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.)
- Active
Links
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)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen Condensed Heterocyclic Rings (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 (cg-RX-API-DMAC10.html) | 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)
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IN2015DN01328A (cg-RX-API-DMAC10.html) * | 2012-09-19 | 2015-07-03 | Novartis Ag | |
| 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 |
| EP4007632A1 (en) * | 2019-08-01 | 2022-06-08 | Praetego, Inc. | Inhibitors of advanced glycation end products |
| EP4483882A3 (en) | 2019-12-10 | 2025-03-05 | F. Hoffmann-La Roche AG | New methylquinazolinone derivatives |
| CR20220252A (es) * | 2019-12-10 | 2022-07-11 | Hoffmann La Roche | Nuevos inhibidores de braf como rompedores de la paradoja |
| AU2021262977B2 (en) * | 2020-04-30 | 2023-07-13 | Suzhou Genhouse Bio Co., Ltd. | Compounds containing benzosultam |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7208498B2 (en) * | 2002-07-15 | 2007-04-24 | Merck & Co., Inc. | Piperidino pyrimidine dipeptidyl peptidase inhibitors for the treatment of diabetes |
| EP1631260A2 (en) | 2003-02-28 | 2006-03-08 | Transform Pharmaceuticals, Inc. | Pharmaceutical co-crystal compositions of drugs such as carbamazepine, celecoxib, olanzapine, itraconazole, topiramate, modafinil, 5-fluorouracil, hydrochlorothazide, acetaminophen, aspirin, flurbiprofen, phenytoin and ibuprofen |
| WO2005068468A2 (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 |
| BRPI0518509A2 (pt) | 2005-01-10 | 2008-11-25 | Pfizer | pirrolopirazàis, inibidores de cinase potentes |
| AU2006326616B2 (en) | 2005-12-13 | 2012-09-06 | Merck Sharp & Dohme Llc | Polycyclic indazole derivatives that are ERK inhibitors |
| TW200911262A (en) | 2007-06-05 | 2009-03-16 | Schering Corp | Novel compounds that are ERK inhibitors |
| 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 |
| US9133187B2 (en) | 2011-02-28 | 2015-09-15 | Array Biopharma Inc. | Serine/threonine kinase inhibitors |
| AU2013225531A1 (en) | 2012-03-02 | 2014-09-25 | Forma Tm, Llc. | Pyridinyl and pyrimidinyl sulfoxide and sulfone derivatives |
| IN2015DN01328A (cg-RX-API-DMAC10.html) * | 2012-09-19 | 2015-07-03 | Novartis Ag |
-
2013
- 2013-09-17 IN IN1328DEN2015 patent/IN2015DN01328A/en unknown
- 2013-09-17 WO PCT/US2013/060032 patent/WO2014047020A1/en not_active Ceased
- 2013-09-17 JP JP2015533126A patent/JP6186440B2/ja active Active
- 2013-09-17 ES ES13771007.5T patent/ES2612885T3/es active Active
- 2013-09-17 EA EA201590600A patent/EA201590600A1/ru unknown
- 2013-09-17 BR BR112015005982A patent/BR112015005982A2/pt not_active IP Right Cessation
- 2013-09-17 AU AU2013318283A patent/AU2013318283A1/en not_active Abandoned
- 2013-09-17 MX MX2015003535A patent/MX2015003535A/es unknown
- 2013-09-17 CN CN201380048493.XA patent/CN104640865B/zh active Active
- 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 KR KR1020157006602A patent/KR20150056550A/ko not_active Withdrawn
- 2013-09-17 EP EP13771007.5A patent/EP2897961B1/en active Active
Also Published As
| Publication number | Publication date |
