エルエルシー Krasg12cの共有結合性阻害剤
US20160024051A1 (en) 2013-03-15 2016-01-28 Infinity Pharmaceuticals, Inc. Salts and solid forms of isoquinolinones and composition comprising and methods of using the same
SG11201509842SA (en) 2013-05-30 2015-12-30 Infinity Pharmaceuticals Inc Treatment of cancers using pi3 kinase isoform modulators
WO2014194030A2 (en) 2013-05-31 2014-12-04 Immunogen, Inc. Conjugates comprising cell-binding agents and cytotoxic agents
ES2865473T3 (es) 2013-07-10 2021-10-15 Sutro Biopharma Inc Anticuerpos que comprenden múltiples residuos de aminoácidos no naturales sitio-específicos, métodos para su preparación y métodos de uso
EP3363800A1 (en) 2013-10-03 2018-08-22 Kura Oncology, Inc. Heterocyclic inhibitors of erk and methods of use
WO2015051241A1 (en) 2013-10-04 2015-04-09 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
MX2021012208A (es) 2013-10-04 2023-01-19 Infinity Pharmaceuticals Inc Compuestos heterocíclicos y usos de los mismos.
TWI659021B (zh) 2013-10-10 2019-05-11 亞瑞克西斯製藥公司 Kras g12c之抑制劑
AU2014331794C1 (en) 2013-10-10 2019-09-12 Araxes Pharma Llc Inhibitors of KRAS G12C
EP3055298B1 (en) 2013-10-11 2020-04-29 Sutro Biopharma, Inc. Modified amino acids comprising tetrazine functional groups, methods of preparation, and methods of their use
WO2015061204A1 (en) 2013-10-21 2015-04-30 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
UA115388C2 (uk) 2013-11-21 2017-10-25 Пфайзер Інк. 2,6-заміщені пуринові похідні та їх застосування в лікуванні проліферативних захворювань
WO2015107139A1 (en) 2014-01-17 2015-07-23 Proyecto De Biomedicina Cima, S.L. Compounds for use as antifibrinolytic agents
WO2015155624A1 (en) 2014-04-10 2015-10-15 Pfizer Inc. Dihydropyrrolopyrimidine derivatives
WO2015168079A1 (en) 2014-04-29 2015-11-05 Infinity Pharmaceuticals, Inc. Pyrimidine or pyridine derivatives useful as pi3k inhibitors
EP3556757A1 (en) 2014-04-30 2019-10-23 Pfizer Inc Cycloalkyl-linked diheterocycle derivatives
CN110526912B (zh) 2014-06-19 2023-02-14 武田药品工业株式会社 用于激酶抑制的杂芳基化合物
WO2016001789A1 (en) 2014-06-30 2016-01-07 Pfizer Inc. Pyrimidine derivatives as pi3k inhibitors for use in the treatment of cancer
US10934360B2 (en) 2014-07-31 2021-03-02 The Hong Kong University Of Science And Technology Human monoclonal antibodies against EPHA4 and their use
JO3556B1 (ar) 2014-09-18 2020-07-05 Araxes Pharma Llc علاجات مدمجة لمعالجة السرطان
ES2826443T3 (es) 2014-09-25 2021-05-18 Araxes Pharma Llc Inhibidores de proteínas mutantes KRAS G12C
US10011600B2 (en) 2014-09-25 2018-07-03 Araxes Pharma Llc Methods and compositions for inhibition of Ras
WO2016054491A1 (en) 2014-10-03 2016-04-07 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
ES2746839T3 (es) 2014-12-18 2020-03-09 Pfizer Derivados de pirimidina y triazina y su uso como inhibidores de AXL
JP2018513853A (ja) 2015-04-10 2018-05-31 アラクセス ファーマ エルエルシー 置換キナゾリン化合物およびその使用方法
JP6789239B2 (ja) 2015-04-15 2020-11-25 アラクセス ファーマ エルエルシー Krasの縮合三環系インヒビターおよびその使用の方法
US9901574B2 (en) 2015-04-20 2018-02-27 Tolero Pharmaceuticals, Inc. Predicting response to alvocidib by mitochondrial profiling
WO2016178876A2 (en) 2015-05-01 2016-11-10 Cocrystal Pharma, Inc. Nucleoside analogs for treatment of the flaviviridae family of viruses and cancer
ES2739749T3 (es) 2015-05-18 2020-02-03 Tolero Pharmaceuticals Inc Profármacos de alvocidib que tienen biodisponibilidad aumentada
AR104020A1 (es) 2015-06-04 2017-06-21 Kura Oncology Inc Métodos y composiciones para inhibir la interacción de menina con proteínas mill
WO2017009751A1 (en) 2015-07-15 2017-01-19 Pfizer Inc. Pyrimidine derivatives
US10144724B2 (en) 2015-07-22 2018-12-04 Araxes Pharma Llc Substituted quinazoline compounds and methods of use thereof
MX2018001289A (es) 2015-08-03 2018-04-30 Tolero Pharmaceuticals Inc Terapias de combinacion para el tratamiento del cancer.
