HRP20171961T1 - Kemijski spojevi - Google Patents

Kemijski spojevi Download PDF

Info

Publication number
HRP20171961T1
HRP20171961T1 HRP20171961TT HRP20171961T HRP20171961T1 HR P20171961 T1 HRP20171961 T1 HR P20171961T1 HR P20171961T T HRP20171961T T HR P20171961TT HR P20171961 T HRP20171961 T HR P20171961T HR P20171961 T1 HRP20171961 T1 HR P20171961T1
Authority
HR
Croatia
Prior art keywords
fluoro
pyrido
phenyl
indol
methylpropyl
Prior art date
Application number
HRP20171961TT
Other languages
English (en)
Inventor
Nadim AKHTAR
Robert Hugh Bradbury
David Buttar
Gordon Stuart Currie
Christopher De Savi
Craig Samuel Donald
Richard Albert Norman
Matthew OSBORNE
Alfred Arthur Rabow
Heather Marie Redfearn
Helen Elizabeth Williams
Neda YAVARI
Original Assignee
Astrazeneca Ab
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
Application filed by Astrazeneca Ab filed Critical Astrazeneca Ab
Publication of HRP20171961T1 publication Critical patent/HRP20171961T1/hr

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C57/00—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms
    • C07C57/02—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms with only carbon-to-carbon double bonds as unsaturation
    • C07C57/13—Dicarboxylic acids
    • C07C57/145—Maleic acid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07—Optical isomers
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Indole Compounds (AREA)

Claims (16)

