CN103936745B - Cdk抑制剂 - Google Patents
Cdk抑制剂 Download PDFInfo
- Publication number
- CN103936745B CN103936745B CN201410184792.2A CN201410184792A CN103936745B CN 103936745 B CN103936745 B CN 103936745B CN 201410184792 A CN201410184792 A CN 201410184792A CN 103936745 B CN103936745 B CN 103936745B
- Authority
- CN
- China
- Prior art keywords
- compound
- alkylene
- tert
- methyl
- butyl
- 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 *C(N(*)C(c1c2)=O)([n]1c1c2cnc(NC2=CC=C(*)**2)n1)I Chemical compound *C(N(*)C(c1c2)=O)([n]1c1c2cnc(NC2=CC=C(*)**2)n1)I 0.000 description 7
- FLUIQZWUIHFXTC-OAHLLOKOSA-N CC(C)(C)OC(NC[C@H](c1ccccc1)[n]1c2nc(Cl)ncc2cc1C(O)=O)=O Chemical compound CC(C)(C)OC(NC[C@H](c1ccccc1)[n]1c2nc(Cl)ncc2cc1C(O)=O)=O FLUIQZWUIHFXTC-OAHLLOKOSA-N 0.000 description 1
- OUKQMJJNYMRRHN-UHFFFAOYSA-N CC(C)(CN1)[n]2c3nc(Cl)ncc3cc2C1=O Chemical compound CC(C)(CN1)[n]2c3nc(Cl)ncc3cc2C1=O OUKQMJJNYMRRHN-UHFFFAOYSA-N 0.000 description 1
- NYYTUGICDWNNQC-UHFFFAOYSA-N CC(C)C(CNC(OC(C)(C)C)=O)Nc1nc(Cl)ncc1Br Chemical compound CC(C)C(CNC(OC(C)(C)C)=O)Nc1nc(Cl)ncc1Br NYYTUGICDWNNQC-UHFFFAOYSA-N 0.000 description 1
- JQBISHBIDUIUDU-UHFFFAOYSA-N CC(C)CC(CN1)[n]2c3nc(Nc(cc4)ncc4N4CCNCC4)ncc3cc2C1=O Chemical compound CC(C)CC(CN1)[n]2c3nc(Nc(cc4)ncc4N4CCNCC4)ncc3cc2C1=O JQBISHBIDUIUDU-UHFFFAOYSA-N 0.000 description 1
- CDCCIDIMKJJXEQ-UHFFFAOYSA-N CC(C)CC(CNC(OC(C)(C)C)=O)NC(OCc1ccccc1)=O Chemical compound CC(C)CC(CNC(OC(C)(C)C)=O)NC(OCc1ccccc1)=O CDCCIDIMKJJXEQ-UHFFFAOYSA-N 0.000 description 1
- ZFAHUHCCRUVXJX-UHFFFAOYSA-N CC(C)CN(CC1)CCN1c(cc1)cnc1Nc1nc([n](C2(CCCC2)CNC2=O)c2c2)c2cn1 Chemical compound CC(C)CN(CC1)CCN1c(cc1)cnc1Nc1nc([n](C2(CCCC2)CNC2=O)c2c2)c2cn1 ZFAHUHCCRUVXJX-UHFFFAOYSA-N 0.000 description 1
- GLEGVQXZOJSYSA-UHFFFAOYSA-N CC(C)CN(CC1)CCN1c1ccc(N)nc1 Chemical compound CC(C)CN(CC1)CCN1c1ccc(N)nc1 GLEGVQXZOJSYSA-UHFFFAOYSA-N 0.000 description 1
- HYQWMHHQUXUURL-XCWJXAQQSA-N CCC(C)[C@@H](CN1)[n]2c3nc(Nc(cc4)ncc4N4CCN(C)CC4)ncc3cc2C1=O Chemical compound CCC(C)[C@@H](CN1)[n]2c3nc(Nc(cc4)ncc4N4CCN(C)CC4)ncc3cc2C1=O HYQWMHHQUXUURL-XCWJXAQQSA-N 0.000 description 1
- ABFYPQJZBKJZOQ-BZSJEYESSA-N CCC(C)[C@@H](CNC(OC(C)(C)C)=O)NC(OCc1ccccc1)=O Chemical compound CCC(C)[C@@H](CNC(OC(C)(C)C)=O)NC(OCc1ccccc1)=O ABFYPQJZBKJZOQ-BZSJEYESSA-N 0.000 description 1
- PBXSLSMTGHZLQB-UHFFFAOYSA-N CCOC(C#Cc(c(NC(CC(C)C)CNC(OC(C)(C)C)=O)n1)cnc1Cl)OCC Chemical compound CCOC(C#Cc(c(NC(CC(C)C)CNC(OC(C)(C)C)=O)n1)cnc1Cl)OCC PBXSLSMTGHZLQB-UHFFFAOYSA-N 0.000 description 1
- LYHIBHHOKUUNDF-UHFFFAOYSA-N CCOC(C#Cc(c(NC1(CNC(OC(C)(C)C)=O)CCCC1)n1)cnc1Cl)OCC Chemical compound CCOC(C#Cc(c(NC1(CNC(OC(C)(C)C)=O)CCCC1)n1)cnc1Cl)OCC LYHIBHHOKUUNDF-UHFFFAOYSA-N 0.000 description 1
