CN102015685A - 作为hif-脯氨酰基-4-羟化酶抑制剂的取代的二氢吡唑啉酮类化合物 - Google Patents
作为hif-脯氨酰基-4-羟化酶抑制剂的取代的二氢吡唑啉酮类化合物 Download PDFInfo
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- CN102015685A CN102015685A CN2009801142929A CN200980114292A CN102015685A CN 102015685 A CN102015685 A CN 102015685A CN 2009801142929 A CN2009801142929 A CN 2009801142929A CN 200980114292 A CN200980114292 A CN 200980114292A CN 102015685 A CN102015685 A CN 102015685A
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- 0 *C1=C*(C(C(ON)=O)C(I=C)=O)*=*1 Chemical compound *C1=C*(C(C(ON)=O)C(I=C)=O)*=*1 0.000 description 6
- FUVCLFWTUQNXGH-XNTDXEJSSA-N CCC(C=C1)C=CN1/C(/C(OCC)=O)=C/CN(C)C=C Chemical compound CCC(C=C1)C=CN1/C(/C(OCC)=O)=C/CN(C)C=C FUVCLFWTUQNXGH-XNTDXEJSSA-N 0.000 description 1
- YDYBTRNQUBEIER-UHFFFAOYSA-N NNc1ncnc(N(C2)CC2O)c1 Chemical compound NNc1ncnc(N(C2)CC2O)c1 YDYBTRNQUBEIER-UHFFFAOYSA-N 0.000 description 1
- HIWAFEGEALLTAD-UHFFFAOYSA-N O=C1N(c2ncnc(N3CCOCCC3)c2)NC=C1[n]1nncc1 Chemical compound O=C1N(c2ncnc(N3CCOCCC3)c2)NC=C1[n]1nncc1 HIWAFEGEALLTAD-UHFFFAOYSA-N 0.000 description 1
- BWJUEGDHDDCCQY-UHFFFAOYSA-N Oc1ncnc(N2CCOCCC2)c1 Chemical compound Oc1ncnc(N2CCOCCC2)c1 BWJUEGDHDDCCQY-UHFFFAOYSA-N 0.000 description 1
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- C—CHEMISTRY; METALLURGY
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- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
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- A61P13/12—Drugs for disorders of the urinary system of the kidneys
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- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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- A—HUMAN NECESSITIES
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- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic 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
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Engineering & Computer Science (AREA)
- Veterinary Medicine (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Health & Medical Sciences (AREA)
- Diabetes (AREA)
- Cardiology (AREA)
- Biomedical Technology (AREA)
- Hematology (AREA)
- Heart & Thoracic Surgery (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Endocrinology (AREA)
- Urology & Nephrology (AREA)
- Virology (AREA)
- Rheumatology (AREA)
- Oncology (AREA)
- Immunology (AREA)
- Hospice & Palliative Care (AREA)
- Communicable Diseases (AREA)
- Obesity (AREA)
- Psychology (AREA)
- Dermatology (AREA)
- Molecular Biology (AREA)
- AIDS & HIV (AREA)
- Psychiatry (AREA)
- Emergency Medicine (AREA)
- Pain & Pain Management (AREA)
- Vascular Medicine (AREA)
- Ophthalmology & Optometry (AREA)
Abstract
Description
实施例编号 | IC50[nM] |
2 | 880 |
5 | 540 |
9 | 760 |
17 | 130 |
20 | 90 |
