CN104684554B - 用于治疗疼痛的氮杂吲唑或二氮杂吲唑型衍生物 - Google Patents

用于治疗疼痛的氮杂吲唑或二氮杂吲唑型衍生物 Download PDF

Info

Publication number
CN104684554B
CN104684554B CN201380049411.3A CN201380049411A CN104684554B CN 104684554 B CN104684554 B CN 104684554B CN 201380049411 A CN201380049411 A CN 201380049411A CN 104684554 B CN104684554 B CN 104684554B
Authority
CN
China
Prior art keywords
aromatic
pain
mmol
solution
pyrazolo
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
CN201380049411.3A
Other languages
English (en)
Chinese (zh)
Other versions
CN104684554A (zh
Inventor
P·索科洛夫
F·卡舒
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.)
Pierre Fabre Medicament SA
Original Assignee
Pierre Fabre Medicament SA
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 Pierre Fabre Medicament SA filed Critical Pierre Fabre Medicament SA
Publication of CN104684554A publication Critical patent/CN104684554A/zh
Application granted granted Critical
Publication of CN104684554B publication Critical patent/CN104684554B/zh
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • A61K31/4985—Pyrazines or piperazines 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
    • A61K31/435—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
    • A61K31/435—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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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]

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
CN201380049411.3A 2012-07-27 2013-07-29 用于治疗疼痛的氮杂吲唑或二氮杂吲唑型衍生物 Active CN104684554B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP12305922.2A EP2689778A1 (en) 2012-07-27 2012-07-27 Derivatives of azaindoles or diazaindoles for treating pain
EP12305922.2 2012-07-27
PCT/EP2013/065907 WO2014016433A1 (en) 2012-07-27 2013-07-29 Derivatives of azaindazole or diazaindazole type for treating pain

Publications (2)

Publication Number Publication Date
CN104684554A CN104684554A (zh) 2015-06-03
CN104684554B true CN104684554B (zh) 2017-05-10

Family

ID=48948392

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201380049411.3A Active CN104684554B (zh) 2012-07-27 2013-07-29 用于治疗疼痛的氮杂吲唑或二氮杂吲唑型衍生物

Country Status (28)

Country Link
US (1) US9381195B2 (2)
EP (2) EP2689778A1 (2)
JP (2) JP6456823B2 (2)
KR (1) KR102120505B1 (2)
CN (1) CN104684554B (2)
AU (1) AU2013294920B2 (2)
BR (1) BR112015001502B1 (2)
CA (1) CA2879595C (2)
CY (1) CY1118478T1 (2)
DK (1) DK2877177T3 (2)
ES (1) ES2612349T3 (2)
HR (1) HRP20170104T1 (2)
HU (1) HUE032919T2 (2)
IL (1) IL236917A (2)
LT (1) LT2877177T (2)
MA (1) MA37866B1 (2)
MX (1) MX363605B (2)
MY (1) MY183398A (2)
NZ (1) NZ705253A (2)
PL (1) PL2877177T3 (2)
PT (1) PT2877177T (2)
RS (1) RS55646B1 (2)
RU (1) RU2640046C2 (2)
SI (1) SI2877177T1 (2)
TN (1) TN2015000034A1 (2)
UA (1) UA116107C2 (2)
WO (1) WO2014016433A1 (2)
ZA (1) ZA201501209B (2)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US12583852B2 (en) 2018-05-02 2026-03-24 Jw Pharmaceutical Corporation Heterocycle derivative