- PAJAZOMVSJXCNJ-UHFFFAOYSA-N CCOC(C#Cc(c(NC1(CNC(OC(C)(C)C)=O)CCCCC1)n1)cnc1Cl)OCC Chemical compound CCOC(C#Cc(c(NC1(CNC(OC(C)(C)C)=O)CCCCC1)n1)cnc1Cl)OCC PAJAZOMVSJXCNJ-UHFFFAOYSA-N 0.000 description 1
- PBMNQMWMHILVLQ-OAQYLSRUSA-N CN(CC1)CCN1c(cc1)cnc1Nc1ncc(cc(C(NC2)=O)[n]3[C@H]2c2ccccc2)c3n1 Chemical compound CN(CC1)CCN1c(cc1)cnc1Nc1ncc(cc(C(NC2)=O)[n]3[C@H]2c2ccccc2)c3n1 PBMNQMWMHILVLQ-OAQYLSRUSA-N 0.000 description 1
- NCACIGFDMRLLIY-UHFFFAOYSA-N CN(CC1)CCN1c(cc1)cnc1Nc1ncc(cc2[n]3C4(CCCC4)CNC2=O)c3n1 Chemical compound CN(CC1)CCN1c(cc1)cnc1Nc1ncc(cc2[n]3C4(CCCC4)CNC2=O)c3n1 NCACIGFDMRLLIY-UHFFFAOYSA-N 0.000 description 1
- TWTKMJWAXOPXSX-UHFFFAOYSA-N O=C1NCC2(CCCCC2)[n]2c3nc(Nc(cc4)ncc4N4CCNCC4)ncc3cc12 Chemical compound O=C1NCC2(CCCCC2)[n]2c3nc(Nc(cc4)ncc4N4CCNCC4)ncc3cc12 TWTKMJWAXOPXSX-UHFFFAOYSA-N 0.000 description 1
- YWBNHAYIHYUOHN-UHFFFAOYSA-N [O-][N+](c(cc1)ncc1N1CCCCC1)=O Chemical compound [O-][N+](c(cc1)ncc1N1CCCCC1)=O YWBNHAYIHYUOHN-UHFFFAOYSA-N 0.000 description 1
- OJCWRUDJYGWJLU-UHFFFAOYSA-N [O-][N+](c(nc1)ccc1N1CCSCC1)=O Chemical compound [O-][N+](c(nc1)ccc1N1CCSCC1)=O OJCWRUDJYGWJLU-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
- C07D487/12—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 three hetero rings
- C07D487/20—Spiro-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
- A61K31/499—Spiro-condensed pyrazines or piperazines
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
- C07D487/12—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 three hetero rings
- C07D487/14—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D498/14—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Plural Heterocyclic Compounds (AREA)
- Indole Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US40649810P | 2010-10-25 | 2010-10-25 | |
| US61/406,498 | 2010-10-25 | ||
| CN201180062297.9A CN103429243B (zh) | 2010-10-25 | 2011-10-25 | Cdk抑制剂 |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201180062297.9A Division CN103429243B (zh) | 2010-10-25 | 2011-10-25 | Cdk抑制剂 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN103936745A CN103936745A (zh) | 2014-07-23 |
| CN103936745B true CN103936745B (zh) | 2017-04-12 |
Family
ID=46024778
Family Applications (5)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201410184794.1A Pending CN104045654A (zh) | 2010-10-25 | 2011-10-25 | Cdk抑制剂 |
| CN201180062297.9A Active CN103429243B (zh) | 2010-10-25 | 2011-10-25 | Cdk抑制剂 |
| CN201611022263.8A Pending CN106967074A (zh) | 2010-10-25 | 2011-10-25 | Cdk抑制剂 |
| CN201410184792.2A Active CN103936745B (zh) | 2010-10-25 | 2011-10-25 | Cdk抑制剂 |
| CN201610323241.9A Active CN106008533B (zh) | 2010-10-25 | 2011-10-25 | Cdk抑制剂 |
Family Applications Before (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201410184794.1A Pending CN104045654A (zh) | 2010-10-25 | 2011-10-25 | Cdk抑制剂 |
