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
- Publication number
- 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
- Authority
- CN
- China
- Prior art keywords
- compound
- base
- formula
- salt
- solvate
- 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
Links
- 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
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- 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
- A61P17/00—Drugs for dermatological disorders
- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/06—Antianaemics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
-
- 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)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Diabetes (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Hematology (AREA)
- Biomedical Technology (AREA)
- Endocrinology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Urology & Nephrology (AREA)
- Hospice & Palliative Care (AREA)
- Obesity (AREA)
- Rheumatology (AREA)
- Immunology (AREA)
- Oncology (AREA)
- Virology (AREA)
- Communicable Diseases (AREA)
- Emergency Medicine (AREA)
- Ophthalmology & Optometry (AREA)
- Molecular Biology (AREA)
- Tropical Medicine & Parasitology (AREA)
- AIDS & HIV (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Vascular Medicine (AREA)
- Psychology (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 |
---|---|---|---|
DE102008020113A DE102008020113A1 (de) | 2008-04-23 | 2008-04-23 | Substituierte Dihydropyrazolone und ihre Verwendung |
DE102008020113.8 | 2008-04-23 | ||
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 |
AU2012318874A1 (en) * | 2011-10-06 | 2014-05-15 | Merck Sharp & Dohme Corp. | 1,3-substituted azetidine PDE10 inhibitors |
US20140329797A1 (en) * | 2011-10-17 | 2014-11-06 | Bayer Intellectual Property Gmbh | Substituted oxadiazolyl pyridinones and oxadiazolyl pyridazinones as hif inhibitors |
CN104736569A (zh) * | 2012-01-12 | 2015-06-24 | 耶鲁大学 | 通过e3泛素连接酶增强靶蛋白质及其他多肽降解的化合物和方法 |
PT2847183T (pt) | 2012-05-08 | 2017-10-02 | Bayer Pharma AG | Processo para preparação de compostos de triazol |
CN111465602B (zh) * | 2017-10-17 | 2023-05-23 | 帕劳制药有限公司 | 4-氨基嘧啶化合物的合成 |
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)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
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)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4075003A (en) | 1975-12-11 | 1978-02-21 | Eli Lilly And Company | Novel herbicidal method utilizing 1,4-diphenyl-3-pyrazolin-5-ones |
GR63123B (en) | 1975-12-11 | 1979-09-11 | Lilly Co Eli | Preparation process of novel 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 |
AU2002308748A1 (en) | 2001-05-16 | 2002-11-25 | Vertex Pharmaceuticals Incorporated | Heterocyclic substituted pyrazoles as inhibitors of src and other protein kinases |
AU2002359714B2 (en) | 2001-12-18 | 2006-12-21 | Merck Sharp & Dohme Corp. | Heteroaryl substituted pyrazole modulators of metabotropic glutamate receptor-5 |
AU2003213673A1 (en) | 2002-03-01 | 2003-09-16 | Pintex Pharmaceuticals, Inc. | Pin1-modulating compounds and methods of use thereof |
US8124582B2 (en) | 2002-12-06 | 2012-02-28 | Fibrogen, Inc. | Treatment of diabetes |
US20060194807A1 (en) | 2003-04-03 | 2006-08-31 | Cosford Nicholas D P | Di-aryl substituted pyrazole modulators of metabotropic glutamate receptor-5 |
US7456179B2 (en) | 2003-05-01 | 2008-11-25 | Panacea Pharmaceuticals, Inc. | Methods of treating ischemic related conditions |
CA2530679A1 (en) | 2003-06-30 | 2005-04-07 | Hif Bio, Inc. | Compounds for treating angiogenesis |
WO2006088491A2 (en) | 2004-06-29 | 2006-08-24 | 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 |
CA2601098C (en) | 2005-03-16 | 2011-07-05 | Aventis Pharmaceuticals Inc. | Dipyrazoles as central nervous system agents |
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 AU AU2009240311A patent/AU2009240311B2/en not_active Ceased
- 2009-04-11 RU RU2010147404/04A patent/RU2509080C9/ru not_active IP Right Cessation
- 2009-04-11 KR KR1020107023631A patent/KR20100135838A/ko not_active Application Discontinuation
- 2009-04-11 BR BRPI0911594A patent/BRPI0911594A2/pt not_active IP Right Cessation
- 2009-04-11 UA UAA201013898A patent/UA105487C2/uk unknown
- 2009-04-11 NZ NZ588721A patent/NZ588721A/xx not_active IP Right Cessation
- 2009-04-11 ES ES09733899.0T patent/ES2535458T3/es active Active
- 2009-04-11 CA CA2722016A patent/CA2722016C/en not_active Expired - Fee Related