实施例编号 | IC50[nM] |
21 | 70 |
25 | 180 |
26 | 380 |
29 | 170 |
Claims (12)
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
DE102008020113.8 | 2008-04-23 | ||
DE102008020113A DE102008020113A1 (de) | 2008-04-23 | 2008-04-23 | Substituierte Dihydropyrazolone und ihre Verwendung |
PCT/EP2009/002693 WO2009129945A1 (de) | 2008-04-23 | 2009-04-11 | Substituierte dihydropyrazolone als hemmer der hif-prolyl-4-hydroxylase |
Publications (2)
Publication Number | Publication Date |
---|---|
CN102015685A true CN102015685A (zh) | 2011-04-13 |
CN102015685B CN102015685B (zh) | 2014-10-15 |
Family
ID=40673347
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CN200980114292.9A Expired - Fee Related CN102015685B (zh) | 2008-04-23 | 2009-04-11 | 作为hif-脯氨酰基-4-羟化酶抑制剂的取代的二氢吡唑啉酮类化合物 |
Country Status (30)
Country | Link |
---|---|
US (3) | US8067407B2 (zh) |
EP (1) | EP2265602B1 (zh) |
JP (1) | JP5579165B2 (zh) |
KR (1) | KR20100135838A (zh) |
CN (1) | CN102015685B (zh) |
AR (1) | AR071376A1 (zh) |
AU (1) | AU2009240311B2 (zh) |
BR (1) | BRPI0911594A2 (zh) |
CA (1) | CA2722016C (zh) |
CL (1) | CL2009000906A1 (zh) |
CO (1) | CO6300844A2 (zh) |
CR (1) | CR11684A (zh) |
DE (1) | DE102008020113A1 (zh) |
DO (1) | DOP2010000282A (zh) |
EC (1) | ECSP10010494A (zh) |
ES (1) | ES2535458T3 (zh) |
HK (1) | HK1156306A1 (zh) |
HN (1) | HN2010001920A (zh) |
IL (1) | IL208136A0 (zh) |
MA (1) | MA32251B1 (zh) |
MX (1) | MX2010010324A (zh) |
NZ (1) | NZ588721A (zh) |
PE (1) | PE20091732A1 (zh) |
RU (1) | RU2509080C9 (zh) |
SV (1) | SV2010003674A (zh) |
TW (1) | TWI433846B (zh) |
UA (1) | UA105487C2 (zh) |
UY (1) | UY31765A (zh) |
WO (1) | WO2009129945A1 (zh) |
ZA (1) | ZA201006719B (zh) |
Cited By (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN104321318A (zh) * | 2012-03-30 | 2015-01-28 | 第一三共株式会社 | 4-烷酰基氨基-3-吡唑啉酮衍生物 |
CN109694380A (zh) * | 2017-10-23 | 2019-04-30 | 中国医药研究开发中心有限公司 | 二氢吡唑啉酮类化合物及其制备方法和医药用途 |
CN110191884A (zh) * | 2016-10-14 | 2019-08-30 | 拜耳公司 | 取代的6-(1h-吡唑-1-基)嘧啶-4-胺衍生物及其用途 |
CN111825690A (zh) * | 2019-04-17 | 2020-10-27 | 中国医药研究开发中心有限公司 | 一种phd抑制剂的新晶型及其制备方法 |
CN114728927A (zh) * | 2019-11-19 | 2022-07-08 | 莫达戈有限公司 | 用于诊断、治疗和预防与α-突触核蛋白的聚集相关的疾病的新颖化合物 |
Families Citing this family (14)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
DE102008020113A1 (de) * | 2008-04-23 | 2009-10-29 | Bayer Schering Pharma Aktiengesellschaft | Substituierte Dihydropyrazolone und ihre Verwendung |
DE102005019712A1 (de) | 2005-04-28 | 2006-11-09 | Bayer Healthcare Ag | Dipyridyl-dihydropyrazolone und ihre Verwendung |
DE102006050516A1 (de) | 2006-10-26 | 2008-04-30 | Bayer Healthcare Ag | Substituierte Dihydropyrazolone und ihre Verwendung |
CN103052632B (zh) * | 2010-08-18 | 2014-03-19 | 山东亨利医药科技有限责任公司 | 二氢吡唑类化合物 |