1. Spoj s formulom (I) [image] naznačen time da: R1 i R2 su svaki neovisno H ili F; R3 je H ili metil; i bilo koji od: a) R4 je H i R5 je F; ili b) R4 je F i R5 je H; ili njegova farmaceutski prihvatljiva sol.
2. Spoj prema zahtjevu 1, ili njegova farmaceutski prihvatljiva sol, naznačen time da spoj je spoj s formulom (IA). [image]
3. Spoj prema zahtjevu 1 ili zahtjevu 2, ili farmaceutski prihvatljiva sol naznačen time da R3 je vodik.
4. Spoj prema bilo kojem od prethodnih zahtjeva, ili njegova farmaceutski prihvatljiva sol naznačen time da R4 je vodik i R5 je fluoro.
5. Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol naznačen time da je spoj odabran od: (E)-3-(3,5-difluoro-4-((1R,3R)-2-(2-fluoro-2-metilpropil)-3-metil-2,3,4,9-tetrahidro-1H-pirido[3,4-b]indol-1-il)fenil)akrilne kiseline; (E)-3-(4-((1R,3R)-2-(2-fluoro-2-metilpropil)-3-metil-2,3,4,9-tetrahidro-1H-pirido[3,4-b]indol-1-il)fenil)akrilne kiseline; (E)-3-(3,5-difluoro-4-((1R,3R)-2-((S)-3-fluoro-2-metilpropil)-3-metil-2,3,4,9-tetrahidro-1H-pirido[3,4-b]indol-1-il)fenil)akrilne kiseline; (E)-3-(4-((1R,3R)-2-((S)-3-fluoro-2-metilpropil)-3-metil-2,3,4,9-tetrahidro-1H-pirido[3,4-b]indol-1-il)fenil)akrilne kiseline; (E)-3-(3,5-difluoro-4-(2-((S)-3-fluoro-2-metilpropil)-3,3-dimetil-2,3,4,9-tetrahidro-1H-pirido[3,4-b]indol-1-il)fenil)akrilne kiseline; (E)-3-(3,5-difluoro-4-(2-(2-fluoro-2-metilpropil)-3,3-dimetil-2,3,4,9-tetrahidro-1H-pirido[3,4-b]indol-1-il)fenil)akrilne kiseline; (E)-3-(4-(2-((S)-3-fluoro-2-metilpropil)-3,3-dimetil-2,3,4,9-tetrahidro-1H-pirido[3,4-b]indol-1-il)fenil)akrilne kiseline; (E)-3-(4-(2-(2-fluoro-2-metilpropil)-3,3-dimetil-2,3,4,9-tetrahidro-1H-pirido[3,4-b]indol-1-il)fenil)akrilne kiseline; (E)-3-(3-fluoro-4-(2-((S)-3-fluoro-2-metilpropil)-3,3-dimetil-2,3,4,9-tetrahidro-1H-pirido[3,4-b]indol-1-il)fenil)akrilne kiseline; i (E)-3-[4-[(1R,3R)-1-deuterio-2-(2-fluoro-2-metil-propil)-3-metil-4,9-dihidro-3H-pirido[3,4-b]indol-1-il]-3,5-difluoro-fenil]prop-2-enske kiseline.
6. Spoj prema zahtjevu 5, naznačen time da je (E)-3-(3,5-difluoro-4-((1R,3R)-2-(2-fluoro-2-metilpropil)-3-metil-2,3,4,9-tetrahidro-1H-pirido[3,4-b]indol-1-il)fenil)akrilne kiseline, koji spoj ima slijedeću strukturu: [image] ili njegova farmaceutski prihvatljiva sol.
7. Spoj prema zahtjevu 6 naznačen time da je (E)-3-(3,5-Difluoro-4-((1R,3R)-2-(2-fluoro-2-metilpropil)-3-metil-2,3,4,9-tetrahidro-1H-pirido[3,4-b]indol-1-il)fenil)akrilne kiseline.
8. Spoj prema zahtjevu 6 naznačen time da je maleatna sol (E)-3-(3,5-Difluoro-4-((1R,3R)-2-(2-fluoro-2-metilpropil)-3-metil-2,3,4,9-tetrahidro-1H-pirido[3,4-b]indol-1-il)fenil)akrilne kiseline.
9. Spoj prema zahtjevu 7 u kristalnom obliku, naznačen time da ima uzorak difrakcije X-zraka na prahu (XRPD) s barem dva specifična maksimuma 2-theta = 8.4° i 10.9° pri čemu navedene vrijednosti mogu biti plus ili minus 0.2° 2-theta.
10. Spoj prema bilo kojem od prethodnih zahtjeva, ili njegova farmaceutski prihvatljiva sol naznačen time da je uporabu kao lijek.
11. Spoj prema bilo kojem od zahtjeva 1 do 9, ili njegova farmaceutski prihvatljiva sol naznačen time da je uporabu za sprječavanje ili liječenje raka kod toplokrvne životinje kao što je čovjek.
12. Spoj za uporabu za sprječavanje ili liječenje raka, prema zahtjevu 11, naznačen time da je (E)-3-(3,5-Difluoro-4-((1R,3R)-2-(2-fluoro-2-metilpropil)-3-metil-2,3,4,9-tetrahidro-1H-pirido[3,4-b]indol-1-il)fenil)akrilna kiselina, ili njegova farmaceutski prihvatljiva sol.
13. Spoj za uporabu za liječenje raka, ili njegova farmaceutski prihvatljiva sol, prema zahtjevu 11 ili zahtjevu 12, naznačen time da rak je rak dojke ili ginekološki karcinom.
14. Farmaceutski pripravak naznačen time da sadrži spoj s Formulom (I) ili njegova farmaceutski prihvatljiva sol, prema bilo kojem od zahtjeva 1 do 9, te farmaceutski prihvatljivo sredstvo za otapanje ili nosač.
15. Farmaceutski pripravak prema zahtjevu 14 naznačen time da sadrži (E)-3-(3,5-difluoro-4-((1R,3R)-2-(2-fluoro-2-metilpropil)-3-metil-2,3,4,9-tetrahidro-1H-pirido[3,4-b]indol-1-il)fenil)akrilne kiseline ili njegova farmaceutski prihvatljiva sol, u kombinaciji s barem jednim farmaceutski prihvatljivim sredstvom za otapanje ili nosačem, pri čemu pripravak sadrži manje od 5% m/m (R,E)-3-(3,5-difluoro-4-(2-(2-fluoro-2-metilpropil)-3-metil-4,9-dihidro-3H-pirido[3,4-b]indol-2-ium-1-il)fenil)akrilata.
16. Farmaceutski pripravak prema zahtjevu 15, naznačen time da pripravak dodatno sadrži antioksidans i proizvoljno dodatno sadrži sredstvo za keliranje metala.
HRP20171961TT 2013-05-28 2014-05-27 Kemijski spojevi HRP20171961T1 (hr)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201361827951P 2013-05-28 2013-05-28
US201361915685P 2013-12-13 2013-12-13
PCT/GB2014/051607 WO2014191726A1 (en) 2013-05-28 2014-05-27 Chemical compounds
EP14727036.7A EP3004090B1 (en) 2013-05-28 2014-05-27 Chemical compounds

Publications (1)

Publication Number Publication Date
HRP20171961T1 true HRP20171961T1 (hr) 2018-02-09

Family

ID=50841880

Family Applications (1)

Application Number Title Priority Date Filing Date
HRP20171961TT HRP20171961T1 (hr) 2013-05-28 2014-05-27 Kemijski spojevi

Country Status (35)

