AR051326A1 - Pirazolobenzodiazepinas disustituidas - Google Patents
Pirazolobenzodiazepinas disustituidasInfo
- Publication number
- AR051326A1 AR051326A1 ARP050104254A ARP050104254A AR051326A1 AR 051326 A1 AR051326 A1 AR 051326A1 AR P050104254 A ARP050104254 A AR P050104254A AR P050104254 A ARP050104254 A AR P050104254A AR 051326 A1 AR051326 A1 AR 051326A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- halogen
- alkoxy
- link
- substituted
- Prior art date
Links
- 125000000217 alkyl group Chemical group 0.000 abstract 9
- 229910052736 halogen Inorganic materials 0.000 abstract 5
- 125000003545 alkoxy group Chemical group 0.000 abstract 4
- 150000002367 halogens Chemical group 0.000 abstract 3
- 125000000623 heterocyclic group Chemical group 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000005843 halogen group Chemical group 0.000 abstract 2
- 206010006187 Breast cancer Diseases 0.000 abstract 1
- 208000026310 Breast neoplasm Diseases 0.000 abstract 1
- 206010009944 Colon cancer Diseases 0.000 abstract 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- JCXJVPUVTGWSNB-UHFFFAOYSA-N Nitrogen dioxide Chemical compound O=[N]=O JCXJVPUVTGWSNB-UHFFFAOYSA-N 0.000 abstract 1
- 206010060862 Prostate cancer Diseases 0.000 abstract 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 abstract 1
- 125000004183 alkoxy alkyl group Chemical group 0.000 abstract 1
- 230000015572 biosynthetic process Effects 0.000 abstract 1
- 210000000481 breast Anatomy 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 1
- 210000001072 colon Anatomy 0.000 abstract 1
- 208000029742 colonic neoplasm Diseases 0.000 abstract 1
- 201000005202 lung cancer Diseases 0.000 abstract 1
- 208000020816 lung neoplasm Diseases 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 210000002307 prostate Anatomy 0.000 abstract 1
- 150000003839 salts Chemical class 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)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (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
Síntesis para la obtencion de tales compuestos, composiciones farmacéuticas que los contienen y usos para tratar el cáncer, en particular el cáncer de mama, de colon, de prostata y de pulmon. Reivindicacion 1: Un compuesto de la formula (1) en la que R1 es alquilo, alcoxi, halogeno, COOH, COO-alquilo, CN, C(O)N(R6)2 u (OCH2CH2)nOCH3;R2 es alquilo, halogeno, alquilo sustituido por halogeno, OH, alcoxi, alcoxi sustituido por halogeno, fenilo, N(R6)2, (OCH2CH2)nOCH3, O(CH2)mNR7R8 o como se muestra en el resto de formula (2) donde C N es un heterociclo de 6 eslabones opcionalmente sustituido por alquilo o C(O)OR6; o bien R1 y R2 juntos forman un anillo heterocíclico de 5 eslabones; R3 es H o alquilo; R4 es H, halogeno, CN, NO2, alquilo o alcoxi; cada R6 con independencia de su aparicion es H o alquilo; R7 y R8 con independencia entre sí son H, alquilo o alcoxialquilo o R7 y R8 junto con el átomo de N al que están unidos forman un heterociclo de 6 eslabones que está opcionalmente sustituido por alquilo; cada n con independencia de su aparicion es 1, 2 o 3; y m es 2, 3 o 4; o una sal farmacéuticamente aceptable del mismo.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US61817404P | 2004-10-13 | 2004-10-13 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR051326A1 true AR051326A1 (es) | 2007-01-03 |
Family
ID=35311946
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP050104254A AR051326A1 (es) | 2004-10-13 | 2005-10-11 | Pirazolobenzodiazepinas disustituidas |
Country Status (25)
| Country | Link |
|---|---|
| US (1) | US7524840B2 (es) |
| EP (1) | EP1802625B1 (es) |
| JP (1) | JP2008515939A (es) |
| KR (1) | KR100858262B1 (es) |
| CN (2) | CN101899049A (es) |
