AR023542A1 - Pirazolbenzodiazepinas - Google Patents

Pirazolbenzodiazepinas

Info

Publication number
AR023542A1
AR023542A1 ARP000101817A ARP000101817A AR023542A1 AR 023542 A1 AR023542 A1 AR 023542A1 AR P000101817 A ARP000101817 A AR P000101817A AR P000101817 A ARP000101817 A AR P000101817A AR 023542 A1 AR023542 A1 AR 023542A1
Authority
AR
Argentina
Prior art keywords
pirazolbenzodiazepinas
pyrazolbenzodiazepines
cdfs
antiproliferatives
colon
Prior art date
Application number
ARP000101817A
Other languages
English (en)
Original Assignee
Hoffmann La Roche
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of AR023542A1 publication Critical patent/AR023542A1/es

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
    • 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)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Oncology (AREA)
  • Urology & Nephrology (AREA)
  • Pulmonology (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

Pirazolbenzodiazepinas que presentan la formula (1) y las sales farmacéuticamente aceptables de las mismas, en donde R1, R2, R3 y R4 son como se handefinido en la memoria, son inhibidores de quinasas dependientes de ciclina (CDFs), en particularCDK2 y son agentes antiproliferativos utiles en eltratamiento o control de los trastornos proliferativos celulares, en particular, tumores de mama, colon, pulmon y prostata.
ARP000101817A 1999-04-21 2000-04-18 Pirazolbenzodiazepinas AR023542A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US13037099P 1999-04-21 1999-04-21

Publications (1)

Publication Number Publication Date
AR023542A1 true AR023542A1 (es) 2002-09-04

Family

ID=22444382

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP000101817A AR023542A1 (es) 1999-04-21 2000-04-18 Pirazolbenzodiazepinas

Country Status (33)

Country Link
US (3) US6440959B1 (es)
EP (1) EP1185529B1 (es)
JP (1) JP3746680B2 (es)
KR (1) KR100481757B1 (es)
CN (2) CN1196703C (es)
AR (1) AR023542A1 (es)
AT (1) ATE279413T1 (es)
AU (1) AU768667B2 (es)
BR (1) BR0009887A (es)
CA (1) CA2367704C (es)
CO (1) CO5170444A1 (es)
CZ (1) CZ20013738A3 (es)
DE (1) DE60014893T2 (es)
DK (1) DK1185529T3 (es)
ES (1) ES2228522T3 (es)
HK (1) HK1046278B (es)
HR (1) HRP20010742A2 (es)
HU (1) HUP0300318A3 (es)
IL (1) IL145764A0 (es)
JO (1) JO2248B1 (es)
MA (1) MA26782A1 (es)
NO (1) NO20015065D0 (es)
NZ (1) NZ514523A (es)
PE (1) PE20010054A1 (es)
PL (1) PL200933B1 (es)
PT (1) PT1185529E (es)
RU (1) RU2249593C2 (es)
SI (1) SI1185529T1 (es)
TR (1) TR200103016T2 (es)
TW (1) TW585866B (es)
WO (1) WO2000064900A1 (es)
YU (1) YU73101A (es)
ZA (1) ZA200108016B (es)