Families Citing this family (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AR074052A1 (es) 2008-10-22 2010-12-22 Array Biopharma Inc Compuestos pirazolo{1,5-a}pirimidina sustituida como inhibidores de trk cinasa
AR077468A1 (es) 2009-07-09 2011-08-31 Array Biopharma Inc Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa
NZ604708A (en) 2010-05-20 2015-05-29 Array Biopharma Inc Macrocyclic compounds as trk kinase inhibitors
EP2689778A1 (en) * 2012-07-27 2014-01-29 Pierre Fabre Medicament Derivatives of azaindoles or diazaindoles for treating pain
WO2015143652A1 (en) * 2014-03-26 2015-10-01 Merck Sharp & Dohme Corp. TrkA KINASE INHIBITORS,COMPOSITIONS AND METHODS THEREOF
AU2015328307B2 (en) * 2014-10-06 2019-11-21 Apm Therapeutics 1, Inc. Triazolopyridine compounds and methods for the treatment of cystic fibrosis
HUE061448T2 (hu) 2014-11-16 2023-07-28 Array Biopharma Inc (S)-N-(5-((R)-2-(2,5-difluorofenil)-pirrolidin-1-il)-pirazolo[1,5-A]pirimidin-3-il) -3-hidroxipirrolidin-1-karboxamid-hidrogénszulfát kristályos formája
US10336707B2 (en) 2014-12-16 2019-07-02 Eudendron S.R.L. Heterocyclic derivatives modulating activity of certain protein kinases
CN108697708A (zh) 2015-10-26 2018-10-23 洛克索肿瘤学股份有限公司 Trk抑制剂抗性癌症中的点突变以及与此相关的方法
US10045991B2 (en) 2016-04-04 2018-08-14 Loxo Oncology, Inc. Methods of treating pediatric cancers
ES2987474T3 (es) 2016-04-04 2024-11-15 Loxo Oncology Inc Formulaciones líquidas de (S)-N-(5-((R)-2-(2,5-difluorofenil)-pirrolidin-1-IL)-pirazolo[1,5-A]pirimidin-3-IL)-3-hidroxipirrolidina-1-carboxamida
ES2836222T3 (es) 2016-05-18 2021-06-24 Loxo Oncology Inc Preparación de (S)-N-(5-((R)-2-(2,5-difluorofenil)pirrolidin-1-il)pirazolo[1,5-a]pirimidin-3-il)-3-hidroxipirrolidina-1-carboxamida
US10246462B2 (en) 2016-09-09 2019-04-02 Flx Bio, Inc. Chemokine receptor modulators and uses thereof
JOP20190092A1 (ar) 2016-10-26 2019-04-25 Array Biopharma Inc عملية لتحضير مركبات بيرازولو[1، 5-a]بيريميدين وأملاح منها
WO2018079759A1 (ja) * 2016-10-31 2018-05-03 塩野義製薬株式会社 ＴｒｋＡ阻害活性を有する縮合複素環および縮合炭素環誘導体
JOP20190213A1 (ar) 2017-03-16 2019-09-16 Array Biopharma Inc مركبات حلقية ضخمة كمثبطات لكيناز ros1
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
EP3725777A1 (en) * 2019-04-17 2020-10-21 Rottapharm Biotech S.r.l. Benzo- and pyrido-pyrazoles as protein kinase inhibitors
CN110105356B (zh) * 2019-05-31 2022-04-01 四川国康药业有限公司 一种氮杂吲哚类化合物及其制备方法和用途
EP4722211A1 (en) * 2023-05-24 2026-04-08 Changchun Genescience Pharmaceutical Co., Ltd. Fgfr2/3 selective inhibitor, pharmaceutical composition and use thereof

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004113303A1 (en) * 2003-06-26 2004-12-29 Astrazeneca Ab INDAZOLE/PYRZOLO[4,3-c]PYRIDIN DERIVATIVES AS JNK INHIBITORS, COMPOSITIONS AND METHODS RELATED THERETO AS WELL AS INTERMEDIATE THEREOF
WO2008089307A2 (en) * 2007-01-18 2008-07-24 Lexicon Pharmaceuticals, Inc. Delta 5 desaturase inhibitors for the treatment of pain, inflammation and cancer
CN101243090A (zh) * 2005-08-25 2008-08-13 霍夫曼-拉罗奇有限公司 p38 MAP激酶抑制剂及使用它的方法
WO2008112695A2 (en) * 2007-03-12 2008-09-18 Irm Llc Pyrazolo [3,4-d] pyrimidines and 1, 2, 5, 6-tetraaza- as- indacenes as protein kinase inhibitors for cancer treatment

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK0970084T3 (da) 1997-03-19 2003-09-29 Abbott Gmbh & Co Kg Pyrrolo[2,3-d]pyrimidiner og deres anvendelse som inhibitorer for tyrosinkinase
EP1215208B1 (en) 1997-10-27 2006-07-12 Agouron Pharmaceuticals, Inc. 4-Aminothiazole derivatives, their preparation and their use as inhibitors of cyclin-dependent kinases
AU2001262597B2 (en) 2000-06-22 2005-10-20 Pfizer Inc. Process for the preparation of pyrazolopyrimidinones
DE102004061288A1 (de) * 2004-12-14 2006-06-29 Schering Ag 3-Amino-Pyrazolo[3,4b]pyridine als Inhibitoren von Proteintyrosinkinasen, deren Herstellung und Verwendung als Arzneimittel
US20100056516A1 (en) 2006-07-17 2010-03-04 Williams Peter D 1-hydroxy naphthyridine compounds as anti-hiv agents
EP2120932B1 (en) * 2006-12-20 2014-07-09 Nerviano Medical Sciences S.r.l. Indazole derivatives as kinase inhibitors for the treatment of cancer
PH12013501594A1 (en) 2007-07-20 2014-05-12 Nerviano Medical Sciences Srl Substituted indazole derivatives active as kinase inhibitors
EP2373626B1 (en) 2008-12-18 2016-08-24 Nerviano Medical Sciences S.r.l. Substituted indazole derivatives active as kinase inhibitors
FR2970967B1 (fr) * 2011-01-27 2013-02-15 Pf Medicament Derives de type azaindazole ou diazaindazole comme medicament
EP2689778A1 (en) * 2012-07-27 2014-01-29 Pierre Fabre Medicament Derivatives of azaindoles or diazaindoles for treating pain

