BRPI0518152A - pirazolbenzodiazepinas dissubstituìdas úteis como inibidores para cdk2 e angiogênese e para o tratamento de cánceres de mama, cólon, pulmão e próstata - Google Patents
pirazolbenzodiazepinas dissubstituìdas úteis como inibidores para cdk2 e angiogênese e para o tratamento de cánceres de mama, cólon, pulmão e próstataInfo
- Publication number
- BRPI0518152A BRPI0518152A BRPI0518152-6A BRPI0518152A BRPI0518152A BR PI0518152 A BRPI0518152 A BR PI0518152A BR PI0518152 A BRPI0518152 A BR PI0518152A BR PI0518152 A BRPI0518152 A BR PI0518152A
- Authority
- BR
- Brazil
- Prior art keywords
- colon
- cdk2
- breast
- angiogenesis
- lung
- Prior art date
Links
- 206010006187 Breast cancer Diseases 0.000 title abstract 3
- 208000026310 Breast neoplasm Diseases 0.000 title abstract 3
- 208000000236 Prostatic Neoplasms Diseases 0.000 title abstract 3
- 230000033115 angiogenesis Effects 0.000 title abstract 3
- 210000000481 breast Anatomy 0.000 title abstract 3
- 210000001072 colon Anatomy 0.000 title abstract 3
- 208000029742 colonic neoplasm Diseases 0.000 title abstract 3
- 208000020816 lung neoplasm Diseases 0.000 title abstract 3
- 239000003112 inhibitor Substances 0.000 title abstract 2
- 210000004072 lung Anatomy 0.000 title abstract 2
- 101150073031 cdk2 gene Proteins 0.000 title 1
- 102000015792 Cyclin-Dependent Kinase 2 Human genes 0.000 abstract 2
- 108010024986 Cyclin-Dependent Kinase 2 Proteins 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 230000002401 inhibitory effect Effects 0.000 abstract 2
- 206010009944 Colon cancer Diseases 0.000 abstract 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 206010060862 Prostate cancer Diseases 0.000 abstract 1
- 102000001253 Protein Kinase Human genes 0.000 abstract 1
- 230000015572 biosynthetic process Effects 0.000 abstract 1
- 201000005202 lung cancer Diseases 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 210000002307 prostate Anatomy 0.000 abstract 1
- 108060006633 protein kinase Proteins 0.000 abstract 1
- 238000003786 synthesis reaction Methods 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
- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
- A61K31/5513—1,4-Benzodiazepines, e.g. diazepam or clozapine
- A61K31/5517—1,4-Benzodiazepines, e.g. diazepam or clozapine condensed with five-membered rings having nitrogen as a ring hetero atom, e.g. imidazobenzodiazepines, triazolam
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
PIRAZOLBENZODIAZEPINAS DISSUBSTITUìDAS úTEIS COMO INIBIDORES PARA CDK2 E ANGIOGéNESE E PARA O TRATAMENTO DE CáNCERES DE MAMA, CóLON, PULMãO E PRóS-TATA. A presente invenção provê compostos da fórmula (I) onde R, R, R e R¬ 4¬ são descritos aqui. A invenção também provê síntese para preparação de tais compostos e composições farmacêuticas contendoos. A invenção provê ainda métodos para inibição de cinases, em particular CDK2, para inibição de angiogênese e para tratamento de cânceres, em particular cânceres de mama, cólon, próstata e pulmão.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US61817404P | 2004-10-13 | 2004-10-13 | |
| PCT/EP2005/010653 WO2006040036A1 (en) | 2004-10-13 | 2005-10-04 | Disubstituted pyrazolobenzodiazepines useful as inhibitors for cdk2 and angiogesis, and for the treatment of breast, colon, lung and prostate cancer |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BRPI0518152A true BRPI0518152A (pt) | 2008-11-04 |
Family
ID=35311946
