HUP0100575A2 - Triazolopiridazin-származékok mint gaba-receptorok ligandumjai - Google Patents

Triazolopiridazin-származékok mint gaba-receptorok ligandumjai

Info

Publication number
HUP0100575A2
HUP0100575A2 HU0100575A HUP0100575A HUP0100575A2 HU P0100575 A2 HUP0100575 A2 HU P0100575A2 HU 0100575 A HU0100575 A HU 0100575A HU P0100575 A HUP0100575 A HU P0100575A HU P0100575 A2 HUP0100575 A2 HU P0100575A2
Authority
HU
Hungary
Prior art keywords
triazolo
ligands
fluorocyclobutyl
methylcyclobutyl
methylcyclohexyl
Prior art date
Application number
HU0100575A
Other languages
English (en)
Inventor
William Robert Carling
Jose Luis Castro Pineiro
Ian James Collins
Alexander Richard Guiblin
Timothy Harrison
Andrew Madin
Kevin William Moore
Michael Geoffrey Neil Russell
Gayle Scott
Leslie Joseph Street
Original Assignee
Merck Sharp & Dohme 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
Priority claimed from GBGB9801233.9A external-priority patent/GB9801233D0/en
Priority claimed from GBGB9821517.1A external-priority patent/GB9821517D0/en
Application filed by Merck Sharp & Dohme Ltd. filed Critical Merck Sharp & Dohme Ltd.
Publication of HUP0100575A2 publication Critical patent/HUP0100575A2/hu
Publication of HUP0100575A3 publication Critical patent/HUP0100575A3/hu

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
    • 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
    • A61P25/08—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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Landscapes

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

Abstract

A találmány új, (I) általános képletű szubsztituált triazolopiridazin-származékokra, valamint ezeknek a gyógyászatban való alkalmazásáravonatkozik. Közelebbről a találmány új, szubsztituált 1,2,4-triazolo[4,3-b]-piridazin-származékokra vonatkozik, amelyek ligandumokGABAA receptorok vonatkozásában, ezért felhasználhatók különböző kórosmentális állapotok terápiájában. A találmány szerinti vegyületek (I)általános képletében Z jelentése trifluormetil-, 2-metilpropil-, 2,2-dimetilpropil-, 3-metilbutil-, 1-fluorbut-3-enil-, ciklobutil-, 1-metilciklobutil-, 1-fluorciklobutil-, 3-fluorciklobutil-, 3,3-difluorciklobutil-, 3-hidroxiciklobutil-, 3-benziloxi-ciklobutil-, 3-oxociklobutil-, 1-metilciklohexil-, 4,4-difluor-1-metilciklo-hexil-,ciklopentilmetil-, 4-fluorciklohex-3-enil-; 3-fluorfenil-, tetra-hidrofur-2-il-, pirrolidin-1-il-, 4-metiltetrahidropirán-4-il- vagy 2-tienil-csoport; R1 jelentése hidrogén- vagy fluoratom; és R2 jelentésemetilizoxazolil-, metilpirazolil-, metilimidazolil-, benzimidazolil-vagy metiltriazolilcsoport; azzal a megkötéssel, hogy ha Z jelentése1-metilciklobutilcsoport, R1 jelentése hidrogénatom és R2 jelentése 1-metil-1 H-1,2,4-triazol-3-il- vagy 2-metil-2H-1,2,4-triazol-3-ilcsoport, akkor a fluoratom nem lehet a fenilgyűrű 2-helyzetében. Ó
HU0100575A 1998-01-21 1999-01-13 Triazolo-pyridazine derivatives as ligands for gaba receptors HUP0100575A3 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GBGB9801233.9A GB9801233D0 (en) 1998-01-21 1998-01-21 Therapeutic agents
GBGB9821517.1A GB9821517D0 (en) 1998-10-02 1998-10-02 Therapeutic agents
PCT/GB1999/000103 WO1999037644A1 (en) 1998-01-21 1999-01-13 Triazolo-pyridazine derivatives as ligands for gaba receptors

Publications (2)

Publication Number Publication Date
HUP0100575A2 true HUP0100575A2 (hu) 2001-09-28
HUP0100575A3 HUP0100575A3 (en) 2003-03-28

