TR200103016T2 - CDK2 önleyicileri olarak pirazolobenzodiazepinler - Google Patents
CDK2 önleyicileri olarak pirazolobenzodiazepinlerInfo
- Publication number
- TR200103016T2 TR200103016T2 TR2001/03016T TR200103016T TR200103016T2 TR 200103016 T2 TR200103016 T2 TR 200103016T2 TR 2001/03016 T TR2001/03016 T TR 2001/03016T TR 200103016 T TR200103016 T TR 200103016T TR 200103016 T2 TR200103016 T2 TR 200103016T2
- Authority
- TR
- Turkey
- Prior art keywords
- pirazolobenzodiazepines
- formula
- cdk2 inhibitors
- cdk2
- pyrazolobenzodiazepines
- Prior art date
Links
- 102000015792 Cyclin-Dependent Kinase 2 Human genes 0.000 title abstract 2
- 108010024986 Cyclin-Dependent Kinase 2 Proteins 0.000 title abstract 2
- 239000003112 inhibitor Substances 0.000 title 1
- 108091007914 CDKs Proteins 0.000 abstract 2
- 102000003903 Cyclin-dependent kinases Human genes 0.000 abstract 2
- 108090000266 Cyclin-dependent kinases Proteins 0.000 abstract 2
- 208000026310 Breast neoplasm Diseases 0.000 abstract 1
- 230000001028 anti-proliverative effect Effects 0.000 abstract 1
- 208000029162 bladder disease Diseases 0.000 abstract 1
- 210000000481 breast Anatomy 0.000 abstract 1
- 210000001072 colon Anatomy 0.000 abstract 1
- 208000029742 colonic neoplasm Diseases 0.000 abstract 1
- 210000004072 lung Anatomy 0.000 abstract 1
- 208000037841 lung tumor Diseases 0.000 abstract 1
- 208000023958 prostate neoplasm Diseases 0.000 abstract 1
- QBCJSMSLBBCZGU-UHFFFAOYSA-N pyrazolo[3,4-i][1,2]benzodiazepine Chemical class C1=CN=NC2=C3C=NN=C3C=CC2=C1 QBCJSMSLBBCZGU-UHFFFAOYSA-N 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/08—Drugs for disorders of the urinary system of the prostate
-
- 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
- A61P35/04—Antineoplastic agents specific for metastasis
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D243/00—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
- C07D243/06—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
- C07D243/10—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
- C07D243/14—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines
- C07D243/16—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals
- C07D243/18—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals substituted in position 2 by nitrogen, oxygen or sulfur atoms
- C07D243/22—Sulfur atoms
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Oncology (AREA)
- Pulmonology (AREA)
- Urology & Nephrology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
R1, R2, R3 ve R4'ün burada tanimlandigi gibi oldugu formül (I)'e ait yeni pirazolobenzodiazepinler ve bunlarin farmasötik açidan kabul gören tuzlari, sikline bagli kinazlari (CDKler), özellikle de CDK2'yi önler; bunlar, hücre artisi olan bozukluklarin özellikle gögüs, kolon, akciger ve prostat tümörlerinin tedavisinde ya da kontrolünde faydali anti-proliferatif maddelerdir. (FORMÜL VAR)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US13037099P | 1999-04-21 | 1999-04-21 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| TR200103016T2 true TR200103016T2 (tr) | 2002-04-22 |
