AR074239A1 - Sales de (r)-3-((e)-2-(pirrolidin-3-il)vinil)-5-(tetrahidroxipiran-4-iloxi)piridina, su sintesis e intermediarios de la misma, composicion farmaceutica que las com-prende y su uso en la preparacion de un medicamento para el tratamiento de enfermedades mediadas por nnr - Google Patents

Sales de (r)-3-((e)-2-(pirrolidin-3-il)vinil)-5-(tetrahidroxipiran-4-iloxi)piridina, su sintesis e intermediarios de la misma, composicion farmaceutica que las com-prende y su uso en la preparacion de un medicamento para el tratamiento de enfermedades mediadas por nnr

Info

Publication number
AR074239A1
AR074239A1 ARP090104608A ARP090104608A AR074239A1 AR 074239 A1 AR074239 A1 AR 074239A1 AR P090104608 A ARP090104608 A AR P090104608A AR P090104608 A ARP090104608 A AR P090104608A AR 074239 A1 AR074239 A1 AR 074239A1
Authority
AR
Argentina
Prior art keywords
vinyl
pyrrolidin
tetrahydropyran
yloxy
pyridine
Prior art date
Application number
ARP090104608A
Other languages
English (en)
Inventor
Craig Harrison Miller
Pieter Albert Otten
Nikolai Fedorov
John Genus
Scott R Breining
Srinivisa Rao Akireddy
Philip S Hammond
Gregory J Gatto
Gary Maurice Dull
Julio A Munoz
Daniel Yohannes
Timothy J Cuthbertson
Balwinder Singh Bhatti
Josep Pike Mitchener Jr
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
Application filed by Targacept Inc filed Critical Targacept Inc
Publication of AR074239A1 publication Critical patent/AR074239A1/es

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

Abstract

(R)-3-((E)-2-(pirrolidin-3-il)vinil)-5-(tetrahidropiran-4-iloxi)piridina, sus formas de sales y con los procesos para la produccion en escala comercial de estos compuestos con pureza y calidad suficiente para su uso en composiciones farmacéuticas para el tratamiento de enfermedades mediadas por la modulacion de los receptores de acetilcolina nicotínico neuronal (NNR). Reivindicacion 1: Mono-L-malato de (R)-3-((E)-2-(pirrolidin-3-il)vinil)-5-(tetrahidropiran-4-iloxi)piridina, o un hidrato o solvato de él. Reivindicacion 2: Hemigalactarato de(R)-3-((E)-2-(pirrolidin-3-il)vinil)-5-(tetrahidropiran-4-iloxi)piridina, o un hidrato o solvato de él. Reivindicacion 3: Oxalato de (R)-3-((E)-2-(pirrolidin-3-il)vinil)-5-(tetrahidropiran-4-iloxi)piridina, o un hidrato o solvato de él. Reivindicacion 4: Di-p-toluoil-D-tartrato de (R)-3-((E)-2-(pirrolidin-3-il)vinil)-5-(tetrahidropiran-4-iloxi)piridina, o un hidrato o solvato de él. Reivindicacion 5: (R)-3-((E)-2-(pirrolidin-3-il)vinil)-5-(tetrahidropiran-4-iloxi)piridina, o una sal farmacéuticamente aceptable de ella sustancialmente libre de (S)-3-((E)-2-(pirrolidin-3-il)vinil)-5-(tetrahidropiran-4-iloxi)piridina. Reivindicacion 16: Un compuesto que se selecciona de: ( R)-2-(1-(terc-butoxicarbonil)pirrolidin-3-il)malonato de dietilo; Ácido ( R)-2-(1-(terc-butoxicarbonil)pirrolidin-3-il)malonico; (R)-3- (2-hidroxietil) pirrolidina-1-carboxilato de terc-butilo; y (R)-3-(2-yodoetil)pirrolidina-1-carboxilato de terc-butilo.
ARP090104608A 2008-12-01 2009-11-30 Sales de (r)-3-((e)-2-(pirrolidin-3-il)vinil)-5-(tetrahidroxipiran-4-iloxi)piridina, su sintesis e intermediarios de la misma, composicion farmaceutica que las com-prende y su uso en la preparacion de un medicamento para el tratamiento de enfermedades mediadas por nnr AR074239A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US11888508P 2008-12-01 2008-12-01

Publications (1)

Publication Number Publication Date
AR074239A1 true AR074239A1 (es) 2010-12-29

Family

ID=41549744

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP090104608A AR074239A1 (es) 2008-12-01 2009-11-30 Sales de (r)-3-((e)-2-(pirrolidin-3-il)vinil)-5-(tetrahidroxipiran-4-iloxi)piridina, su sintesis e intermediarios de la misma, composicion farmaceutica que las com-prende y su uso en la preparacion de un medicamento para el tratamiento de enfermedades mediadas por nnr

