EA020071B1 - Замещенные производные триазолопиридазина - Google Patents

Замещенные производные триазолопиридазина Download PDF

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Publication number
EA020071B1
EA020071B1 EA201100409A EA201100409A EA020071B1 EA 020071 B1 EA020071 B1 EA 020071B1 EA 201100409 A EA201100409 A EA 201100409A EA 201100409 A EA201100409 A EA 201100409A EA 020071 B1 EA020071 B1 EA 020071B1
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EA
Eurasian Patent Office
Prior art keywords
compound
present
compounds
deuterium
pharmaceutically acceptable
Prior art date
Application number
EA201100409A
Other languages
English (en)
Russian (ru)
Other versions
EA201100409A1 (ru
Inventor
Скотт Харбесон
Original Assignee
Консерт Фармасьютикалс Инк.
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 Консерт Фармасьютикалс Инк. filed Critical Консерт Фармасьютикалс Инк.
Publication of EA201100409A1 publication Critical patent/EA201100409A1/ru
Publication of EA020071B1 publication Critical patent/EA020071B1/ru

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed 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
    • A61K31/495Heterocyclic 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
    • A61K31/50Pyridazines; Hydrogenated pyridazines
    • A61K31/5025Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02Muscle relaxants, e.g. for tetanus or cramps
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/06Antimigraine agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B59/00Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
    • C07B59/002Heterocyclic compounds

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (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)
  • Epidemiology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
EA201100409A 2008-08-29 2009-08-28 Замещенные производные триазолопиридазина EA020071B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US9329308P 2008-08-29 2008-08-29
PCT/US2009/055427 WO2010025407A1 (en) 2008-08-29 2009-08-28 Substituted triazolo-pyridazine derivatives

Publications (2)

Publication Number Publication Date
EA201100409A1 EA201100409A1 (ru) 2011-10-31
EA020071B1 true EA020071B1 (ru) 2014-08-29

Family

ID=41721962

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201100409A EA020071B1 (ru) 2008-08-29 2009-08-28 Замещенные производные триазолопиридазина

Country Status (17)

Country Link
US (4) US8003646B2 (enExample)
EP (2) EP2716158A1 (enExample)
JP (3) JP5183808B2 (enExample)
KR (1) KR20110063479A (enExample)
CN (2) CN102176826B (enExample)
AU (1) AU2009285533B2 (enExample)
BR (1) BRPI0912928A2 (enExample)
CA (1) CA2735549A1 (enExample)
DK (1) DK2328414T3 (enExample)
EA (1) EA020071B1 (enExample)
ES (1) ES2451542T3 (enExample)
HR (1) HRP20140195T1 (enExample)
MX (1) MX2011002278A (enExample)
PL (1) PL2328414T3 (enExample)
PT (1) PT2328414E (enExample)
WO (1) WO2010025407A1 (enExample)
ZA (1) ZA201102123B (enExample)