Country Link
US (4) US9155727B2 (hr)
EP (2) EP3360875A1 (hr)
JP (1) JP6286031B2 (hr)
KR (1) KR20160013198A (hr)
CN (1) CN105229004B (hr)
AP (1) AP2015008858A0 (hr)
AU (1) AU2014272856B2 (hr)
BR (1) BR112015029455A8 (hr)
CA (1) CA2911859A1 (hr)
CL (1) CL2015003491A1 (hr)
CR (1) CR20150629A (hr)
CY (1) CY1120474T1 (hr)
DK (1) DK3004090T3 (hr)
DO (1) DOP2015000274A (hr)
ES (1) ES2654161T3 (hr)
HR (1) HRP20171961T1 (hr)
HU (1) HUE035738T2 (hr)
IL (1) IL242559B (hr)
LT (1) LT3004090T (hr)
ME (1) ME02892B (hr)
MX (1) MX361538B (hr)
NI (1) NI201500167A (hr)
PE (1) PE20160874A1 (hr)
PH (1) PH12015502615A1 (hr)
PL (1) PL3004090T3 (hr)
PT (1) PT3004090T (hr)
RS (1) RS56678B1 (hr)
RU (1) RU2664109C2 (hr)
SG (1) SG11201509393VA (hr)
SI (1) SI3004090T1 (hr)
SM (1) SMT201700589T1 (hr)
TN (1) TN2015000516A1 (hr)
TW (1) TWI653235B (hr)
UY (1) UY35590A (hr)
WO (1) WO2014191726A1 (hr)