EP4585268A3 (en) 2015-09-14 2025-10-15 Twelve Therapeutics, Inc. Solid forms of isoquinolinone derivatives, process of making, compositions comprising, and methods of using the same
EP3356353A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
US10647703B2 (en) 2015-09-28 2020-05-12 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
US10882847B2 (en) 2015-09-28 2021-01-05 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
EP3356354A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
WO2017058915A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
WO2017058807A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
WO2017058902A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
JP2018533939A (ja) 2015-10-19 2018-11-22 アラクセス ファーマ エルエルシー Rasの阻害剤をスクリーニングするための方法
KR20180081596A (ko) 2015-11-16 2018-07-16 아락세스 파마 엘엘씨 치환된 헤테로사이클릭 그룹을 포함하는 2-치환된 퀴나졸린 화합물 및 이의 사용 방법
CN108601752A (zh) 2015-12-03 2018-09-28 安吉奥斯医药品有限公司 用于治疗mtap缺失型癌症的mat2a抑制剂
WO2017100546A1 (en) 2015-12-09 2017-06-15 Araxes Pharma Llc Methods for preparation of quinazoline derivatives
SG11201806419RA (en) 2016-01-27 2018-08-30 Sutro Biopharma Inc Anti-cd74 antibody conjugates, compositions comprising anti-cd74 antibody conjugates and methods of using anti-cd74 antibody conjugates
CN109640987B (zh) 2016-03-16 2022-12-02 库拉肿瘤学公司 Menin-mll的桥联双环抑制剂及使用方法
CN109152784B (zh) 2016-03-16 2021-12-28 库拉肿瘤学公司 经取代的menin-mll抑制剂及使用方法
WO2017172979A1 (en) 2016-03-30 2017-10-05 Araxes Pharma Llc Substituted quinazoline compounds and methods of use
AU2017263574B2 (en) 2016-05-12 2022-11-17 The Regents Of The University Of Michigan ASH1L inhibitors and methods of treatment therewith
US11118233B2 (en) 2016-05-18 2021-09-14 The University Of Chicago BTK mutation and ibrutinib resistance
WO2017214269A1 (en) 2016-06-08 2017-12-14 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
US10646488B2 (en) 2016-07-13 2020-05-12 Araxes Pharma Llc Conjugates of cereblon binding compounds and G12C mutant KRAS, HRAS or NRAS protein modulating compounds and methods of use thereof
CA3035081A1 (en) 2016-09-02 2018-03-08 Dana-Farber Cancer Institute, Inc. Composition and methods of treating b cell disorders
US10280172B2 (en) 2016-09-29 2019-05-07 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
EP3523289A1 (en) 2016-10-07 2019-08-14 Araxes Pharma LLC Heterocyclic compounds as inhibitors of ras and methods of use thereof
WO2018094275A1 (en) 2016-11-18 2018-05-24 Tolero Pharmaceuticals, Inc. Alvocidib prodrugs and their use as protein kinase inhibitors
KR20190099260A (ko) 2016-12-19 2019-08-26 톨레로 파마수티컬스, 인크. 프로파일링 펩티드 및 감도 프로파일링을 위한 방법
WO2018119183A2 (en) 2016-12-22 2018-06-28 Amgen Inc. Kras g12c inhibitors and methods of using the same
CN110382482A (zh) 2017-01-26 2019-10-25 亚瑞克西斯制药公司 稠合的杂-杂二环化合物及其使用方法
WO2018140514A1 (en) 2017-01-26 2018-08-02 Araxes Pharma Llc 1-(6-(3-hydroxynaphthalen-1-yl)quinazolin-2-yl)azetidin-1-yl)prop-2-en-1-one derivatives and similar compounds as kras g12c inhibitors for the treatment of cancer
WO2018140599A1 (en) 2017-01-26 2018-08-02 Araxes Pharma Llc Benzothiophene and benzothiazole compounds and methods of use thereof