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BRPI0518152-6A BRPI0518152A (pt) | 2004-10-13 | 2005-10-04 | pirazolbenzodiazepinas dissubstituìdas úteis como inibidores para cdk2 e angiogênese e para o tratamento de cánceres de mama, cólon, pulmão e próstata |
Country Status (25)
| Country | Link |
|---|---|
| US (1) | US7524840B2 (pt) |
| EP (1) | EP1802625B1 (pt) |
| JP (1) | JP2008515939A (pt) |
| KR (1) | KR100858262B1 (pt) |
| CN (2) | CN101039946B (pt) |
| AR (1) | AR051326A1 (pt) |
| AT (1) | ATE398619T1 (pt) |
| AU (1) | AU2005293818A1 (pt) |
| BR (1) | BRPI0518152A (pt) |
| CA (1) | CA2582985A1 (pt) |
| DE (1) | DE602005007623D1 (pt) |
| DK (1) | DK1802625T3 (pt) |
| ES (1) | ES2308551T3 (pt) |
| HR (1) | HRP20080429T3 (pt) |
| IL (1) | IL182423A0 (pt) |
| MX (1) | MX2007004464A (pt) |
| NO (1) | NO20071794L (pt) |
| NZ (1) | NZ554353A (pt) |
| PL (1) | PL1802625T3 (pt) |
| PT (1) | PT1802625E (pt) |
| RU (1) | RU2394826C2 (pt) |
| SI (1) | SI1802625T1 (pt) |
| TW (1) | TWI309652B (pt) |
| WO (1) | WO2006040036A1 (pt) |
| ZA (1) | ZA200702973B (pt) |
Families Citing this family (38)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP5119154B2 (ja) * | 2005-09-22 | 2013-01-16 | インサイト・コーポレイション | Janusキナーゼの四環系阻害剤 |
| EP1940410A1 (en) * | 2005-10-14 | 2008-07-09 | F.Hoffmann-La Roche Ag | Regimen of administration for 5-(2-chlorophenyl)-1 ,2-dihydro-7-fluoro-8-methoxy-3-methyl-pyrazolo [3, 4.-b] [1, 4] benzodiazepine |
| TWI630207B (zh) | 2005-12-13 | 2018-07-21 | 英塞特控股公司 | 作為傑納斯激酶(JANUS KINASE)抑制劑之經雜芳基取代之吡咯并〔2,3-b〕吡啶及吡咯并〔2,3-b〕嘧啶 |
| EP3070090B1 (en) | 2007-06-13 | 2018-12-12 | Incyte Holdings Corporation | Use of salts of the janus kinase inhibitor (r)-3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h- pyrazol-1-yl)-3- cyclopentylpropanenitrile |
| CL2009001884A1 (es) * | 2008-10-02 | 2010-05-14 | Incyte Holdings Corp | Uso de 3-ciclopentil-3-[4-(7h-pirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il)propanonitrilo, inhibidor de janus quinasa, y uso de una composición que lo comprende para el tratamiento del ojo seco. |
| KR20100073454A (ko) * | 2008-12-23 | 2010-07-01 | 국립암센터 | 트란스글루타미나제 억제제로 사용되는 신규한 피라졸로디아제핀계 화합물, 이의 제조방법 및 이를 포함하는 조성물 |
| EP3643312A1 (en) | 2009-05-22 | 2020-04-29 | Incyte Holdings Corporation | 3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl]octane- or heptane-nitrile as jak inhibitors |
| AR076794A1 (es) | 2009-05-22 | 2011-07-06 | Incyte Corp | Derivados de n-(hetero)aril-pirrolidina de pirazol-4-il-pirrolo [2,3-d]pirimidinas y pirrol-3-il-pirrolo [2,3-d ]pirimidinas como inhibidores de la quinasa janus y composiciones farmaceuticas que los contienen |
| AR078012A1 (es) * | 2009-09-01 | 2011-10-05 | Incyte Corp | Derivados heterociclicos de las pirazol-4-il- pirrolo (2,3-d) pirimidinas como inhibidores de la quinasa janus |
| EP3050882B1 (en) | 2010-03-10 | 2018-01-31 | Incyte Holdings Corporation | Piperidin-4-yl azetidine derivatives as jak1 inhibitors |
| JP2011201794A (ja) * | 2010-03-24 | 2011-10-13 | Fujifilm Corp | 5−アミノピラゾール誘導体及びその塩の製造方法 |
| SG10201503983QA (en) | 2010-05-21 | 2015-06-29 | Incyte Corp | Topical Formulation for a JAK Inhibitor |
| US9034884B2 (en) | 2010-11-19 | 2015-05-19 | Incyte Corporation | Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as JAK inhibitors |
| CN103415515B (zh) | 2010-11-19 | 2015-08-26 | 因塞特公司 | 作为jak抑制剂的环丁基取代的吡咯并吡啶和吡咯并嘧啶衍生物 |
| PE20140832A1 (es) | 2011-06-20 | 2014-07-14 | Incyte Corp | Derivados de azetidinil fenil, piridil o pirazinil carboxamida como inhibidores de jak |
