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TN2015000261A1 - Dérivés d'imidazopyridazine servant de modulateurs des recepteurs gabaa - Google Patents

Dérivés d'imidazopyridazine servant de modulateurs des recepteurs gabaa

Info

Publication number
TN2015000261A1
TN2015000261A1 TNP2015000261A TN2015000261A TN2015000261A1 TN 2015000261 A1 TN2015000261 A1 TN 2015000261A1 TN P2015000261 A TNP2015000261 A TN P2015000261A TN 2015000261 A TN2015000261 A TN 2015000261A TN 2015000261 A1 TN2015000261 A1 TN 2015000261A1
Authority
TN
Tunisia
Prior art keywords
receptor modulators
gabaa receptor
derivatives
imidazopyridazine derivatives
imidazopyridazine
Prior art date
Application number
TNP2015000261A
Other languages
English (en)
Inventor
Kiyoyuki Omoto
Robert Mckenzie Owen
David Cameron Pryde
Christine Anne Louise Watson
Mifune Takeuchi
Original Assignee
Pfizer Ltd
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 Pfizer Ltd filed Critical Pfizer Ltd
Publication of TN2015000261A1 publication Critical patent/TN2015000261A1/fr

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
    • 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
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/08—Antiepileptics; Anticonvulsants
    • 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
    • A61P25/22—Anxiolytics
    • 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]
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Cosmetics (AREA)

Abstract

La présente invention concerne des dérivés d'imidazopyridazine. Plus particulièrement elle concerne des dérivés de 4-(biphényl-3-yl)-7H-imidazo[4,5-c]pyridazine de formule (I) et leurs sels pharmaceutiquement acceptables dans lesquels R1, R2, R3, R4 et R5 sont tels que définis dans la description. Les dérivés d'imidazopyridazine de la présente invention modulent l'activité du récepteur GABAA. Ils sont utiles dans le traitement d'un certain nombre d'affections,comprenant la douleur.
TNP2015000261A 2012-12-14 2015-06-09 Dérivés d'imidazopyridazine servant de modulateurs des recepteurs gabaa TN2015000261A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201261737157P 2012-12-14 2012-12-14
PCT/IB2013/060631 WO2014091368A1 (fr) 2012-12-14 2013-12-04 Dérivés d'imidazopyridazine en tant que modulateurs d'un récepteur gabaa

Publications (1)

Publication Number Publication Date
TN2015000261A1 true TN2015000261A1 (fr) 2016-10-03

Family

ID=49880883

Family Applications (1)

Application Number Title Priority Date Filing Date
TNP2015000261A TN2015000261A1 (fr) 2012-12-14 2015-06-09 Dérivés d'imidazopyridazine servant de modulateurs des recepteurs gabaa

Country Status (43)

