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MX2012006293A - Derivados de pirrolidina como antagonista del receptor nk-3. - Google Patents

Derivados de pirrolidina como antagonista del receptor nk-3.

Info

Publication number
MX2012006293A
MX2012006293A MX2012006293A MX2012006293A MX2012006293A MX 2012006293 A MX2012006293 A MX 2012006293A MX 2012006293 A MX2012006293 A MX 2012006293A MX 2012006293 A MX2012006293 A MX 2012006293A MX 2012006293 A MX2012006293 A MX 2012006293A
Authority
MX
Mexico
Prior art keywords
lower alkyl
halogen
cycloalkyl
cyano
substituted
Prior art date
Application number
MX2012006293A
Other languages
English (en)
Inventor
Claus Riemer
Andreas Koblet
Hasane Ratni
Matthias Nettekoven
Walter Vifian
Hanner Knust
Original Assignee
Hoffmann La Roche
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 Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of MX2012006293A publication Critical patent/MX2012006293A/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/14—Heterocyclic 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
    • 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
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A61P25/22—Anxiolytics
    • 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]
    • 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
    • C07D207/10—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 hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D207/14—Nitrogen atoms not forming part of a nitro radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/06—Heterocyclic 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 carbon chain containing only aliphatic carbon atoms
    • 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

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

Abstract

La presente solicitud se refiere a compuestos de la fórmula (I) en donde R1 es hidrógeno, halógeno, ciano, alquilo inferior o alquilo inferior sustituido por halógeno; R2 es alquilo-C2-7 o cicloalquilo-C3-6 R3 es el grupo (II) en donde X es CH o N; R5 es hidrógeno, -C(Q)alquilo inferior, -C(0)0-alquilo inferior, S(0)2-alquilo inferior, -C(0)CH2O-alquilo inferior, -C(0)-CH2-CN, o es - C(0)-cicloalquilo, cicloalquilo, o -CH2-cicloalquilo, en donde los grupos cicloalquilo son opcionalmente sustituidos por un alquilo inferior, -CH2-0-alquilo inferior, alcoxilo inferior, CF3 halógeno o ciano, o es - C(0)-heterocicloalquilo, o es -C(0)-heteroarilo o es heteroarilo o es -C(0)-arilo o arilo, en donde los grupos heterocicloalquilo, heteroarilo o arilo son opcionalmente sustituidos por halógeno, alquilo inferior, =0, alcoxilo inferior, alquilo inferior sustituido por halógeno, alquilo inferior sustituido por hidroxi, -C(O)-CH2-N(di- alquilo inferior), C(0)NH-alquilo inferior, C(0)NH2, -0- C(0)-alquilo inferior, C(0)-alquilo inferior, S(0)2-alquilo inferior o ciano; R4 es arilo, que es opcionalmente sustituido por halógeno, hidroxi, alquilo inferior, alquilo inferior sustituido por halógeno, S(0)2-alquilo inferior, ciano o por un alcoxi inferior; o a una sal farmacéuticamente activa de los mismos. Se ha encontrado que los compuestos presentes son altamente potenciales antagonistas del receptor NK-3 para el tratamiento de depresión, dolor, psicosis, enfermedad de Parkinson, esquizofrenia, ansiedad y trastorno de hiperactividad por déficit de atención (ADHD).
MX2012006293A 2009-12-18 2010-12-14 Derivados de pirrolidina como antagonista del receptor nk-3. MX2012006293A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP09179797 2009-12-18
PCT/EP2010/069564 WO2011073160A1 (en) 2009-12-18 2010-12-14 Pyrrolidine derivatives as nk - 3 receptor antagonists

Publications (1)

Publication Number Publication Date
MX2012006293A true MX2012006293A (es) 2012-07-03

Family

ID=43480770

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2012006293A MX2012006293A (es) 2009-12-18 2010-12-14 Derivados de pirrolidina como antagonista del receptor nk-3.