| TW201313721A (zh) | 2011-08-18 | 2013-04-01 | Incyte Corp | 作為jak抑制劑之環己基氮雜環丁烷衍生物 |
| UA111854C2 (uk) | 2011-09-07 | 2016-06-24 | Інсайт Холдінгс Корпорейшн | Способи і проміжні сполуки для отримання інгібіторів jak |
| 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 |
| TW201406761A (zh) | 2012-05-18 | 2014-02-16 | Incyte Corp | 做爲jak抑制劑之哌啶基環丁基取代之吡咯并吡啶及吡咯并嘧啶衍生物 |
| CN103626761B (zh) * | 2012-08-24 | 2015-07-29 | 上海医药工业研究院 | 苯并吡啶氮杂卓类化合物及其作为抗肿瘤药物的应用 |
| PL2919766T3 (pl) | 2012-11-15 | 2021-10-04 | Incyte Holdings Corporation | Postacie dawkowania ruksolitynibu o przedłużonym uwalnianiu |
| CN105189509B (zh) | 2013-03-06 | 2017-12-19 | 因赛特公司 | 用于制备jak抑制剂的方法及中间体 |
| SG10201912203XA (en) | 2013-08-07 | 2020-02-27 | Incyte Corp | Sustained release dosage forms for a jak1 inhibitor |
| WO2015184305A1 (en) | 2014-05-30 | 2015-12-03 | Incyte Corporation | TREATMENT OF CHRONIC NEUTROPHILIC LEUKEMIA (CNL) AND ATYPICAL CHRONIC MYELOID LEUKEMIA (aCML) BY INHIBITORS OF JAK1 |
| EP3353164B1 (en) | 2015-09-23 | 2021-11-03 | Janssen Pharmaceutica, N.V. | Bi-heteroaryl substituted 1,4-benzodiazepines and uses thereof for the treatment of cancer |
| CA2996857C (en) * | 2015-09-23 | 2024-05-21 | Janssen Pharmaceutica Nv | Quinoxaline, quinoline and quinazolinone derivative compounds for the treatment of cancer |
| CN106928040A (zh) * | 2015-12-31 | 2017-07-07 | 上海医药工业研究院 | Sglt2抑制剂中间体的制备方法 |
| FI3551631T3 (fi) * | 2016-12-12 | 2025-01-16 | Kinoxis Therapeutics Pty Ltd | Ei-peptidit-oksytosiinireseptoriagonistit |
| JP6594571B2 (ja) * | 2016-12-13 | 2019-10-23 | 南京薬捷安康生物科技有限公司 | マルチキナーゼ阻害剤化合物、並びにその結晶形及びその使用 |
| 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 |
| WO2019113487A1 (en) | 2017-12-08 | 2019-06-13 | Incyte Corporation | Low dose combination therapy for treatment of myeloproliferative neoplasms |
| EP3746429B1 (en) | 2018-01-30 | 2022-03-09 | Incyte Corporation | Processes for preparing (1-(3-fluoro-2-(trifluoromethyl)isonicotinyl)piperidine-4-one) |
| PT3773593T (pt) | 2018-03-30 | 2024-06-25 | Incyte Corp | Tratamento da hidradenite supurativa com inibidores de jak |
| US11833155B2 (en) | 2020-06-03 | 2023-12-05 | Incyte Corporation | Combination therapy for treatment of myeloproliferative neoplasms |
| AR124154A1 (es) | 2020-11-27 | 2023-02-22 | Rhizen Pharmaceuticals Ag | Inhibidores de cdk |
| WO2022149057A1 (en) | 2021-01-05 | 2022-07-14 | Rhizen Pharmaceuticals Ag | Cdk inhibitors |
| KR20240020735A (ko) | 2021-05-07 | 2024-02-15 | 카이메라 쎄라퓨틱스 인코포레이티드 | Cdk2 분해제 및 그 용도 |
| CN120051473A (zh) | 2022-08-17 | 2025-05-27 | 韩国化学研究院 | 抑制或降解cdk2和/或cdk9的化合物及其医学用途 |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3681341A (en) | 1970-12-23 | 1972-08-01 | Hoffmann La Roche | Process for preparing 1-lower alkyl-1,4-benzodiazepin-2-ones |
| ZA889116B (en) * | 1987-12-18 | 1989-08-30 | Hoffmann La Roche | Tricyclic compounds |
| MC1999A1 (fr) * | 1987-12-18 | 1990-01-26 | Hoffmann La Roche | Composes tricycliques |
| US5625031A (en) | 1994-02-08 | 1997-04-29 | Bristol-Myers Squibb Company | Peptide inhibitors of the p33cdk2 and p34cdc2 cell cycle regulatory kinases and human papillomavirus E7 oncoprotein |
| US5631156A (en) | 1994-06-21 | 1997-05-20 | The University Of Michigan | DNA encoding and 18 KD CDK6 inhibiting protein |
| US5733920A (en) | 1995-10-31 | 1998-03-31 | Mitotix, Inc. | Inhibitors of cyclin dependent kinases |
| FR2741881B1 (fr) | 1995-12-01 | 1999-07-30 | Centre Nat Rech Scient | Nouveaux derives de purine possedant notamment des prorietes anti-proliferatives et leurs applications biologiques |