Family
ID=22444382
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| TR2001/03016T TR200103016T2 (tr) | 1999-04-21 | 2000-04-14 | CDK2 önleyicileri olarak pirazolobenzodiazepinler |
Country Status (33)
| Country | Link |
|---|---|
| US (3) | US6440959B1 (tr) |
| EP (1) | EP1185529B1 (tr) |
| JP (1) | JP3746680B2 (tr) |
| KR (1) | KR100481757B1 (tr) |
| CN (2) | CN1196703C (tr) |
| AR (1) | AR023542A1 (tr) |
| AT (1) | ATE279413T1 (tr) |
| AU (1) | AU768667B2 (tr) |
| BR (1) | BR0009887A (tr) |
| CA (1) | CA2367704C (tr) |
| CO (1) | CO5170444A1 (tr) |
| CZ (1) | CZ20013738A3 (tr) |
| DE (1) | DE60014893T2 (tr) |
| DK (1) | DK1185529T3 (tr) |
| ES (1) | ES2228522T3 (tr) |
| HK (1) | HK1046278B (tr) |
| HR (1) | HRP20010742A2 (tr) |
| HU (1) | HUP0300318A3 (tr) |
| IL (1) | IL145764A0 (tr) |
| JO (1) | JO2248B1 (tr) |
| MA (1) | MA26782A1 (tr) |
| NO (1) | NO20015065L (tr) |
| NZ (1) | NZ514523A (tr) |
| PE (1) | PE20010054A1 (tr) |
| PL (1) | PL200933B1 (tr) |
| PT (1) | PT1185529E (tr) |
| RU (1) | RU2249593C2 (tr) |
| SI (1) | SI1185529T1 (tr) |
| TR (1) | TR200103016T2 (tr) |
| TW (1) | TW585866B (tr) |
| WO (1) | WO2000064900A1 (tr) |
| YU (1) | YU73101A (tr) |
| ZA (1) | ZA200108016B (tr) |
Families Citing this family (36)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6520951B1 (en) | 1996-09-13 | 2003-02-18 | Scimed Life Systems, Inc. | Rapid exchange catheter with detachable hood |
| PT1443937E (pt) * | 2001-11-13 | 2008-09-23 | Ortho Mcneil Janssen Pharm | 1,4-benzodiazepinas substituídas e as suas utilizações para o tratamento de cancro |
| FR2847253B1 (fr) * | 2002-11-19 | 2007-05-18 | Aventis Pharma Sa | Nouveaux derives de pyridazinones a titre de medicaments et compositions pharmaceutiques les renfermant |
| ES2545666T3 (es) * | 2003-02-27 | 2015-09-14 | Abbvie Inc. | 5,10-Dihidro-11H-dibenzo[b,e][1,4]diazepin-11-ona como inhibidores de quinasa |
| WO2006040036A1 (en) * | 2004-10-13 | 2006-04-20 | F. Hoffmann-La Roche Ag | Disubstituted pyrazolobenzodiazepines useful as inhibitors for cdk2 and angiogesis, and for the treatment of breast, colon, lung and prostate cancer |
| BRPI0617252A2 (pt) * | 2005-10-14 | 2011-07-19 | Hoffmann La Roche | regime de administração para benzodiazepina 5-2-clorofenil)-1,2-diidro-7-flìor-8-metóxi-3-metil-pira zolo [3,4-b] [1,4] |
| CA2657347C (en) | 2006-07-10 | 2014-11-18 | Paion Uk Limited | Short-acting benzodiazepine salts and their polymorphic forms |
| KR20100073454A (ko) * | 2008-12-23 | 2010-07-01 | 국립암센터 | 트란스글루타미나제 억제제로 사용되는 신규한 피라졸로디아제핀계 화합물, 이의 제조방법 및 이를 포함하는 조성물 |
| EP2305647A1 (en) * | 2009-09-18 | 2011-04-06 | PAION UK Limited | Process for preparing 3-[(4S)-8-bromo-1-methyl-6-(2-pyridinyl)-4 H-imidazo[1,2-a][1,4]benzodiazepine-4-yl] propionic acid methyl ester or the benzene sulfonate salt thereof, and compounds useful in that process |
| EP2450039A1 (en) | 2010-11-08 | 2012-05-09 | PAION UK Ltd. | Dosing regimen for sedation with CNS 7056 (Remimazolam) |
