CN103402997B - 二氨基嘧啶衍生物及其制备方法 - Google Patents
二氨基嘧啶衍生物及其制备方法 Download PDFInfo
- Publication number
- CN103402997B CN103402997B CN201280010406.7A CN201280010406A CN103402997B CN 103402997 B CN103402997 B CN 103402997B CN 201280010406 A CN201280010406 A CN 201280010406A CN 103402997 B CN103402997 B CN 103402997B
- Authority
- CN
- China
- Prior art keywords
- pyrrolidin
- propylpyrimidin
- ylamino
- group
- benzonitrile
- 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.)
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- 0 C*CC(CC(*)C1*)N1c1nc(N*)nc(*)c1 Chemical compound C*CC(CC(*)C1*)N1c1nc(N*)nc(*)c1 0.000 description 9
Classifications
-
- 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
-
- 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
- C07D403/02—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 two hetero rings
- C07D403/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/10—Laxatives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/12—Antidiarrhoeals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
- C07D401/02—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 two hetero rings
- C07D401/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
- C07D403/02—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 two hetero rings
- C07D403/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero 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
- C07D413/02—Heterocyclic 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
- C07D413/04—Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nutrition Science (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| KR20110016981 | 2011-02-25 | ||
| KR10-2011-0016981 | 2011-02-25 | ||
| PCT/KR2012/001427 WO2012115480A2 (en) | 2011-02-25 | 2012-02-24 | Diaminopyrimidine derivatives and processes for the preparation thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN103402997A CN103402997A (zh) | 2013-11-20 |
| CN103402997B true CN103402997B (zh) | 2015-08-26 |
Family
ID=46721361
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201280010406.7A Active CN103402997B (zh) | 2011-02-25 | 2012-02-24 | 二氨基嘧啶衍生物及其制备方法 |
| CN201280010354.3A Active CN103391935B (zh) | 2011-02-25 | 2012-02-24 | 二氨基嘧啶衍生物及其制备方法 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201280010354.3A Active CN103391935B (zh) | 2011-02-25 | 2012-02-24 | 二氨基嘧啶衍生物及其制备方法 |
Country Status (17)
| Country | Link |
|---|---|
| US (4) | US9850227B2 (enExample) |
| EP (2) | EP2678332B1 (enExample) |
| JP (2) | JP5980236B2 (enExample) |
| KR (2) | KR101671341B1 (enExample) |
| CN (2) | CN103402997B (enExample) |
| AU (2) | AU2012221925B2 (enExample) |
| BR (2) | BR112013019942B1 (enExample) |
| CA (2) | CA2827072C (enExample) |
| DK (1) | DK2678332T3 (enExample) |
| ES (2) | ES2587304T3 (enExample) |
| HU (1) | HUE029988T2 (enExample) |
| IN (1) | IN2013MN01519A (enExample) |
| MX (2) | MX336155B (enExample) |
| PL (2) | PL2678331T3 (enExample) |
| PT (1) | PT2678332T (enExample) |
| RU (1) | RU2587493C2 (enExample) |
| WO (2) | WO2012115478A2 (enExample) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2587304T3 (es) * | 2011-02-25 | 2016-10-21 | Yuhan Corporation | Derivados de diaminopirimidina y procedimientos para la preparación de los mismos |
| PH12015501130B1 (en) | 2012-11-21 | 2023-01-27 | Ptc Therapeutics Inc | Substituted reverse pyrimidine bmi-1 inhibitors |
| KR101657616B1 (ko) * | 2013-05-24 | 2016-09-19 | 주식회사유한양행 | 피리미딘 고리를 포함하는 바이사이클릭 유도체 및 그의 제조방법 |
| MX370588B (es) * | 2013-08-30 | 2019-12-16 | Ptc Therapeutics Inc | Inhibidores de la bmi-1 de pirimidina sustituida. |
| US10584115B2 (en) | 2013-11-21 | 2020-03-10 | Ptc Therapeutics, Inc. | Substituted pyridine and pyrazine BMI-1 inhibitors |
| CN104003944B (zh) * | 2014-05-29 | 2016-08-24 | 西北师范大学 | 一种嘧菌胺的制备方法 |
