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MX2011008178A - Derivados de pirrolidina como antagonistas del receptor de neuroquinina 3 (nk3). - Google Patents

Derivados de pirrolidina como antagonistas del receptor de neuroquinina 3 (nk3).

Info

Publication number
MX2011008178A
MX2011008178A MX2011008178A MX2011008178A MX2011008178A MX 2011008178 A MX2011008178 A MX 2011008178A MX 2011008178 A MX2011008178 A MX 2011008178A MX 2011008178 A MX2011008178 A MX 2011008178A MX 2011008178 A MX2011008178 A MX 2011008178A
Authority
MX
Mexico
Prior art keywords
lower alkyl
halogen
hydrogen
receptor antagonists
substituted
Prior art date
Application number
MX2011008178A
Other languages
English (en)
Inventor
Claus Riemer
Anja Limberg
Hasane Ratni
Henner Knust
Matthias Nettekoven
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 MX2011008178A publication Critical patent/MX2011008178A/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
    • C07D207/08Heterocyclic 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
    • 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
    • C07D403/06Heterocyclic 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 carbon chain containing only aliphatic carbon atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61P25/14Drugs 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
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • 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
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • 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
    • C07D207/08Heterocyclic 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
    • C07D207/09Radicals substituted by nitrogen atoms, not forming part of a nitro radical
    • 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
    • C07D401/06Heterocyclic 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
    • 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
    • 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
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings

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

Abstract

La presente invención se relaciona con compuestos de la fórmula I en donde A es - NR'-, -S, -S(O)- o - S(O)2-; R´ es hidrógeno o alquilo inferior; Ar es arilo o es un grupo heteroarilo de cinco o seis miembros, que contiene uno o dos átomos de N; R es un grupo heterocíclico de cinco o seis miembros, X1 es N o CH; y X2 es -N(R1)-, -CH2-, -O-, -S, -S(O)-, o -S(O)2-, R1 es hidrógeno, alquilo inferior, S(O)2-alquilo inferior, C(O)-alquilo inferior, C(O)-cicloalquilo opcionalmente substituido por alquilo inferior; con la condición de que por lo menos uno de X1 o X2 contenga un heteroátomo, o sea un grupo heteroarilo de cinco o seis miembros, que contiene uno o dos átomos de N, cuyos grupos están sin sustituir o pueden ser substituidos por uno o dos R1; en donde R1 es un alquilo inferior o ciano; R2 es un alquilo inferior substituido por halógeno, halógeno, ciano o nitro; R3 es halógeno; R4 es hidrógeno o alquilo inferior; o es 1 o 2; en caso de que o sea 2, R2 puede ser igual o diferente; p es 1 o 2; en caso de que p sea 2, R3 puede ser igual o diferente; o una sal farmacéuticamente activa del mismo. Se ha encontrado que los presentes compuestos son antagonistas del receptor NK-3 de alto potencial para el tratamiento de depresión, dolor, psicosis, enfermedad de Parkinson, esquizofrenia, trastornos bipolares, ansiedad y trastorno de déficit de atención con hiperactividad (ADHD).
MX2011008178A 2009-02-18 2010-02-16 Derivados de pirrolidina como antagonistas del receptor de neuroquinina 3 (nk3). MX2011008178A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP09153097 2009-02-18
PCT/EP2010/051887 WO2010094667A1 (en) 2009-02-18 2010-02-16 Pyrrolidine derivatives as nk3 receptor antagonists

Publications (1)

Publication Number Publication Date
MX2011008178A true MX2011008178A (es) 2011-08-17

Family

ID=42115644

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2011008178A MX2011008178A (es) 2009-02-18 2010-02-16 Derivados de pirrolidina como antagonistas del receptor de neuroquinina 3 (nk3).

Country Status (12)

Country Link
US (1) US8318759B2 (es)
EP (1) EP2398768B1 (es)
JP (1) JP5452622B2 (es)
KR (1) KR101304130B1 (es)
CN (1) CN102307853B (es)
AU (1) AU2010215513B2 (es)
BR (1) BRPI1016115A8 (es)
CA (1) CA2748701A1 (es)
IL (1) IL213763A (es)
MX (1) MX2011008178A (es)
SG (1) SG173638A1 (es)
WO (1) WO2010094667A1 (es)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102177136A (zh) * 2008-10-09 2011-09-07 弗·哈夫曼-拉罗切有限公司 吡咯烷n-苄基衍生物
US8618303B2 (en) * 2011-01-07 2013-12-31 Hoffmann-La Roche Inc. Pyrrolidine derivatives
WO2017072629A1 (en) 2015-10-29 2017-05-04 Cadila Healthcare Limited Pharmaceutical combination of nk3 receptor antagonist and biguanides
CN115335050B (zh) * 2020-01-29 2024-05-17 卡玛瑞制药有限公司 用于治疗皮肤病症的化合物和组合物

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2635838T3 (es) * 2002-08-26 2017-10-05 Takeda Pharmaceutical Company Limited Compuesto modulador de receptores de calcio y su uso
US7138423B2 (en) * 2004-07-20 2006-11-21 Bristol-Myers Squibb Company Arylpyrrolidine derivatives as NK-1 /SSRI antagonists
WO2006123725A1 (ja) * 2005-05-19 2006-11-23 Astellas Pharma Inc. ピロリジン誘導体またはその塩
EP2148857B1 (en) 2007-04-20 2010-07-28 F. Hoffmann-La Roche AG Pyrrolidine derivatives as dual nk1/nk3 receptors antagonists
CN101778837A (zh) * 2007-08-07 2010-07-14 弗·哈夫曼-拉罗切有限公司 作为nk3受体拮抗剂的吡咯烷芳基-醚
BRPI0815085A2 (pt) 2007-08-09 2014-09-30 Basf Se Misturas fungicidas, agente fungicida, processo para combater fungos nocivos fitopatogênicos, semente, e, uso de compostos.
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
US8022099B2 (en) * 2008-11-03 2011-09-20 Hoffmann-La Roche Inc. N-benzyl pyrrolidine derivatives

Also Published As

Publication number Publication date
JP5452622B2 (ja) 2014-03-26
US8318759B2 (en) 2012-11-27
WO2010094667A1 (en) 2010-08-26
AU2010215513B2 (en) 2014-06-12
CN102307853A (zh) 2012-01-04
AU2010215513A1 (en) 2011-08-11
JP2012517981A (ja) 2012-08-09
IL213763A0 (en) 2011-07-31
BRPI1016115A2 (pt) 2016-04-12
BRPI1016115A8 (pt) 2018-01-02
US20100210659A1 (en) 2010-08-19
KR101304130B1 (ko) 2013-09-05
CA2748701A1 (en) 2010-08-26
KR20110120957A (ko) 2011-11-04
SG173638A1 (en) 2011-09-29
CN102307853B (zh) 2015-09-02
EP2398768B1 (en) 2016-08-24
IL213763A (en) 2014-12-31
EP2398768A1 (en) 2011-12-28

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