EA201170736A1 - Синтез и новые солевые формы (r)-3-((e)-2-(пирролидин-3-ил)винил)-5-(тетрагидропиран-4-илокси) пиридина - Google Patents

Синтез и новые солевые формы (r)-3-((e)-2-(пирролидин-3-ил)винил)-5-(тетрагидропиран-4-илокси) пиридина

Info

Publication number
EA201170736A1
EA201170736A1 EA201170736A EA201170736A EA201170736A1 EA 201170736 A1 EA201170736 A1 EA 201170736A1 EA 201170736 A EA201170736 A EA 201170736A EA 201170736 A EA201170736 A EA 201170736A EA 201170736 A1 EA201170736 A1 EA 201170736A1
Authority
EA
Eurasian Patent Office
Prior art keywords
synthesis
new salt
shapes
relates
present
Prior art date
Application number
EA201170736A
Other languages
English (en)
Other versions
EA021054B1 (ru
Inventor
Сринивиса Рао Акиредди
Скотт Р. Брейнинг
Тимоти Дж. Катбертсон
Гари Морис Далл
Грегори Дж. Гатто
Джон Дженус
Филип С. Хэммонд
Джозеф Пайк мл. Митченер
Хулио А. Муньос
Питер Альберт Оттен
Дэниел Йоханнес
Николай Федоров
Original Assignee
Таргасепт, 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 Таргасепт, Инк. filed Critical Таргасепт, Инк.
Publication of EA201170736A1 publication Critical patent/EA201170736A1/ru
Publication of EA021054B1 publication Critical patent/EA021054B1/ru

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
    • A61K31/435—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
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/08—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • 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
    • A61P25/18—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
    • A61P25/28—Drugs 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
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Obesity (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Hospice & Palliative Care (AREA)
  • Virology (AREA)
  • Rheumatology (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Pyridine Compounds (AREA)

Abstract

Настоящее изобретение относится к (R)-3-((Е)-2-(пирролидин-3-ил)винил)-5-(тетрагидропиран-4-илокси)пиридину и его солевым формам, а также к способам промышленного производства этих соединений с чистотой и качеством, достаточными для их применения в фармацевтических композициях. Настоящее изобретение также относится к применению указанного соединения в целях приготовления лекарственного средства для лечения расстройств ЦНС.
EA201170736A 2008-12-01 2009-11-30 Синтез и новые солевые формы (r)-3-((e)-2-(пирролидин-3-ил)винил)-5-(тетрагидропиран-4-илокси)пиридина EA021054B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US11888508P 2008-12-01 2008-12-01
PCT/US2009/066092 WO2010065449A1 (en) 2008-12-01 2009-11-30 (r) -3- (e) -2- (pyrr0lidin-3-yl) vinyl) -5- (tetrahydr0pyran-4-yl0xy) pyridine, its salts, its synthesis and its use as ligand for nicotinic acetylcholinergic receptors

Publications (2)

Publication Number Publication Date
EA201170736A1 true EA201170736A1 (ru) 2011-12-30
EA021054B1 EA021054B1 (ru) 2015-03-31

Family

ID=41549744

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201170736A EA021054B1 (ru) 2008-12-01 2009-11-30 Синтез и новые солевые формы (r)-3-((e)-2-(пирролидин-3-ил)винил)-5-(тетрагидропиран-4-илокси)пиридина

Country Status (28)

Country Link
US (3) US8153821B2 (ru)
EP (3) EP2896619A1 (ru)
JP (2) JP5698673B2 (ru)
KR (2) KR20110094100A (ru)
CN (2) CN102227406B (ru)
AR (1) AR074239A1 (ru)
AU (2) AU2009322630A1 (ru)
BR (2) BRPI0922152A2 (ru)
CA (2) CA2744191A1 (ru)
CL (2) CL2009002146A1 (ru)
CO (1) CO6382158A2 (ru)
EA (1) EA021054B1 (ru)
EC (1) ECSP11011135A (ru)
ES (1) ES2403022T3 (ru)
HK (1) HK1157778A1 (ru)
IL (2) IL212796A0 (ru)
MX (2) MX2011005713A (ru)
MY (1) MY159040A (ru)
NZ (1) NZ593058A (ru)
PE (1) PE20100467A1 (ru)
RU (1) RU2507197C2 (ru)
SA (1) SA109300715B1 (ru)
SG (2) SG171876A1 (ru)
TW (1) TW201024283A (ru)
UA (1) UA106217C2 (ru)
UY (1) UY32278A (ru)
WO (2) WO2010065447A2 (ru)
ZA (1) ZA201103497B (ru)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3279195B1 (en) * 2008-12-01 2020-07-01 Oyster Point Pharma, Inc. Synthesis and novel salt forms of (r)-5-((e)-2-pyrrolidin-3-ylvinyl)pyrimidine
US9145396B2 (en) 2008-12-01 2015-09-29 Targacept, Inc. Synthesis and novel salt forms of (R)-5-((E)-2-pyrrolidin-3ylvinyl)pyrimidine
US20130196340A1 (en) * 2012-01-30 2013-08-01 Roar Holding Llc Ex vivo plasma enzyme activity assay using inhibitors as a negative control
AP2015008579A0 (en) 2013-02-05 2015-07-31 Purdue Pharma Lp Tamper resistant pharmaceutical formulations
US20160262372A1 (en) * 2015-03-13 2016-09-15 Cornell Kunz Extermination Treatment Appliance And Method
JP7090551B2 (ja) 2016-04-07 2022-06-24 オイスター ポイント ファーマ インコーポレイテッド 眼状態の治療方法

