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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- Prior art keywords
- alkyl
- compound
- cycloalkyl
- independently
- mmol
- Prior art date
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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)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Oncology (AREA)
- Hematology (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 (https=) |
| EP (1) | EP2897961B1 (https=) |
| JP (1) | JP6186440B2 (https=) |
| KR (1) | KR20150056550A (https=) |
| CN (1) | CN104640865B (https=) |
| AU (1) | AU2013318283A1 (https=) |
| BR (1) | BR112015005982A2 (https=) |
| CA (1) | CA2882410A1 (https=) |
| EA (1) | EA201590600A1 (https=) |
| ES (1) | ES2612885T3 (https=) |
| IN (1) | IN2015DN01328A (https=) |
| MX (1) | MX2015003535A (https=) |
| WO (1) | WO2014047020A1 (https=) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2612885T3 (es) * | 2012-09-19 | 2017-05-19 | Novartis Ag | Dihidro-pirrolidino-pirimidinas como inhibidoras de cinasa |
| JP7349491B2 (ja) * | 2018-07-12 | 2023-09-22 | ユーシービー バイオファルマ エスアールエル | Ｉｌ－１７モジュレーターとしてのスピロ環状インダン類似体 |
| WO2020243457A1 (en) * | 2019-05-29 | 2020-12-03 | Viogen Biosciences, Llc | Compounds and therapeutic uses thereof |
| CN120247783A (zh) * | 2019-08-01 | 2025-07-04 | 普拉特戈公司 | 晚期糖基化终产物的抑制剂 |
| PH12022551118A1 (en) * | 2019-12-10 | 2023-09-18 | Hoffmann La Roche | New braf inhibitors as paradox breakers |
| PL4073065T3 (pl) | 2019-12-10 | 2025-05-19 | F. Hoffmann-La Roche Ag | Nowe pochodne metylochinazolinonu |
| WO2021218912A1 (zh) | 2020-04-30 | 2021-11-04 | 南京明德新药研发有限公司 | 含苯基并内磺酰胺的化合物 |
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 |
| US7208498B2 (en) * | 2002-07-15 | 2007-04-24 | 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 |
| AU2005323797B2 (en) | 2005-01-10 | 2009-07-09 | Pfizer Inc. | Pyrrolopyrazoles, potent kinase inhibitors |
| HRP20110892T1 (hr) | 2005-12-13 | 2011-12-31 | Schering Corporation | Policiklični derivati indazola koji su inhibitori 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 |
| WO2012030685A2 (en) | 2010-09-01 | 2012-03-08 | Schering Corporation | 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 |
| KR20130121122A (ko) | 2010-11-17 | 2013-11-05 | 에프. 호프만-라 로슈 아게 | 종양의 치료 방법 |
| 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 |
| ES2620612T3 (es) * | 2012-03-02 | 2017-06-29 | Genentech, Inc. | Derivados de sulfóxidos y sulfonas de piridinilo y pirimidinilo |
| ES2612885T3 (es) * | 2012-09-19 | 2017-05-19 | Novartis Ag | Dihidro-pirrolidino-pirimidinas como inhibidoras de cinasa |
-
2013
- 2013-09-17 ES ES13771007.5T patent/ES2612885T3/es active Active
- 2013-09-17 US US14/428,546 patent/US9546173B2/en active Active
- 2013-09-17 AU AU2013318283A patent/AU2013318283A1/en not_active Abandoned
- 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 EP EP13771007.5A patent/EP2897961B1/en active Active
- 2013-09-17 KR KR1020157006602A patent/KR20150056550A/ko not_active Withdrawn
- 2013-09-17 CA CA2882410A patent/CA2882410A1/en not_active Abandoned
- 2013-09-17 WO PCT/US2013/060032 patent/WO2014047020A1/en not_active Ceased
- 2013-09-17 CN CN201380048493.XA patent/CN104640865B/zh active Active
- 2013-09-17 EA EA201590600A patent/EA201590600A1/ru unknown
- 2013-09-17 MX MX2015003535A patent/MX2015003535A/es unknown
- 2013-09-17 IN IN1328DEN2015 patent/IN2015DN01328A/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| IN2015DN01328A (https=) | 2015-07-03 |
| MX2015003535A (es) | 2015-07-14 |
| US9546173B2 (en) | 2017-01-17 |
| EA201590600A1 (ru) | 2015-07-30 |
| CN104640865A (zh) | 2015-05-20 |
| ES2612885T3 (es) | 2017-05-19 |
| EP2897961A1 (en) | 2015-07-29 |
| AU2013318283A1 (en) | 2015-03-05 |
| BR112015005982A2 (pt) | 2017-07-04 |
| JP2015529248A (ja) | 2015-10-05 |
| CA2882410A1 (en) | 2014-03-27 |
| JP6186440B2 (ja) | 2017-08-23 |
| WO2014047020A1 (en) | 2014-03-27 |
| KR20150056550A (ko) | 2015-05-26 |
| US20150274733A1 (en) | 2015-10-01 |
| EP2897961B1 (en) | 2016-10-26 |
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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 |