Families Citing this family (95)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR101939710B1 (ko) 2011-12-21 2019-01-17 노비라 테라퓨틱스, 인코포레이티드 B형 간염의 항바이러스성 제제
UY34993A (es) 2012-08-28 2014-02-28 Janssen R & D Ireland Sulfamoilarilamidas y su uso como medicamentos para el tratamiento de la hepatitis b
WO2014131847A1 (en) 2013-02-28 2014-09-04 Janssen R&D Ireland Sulfamoyl-arylamides and the use thereof as medicaments for the treatment of hepatitis b
JP6419155B2 (ja) 2013-04-03 2018-11-07 ヤンセン・サイエンシズ・アイルランド・ユーシー Ｎ−フェニル−カルボキサミド誘導体およびｂ型肝炎を治療するための医薬品としてのその使用
JO3583B1 (ar) 2013-05-17 2020-07-05 Janssen Sciences Ireland Uc مشتقات سلفامويل بيرولاميد واستخدامها كادوية لمعالجة التهاب الكبد نوع بي
HRP20181863T1 (hr) 2013-05-17 2018-12-28 Janssen Sciences Ireland Uc Derivati sulfamoiltiofenamida i njihova uporaba kao lijekova za liječenje hepatitisa b
NO3024819T3 (hr) 2013-07-25 2018-07-21
MX368158B (es) 2013-10-23 2019-09-20 Janssen Sciences Ireland Uc Derivados de carboxamida y su uso como medicamentos para el tratamiento de la hepatitis b.
US10392349B2 (en) 2014-01-16 2019-08-27 Novira Therapeutics, Inc. Azepane derivatives and methods of treating hepatitis B infections
US9169212B2 (en) 2014-01-16 2015-10-27 Novira Therapeutics, Inc. Azepane derivatives and methods of treating hepatitis B infections
WO2015120178A1 (en) 2014-02-05 2015-08-13 Novira Therapeutics, Inc. Combination therapy for treatment of hbv infections
DK3102572T3 (en) 2014-02-06 2019-02-04 Janssen Sciences Ireland Uc SULFAMOYLPYRROLAMIDE DERIVATIVES AND THEIR USE AS MEDICINES TO TREAT HEPATITIS B
CN117865872A (zh) 2014-12-18 2024-04-12 豪夫迈·罗氏有限公司 四氢-吡啶并[3,4-b]吲哚雌激素受体调节剂及其用途
WO2016146591A1 (en) * 2015-03-16 2016-09-22 Astrazeneca Ab Combination treatment
HK1247147A1 (zh) 2015-03-19 2018-09-21 诺维拉治疗公司 氮杂环辛烷和氮杂环壬烷衍生物以及治疗乙型肝炎感染的方法
KR20180012853A (ko) 2015-06-16 2018-02-06 지앙수 헨그루이 메디슨 컴퍼니 리미티드 피페리딘 유도체 및 이의 제조 방법 및 약학적 용도
US10875876B2 (en) 2015-07-02 2020-12-29 Janssen Sciences Ireland Uc Cyclized sulfamoylarylamide derivatives and the use thereof as medicaments for the treatment of hepatitis B
AU2016301196B2 (en) 2015-08-06 2022-09-08 Dana-Farber Cancer Institute, Inc. Tunable endogenous protein degradation
CN108430971A (zh) 2015-09-29 2018-08-21 诺维拉治疗公司 乙型肝炎抗病毒剂的晶体形式
DK3355884T3 (da) 2015-10-01 2021-08-02 Olema Pharmaceuticals Inc Tetrahydro-1h-pyrido[3,4-b]indol-antiøstrogenlægemidler
CA3011391C (en) 2015-11-12 2021-02-09 Zhejiang Hisun Pharmaceutical Co., Ltd. Acrylic acid derivative, preparation method and use in medicine thereof
ES2935125T3 (es) 2015-12-09 2023-03-01 Univ Illinois Reguladores a la baja selectivos de los receptores de estrógenos con base en benzotiofeno
HK1244808A1 (zh) 2015-12-22 2018-08-17 江苏恒瑞医药股份有限公司 苯并哌啶类衍生物、其制备方法及其在医药上的应用
KR102479822B1 (ko) 2016-02-05 2022-12-21 인벤티스바이오 엘엘씨 선택적 에스트로겐 수용체 분해제 및 이들의 용도
US20190142811A1 (en) * 2016-04-01 2019-05-16 Zeno Royalties & Milestones, LLC Estrogen receptor modulators
KR20180129943A (ko) 2016-04-15 2018-12-05 노비라 테라퓨틱스, 인코포레이티드 캡시드 조립 억제제를 포함하는 배합물 및 방법
US10125135B2 (en) 2016-04-20 2018-11-13 Astrazeneca Ab Chemical compounds
CA3022377A1 (en) 2016-04-29 2017-11-02 Board Of Regents, The University Of Texas System Targeted measure of transcriptional activity related to hormone receptors
WO2017197904A2 (zh) * 2016-05-08 2017-11-23 上海诚妙医药科技有限公司 帕布昔利布的新晶型及其制备方法及其用途
CN109562107A (zh) 2016-05-10 2019-04-02 C4医药公司 用于靶蛋白降解的杂环降解决定子体
EP3455219A4 (en) 2016-05-10 2019-12-18 C4 Therapeutics, Inc. AMINE-RELATED C3-GLUTARIMIDE DEGRONIMERS FOR TARGET PROTEIN REDUCTION
