JP6186440B2 - キナーゼ阻害剤としてのジヒドロピロリジノピリミジン - Google Patents
キナーゼ阻害剤としてのジヒドロピロリジノピリミジン Download PDFInfo
- Publication number
- JP6186440B2 JP6186440B2 JP2015533126A JP2015533126A JP6186440B2 JP 6186440 B2 JP6186440 B2 JP 6186440B2 JP 2015533126 A JP2015533126 A JP 2015533126A JP 2015533126 A JP2015533126 A JP 2015533126A JP 6186440 B2 JP6186440 B2 JP 6186440B2
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- cancer
- cycloalkyl
- membered
- mmol
- 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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Classifications
-
- 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic 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
- A61K31/527—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim spiro-condensed
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
- C07D207/34—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D207/36—Oxygen or sulfur atoms
-
- 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
- C07D487/10—Spiro-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261702981P | 2012-09-19 | 2012-09-19 | |
| US61/702,981 | 2012-09-19 | ||
| PCT/US2013/060032 WO2014047020A1 (en) | 2012-09-19 | 2013-09-17 | Dihydropyrrolidino-pyrimidines as kinase inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015529248A JP2015529248A (ja) | 2015-10-05 |
| JP2015529248A5 JP2015529248A5 (enExample) | 2017-08-17 |
| JP6186440B2 true JP6186440B2 (ja) | 2017-08-23 |
Family
ID=49274870
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015533126A Active JP6186440B2 (ja) | 2012-09-19 | 2013-09-17 | キナーゼ阻害剤としてのジヒドロピロリジノピリミジン |
Country Status (13)
| Country | Link |
|---|---|
| US (1) | US9546173B2 (enExample) |
| EP (1) | EP2897961B1 (enExample) |
| JP (1) | JP6186440B2 (enExample) |
| KR (1) | KR20150056550A (enExample) |
| CN (1) | CN104640865B (enExample) |
| AU (1) | AU2013318283A1 (enExample) |
| BR (1) | BR112015005982A2 (enExample) |
| CA (1) | CA2882410A1 (enExample) |
| EA (1) | EA201590600A1 (enExample) |
| ES (1) | ES2612885T3 (enExample) |
| IN (1) | IN2015DN01328A (enExample) |
| MX (1) | MX2015003535A (enExample) |
| WO (1) | WO2014047020A1 (enExample) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2013318283A1 (en) * | 2012-09-19 | 2015-03-05 | Novartis Ag | Dihydropyrrolidino-pyrimidines as kinase inhibitors |
| CA3103711A1 (en) | 2018-07-12 | 2020-01-16 | UCB Biopharma SRL | Spirocyclic indane analogues as il-17 modulators |
| WO2020243457A1 (en) * | 2019-05-29 | 2020-12-03 | Viogen Biosciences, Llc | Compounds and therapeutic uses thereof |
| CN114502546A (zh) * | 2019-08-01 | 2022-05-13 | 普拉特戈公司 | 晚期糖基化终产物的抑制剂 |
| KR20220112777A (ko) * | 2019-12-10 | 2022-08-11 | 에프. 호프만-라 로슈 아게 | 패러독스 파괴제로서의 새로운 braf 억제제 |
| FI4073065T3 (fi) | 2019-12-10 | 2025-04-16 | Hoffmann La Roche | Uusia metyylikinatsolinonijohdannaisia |
| CA3177298C (en) * | 2020-04-30 | 2023-11-21 | Xile LIU | Compounds containing benzosultam as erk inhibitors |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP4530852B2 (ja) * | 2002-07-15 | 2010-08-25 | メルク・シャープ・エンド・ドーム・コーポレイション | 糖尿病治療のためのピペリジノピリミジンジペプチジルペプチダーゼ阻害剤 |