Family

ID=26312988

Family Applications (1)

Application Number Title Priority Date Filing Date
HU0100575A HUP0100575A3 (en) 1998-01-21 1999-01-13 Triazolo-pyridazine derivatives as ligands for gaba receptors

Country Status (24)

Country Link
US (2) US6579875B1 (hu)
EP (1) EP1049696A1 (hu)
JP (1) JP2002501066A (hu)
KR (1) KR20010034257A (hu)
CN (1) CN1110498C (hu)
AU (1) AU748737B2 (hu)
BG (1) BG104671A (hu)
BR (1) BR9906905A (hu)
CA (1) CA2315763A1 (hu)
CZ (1) CZ290883B6 (hu)
EA (1) EA002755B1 (hu)
EE (1) EE200000430A (hu)
GE (1) GEP20032868B (hu)
HR (1) HRP20000492A2 (hu)
HU (1) HUP0100575A3 (hu)
IL (1) IL136442A0 (hu)
IS (1) IS5540A (hu)
MX (1) MXPA00007135A (hu)
NO (1) NO315516B1 (hu)
NZ (1) NZ504870A (hu)
PL (1) PL341652A1 (hu)
SK (1) SK10922000A3 (hu)
WO (1) WO1999037644A1 (hu)
YU (1) YU43800A (hu)

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WO1999037644A1 (en) * 1998-01-21 1999-07-29 Merck Sharp & Dohme Limited Triazolo-pyridazine derivatives as ligands for gaba receptors
GB9929685D0 (en) * 1999-12-15 2000-02-09 Merck Sharp & Dohme Therapeutic agents
GB0017543D0 (en) 2000-07-17 2000-09-06 Merck Sharp & Dohme Therapeutic agents
WO2005058860A1 (ja) * 2003-12-19 2005-06-30 Ube Industries, Ltd. ４−置換又は非置換テトラヒドロピラン−４−カルボン酸化合物又はそのエステル化合物の製法
EP2258359A3 (en) 2005-08-26 2011-04-06 Braincells, Inc. Neurogenesis by muscarinic receptor modulation with sabcomelin
US7678363B2 (en) 2005-08-26 2010-03-16 Braincells Inc Methods of treating psychiatric conditions comprising administration of muscarinic agents in combination with SSRIs
EP1940389A2 (en) 2005-10-21 2008-07-09 Braincells, Inc. Modulation of neurogenesis by pde inhibition
US20070112017A1 (en) * 2005-10-31 2007-05-17 Braincells, Inc. Gaba receptor mediated modulation of neurogenesis
US8030305B2 (en) * 2005-12-21 2011-10-04 Janssen Pharmaceutica N.V. Triazolopyridazines as kinase modulators
US20100216734A1 (en) 2006-03-08 2010-08-26 Braincells, Inc. Modulation of neurogenesis by nootropic agents
MX2008014320A (es) 2006-05-09 2009-03-25 Braincells Inc Neurogenesis mediada por el receptor de 5-hidroxitriptamina.
EP2021000A2 (en) 2006-05-09 2009-02-11 Braincells, Inc. Neurogenesis by modulating angiotensin
EP2068872A1 (en) 2006-09-08 2009-06-17 Braincells, Inc. Combinations containing a 4-acylaminopyridine derivative
US20100184806A1 (en) 2006-09-19 2010-07-22 Braincells, Inc. Modulation of neurogenesis by ppar agents
EP2123619A1 (de) 2008-05-20 2009-11-25 Bayer Schering Pharma AG Neue [F-18]-Markierte L-Glutaminsäure-und L-Glutaminderivate (II), ihre Verwendung sowie Verfahren zu ihrer Herstellung
DK2328414T3 (en) * 2008-08-29 2014-03-10 Concert Pharmaceuticals Inc Substituted triazolopyridazine derivatives
US20100216805A1 (en) 2009-02-25 2010-08-26 Braincells, Inc. Modulation of neurogenesis using d-cycloserine combinations
WO2011005520A1 (en) 2009-06-23 2011-01-13 Concert Pharmaceuticals, Inc. Deuterium-modified triazolo-pyridazine derivatives as gaba-a receptor modulators
LT2464645T (lt) * 2009-07-27 2017-10-25 Gilead Sciences, Inc. Kondensuoti heterocikliniai junginiai, kaip jonų kanalų moduliatoriai
US9089531B2 (en) 2010-09-28 2015-07-28 The Regents Of The University Of California GABA agonists in the treatment of disorders associated with metabolic syndrome and GABA combinations in treatment or prophylaxis of type I diabetes
PT2707361T (pt) 2011-05-10 2017-11-28 Gilead Sciences Inc Compostos heterocíclicos fusionados como moduladores do canal de sódio
NO3175985T3 (hu) 2011-07-01 2018-04-28
TWI622583B (zh) 2011-07-01 2018-05-01 基利科學股份有限公司 作為離子通道調節劑之稠合雜環化合物
GB201321745D0 (en) * 2013-12-09 2014-01-22 Ucb Pharma Sa Therapeutic agents
JP7105696B2 (ja) 2016-02-29 2022-07-25 デイナ ファーバー キャンサー インスティチュート，インコーポレイテッド 感染症を治療するステープル化細胞内ターゲティング抗微生物ペプチド
CN107344936B (zh) * 2016-05-06 2022-06-03 上海赛默罗生物科技有限公司 ***哒嗪类衍生物、其制备方法、药物组合物和用途
US11325955B2 (en) 2017-07-19 2022-05-10 Dana-Farber Cancer Institute, Inc. Stabilized anti-microbial peptides for the treatment of antibiotic-resistant bacterial infections