Family Cites Families (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SK94393A3 (en) * 1992-09-11 1994-08-10 Thomae Gmbh Dr K Cyclic derivatives of urea, process for their production and their pharmaceutical agents with the content of those
IL107184A (en) 1992-10-09 1997-08-14 Abbott Lab Heterocyclic ether compounds that enhance cognitive function
US5852041A (en) 1993-04-07 1998-12-22 Sibia Neurosciences, Inc. Substituted pyridines useful as modulators of acethylcholine receptors
US5604231A (en) 1995-01-06 1997-02-18 Smith; Carr J. Pharmaceutical compositions for prevention and treatment of ulcerative colitis
US5597919A (en) 1995-01-06 1997-01-28 Dull; Gary M. Pyrimidinyl or Pyridinyl alkenyl amine compounds
JP3745433B2 (ja) * 1995-02-02 2006-02-15 第一製薬株式会社 複素環式化合物
US5585388A (en) 1995-04-07 1996-12-17 Sibia Neurosciences, Inc. Substituted pyridines useful as modulators of acetylcholine receptors
US5583140A (en) 1995-05-17 1996-12-10 Bencherif; Merouane Pharmaceutical compositions for the treatment of central nervous system disorders
IL118279A (en) 1995-06-07 2006-10-05 Abbott Lab Compounds 3 - Pyridyloxy (or Thio) Alkyl Heterocyclic Pharmaceutical Compositions Containing Them and Their Uses for Preparing Drugs to Control Synaptic Chemical Transmission
PL332240A1 (en) * 1996-09-13 1999-08-30 Schering Corp Tricyclic compounds useful in inhibiting g-proteinic function and in treating proliferative diseases
TW492957B (en) * 1996-11-07 2002-07-01 Novartis Ag N-substituted 2-cyanopyrrolidnes
ZA9711092B (en) 1996-12-11 1999-07-22 Smithkline Beecham Corp Novel compounds.
JPH1171345A (ja) * 1997-08-30 1999-03-16 Nippon Nohyaku Co Ltd 光学活性なピロリジン誘導体及びその中間体並びにそれらの製造法
US6310043B1 (en) 1998-08-07 2001-10-30 Governors Of The University Of Alberta Treatment of bacterial infections
GB9821503D0 (en) 1998-10-02 1998-11-25 Novartis Ag Organic compounds
EP1302458A4 (en) * 2000-07-11 2005-10-19 Banyu Pharma Co Ltd ESTERDERIVATE
WO2003013526A1 (en) * 2001-08-08 2003-02-20 Merck & Co. Inc. Anticoagulant compounds
US7098331B2 (en) * 2003-03-05 2006-08-29 Targacept, Inc. Arylvinylazacycloalkane compounds and methods of preparation and use thereof
WO2007054777A1 (en) * 2005-11-09 2007-05-18 Orchid Chemicals & Pharmaceuticals Limited Depletion of isomer in cephalosporin antibiotic
CN101490052B (zh) * 2006-05-12 2012-08-08 美瑞德生物工程公司 治疗性化合物及其在癌症中的用途

