ES2546833T3 - Derivados de pirrolidina como antagonistas de receptores de NK-3 - Google Patents

Derivados de pirrolidina como antagonistas de receptores de NK-3 Download PDF

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Publication number
ES2546833T3
ES2546833T3 ES10790561.4T ES10790561T ES2546833T3 ES 2546833 T3 ES2546833 T3 ES 2546833T3 ES 10790561 T ES10790561 T ES 10790561T ES 2546833 T3 ES2546833 T3 ES 2546833T3
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Spain
Prior art keywords
alkyl
halogen
cycloalkyl
substituted
cyano
Prior art date
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Active
Application number
ES10790561.4T
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English (en)
Inventor
Henner Knust
Andreas Koblet
Matthias Nettekoven
Hasane Ratni
Claus Riemer
Walter Vifian
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F Hoffmann La Roche AG
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F Hoffmann La Roche AG
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Publication of ES2546833T3 publication Critical patent/ES2546833T3/es
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    • 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

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

Abstract

Compuesto de fórmula (I):**Fórmula** en la que: R1 es hidrógeno, halógeno, ciano, alquilo C2-4 o alquilo C1-5 sustituido con halógeno; n es 1, 2 ó 3; en el caso de que n sea 2 ó 3, R1 puede ser diferente, R2 es alquilo C2-7 o cicloalquilo C3-6, R3 es el grupo: **Fórmula** en el que: X es CH o N, R5 es hidrógeno, -C(O)-alquilo C2-4, -C(O)O-alquilo C2-4, S(O)2-alquilo C2-4, -C(O)CH2O-alquilo C2-4,-C(O)- CH2-CN, o es -C(O)-cicloalquilo, cicloalquilo o -CH2-cicloalquilo, en el que los grupos cicloalquilo se sustituyen opcionalmente con alquilo C2-4, -CH2-O-alquilo C2-4, alcoxi C2-4, CF3, halógeno o ciano, o es -C(O)-heterocicloalquilo o heterocicloalquilo, o es -C(O)-heteroarilo o es heteroarilo o es -C(O)-arilo o arilo, en los que los grupos heterocicloalquilo, heteroarilo o arilo se sustituyen opcionalmente con halógeno, alquilo C2-4, >=O, alcoxi C2-4, alquilo C1-5 sustituido con halógeno, alquilo C2-4 sustituido con hidroxi, -C(O)-CH2-N(di-alquilo C2-4), C(O)NH-alquilo C2-4, C(O)NH2, -O-C(O)-alquilo C2-4, C(O)-alquilo C2- 4, S(O)2-alquilo C2-4 o ciano, R4 es arilo, que se sustituye opcionalmente con halógeno, hidroxi, alquilo C2-4, alquilo C1-5 sustituido con halógeno, S(O)2-alquilo C2-4, ciano o con alcoxi C2-4, o una sal farmacéuticamente activa de los mismos
ES10790561.4T 2009-12-18 2010-12-14 Derivados de pirrolidina como antagonistas de receptores de NK-3 Active ES2546833T3 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP09179797 2009-12-18
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
ES2546833T3 true ES2546833T3 (es) 2015-09-29

Family

ID=43480770

Family Applications (1)

Application Number Title Priority Date Filing Date
ES10790561.4T Active ES2546833T3 (es) 2009-12-18 2010-12-14 Derivados de pirrolidina como antagonistas de receptores de 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
CA2835835C (en) 2011-05-13 2019-04-02 Array Biopharma Inc. Pyrrolidinyl urea and pyrrolidinyl thiourea compounds as trka kinase inhibitors
ES2802251T3 (es) * 2012-01-06 2021-01-18 Novartis Ag Compuestos heterocíclicos y métodos para su uso

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
EP1578744B1 (en) * 2002-12-23 2008-07-09 Janssen Pharmaceutica N.V. Substituted 4-(4-piperidin-4-yl-piperazin-1-yl)-azepane derivatives and their use as neurokinin antagonists
JP2007521276A (ja) * 2003-06-25 2007-08-02 スミスクライン・ビーチャム・コーポレイション Ｎｋ−２およびｎｋ−３として用いるための４−カルボキサミドキノリン誘導体
US7550487B2 (en) * 2004-03-26 2009-06-23 Hoffmann-La Roche Inc. Pyrrolidine-3,4-dicarboxamide derivatives
AU2008240804B2 (en) 2007-04-20 2013-02-21 F. Hoffmann-La Roche Ag Pyrrolidine derivatives as dual NK1/NK3 receptor antagonists
ATE519738T1 (de) * 2007-08-22 2011-08-15 Hoffmann La Roche Pyrrolidinarylether als nk3-rezeptorantagonisten
US8063075B2 (en) * 2008-06-10 2011-11-22 Hoffmann-La Roche Inc. Pyrrolidine ether derivatives as NK3 receptor antagonists
KR20110010781A (ko) * 2008-06-16 2011-02-07 에프. 호프만-라 로슈 아게 Ｎｋ2 수용체 길항제로서의 피롤리딘 유도체
US8592454B2 (en) * 2008-09-19 2013-11-26 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
CA2781495A1 (en) 2011-06-23
KR101490004B1 (ko) 2015-02-04
MX2012006293A (es) 2012-07-03
US9346786B2 (en) 2016-05-24
JP5551267B2 (ja) 2014-07-16
BR112012014576A2 (pt) 2016-03-01
US20130203728A1 (en) 2013-08-08
CN102656157B (zh) 2015-04-29
CN102656157A (zh) 2012-09-05
KR20120096086A (ko) 2012-08-29
JP2013514304A (ja) 2013-04-25
HK1169992A1 (en) 2013-02-15
RU2561271C2 (ru) 2015-08-27
EP2513084B1 (en) 2015-07-22
WO2011073160A1 (en) 2011-06-23
EP2513084A1 (en) 2012-10-24
RU2012129361A (ru) 2014-01-27
US20110152233A1 (en) 2011-06-23

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