EP4483875A3 (en) 2016-05-10 2025-04-02 C4 Therapeutics, Inc. Spirocyclic degronimers for target protein degradation
CN109641874A (zh) 2016-05-10 2019-04-16 C4医药公司 用于靶蛋白降解的c3-碳连接的戊二酰亚胺降解决定子体
US20170362228A1 (en) 2016-06-16 2017-12-21 Genentech, Inc. TETRAHYDRO-PYRIDO[3,4-b]INDOLE ESTROGEN RECEPTOR MODULATORS AND USES THEREOF
WO2017216279A1 (en) * 2016-06-16 2017-12-21 F. Hoffmann-La Roche Ag Heteroaryl estrogen receptor modulators and uses thereof
CN109415361B (zh) * 2016-06-29 2022-03-08 浙江海正药业股份有限公司 丙烯酸类衍生物及其制备方法和其在医药上的用途
BR112018077136A2 (pt) 2016-07-01 2019-04-30 G1 Therapeutics, Inc. composto, e, métodos para tratar um distúrbio associado com proliferação celular anormal e para reduzir o efeito de quimioterapia em células saudáveis.
US10149839B2 (en) 2016-07-25 2018-12-11 Astrazeneca Ab Chemical compounds
CN107814798B (zh) * 2016-09-14 2020-11-03 四川科伦博泰生物医药股份有限公司 3-取代丙烯酸类化合物及其制备方法和用途
EP3522933B1 (en) 2016-10-05 2021-12-15 F. Hoffmann-La Roche AG Methods for preparing antibody drug conjugates
WO2018081168A2 (en) 2016-10-24 2018-05-03 The Board Of Trustees Of The University Of Illinois Benzothiophene-based selective mixed estrogen receptor downregulators
JOP20190090B1 (ar) 2016-10-24 2023-03-28 Astrazeneca Ab مشتقات 9،8،7،6-رابع هيدرو-3h-بيرازولو [4،3-f]أيزوكينولين مفيدة في علاج السرطان
AR110728A1 (es) 2017-01-06 2019-04-24 G1 Therapeutics Inc Terapia combinada para el tratamiento del cáncer
WO2018130123A1 (zh) * 2017-01-11 2018-07-19 南京圣和药业股份有限公司 作为选择性雌激素受体下调剂的五环类化合物及其应用
WO2018130124A1 (zh) * 2017-01-11 2018-07-19 南京圣和药业股份有限公司 作为选择性雌激素受体下调剂的三环类化合物及其应用
EP3689873B1 (en) * 2017-01-30 2022-09-14 Astrazeneca AB Estrogen receptor modulators
EP3580212A4 (en) 2017-02-08 2021-03-17 Dana Farber Cancer Institute, Inc. REGULATION OF CHEMERIC ANTIGEN RECEPTORS
TW201835064A (zh) 2017-02-10 2018-10-01 美商G1治療公司 苯并噻吩雌激素受體調節劑
CN108864080B (zh) * 2017-05-09 2021-10-15 南京圣和药业股份有限公司 作为选择性雌激素受体下调剂的四环类化合物及其应用
EP3641762B1 (en) 2017-06-20 2026-02-18 C4 Therapeutics, Inc. N/o-linked degrons and degronimers for protein degradation
CN110536888B (zh) * 2017-06-20 2022-07-26 江苏恒瑞医药股份有限公司 一种苯并哌啶类衍生物的盐、其晶型及盐、其晶型的制备方法
CA3067873A1 (en) 2017-06-29 2019-01-03 G1 Therapeutics, Inc. Morphic forms of g1t38 and methods of manufacture thereof
KR20200086278A (ko) 2017-10-18 2020-07-16 노파르티스 아게 선택적 단백질 분해를 위한 조성물 및 방법
EA038160B1 (ru) * 2017-11-30 2021-07-15 Астразенека Аб Модуляторы рецептора эстрогена
CN109867659A (zh) * 2017-12-04 2019-06-11 江苏恒瑞医药股份有限公司 苯并哌啶类衍生物的制备方法
US10519152B2 (en) * 2017-12-21 2019-12-31 Astrazeneca Ab Compounds and their use in treating cancer
EP3755683A1 (en) * 2018-02-23 2020-12-30 Center for Intelligent Research in Crystal Engineering, S.L. Cocrystals of ubiquinol and compositions comprising them
JP2021515769A (ja) 2018-03-14 2021-06-24 ヤンセン・サイエンシズ・アイルランド・アンリミテッド・カンパニー カプシド集合調節剤の投薬レジメン
SG11202011135WA (en) 2018-05-14 2020-12-30 Nuvation Bio Inc Anti-cancer nuclear hormone receptor-targeting compounds
WO2019228443A1 (en) * 2018-05-30 2019-12-05 Dizal (Jiangsu) Pharmaceutical Co., Ltd. Selective estrogen receptor downregulators and uses thereof
TWI915239B (zh) 2018-06-21 2026-02-11 瑞士商赫孚孟拉羅股份公司 3-((1r,3r)-1-(2,6-二氟-4-((1-(3-氟丙基)氮雜環丁-3-基)胺基)苯基)-3-甲基-1,3,4,9-四氫-2h-吡啶并[3,4-b]吲哚-2-基)-2,2-二氟丙-1-醇之固體形式及用於製備包含經取代苯基或吡啶基部分之稠合三環化合物之製程，包括其使用方法
MA53105A (fr) 2018-07-03 2021-05-12 Univ Illinois Activateurs de la réponse à une protéine non dépliée
CN120698983A (zh) 2018-12-20 2025-09-26 C4医药公司 靶向蛋白降解
CN113164467B (zh) * 2018-12-24 2023-12-26 益方生物科技(上海)股份有限公司 选择性雌激素受体降解剂的新型盐
