BRPI0922759A2 - síntese e novas formas de sal de (r)-5((e)-2-(pirrolidin-3-ilvinil)pirimidina - Google Patents

síntese e novas formas de sal de (r)-5((e)-2-(pirrolidin-3-ilvinil)pirimidina

Info

Publication number
BRPI0922759A2
BRPI0922759A2 BRPI0922759A BRPI0922759A BRPI0922759A2 BR PI0922759 A2 BRPI0922759 A2 BR PI0922759A2 BR PI0922759 A BRPI0922759 A BR PI0922759A BR PI0922759 A BRPI0922759 A BR PI0922759A BR PI0922759 A2 BRPI0922759 A2 BR PI0922759A2
Authority
BR
Brazil
Prior art keywords
ylvinyl
pyrrolidin
pyrimidine
synthesis
salt forms
Prior art date
Application number
BRPI0922759A
Other languages
English (en)
Inventor
Balwinder Singh Bhatti
Craig Harrison Miller
Gary Maurice Dull
Joseph Pike Mitchener Jr
Julio A Munoz
Pieter Albert Otten
Srinivisa Rao Akireddy
Timothy J Cuthbertson
Original Assignee
Targacept Inc
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=41650077&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=BRPI0922759(A2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Targacept Inc filed Critical Targacept Inc
Publication of BRPI0922759A2 publication Critical patent/BRPI0922759A2/pt

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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/10—Laxatives
    • 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
    • A61P25/24—Antidepressants
    • 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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A61P29/02—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect
    • 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
    • C07D207/06—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 radicals, containing only hydrogen and carbon atoms, attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Rheumatology (AREA)
  • Epidemiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
BRPI0922759A 2008-12-01 2009-11-30 síntese e novas formas de sal de (r)-5((e)-2-(pirrolidin-3-ilvinil)pirimidina BRPI0922759A2 (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US11879608P 2008-12-01 2008-12-01
PCT/US2009/066078 WO2010065443A1 (en) 2008-12-01 2009-11-30 Synthesis and novel salt forms of (r)-5-((e)-2-(pyrrolidin-3-ylvinyl)pyrimidine

Publications (1)

Publication Number Publication Date
BRPI0922759A2 true BRPI0922759A2 (pt) 2016-01-05

Family

ID=41650077

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI0922759A BRPI0922759A2 (pt) 2008-12-01 2009-11-30 síntese e novas formas de sal de (r)-5((e)-2-(pirrolidin-3-ilvinil)pirimidina

Country Status (25)

Country Link
US (1) US8604191B2 (pt)
EP (2) EP2364307B1 (pt)
JP (1) JP5710490B2 (pt)
KR (1) KR20110098763A (pt)
CN (1) CN102232070A (pt)
AU (1) AU2009322624B2 (pt)
BR (1) BRPI0922759A2 (pt)
CA (2) CA3090738C (pt)
CL (1) CL2011001258A1 (pt)
CO (1) CO6390106A2 (pt)
DK (1) DK3279195T3 (pt)
EC (1) ECSP11011167A (pt)
ES (2) ES2820857T3 (pt)
HU (1) HUE050540T2 (pt)
IL (2) IL266097B (pt)
MX (1) MX2011005611A (pt)
NZ (3) NZ592554A (pt)
PE (1) PE20110589A1 (pt)
PL (1) PL3279195T3 (pt)
PT (1) PT3279195T (pt)
RU (2) RU2533819C2 (pt)
SG (2) SG10201902903RA (pt)
UA (1) UA107336C2 (pt)
WO (1) WO2010065443A1 (pt)
ZA (1) ZA201103737B (pt)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9145396B2 (en) * 2008-12-01 2015-09-29 Targacept, Inc. Synthesis and novel salt forms of (R)-5-((E)-2-pyrrolidin-3ylvinyl)pyrimidine
US20130237550A1 (en) * 2010-03-11 2013-09-12 Targacept, Inc. Arylvinylazacycloalkane compounds for constipation
EP3848028B9 (en) 2014-10-20 2024-10-16 Oyster Point Pharma, Inc. Methods of treating ocular conditions
MX385698B (es) * 2016-04-07 2025-03-18 Oyster Point Pharma Inc Uso de un compuesto que comprende un grupo pirrolidinilo y pirimidinilo para tratar enfermedades oculares
EP3820443A1 (en) 2018-07-10 2021-05-19 Oyster Point Pharma, Inc. Combinations of positive allosteric modulators and nicotinic acetylcholine receptor agonists for treating ocular conditions
WO2020014217A1 (en) 2018-07-10 2020-01-16 Oyster Point Pharma, Inc. Methods of treating ocular conditions
ES3039903T3 (en) 2020-04-28 2025-10-27 Oyster Point Pharma Inc Local administration of nicotinic acetylcholine receptor agonists for the inhibition of coronavirus infections