| CN201180062297.9A Active CN103429243B (zh) | 2010-10-25 | 2011-10-25 | Cdk抑制剂 |
| CN201611022263.8A Pending CN106967074A (zh) | 2010-10-25 | 2011-10-25 | Cdk抑制剂 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201610323241.9A Active CN106008533B (zh) | 2010-10-25 | 2011-10-25 | Cdk抑制剂 |
Country Status (25)
| Country | Link |
|---|---|
| US (2) | US8598186B2 (enExample) |
| EP (6) | EP2632467B1 (enExample) |
| JP (4) | JP5923509B2 (enExample) |
| KR (4) | KR20200137048A (enExample) |
| CN (5) | CN104045654A (enExample) |
| AU (5) | AU2011323739B2 (enExample) |
| BR (1) | BR112013010018B1 (enExample) |
| CA (2) | CA2961937C (enExample) |
| CY (1) | CY1118004T1 (enExample) |
| DK (1) | DK2632467T3 (enExample) |
| ES (1) | ES2592515T3 (enExample) |
| HK (2) | HK1197067A1 (enExample) |
| HR (1) | HRP20161092T1 (enExample) |
| HU (1) | HUE030714T2 (enExample) |
| IL (5) | IL225940A0 (enExample) |
| LT (1) | LT2632467T (enExample) |
| MX (4) | MX338327B (enExample) |
| PL (1) | PL2632467T3 (enExample) |
| PT (1) | PT2632467T (enExample) |
| RS (1) | RS55135B1 (enExample) |
| RU (1) | RU2621674C2 (enExample) |
| SG (2) | SG189525A1 (enExample) |
| SI (1) | SI2632467T1 (enExample) |
| SM (1) | SMT201600311B (enExample) |
| WO (1) | WO2012061156A1 (enExample) |
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| AU2006244068B9 (en) | 2005-05-10 | 2012-10-25 | Incyte Holdings Corporation | Modulators of indoleamine 2,3-dioxygenase and methods of using the same |
| SG192485A1 (en) | 2008-07-08 | 2013-08-30 | Incyte Corp | 1,2,5-oxadiazoles as inhibitors of indoleamine 2,3-dioxygenase |
| EP3718560A3 (en) | 2009-05-13 | 2020-12-09 | The University of North Carolina at Chapel Hill | Cyclin dependent kinase inhibitors and methods of use |
| US8691830B2 (en) | 2010-10-25 | 2014-04-08 | G1 Therapeutics, Inc. | CDK inhibitors |
| US9808461B2 (en) | 2010-11-17 | 2017-11-07 | The University Of North Carolina At Chapel Hill | Protection of renal tissues from ischemia through inhibition of the proliferative kinases CDK4 and CDK6 |
| CA2868966C (en) | 2012-03-29 | 2021-01-26 | Francis Xavier Tavares | Lactam kinase inhibitors |
| US10202392B2 (en) * | 2012-04-26 | 2019-02-12 | Francis Xavier Tavares | Synthesis of lactams |
| PE20190736A1 (es) | 2012-06-13 | 2019-05-23 | Incyte Holdings Corp | Compuestos triciclicos sustituidos como inhibidores del receptor del factor de crecimiento de fibroblastos (fgfr) |
| CN105407723A (zh) * | 2013-03-15 | 2016-03-16 | G1治疗公司 | 高效的抗赘生剂和抗增生剂 |
| WO2014144596A2 (en) * | 2013-03-15 | 2014-09-18 | G1 Therapeutics, Inc. | Transient protection of hematopoietic stem and progenitor cells against ionizing radiation |
| WO2014144326A1 (en) | 2013-03-15 | 2014-09-18 | G1 Therapeutics, Inc. | Transient protection of normal cells during chemotherapy |
