ES2168237T1 - Pirazolopirimidinas que actuan como antagonistas del receptor del crf. - Google Patents

Pirazolopirimidinas que actuan como antagonistas del receptor del crf.

Info

Publication number
ES2168237T1
ES2168237T1 ES97902295T ES97902295T ES2168237T1 ES 2168237 T1 ES2168237 T1 ES 2168237T1 ES 97902295 T ES97902295 T ES 97902295T ES 97902295 T ES97902295 T ES 97902295T ES 2168237 T1 ES2168237 T1 ES 2168237T1
Authority
ES
Spain
Prior art keywords
rent
crf
formula
hydroxial
cyclealkyl
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.)
Granted
Application number
ES97902295T
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English (en)
Other versions
ES2168237T3 (es
Inventor
Chen-Neurocrine Bioscienc Chen
Thomas R-Neurocrine Biosc Webb
James R-Neurocrine Bi Mccarthy
Terence J-Neurocrine Bio Moran
Keith M-Neurocrine Bi Wilcoxen
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.)
Janssen Pharmaceutica NV
Neurocrine Biosciences Inc
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Janssen Pharmaceutica NV
Neurocrine Biosciences Inc
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Application filed by Janssen Pharmaceutica NV, Neurocrine Biosciences Inc filed Critical Janssen Pharmaceutica NV
Publication of ES2168237T1 publication Critical patent/ES2168237T1/es
Application granted granted Critical
Publication of ES2168237T3 publication Critical patent/ES2168237T3/es
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

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    • 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
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    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/12—Antidiarrhoeals
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P11/00—Drugs for disorders of the respiratory system
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    • A61P13/00—Drugs for disorders of the urinary system
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    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
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    • A61P25/32—Alcohol-abuse
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    • A61P5/00—Drugs for disorders of the endocrine system
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    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • 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
    • C07D471/10—Spiro-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Immunology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Pulmonology (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Diabetes (AREA)
  • Addiction (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Rheumatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Transplantation (AREA)
  • Endocrinology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Nutrition Science (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

ESTA INVENCION SE REFIERE A COMPUESTOS DE FORMULA (I), INCLUIDOS ESTEREOISOMEROS Y LAS FORMAS DE SALES DE ADICION ACIDAS FARMACEUTICAMENTE ACEPTABLES DE LOS MISMOS, EN LA QUE R 1 ES NR 4 R 5 U OR 5 ; R 2 ES ALQUILO C 1-6 , ALQUILOXI C 1-6 O ALQUILTIO C 1-6 ; R 3 ES HIDROGENO, ALQUILO C 1-6 , ALQUILSULFONILO C 1-6 , ALQUILSULFOXI C 1-6 O ALQUILTIO C 1-6 ; R 4 ES HIDR OGENO, ALQUILO C 1-6 , MONO - O DI(CICLOALQUIL C 36 ) METILO, CICLOALQUILO C 3-6 , ALQUENILO C 3-6 , HIDROXIALQUILO C 3-6 , ALQUILCARBONILOXI C 1-6 ALQUILO C SUB ,1-6 O ALQUILOXI C 1-6 ALQUILO C 1-6 ; R 5 ES ALQUILO C 1-8 , MONO - O DI(CICLOALQUIL C 3-6 )METILO, AR 1 CH 2 , ALQUILOXI C 1-6 ALQUILO C 1-6 , HIDROXIALQUILO C 1-6 , ALQUENILO C 3-6 , TIENILMETILO, FURANILMETILO, ALQUILTIO C 1-6 ALQUILO C 1-6 , MORFOLINILO, MONO - O DI(ALQUIL C 1-6 )AMINOALQUILO C 16 , D I(ALQUIL C 1-6 )AMINO, ALQUILCARBONIL C 1-6 ALQUILO C1-6 , ALQUILO C 1-6 SUSTITUIDO CON IMIDAZOLILO; O UN RADICAL DE LA FORMULA - ALK - O - CO - AR 1 ; O R 4 O R 5 TOMADOS JUNTO CON EL ATOMO DE NITROGENO AL QUE ESTAN UNIDOS PUEDEN FORMAR UN GRUPO PIRROLIDINILO, PIPERIDINILO, HOMOPIPERIDINILO O MORFOLINILO OPCIONALMENTE SUSTITUIDO; QUE POSEEN PROPIEDADES ANTAGONISTICAS AL RECEPTOR DEL CRF; A COMPOSICIONES FARMACEUTICAS QUE CONTIENEN TALES COMPUESTOS COMO INGREDIENTES ACTIVOS; METODO PARA EL TRATAMIENTO DE TRASTORNOS RELACIONADOS CON LA HIPERSECRECION DE CRF TALES COMO LA DEPRESION, ANSIEDAD, ABUSO DE SUSTANCIAS, MEDIANTE LA ADMINISTRACION DE UNA CANTIDAD EFECTIVA DE UN COMPUESTO DE FORMULA (I).
ES97902295T 1996-02-07 1997-01-30 Pirazolopirimidinas como antagonistas de receptores de crf. Expired - Lifetime ES2168237T3 (es)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US1127996P 1996-02-07 1996-02-07
US11279 1996-02-07
US2768896P 1996-10-08 1996-10-08
US27688 1996-10-08