Country Link
US (3) US8952008B2 (fr)
EP (1) EP2938615B1 (fr)
JP (1) JP5869740B2 (fr)
KR (1) KR101746314B1 (fr)
CN (1) CN104837843B (fr)
AP (1) AP2015008526A0 (fr)
AR (1) AR093937A1 (fr)
AU (1) AU2013356894B2 (fr)
BR (1) BR112015014097B1 (fr)
CA (1) CA2892174C (fr)
CL (1) CL2015001652A1 (fr)
CR (1) CR20150254A (fr)
CU (1) CU24338B1 (fr)
CY (1) CY1118568T1 (fr)
DK (1) DK2938615T3 (fr)
DO (1) DOP2015000147A (fr)
EA (1) EA025635B1 (fr)
EC (1) ECSP15029822A (fr)
ES (1) ES2608640T3 (fr)
GE (1) GEP201706710B (fr)
GT (1) GT201500159A (fr)
HR (1) HRP20161559T1 (fr)
HU (1) HUE032400T2 (fr)
IL (1) IL239243A0 (fr)
LT (1) LT2938615T (fr)
MA (1) MA38112B1 (fr)
MD (1) MD4651B1 (fr)
ME (1) ME02566B (fr)
MX (1) MX366023B (fr)
NI (1) NI201500081A (fr)
PE (1) PE20151163A1 (fr)
PH (1) PH12015501293A1 (fr)
PL (1) PL2938615T3 (fr)
PT (1) PT2938615T (fr)
RS (1) RS55307B1 (fr)
SG (1) SG11201503735YA (fr)
SI (1) SI2938615T1 (fr)
TN (1) TN2015000261A1 (fr)
TW (1) TWI478926B (fr)
UA (1) UA112028C2 (fr)
UY (1) UY35185A (fr)
WO (1) WO2014091368A1 (fr)
ZA (1) ZA201504226B (fr)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2664810T3 (es) * 2014-06-12 2018-04-23 Pfizer Limited Derivados de imidazopiridazina como moduladores de la actividad del receptor GABAA
RU2712192C2 (ru) 2014-07-31 2020-01-24 Басф Се Способ получения пиразолов
BR112017023935B1 (pt) 2015-05-11 2020-07-07 Basf Se processo para a preparação de um composto
EP3386983A1 (fr) * 2015-12-10 2018-10-17 Pfizer Limited Dérivés 4-(biphényl-3-yl)-1h-pyrazolo[3,4-c]pyridazine de formule (i) utilisés comme modulateurs de récepteur gaba pour le traitement de l'épilepsie et de la douleur
MY196425A (en) * 2016-09-23 2023-04-10 Novartis Ag Indazole Compounds For Use In Tendon And/Or Ligament Injuries
JOP20190053A1 (ar) * 2016-09-23 2019-03-21 Novartis Ag مركبات أزا إندازول للاستخدام في إصابات الأوتار و/ أو الرباط
WO2018082964A1 (fr) 2016-11-04 2018-05-11 Basf Se Procédé de production de pyridazinyle-amides dans une synthèse one pot
CN110573513B (zh) 2017-05-02 2022-08-09 拜耳公司 作为害虫防治剂的2-(杂)芳基取代的稠合双环杂环衍生物
EP3634420A1 (fr) * 2017-06-06 2020-04-15 Urovant Sciences GmbH Utilisation de vibegron dans le traitement de la vessie hyperactive
WO2019226820A1 (fr) * 2018-05-22 2019-11-28 Neurocycle Therapeutics, Inc. Composés modulateurs allostériques positifs gabaa pour le traitement du prurit et/ou de la dermatite
TW202214648A (zh) * 2019-01-07 2022-04-16 美商美國禮來大藥廠 Il-17a抑制劑
CN120865250A (zh) * 2022-02-25 2025-10-31 上海赛默罗生物科技有限公司 咪唑并哒嗪类衍生物、其制备方法、药物组合物和用途
CN117069725A (zh) * 2022-05-10 2023-11-17 上海赛默罗生物科技有限公司 咪唑并哒嗪取代苯环类衍生物、制备方法、药物组合物及用途
CN116655475B (zh) * 2023-05-19 2024-12-31 山东轩鸿生物医药有限公司 一种盐酸氟西汀的制备方法
WO2025137437A1 (fr) 2023-12-21 2025-06-26 Pfizer Inc. Formes solides d'un modulateur du récepteur gabaa et leurs procédés d'utilisation