| AR (1) | AR051326A1 (es) |
| AT (1) | ATE398619T1 (es) |
| AU (1) | AU2005293818A1 (es) |
| BR (1) | BRPI0518152A (es) |
| CA (1) | CA2582985A1 (es) |
| DE (1) | DE602005007623D1 (es) |
| DK (1) | DK1802625T3 (es) |
| ES (1) | ES2308551T3 (es) |
| HR (1) | HRP20080429T3 (es) |
| IL (1) | IL182423A0 (es) |
| MX (1) | MX2007004464A (es) |
| NO (1) | NO20071794L (es) |
| NZ (1) | NZ554353A (es) |
| PL (1) | PL1802625T3 (es) |
| PT (1) | PT1802625E (es) |
| RU (1) | RU2394826C2 (es) |
| SI (1) | SI1802625T1 (es) |
| TW (1) | TWI309652B (es) |
| WO (1) | WO2006040036A1 (es) |
| ZA (1) | ZA200702973B (es) |
Families Citing this family (38)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2270014A1 (en) | 2005-09-22 | 2011-01-05 | Incyte Corporation | Azepine inhibitors of janus kinases |
| 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] |
| EP3838903B1 (en) | 2005-12-13 | 2023-11-22 | Incyte Holdings Corporation | Pyrrolo[2,3-d]pyrimidine derivative as janus kinase inhibitor |
| CN101932582B (zh) | 2007-06-13 | 2013-09-25 | 因塞特公司 | 詹纳斯激酶抑制剂(R)-3-(4-(7H-吡咯并[2,3-d]嘧啶-4-基)-1H-吡唑-1-基)-3-环戊基丙腈的盐 |
| 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 |
| US8716303B2 (en) * | 2009-05-22 | 2014-05-06 | Incyte Corporation | N-(hetero)aryl-pyrrolidine derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines and pyrrol-3-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors |
| RS59632B1 (sr) | 2009-05-22 | 2020-01-31 | Incyte Holdings Corp | 3-[4-(7h-pirolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il]oktan- ili heptan-nitril kao jak inhibitori |
| TW201113285A (en) * | 2009-09-01 | 2011-04-16 | Incyte Corp | Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors |
| ME02386B (me) | 2010-03-10 | 2016-09-20 | Incyte Holdings Corp | Derivati piperidin-4-il azetidina kao inhibitori jak1 |
| 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 |
| NZ603686A (en) | 2010-05-21 | 2014-11-28 | Incyte Corp | Topical formulation for a jak inhibitor |
| TW201249845A (en) | 2010-11-19 | 2012-12-16 | Incyte Corp | Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as JAK inhibitors |
| JP5917544B2 (ja) | 2010-11-19 | 2016-05-18 | インサイト・ホールディングス・コーポレイションＩｎｃｙｔｅ Ｈｏｌｄｉｎｇｓ Ｃｏｒｐｏｒａｔｉｏｎ | Ｊａｋ阻害剤としての複素環置換ピロロピリジンおよびピロロピリミジン |
| KR20140040819A (ko) | 2011-06-20 | 2014-04-03 | 인사이트 코포레이션 | Ｊａｋ 저해제로서의 아제티디닐 페닐, 피리딜 또는 피라지닐 카르복스아미드 유도체 |
| 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 |
| US10166191B2 (en) | 2012-11-15 | 2019-01-01 | Incyte Corporation | Sustained-release dosage forms of ruxolitinib |
| DK2964650T3 (en) | 2013-03-06 | 2019-02-11 | Incyte Holdings Corp | PROCEDURES AND INTERMEDIATES FOR THE MANUFACTURE OF A JAK INHIBITOR |
| SI3030227T1 (sl) | 2013-08-07 | 2020-08-31 | Incyte Corporation | Dozirne oblike s podaljšanim sproščanjem za inhibitor JAK1 |
| 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 |
| US11542247B2 (en) | 2015-09-23 | 2023-01-03 | Janssen Pharmaceutica Nv | Bi-heteroaryl substitute 1,4-benzodiazepines and uses thereof for the treatment of cancer |
| ES2811845T3 (es) | 2015-09-23 | 2021-03-15 | Janssen Pharmaceutica Nv | Heterociclos tricíclicos para el tratamiento del cáncer |
| 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 |
| MX2019006942A (es) * | 2016-12-12 | 2019-10-21 | Univ Sydney | Agonistas de receptores de oxitocina no peptidicos. |
| CN108218868B (zh) | 2016-12-13 | 2019-02-19 | 南京药捷安康生物科技有限公司 | 多激酶抑制剂化合物、其晶型及用途 |
| 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 |
| US10596161B2 (en) | 2017-12-08 | 2020-03-24 | Incyte Corporation | Low dose combination therapy for treatment of myeloproliferative neoplasms |
| LT3746429T (lt) | 2018-01-30 | 2022-05-10 | Incyte Corporation | (1-(3-fluor-2-(trifluormetil)izonikotinil)piperidin-4-ono) gamybos būdai |