Publications (2)

Publication Number Publication Date
ES2168237T1 true ES2168237T1 (es) 2002-06-16
ES2168237T3 ES2168237T3 (es) 2007-04-01

Family

ID=26682204

Family Applications (1)

Application Number Title Priority Date Filing Date
ES97902295T Expired - Lifetime ES2168237T3 (es) 1996-02-07 1997-01-30 Pirazolopirimidinas como antagonistas de receptores de crf.

Country Status (27)

Country Link
EP (1) EP0880523B1 (es)
JP (2) JP3356291B2 (es)
KR (1) KR100421626B1 (es)
CN (1) CN1090189C (es)
AR (1) AR008577A1 (es)
AT (1) ATE336495T1 (es)
AU (1) AU713673B2 (es)
BG (1) BG102349A (es)
BR (1) BR9707391A (es)
CA (1) CA2233285C (es)
CZ (1) CZ244598A3 (es)
DE (2) DE880523T1 (es)
DK (1) DK0880523T3 (es)
EA (1) EA000803B1 (es)
EE (1) EE04282B1 (es)
ES (1) ES2168237T3 (es)
HU (1) HUP9900575A3 (es)
ID (1) ID15905A (es)
IL (1) IL123835A0 (es)
NO (1) NO310292B1 (es)
NZ (1) NZ330119A (es)
PL (1) PL191271B1 (es)
PT (1) PT880523E (es)
SK (1) SK106398A3 (es)
TR (1) TR199800792T2 (es)
TW (1) TW449599B (es)
WO (1) WO1997029109A1 (es)

Families Citing this family (70)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6060478A (en) * 1996-07-24 2000-05-09 Dupont Pharmaceuticals Azolo triazines and pyrimidines
US7094782B1 (en) 1996-07-24 2006-08-22 Bristol-Myers Squibb Company Azolo triazines and pyrimidines
HU229024B1 (en) * 1996-07-24 2013-07-29 Bristol Myers Squibb Pharma Co Azolo-pyridimidines, pharmaceutical compositions containing the same and use thereof
US6124289A (en) * 1996-07-24 2000-09-26 Dupont Pharmaceuticals Co. Azolo triazines and pyrimidines
US6191131B1 (en) 1997-07-23 2001-02-20 Dupont Pharmaceuticals Company Azolo triazines and pyrimidines
US6313124B1 (en) 1997-07-23 2001-11-06 Dupont Pharmaceuticals Company Tetrazine bicyclic compounds
EA003188B1 (ru) 1996-08-06 2003-02-27 Пфайзер Инк Замещенные пиридо- или пиримидосодержащие 6,6- или 6,7-бициклические производные
US5723608A (en) 1996-12-31 1998-03-03 Neurogen Corporation 3-aryl substituted pyrazolo 4,3-d!pyrimidine derivatives; corticotropin-releasing factor receptor (CRF1) specific ligands
CA2281525A1 (en) 1997-02-18 1998-08-20 Neurocrine Biosciences, Inc. Biazacyclic crf antagonists
AU734009B2 (en) * 1997-05-30 2001-05-31 Merck & Co., Inc. Novel angiogenesis inhibitors
US6235741B1 (en) * 1997-05-30 2001-05-22 Merck & Co., Inc. Angiogenesis inhibitors
NL1010018C2 (nl) 1997-09-09 1999-03-10 Duphar Int Res Chinoline en chinazoline derivaten met corticotropine releasing factor (CRF) antagonistische werking.
US6380203B1 (en) 1998-01-14 2002-04-30 Merck & Co., Inc. Angiogenesis inhibitors
EP1049699B1 (en) * 1998-01-28 2004-04-21 Bristol-Myers Squibb Pharma Company Pyrazolotriazines as crf antagonists
WO1999045007A1 (en) * 1998-03-06 1999-09-10 Janssen Pharmaceutica N.V. Crf antagonistic pyrazolo[4,3-b]pyridines
US6472402B1 (en) 1998-04-02 2002-10-29 Neurogen Corporation Aminoalkyl substituted 5,6,7,8-Tetrahydro-9H-Pyridino [2,3-B]indole derivatives
EP1068205A1 (en) 1998-04-02 2001-01-17 Neurogen Corporation Aminoalkyl substituted 5,6,7,8-tetrahydro-9h pyrimidino 2,3-b]indole and 5,6,7,8-tetrahydro-9h-pyrimidino 4,5-b]indole derivatives: crf1 specific ligands
EP1149835A4 (en) * 1999-01-29 2002-08-21 Sumitomo Chemical Co AGENTS FOR INHIBITATION OF FAT
WO2000059907A2 (en) 1999-04-06 2000-10-12 Du Pont Pharmaceuticals Company Pyrazolotriazines as crf antagonists
AU4203500A (en) 1999-04-06 2000-10-23 Du Pont Pharmaceuticals Company Pyrazolopyrimidines as crf antagonists
US6432989B1 (en) 1999-08-27 2002-08-13 Pfizer Inc Use of CRF antagonists to treat circadian rhythm disorders
JP2003510325A (ja) 1999-09-30 2003-03-18 ニューロジェン・コーポレーション ある種のアルキレンジアミン−置換ピラゾロ［１，５−ａ］−１，５−ピリミジン及びピラゾロ［１，５−ａ］−１，３，５−トリアジン
IL139197A0 (en) 1999-10-29 2001-11-25 Pfizer Prod Inc Use of corticotropin releasing factor antagonists and related compositions
TWI271406B (en) 1999-12-13 2007-01-21 Eisai Co Ltd Tricyclic condensed heterocyclic compounds, preparation method of the same and pharmaceuticals comprising the same
CA2398956A1 (en) * 2000-02-14 2001-08-16 Japan Tobacco Inc. A pharmaceutical composition for prophylaxis or therapy of a postoperative stress
HRP20030675A2 (en) * 2001-01-26 2004-08-31 Bristol Myers Squibb Co Imidazolyl derivatives as corticotropin relasing factor inhibitors
TWI312347B (en) 2001-02-08 2009-07-21 Eisai R&D Man Co Ltd Bicyclic nitrogen-containing condensed ring compounds
RU2308457C2 (ru) 2001-04-27 2007-10-20 Эйсай Ар Энд Ди Менеджмент Ко., Лтд. Пиразоло [1, 5-а] пиридины и содержащие их лекарственные средства
US6872827B2 (en) 2002-04-26 2005-03-29 Chembridge Research Laboratories, Inc. Somatostatin analogue compounds
US7161003B1 (en) * 2002-09-04 2007-01-09 Schering Corporation Pyrazolopyrimidines as cyclin dependent kinase inhibitors
TWI283679B (en) 2002-10-22 2007-07-11 Eisai Co Ltd 7-phenylpyrazolopyridine compounds
US7176216B2 (en) 2002-10-22 2007-02-13 Eisai Co., Ltd. 7-phenylpyrazolopyridine compounds
KR101078098B1 (ko) 2003-01-14 2011-10-28 아레나 파마슈티칼스, 인크. 대사 조절제로서의 １,２,３-삼치환된 아릴 및 헤테로아릴유도체, 및 당뇨병 및 고혈당증을 비롯한 이에 관련된장애의 예방 및 치료
EP1608652A1 (en) * 2003-03-31 2005-12-28 Vernalis (Cambridge) Limited Pyrazolopyrimidine compounds and their use in medicine
AR045047A1 (es) 2003-07-11 2005-10-12 Arena Pharm Inc Derivados arilo y heteroarilo trisustituidos como moduladores del metabolismo y de la profilaxis y tratamiento de desordenes relacionados con los mismos
AR045697A1 (es) 2003-07-14 2005-11-09 Arena Pharm Inc Aril y heteroaril derivados fusionados como moduladores del metabolismo y la prevencion y tratamiento de trastornos relacionados con el mismo
US7329662B2 (en) 2003-10-03 2008-02-12 Hoffmann-La Roche Inc. Pyrazolo-pyridine
AR046967A1 (es) 2003-12-22 2006-01-04 Sb Pharmco Inc Compuesto de pirazol[1,5-a]pirimidina, composicion farmaceutica que lo comprende y su uso para preparar dicha composicion
JP2007515474A (ja) * 2003-12-22 2007-06-14 エスビー・ファルムコ・プエルト・リコ・インコーポレイテッド Ｃｒｆ受容体アンタゴニストおよびそれらに関連する方法
JP2008503444A (ja) * 2004-02-13 2008-02-07 エスビー・ファルムコ・プエルト・リコ・インコーポレイテッド Ｃｒｆ受容体アンタゴニスト、その調製法、その医薬組成物およびその使用
GB0519957D0 (en) 2005-09-30 2005-11-09 Sb Pharmco Inc Chemical compound
CA2597608C (en) 2005-02-11 2013-12-24 F. Hoffmann-La Roche Ag Pyrazolo-pyrimidine derivatives as mglur2 antagonists
PL1869049T3 (pl) * 2005-03-21 2009-07-31 Lilly Co Eli Związki imidazopirydazyny
ATE460417T1 (de) 2005-03-23 2010-03-15 Hoffmann La Roche Acetylenylpyrazolopyrimidinderivate als mglur2- antagonsten
US7557103B2 (en) 2005-04-05 2009-07-07 Eli Lilly And Company Imidazopyridazine compounds
WO2007017678A1 (en) * 2005-08-09 2007-02-15 Eirx Therapeutics Limited Pyrazolo[1,5-a] pyrimidine compounds and pharmaceutical compositions containing them
ES2340321T3 (es) 2005-09-27 2010-06-01 F.Hoffmann-La Roche Ag Oxadiazolilpirazolo-pirimidinas, como antagonistas de mglur2.
MX2009003098A (es) 2006-09-20 2009-04-01 Lilly Co Eli Compuestos de tiofen pirazolopirimidina.
CA2663511C (en) * 2006-09-20 2012-12-04 Eli Lilly And Company Thiazole pyrazolopyrimidines as crf1 receptor antagonists
