CN106456581A - TrkA激酶抑制剂、组合物及其方法 - Google Patents

TrkA激酶抑制剂、组合物及其方法 Download PDF

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Publication number: CN106456581A
Authority: CN; China
Prior art keywords: methyl; trifluoromethyl; benzamide; pyridin; alkyl
Prior art date: 2014-03-26
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.): Pending

Application number

CN201580027483.7A

Other languages

English (en)

Chinese (zh)

Inventor

H·米切尔

M·E·弗雷利

A·J·库克

C·A·斯顿普

Y·H·陈

D·C·比肖氏

X-F·张

C·C·麦科马斯

K·斯基里帕

M·麦克惠特

S·P·默塞尔

K·P·穆尔

P·刘

H·B·伍德

C·S·李

毛庆华

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.)

Merck Sharp and Dohme LLC

Original Assignee

Schering Corp

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.)

2014-03-26

Filing date

2015-03-23

Publication date

2017-02-22

2015-03-23 Application filed by Schering Corp filed Critical Schering Corp

2017-02-22 Publication of CN106456581A publication Critical patent/CN106456581A/zh

Status Pending legal-status Critical Current

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0 **c1c(*)c(*)c(*)c(*)c1C(*)=O Chemical compound **c1c(*)c(*)c(*)c(*)c1C(*)=O 0.000 description 3
GQPLHGOMZJVDIJ-JENYYRDCSA-N BC(C=CN1/C=C\C=C)=CC1=N Chemical compound BC(C=CN1/C=C\C=C)=CC1=N GQPLHGOMZJVDIJ-JENYYRDCSA-N 0.000 description 1
PYODQGKGCXQAQJ-UHFFFAOYSA-N Bc1cc2nc(-c3ccccc3)c(N)[n]2cc1 Chemical compound Bc1cc2nc(-c3ccccc3)c(N)[n]2cc1 PYODQGKGCXQAQJ-UHFFFAOYSA-N 0.000 description 1
UEDKSMIHDDPTAG-UHFFFAOYSA-N CC(C)(C)CC(C)(C)C#N Chemical compound CC(C)(C)CC(C)(C)C#N UEDKSMIHDDPTAG-UHFFFAOYSA-N 0.000 description 1
SHWBWNUYILPUSO-UHFFFAOYSA-N CC(C)C(CC(C)(C)C)N Chemical compound CC(C)C(CC(C)(C)C)N SHWBWNUYILPUSO-UHFFFAOYSA-N 0.000 description 1
PJJBDUNABUYNPZ-UHFFFAOYSA-N C[n](cc1)nc1-c1cc(C(O)=O)ccc1OC(F)(F)F Chemical compound C[n](cc1)nc1-c1cc(C(O)=O)ccc1OC(F)(F)F PJJBDUNABUYNPZ-UHFFFAOYSA-N 0.000 description 1
RPEZXBNSHYRNCX-UHFFFAOYSA-N Cc1c[o]c(-c2cc(C(Nc3c(-c4ccccc4)nc4[n]3cccc4)=O)ccc2C(F)(F)F)n1 Chemical compound Cc1c[o]c(-c2cc(C(Nc3c(-c4ccccc4)nc4[n]3cccc4)=O)ccc2C(F)(F)F)n1 RPEZXBNSHYRNCX-UHFFFAOYSA-N 0.000 description 1
WGOLHUGPTDEKCF-UHFFFAOYSA-N Nc(nc1)ccc1Br Chemical compound Nc(nc1)ccc1Br WGOLHUGPTDEKCF-UHFFFAOYSA-N 0.000 description 1
HUMNYLRZRPPJDN-UHFFFAOYSA-N O=Cc1ccccc1 Chemical compound O=Cc1ccccc1 HUMNYLRZRPPJDN-UHFFFAOYSA-N 0.000 description 1

Classifications

- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
- A61K31/429—Thiazoles condensed with heterocyclic ring 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
- 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
- A61K31/495—Heterocyclic 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
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/5025—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring 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
- A61K31/495—Heterocyclic 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- 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
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic 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
- C07D471/02—Heterocyclic 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 two hetero rings
- C07D471/04—Ortho-condensed systems
- 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
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic 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
- C07D513/02—Heterocyclic 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 two hetero rings
- C07D513/04—Ortho-condensed systems

