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

Carboxamidas n-fenil-bipirrolidina sustituidas y su uso terapeutico

Info

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

Landscapes

  • 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)
  • Hospice & Palliative Care (AREA)
  • Anesthesiology (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 Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (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
PL2215058T3 (pl) 2007-10-17 2012-04-30 Sanofi Sa Podstawione N-fenylo-bipirolidynomoczniki oraz ich zastosowanie terapeutyczne
AU2008312635B2 (en) * 2007-10-17 2013-05-16 Sanofi Substituted N-phenyl-bipyrrolidine carboxamides and therapeutic use thereof
ES2392122T3 (es) * 2007-10-17 2012-12-04 Sanofi N-fenil-pirrolidinilmetilpirrolidin amidas sustituidas y uso terapéutico de las mismas
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.
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.
JP2013526529A (ja) * 2010-05-11 2013-06-24 サノフイ 置換されたn−ヘテロアリールビピロリジンカルボキサミド、その製造及び治療上の使用
WO2011143163A1 (en) * 2010-05-11 2011-11-17 Sanofi Substituted n-phenyl spirolactam bipyrrolidines, preparation and therapeutic use thereof
JP5766278B2 (ja) * 2010-05-11 2015-08-19 サノフイ 置換されたn−アルキルおよびn−アシルテトラヒドロ−イソキノリン誘導体、それらの製造および治療上の使用
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
AR081034A1 (es) * 2010-05-11 2012-05-30 Sanofi Aventis Derivados de n-heteroaril tetrahidro-isoquinolina sustituidos, composiciones farmaceuticas que los contienen y uso de los mismos para el tratamiento de enfermedades del sistema nervioso central
JP5833105B2 (ja) * 2010-05-11 2015-12-16 サノフイ 置換n−ヘテロアリールスピロラクタムビピロリジン類、その製造及び治療的使用
AR083718A1 (es) 2010-05-11 2013-03-20 Sanofi Aventis Fenil cicloalquil pirrolidina (piperidina) espirolactamas y amidas sustituidas, preparacion y uso terapeutico de las mismas
EP2714941A4 (en) * 2011-05-24 2014-12-03 Wistar Inst COMPOSITIONS AND METHODS FOR MODULATING THE EFFECT OF THE EPSTEIN-BARR NUCLEAR ANTIGEN 1
AR094929A1 (es) 2013-02-28 2015-09-09 Bristol Myers Squibb Co Derivados de fenilpirazol como inhibidores potentes de rock1 y rock2
JP6423372B2 (ja) 2013-02-28 2018-11-14 ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company 強力なrock1およびrock2阻害剤としてのフェニルピラゾール誘導体

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* Cited by examiner, † Cited by third party
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PE20020507A1 (es) * 2000-10-17 2002-06-25 Schering Corp Compuestos no-imidazoles como antagonistas del receptor histamina h3
JP2006505590A (ja) * 2002-10-23 2006-02-16 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ ヒスタミンh3受容体調節物質としてのフェニルピペリジンおよびフェニルピロリジン
DE10306250A1 (de) * 2003-02-14 2004-09-09 Aventis Pharma Deutschland Gmbh Substituierte N-Arylheterozyklen, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel
US7223788B2 (en) * 2003-02-14 2007-05-29 Sanofi-Aventis Deutschland Gmbh Substituted N-aryl heterocycles, process for their preparation and their use as medicaments
CA2600757C (en) 2005-03-17 2014-02-18 Eli Lilly And Company Pyrrolidine derivatives as histamine h3 receptor antagonists
CN101151244B (zh) * 2005-04-01 2014-09-03 伊莱利利公司 组胺h3受体活性剂、制备和治疗用途
ATE523488T1 (de) * 2005-07-01 2011-09-15 Lilly Co Eli Histamin-h3-rezeptor-mittel, deren herstellung und therapeutische verwendung
WO2007048595A1 (en) * 2005-10-27 2007-05-03 Ucb Pharma, S.A. Compounds comprising a lactam or a lactam derivative moiety, processes for making them, and their uses
ES2392122T3 (es) * 2007-10-17 2012-12-04 Sanofi N-fenil-pirrolidinilmetilpirrolidin amidas sustituidas y uso terapéutico de las mismas
AU2008312635B2 (en) * 2007-10-17 2013-05-16 Sanofi Substituted N-phenyl-bipyrrolidine carboxamides and therapeutic use thereof
PL2215058T3 (pl) * 2007-10-17 2012-04-30 Sanofi Sa Podstawione N-fenylo-bipirolidynomoczniki oraz ich zastosowanie terapeutyczne

Also Published As

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

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