WO2018140513A1 (en) 2017-01-26 2018-08-02 Araxes Pharma Llc 1-(3-(6-(3-hydroxynaphthalen-1-yl)benzofuran-2-yl)azetidin-1yl)prop-2-en-1-one derivatives and similar compounds as kras g12c modulators for treating cancer
EP3574009A4 (en) 2017-01-26 2020-11-25 Zlip Holding Limited CD47 ANTIGEN BINDING UNIT AND ITS USES
EP3573954A1 (en) 2017-01-26 2019-12-04 Araxes Pharma LLC Fused bicyclic benzoheteroaromatic compounds and methods of use thereof
US20200385364A1 (en) 2017-01-26 2020-12-10 Araxes Pharma Llc Fused n-heterocyclic compounds and methods of use thereof
CN110691779B (zh) 2017-03-24 2023-10-10 库拉肿瘤学公司 治疗血液系统恶性肿瘤和尤因肉瘤的方法
EA201992781A1 (ru) 2017-05-22 2020-04-01 Эмджен Инк. Ингибиторы g12c kras и способы их применения
AU2018271990A1 (en) 2017-05-25 2019-12-12 Araxes Pharma Llc Covalent inhibitors of KRAS
JP2020521741A (ja) 2017-05-25 2020-07-27 アラクセス ファーマ エルエルシー がんの処置のための化合物およびその使用の方法
US11639346B2 (en) 2017-05-25 2023-05-02 Araxes Pharma Llc Quinazoline derivatives as modulators of mutant KRAS, HRAS or NRAS
US11542248B2 (en) 2017-06-08 2023-01-03 Kura Oncology, Inc. Methods and compositions for inhibiting the interaction of menin with MLL proteins
US20200207859A1 (en) 2017-07-26 2020-07-02 Sutro Biopharma, Inc. Methods of using anti-cd74 antibodies and antibody conjugates in treatment of t-cell lymphoma
MA50077A (fr) 2017-09-08 2020-07-15 Amgen Inc Inhibiteurs de kras g12c et leurs procédés d'utilisation
WO2019055579A1 (en) 2017-09-12 2019-03-21 Tolero Pharmaceuticals, Inc. TREATMENT REGIME FOR CANCERS THAT ARE INSENSITIVE TO BCL-2 INHIBITORS USING THE MCL-1 ALVOCIDIB INHIBITOR
JP7423513B2 (ja) 2017-09-18 2024-01-29 ストロ バイオファーマ インコーポレーテッド 抗葉酸受容体α抗体コンジュゲート及びその使用
US11649251B2 (en) 2017-09-20 2023-05-16 Kura Oncology, Inc. Substituted inhibitors of menin-MLL and methods of use
US20200237766A1 (en) 2017-10-13 2020-07-30 Tolero Pharmaceuticals, Inc. Pkm2 activators in combination with reactive oxygen species for treatment of cancer
WO2019094772A1 (en) 2017-11-10 2019-05-16 The Regents Of The University Of Michigan Ash1l degraders and methods of treatment therewith
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
WO2019213516A1 (en) 2018-05-04 2019-11-07 Amgen Inc. Kras g12c inhibitors and methods of using the same
ES2995514T3 (en) 2018-05-04 2025-02-10 Amgen Inc Kras g12c inhibitors and methods of using the same
EP3790886B1 (en) 2018-05-10 2024-06-26 Amgen Inc. Kras g12c inhibitors for the treatment of cancer
ES2938987T3 (es) 2018-06-01 2023-04-18 Amgen Inc Inhibidores de KRAS G12c y métodos de uso de los mismos
EP3813784B1 (en) 2018-06-07 2024-01-10 The Regents Of The University Of Michigan Prc1 inhibitors and prc1 inhibitors for use in methods of treatment therewith
US20190375749A1 (en) 2018-06-11 2019-12-12 Amgen Inc. Kras g12c inhibitors and methods of using the same
ES3060664T3 (en) 2018-06-12 2026-03-27 Amgen Inc Kras g12c inhibitors encompassing a piperazine ring and use thereof in the treatment of cancer
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.
