CN103391935B - 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
- CN103391935B CN103391935B CN201280010354.3A CN201280010354A CN103391935B CN 103391935 B CN103391935 B CN 103391935B CN 201280010354 A CN201280010354 A CN 201280010354A CN 103391935 B CN103391935 B CN 103391935B
- Authority
- CN
- China
- Prior art keywords
- propylpyrimidin
- group
- piperidin
- amine
- amino
- 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 **CCC[N+]=C(*)CC(*)* Chemical compound **CCC[N+]=C(*)CC(*)* 0.000 description 4
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
- C07D403/02—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
-
- 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
-
- 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/KR2012/001423 WO2012115478A2 (en) | 2011-02-25 | 2012-02-24 | Diaminopyrimidine derivatives and processes for the preparation thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN103391935A CN103391935A (zh) | 2013-11-13 |
| CN103391935B true CN103391935B (zh) | 2015-12-23 |
Family
ID=46721361
Family Applications (2)
| 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 |
| 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 |
Family Applications After (1)
| 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 |
Country Status (17)
| Country | Link |
|---|---|
| US (4) | US9890138B2 (enExample) |
| EP (2) | EP2678331B1 (enExample) |
| JP (2) | JP5980236B2 (enExample) |
| KR (2) | KR101671341B1 (enExample) |
| CN (2) | CN103391935B (enExample) |
| AU (2) | AU2012221925B2 (enExample) |
| BR (2) | BR112013020641B1 (enExample) |
| CA (2) | CA2827030C (enExample) |
| DK (1) | DK2678332T3 (enExample) |
| ES (2) | ES2587304T3 (enExample) |
| HU (1) | HUE029988T2 (enExample) |
| IN (1) | IN2013MN01519A (enExample) |
| MX (2) | MX336155B (enExample) |
| PL (2) | PL2678332T3 (enExample) |
| PT (1) | PT2678332T (enExample) |
| RU (1) | RU2587493C2 (enExample) |
| WO (2) | WO2012115480A2 (enExample) |
Families Citing this family (16)
| 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 |
| DK2922828T3 (da) | 2012-11-21 | 2020-08-31 | Ptc Therapeutics Inc | 4,6-diamino-pyrimidin-derivater som bmi-1-inhibitorer til at behandle cancer |
| KR101657616B1 (ko) * | 2013-05-24 | 2016-09-19 | 주식회사유한양행 | 피리미딘 고리를 포함하는 바이사이클릭 유도체 및 그의 제조방법 |
| CA2922657C (en) * | 2013-08-30 | 2022-04-12 | Ptc Therapeutics, Inc. | Substituted pyrimidine bmi-1 inhibitors |
| 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 |
| PL3604294T3 (pl) * | 2014-10-13 | 2021-11-02 | Yuhan Corporation | Związki i kompozycje do modulowania aktywności zmutowanych kinaz EGFR |
| 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 |
| BR112021002630A2 (pt) | 2018-08-17 | 2021-05-11 | Ptc Therapeutics, Inc. | método para tratar câncer pancreático |
| BR112021011330A2 (pt) | 2018-12-18 | 2021-08-31 | Astrazeneca Ab | Processo farmacêutico e intermediários |
| 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 |
Family Cites Families (23)
| 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 |
| SK289787A3 (en) | 1986-04-30 | 1998-06-03 | Dainippon Pharmaceutical Co | Substituted n-£(2-morpholinyl)alkyl|benzamide derivative, method of producing the same and a pharmaceutical composition on its base |
| 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 |
| PL313973A1 (en) * | 1993-10-12 | 1996-08-05 | Du Pont Merck Pharma | 1 n-alkyl-n-arylopyrimidin amines and their derivatives |