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MX2011002278A (es) 2008-08-29 2011-04-14 Concert Pharmaceuticals Inc Derivados de triazolo-piridazina sustituidos.
EP2340782A4 (en) 2008-10-03 2014-04-02 Inst Alberto Luiz Coimbra De Pos Graduacao E Pesquisa De Engenharia Coppe Ufrj METHOD AND DEVICE FOR REMOVING METAL FRAGMENTS AND METAL ELEMENTS FROM TOOTH ROOT CHANNELS
JP2012531419A (ja) 2009-06-23 2012-12-10 コンサート ファーマシューティカルズ インコーポレイテッド Gaba−a受容体修飾物質としての重水素修飾されたトリアゾロピリダジン誘導体
KR20140077963A (ko) 2011-10-20 2014-06-24 글락소스미스클라인 엘엘씨 시르투인 조절제로서의 치환된 비시클릭 아자-헤테로사이클 및 유사체
KR20140077964A (ko) * 2011-10-20 2014-06-24 글락소스미스클라인 엘엘씨 시르투인 조절제로서의 치환된 비시클릭 아자-헤테로사이클 및 유사체
BR112014016930A8 (pt) 2012-01-11 2017-12-26 Bayer Ip Gmbh compostos tetrazol-5-il- e triazol-5-il-arila e uso destes como herbicidas
US20150099753A1 (en) * 2012-05-11 2015-04-09 Concert Pharmaceuticals Inc. Form 5 polymorph of 7-(tert-butyl-d9)-3-(2,5-difluorophenyl)-6-((1-methyl-1h-1,2,4-triazol-5-yl)methoxy)-[1,2,4]triazolo[4,3-b]pyridazine
JP2015516440A (ja) * 2012-05-11 2015-06-11 コンサート ファーマシューティカルズ インコーポレイテッド 7−(tert−ブチル−d9)−3−(2,5−ジフルオロフェニル)−6−((1−メチル−1H−1,2,4−トリアゾール−5−イル)メトキシ)−[1,2,4]トリアゾロ[4,3−b]ピリダジンの2型多形
US20150158870A1 (en) * 2012-05-11 2015-06-11 Concert Pharmaceuticals Inc. Polymorphs of 7-(tert-butyl-d9)-3-(2,5-difluorophenyl)-6-((1-methyl-1h-1,2,4-triazol-5-yl)methoxy)-[1,2,4]triazolo[4,3-b]pyridazine
WO2015052178A1 (en) 2013-10-10 2015-04-16 Basf Se 1,2,5-oxadiazole compounds and their use as herbicides
WO2015052173A1 (en) 2013-10-10 2015-04-16 Basf Se Tetrazole and triazole compounds and their use as herbicides
WO2015095549A1 (en) * 2013-12-18 2015-06-25 Concert Pharmaceuticals, Inc. Dosage regimen for gabaa receptor subtype selective drug
EA201691582A1 (ru) 2014-02-07 2017-01-30 Оспекс Фармасьютикалз, Инк. Новые фармацевтические препараты
CN104474549A (zh) * 2014-11-24 2015-04-01 王寿世 异丙酚和gabaa受体拮抗剂在制备麻醉药物中的用途
CN104353078B (zh) * 2014-11-24 2017-10-24 王寿世 一种麻醉用药物组合物
US10026332B1 (en) 2017-04-10 2018-07-17 Jasmine Gupta Method to deliver contextual educational information utilizing smart wearables
WO2020191047A1 (en) * 2019-03-18 2020-09-24 Neurocycle Therapeutics, Inc. Use of gabaa receptor modulators for treatment of pain
WO2023205722A1 (en) * 2022-04-20 2023-10-26 Engrail Therapeutics, Inc. Gabaa receptor modulator salts, particles, and uses thereof

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2136684C1 (ru) * 1993-10-13 1999-09-10 Кноль Аг Производные 1,2,4-триазоло [1,5-a]пиримидинов, их фармацевтически приемлемые соли и стереоизомеры, фармацевтическая композиция и способ ингибирования припадков
US6255305B1 (en) * 1996-07-25 2001-07-03 Merck Sharp & Dohme Limited Substituted triazolo-pyridazine derivatives as ligands for GABA receptors
US20020165217A1 (en) * 2001-05-01 2002-11-07 Pfizer Inc. Combination treatment for anxiety and depression