| EP3929190B1 (en) * | 2014-10-13 | 2024-12-25 | Yuhan Corporation | Compounds and compositions for modulating egfr mutant kinase activities |
| US10300155B2 (en) | 2015-12-31 | 2019-05-28 | Washington University | Alpha-synuclein ligands |
| CN105646321A (zh) * | 2016-01-07 | 2016-06-08 | 中国药科大学 | (s)-3-羟基吡咯烷盐酸盐的制备方法 |
| GB201604647D0 (en) | 2016-03-18 | 2016-05-04 | Mission Therapeutics Ltd | Novel compounds |
| KR102441327B1 (ko) * | 2018-05-18 | 2022-09-07 | 주식회사유한양행 | 다이아미노피리미딘 유도체 또는 이의 산부가염의 신규의 제조방법 |
| JP2021535198A (ja) | 2018-08-17 | 2021-12-16 | ピーティーシー セラピューティクス， インコーポレイテッド | 膵臓癌を治療する方法 |
| CA3122182A1 (en) | 2018-12-18 | 2020-06-25 | Astrazeneca Ab | Pharmaceutical process and intermediates |
| CN110317176A (zh) * | 2019-07-04 | 2019-10-11 | 沈阳药科大学 | 2-氨基嘧啶类化合物及其用途 |
| KR20220006776A (ko) * | 2020-07-09 | 2022-01-18 | 주식회사유한양행 | 다이아미노피리미딘 유도체 또는 이의 약학적으로 허용가능한 염을 포함하는 약학 조성물 및 이의 제조방법 |
| WO2025104079A1 (en) * | 2023-11-17 | 2025-05-22 | Helmholtz-Zentrum für Infektionsforschung GmbH | Salicylic acid and picolinic acid derivatives as inhibitors of energy coupling factor (ecf) transporters for the treatment of bacterial infections |
| WO2026061469A1 (zh) * | 2024-09-19 | 2026-03-26 | 马应龙药业集团股份有限公司 | 杂芳胺类化合物、其药物组合物及其应用 |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2006057972A1 (en) * | 2004-11-24 | 2006-06-01 | Bristol-Myers Squibb Company | Process for preparing novel crystalline forms of (2s)-1-[[(7r)-7-(3,4-dichlorophenyl)-4,7-dihydro-5-methylpyrazolo[1,5]pyrimidine-6-yl]carbonyl]-2-(4-fluorophenyl) pyrrolidine, novel stable forms produced therein and formulations |
| WO2007062417A1 (en) * | 2005-11-28 | 2007-05-31 | Kalypsys, Inc. | Methods of preparing 2-imidazol-1-yl-4-methyl-6-pyrrolidin-2-yl-pyrimidine and 4-(1-alkylpyrrolidin-2-yl)-2-(1h-imidazol-1-yl)-6-methylpyrimidine derivatives |
Family Cites Families (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4962115A (en) | 1981-10-01 | 1990-10-09 | Janssen Pharmaceutica N.V. | Novel N-(3-hydroxy-4-piperidinyl)benzamide derivatives |
| CZ284687B6 (cs) | 1986-04-30 | 1999-02-17 | Dainippon Pharmaceutical Co., Ltd. | Substituovaný benzamidový derivát, způsob jeho výroby a farmaceutický prostředek na jeho bázi |
| GB9005014D0 (en) | 1990-03-06 | 1990-05-02 | Janssen Pharmaceutica Nv | N.(4.piperidinyl)(dihydrobenzofuran or dihydro.2h.benzopyran)carboxamide derivatives |
| HUT64023A (en) | 1991-03-22 | 1993-11-29 | Sandoz Ag | Process for producing aminoguanidine derivatives and pharmaceutical compositions comprising such compounds |
| JP3398152B2 (ja) * | 1993-10-12 | 2003-04-21 | ブリストル‐マイヤーズ・スクイブ・ファーマ・カンパニー | １ｎ−アルキル−ｎ−アリールピリミジンアミンおよびその誘導体 |
| NZ274978A (en) * | 1993-10-12 | 1998-04-27 | Du Pont Merck Pharma | 1n-alkyl-n-aryl pyrimidinamine derivatives and pharmaceutical compositions thereof |
| IL112024A (en) | 1993-12-21 | 1999-07-14 | Novo Nordisk As | Pharmaceutical compositions comprising tetrahydropyridine derivatives substituted with oxadiazole or thiadiazole for treating gastrointestinal motility disorders |
| EP0775120B1 (en) | 1994-08-13 | 2003-06-04 | Yuhan Corporation | Novel pyrimidine derivatives and processes for the preparation thereof |
| US5739151A (en) * | 1996-07-19 | 1998-04-14 | Sepracor Inc. | Method for treating emesis and central nervous system disorders using optically pure (+) norcisapride |
| IN188411B (enExample) * | 1997-03-27 | 2002-09-21 | Yuhan Corp | |
| US6825198B2 (en) * | 2001-06-21 | 2004-11-30 | Pfizer Inc | 5-HT receptor ligands and uses thereof |
| KR20060052806A (ko) * | 2003-07-25 | 2006-05-19 | 시바 스폐셜티 케미칼스 홀딩 인코포레이티드 | 항균제로서 치환된 2,4-비스(알킬아미노)피리미딘 또는-퀴나졸린의 용도 |
| CA2537182A1 (en) * | 2003-08-29 | 2005-03-10 | Dynogen Pharmaceuticals, Inc. | Compositions useful for treating gastrointestinal motility disorders |