| MY206999A (en) | 2018-03-30 | 2025-01-23 | Incyte Corp | Treatment of hidradenitis suppurativa using jak inhibitors |
| US11833155B2 (en) | 2020-06-03 | 2023-12-05 | Incyte Corporation | Combination therapy for treatment of myeloproliferative neoplasms |
| 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 |
| IL308314A (en) | 2021-05-07 | 2024-01-01 | Kymera Therapeutics Inc | CDK2 compounds and their uses |
| AU2023326499A1 (en) | 2022-08-17 | 2025-03-27 | Korea Research Institute Of Bioscience And Biotechnology | Compounds for inhibiting or decomposing cdk2 and/or cdk9, and medicinal uses thereof |
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 |
| MC1999A1 (fr) * | 1987-12-18 | 1990-01-26 | Hoffmann La Roche | Composes tricycliques |
| ZA889116B (en) * | 1987-12-18 | 1989-08-30 | Hoffmann La Roche | Tricyclic compounds |
| 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 |
| CN1269818C (zh) * | 2000-12-01 | 2006-08-16 | 味之素株式会社 | 内酰胺化合物及其药物用途 |
-
2005
- 2005-10-04 PL PL05792946T patent/PL1802625T3/pl unknown
- 2005-10-04 NZ NZ554353A patent/NZ554353A/en not_active IP Right Cessation
- 2005-10-04 RU RU2007117770/04A patent/RU2394826C2/ru not_active IP Right Cessation
- 2005-10-04 EP EP05792946A patent/EP1802625B1/en not_active Expired - Lifetime
- 2005-10-04 CA CA002582985A patent/CA2582985A1/en not_active Abandoned
- 2005-10-04 KR KR1020077008406A patent/KR100858262B1/ko not_active Expired - Fee Related
- 2005-10-04 AT AT05792946T patent/ATE398619T1/de active
- 2005-10-04 DE DE602005007623T patent/DE602005007623D1/de not_active Expired - Lifetime
- 2005-10-04 BR BRPI0518152-6A patent/BRPI0518152A/pt not_active IP Right Cessation
- 2005-10-04 ES ES05792946T patent/ES2308551T3/es not_active Expired - Lifetime
- 2005-10-04 JP JP2007536037A patent/JP2008515939A/ja active Pending
- 2005-10-04 DK DK05792946T patent/DK1802625T3/da active
- 2005-10-04 HR HR20080429T patent/HRP20080429T3/xx unknown
- 2005-10-04 CN CN2010101585349A patent/CN101899049A/zh active Pending
- 2005-10-04 SI SI200530331T patent/SI1802625T1/sl unknown
- 2005-10-04 PT PT05792946T patent/PT1802625E/pt unknown
- 2005-10-04 WO PCT/EP2005/010653 patent/WO2006040036A1/en not_active Ceased
- 2005-10-04 MX MX2007004464A patent/MX2007004464A/es active IP Right Grant
- 2005-10-04 CN CN2005800351219A patent/CN101039946B/zh not_active Expired - Fee Related
- 2005-10-04 AU AU2005293818A patent/AU2005293818A1/en not_active Abandoned
- 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 |
|---|---|
| DE602005007623D1 (de) | 2008-07-31 |
| EP1802625A1 (en) | 2007-07-04 |
| ES2308551T3 (es) | 2008-12-01 |
| IL182423A0 (en) | 2007-07-24 |
| TWI309652B (en) | 2009-05-11 |
| BRPI0518152A (pt) | 2008-11-04 |
| CA2582985A1 (en) | 2006-04-20 |
| ZA200702973B (en) | 2009-09-30 |
| CN101899049A (zh) | 2010-12-01 |
| PT1802625E (pt) | 2008-08-06 |
| WO2006040036A1 (en) | 2006-04-20 |
| JP2008515939A (ja) | 2008-05-15 |
| EP1802625B1 (en) | 2008-06-18 |
| PL1802625T3 (pl) | 2008-12-31 |
| HRP20080429T3 (en) | 2008-09-30 |
| KR100858262B1 (ko) | 2008-09-11 |
| MX2007004464A (es) | 2007-05-07 |
| KR20070054243A (ko) | 2007-05-28 |
| HK1108284A1 (en) | 2008-05-02 |
| ATE398619T1 (de) | 2008-07-15 |
| AU2005293818A1 (en) | 2006-04-20 |
| CN101039946B (zh) | 2010-12-08 |
| RU2394826C2 (ru) | 2010-07-20 |
| SI1802625T1 (sl) | 2008-10-31 |
| RU2007117770A (ru) | 2008-11-20 |
| DK1802625T3 (da) | 2008-09-01 |
| TW200628469A (en) | 2006-08-16 |
| NZ554353A (en) | 2010-01-29 |
| US7524840B2 (en) | 2009-04-28 |
| US20060079511A1 (en) | 2006-04-13 |
| CN101039946A (zh) | 2007-09-19 |
| NO20071794L (no) | 2007-07-10 |
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