| US5866702A (en) | 1996-08-02 | 1999-02-02 | Cv Therapeutics, Incorporation | Purine inhibitors of cyclin dependent kinase 2 |
| US6440959B1 (en) | 1999-04-21 | 2002-08-27 | Hoffman-La Roche Inc. | Pyrazolobenzodiazepines |
| JP3826400B2 (ja) * | 2000-12-01 | 2006-09-27 | 味の素株式会社 | ラクタム化合物及びその医薬用途 |
-
2005
- 2005-10-04 RU RU2007117770/04A patent/RU2394826C2/ru not_active IP Right Cessation
- 2005-10-04 CN CN2005800351219A patent/CN101039946B/zh not_active Expired - Fee Related
- 2005-10-04 BR BRPI0518152-6A patent/BRPI0518152A/pt not_active IP Right Cessation
- 2005-10-04 PT PT05792946T patent/PT1802625E/pt unknown
- 2005-10-04 JP JP2007536037A patent/JP2008515939A/ja active Pending
- 2005-10-04 WO PCT/EP2005/010653 patent/WO2006040036A1/en not_active Ceased
- 2005-10-04 ES ES05792946T patent/ES2308551T3/es not_active Expired - Lifetime
- 2005-10-04 KR KR1020077008406A patent/KR100858262B1/ko not_active Expired - Fee Related
- 2005-10-04 MX MX2007004464A patent/MX2007004464A/es active IP Right Grant
- 2005-10-04 CN CN2010101585349A patent/CN101899049A/zh active Pending
- 2005-10-04 EP EP05792946A patent/EP1802625B1/en not_active Expired - Lifetime
- 2005-10-04 AT AT05792946T patent/ATE398619T1/de active
- 2005-10-04 DK DK05792946T patent/DK1802625T3/da active
- 2005-10-04 CA CA002582985A patent/CA2582985A1/en not_active Abandoned
- 2005-10-04 PL PL05792946T patent/PL1802625T3/pl unknown
- 2005-10-04 DE DE602005007623T patent/DE602005007623D1/de not_active Expired - Lifetime
- 2005-10-04 AU AU2005293818A patent/AU2005293818A1/en not_active Abandoned
- 2005-10-04 NZ NZ554353A patent/NZ554353A/en not_active IP Right Cessation
- 2005-10-04 HR HR20080429T patent/HRP20080429T3/xx unknown
- 2005-10-04 SI SI200530331T patent/SI1802625T1/sl unknown
- 2005-10-05 US US11/244,251 patent/US7524840B2/en not_active Expired - Fee Related
- 2005-10-11 AR ARP050104254A patent/AR051326A1/es not_active Application Discontinuation
- 2005-10-12 TW TW094135532A patent/TWI309652B/zh not_active IP Right Cessation
-
2007
- 2007-04-03 NO NO20071794A patent/NO20071794L/no not_active Application Discontinuation
- 2007-04-10 IL IL182423A patent/IL182423A0/en unknown
- 2007-04-11 ZA ZA200702973A patent/ZA200702973B/xx unknown
Also Published As
| Publication number | Publication date |
|---|---|
| MX2007004464A (es) | 2007-05-07 |
| DE602005007623D1 (de) | 2008-07-31 |
| RU2394826C2 (ru) | 2010-07-20 |
| WO2006040036A1 (en) | 2006-04-20 |
| EP1802625A1 (en) | 2007-07-04 |
| CN101039946B (zh) | 2010-12-08 |
| AU2005293818A1 (en) | 2006-04-20 |
| NZ554353A (en) | 2010-01-29 |
| PL1802625T3 (pl) | 2008-12-31 |
| EP1802625B1 (en) | 2008-06-18 |
| JP2008515939A (ja) | 2008-05-15 |
| RU2007117770A (ru) | 2008-11-20 |
| IL182423A0 (en) | 2007-07-24 |
| KR20070054243A (ko) | 2007-05-28 |
| SI1802625T1 (sl) | 2008-10-31 |
| ZA200702973B (en) | 2009-09-30 |
| US7524840B2 (en) | 2009-04-28 |
| CN101039946A (zh) | 2007-09-19 |
| US20060079511A1 (en) | 2006-04-13 |
| CA2582985A1 (en) | 2006-04-20 |
| PT1802625E (pt) | 2008-08-06 |
| CN101899049A (zh) | 2010-12-01 |
| AR051326A1 (es) | 2007-01-03 |
| KR100858262B1 (ko) | 2008-09-11 |
| TW200628469A (en) | 2006-08-16 |
| ATE398619T1 (de) | 2008-07-15 |
| TWI309652B (en) | 2009-05-11 |
| ES2308551T3 (es) | 2008-12-01 |
| DK1802625T3 (da) | 2008-09-01 |
| NO20071794L (no) | 2007-07-10 |
| HK1108284A1 (en) | 2008-05-02 |
| HRP20080429T3 (en) | 2008-09-30 |
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