CO6190616A2 - Carboxamidas n-fenil-bipirrolidina sustituidas y su uso terapeutico - Google Patents

Carboxamidas n-fenil-bipirrolidina sustituidas y su uso terapeutico

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Publication number
CO6190616A2
CO6190616A2 CO10044768A CO10044768A CO6190616A2 CO 6190616 A2 CO6190616 A2 CO 6190616A2 CO 10044768 A CO10044768 A CO 10044768A CO 10044768 A CO10044768 A CO 10044768A CO 6190616 A2 CO6190616 A2 CO 6190616A2
Authority
CO
Colombia
Prior art keywords
phenyl
substituted
bipirrolidine
carboxamids
therapeutic use
Prior art date
Application number
CO10044768A
Other languages
English (en)
Inventor
Werngard Czechtizky
Zhongli Gao
William J Hurst
Lothar Schwink
Siegfried Stengelin
Original Assignee
Sanofi Aventis
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 Sanofi Aventis filed Critical Sanofi Aventis
Publication of CO6190616A2 publication Critical patent/CO6190616A2/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic 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
    • C07D207/04Heterocyclic 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
    • C07D207/06Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • 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
    • 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
    • A61P25/08Antiepileptics; 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
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/20Hypnotics; Sedatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/12Heterocyclic 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 chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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 two hetero rings
    • C07D405/12Heterocyclic 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 two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • Neurology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Medicinal Chemistry (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Pain & Pain Management (AREA)
  • Pulmonology (AREA)
  • Psychology (AREA)
  • Psychiatry (AREA)
  • Anesthesiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

La presente invención describe y reivindica una serie de carboxarnidas N-fenil-bipirrolidina sustituida de fórmula (I).En la que R, R1, R2, R3 y R4 son como se describieron en la presente. Más específicamente, los compuestos de esta invención son moduladores de los receptores H3 y, por lo tanto, son útiles como agentes farmacéuticos, especialmente en el tratamiento y/o la prevención de una variedad de enfermedades moduladas por los receptores H3, incluyendo enfermedades asociadas con el sistema nervioso central. Además, la presente invención también describe métodos para la preparación de carboxamidas N-fenil-bipirrolidina sustituidas e intermedios para ello. 1.- Un compuesto de fórmula (I):en la que R, R1, R2 y R3 son iguales o diferentes e independientemente uno del otro se seleccionan entre hidrógeno, alquilo (C1-C4) o CF3;R4 se selecciona del grupo que consiste en dimetilaminometilo, metanosulfonilmetilo, fenoximetilo, vinilbenceno, etinilbenceno, vinilpiridina, fenilo, benzofuranilo, dihidro-benzofuranilo, oxo-tetrahidro-benzofuranilo, benzodioxolilo, oxo-cromenilo, dihidrobenzo-dioxinilo, dioxo tetrahidro-1H-benzo[e]diazepinilo, imidazopiridinilo, benzotriazolilo, benzoimidazolilo, oxo-dihidro-benzoimidazolilo, indolilo, indazolilo, naftiridinilo, quinolinilo, benzoimidazotiazolilo, piridinilo, pirimidinilo, pirrolilo, triazolilo, tienilo, tiazolilo, tetrahidrofuranilo o pirrolidinilo; donde dicho R4 está opcionalmente sustituido una o más veces con un sustituyente seleccionado entre halógeno, hidroxi, metilo, etilo, isopropilo, propoxietilo, fenilo, benzoilo, metoxi, difluorometoxi, CF3, CN, acetilo, metanosulfonilo, sulfamoilo, dimetilamino, N-formil-metilamino, 2-hidroxietilamino, 2-metoxietilamido, benciloximetilo, carboxifenoxi, pirazolilo, 3,5-dimetil-pirazolilo, imidazolilo, triazolilo, oxazolilo, piridinilo, oxo-dihidro-piridinilo, pirimidinil-metilamino, N-acetil-piperidinilo, morfolinilo, morfolinilmetilo o 2-oxo-pirrolidinilo; o su sal o su enantiómero o diastereómero.
CO10044768A 2007-10-17 2010-04-16 Carboxamidas n-fenil-bipirrolidina sustituidas y su uso terapeutico CO6190616A2 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US98060107P 2007-10-17 2007-10-17

Publications (1)

Publication Number Publication Date
CO6190616A2 true CO6190616A2 (es) 2010-08-19

Family

ID=40243633

Family Applications (1)

Application Number Title Priority Date Filing Date
CO10044768A CO6190616A2 (es) 2007-10-17 2010-04-16 Carboxamidas n-fenil-bipirrolidina sustituidas y su uso terapeutico

Country Status (26)