ATE522249T1 (de) 2007-07-26 2011-09-15 Novartis Ag Organische verbindungen
BRPI0911659B8 (pt) 2008-04-15 2021-05-25 Eisai R&D Man Co Ltd composto 3-fenilpirazolo[5,1-b]tiazol e composição farmacêutica compreendendo o mesmo
AR078521A1 (es) 2009-10-08 2011-11-16 Eisai R&D Man Co Ltd Compuesto pirazolotiazol
SG188548A1 (en) 2010-09-22 2013-04-30 Arena Pharm Inc Modulators of the gpr119 receptor and the treatment of disorders related thereto
GB201210686D0 (en) 2012-06-15 2012-08-01 Holsboermaschmeyer Neurochemie Gmbh V1B receptor antagonist for use in the treatment of patients having an elevated AVP level and/or an elevated copeptin level
GB201310782D0 (en) 2013-06-17 2013-07-31 Max Planck Innovation Gmbh Method for predicting a treatment response to a CRHR1 antagonist and/or V1B antagonist in a patient with depressive and/or anxiety symptoms
PL3242666T3 (pl) 2015-01-06 2025-02-17 Arena Pharmaceuticals, Inc. Związek do zastosowania w leczeniu dolegliwości związanych z receptorem s1p1
PL236355B1 (pl) * 2015-04-02 2021-01-11 Celon Pharma Spolka Akcyjna Pochodne 7-(morfolin-4-ylo)pirazolo[1,5-α]pirymidyny jako inhibitory kinazy PI3
HUE060476T2 (hu) 2015-06-22 2023-03-28 Arena Pharm Inc (R)-2-(7-(4-ciklopentil-3-(trifluormetil)benziloxi)-1,2,3,4- tetrahidrociklopenta[B]indol-3-il)ecetsav kristályos L-arginin-sója S1P1 receptorral kapcsolatos rendellenességek esetén való alkalmazásra
KR102598895B1 (ko) 2016-07-12 2023-11-07 레볼루션 메디슨즈, 인크. 다른자리 입체성 shp2 억제제로서의 2,5-이치환 3-메틸 피라진 및 2,5,6-3치환 3-메틸 피라진
JP7240319B2 (ja) 2017-01-23 2023-03-15 レヴォリューション・メディスンズ，インコーポレイテッド アロステリックｓｈｐ２阻害剤としての二環式化合物
KR20190110588A (ko) 2017-01-23 2019-09-30 레볼루션 메디슨즈, 인크. 알로스테릭 shp2 억제제로서의 피리딘 화합물
TW202400179A (zh) * 2017-08-14 2024-01-01 美商雲杉生物科技股份有限公司 促皮質素釋放因子受體拮抗劑
CN118845788A (zh) 2017-08-14 2024-10-29 云杉生物科学公司 促肾上腺皮质激素释放因子受体拮抗剂
WO2019051084A1 (en) 2017-09-07 2019-03-14 Revolution Medicines, Inc. SHP2 INHIBITOR COMPOSITIONS AND METHODS OF TREATING CANCER
MX2020003579A (es) 2017-10-12 2020-07-22 Revolution Medicines Inc Compuestos de piridina, pirazina, y triazina como inhibidores de shp2 alostericos.
TW201927791A (zh) 2017-12-15 2019-07-16 美商銳新醫藥公司 作為變構shp2抑制劑的多環化合物
MX2020011344A (es) 2018-04-27 2021-02-09 Spruce Biosciences Inc Métodos para tratar tumores en reposo suprarrenales testiculares y de ovarios.
US12156866B2 (en) 2018-06-06 2024-12-03 Arena Pharmaceuticals, Inc. Methods of treating conditions related to the S1P1 receptor
CN118948857A (zh) 2020-08-12 2024-11-15 云杉生物科学公司 用于治疗多囊卵巢综合征的方法和组合物
US11708372B2 (en) 2021-11-19 2023-07-25 Spruce Biosciences, Inc. Crystalline composition of tildacerfont and methods of use and preparation thereof

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS4211753Y1 (es) * 1964-06-06 1967-06-30
JPS6157587A (ja) * 1984-08-29 1986-03-24 Shionogi & Co Ltd 縮合複素環誘導体および抗潰瘍剤
JPH0211753A (ja) * 1988-06-29 1990-01-16 Raimuzu:Kk ＴｉＡｌ系複合部材及びその製造方法
TW444018B (en) * 1992-12-17 2001-07-01 Pfizer Pyrazolopyrimidines

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