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US4649041A (en) * 1983-07-20 1987-03-10 Warner-Lambert Company Magnesium trisilicate suitable for preparation of medicament adsorbates of antinauseants
SU1605922A3 (ru) * 1987-05-01 1990-11-07 Фудзисава Фармасьютикал Ко., Лтд (Фирма) Способ получени производных пирролидина или их солей
US5202128A (en) * 1989-01-06 1993-04-13 F. H. Faulding & Co. Limited Sustained release pharmaceutical composition
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
US5493026A (en) 1993-10-25 1996-02-20 Organix, Inc. Substituted 2-carboxyalkyl-3-(fluorophenyl)-8-(3-halopropen-2-yl) nortropanes and their use as imaging for agents for neurodegenerative disorders
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
US5585388A (en) 1995-04-07 1996-12-17 Sibia Neurosciences, Inc. Substituted pyridines useful as modulators of acetylcholine receptors
ES2097703B1 (es) * 1995-04-12 1997-12-01 Decox S L Una nueva composicion estimulante de la actividad cerebral basada en alcaloides de nucleo de eburnamenina, y sus metodos de preparacion.
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
US5726189A (en) 1996-05-03 1998-03-10 The United States Of America, Represented By The Secretary, Department Of Health And Human Services Method for imaging nicotinic acetylcholinergic receptors in the brain using radiolabeled pyridyl-7-azabicyclo 2.2.1!heptanes
US5795909A (en) * 1996-05-22 1998-08-18 Neuromedica, Inc. DHA-pharmaceutical agent conjugates of taxanes
ZA9711092B (en) 1996-12-11 1999-07-22 Smithkline Beecham Corp Novel compounds.
US5952339A (en) 1998-04-02 1999-09-14 Bencherif; Merouane Pharmaceutical compositions and methods of using nicotinic antagonists for treating a condition or disorder characterized by alteration in normal neurotransmitter release
US6310043B1 (en) 1998-08-07 2001-10-30 Governors Of The University Of Alberta Treatment of bacterial infections
US6761903B2 (en) * 1999-06-30 2004-07-13 Lipocine, Inc. Clear oil-containing pharmaceutical compositions containing a therapeutic agent
EP1225955A1 (en) * 1999-11-01 2002-07-31 Targacept, Inc. Aryl olefinic azacyclic, and aryl acetylenic azacyclic compounds, pharmaceutical compositions containing them and their use as inhibitors of nicotinic cholinergic receptors
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
US6872827B2 (en) * 2002-04-26 2005-03-29 Chembridge Research Laboratories, Inc. Somatostatin analogue compounds
US7098331B2 (en) * 2003-03-05 2006-08-29 Targacept, Inc. Arylvinylazacycloalkane compounds and methods of preparation and use thereof
AU2005226729B2 (en) * 2004-03-25 2010-01-28 Janssen Pharmaceutica N.V. Imidazole compounds
TW200716110A (en) * 2005-04-20 2007-05-01 Smithkline Beecham Corp Inhibitors of AKT activity
US7598255B2 (en) * 2005-08-04 2009-10-06 Janssen Pharmaceutica Nv Pyrimidine compounds as serotonin receptor modulators
US20060223820A1 (en) * 2006-03-21 2006-10-05 Chemagis Ltd. Crystalline aripiprazole salts and processes for preparation and purification thereof
WO2008157365A2 (en) * 2007-06-15 2008-12-24 Targacept, Inc. Vinylazacycloalkanes for treating neuropathic pain
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Also Published As

Publication number Publication date
UA107336C2 (ru) 2014-12-25
RU2011127010A (ru) 2013-01-10
NZ592554A (en) 2013-08-30
PE20110589A1 (es) 2011-09-07
NZ611965A (en) 2015-01-30
JP2012510471A (ja) 2012-05-10
SG10201902903RA (en) 2019-05-30
RU2014136983A (ru) 2016-04-10
ZA201103737B (en) 2012-01-25
CA2742366A1 (en) 2010-06-10
AU2009322624B2 (en) 2015-06-11
PT3279195T (pt) 2020-09-29
PL3279195T3 (pl) 2020-12-14
IL266097A (en) 2019-06-30
RU2533819C2 (ru) 2014-11-20
KR20110098763A (ko) 2011-09-01
US8604191B2 (en) 2013-12-10
EP3279195A1 (en) 2018-02-07
WO2010065443A1 (en) 2010-06-10
EP2364307B1 (en) 2017-07-05
CN102232070A (zh) 2011-11-02
CA2742366C (en) 2020-09-22
IL212798B (en) 2019-05-30
EP3279195B1 (en) 2020-07-01
HUE050540T2 (hu) 2020-12-28
CO6390106A2 (es) 2012-02-29
IL266097B (en) 2022-07-01
RU2700796C2 (ru) 2019-09-23
AU2009322624A1 (en) 2010-06-10
CA3090738C (en) 2023-06-13
ES2820857T3 (es) 2021-04-22
NZ703381A (en) 2016-03-31
ECSP11011167A (es) 2011-10-31
CA3090738A1 (en) 2010-06-10
DK3279195T3 (en) 2020-08-17
CL2011001258A1 (es) 2011-09-02
JP5710490B2 (ja) 2015-04-30
HK1250572A1 (en) 2018-12-28
US20110281895A1 (en) 2011-11-17
SG10201406410UA (en) 2014-11-27
ES2641762T3 (es) 2017-11-13
IL212798A0 (en) 2011-07-31
EP2364307A1 (en) 2011-09-14
MX2011005611A (es) 2011-09-15

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Legal Events

Date Code Title Description
B08F Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette]

Free format text: REFERENTE A 7A ANUIDADE.

B08K Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette]

Free format text: EM VIRTUDE DO ARQUIVAMENTO PUBLICADO NA RPI 2386 DE 27-09-2016 E CONSIDERANDO AUSENCIA DE MANIFESTACAO DENTRO DOS PRAZOS LEGAIS, INFORMO QUE CABE SER MANTIDO O ARQUIVAMENTO DO PEDIDO DE PATENTE, CONFORME O DISPOSTO NO ARTIGO 12, DA RESOLUCAO 113/2013.