Country Link
US (1) US8618159B2 (es)
EP (1) EP2212282B1 (es)
JP (1) JP5255644B2 (es)
KR (1) KR20100092441A (es)
CN (1) CN101903339B (es)
AT (1) ATE525350T1 (es)
AU (1) AU2008312638B2 (es)
BR (1) BRPI0818626A2 (es)
CA (1) CA2702482C (es)
CO (1) CO6190616A2 (es)
CY (1) CY1112683T1 (es)
DK (1) DK2212282T3 (es)
ES (1) ES2374116T3 (es)
HK (1) HK1146054A1 (es)
HR (1) HRP20110953T1 (es)
IL (1) IL205003A0 (es)
MA (1) MA31855B1 (es)
MX (1) MX2010004094A (es)
MY (1) MY149650A (es)
NZ (1) NZ584688A (es)
PL (1) PL2212282T3 (es)
PT (1) PT2212282E (es)
RU (1) RU2477719C2 (es)
SI (1) SI2212282T1 (es)
WO (1) WO2009052065A1 (es)
ZA (1) ZA201001946B (es)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX2010003949A (es) 2007-10-17 2010-04-30 Sanofi Aventis N-fenil-bipirrolidina carboxamidas sustituidas y uso terapeutico de las mismas.
PT2205558E (pt) 2007-10-17 2012-11-02 Sanofi Sa Amidas de n-fenil-pirrolidinilmetilpirrolidina substituídas e sua utilização terapêutica como moduladores do receptor h3 da histamina
EP2215058B1 (en) 2007-10-17 2011-11-23 Sanofi Substituted n-phenyl-bipyrrolidine ureas and therapeutic use thereof
AR074466A1 (es) 2008-12-05 2011-01-19 Sanofi Aventis Piperidina espiro pirrolidinona y piperidinona sustituidas y su uso terapeutico en enfermedades mediadas por la modulacion de los receptores h3.
AR074467A1 (es) 2008-12-05 2011-01-19 Sanofi Aventis Tetrahidropiran espiro pirrolidinonas y piperidinonas sustituidas, composiciones farmaceuticas que las contienen y uso de las mismas en el tratamiento y/o prevencion de enfermedades del snc ,tales como alzheimer y parkinson, entre otras.
WO2011143148A1 (en) 2010-05-11 2011-11-17 Sanofi Substituted n-heteroaryl spirolactam bipyrrolidines, preparation and therapeutic use thereof
TW201206444A (en) 2010-05-11 2012-02-16 Sanofi Aventis Substituted N-heteroaryl tetrahydro-isoquinoline derivatives, preparation and therapeutic use thereof
EP2569296A1 (en) * 2010-05-11 2013-03-20 Sanofi Substituted n-phenyl spirolactam bipyrrolidines, preparation and therapeutic use thereof
TW201206889A (en) * 2010-05-11 2012-02-16 Sanofi Aventis Substituted N-alkyl and N-acyl tetrahydro-isoquinoline derivatives, preparation and therapeutic use thereof
JP5968307B2 (ja) * 2010-05-11 2016-08-10 サノフイ 置換フェニルシクロアルキルピロリジン(ピペリジン)スピロラクタム類及びアミド類、それらの製造及び治療的使用
AR081383A1 (es) 2010-05-11 2012-08-29 Sanofi Aventis N-heteroaril bipirrolidin carboxamidas sustituidas, composiciones farmaceuticas que las contienen y uso de las mismas para el tratamiento de enfermedades del sistema nervioso central.
JP2013529198A (ja) * 2010-05-11 2013-07-18 サノフイ 置換されたn−ヘテロシクロアルキルビピロリジニルフェニルアミド誘導体、その製造及び治療上の使用
CN103717757A (zh) * 2011-05-24 2014-04-09 威斯特研究所 用于调节爱泼斯坦-巴尔核抗原1的活性的组合物和方法
US9828345B2 (en) 2013-02-28 2017-11-28 Bristol-Myers Squibb Company Phenylpyrazole derivatives as potent ROCK1 and ROCK2 inhibitors
TW201444798A (zh) 2013-02-28 2014-12-01 必治妥美雅史谷比公司 作爲強效rock1及rock2抑制劑之苯基吡唑衍生物

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AU2003287206A1 (en) * 2002-10-23 2004-05-13 Janssen Pharmaceutica, N.V. Phenylpiperidines and phenylpyrrolidines as histamine h3 receptor modulators
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PT2205558E (pt) * 2007-10-17 2012-11-02 Sanofi Sa Amidas de n-fenil-pirrolidinilmetilpirrolidina substituídas e sua utilização terapêutica como moduladores do receptor h3 da histamina
EP2215058B1 (en) * 2007-10-17 2011-11-23 Sanofi Substituted n-phenyl-bipyrrolidine ureas and therapeutic use thereof
MX2010003949A (es) 2007-10-17 2010-04-30 Sanofi Aventis N-fenil-bipirrolidina carboxamidas sustituidas y uso terapeutico de las mismas.

Also Published As

Publication number Publication date
PL2212282T3 (pl) 2012-02-29
CA2702482C (en) 2012-11-27
ZA201001946B (en) 2010-10-27
MA31855B1 (fr) 2010-11-01
HRP20110953T1 (hr) 2012-01-31
US20100173897A1 (en) 2010-07-08
KR20100092441A (ko) 2010-08-20
EP2212282A1 (en) 2010-08-04
AU2008312638B2 (en) 2013-05-16
AU2008312638A1 (en) 2009-04-23
PT2212282E (pt) 2012-01-09
DK2212282T3 (da) 2012-01-23
MX2010004094A (es) 2010-04-30
RU2010119560A (ru) 2011-11-27
NZ584688A (en) 2011-12-22
CA2702482A1 (en) 2009-04-23
CY1112683T1 (el) 2016-02-10
CN101903339A (zh) 2010-12-01
EP2212282B1 (en) 2011-09-21
WO2009052065A1 (en) 2009-04-23
ATE525350T1 (de) 2011-10-15
US8618159B2 (en) 2013-12-31
JP5255644B2 (ja) 2013-08-07
CN101903339B (zh) 2012-06-27
ES2374116T3 (es) 2012-02-13
HK1146054A1 (en) 2011-05-13
RU2477719C2 (ru) 2013-03-20
IL205003A0 (en) 2010-11-30
BRPI0818626A2 (pt) 2015-09-29
MY149650A (en) 2013-09-30
SI2212282T1 (sl) 2012-01-31
JP2011500696A (ja) 2011-01-06

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