| UA117342C2 (uk) * | 2012-02-02 | 2018-07-25 | Сенекс Біотекнолоджи Інк. | Селективні інгібітори cdk8/cdk19 та їх застосування як протиметастатичних та хіміопрофілактичних засобів у способах лікування раку |
| CN102603743B (zh) * | 2012-02-24 | 2014-05-28 | 南京天易生物科技有限公司 | 抗肿瘤的氮杂苯并[f]薁衍生物其制备方法及其用途 |
| CN103288828A (zh) * | 2012-02-24 | 2013-09-11 | 中国科学院大连化学物理研究所 | 一种合成手性二氢-6H-吲哚并[2,1-c][1,4]-苯并二氮杂卓的方法 |
| CN103288830A (zh) * | 2012-02-24 | 2013-09-11 | 中国科学院大连化学物理研究所 | 一种合成手性二氢-5H-吡咯并[2,1-c][1,4]-苯并二氮杂卓的方法 |
| AR094963A1 (es) | 2013-03-04 | 2015-09-09 | Ono Pharmaceutical Co | Reacción de oxidación excelente en el índice de conversión |
| CN106608877B (zh) * | 2015-10-21 | 2018-11-13 | 新发药业有限公司 | 一种依鲁替尼中间体4-氨基-3-(4-苯氧基)苯基-1H-吡唑并[3,4-d]嘧啶的制备方法 |
| JP7139323B2 (ja) * | 2016-11-01 | 2022-09-20 | エフ.ホフマン-ラ ロシュ アーゲー | Cns関連疾患を処置するための1,3-ジヒドロ-1,4-ベンゾジアゼピン-2-チオン |
| LT3447056T (lt) * | 2016-12-13 | 2025-07-10 | Transthera Sciences (Nanjing), Inc. | Daugiafunkcių kinazių inhibitoriaus junginys ir jo kristalinė forma bei naudojimas |
| CN109020980B (zh) * | 2017-06-09 | 2020-11-20 | 华东师范大学 | 一类抗肿瘤作用的吡唑并嘧啶二氮*衍生物 |
| US11066404B2 (en) | 2018-10-11 | 2021-07-20 | Incyte Corporation | Dihydropyrido[2,3-d]pyrimidinone compounds as CDK2 inhibitors |
| WO2020168197A1 (en) | 2019-02-15 | 2020-08-20 | Incyte Corporation | Pyrrolo[2,3-d]pyrimidinone compounds as cdk2 inhibitors |
| WO2020180959A1 (en) | 2019-03-05 | 2020-09-10 | Incyte Corporation | Pyrazolyl pyrimidinylamine compounds as cdk2 inhibitors |
| WO2020205560A1 (en) | 2019-03-29 | 2020-10-08 | Incyte Corporation | Sulfonylamide compounds as cdk2 inhibitors |
| US11440914B2 (en) | 2019-05-01 | 2022-09-13 | Incyte Corporation | Tricyclic amine compounds as CDK2 inhibitors |
| WO2020223558A1 (en) * | 2019-05-01 | 2020-11-05 | Incyte Corporation | Tricyclic amine compounds as cdk2 inhibitors |
| TW202115024A (zh) | 2019-08-14 | 2021-04-16 | 美商英塞特公司 | 作為cdk2 抑制劑之咪唑基嘧啶基胺化合物 |
| AU2020364007A1 (en) | 2019-10-11 | 2022-04-28 | Incyte Corporation | Bicyclic amines as CDK2 inhibitors |
| KR20230008792A (ko) * | 2020-05-08 | 2023-01-16 | 트랜스테라 사이언시즈 (난징), 인크. | 항종양 화합물의 합성방법 및 그 중간체 |
| WO2022113003A1 (en) | 2020-11-27 | 2022-06-02 | Rhizen Pharmaceuticals Ag | Cdk inhibitors |
| WO2022149057A1 (en) | 2021-01-05 | 2022-07-14 | Rhizen Pharmaceuticals Ag | Cdk inhibitors |
| AU2022271290A1 (en) | 2021-05-07 | 2023-11-23 | Kymera Therapeutics, Inc. | Cdk2 degraders and uses thereof |
| KR20240006610A (ko) * | 2021-05-10 | 2024-01-15 | 트랜스테라 사이언시즈 (난징), 인크. | 다중-키나제 억제제의 제약 조성물 및 용도 |
| US11981671B2 (en) | 2021-06-21 | 2024-05-14 | Incyte Corporation | Bicyclic pyrazolyl amines as CDK2 inhibitors |
| US11976073B2 (en) | 2021-12-10 | 2024-05-07 | Incyte Corporation | Bicyclic amines as CDK2 inhibitors |
| WO2024030399A2 (en) * | 2022-08-02 | 2024-02-08 | Lab1636, Llc | Use of a gaba-a pam for reduction of tactile hypersensitivity |
| WO2026024674A1 (en) | 2024-07-22 | 2026-01-29 | Genesis Therapeutics, Inc. | Methods of treating skp2-associated cancers |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2071092A1 (en) * | 1991-06-14 | 1992-12-15 | Roger M. Freidinger | 1,4-benzodiazepines with 5-membered heterocyclic rings |