Family Cites Families (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5376645A (en) 1990-01-23 1994-12-27 University Of Kansas Derivatives of cyclodextrins exhibiting enhanced aqueous solubility and the use thereof
KR0166088B1 (ko) 1990-01-23 1999-01-15 . 수용해도가 증가된 시클로덱스트린 유도체 및 이의 용도
GB9518953D0 (en) 1995-09-15 1995-11-15 Pfizer Ltd Pharmaceutical formulations
WO2000035298A1 (fr) 1996-11-27 2000-06-22 Wm. Wrigley Jr. Company Chewing-gum contenant des agents medicamenteux actifs
GB9711643D0 (en) 1997-06-05 1997-07-30 Janssen Pharmaceutica Nv Glass thermoplastic systems
US6365589B1 (en) 1998-07-02 2002-04-02 Bristol-Myers Squibb Pharma Company Imidazo-pyridines, -pyridazines, and -triazines as corticotropin releasing factor antagonists
GB0117277D0 (en) 2001-07-16 2001-09-05 Merck Sharp & Dohme Therapeutic agents
JP4302980B2 (ja) 2000-11-10 2009-07-29 メルク シャープ エンド ドーム リミテッド Ｇａｂａ受容体リガンドとしてのイミダゾ−トリアジン誘導体
CA2555263A1 (fr) * 2004-02-12 2005-09-01 Neurogen Corporation Imidazo-pyridazines, triazolo-pyridazines et ligands associes des recepteurs de benzodiazepine
US20080132510A1 (en) 2005-01-21 2008-06-05 Bingsong Han Imidazolylmethyl and Pyrazolylmethyl Heteroaryl Derivatives
EP1845098A1 (fr) * 2006-03-29 2007-10-17 Ferrer Internacional, S.A. Imidazo[1,2-b]pyridazines, leur procédés de préparation et leur utilisation comme ligands du recepteur GABA
DE602008000809D1 (de) 2007-03-23 2010-04-29 Icagen Inc Ionenkanal-Hemmer
EA020460B1 (ru) 2009-01-12 2014-11-28 Пфайзер Лимитед Производные сульфонамида
US20120220581A1 (en) * 2009-10-30 2012-08-30 Janssen-Cilag, S.A. IMIDAZO[1,2-b]PYRIDAZINE DERIVATIVES AND THEIR USE AS PDE10 INHIBITORS
WO2012004714A2 (fr) * 2010-07-09 2012-01-12 Pfizer Limited Composés chimiques

Also Published As

Publication number Publication date
ME02566B (fr) 2017-02-20
PE20151163A1 (es) 2015-08-14
US20150105396A1 (en) 2015-04-16
ZA201504226B (en) 2016-06-29
GT201500159A (es) 2015-09-23
PL2938615T3 (pl) 2017-04-28
KR101746314B1 (ko) 2017-06-12
MD20150051A2 (ro) 2015-09-30
BR112015014097B1 (pt) 2022-11-29
US20150259352A1 (en) 2015-09-17
DK2938615T3 (da) 2017-01-02
BR112015014097A2 (pt) 2019-12-17
RS55307B1 (sr) 2017-03-31
ES2608640T3 (es) 2017-04-12
MA38112B1 (fr) 2018-10-31
HUE032400T2 (hu) 2017-09-28
LT2938615T (lt) 2016-12-27
DOP2015000147A (es) 2015-09-15
HRP20161559T1 (hr) 2016-12-30
CA2892174A1 (fr) 2014-06-19
PH12015501293B1 (en) 2015-08-24
MX366023B (es) 2019-06-24
UA112028C2 (uk) 2016-07-11
CL2015001652A1 (es) 2015-08-14
HK1209743A1 (zh) 2016-04-08
US20140171435A1 (en) 2014-06-19
AR093937A1 (es) 2015-07-01
ECSP15029822A (es) 2017-08-31
CY1118568T1 (el) 2017-07-12
CA2892174C (fr) 2018-02-06
CU24338B1 (es) 2018-04-03
PH12015501293A1 (en) 2015-08-24
JP2016503001A (ja) 2016-02-01
CU20150058A7 (es) 2015-11-27
US8952008B2 (en) 2015-02-10
EP2938615B1 (fr) 2016-10-26
AU2013356894B2 (en) 2015-11-12
AU2013356894A1 (en) 2015-05-28
EA025635B1 (ru) 2017-01-30
MA38112A1 (fr) 2018-03-30
EA201590761A1 (ru) 2015-12-30
JP5869740B2 (ja) 2016-02-24
IL239243A0 (en) 2015-07-30
GEP201706710B (en) 2017-07-25
UY35185A (es) 2014-07-31
SG11201503735YA (en) 2015-07-30
CN104837843A (zh) 2015-08-12
EP2938615A1 (fr) 2015-11-04
NI201500081A (es) 2015-09-16
MX2015007598A (es) 2015-10-22
WO2014091368A1 (fr) 2014-06-19
PT2938615T (pt) 2016-12-26
AP2015008526A0 (en) 2015-06-30
SI2938615T1 (sl) 2017-02-28
CR20150254A (es) 2015-07-09
KR20150088877A (ko) 2015-08-03
CN104837843B (zh) 2016-08-31
TW201434840A (zh) 2014-09-16
TWI478926B (zh) 2015-04-01
MD4651B1 (ro) 2019-09-30

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