CN104640865B - 作为激酶抑制剂的二氢吡咯烷子基-嘧啶 - Google Patents
作为激酶抑制剂的二氢吡咯烷子基-嘧啶 Download PDFInfo
- Publication number
- CN104640865B CN104640865B CN201380048493.XA CN201380048493A CN104640865B CN 104640865 B CN104640865 B CN 104640865B CN 201380048493 A CN201380048493 A CN 201380048493A CN 104640865 B CN104640865 B CN 104640865B
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- China
- Prior art keywords
- alkyl
- compound
- cycloalkyl
- independently
- 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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Links
- 0 **c1ncc(C(*)(*)N(C2)C(*II)=O)c2n1 Chemical compound **c1ncc(C(*)(*)N(C2)C(*II)=O)c2n1 0.000 description 7
- NMXRJWVVQWWXEU-PZYJYFCTSA-N C/C=C\C=C(\[C@@H](CO)NC(N(C1)C2(CCC2)c2c1nc(NC1CCOCC1)nc2)=O)/C#C Chemical compound C/C=C\C=C(\[C@@H](CO)NC(N(C1)C2(CCC2)c2c1nc(NC1CCOCC1)nc2)=O)/C#C NMXRJWVVQWWXEU-PZYJYFCTSA-N 0.000 description 1
- BKTXSVXCONQOAA-OAHLLOKOSA-N CC(C)(c(cn1)c(C2)nc1S(C)(=O)=O)N2C(N[C@H](CO)c1ccccc1)=O Chemical compound CC(C)(c(cn1)c(C2)nc1S(C)(=O)=O)N2C(N[C@H](CO)c1ccccc1)=O BKTXSVXCONQOAA-OAHLLOKOSA-N 0.000 description 1
- YAZULJUJKCJNKB-UHFFFAOYSA-N CC1(CO)NCC2NC(NC3CCOCC3)=NC=C12 Chemical compound CC1(CO)NCC2NC(NC3CCOCC3)=NC=C12 YAZULJUJKCJNKB-UHFFFAOYSA-N 0.000 description 1
- KBTAWWGYJCJSCV-UHFFFAOYSA-N CCCC(CC)OC(N1CC(C)CC1)=O Chemical compound CCCC(CC)OC(N1CC(C)CC1)=O KBTAWWGYJCJSCV-UHFFFAOYSA-N 0.000 description 1
- CRMPOXVAGBGAMB-UHFFFAOYSA-N CCCCC(C1)C1OC(N(C)C)N(C)C Chemical compound CCCCC(C1)C1OC(N(C)C)N(C)C CRMPOXVAGBGAMB-UHFFFAOYSA-N 0.000 description 1
- XPMIKUMIKAYOQP-UHFFFAOYSA-N CCCCOC(N(Cc1n2)C(C(OC)=O)c1cnc2SC)=O Chemical compound CCCCOC(N(Cc1n2)C(C(OC)=O)c1cnc2SC)=O XPMIKUMIKAYOQP-UHFFFAOYSA-N 0.000 description 1
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 (2)
| Publication Number | Publication Date |
|---|---|
| CN104640865A CN104640865A (zh) | 2015-05-20 |
| CN104640865B true CN104640865B (zh) | 2018-05-11 |
Family
ID=49274870
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201380048493.XA Active CN104640865B (zh) | 2012-09-19 | 2013-09-17 | 作为激酶抑制剂的二氢吡咯烷子基-嘧啶 |
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 |
|---|---|---|---|---|
| CA2882410A1 (en) * | 2012-09-19 | 2014-03-27 | Novartis Ag | Dihydropyrrolidino-pyrimidines as kinase inhibitors |
| WO2020011731A1 (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 |
| KR20220042184A (ko) * | 2019-08-01 | 2022-04-04 | 프레테고 인코포레이티드 | 최종 당화 산물의 억제제 |
| SI4073065T1 (sl) | 2019-12-10 | 2025-06-30 | F. Hoffmann-La Roche Ag | Novi derivati metilkinazolinona |
| CA3158541A1 (en) * | 2019-12-10 | 2021-06-17 | Cosimo Dolente | New braf inhibitors as paradox breakers |
| EP4144731B1 (en) * | 2020-04-30 | 2025-01-22 | Suzhou Genhouse Bio Co., Ltd. | Compounds containing benzosultam |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2004078163A2 (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 |
| WO2004007468A1 (en) * | 2002-07-15 | 2004-01-22 | Merck & Co., Inc. | Piperidino pyrimidine dipeptidyl peptidase inhibitors for the treatment of diabetes |
| CA2547080A1 (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 |
| CA2593428C (en) | 2005-01-10 | 2012-04-17 | Pfizer Inc. | Pyrrolopyrazoles, potent kinase inhibitors |
| ES2372976T3 (es) | 2005-12-13 | 2012-01-30 | Schering Corporation | Derivados de indazol policíclicos que son inhibidores de 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 |
| BR112013012175A2 (pt) | 2010-11-17 | 2019-09-24 | Hoffmann La Roche | combinação, coadministração, uso e método |
| US9133187B2 (en) | 2011-02-28 | 2015-09-15 | Array Biopharma Inc. | Serine/threonine kinase inhibitors |
| EP2820017B1 (en) | 2012-03-02 | 2016-12-21 | Genentech, Inc. | Pyridinyl and pyrimidinyl sulfoxide and sulfone derivatives |
| CA2882410A1 (en) * | 2012-09-19 | 2014-03-27 | Novartis Ag | Dihydropyrrolidino-pyrimidines as kinase inhibitors |
-
2013
- 2013-09-17 CA CA2882410A patent/CA2882410A1/en not_active Abandoned
- 2013-09-17 EP EP13771007.5A patent/EP2897961B1/en active Active
- 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 MX MX2015003535A patent/MX2015003535A/es unknown
- 2013-09-17 CN CN201380048493.XA patent/CN104640865B/zh active Active
- 2013-09-17 KR KR1020157006602A patent/KR20150056550A/ko not_active Withdrawn
- 2013-09-17 US US14/428,546 patent/US9546173B2/en active Active
- 2013-09-17 IN IN1328DEN2015 patent/IN2015DN01328A/en unknown
- 2013-09-17 AU AU2013318283A patent/AU2013318283A1/en not_active Abandoned
- 2013-09-17 EA EA201590600A patent/EA201590600A1/ru unknown
- 2013-09-17 WO PCT/US2013/060032 patent/WO2014047020A1/en not_active Ceased
Also Published As
| Publication number | Publication date |
|---|---|
| EP2897961A1 (en) | 2015-07-29 |
| CA2882410A1 (en) | 2014-03-27 |
| AU2013318283A1 (en) | 2015-03-05 |
| ES2612885T3 (es) | 2017-05-19 |
| CN104640865A (zh) | 2015-05-20 |
| IN2015DN01328A (enExample) | 2015-07-03 |
| US9546173B2 (en) | 2017-01-17 |
| WO2014047020A1 (en) | 2014-03-27 |
| EP2897961B1 (en) | 2016-10-26 |
| MX2015003535A (es) | 2015-07-14 |
| KR20150056550A (ko) | 2015-05-26 |
| US20150274733A1 (en) | 2015-10-01 |
| JP2015529248A (ja) | 2015-10-05 |
| JP6186440B2 (ja) | 2017-08-23 |
| EA201590600A1 (ru) | 2015-07-30 |
| BR112015005982A2 (pt) | 2017-07-04 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| EXSB | Decision made by sipo to initiate substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| GR01 | Patent grant | ||
| GR01 | Patent grant |