| 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 |
| RU2129549C1 (ru) * | 1994-08-13 | 1999-04-27 | Юхан Корпорейшн | Производные пиримидина и способы их получения |
| 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 |
| BRPI0412915A (pt) | 2003-07-25 | 2006-09-26 | Ciba Sc Holding Ag | uso de 2,4-bis(alquilamino)pirimidinas ou -quinazolinas substituìdas como antimicrobianos |
| US20050059704A1 (en) * | 2003-08-29 | 2005-03-17 | 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 |
| US20060128726A1 (en) | 2004-11-24 | 2006-06-15 | Xuebao Wang | 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 |
| WO2006090224A1 (en) * | 2005-02-25 | 2006-08-31 | Pfizer Japan Inc. | Benzisoxazole derivatives |
| US20070032514A1 (en) * | 2005-07-01 | 2007-02-08 | Zahn Stephan K | 2,4-diamino-pyrimidines as aurora inhibitors |
| 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 |
| JPWO2007114323A1 (ja) * | 2006-04-04 | 2009-08-20 | 大正製薬株式会社 | アミノピロリジン化合物 |
| JP2009533378A (ja) | 2006-04-10 | 2009-09-17 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | ２，４−ジアミノピリミジン誘導体及び癌の治療のためのそれらの使用 |
| EP2257541B1 (en) * | 2008-02-22 | 2013-08-14 | F. Hoffmann-La Roche AG | Modulators for amyloid beta |
| JP5918693B2 (ja) * | 2009-05-05 | 2016-05-18 | ダナ ファーバー キャンサー インスティテュート インコーポレイテッド | Ｅｇｆｒ阻害剤及び疾患の治療方法 |
| 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 JP JP2013555368A patent/JP5980236B2/ja active Active
- 2012-02-24 US US14/001,489 patent/US9890138B2/en active Active
- 2012-02-24 AU AU2012221925A patent/AU2012221925B2/en active Active
- 2012-02-24 IN IN1519MUN2013 patent/IN2013MN01519A/en unknown
- 2012-02-24 MX MX2013009627A patent/MX336155B/es unknown
- 2012-02-24 PL PL12750114.6T patent/PL2678332T3/pl unknown
- 2012-02-24 JP JP2013555369A patent/JP5890436B2/ja active Active
- 2012-02-24 AU AU2012221927A patent/AU2012221927B2/en active Active
- 2012-02-24 RU RU2013142187/04A patent/RU2587493C2/ru active
- 2012-02-24 PT PT127501146T patent/PT2678332T/pt unknown
- 2012-02-24 CA CA2827030A patent/CA2827030C/en active Active
- 2012-02-24 KR KR1020120018926A patent/KR101671341B1/ko active Active
- 2012-02-24 PL PL12749916.8T patent/PL2678331T3/pl unknown
- 2012-02-24 CN CN201280010354.3A patent/CN103391935B/zh active Active
- 2012-02-24 KR KR1020120018933A patent/KR101671348B1/ko active Active
- 2012-02-24 CN CN201280010406.7A patent/CN103402997B/zh active Active
- 2012-02-24 EP EP12749916.8A patent/EP2678331B1/en active Active
- 2012-02-24 MX MX2013009549A patent/MX337477B/es active IP Right Grant
- 2012-02-24 BR BR112013020641-1A patent/BR112013020641B1/pt active IP Right Grant
- 2012-02-24 ES ES12749916.8T patent/ES2579830T3/es active Active
- 2012-02-24 DK DK12750114.6T patent/DK2678332T3/en active
- 2012-02-24 BR BR112013019942-3A patent/BR112013019942B1/pt active IP Right Grant
- 2012-02-24 CA CA2827072A patent/CA2827072C/en active Active
- 2012-02-24 US US14/001,475 patent/US9850227B2/en active Active
- 2012-02-24 WO PCT/KR2012/001427 patent/WO2012115480A2/en not_active Ceased
- 2012-02-24 HU HUE12750114A patent/HUE029988T2/en unknown
- 2012-02-24 EP EP12750114.6A patent/EP2678332B1/en active Active
- 2012-02-24 WO PCT/KR2012/001423 patent/WO2012115478A2/en not_active Ceased
-
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
Also Published As
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