MX2021000887A (es) 2018-08-01 2021-03-31 Araxes Pharma Llc Compuestos espiroheterociclicos y metodos de uso de los mismos para el tratamiento de cancer.
JP2022500454A (ja) 2018-09-17 2022-01-04 ストロ バイオファーマ インコーポレーテッド 抗葉酸受容体抗体コンジュゲートによる併用療法
WO2020086739A1 (en) 2018-10-24 2020-04-30 Araxes Pharma Llc 2-(2-acryloyl-2,6-diazaspiro[3.4]octan-6-yl)-6-(1h-indazol-4-yl)-benzonitrile derivatives and related compounds as inhibitors of g12c mutant kras protein for inhibiting tumor metastasis
JP7516029B2 (ja) 2018-11-16 2024-07-16 アムジエン・インコーポレーテツド Kras g12c阻害剤化合物の重要な中間体の改良合成法
US11053226B2 (en) 2018-11-19 2021-07-06 Amgen Inc. KRAS G12C inhibitors and methods of using the same
JP7377679B2 (ja) 2018-11-19 2023-11-10 アムジエン・インコーポレーテツド がん治療のためのkrasg12c阻害剤及び1種以上の薬学的に活性な追加の薬剤を含む併用療法
AU2019388998A1 (en) 2018-11-29 2021-06-03 Araxes Pharma Llc Compounds and methods of use thereof for treatment of cancer
US11034710B2 (en) 2018-12-04 2021-06-15 Sumitomo Dainippon Pharma Oncology, Inc. CDK9 inhibitors and polymorphs thereof for use as agents for treatment of cancer
WO2020132651A1 (en) 2018-12-20 2020-06-25 Amgen Inc. Kif18a inhibitors
TWI844602B (zh) 2018-12-20 2024-06-11 美商安進公司 Kif18a抑制劑
JP7676308B2 (ja) 2018-12-20 2025-05-14 アムジエン・インコーポレーテツド Kif18a阻害剤として有用なヘテロアリールアミド
EP3898616B1 (en) 2018-12-20 2024-10-02 Amgen Inc. Heteroaryl amides useful as kif18a inhibitors
NZ778055A (en) 2019-02-12 2025-11-28 Sumitomo Pharma America Inc Formulations comprising heterocyclic protein kinase inhibitors
CN113727758A (zh) 2019-03-01 2021-11-30 锐新医药公司 双环杂环基化合物及其用途
WO2020180768A1 (en) 2019-03-01 2020-09-10 Revolution Medicines, Inc. Bicyclic heteroaryl compounds and uses thereof
US11793802B2 (en) 2019-03-20 2023-10-24 Sumitomo Pharma Oncology, Inc. Treatment of acute myeloid leukemia (AML) with venetoclax failure
CA3133460A1 (en) 2019-03-22 2020-10-01 Sumitomo Dainippon Pharma Oncology, Inc. Compositions comprising pkm2 modulators and methods of treatment using the same
EP3962951A1 (en) 2019-05-03 2022-03-09 Sutro Biopharma, Inc. Anti-bcma antibody conjugates
EP3738593A1 (en) 2019-05-14 2020-11-18 Amgen, Inc Dosing of kras inhibitor for treatment of cancers
NZ782284A (en) 2019-05-21 2024-11-29 Amgen Inc Solid state forms
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
US12540129B2 (en) 2019-08-02 2026-02-03 Amgen Inc. KIF18A inhibitors
EP4007756B1 (en) 2019-08-02 2025-12-24 Amgen Inc. Kif18a inhibitors
WO2021026099A1 (en) 2019-08-02 2021-02-11 Amgen Inc. Kif18a inhibitors
AU2020326627B2 (en) 2019-08-02 2026-01-29 Amgen Inc. KIF18A inhibitors
EP4031542B1 (en) 2019-09-18 2025-10-15 Merck Sharp & Dohme LLC Small molecule inhibitors of kras g12c mutant
TW202126636A (zh) 2019-09-30 2021-07-16 美商阿吉歐斯製藥公司 作為menin抑制劑之六氫吡啶化合物
EP4684786A3 (en) 2019-10-24 2026-04-08 Amgen Inc. Pyridopyrimidine derivatives useful as kras g12c and kras g12d inhibitors in the treatment of cancer
CN114867726B (zh) 2019-10-28 2023-11-28 默沙东有限责任公司 Kras g12c突变体的小分子抑制剂
WO2021085653A1 (en) 2019-10-31 2021-05-06 Taiho Pharmaceutical Co., Ltd. 4-aminobut-2-enamide derivatives and salts thereof
CN120699039A (zh) 2019-11-04 2025-09-26 锐新医药公司 Ras抑制剂
WO2021091956A1 (en) 2019-11-04 2021-05-14 Revolution Medicines, Inc. Ras inhibitors
MX2022005359A (es) 2019-11-04 2022-06-02 Revolution Medicines Inc Inhibidores de ras.
TW202128688A (zh) 2019-11-08 2021-08-01 美商銳新醫藥公司 雙環雜芳基化合物及其用途
WO2021097207A1 (en) 2019-11-14 2021-05-20 Amgen Inc. Improved synthesis of kras g12c inhibitor compound
JP2023501528A (ja) 2019-11-14 2023-01-18 アムジエン・インコーポレーテツド Kras g12c阻害剤化合物の改善された合成
EP4065231A1 (en) 2019-11-27 2022-10-05 Revolution Medicines, Inc. Covalent ras inhibitors and uses thereof
WO2021106231A1 (en) 2019-11-29 2021-06-03 Taiho Pharmaceutical Co., Ltd. A compound having inhibitory activity against kras g12d mutation
CN114929279A (zh) 2020-01-07 2022-08-19 锐新医药公司 Shp2抑制剂给药和治疗癌症的方法
WO2021155006A1 (en) 2020-01-31 2021-08-05 Les Laboratoires Servier Sas Inhibitors of cyclin-dependent kinases and uses thereof
US20230095053A1 (en) 2020-03-03 2023-03-30 Sutro Biopharma, Inc. Antibodies comprising site-specific glutamine tags, methods of their preparation and methods of their use
TW202204333A (zh) 2020-04-08 2022-02-01 美商阿吉歐斯製藥公司 Menin抑制劑及治療癌症之使用方法
WO2021207310A1 (en) 2020-04-08 2021-10-14 Agios Pharmaceuticals, Inc. Menin inhibitors and methods of use for treating cancer
WO2021215545A1 (en) 2020-04-24 2021-10-28 Taiho Pharmaceutical Co., Ltd. Anticancer combination therapy with n-(1-acryloyl-azetidin-3-yl)-2-((1h-indazol-3-yl)amino)methyl)-1h-imidazole-5-carboxamide inhibitor of kras-g12c
WO2021215544A1 (en) 2020-04-24 2021-10-28 Taiho Pharmaceutical Co., Ltd. Kras g12d protein inhibitors
IL299131A (en) 2020-06-18 2023-02-01 Revolution Medicines Inc Methods for delaying, preventing and treating acquired resistance to RAS inhibitors
CA3185209A1 (en) 2020-07-10 2021-01-27 Alyssa WINKLER Gas41 inhibitors and methods of use thereof
EP4183395A4 (en) 2020-07-15 2024-07-24 Taiho Pharmaceutical Co., Ltd. PYRIMIDINE COMPOUND-CONTAINING COMBINATION FOR USE IN TUMOR TREATMENT
US12605387B2 (en) 2020-07-24 2026-04-21 Secura Bio, Inc. Treatment of cancers using PI3 kinase isoform modulators
MX2023002248A (es) 2020-09-03 2023-05-16 Revolution Medicines Inc Uso de inhibidores de sos1 para tratar neoplasias malignas con mutaciones de shp2.
MX2023003060A (es) 2020-09-15 2023-04-05 Revolution Medicines Inc Derivados indolicos como inhibidores de ras en el tratamiento del cancer.
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
US20240051956A1 (en) 2020-12-22 2024-02-15 Qilu Regor Therapeutics Inc. Sos1 inhibitors and uses thereof
EP4323356A1 (en) 2021-04-13 2024-02-21 Nuvalent, Inc. Amino-substituted heterocycles for treating cancers with egfr mutations
US11931420B2 (en) 2021-04-30 2024-03-19 Celgene Corporation Combination therapies using an anti-BCMA antibody drug conjugate (ADC) in combination with a gamma secretase inhibitor (GSI)
AU2022268962A1 (en) 2021-05-05 2023-12-14 Revolution Medicines, Inc. Ras inhibitors for the treatment of cancer
CA3217393A1 (en) 2021-05-05 2022-11-10 Elena S. Koltun Ras inhibitors
WO2022235866A1 (en) 2021-05-05 2022-11-10 Revolution Medicines, Inc. Covalent ras inhibitors and uses thereof
WO2022250170A1 (en) 2021-05-28 2022-12-01 Taiho Pharmaceutical Co., Ltd. Small molecule inhibitors of kras mutated proteins
CN117580579A (zh) 2021-06-10 2024-02-20 纽瑞莱斯有限公司 用于治疗儿科患者的癫痫发作病症的方法和组合物
WO2023056589A1 (en) 2021-10-08 2023-04-13 Servier Pharmaceuticals Llc Menin inhibitors and methods of use for treating cancer
AR127308A1 (es) 2021-10-08 2024-01-10 Revolution Medicines Inc Inhibidores ras
WO2023064058A1 (en) 2021-10-12 2023-04-20 Peloton Therapeutics Inc. Tricyclic sultams and sulfamides as antitumor agents
TW202340214A (zh) 2021-12-17 2023-10-16 美商健臻公司 做為shp2抑制劑之吡唑并吡𠯤化合物
EP4227307A1 (en) 2022-02-11 2023-08-16 Genzyme Corporation Pyrazolopyrazine compounds as shp2 inhibitors
WO2023172858A1 (en) 2022-03-07 2023-09-14 Amgen Inc. A process for preparing 4-methyl-2-propan-2-yl-pyridine-3-carbonitrile
CN119136806A (zh) 2022-03-08 2024-12-13 锐新医药公司 用于治疗免疫难治性肺癌的方法
TW202412755A (zh) 2022-04-25 2024-04-01 美商耐斯泰德醫療公司 促分裂原活化蛋白激酶(mek)抑制劑
WO2023240263A1 (en) 2022-06-10 2023-12-14 Revolution Medicines, Inc. Macrocyclic ras inhibitors
KR20250043602A (ko) 2022-06-30 2025-03-28 서트로 바이오파마, 인크. 항-ror1 항체 및 항체 접합체, 항-ror1 항체 또는 항체 접합체를 포함하는 조성물, 및 항-ror1 항체 및 항체 접합체의 제조 및 사용 방법
MA71389A (fr) 2022-07-08 2025-04-30 Nested Therapeutics, Inc. Inhibiteurs de protéine kinase activée par mitogène (mek)
AU2023358792A1 (en) 2022-10-14 2025-04-17 Black Diamond Therapeutics, Inc. Methods of treating cancers using isoquinoline or 6-aza-quinoline derivatives
EP4687905A1 (en) 2023-03-30 2026-02-11 Revolution Medicines, Inc. Compositions for inducing ras gtp hydrolysis and uses thereof
CN121263418A (zh) 2023-04-07 2026-01-02 锐新医药公司 大环ras抑制剂
KR20260005904A (ko) 2023-04-07 2026-01-12 레볼루션 메디슨즈, 인크. 매크로사이클릭 ras 억제제
AU2024252105A1 (en) 2023-04-14 2025-10-16 Revolution Medicines, Inc. Crystalline forms of ras inhibitors, compositions containing the same, and methods of use thereof
KR20250172857A (ko) 2023-04-14 2025-12-09 레볼루션 메디슨즈, 인크. Ras 억제제의 결정형