| KR102269032B1 (ko) | 2013-04-19 | 2021-06-24 | 인사이트 홀딩스 코포레이션 | Fgfr 저해제로서 이환식 헤테로사이클 |
| US20150297606A1 (en) * | 2014-04-17 | 2015-10-22 | G1 Therapeutics, Inc. | Tricyclic Lactams for Use in the Protection of Hematopoietic Stem and Progenitor Cells Against Ionizing Radiation |
| WO2016040858A1 (en) * | 2014-09-12 | 2016-03-17 | G1 Therapeutics, Inc. | Combinations and dosing regimes to treat rb-positive tumors |
| WO2016040848A1 (en) | 2014-09-12 | 2016-03-17 | G1 Therapeutics, Inc. | Treatment of rb-negative tumors using topoisomerase inhibitors in combination with cyclin dependent kinase 4/6 inhibitors |
| US20160220569A1 (en) * | 2015-02-03 | 2016-08-04 | G1 Therapeutics, Inc. | CDK4/6 Inhibitor Dosage Formulations For The Protection Of Hematopoietic Stem And Progenitor Cells During Chemotherapy |
| ES2895769T3 (es) | 2015-02-20 | 2022-02-22 | Incyte Corp | Heterociclos bicíclicos como inhibidores de FGFR |
| MA41551A (fr) | 2015-02-20 | 2017-12-26 | Incyte Corp | Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4 |
| KR20190025943A (ko) * | 2016-07-01 | 2019-03-12 | 쥐원 쎄라퓨틱스, 인크. | 피리미딘-기재 항증식제 |
| WO2018005863A1 (en) * | 2016-07-01 | 2018-01-04 | G1 Therapeutics, Inc. | Pyrimidine-based compounds for the treatment of cancer |
| EA201990189A1 (ru) | 2016-07-01 | 2019-06-28 | Г1 Терапьютикс, Инк. | Синтез n-(гетероарил)пирроло[3,2-d]пиримидин-2-аминов |
| WO2018005533A1 (en) | 2016-07-01 | 2018-01-04 | G1 Therapeutics, Inc. | Antiproliferative pyrimidine-based compounds |
| IL264950B2 (en) | 2016-08-23 | 2024-01-01 | Eisai R&D Man Co Ltd | Combined treatments for the treatment of malignant liver cell carcinoma |
| BR112019005526A2 (pt) | 2016-10-20 | 2019-06-18 | Pfizer | agentes antiproliferativos para tratamento de pah |
| AU2017359333B2 (en) | 2016-11-08 | 2024-03-21 | Dana-Farber Cancer Institute, Inc. | Compositions and methods of modulating anti-tumor immunity |
| DK3505519T3 (da) * | 2016-11-11 | 2022-02-07 | Yangtze River Pharm Group Co | Pyridinamin-substituerede heterotricyclo-forbindelser, fremstilling deraf og anvendelse i medicin |
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| US11395821B2 (en) | 2017-01-30 | 2022-07-26 | G1 Therapeutics, Inc. | Treatment of EGFR-driven cancer with fewer side effects |
| CN110636862A (zh) | 2017-03-16 | 2019-12-31 | 卫材 R&D 管理有限公司 | 用于治疗乳腺癌的组合疗法 |
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| CN109985241B (zh) * | 2017-12-29 | 2024-10-18 | 广州威溶特医药科技有限公司 | Cdk抑制剂和溶瘤病毒在制备抗肿瘤药物的应用 |
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| CN111377935B (zh) * | 2018-12-29 | 2021-06-29 | 武汉光谷通用名药物研究院有限公司 | 选择性cdk4/6抑制剂及其应用 |
| TWI829857B (zh) | 2019-01-29 | 2024-01-21 | 美商英塞特公司 | 作為a2a / a2b抑制劑之吡唑并吡啶及三唑并吡啶 |
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