DE102010044131A1 (de) | 2010-11-18 | 2012-05-24 | Bayer Schering Pharma Aktiengesellschaft | Substituiertes Natrium-1H-pyrazol-5-olat |
GB201102659D0 (en) | 2011-02-15 | 2011-03-30 | Isis Innovation | Assay |
WO2012126275A1 (zh) * | 2011-03-18 | 2012-09-27 | 山东亨利医药科技有限责任公司 | 含有螺环的二氢吡唑类化合物 |
GB201113101D0 (en) | 2011-07-28 | 2011-09-14 | Isis Innovation | Assay |
JP2014528446A (ja) | 2011-10-06 | 2014-10-27 | メルク・シャープ・アンド・ドーム・コーポレーションMerck Sharp & Dohme Corp. | 1,3−置換アゼチジンpde10阻害剤 |
CN104144925A (zh) * | 2011-10-17 | 2014-11-12 | 拜耳知识产权有限责任公司 | 作为hif抑制剂的取代的噁二唑基吡啶酮和噁二唑基哒嗪酮 |
EP2802608A4 (en) | 2012-01-12 | 2015-08-05 | Univ Yale | COMPOUNDS AND METHODS FOR ENHANCED DEGRADATION OF TARGET PROTEINS AND OTHER POLYPEPTIDES BY E3 UBIQUITIN LIGASE |
SG11201407043PA (en) * | 2012-05-08 | 2014-12-30 | Bayer Pharma AG | Method for the preparation of triazole compounds |
WO2019076974A1 (en) * | 2017-10-17 | 2019-04-25 | Sensorion | SYNTHESIS OF 4-AMINOPYRIMIDINE COMPOUNDS |
CN111825689B (zh) * | 2019-04-17 | 2023-05-05 | 中国医药研究开发中心有限公司 | 一种二氢吡唑啉酮类化合物的晶型及其制备方法 |
Citations (4)
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WO2004087066A2 (en) * | 2003-03-27 | 2004-10-14 | Emory University | Hif-1 inhibitors |
CN1842332A (zh) * | 2003-06-30 | 2006-10-04 | Hif生物公司 | 化合物、组合物及方法 |
WO2006114213A1 (de) * | 2005-04-28 | 2006-11-02 | Bayer Healthcare Ag | Dipyridyl-dihydropyrazolone und ihre verwendung 4- (pyridin-3-yl) -2- (pyridin-2-yl) -1,2-dihydro-3h-pyrazol-3-on derivate als spezifische hemmstoffe der hif-prolyl-4-hydroxylasen zur behandlung kardiovaskulärer und hämatologischer erkrankungen |
WO2008067871A1 (de) * | 2006-10-26 | 2008-06-12 | Bayer Schering Pharma Aktiengesellschaft | Substituierte dihydropyrazolone zur behandlung kardiovaskulärer und hämatologischer erkrankungen |
Family Cites Families (23)
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GR63123B (en) | 1975-12-11 | 1979-09-11 | Lilly Co Eli | Preparation process of novel 1,4-diphenyl-3-pyrazolin-5-ones |
US4075003A (en) | 1975-12-11 | 1978-02-21 | Eli Lilly And Company | Novel herbicidal method utilizing 1,4-diphenyl-3-pyrazolin-5-ones |
PL103509B1 (pl) | 1976-09-20 | 1979-06-30 | Lilly Co Eli | Srodek chwastobojczy |
US4663327A (en) | 1984-05-23 | 1987-05-05 | Bayer Aktiengesellschaft | 1-heteroaryl-4-aryl-pyrazolin-5-ones |
DE3443308A1 (de) | 1984-11-28 | 1986-05-28 | Bayer Ag, 5090 Leverkusen | 1-heteroaryl-4-aryl-pyrazolin-5-one zur verwendung als arzneimittel |
DE3527157A1 (de) | 1985-07-30 | 1987-02-12 | Bayer Ag | 1-heteroaryl-4-aryl-pyrazol-derivate |
FR2725988B1 (fr) | 1994-10-24 | 1997-01-24 | Roussel Uclaf | Nouveaux derives de pyrazolones et pyrazoles acides, leur procede de preparation, les nouveaux intermediaires obtenus, leur application a titre de medicaments et les compositions pharmaceutiques les renfermant |