| US6251911B1 (en) | 1996-10-02 | 2001-06-26 | Novartis Ag | Pyrimidine derivatives and processes for the preparation thereof |
| US6350786B1 (en) * | 1998-09-22 | 2002-02-26 | Hoffmann-La Roche Inc. | Stable complexes of poorly soluble compounds in ionic polymers |
-
2000
- 2000-04-12 US US09/548,091 patent/US6440959B1/en not_active Expired - Fee Related
- 2000-04-14 RU RU2001130446/04A patent/RU2249593C2/ru not_active IP Right Cessation
- 2000-04-14 PL PL354405A patent/PL200933B1/pl not_active IP Right Cessation
- 2000-04-14 CN CNB008065543A patent/CN1196703C/zh not_active Expired - Fee Related
- 2000-04-14 TR TR2001/03016T patent/TR200103016T2/tr unknown
- 2000-04-14 SI SI200030524T patent/SI1185529T1/xx unknown
- 2000-04-14 HU HU0300318A patent/HUP0300318A3/hu unknown
- 2000-04-14 CZ CZ20013738A patent/CZ20013738A3/cs unknown
- 2000-04-14 HK HK02107815.6A patent/HK1046278B/zh not_active IP Right Cessation
- 2000-04-14 JP JP2000614252A patent/JP3746680B2/ja not_active Expired - Fee Related
- 2000-04-14 KR KR10-2001-7013228A patent/KR100481757B1/ko not_active Expired - Fee Related
- 2000-04-14 CA CA002367704A patent/CA2367704C/en not_active Expired - Fee Related
- 2000-04-14 WO PCT/EP2000/003394 patent/WO2000064900A1/en not_active Ceased
- 2000-04-14 AT AT00929360T patent/ATE279413T1/de active
- 2000-04-14 IL IL14576400A patent/IL145764A0/xx unknown
- 2000-04-14 ES ES00929360T patent/ES2228522T3/es not_active Expired - Lifetime
- 2000-04-14 CN CNB2004100682242A patent/CN1279029C/zh not_active Expired - Fee Related
- 2000-04-14 HR HR20010742A patent/HRP20010742A2/hr not_active Application Discontinuation
- 2000-04-14 BR BR0009887-6A patent/BR0009887A/pt not_active IP Right Cessation
- 2000-04-14 YU YU73101A patent/YU73101A/sh unknown
- 2000-04-14 DE DE60014893T patent/DE60014893T2/de not_active Expired - Lifetime
- 2000-04-14 NZ NZ514523A patent/NZ514523A/en unknown
- 2000-04-14 PT PT00929360T patent/PT1185529E/pt unknown
- 2000-04-14 AU AU47480/00A patent/AU768667B2/en not_active Ceased
- 2000-04-14 EP EP00929360A patent/EP1185529B1/en not_active Expired - Lifetime
- 2000-04-14 DK DK00929360T patent/DK1185529T3/da active
- 2000-04-17 JO JO200054A patent/JO2248B1/en active
- 2000-04-18 AR ARP000101817A patent/AR023542A1/es not_active Application Discontinuation
- 2000-04-18 CO CO00028559A patent/CO5170444A1/es not_active Application Discontinuation
- 2000-04-19 TW TW089107370A patent/TW585866B/zh not_active IP Right Cessation
- 2000-04-19 PE PE2000000370A patent/PE20010054A1/es not_active Application Discontinuation
-
2001
- 2001-09-29 ZA ZA200108016A patent/ZA200108016B/xx unknown
- 2001-10-18 NO NO20015065A patent/NO20015065L/no not_active Application Discontinuation
- 2001-10-19 MA MA26368A patent/MA26782A1/fr unknown
-
2002
- 2002-04-15 US US10/122,559 patent/US6838558B2/en not_active Expired - Fee Related
-
2004
- 2004-04-19 US US10/827,667 patent/US6916923B2/en not_active Expired - Fee Related
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