EP4701735A1 (en) 2023-04-24 2026-03-04 Nested Therapeutics, Inc. Heterocyclic derivative as mitogen-activated protein kinase (mek) inhibitor
AU2024265078A1 (en) 2023-05-04 2025-12-11 Revolution Medicines, Inc. Combination therapy for a ras related disease or disorder
IL326136A (en) 2023-08-07 2026-03-01 Revolution Medicines Inc RMC-6291 for use in the treatment of a disease or disorder associated with the RAS protein
KR20260042550A (ko) 2023-08-24 2026-03-31 다이호야쿠힌고교 가부시키가이샤 세다주리딘 및 아자시티딘의 고정 용량 조합물
US20250154171A1 (en) 2023-10-12 2025-05-15 Revolution Medicines, Inc. Ras inhibitors
AU2024358957A1 (en) 2023-10-13 2026-04-02 Sutro Biopharma, Inc. Anti-tissue factor antibodies and antibody conjugates, compositions comprising anti-tissue factor antibodies or antibody conjugates, and methods of making and using anti-tissue factor antibodies and antibody conjugates
WO2025085748A1 (en) 2023-10-20 2025-04-24 Merck Sharp & Dohme Llc Small molecule inhibitors of kras proteins
WO2025090905A1 (en) 2023-10-26 2025-05-01 Nested Therapeutics, Inc. Crystalline forms of 3-[[3-fluoro-2-(methylsulfamoylamino)-4-pyridyl]methyl]-7-[(3-fluoro-2-pyridyl)oxy]-4-methyl-chromen-2-one
TW202542151A (zh) 2023-12-22 2025-11-01 美商銳格醫藥有限公司 Sos1抑制劑及其用途
WO2025240847A1 (en) 2024-05-17 2025-11-20 Revolution Medicines, Inc. Ras inhibitors
WO2025250825A1 (en) 2024-05-30 2025-12-04 Sutro Biopharma, Inc. Anti-trop2 antibodies, compositions comprising anti-trop2 antibodies and methods of making and using anti-trop2 antibodies
US20250375445A1 (en) 2024-06-07 2025-12-11 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
WO2025259841A1 (en) 2024-06-13 2025-12-18 Nested Therapeutics, Inc. Crystalline forms of 3-[[3-fluoro-2-(methylsulfamoylamino)-4-pyridyl]jmethyl]-7-[(3-fluoro-2-pyridyl)oxy]-4-methyl-chromen-2-one
WO2025265060A1 (en) 2024-06-21 2025-12-26 Revolution Medicines, Inc. Therapeutic compositions and methods for managing treatment-related effects
WO2026006747A1 (en) 2024-06-28 2026-01-02 Revolution Medicines, Inc. Ras inhibitors
WO2026015801A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015796A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015825A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Use of ras inhibitor for treating pancreatic cancer
WO2026015790A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026035750A1 (en) 2024-08-05 2026-02-12 Pivot Therapeutics, Inc. Inhibitors of akt and uses thereof
WO2026043823A2 (en) 2024-08-19 2026-02-26 Sutro Biopharma, Inc. Antibodies comprising site-specific non-natural amino acid residues, methods of preparation and uses thereof
WO2026050446A1 (en) 2024-08-29 2026-03-05 Revolution Medicines, Inc. Ras inhibitors
WO2026072904A2 (en) 2024-09-26 2026-04-02 Revolution Medicines, Inc. Compositions and methods for treating lung cancer
WO2026080697A1 (en) 2024-10-09 2026-04-16 Sutro Biopharma, Inc. Antibody conjugates with high payload to antibody ratios, compositions comprising the same, and methods of their use