DE19909237A1 (de) | 1999-03-03 | 2000-09-07 | Merck Patent Gmbh | Pyrazol-3-on-derivate |
US6878729B2 (en) | 2001-05-04 | 2005-04-12 | The Procter & Gamble Company | Medicinal uses of dihydropyrazoles |
CA2446864C (en) | 2001-05-16 | 2011-02-15 | Vertex Pharmaceuticals Incorporated | Inhibitors of src and other protein kinases |
JP4286146B2 (ja) | 2001-12-18 | 2009-06-24 | メルク エンド カムパニー インコーポレーテッド | メタボトロピックグルタミン酸受容体−5のヘテロアリール置換ピラゾール系調節剤 |
WO2003074550A2 (en) | 2002-03-01 | 2003-09-12 | Pintex Pharmaceuticals, Inc. | Pin1-modulating compounds and methods of use thereof |
US8124582B2 (en) | 2002-12-06 | 2012-02-28 | Fibrogen, Inc. | Treatment of diabetes |
AU2004228057A1 (en) | 2003-04-03 | 2004-10-21 | Merck & Co., Inc. | Di-aryl substituted pyrazole modulators of metabotropic glutamate receptor-5 |
WO2004099371A2 (en) | 2003-05-01 | 2004-11-18 | Panacea Pharmaceuticals, Inc. | Methods of treating ischemic related conditions |
WO2005030121A2 (en) | 2003-06-30 | 2005-04-07 | Hif Bio, Inc. | Compounds, compositions and methods |
US8529889B2 (en) | 2004-06-29 | 2013-09-10 | Massachusetts Institute Of Technology | Methods and compositions related to the modulation of intercellular junctions |
DE102008020113A1 (de) * | 2008-04-23 | 2009-10-29 | Bayer Schering Pharma Aktiengesellschaft | Substituierte Dihydropyrazolone und ihre Verwendung |
JP2008533162A (ja) | 2005-03-16 | 2008-08-21 | アベンティス・ファーマスーティカルズ・インコーポレイテツド | 中枢神経系用薬剤としてのジピラゾール |
WO2007008541A2 (en) | 2005-07-08 | 2007-01-18 | Kalypsys, Inc. | Cellular cholesterol absorption modifiers |
DE102006050513A1 (de) | 2006-10-26 | 2008-04-30 | Bayer Healthcare Ag | Substitiuierte Dihydropyrazolone und ihre Verwendung |
DE102006050515A1 (de) | 2006-10-26 | 2008-04-30 | Bayer Healthcare Ag | Substituierte Dipyridiyl-dihydropyrazolone und ihre Verwendung |
JP5237712B2 (ja) * | 2008-07-25 | 2013-07-17 | 公立大学法人 滋賀県立大学 | 静電紡糸装置 |
-
2008
- 2008-04-23 DE DE102008020113A patent/DE102008020113A1/de not_active Withdrawn
-
2009
- 2009-04-11 CA CA2722016A patent/CA2722016C/en not_active Expired - Fee Related
- 2009-04-11 AU AU2009240311A patent/AU2009240311B2/en not_active Ceased
- 2009-04-11 UA UAA201013898A patent/UA105487C2/uk unknown
- 2009-04-11 WO PCT/EP2009/002693 patent/WO2009129945A1/de active Application Filing
- 2009-04-11 CN CN200980114292.9A patent/CN102015685B/zh not_active Expired - Fee Related
- 2009-04-11 KR KR1020107023631A patent/KR20100135838A/ko not_active Application Discontinuation
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CN111825690A (zh) * | 2019-04-17 | 2020-10-27 | 中国医药研究开发中心有限公司 | 一种phd抑制剂的新晶型及其制备方法 |
CN111825690B (zh) * | 2019-04-17 | 2022-09-27 | 中国医药研究开发中心有限公司 | 一种phd抑制剂的新晶型及其制备方法 |
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