Also Published As

Publication number Publication date
WO2010065447A3 (en) 2010-07-22
UA106217C2 (en) 2014-08-11
EP2358670A2 (en) 2011-08-24
CA2744191A1 (en) 2010-06-10
MX2011005713A (es) 2011-06-17
CN102227406B (zh) 2013-07-31
CN102232072A (zh) 2011-11-02
SA109300715B1 (ar) 2014-06-25
JP2012510472A (ja) 2012-05-10
WO2010065447A2 (en) 2010-06-10
US20110269975A1 (en) 2011-11-03
US20120015983A1 (en) 2012-01-19
CA2744197A1 (en) 2010-06-10
KR20110094100A (ko) 2011-08-19
UY32278A (es) 2011-06-30
HK1157778A1 (en) 2012-07-06
BRPI0922630A2 (pt) 2016-01-05
SG171432A1 (en) 2011-07-28
MX2011005712A (es) 2011-06-17
IL212796A0 (en) 2011-07-31
NZ593058A (en) 2013-06-28
EP2896619A1 (en) 2015-07-22
SG171876A1 (en) 2011-07-28
RU2011127004A (ru) 2013-01-10
AR074239A1 (es) 2010-12-29
CL2009002145A1 (es) 2010-04-30
US20140107163A1 (en) 2014-04-17
AU2009322630A1 (en) 2010-06-10
AU2009322628A1 (en) 2010-06-10
KR20110094318A (ko) 2011-08-23
CL2009002146A1 (es) 2010-04-30
US8153821B2 (en) 2012-04-10
US8633227B2 (en) 2014-01-21
PE20100467A1 (es) 2010-08-03
IL212799A0 (en) 2011-07-31
JP2012510473A (ja) 2012-05-10
MY159040A (en) 2016-12-15
CN102227406A (zh) 2011-10-26
EP2358705A1 (en) 2011-08-24
IL212799A (en) 2013-12-31
ES2403022T3 (es) 2013-05-13
WO2010065449A1 (en) 2010-06-10
CO6382158A2 (es) 2012-02-15
EA021054B1 (ru) 2015-03-31
ZA201103497B (en) 2012-01-25
CN102232072B (zh) 2014-09-24
RU2507197C2 (ru) 2014-02-20
ECSP11011135A (es) 2011-07-29
TW201024283A (en) 2010-07-01
JP5698673B2 (ja) 2015-04-08
EP2358670B1 (en) 2012-10-24
JP5615836B2 (ja) 2014-10-29
BRPI0922152A2 (pt) 2015-08-18

Similar Documents

Publication Publication Date Title
EA201300250A1 (ru) Оксадиазольные ингибиторы продуцирования лейкотриена
EA201001585A1 (ru) Производные тиенопиридона в качестве активаторов амр-активированной протеинкиназы (амрк)
EA201391532A1 (ru) Конденсированные гетероциклические соединения в качестве модуляторов ионных каналов
MX2007007845A (es) Sulfonilpirrolidinas, metodo para producir las mismas y su uso como medicamento.
EA201290121A1 (ru) Конденсированные гетероциклические соединения в качестве модуляторов ионных каналов
EA201001733A1 (ru) Производные тиенопиридона в качестве активаторов амр-активированной протеинкиназы (амрк)
EA200901138A1 (ru) Производные дианилинопиримидина как ингибиторы киназы wee1, фармацевтическая композиция и применение
EA200702329A1 (ru) Замещенные пирролпиридины, содержащие их композиции, способ получения и применение
NZ716487A (en) Process for the preparation of n-[5-(3,5-difluoro-benzyl)-1h-indazol-3-yl]-4-(4-methyl-piperazin-1-yl)-2-(tetrahydro-pyran-4-ylamino)-benzamide
EA201190235A1 (ru) Замещенные 1-цианоэтилгетероциклилкарбоксамидные соединения 750
EA201500298A1 (ru) Алкоксипиразолы в качестве активаторов растворимой гуанилатциклазы
EA201071298A1 (ru) Соединение 3-аминокарбазола, фармацевтическая композиция, его содержащая, и способ их получения
EA201001647A1 (ru) Производные бензофурана, бензотиофена, бензотиазола в качестве fxr модуляторов
EA201100503A1 (ru) Глюкозидные производные и их применения
EA201001683A1 (ru) Производные фенил- или пиридинилзамещенных индазолов
EA201301181A1 (ru) Триазолопиридины
MX2014000536A (es) Compuestos de 4-piperidinilo para usarse como inhibidores de tanquirasa.
EA201370166A1 (ru) Содержащие диарилацетиленгидразид ингибиторы тирозинкиназы
MY160785A (en) Manufacturing process for pyrimidine derivatives
EA201500182A1 (ru) 4-МЕТИЛ-2,3,5,9,9b-ПЕНТААЗАЦИКЛОПЕНТА[a]НАФТАЛИНЫ
EA200702253A1 (ru) Фармацевтическая композиция
EA201170736A1 (ru) Синтез и новые солевые формы (r)-3-((e)-2-(пирролидин-3-ил)винил)-5-(тетрагидропиран-4-илокси) пиридина
PH12015500860A1 (en) 2-phenyl -5- heterocyclyl -tetrahydro-2h- pyran-3-amine compounds for use in the treatment of diabetes and its associated disorders
MX2009011059A (es) Aminopirimidinas utiles como inhibidores de cinasas.
EA201391026A1 (ru) Кристаллическое производное оксазина и его применение в качестве ингибитора bace

Legal Events

Date Code Title Description
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