Country Status (11)

Country Link
US (2) US20110152233A1 (es)
EP (1) EP2513084B1 (es)
JP (1) JP5551267B2 (es)
KR (1) KR101490004B1 (es)
CN (1) CN102656157B (es)
BR (1) BR112012014576A2 (es)
CA (1) CA2781495A1 (es)
ES (1) ES2546833T3 (es)
MX (1) MX2012006293A (es)
RU (1) RU2561271C2 (es)
WO (1) WO2011073160A1 (es)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8022099B2 (en) * 2008-11-03 2011-09-20 Hoffmann-La Roche Inc. N-benzyl pyrrolidine derivatives
US20110144081A1 (en) * 2009-12-15 2011-06-16 Henner Knust Pyrrolidine derivatives
US8618303B2 (en) * 2011-01-07 2013-12-31 Hoffmann-La Roche Inc. Pyrrolidine derivatives
RS55582B1 (sr) * 2011-05-13 2017-06-30 Array Biopharma Inc Jedinjenja pirolidinil uree, pirolidinil tiouree i pirolidinil guanidina kao inhibitori trka kinaze
AU2013202982C1 (en) * 2012-01-06 2017-01-05 Novartis Ag Heterocyclic compounds and methods for their use

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2824828B1 (fr) * 2001-05-21 2005-05-20 Sanofi Synthelabo Nouveaux derives de piperidinecarboxamide, un procede pour leur preparation et les compositions pharmaceutiques les contenant
AU2003298369B2 (en) * 2002-12-23 2009-08-27 Janssen Pharmaceutica N.V. Substituted 4-(4-piperidin-4-yl-piperazin-1-yl)-azepane derivatives and their use as neurokinin antagonists
EP1635834A4 (en) 2003-06-25 2009-12-02 Smithkline Beecham Corp NEW CONNECTIONS
US7550487B2 (en) * 2004-03-26 2009-06-23 Hoffmann-La Roche Inc. Pyrrolidine-3,4-dicarboxamide derivatives
CA2682506C (en) 2007-04-20 2016-05-24 F. Hoffmann-La Roche Ag Pyrrolidine derivatives as dual nk1/nk3 receptor antagonists
CA2697325A1 (en) * 2007-08-22 2009-02-26 F. Hoffmann-La Roche Ag Pyrrolidine aryl-ether as nk3 receptor antagonists
US8063075B2 (en) * 2008-06-10 2011-11-22 Hoffmann-La Roche Inc. Pyrrolidine ether derivatives as NK3 receptor antagonists
CN102066321A (zh) * 2008-06-16 2011-05-18 弗·哈夫曼-拉罗切有限公司 作为nk2受体拮抗剂的吡咯烷衍生物
EP2336105B9 (en) * 2008-09-19 2014-09-17 Takeda Pharmaceutical Company Limited Nitrogen-containing heterocyclic compound and use of same
US8022099B2 (en) * 2008-11-03 2011-09-20 Hoffmann-La Roche Inc. N-benzyl pyrrolidine derivatives
US20110144081A1 (en) * 2009-12-15 2011-06-16 Henner Knust Pyrrolidine derivatives
US8618303B2 (en) * 2011-01-07 2013-12-31 Hoffmann-La Roche Inc. Pyrrolidine derivatives

Also Published As

Publication number Publication date
KR20120096086A (ko) 2012-08-29
CA2781495A1 (en) 2011-06-23
JP2013514304A (ja) 2013-04-25
KR101490004B1 (ko) 2015-02-04
BR112012014576A2 (pt) 2016-03-01
US20110152233A1 (en) 2011-06-23
CN102656157A (zh) 2012-09-05
JP5551267B2 (ja) 2014-07-16
RU2561271C2 (ru) 2015-08-27
RU2012129361A (ru) 2014-01-27
HK1169992A1 (en) 2013-02-15
ES2546833T3 (es) 2015-09-29
CN102656157B (zh) 2015-04-29
EP2513084A1 (en) 2012-10-24
US20130203728A1 (en) 2013-08-08
EP2513084B1 (en) 2015-07-22
WO2011073160A1 (en) 2011-06-23
US9346786B2 (en) 2016-05-24

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