US11096931B2 (en) 2019-02-22 2021-08-24 Janssen Sciences Ireland Unlimited Company Amide derivatives useful in the treatment of HBV infection or HBV-induced diseases
EP3959320A1 (en) 2019-04-24 2022-03-02 Novartis AG Compositions and methods for selective protein degradation
US11491148B2 (en) 2019-05-06 2022-11-08 Janssen Sciences Ireland Unlimited Company Amide derivatives useful in the treatment of HBV infection or HBV-induced diseases
US11826430B2 (en) * 2019-05-14 2023-11-28 Nuvation Bio Inc. Anti-cancer nuclear hormone receptor-targeting compounds
CA3144791A1 (en) 2019-07-07 2021-01-14 Olema Pharmaceuticals, Inc. Regimens of estrogen receptor antagonists
EP3993787A4 (en) 2019-08-06 2023-07-12 Recurium IP Holdings, LLC Estrogen receptor modulators for treating mutants
US20220389006A1 (en) * 2019-11-04 2022-12-08 Recurium Ip Holdings, Llc Salts and forms of an estrogen receptor modulator
US11952349B2 (en) 2019-11-13 2024-04-09 Nuvation Bio Inc. Anti-cancer nuclear hormone receptor-targeting compounds
EP4681715A3 (en) 2019-12-20 2026-01-28 C4 Therapeutics, Inc. Isoindolinone and indazole compounds for the degradation of egfr
MX2022008091A (es) 2020-01-10 2022-07-11 Jiangsu Hengrui Medicine Co Derivado de tetrahidroisoquinolina triciclica, metodo de preparacion del mismo y aplicacion del mismo en medicina.
IL295709A (en) 2020-03-05 2022-10-01 C4 Therapeutics Inc Compounds for targeted degradation of brd9
MX2022010425A (es) 2020-03-06 2022-09-07 Olema Pharmaceuticals Inc Metodos de tratamiento de enfermedades asociadas a los receptores de estrogenos.
JP7712955B2 (ja) 2020-04-24 2025-07-24 アストラゼネカ・アクチエボラーグ 癌の治療のための投薬レジメン
MX2022013258A (es) 2020-04-24 2022-11-14 Astrazeneca Ab Formulaciones farmaceuticas.
WO2021253380A1 (en) * 2020-06-19 2021-12-23 InventisBio Co., Ltd. Oral formulations and uses thereof
WO2022029799A1 (en) * 2020-08-05 2022-02-10 Aizant Drug Research Solutions Private Limited Solid dosage forms of palbociclib
EP4192458A4 (en) 2020-08-05 2024-09-04 C4 Therapeutics, Inc. COMPOUNDS FOR TARGETED DEGRADATION OF RET
WO2022109395A2 (en) 2020-11-23 2022-05-27 Sanofi Panel of er regulated genes for use in monitoring endocrine therapy in breast cancer
JP2024502270A (ja) * 2020-12-23 2024-01-18 リキュリウム アイピー ホールディングス リミテッド ライアビリティー カンパニー エストロゲン受容体調節薬
KR20230160299A (ko) 2021-03-23 2023-11-23 누베이션 바이오 인크. 항암 핵 호르몬 수용체 표적화 화합물
US12006314B2 (en) 2021-05-03 2024-06-11 Nuvation Bio Inc. Anti-cancer nuclear hormone receptor-targeting compounds
JP2024523839A (ja) 2021-06-08 2024-07-02 シーフォー セラピューティクス， インコーポレイテッド 突然変異体ｂｒａｆを分解する療法薬
IL309986A (en) * 2021-07-08 2024-03-01 Olema Pharmaceuticals Inc Methods of treating estrogen receptor-associated diseases
EP4368624A4 (en) 2021-07-09 2024-12-18 Jiangsu Hengrui Pharmaceuticals Co., Ltd. SALT TYPES OF A TRICYCLIC TETRAHYDROISOQUINOLINE DERIVATIVE
WO2023221123A1 (en) * 2022-05-20 2023-11-23 Olema Pharmaceuticals, Inc. Crystalline forms of an estrogen receptor antagonist
KR20250055538A (ko) 2022-08-03 2025-04-24 브리스톨-마이어스 스큅 컴퍼니 Ret 단백질을 조정하기 위한 화합물
CN120569388A (zh) 2022-11-04 2025-08-29 百时美施贵宝公司 Ret-ldd蛋白降解剂
JP2025540906A (ja) 2022-11-04 2025-12-17 ブリストル－マイヤーズ スクイブ カンパニー Ｒｅｔ－ｌｄｄタンパク質阻害剤
KR20240170460A (ko) * 2023-05-25 2024-12-03 주식회사 삼양홀딩스 팔보시클립의 경구용 조성물
AU2024310341A1 (en) 2023-06-30 2026-02-12 Merck Patent Gmbh Heterobifunctional compounds for the degradation of kras protein
US12558428B2 (en) 2024-03-08 2026-02-24 Halda Therapeutics Opco, Inc. Heterobifunctional compounds and their use in treating disease