| US20060057972A1 (en) | 2004-09-14 | 2006-03-16 | Wikel Harold L | Adapter for a modular wireless communication device |
| US8816090B2 (en) | 2005-02-25 | 2014-08-26 | Pfizer Inc. | Benzisoxazole derivatives |
| US20070032514A1 (en) | 2005-07-01 | 2007-02-08 | Zahn Stephan K | 2,4-diamino-pyrimidines as aurora inhibitors |
| EP2003131A4 (en) * | 2006-04-04 | 2009-12-16 | Taisho Pharmaceutical Co Ltd | AMINOPYRROLIDINE COMPOUND |
| EP2007754A1 (en) * | 2006-04-10 | 2008-12-31 | Boehringer Ingelheim International GmbH | 2, 4-diaminopyrimidine derivatives and their use for the treatment of cancer |
| KR101247840B1 (ko) * | 2008-02-22 | 2013-03-26 | 에프. 호프만-라 로슈 아게 | 아밀로이드 베타 조절제 |
| KR101705158B1 (ko) * | 2009-05-05 | 2017-02-09 | 다나-파버 캔서 인스티튜트 인크. | Ｅｇｆｒ 억제제 및 질환 치료방법 |
| ES2587304T3 (es) * | 2011-02-25 | 2016-10-21 | Yuhan Corporation | Derivados de diaminopirimidina y procedimientos para la preparación de los mismos |
-
2012
- 2012-02-24 ES ES12750114.6T patent/ES2587304T3/es active Active
- 2012-02-24 PL PL12749916.8T patent/PL2678331T3/pl unknown
- 2012-02-24 PT PT127501146T patent/PT2678332T/pt unknown
- 2012-02-24 DK DK12750114.6T patent/DK2678332T3/en active
- 2012-02-24 CN CN201280010406.7A patent/CN103402997B/zh active Active
- 2012-02-24 EP EP12750114.6A patent/EP2678332B1/en active Active
- 2012-02-24 WO PCT/KR2012/001423 patent/WO2012115478A2/en not_active Ceased
- 2012-02-24 JP JP2013555368A patent/JP5980236B2/ja active Active
- 2012-02-24 KR KR1020120018926A patent/KR101671341B1/ko active Active
- 2012-02-24 MX MX2013009627A patent/MX336155B/es unknown
- 2012-02-24 CA CA2827072A patent/CA2827072C/en active Active
- 2012-02-24 MX MX2013009549A patent/MX337477B/es active IP Right Grant
- 2012-02-24 JP JP2013555369A patent/JP5890436B2/ja active Active
- 2012-02-24 BR BR112013019942-3A patent/BR112013019942B1/pt active IP Right Grant
- 2012-02-24 AU AU2012221925A patent/AU2012221925B2/en active Active
- 2012-02-24 IN IN1519MUN2013 patent/IN2013MN01519A/en unknown
- 2012-02-24 US US14/001,475 patent/US9850227B2/en active Active
- 2012-02-24 CN CN201280010354.3A patent/CN103391935B/zh active Active
- 2012-02-24 BR BR112013020641-1A patent/BR112013020641B1/pt active IP Right Grant
- 2012-02-24 AU AU2012221927A patent/AU2012221927B2/en active Active
- 2012-02-24 ES ES12749916.8T patent/ES2579830T3/es active Active
- 2012-02-24 RU RU2013142187/04A patent/RU2587493C2/ru active
- 2012-02-24 US US14/001,489 patent/US9890138B2/en active Active
- 2012-02-24 KR KR1020120018933A patent/KR101671348B1/ko active Active
- 2012-02-24 PL PL12750114.6T patent/PL2678332T3/pl unknown
- 2012-02-24 WO PCT/KR2012/001427 patent/WO2012115480A2/en not_active Ceased
- 2012-02-24 EP EP12749916.8A patent/EP2678331B1/en active Active
- 2012-02-24 CA CA2827030A patent/CA2827030C/en active Active
- 2012-02-24 HU HUE12750114A patent/HUE029988T2/en unknown
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2017
- 2017-11-15 US US15/813,741 patent/US10640490B2/en active Active
- 2017-12-20 US US15/848,760 patent/US10227330B2/en active Active
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2006057972A1 (en) * | 2004-11-24 | 2006-06-01 | Bristol-Myers Squibb Company | Process for preparing novel crystalline forms of (2s)-1-[[(7r)-7-(3,4-dichlorophenyl)-4,7-dihydro-5-methylpyrazolo[1,5]pyrimidine-6-yl]carbonyl]-2-(4-fluorophenyl) pyrrolidine, novel stable forms produced therein and formulations |
| WO2007062417A1 (en) * | 2005-11-28 | 2007-05-31 | Kalypsys, Inc. | Methods of preparing 2-imidazol-1-yl-4-methyl-6-pyrrolidin-2-yl-pyrimidine and 4-(1-alkylpyrrolidin-2-yl)-2-(1h-imidazol-1-yl)-6-methylpyrimidine derivatives |
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