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Veterinary Medicine (AREA)
Life Sciences & Earth Sciences (AREA)
Pharmacology & Pharmacy (AREA)
Public Health (AREA)
General Health & Medical Sciences (AREA)
Medicinal Chemistry (AREA)
Animal Behavior & Ethology (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
General Chemical & Material Sciences (AREA)
Chemical Kinetics & Catalysis (AREA)
Bioinformatics & Cheminformatics (AREA)
Engineering & Computer Science (AREA)
Epidemiology (AREA)
Physical Education & Sports Medicine (AREA)
Rheumatology (AREA)
Orthopedic Medicine & Surgery (AREA)
Neurology (AREA)
Neurosurgery (AREA)
Biomedical Technology (AREA)
Cardiology (AREA)
Vascular Medicine (AREA)
Pain & Pain Management (AREA)
Heart & Thoracic Surgery (AREA)
Dermatology (AREA)
Hematology (AREA)
Urology & Nephrology (AREA)
Immunology (AREA)
Diabetes (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Nitrogen Condensed Heterocyclic Rings (AREA)
Plural Heterocyclic Compounds (AREA)
Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

CN201580027483.7A 2014-03-26 2015-03-23 TrkA激酶抑制剂、组合物及其方法 Pending CN106456581A (zh)

Applications Claiming Priority (3)

Application Number	Priority Date	Filing Date	Title
CNPCT/CN2014/074143		2014-03-26
PCT/CN2014/074143 WO2015143652A1 (en)	2014-03-26	2014-03-26	TrkA KINASE INHIBITORS,COMPOSITIONS AND METHODS THEREOF
PCT/US2015/022004 WO2015148373A2 (en)	2014-03-26	2015-03-23	TrkA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF

Publications (1)

Publication Number	Publication Date
CN106456581A true CN106456581A (zh)	2017-02-22

Family

ID=54193893

Family Applications (2)

Application Number	Title	Priority Date	Filing Date
CN201580027483.7A Pending CN106456581A (zh)	2014-03-26	2015-03-23	TrkA激酶抑制剂、组合物及其方法
CN201580027484.1A Pending CN106456582A (zh)	2014-03-26	2015-03-23	TrkA 激酶抑制剂、组合物及其方法

Family Applications After (1)

Application Number	Title	Priority Date	Filing Date
CN201580027484.1A Pending CN106456582A (zh)	2014-03-26	2015-03-23	TrkA 激酶抑制剂、组合物及其方法

Country Status (10)

Country	Link
US (2)	US9862716B2 (2)
EP (2)	EP3122345B1 (2)
JP (2)	JP2017512786A (2)
KR (2)	KR20160131119A (2)
CN (2)	CN106456581A (2)
AU (2)	AU2015236363A1 (2)
CA (2)	CA2942957A1 (2)
MX (2)	MX2016012481A (2)
RU (2)	RU2016141647A (2)
WO (3)	WO2015143652A1 (2)

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WO2020114465A1 (zh) *	2018-12-05	2020-06-11	上海轶诺药业有限公司	一类咪唑并芳环类化合物的制备和应用
WO2021197467A1 (zh) *	2020-04-02	2021-10-07	上海华汇拓医药科技有限公司	多靶点的抗肿瘤化合物及其制备方法和应用
CN113666862A (zh) *	2021-08-18	2021-11-19	山东大学	一种通过镍催化不对称硝化反应制备手性3-硝基吲哚类化合物的方法
CN115667241A (zh) *	2020-05-28	2023-01-31	伊莱利利公司	TrkA抑制剂

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KR102129114B1 (ko) *	2018-07-26	2020-07-02	주식회사 온코파마텍	TrkA 저해 활성을 갖는 화합물 및 이를 유효성분으로 함유하는 통증의 예방 또는 치료용 약학적 조성물
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EA202192575A1 (ru)	2019-03-21	2022-01-14	Онксео	Соединения dbait в сочетании с ингибиторами киназ для лечения рака
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CN114761006A (zh)	2019-11-08	2022-07-15	Inserm(法国国家健康医学研究院)	对激酶抑制剂产生耐药性的癌症的治疗方法
TW202134226A (zh)	2019-11-18	2021-09-16	德商拜耳廠股份有限公司	作為殺蟲劑之新穎雜芳基-三唑化合物
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EP4110772A4 (en)	2020-02-26	2024-04-03	Cullgen (Shanghai), Inc.	TROPOMYOSIN RECEPTOR KINASE (TRK) DEGRADATION COMPOUNDS AND METHODS OF USE

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RU2016141645A3 (2)	2018-10-26
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AU2015236363A1 (en)	2016-09-01
RU2016141647A (ru)	2018-04-27
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US20170114056A1 (en)	2017-04-27
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EP3122345A2 (en)	2017-02-01
WO2015148354A3 (en)	2015-12-03
MX2016012483A (es)	2016-12-16
US9862716B2 (en)	2018-01-09
EP3122344A2 (en)	2017-02-01
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