Family Cites Families (39)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4683202A (en) 1985-03-28 1987-07-28 Cetus Corporation Process for amplifying nucleic acid sequences
US4683195A (en) 1986-01-30 1987-07-28 Cetus Corporation Process for amplifying, detecting, and/or-cloning nucleic acid sequences
JP2000509373A (ja) 1996-04-19 2000-07-25 ノボ ノルディスク アクティーゼルスカブ ホスホチロシン認識ユニットを有する分子のモジュレーター
FR2778404B1 (fr) * 1998-05-06 2000-06-30 Hoechst Marion Roussel Inc Derives du dihydro ou tetrahydronaphtalene, et les compositions pharmaceutiques les renfermant
GB9814414D0 (en) 1998-07-03 1998-09-02 Celltech Therapeutics Ltd Chemical compounds
IL145922A0 (en) 1999-04-28 2002-07-25 Aventis Pharma Gmbh Di-aryl acid derivatives as ppar receptor ligands
FR2796644B1 (fr) * 1999-07-23 2001-09-07 Adir Nouveaux derives de beta-carboline, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
MEP28108A (en) * 2000-03-15 2010-10-10 Sanofi Aventis Deutschland Substituted beta-carbolines with ikb-kinase inhibiting activity
US6720331B2 (en) 2001-04-03 2004-04-13 National Sun Yat-Sen University 1-substituted 1,2,3,4-tetrahydro-β-carboline and 3,4-dihydro-β-carboline and analogs as antitumor agents
JP2005516967A (ja) 2002-01-18 2005-06-09 ザ ジェネティクス カンパニー インコーポレーティッド β−セクレターゼインヒビター
AU2003231032B2 (en) 2002-04-22 2008-07-10 Johns Hopkins University School Of Medicine Modulators of hedgehog signaling pathways, compositions and uses related thereto
TWI329111B (en) 2002-05-24 2010-08-21 X Ceptor Therapeutics Inc Azepinoindole and pyridoindole derivatives as pharmaceutical agents
US20050004164A1 (en) 2003-04-30 2005-01-06 Caggiano Thomas J. 2-Cyanopropanoic acid amide and ester derivatives and methods of their use
WO2004113300A1 (ja) 2003-06-23 2004-12-29 Ono Pharmaceutical Co., Ltd. 新規三環性複素環化合物
MXPA06001094A (es) * 2003-07-28 2006-04-11 Smithkline Beecham Corp Compuestos quimicos.
DE10335725A1 (de) 2003-08-05 2005-03-03 Bayer Cropscience Gmbh Safener auf Basis aromatisch-aliphatischer Carbonsäuredarivate
US7855295B2 (en) * 2004-01-23 2010-12-21 Novartis Vaccines And Diagnostics, Inc. Tetrahydrocarboline compounds as anticancer agents
US7714132B2 (en) * 2004-03-11 2010-05-11 Actelion Pharmaceuticals, Ltd. Tetrahydropyridoindole derivatives
US8076352B2 (en) 2004-03-15 2011-12-13 Ptc Therapeutics, Inc. Administration of carboline derivatives useful in the treatment of cancer and other diseases
GB0422057D0 (en) 2004-10-05 2004-11-03 Astrazeneca Ab Novel compounds
EP1805159A1 (en) 2004-10-28 2007-07-11 The Institutes for Pharmaceutical Discovery, LLC Substituted carboxylic acids
CA2587566A1 (en) 2004-11-18 2006-05-26 The Institutes For Pharmaceutical Discovery, Llc Heterocyclylbiphenyl derivates as protein tyrosine phosphatase inhibitors
CA2596015A1 (en) 2005-02-14 2006-08-24 Sampath K. Anandan Fused heterocyclic compounds useful as inhibitors of histone deacetylase
WO2006101434A1 (en) * 2005-03-22 2006-09-28 Astrazeneca Ab NOVEL TETRAHYDRO-1H-PYRIDO [4,3-b] INDOLE DERIVATIVES AS CB1’ RECEPTOR LIGANDS
US20070032385A1 (en) 2005-06-20 2007-02-08 Dunetz Joshua R Sustainable chemical processes
AU2007249827A1 (en) 2006-05-09 2007-11-22 Colorado State University Research Foundation Methods for treating blood disorders
PT2057156T (pt) 2006-08-23 2017-05-04 Kudos Pharm Ltd Derivados de 2-metilmorfolina pirido-, pirazo- e pirimidopirimidina como inibidores de mtor
WO2008025965A2 (en) 2006-08-29 2008-03-06 Reinnervate Limited Retinoid compounds and their use
US20100249234A1 (en) 2007-04-10 2010-09-30 Uwm Research Foundation, Inc. Methods of reducing virulence in bacteria
WO2008124838A1 (en) 2007-04-10 2008-10-16 University Of Maryland, Baltimore Compounds that inhibit human dna ligases and methods of treating cancer
AU2008239598A1 (en) 2007-04-13 2008-10-23 Ptc Therapeutics, Inc. Administration of carboline derivatives useful in the treatment of cancer and other diseases
JP2010533712A (ja) 2007-07-19 2010-10-28 メルク・シャープ・エンド・ドーム・コーポレイション 抗糖尿病化合物としてのベータカルボリン誘導体
US8198292B2 (en) 2008-07-03 2012-06-12 Osteogenex, Inc. Vinpocetine and eburnamonine derivatives for promoting bone growth, treating renal damage and cancer, and devices thereof
TW201028414A (en) 2009-01-16 2010-08-01 Merck Sharp & Dohme Oxadiazole beta carboline derivatives as antidiabetic compounds
WO2010107485A1 (en) 2009-03-17 2010-09-23 The Trustees Of Columbia University In The City Of New York E3 ligase inhibitors
HUE052510T2 (hu) * 2009-05-27 2021-05-28 Ptc Therapeutics Inc Módszerek a rák és a nem daganatos állapotok kezelésére
WO2010138706A1 (en) 2009-05-27 2010-12-02 Ptc Therapeutics, Inc. Methods for treating breast cancer
WO2012112961A1 (en) 2011-02-18 2012-08-23 Medivation Technologies, Inc. Compounds and methods of treating hypertension
WO2013022740A2 (en) 2011-08-05 2013-02-14 Corning Incorporated Gpr35 ligands and the uses thereof