- 2009-04-11 CN CN200980114292.9A patent/CN102015685B/zh not_active Expired - Fee Related
- 2009-04-11 WO PCT/EP2009/002693 patent/WO2009129945A1/de active Application Filing
- 2009-04-11 EP EP09733899.0A patent/EP2265602B1/de active Active
- 2009-04-11 MX MX2010010324A patent/MX2010010324A/es active IP Right Grant
- 2009-04-11 JP JP2011505403A patent/JP5579165B2/ja not_active Expired - Fee Related
- 2009-04-14 UY UY0001031765A patent/UY31765A/es not_active Application Discontinuation
- 2009-04-14 PE PE2009000514A patent/PE20091732A1/es not_active Application Discontinuation
- 2009-04-15 CL CL2009000906A patent/CL2009000906A1/es unknown
- 2009-04-17 AR ARP090101367A patent/AR071376A1/es not_active Application Discontinuation
- 2009-04-22 TW TW098113265A patent/TWI433846B/zh not_active IP Right Cessation
- 2009-04-22 US US12/427,749 patent/US8067407B2/en active Active
-
2010
- 2010-09-14 IL IL208136A patent/IL208136A0/en unknown
- 2010-09-20 ZA ZA2010/06719A patent/ZA201006719B/en unknown
- 2010-09-21 SV SV2010003674A patent/SV2010003674A/es not_active Application Discontinuation
- 2010-09-21 CR CR11684A patent/CR11684A/es not_active Application Discontinuation
- 2010-09-21 EC EC2010010494A patent/ECSP10010494A/es unknown
- 2010-09-22 CO CO10117239A patent/CO6300844A2/es active IP Right Grant
- 2010-09-22 DO DO2010000282A patent/DOP2010000282A/es unknown
- 2010-09-22 HN HN2010001920A patent/HN2010001920A/es unknown
- 2010-10-20 MA MA33277A patent/MA32251B1/fr unknown
-
2011
- 2011-10-04 HK HK11110487.6A patent/HK1156306A1/zh not_active IP Right Cessation
- 2011-10-12 US US13/271,957 patent/US8580778B2/en active Active
-
2013
- 2013-10-07 US US14/047,652 patent/US20140038938A1/en not_active Abandoned
Patent Citations (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
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 |
Cited By (8)
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 |
US9212170B2 (en) | 2012-03-30 | 2015-12-15 | Daiichi Sankyo Company, Limited | 4-alkanoylamino-3-pyrazolone derivative |
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 |
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 |
CN109694380B (zh) * | 2017-10-23 | 2022-09-27 | 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 |
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 |
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 |
Also Published As
Similar Documents
Publication | Publication Date | Title |
---|---|---|
CN102015685B (zh) | 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 | |
CN101631785B (zh) | 用于治疗心血管和血液病的取代的二氢吡唑啉酮 | |
CN101213189B (zh) | 4-(吡啶-3-基)-2-(吡啶-2-基)-1,2-二氢-3h-吡唑啉-3-酮衍生物作为用于治疗心血管和血液学疾病的转录因子-脯氨酰-4-羟化酶的特异性抑制剂 | |
JP5300729B2 (ja) | 置換ジヒドロピラゾロン類およびhif−プロリル−4−ヒドロキシラーゼ阻害剤としてのそれらの使用 | |
CN101600710A (zh) | 取代的二吡啶基二氢吡唑啉酮和它们的应用 | |
JP5918779B2 (ja) | 置換1h−ピラゾール−5−オール=ナトリウム塩 |
Legal Events
Date | Code | Title | Description |
---|---|---|---|
C06 | Publication | ||
PB01 | Publication | ||
C10 | Entry into substantive examination | ||
SE01 | Entry into force of request for substantive examination | ||
REG | Reference to a national code |
Ref country code: HK Ref legal event code: DE Ref document number: 1156306 Country of ref document: HK |
|
ASS | Succession or assignment of patent right |
Owner name: BAYER INTELLECTUAL PROPERTY GMBH Free format text: FORMER OWNER: BAYER PHARMACEUTICALS AG Effective date: 20130322 |
|
C41 | Transfer of patent application or patent right or utility model | ||
C53 | Correction of patent of invention or patent application | ||
CB02 | Change of applicant information |
Address after: Berlin Applicant after: BAYER PHARMA AG Address before: Berlin Applicant before: Bayer Schering Pharma AG |
|
COR | Change of bibliographic data |
Free format text: CORRECT: APPLICANT; FROM: BAYER SCHERING PHARMA AG TO: BAYER PHARMACEUTICALS AG |
|
TA01 | Transfer of patent application right |
Effective date of registration: 20130322 Address after: German Monheim Applicant after: BAYER INTELLECTUAL PROPERTY GmbH Address before: Berlin Applicant before: BAYER PHARMA AG |
|
C14 | Grant of patent or utility model | ||
GR01 | Patent grant | ||
REG | Reference to a national code |
Ref country code: HK Ref legal event code: GR Ref document number: 1156306 Country of ref document: HK |
|
CF01 | Termination of patent right due to non-payment of annual fee | ||
CF01 | Termination of patent right due to non-payment of annual fee |
Granted publication date: 20141015 Termination date: 20180411 |