| CA2514733A1 (en) | 2003-02-28 | 2004-09-16 | Transform Pharmaceuticals, Inc. | Pharmaceutical co-crystal compositions of drugs such as carbamazepine, celecoxib, olanzapine, itraconazole, topiramate, modafinil, 5-fluorouracil, hydrochlorothiazide, acetaminophen, aspirin, flurbiprofen, phenytoin and ibuprofen |
| AU2004313928A1 (en) * | 2003-12-02 | 2005-07-28 | Vertex Pharmaceuticals, Inc. | Heterocyclic protein kinase inhibitors and uses thereof |
| PE20060426A1 (es) | 2004-06-02 | 2006-06-28 | Schering Corp | DERIVADOS DE ACIDO TARTARICO COMO INHIBIDORES DE MMPs, ADAMs, TACE Y TNF-alfa |
| KR100919343B1 (ko) | 2005-01-10 | 2009-09-25 | 화이자 인코포레이티드 | 키네이스 억제제로서 피롤로피라졸 |
| RU2442778C9 (ru) | 2005-12-13 | 2012-08-10 | Шеринг Корпорейшн | Новые соединения, действующие как ингибиторы erk |
| AR068046A1 (es) | 2007-06-05 | 2009-11-04 | Schering Corp | Derivados policiclicos de indazol y su uso como inhibidores de erk para el tratamiento del cancer |
| EP2613782B1 (en) | 2010-09-01 | 2016-11-02 | Merck Sharp & Dohme Corp. | Indazole derivatives useful as erk inhibitors |
| US9242981B2 (en) * | 2010-09-16 | 2016-01-26 | Merck Sharp & Dohme Corp. | Fused pyrazole derivatives as novel ERK inhibitors |
| WO2012065935A1 (en) | 2010-11-17 | 2012-05-24 | F. Hoffmann-La Roche Ag | Methods of treating tumors |
| CN103635472B (zh) | 2011-02-28 | 2018-01-12 | 阵列生物制药公司 | 丝氨酸/苏氨酸激酶抑制剂 |
| CN104507936A (zh) | 2012-03-02 | 2015-04-08 | 基因科技股份有限公司 | 吡啶基和嘧啶基亚砜和砜衍生物 |
| AU2013318283A1 (en) * | 2012-09-19 | 2015-03-05 | Novartis Ag | Dihydropyrrolidino-pyrimidines as kinase inhibitors |
-
2013
- 2013-09-17 AU AU2013318283A patent/AU2013318283A1/en not_active Abandoned
- 2013-09-17 IN IN1328DEN2015 patent/IN2015DN01328A/en unknown
- 2013-09-17 BR BR112015005982A patent/BR112015005982A2/pt not_active IP Right Cessation
- 2013-09-17 JP JP2015533126A patent/JP6186440B2/ja active Active
- 2013-09-17 ES ES13771007.5T patent/ES2612885T3/es active Active
- 2013-09-17 CN CN201380048493.XA patent/CN104640865B/zh active Active
- 2013-09-17 EA EA201590600A patent/EA201590600A1/ru unknown
- 2013-09-17 WO PCT/US2013/060032 patent/WO2014047020A1/en not_active Ceased
- 2013-09-17 KR KR1020157006602A patent/KR20150056550A/ko not_active Withdrawn
- 2013-09-17 MX MX2015003535A patent/MX2015003535A/es unknown
- 2013-09-17 US US14/428,546 patent/US9546173B2/en active Active
- 2013-09-17 CA CA2882410A patent/CA2882410A1/en not_active Abandoned
- 2013-09-17 EP EP13771007.5A patent/EP2897961B1/en active Active
Also Published As
| Publication number | Publication date |
|---|---|
| MX2015003535A (es) | 2015-07-14 |
| BR112015005982A2 (pt) | 2017-07-04 |
| CA2882410A1 (en) | 2014-03-27 |
| WO2014047020A1 (en) | 2014-03-27 |
| CN104640865A (zh) | 2015-05-20 |
| KR20150056550A (ko) | 2015-05-26 |
| US20150274733A1 (en) | 2015-10-01 |
| IN2015DN01328A (enExample) | 2015-07-03 |
| EP2897961A1 (en) | 2015-07-29 |
| ES2612885T3 (es) | 2017-05-19 |
| EA201590600A1 (ru) | 2015-07-30 |
| AU2013318283A1 (en) | 2015-03-05 |
| CN104640865B (zh) | 2018-05-11 |
| US9546173B2 (en) | 2017-01-17 |
| JP2015529248A (ja) | 2015-10-05 |
| EP2897961B1 (en) | 2016-10-26 |
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