Country Status (28)

Country Link
US (3) US8153821B2 (es)
EP (3) EP2896619A1 (es)
JP (2) JP5615836B2 (es)
KR (2) KR20110094318A (es)
CN (2) CN102227406B (es)
AR (1) AR074239A1 (es)
AU (2) AU2009322630A1 (es)
BR (2) BRPI0922630A2 (es)
CA (2) CA2744197A1 (es)
CL (2) CL2009002146A1 (es)
CO (1) CO6382158A2 (es)
EA (1) EA021054B1 (es)
EC (1) ECSP11011135A (es)
ES (1) ES2403022T3 (es)
HK (1) HK1157778A1 (es)
IL (2) IL212799A (es)
MX (2) MX2011005712A (es)
MY (1) MY159040A (es)
NZ (1) NZ593058A (es)
PE (1) PE20100467A1 (es)
RU (1) RU2507197C2 (es)
SA (1) SA109300715B1 (es)
SG (2) SG171876A1 (es)
TW (1) TW201024283A (es)
UA (1) UA106217C2 (es)
UY (1) UY32278A (es)
WO (2) WO2010065447A2 (es)
ZA (1) ZA201103497B (es)

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US9145396B2 (en) 2008-12-01 2015-09-29 Targacept, Inc. Synthesis and novel salt forms of (R)-5-((E)-2-pyrrolidin-3ylvinyl)pyrimidine
WO2013116371A1 (en) * 2012-01-30 2013-08-08 Roar Biomedical Inc. Ex vivo plasma enzyme activity assay using inhibitors as a negative control
US9149533B2 (en) 2013-02-05 2015-10-06 Purdue Pharma L.P. Tamper resistant pharmaceutical formulations
US20160262372A1 (en) * 2015-03-13 2016-09-15 Cornell Kunz Extermination Treatment Appliance And Method
KR102485299B1 (ko) 2016-04-07 2023-01-06 오이스터 포인트 파마 인코포레이티드 안구 장애의 치료 방법

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Also Published As

Publication number Publication date
CL2009002145A1 (es) 2010-04-30
CN102227406B (zh) 2013-07-31
IL212799A (en) 2013-12-31
UA106217C2 (en) 2014-08-11
JP5615836B2 (ja) 2014-10-29
IL212799A0 (en) 2011-07-31
US20110269975A1 (en) 2011-11-03
KR20110094318A (ko) 2011-08-23
SA109300715B1 (ar) 2014-06-25
WO2010065447A3 (en) 2010-07-22
US20140107163A1 (en) 2014-04-17
MX2011005712A (es) 2011-06-17
EP2358670B1 (en) 2012-10-24
EP2896619A1 (en) 2015-07-22
WO2010065449A1 (en) 2010-06-10
RU2507197C2 (ru) 2014-02-20
BRPI0922152A2 (pt) 2015-08-18
PE20100467A1 (es) 2010-08-03
CN102232072A (zh) 2011-11-02
UY32278A (es) 2011-06-30
JP5698673B2 (ja) 2015-04-08
CN102227406A (zh) 2011-10-26
ECSP11011135A (es) 2011-07-29
CN102232072B (zh) 2014-09-24
AU2009322630A1 (en) 2010-06-10
EA201170736A1 (ru) 2011-12-30
CO6382158A2 (es) 2012-02-15
IL212796A0 (en) 2011-07-31
MY159040A (en) 2016-12-15
US8153821B2 (en) 2012-04-10
KR20110094100A (ko) 2011-08-19
ES2403022T3 (es) 2013-05-13
EA021054B1 (ru) 2015-03-31
ZA201103497B (en) 2012-01-25
RU2011127004A (ru) 2013-01-10
CA2744191A1 (en) 2010-06-10
WO2010065447A2 (en) 2010-06-10
JP2012510473A (ja) 2012-05-10
SG171876A1 (en) 2011-07-28
SG171432A1 (en) 2011-07-28
NZ593058A (en) 2013-06-28
HK1157778A1 (en) 2012-07-06
CL2009002146A1 (es) 2010-04-30
EP2358705A1 (en) 2011-08-24
US20120015983A1 (en) 2012-01-19
AU2009322628A1 (en) 2010-06-10
CA2744197A1 (en) 2010-06-10
JP2012510472A (ja) 2012-05-10
MX2011005713A (es) 2011-06-17
US8633227B2 (en) 2014-01-21
BRPI0922630A2 (pt) 2016-01-05
EP2358670A2 (en) 2011-08-24
TW201024283A (en) 2010-07-01

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