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Publication number Priority date Publication date Assignee Title
US4230705A (en) * 1976-09-22 1980-10-28 American Cyanamid Company 6-Phenyl-1,2,4-triazolo[4,3-b]pyridazines and their uses in treating anxiety
CA1080712A (en) 1976-09-22 1980-07-01 Jay D. Albright Hypotensive agents
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PH21834A (en) 1982-01-18 1988-03-17 Lepetit Spa New 6-substituted-s-triazolo(3,4-a)phthalazine derivatives
IT1194310B (it) * 1983-07-12 1988-09-14 Lepetit Spa Derivati triazolo (3,4-a) ftalazinici 3,6-disostituiti
US4654343A (en) 1985-10-31 1987-03-31 American Cyanamid Company N-substituted-N[3-(1,2,4-triazolo[4,3-b]pyridazin-6-yl)phenyl]alkanamides, carbamates and ureas
EA002436B1 (ru) * 1996-07-25 2002-04-25 Мерк Шарп Энд Домэ Лимитед Замещенные производные триазоло-пиридазина в качестве лигандов рецепторов гамк
WO1999037644A1 (en) 1998-01-21 1999-07-29 Merck Sharp & Dohme Limited Triazolo-pyridazine derivatives as ligands for gaba receptors

Also Published As

Publication number Publication date
CN1288465A (zh) 2001-03-21
IS5540A (is) 2000-06-16
CZ20002691A3 (cs) 2000-12-13
WO1999037644A1 (en) 1999-07-29
PL341652A1 (en) 2001-04-23
GEP20032868B (en) 2003-01-27
CN1110498C (zh) 2003-06-04
AU2065799A (en) 1999-08-09
NO20003730D0 (no) 2000-07-20
HRP20000492A2 (en) 2000-12-31
US6828322B2 (en) 2004-12-07
BG104671A (en) 2001-05-31
EP1049696A1 (en) 2000-11-08
MXPA00007135A (es) 2002-11-07
KR20010034257A (ko) 2001-04-25
JP2002501066A (ja) 2002-01-15
HUP0100575A3 (en) 2003-03-28
US20040063714A1 (en) 2004-04-01
CZ290883B6 (cs) 2002-11-13
NZ504870A (en) 2002-11-26
AU748737B2 (en) 2002-06-13
EA002755B1 (ru) 2002-08-29
YU43800A (sh) 2002-12-10
EA200000783A1 (ru) 2000-12-25
NO20003730L (no) 2000-09-20
US6579875B1 (en) 2003-06-17
NO315516B1 (no) 2003-09-15
EE200000430A (et) 2001-12-17
CA2315763A1 (en) 1999-07-29
SK10922000A3 (sk) 2001-03-12
BR9906905A (pt) 2000-10-10
IL136442A0 (en) 2001-06-14

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