Families Citing this family (33)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE60227185D1 (de) * 2001-11-13 2008-07-31 Ortho Mcneil Pharm Inc Substituierte 1,4-benzodiazepine und ihre anwendung in der krebsbehandlung
FR2847253B1 (fr) * 2002-11-19 2007-05-18 Aventis Pharma Sa Nouveaux derives de pyridazinones a titre de medicaments et compositions pharmaceutiques les renfermant
PL378116A1 (pl) * 2003-02-27 2006-03-06 Abbott Laboratories Heterocykliczne inhibitory kinazy
EP1802625B1 (en) * 2004-10-13 2008-06-18 F. Hoffmann-Roche AG Disubstituted pyrazolobenzodiazepines useful as inhibitors for cdk2 and angiogesis, and for the treatment of breast, colon, lung and prostate cancer
KR20110010813A (ko) * 2005-10-14 2011-02-07 에프. 호프만-라 로슈 아게 5-(2-클로로페닐)-1,2-디히드로-7-플루오로-8-메톡시-3-메틸-피라졸로[3,4-ｂ][1,4] 벤조디아제핀의 투여 섭생
DK2081921T3 (da) 2006-07-10 2011-01-03 Paion Uk Ltd Korttidsvirkende benzodiazepinsalte og deres polymorfe former
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)
EP2809324B1 (en) * 2012-02-02 2018-08-01 Senex Biotechnology, Inc. Cdk8/cdk19 selective inhibitors and their use in anti-metastatic and chemopreventive methods for cancer
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
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
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
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
EP3535253A1 (en) * 2016-11-01 2019-09-11 H. Hoffnabb-La Roche Ag 1,3-dihydro-1,4-benzodiazepine-2-thiones for the treatment of cns related diseases
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
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
TW202100520A (zh) 2019-03-05 2021-01-01 美商英塞特公司 作為cdk2 抑制劑之吡唑基嘧啶基胺化合物
WO2020205560A1 (en) 2019-03-29 2020-10-08 Incyte Corporation Sulfonylamide compounds as cdk2 inhibitors
WO2020223469A1 (en) 2019-05-01 2020-11-05 Incyte Corporation N-(1-(methylsulfonyl)piperidin-4-yl)-4,5-di hydro-1h-imidazo[4,5-h]quinazolin-8-amine derivatives and related compounds as cyclin-dependent kinase 2 (cdk2) inhibitors for treating cancer
US11447494B2 (en) 2019-05-01 2022-09-20 Incyte Corporation Tricyclic amine compounds as CDK2 inhibitors
US11427567B2 (en) 2019-08-14 2022-08-30 Incyte Corporation Imidazolyl pyrimidinylamine compounds as CDK2 inhibitors
CN115298177A (zh) 2019-10-11 2022-11-04 因赛特公司 作为cdk2抑制剂的双环胺
KR20230008792A (ko) * 2020-05-08 2023-01-16 트랜스테라 사이언시즈 (난징), 인크. 항종양 화합물의 합성방법 및 그 중간체
TW202237585A (zh) 2020-11-27 2022-10-01 瑞士商瑞森製藥公司 Ｃｄｋ抑制劑
WO2022149057A1 (en) 2021-01-05 2022-07-14 Rhizen Pharmaceuticals Ag Cdk inhibitors
JP2024517309A (ja) * 2021-05-10 2024-04-19 薬捷安康（南京）科技股▲分▼有限公司 マルチキナーゼ阻害剤の医薬組成物および使用
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

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0929553B1 (en) 1996-10-02 2005-03-16 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

Also Published As

Publication number Publication date
MA26782A1 (fr) 2004-12-20
YU73101A (sh) 2004-05-12
US6838558B2 (en) 2005-01-04
RU2249593C2 (ru) 2005-04-10
EP1185529A1 (en) 2002-03-13
KR20010112435A (ko) 2001-12-20
CN1196703C (zh) 2005-04-13
JP2002543081A (ja) 2002-12-17
NZ514523A (en) 2003-11-28
CN1348455A (zh) 2002-05-08
CN1279029C (zh) 2006-10-11
CN1603314A (zh) 2005-04-06
DK1185529T3 (da) 2005-02-07
PE20010054A1 (es) 2001-02-07
TW585866B (en) 2004-05-01
SI1185529T1 (en) 2005-02-28
HK1046278A1 (en) 2003-01-03
TR200103016T2 (tr) 2002-04-22
CZ20013738A3 (cs) 2002-08-14
CA2367704C (en) 2008-06-17
KR100481757B1 (ko) 2005-04-11
NO20015065L (no) 2001-10-18
US20040198976A1 (en) 2004-10-07
US6916923B2 (en) 2005-07-12
US20020183514A1 (en) 2002-12-05
HUP0300318A3 (en) 2004-11-29
HUP0300318A2 (hu) 2003-06-28
AU4748000A (en) 2000-11-10
PL200933B1 (pl) 2009-02-27
PL354405A1 (en) 2004-01-12
ES2228522T3 (es) 2005-04-16
BR0009887A (pt) 2002-01-22
CA2367704A1 (en) 2000-11-02
JO2248B1 (en) 2004-10-07
PT1185529E (pt) 2005-02-28
JP3746680B2 (ja) 2006-02-15
CO5170444A1 (es) 2002-06-27
ZA200108016B (en) 2003-03-26
DE60014893T2 (de) 2005-10-13
ATE279413T1 (de) 2004-10-15
IL145764A0 (en) 2002-07-25
HK1046278B (zh) 2005-08-12
US6440959B1 (en) 2002-08-27
NO20015065D0 (no) 2001-10-18
WO2000064900A1 (en) 2000-11-02
HRP20010742A2 (en) 2002-12-31
EP1185529B1 (en) 2004-10-13
DE60014893D1 (de) 2004-11-18
AU768667B2 (en) 2003-12-18

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Legal Events

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FA Abandonment or withdrawal