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004113303A1 (en) * 2003-06-26 2004-12-29 Astrazeneca Ab INDAZOLE/PYRZOLO[4,3-c]PYRIDIN DERIVATIVES AS JNK INHIBITORS, COMPOSITIONS AND METHODS RELATED THERETO AS WELL AS INTERMEDIATE THEREOF
CN101243090A (zh) * 2005-08-25 2008-08-13 霍夫曼-拉罗奇有限公司 p38 MAP激酶抑制剂及使用它的方法
WO2008089307A2 (en) * 2007-01-18 2008-07-24 Lexicon Pharmaceuticals, Inc. Delta 5 desaturase inhibitors for the treatment of pain, inflammation and cancer
WO2008112695A2 (en) * 2007-03-12 2008-09-18 Irm Llc Pyrazolo [3,4-d] pyrimidines and 1, 2, 5, 6-tetraaza- as- indacenes as protein kinase inhibitors for cancer treatment

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US12583852B2 (en) 2018-05-02 2026-03-24 Jw Pharmaceutical Corporation Heterocycle derivative

Also Published As

Publication number Publication date
JP6732855B2 (ja) 2020-07-29
DK2877177T3 (en) 2017-02-06
MX363605B (es) 2019-03-26
US9381195B2 (en) 2016-07-05
IL236917A (en) 2016-11-30
MA37866B1 (fr) 2016-12-30
KR102120505B1 (ko) 2020-06-08
CY1118478T1 (el) 2017-07-12
US20150190394A1 (en) 2015-07-09
SI2877177T1 (sl) 2017-02-28
PT2877177T (pt) 2017-02-06
JP2015522650A (ja) 2015-08-06
BR112015001502B1 (pt) 2023-03-07
EP2877177A1 (en) 2015-06-03
LT2877177T (lt) 2017-01-25
BR112015001502A2 (pt) 2017-07-04
ZA201501209B (en) 2016-03-30
JP6456823B2 (ja) 2019-01-23
EP2877177B1 (en) 2016-10-26
CN104684554A (zh) 2015-06-03
HUE032919T2 (hu) 2017-11-28
AU2013294920A1 (en) 2015-03-12
PL2877177T3 (pl) 2017-04-28
RU2640046C2 (ru) 2017-12-26
AU2013294920B2 (en) 2017-08-24
TN2015000034A1 (en) 2016-06-29
NZ705253A (en) 2017-05-26
MY183398A (en) 2021-02-18
EP2689778A1 (en) 2014-01-29
JP2019031542A (ja) 2019-02-28
HK1207302A1 (en) 2016-01-29
MA37866A1 (fr) 2016-05-31
CA2879595A1 (en) 2014-01-30
RS55646B1 (sr) 2017-06-30
KR20150038295A (ko) 2015-04-08
WO2014016433A1 (en) 2014-01-30
HRP20170104T1 (hr) 2017-03-24
ES2612349T3 (es) 2017-05-16
MX2015001009A (es) 2015-06-04
CA2879595C (en) 2020-07-28
RU2015106434A (ru) 2016-09-20
UA116107C2 (uk) 2018-02-12

Similar Documents

Publication Publication Date Title
CN104684554B (zh) 用于治疗疼痛的氮杂吲唑或二氮杂吲唑型衍生物
CN103339129B (zh) 作为药物的氮杂吲唑或二氮杂吲唑类衍生物
US9428510B2 (en) Derivatives of azaindazole or diazaindazole type for treating a cancer overexpressing Trk
HK1207302B (en) Derivatives of azaindazole or diazaindazole type for treating pain
HK1186737B (en) Derivatives of azaindazole or diazaindazole type as medicament
OA17324A (en) Derivatives of azaindazole or diazaindazole type for treating pain.

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
REG Reference to a national code

Ref country code: HK

Ref legal event code: DE

Ref document number: 1207302

Country of ref document: HK

GR01 Patent grant
GR01 Patent grant
REG Reference to a national code

Ref country code: HK

Ref legal event code: GR

Ref document number: 1207302

Country of ref document: HK