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US6221335B1 (en) 1994-03-25 2001-04-24 Isotechnika, Inc. Method of using deuterated calcium channel blockers
AU707748B2 (en) 1994-03-25 1999-07-22 Isotechnika Inc. Enhancement of the efficacy of drugs by deuteration
MXPA00007135A (es) * 1998-01-21 2002-11-07 Merck Sharp & Dohme Derivados de triazolo-piridazina como ligandos para receptores gaba.
US6440710B1 (en) 1998-12-10 2002-08-27 The Scripps Research Institute Antibody-catalyzed deuteration, tritiation, dedeuteration or detritiation of carbonyl compounds
ES2232416T3 (es) * 1999-01-27 2005-06-01 MERCK SHARP & DOHME LTD. Derivados de triazolo-piridazina como ligandos para receptores gaba.
ES2193921T3 (es) 1999-12-03 2003-11-16 Pfizer Prod Inc Compuestos de sulfamoilheteroaril-pirazol como agentes antinflamatorios/analgesicos.
TW200413273A (en) 2002-11-15 2004-08-01 Wako Pure Chem Ind Ltd Heavy hydrogenation method of heterocyclic rings
DE60315876T2 (de) * 2002-11-28 2008-05-21 Neurosearch A/S Verfahren zum screening für verbindungen mit sedativer oder anxiolytischer potenz
WO2006061428A2 (en) 2004-12-10 2006-06-15 Universität Zürich Gaba-a alpha 2 and alpha 3 receptor agonists for treating neuropathic, inflammatory and migraine associated pain
US7598273B2 (en) 2005-10-06 2009-10-06 Auspex Pharmaceuticals, Inc Inhibitors of the gastric H+, K+-ATPase with enhanced therapeutic properties
US7750168B2 (en) 2006-02-10 2010-07-06 Sigma-Aldrich Co. Stabilized deuteroborane-tetrahydrofuran complex
JO2630B1 (en) 2006-04-13 2012-06-17 نوفارتيس ايه جي Organic compounds
CN101594870A (zh) * 2006-08-22 2009-12-02 康塞特医药品有限公司 4-氨基喹唑啉衍生物及其使用方法
EP2059241A1 (en) 2006-09-05 2009-05-20 Schering Corporation Pharmaceutical combinations for lipid management and in the treatment of atherosclerosis and hepatic steatosis
BRPI0809171A2 (pt) * 2007-04-02 2014-09-16 Auspex Pharmaceuticals Inc "composto, composição farmacêutica, método para tratamento,prevençõ ou melhora de um ou mais , sintomas de uma desordem mediada pela endotelina em um sujeito, método de inibição de ligação d euma endotelina a um receptor eta ou etb e método para modular a atividade mediada pelo receptor de endotelina"
MX2011002278A (es) * 2008-08-29 2011-04-14 Concert Pharmaceuticals Inc Derivados de triazolo-piridazina sustituidos.

Patent Citations (3)

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Publication number Priority date Publication date Assignee Title
RU2136684C1 (ru) * 1993-10-13 1999-09-10 Кноль Аг Производные 1,2,4-триазоло [1,5-a]пиримидинов, их фармацевтически приемлемые соли и стереоизомеры, фармацевтическая композиция и способ ингибирования припадков
US6255305B1 (en) * 1996-07-25 2001-07-03 Merck Sharp & Dohme Limited Substituted triazolo-pyridazine derivatives as ligands for GABA receptors
US20020165217A1 (en) * 2001-05-01 2002-11-07 Pfizer Inc. Combination treatment for anxiety and depression

Also Published As

Publication number Publication date
AU2009285533A1 (en) 2010-03-04
JP5183808B2 (ja) 2013-04-17
WO2010025407A1 (en) 2010-03-04
MX2011002278A (es) 2011-04-14
PL2328414T3 (pl) 2014-05-30
US20150111895A1 (en) 2015-04-23
CN104098578A (zh) 2014-10-15
US8003646B2 (en) 2011-08-23
AU2009285533A2 (en) 2011-04-21
EP2716158A1 (en) 2014-04-09
JP2014058518A (ja) 2014-04-03
ES2451542T3 (es) 2014-03-27
JP2012501346A (ja) 2012-01-19
JP2013100322A (ja) 2013-05-23
ZA201102123B (en) 2011-12-28
HRP20140195T1 (hr) 2014-04-11
KR20110063479A (ko) 2011-06-10
US8921366B2 (en) 2014-12-30
EA201100409A1 (ru) 2011-10-31
CA2735549A1 (en) 2010-03-04
PT2328414E (pt) 2014-03-17
US20100056529A1 (en) 2010-03-04
EP2328414A1 (en) 2011-06-08
JP5373982B2 (ja) 2013-12-18
US20130225590A1 (en) 2013-08-29
EP2328414A4 (en) 2011-11-16
DK2328414T3 (en) 2014-03-10
AU2009285533B2 (en) 2014-02-13
BRPI0912928A2 (pt) 2015-08-04
US8399467B2 (en) 2013-03-19
US20120004236A1 (en) 2012-01-05
CN102176826A (zh) 2011-09-07
CN102176826B (zh) 2014-08-20
EP2328414B1 (en) 2013-12-11

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Legal Events

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MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ BY KZ KG MD TJ TM RU