Family Cites Families (26)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4394520A (en) * 1964-01-29 1983-07-19 Societe Anonyme Dite: L'oreal 5-Ureido-3-thia hexanedioic acid
FR1580899A (es) * 1968-03-29 1969-09-12
US4046647A (en) * 1976-06-17 1977-09-06 M&T Chemicals Inc. Additive for improved electroplating process
JPS5527116A (en) * 1978-08-15 1980-02-27 Hokko Chem Ind Co Ltd Preparation of organic sulfur compound
US4268516A (en) * 1978-10-11 1981-05-19 Pfizer Inc. [1]Benzothiopyrano[4,3-c]pyrazoles as immunoregulatory agents
ZW23187A1 (en) * 1986-12-15 1988-06-29 Hoffmann La Roche Phosphinic acid derivatives
GB8827305D0 (en) * 1988-11-23 1988-12-29 British Bio Technology Compounds
GB9000846D0 (en) * 1990-01-15 1990-03-14 Beecham Group Plc Novel compounds
GB9022117D0 (en) * 1990-10-11 1990-11-21 Beecham Group Plc Novel compounds
EP0813868B1 (en) * 1990-11-19 2005-06-01 Monsanto Company Retroviral protease inhibitors
US5475013A (en) * 1990-11-19 1995-12-12 Monsanto Company Retroviral protease inhibitors
US5239078A (en) * 1990-11-21 1993-08-24 Glycomed Incorporated Matrix metalloprotease inhibitors
US5189178A (en) * 1990-11-21 1993-02-23 Galardy Richard E Matrix metalloprotease inhibitors
US5183900A (en) * 1990-11-21 1993-02-02 Galardy Richard E Matrix metalloprotease inhibitors
EP0586537A4 (en) * 1991-05-28 1997-06-25 Merck & Co Inc Substituted n-carboxyalkylpeptidyl derivatives as antidegenerative active agents
US5525629A (en) * 1992-04-07 1996-06-11 British Bio-Technology Limited Inhibition of cytokine production
US5268391A (en) * 1992-07-20 1993-12-07 C. D. Searle & Co. Propargyl-terminated cycloalkylalkyl-P2-site substituted aryl/alkylsulfonyl-terminated alanine amino-diol compounds for treatment of hypertension
US5455258A (en) * 1993-01-06 1995-10-03 Ciba-Geigy Corporation Arylsulfonamido-substituted hydroxamic acids
US5714491A (en) * 1993-04-27 1998-02-03 Celltech Therapeutics Limited Peptidyl derivatives as metalloproteinase inhibitors
GB9320660D0 (en) * 1993-10-07 1993-11-24 British Bio Technology Inhibition of cytokine production
JPH08127581A (ja) * 1994-01-21 1996-05-21 Sankyo Co Ltd ジ置換チオフェン化合物
AU2394795A (en) * 1994-04-28 1995-11-29 Du Pont Merck Pharmaceutical Company, The Hydroxamic acid and amino acid derivatives and their use as anti-arthritic agents
GB9411598D0 (en) * 1994-06-09 1994-08-03 Hoffmann La Roche Hydroxamic acid derivatives
GB9416897D0 (en) * 1994-08-20 1994-10-12 British Biotech Pharm Metalloproteinase inhibitors
US5789434A (en) * 1994-11-15 1998-08-04 Bayer Corporation Derivatives of substituted 4-biarylbutyric acid as matrix metalloprotease inhibitors
JP4358908B2 (ja) * 1996-01-02 2009-11-04 アヴェンティス ファーマシューティカルズ インコーポレイテッド 置換(アリール、ヘテロアリール、アリールメチル又はヘテロアリールメチル)ヒドロキサム酸化合物

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BR9606134A (pt) 1998-11-03
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