Also Published As

Publication number Publication date
CL2015003491A1 (es) 2016-06-03
CN105229004A (zh) 2016-01-06
PH12015502615B1 (en) 2016-02-29
RU2015151502A (ru) 2017-07-04
ES2654161T3 (es) 2018-02-12
PT3004090T (pt) 2017-12-22
TN2015000516A1 (en) 2017-04-06
US20190038607A1 (en) 2019-02-07
US9155727B2 (en) 2015-10-13
HK1222859A1 (en) 2017-07-14
US9616050B2 (en) 2017-04-11
TWI653235B (zh) 2019-03-11
EP3004090A1 (en) 2016-04-13
LT3004090T (lt) 2018-01-10
SG11201509393VA (en) 2015-12-30
SI3004090T1 (en) 2018-01-31
BR112015029455A8 (pt) 2020-03-17
SMT201700589T1 (it) 2018-03-08
AP2015008858A0 (en) 2015-11-30
US20170326115A1 (en) 2017-11-16
DOP2015000274A (es) 2015-12-31
MX2015016428A (es) 2016-03-03
HUE035738T2 (en) 2018-05-28
RU2664109C2 (ru) 2018-08-15
IL242559B (en) 2018-11-29
PE20160874A1 (es) 2016-09-04
DK3004090T3 (en) 2018-01-08
AU2014272856A1 (en) 2015-11-26
JP2016522835A (ja) 2016-08-04
WO2014191726A1 (en) 2014-12-04
PH12015502615A1 (en) 2016-02-29
BR112015029455A2 (pt) 2017-07-25
CY1120474T1 (el) 2019-07-10
CA2911859A1 (en) 2014-12-04
EP3004090B1 (en) 2017-10-25
JP6286031B2 (ja) 2018-02-28
KR20160013198A (ko) 2016-02-03
ME02892B (me) 2018-04-20
RS56678B1 (sr) 2018-03-30
NI201500167A (es) 2018-10-18
US20140357661A1 (en) 2014-12-04
TW201536779A (zh) 2015-10-01
UY35590A (es) 2014-11-28
PL3004090T3 (pl) 2018-02-28
RU2015151502A3 (hr) 2018-03-23
CR20150629A (es) 2016-04-05
US20160136140A1 (en) 2016-05-19
US10130617B2 (en) 2018-11-20
MX361538B (es) 2018-12-10
AU2014272856B2 (en) 2017-08-17
EP3360875A1 (en) 2018-08-15
CN105229004B (zh) 2017-05-03

Similar Documents

Publication Publication Date Title
ME02892B (me) Hemijska jedinjenja
JP2016522835A5 (hr)
ME02729B (me) Indolski i indazolski spojevi koji aktiviraju ampk
ME02838B (me) 3,4-dihidroizokinolin-2(1h)-ilni spojevi
MY173946A (en) (6s,9as)-n-benzyl-6-[(4-hydroxyphenyl)methyl]-4,7-dioxo-8-({6-[3-(piperazin-1-yl) azetidin-1-yl]pyridin-2-yl}methyl)-2-(prop-2-en-1-yl)-octahydro-1h-pyrazino[2,1-c] [1,2,4]triazine-1-carboxamide compound
ME02452B (me) Sredstva za induciranje apoptoze namijenjena liječenju raka i imunih i autoimunih bolesti
HRP20201043T1 (hr) Spojevi 4-amino-imidazokinolina
CA2826751C (en) Processes for preparing quinoline compounds and pharmaceutical compositions containing such compounds
JP2015078230A5 (hr)
JP2013032389A5 (hr)
PH12015501585A1 (en) Manufacturing process for pyrimidine derivatives
NZ716840A (en) Combination formulation of two antiviral compounds
PH12016500169A1 (en) Polymorph of syk inhibitors
JP2011105738A5 (hr)
SG11201709593VA (en) CRYSTAL OF (6S,9aS)-N-BENZYL-6-[(4-HYDROXYPHENYL)METHYL]- 4,7-DIOXO-8-({6-[3-(PIPERAZIN-1-YL)AZETIDIN-1-YL]PYRIDIN- 2-YL}METHYL)-2-(PROP-2-EN-1-YL)-OCTAHYDRO-1H-PYRAZINO[2,1-c][1,2,4]TRIAZINE-1-CARBOXAMIDE COMPOUND
JP2016518317A5 (hr)
PH12015502802A1 (en) Formulation comprising a hypolipidemic agent
HRP20241103T1 (hr) 2,4-di-(skupina koja sadrži dušik)-supstituirani pirimidinski spoj i postupak pripreme i njegova upotreba
SMT201700142T1 (it) SALE DI CAMSILATO DI (1r, 1’R, 4R)-4-METOSSI-5’’-METIL-6’-[5-(PROP-1-IN-1-IL)PIRIDIN-3-IL]-3’H-DISPIRO[CICLOESANO-1,2’-INDEN-1’2’-IMIDAZOLO]-4’’-AMMINA E SUE FORME CRISTALLINE PER IL TRATTAMENTO DI PATOLOGIE A[BETA]-CORRELATE COME PER ESEMPIO LA MALATTIA DI ALZHEIMER
JP2016532632A5 (hr)
CA2922375C (en) Alpha-tea salt forms: compositions and uses for treating disease
HRP20250183T1 (hr) Hidrokloridna sol 1,5 hidrata heterocikličkog spoja kao derivata
AR081034A1 (es) Derivados de n-heteroaril tetrahidro-isoquinolina sustituidos, composiciones farmaceuticas que los contienen y uso de los mismos para el tratamiento de enfermedades del sistema nervioso central
SI3083605T1 (en) COMPOUNDS OF FLUOROFENYL PIRAZOLE
JP2013522207A5 (hr)