|---|---|
| EA201590600A1 (ru) | 2015-07-30 |
| MX2015003535A (es) | 2015-07-14 |
| JP2015529248A (ja) | 2015-10-05 |
| EP2897961B1 (en) | 2016-10-26 |
| CN104640865B (zh) | 2018-05-11 |
| CN104640865A (zh) | 2015-05-20 |
| US9546173B2 (en) | 2017-01-17 |
| EP2897961A1 (en) | 2015-07-29 |
| IN2015DN01328A (cg-RX-API-DMAC10.html) | 2015-07-03 |
| CA2882410A1 (en) | 2014-03-27 |
| ES2612885T3 (es) | 2017-05-19 |
| KR20150056550A (ko) | 2015-05-26 |
| US20150274733A1 (en) | 2015-10-01 |
| BR112015005982A2 (pt) | 2017-07-04 |
| WO2014047020A1 (en) | 2014-03-27 |
| AU2013318283A1 (en) | 2015-03-05 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CN104379575B (zh) | 用于调节egfr活性的化合物和组合物 | |
| JP6186440B2 (ja) | 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 | |
| CA2828478A1 (en) | Serine/threonine kinase inhibitors | |
| TW202523326A (zh) | 雜環及其用途 | |
| CN116685585A (zh) | 一种高活性的hpk1激酶抑制剂 | |
| EP3840747B1 (en) | Novel aryloxypiperidine pyrazole compounds as indoleamine 2,3-dioxygenase inhibitors | |
| AU2016349148C1 (en) | 1,4-dicarbonyl-piperidyl derivatives | |
| TW202220998A (zh) | 雜芳基雜環化合物及其用途 | |
| CN116848115B (zh) | Wnt通路抑制剂化合物 | |
| JP2025527934A (ja) | ピラゾリルスルホンアミド化合物、及び療法におけるそれらの使用 | |
| WO2024044344A1 (en) | Pyridinylsulfonamide compounds and their use in therapy | |
| TWI768781B (zh) | 轉化生長因子－β受體抑制劑 | |
| TW202304906A (zh) | 高活性hpk1激酶抑制劑 | |
| WO2025072437A1 (en) | Heteroaryl compounds and their use in treating medical conditions | |
| CA2989684C (en) | Hpk1 inhibitors and methods of using same | |
| HK40094658B (zh) | 杂芳基杂环化合物及其用途 | |
| HK40094658A (zh) | 杂芳基杂环化合物及其用途 | |
| WO2024059559A1 (en) | Isothiazolylcarboxamide compounds and their use in therapy | |
| WO2025117672A1 (en) | Indazolyl-piperidine sulfonamides and related compounds and their use in therapy | |
| EP4536642A1 (en) | Heterocyclic compounds as pi3ka inhibitors | |
| HK40091563B (zh) | 嘧啶酮类化合物及其用途 | |
| HK40091563A (zh) | 嘧啶酮类化合物及其用途 | |
| JP2023538097A (ja) | ピリミジノン化合物およびその使用 |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20160708 |
|
| A621 | Written request for application examination |
Free format text: JAPANESE INTERMEDIATE CODE: A621 Effective date: 20160708 |
|
| A131 | Notification of reasons for refusal |
Free format text: JAPANESE INTERMEDIATE CODE: A131 Effective date: 20170418 |
|
| A977 | Report on retrieval |
Free format text: JAPANESE INTERMEDIATE CODE: A971007 Effective date: 20170420 |
|
| A524 | Written submission of copy of amendment under article 19 pct |
Free format text: JAPANESE INTERMEDIATE CODE: A524 Effective date: 20170705 |
|
| TRDD | Decision of grant or rejection written | ||
| A01 | Written decision to grant a patent or to grant a registration (utility model) |
Free format text: JAPANESE INTERMEDIATE CODE: A01 Effective date: 20170718 |
|
| A61 | First payment of annual fees (during grant procedure) |
Free format text: JAPANESE INTERMEDIATE CODE: A61 Effective date: 20170731 |
|
| R150 | Certificate of patent or registration of utility model |
Ref document number: 6186440 Country of ref document: JP Free format text: JAPANESE INTERMEDIATE CODE: R150 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |