CN106029672B - 丝氨酸/苏氨酸激酶抑制剂 - Google Patents

丝氨酸/苏氨酸激酶抑制剂 Download PDF

Info

Publication number
CN106029672B
CN106029672B CN201480074890.9A CN201480074890A CN106029672B CN 106029672 B CN106029672 B CN 106029672B CN 201480074890 A CN201480074890 A CN 201480074890A CN 106029672 B CN106029672 B CN 106029672B
Authority
CN
China
Prior art keywords
methyl
base
pyrazol
compound
dihydro
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.)
Active
Application number
CN201480074890.9A
Other languages
English (en)
Chinese (zh)
Other versions
CN106029672A (zh
Inventor
A·科莱斯尼科夫
S·多
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Genentech Inc
Original Assignee
Genentech Inc
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 Genentech Inc filed Critical Genentech Inc
Publication of CN106029672A publication Critical patent/CN106029672A/zh
Application granted granted Critical
Publication of CN106029672B publication Critical patent/CN106029672B/zh
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/53Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5365Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/542Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/553Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/12Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
    • C07D471/16Peri-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12Heterocyclic 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
    • C07D498/16Peri-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/12Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains three hetero rings
    • C07D513/16Peri-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN201480074890.9A 2013-12-06 2014-12-03 丝氨酸/苏氨酸激酶抑制剂 Active CN106029672B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201361912905P 2013-12-06 2013-12-06
US61/912,905 2013-12-06
PCT/US2014/068452 WO2015085007A1 (en) 2013-12-06 2014-12-03 Serine/threonine kinase inhibitors

Publications (2)

Publication Number Publication Date
CN106029672A CN106029672A (zh) 2016-10-12
CN106029672B true CN106029672B (zh) 2019-03-29

Family

ID=52350292

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201480074890.9A Active CN106029672B (zh) 2013-12-06 2014-12-03 丝氨酸/苏氨酸激酶抑制剂

Country Status (23)

Country Link
US (5) US9867833B2 (cg-RX-API-DMAC7.html)
EP (1) EP3077401B1 (cg-RX-API-DMAC7.html)
JP (2) JP6449293B2 (cg-RX-API-DMAC7.html)
KR (1) KR102359759B1 (cg-RX-API-DMAC7.html)
CN (1) CN106029672B (cg-RX-API-DMAC7.html)
AR (1) AR098647A1 (cg-RX-API-DMAC7.html)
AU (1) AU2014360455B2 (cg-RX-API-DMAC7.html)
BR (1) BR112016012844B1 (cg-RX-API-DMAC7.html)
CA (1) CA2932729C (cg-RX-API-DMAC7.html)
CL (1) CL2016001368A1 (cg-RX-API-DMAC7.html)
CR (1) CR20160309A (cg-RX-API-DMAC7.html)
EA (1) EA031243B1 (cg-RX-API-DMAC7.html)
IL (1) IL246017B (cg-RX-API-DMAC7.html)
MA (1) MA39170B1 (cg-RX-API-DMAC7.html)
MX (1) MX368443B (cg-RX-API-DMAC7.html)
MY (1) MY176049A (cg-RX-API-DMAC7.html)
PE (1) PE20160886A1 (cg-RX-API-DMAC7.html)
PH (1) PH12016501071B1 (cg-RX-API-DMAC7.html)
SG (1) SG11201604573WA (cg-RX-API-DMAC7.html)
TW (1) TWI557126B (cg-RX-API-DMAC7.html)
UA (1) UA120506C2 (cg-RX-API-DMAC7.html)
WO (1) WO2015085007A1 (cg-RX-API-DMAC7.html)
ZA (1) ZA201604461B (cg-RX-API-DMAC7.html)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX2015004615A (es) 2012-10-16 2015-07-17 Hoffmann La Roche Inhibidores de serina/treonina cinasa.
US9532987B2 (en) 2013-09-05 2017-01-03 Genentech, Inc. Use of a combination of a MEK inhibitor and an ERK inhibitor for treatment of hyperproliferative diseases
BR112016012844B1 (pt) 2013-12-06 2023-01-10 Genentech, Inc Composto e composições farmacêuticas
EP3089980B1 (en) 2013-12-30 2018-01-31 Array Biopharma, Inc. Serine/threonine kinase inhibitors
EP3089788B1 (en) 2013-12-30 2018-10-24 Genentech, Inc. Serine/threonine kinase inhibitors
CN108349983B (zh) 2015-11-09 2021-02-26 阿斯利康(瑞典)有限公司 治疗癌症有用的二氢咪唑并吡嗪酮衍生物
EP3443114A1 (en) 2016-04-15 2019-02-20 H. Hoffnabb-La Roche Ag Diagnostic and therapeutic methods for cancer
TW202428305A (zh) 2017-09-08 2024-07-16 美商建南德克公司 癌症之診斷及治療方法
WO2019158579A1 (en) 2018-02-13 2019-08-22 Vib Vzw Targeting minimal residual disease in cancer with rxr antagonists
CN117486890A (zh) * 2019-06-06 2024-02-02 和记黄埔医药(上海)有限公司 三环类化合物及其用途
CA3206898A1 (en) * 2021-02-03 2022-08-11 Tuojie Biotech (Shanghai) Co., Ltd. Fused tricyclic cyclin-dependent kinase inhibitor, and preparation method therefor and pharmaceutical use thereof

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2002836A1 (en) * 2007-05-31 2008-12-17 Nerviano Medical Sciences S.r.l. Cyclocondensed azaindoles active as kinase inhibitors
CN101679409A (zh) * 2006-12-22 2010-03-24 Astex治疗学有限公司 新颖化合物
WO2013130976A1 (en) * 2012-03-01 2013-09-06 Array Biopharma Inc. Serine/threonine kinase inhibitors

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1438027A1 (en) * 2001-10-25 2004-07-21 DepoMed, Inc. Methods of treatment using a gastric retained losartan dosage
AU2006291927A1 (en) 2005-09-15 2007-03-22 Painceptor Pharma Corporation Methods of modulating neurotrophin-mediated activity
NZ610151A (en) 2010-11-23 2015-06-26 Abbvie Inc Salts and crystalline forms of an apoptosis-inducing agent
MX339873B (es) 2011-02-28 2016-06-15 Genentech Inc Inhibidores de serina/treonina cinasa.
WO2013020062A1 (en) 2011-08-04 2013-02-07 Array Biopharma Inc. Quinazoline compounds as serine/threonine kinase inhibitors
US9388171B2 (en) 2012-08-27 2016-07-12 Genetech, Inc. Serine/threonine kinase inhibitors
MX2015004615A (es) 2012-10-16 2015-07-17 Hoffmann La Roche Inhibidores de serina/treonina cinasa.
US9532987B2 (en) 2013-09-05 2017-01-03 Genentech, Inc. Use of a combination of a MEK inhibitor and an ERK inhibitor for treatment of hyperproliferative diseases
BR112016012844B1 (pt) 2013-12-06 2023-01-10 Genentech, Inc Composto e composições farmacêuticas
EP3089980B1 (en) 2013-12-30 2018-01-31 Array Biopharma, Inc. Serine/threonine kinase inhibitors
EP3089788B1 (en) 2013-12-30 2018-10-24 Genentech, Inc. Serine/threonine kinase inhibitors
RU2684102C2 (ru) 2014-04-09 2019-04-04 Дженентек, Инк. Способ получения лекарственных средств

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101679409A (zh) * 2006-12-22 2010-03-24 Astex治疗学有限公司 新颖化合物
EP2002836A1 (en) * 2007-05-31 2008-12-17 Nerviano Medical Sciences S.r.l. Cyclocondensed azaindoles active as kinase inhibitors
WO2013130976A1 (en) * 2012-03-01 2013-09-06 Array Biopharma Inc. Serine/threonine kinase inhibitors

Also Published As

Publication number Publication date
US20210106593A1 (en) 2021-04-15
CA2932729C (en) 2021-02-23
KR102359759B1 (ko) 2022-02-09
PH12016501071A1 (en) 2016-07-25
US10517878B2 (en) 2019-12-31
CL2016001368A1 (es) 2016-12-09
US20200078371A1 (en) 2020-03-12
IL246017B (en) 2019-10-31
JP2019034970A (ja) 2019-03-07
BR112016012844B1 (pt) 2023-01-10
MX368443B (es) 2019-10-02
EA031243B1 (ru) 2018-12-28
UA120506C2 (uk) 2019-12-26
IL246017A0 (en) 2016-08-02
EA201691177A1 (ru) 2016-10-31
CR20160309A (es) 2016-08-25
CN106029672A (zh) 2016-10-12
US11376260B2 (en) 2022-07-05
MA39170A1 (fr) 2018-04-30
US9867833B2 (en) 2018-01-16
US20150182537A1 (en) 2015-07-02
PE20160886A1 (es) 2016-09-14
WO2015085007A1 (en) 2015-06-11
MX2016007352A (es) 2016-09-08
CA2932729A1 (en) 2015-06-11
US20180000833A1 (en) 2018-01-04
EP3077401B1 (en) 2018-04-18
BR112016012844A2 (cg-RX-API-DMAC7.html) 2017-08-08
SG11201604573WA (en) 2016-07-28
US10278975B2 (en) 2019-05-07
KR20160093703A (ko) 2016-08-08
MY176049A (en) 2020-07-22
NZ721361A (en) 2021-07-30
JP2016539153A (ja) 2016-12-15
ZA201604461B (en) 2022-05-25
US20190192534A1 (en) 2019-06-27
JP6449293B2 (ja) 2019-01-09
TWI557126B (zh) 2016-11-11
AU2014360455A1 (en) 2016-07-07
EP3077401A1 (en) 2016-10-12
MA39170B1 (fr) 2019-05-31
AU2014360455B2 (en) 2018-05-10
US10842799B2 (en) 2020-11-24
PH12016501071B1 (en) 2019-04-26
TW201522338A (zh) 2015-06-16
AR098647A1 (es) 2016-06-01

Similar Documents

Publication Publication Date Title
CN106029672B (zh) 丝氨酸/苏氨酸激酶抑制剂
JP6378182B2 (ja) 過剰増殖性│疾患の処置のためのセリン/スレオニンキナーゼ阻害剤
CN103635472B (zh) 丝氨酸/苏氨酸激酶抑制剂
CN107857755B (zh) 作为trka激酶抑制剂的n-吡咯烷基、n′-吡唑基-脲、硫脲、胍和氰基胍化合物
CN103958502B (zh) 作为丝氨酸/苏氨酸激酶抑制剂的喹唑啉化合物
HK1197232A1 (en) Serine/threonine pak1 inhibitors
HK1227022A1 (en) Serine/threonine kinase inhibitors
HK1227022B (zh) 絲氨酸/蘇氨酸激酶抑制劑
NZ721361B2 (en) Serine/threonine kinase inhibitors
HK1191010A (en) Serine/threonine kinase inhibitors
HK1191010B (en) Serine/threonine kinase inhibitors

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
CB02 Change of applicant information

Address after: American California

Applicant after: Genentech Inc.

Address before: American Minnesota

Applicant before: Genentech Inc.

COR Change of bibliographic data
REG Reference to a national code

Ref country code: HK

Ref legal event code: DE

Ref document number: 1227022

Country of ref document: HK

GR01 Patent grant
GR01 Patent grant