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MX2009011051A - Derivados de pirrolidina como antagonistas del receptor nk1/nk3 doble. - Google Patents

Derivados de pirrolidina como antagonistas del receptor nk1/nk3 doble.

Info

Publication number
MX2009011051A
MX2009011051A MX2009011051A MX2009011051A MX2009011051A MX 2009011051 A MX2009011051 A MX 2009011051A MX 2009011051 A MX2009011051 A MX 2009011051A MX 2009011051 A MX2009011051 A MX 2009011051A MX 2009011051 A MX2009011051 A MX 2009011051A
Authority
MX
Mexico
Prior art keywords
lower alkyl
substituted
halogen
hydroxy
crr
Prior art date
Application number
MX2009011051A
Other languages
English (en)
Inventor
Torsten Hoffmann
Hasane Ratni
Henner Knust
Caterina Bissantz
Matthias Nettekoven
Xihan Wu
Philippe Jablonski
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 MX2009011051A publication Critical patent/MX2009011051A/es

Links

Classifications

    • 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
    • C07D207/08—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 hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
    • 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
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61P25/28—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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/06—Heterocyclic 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
    • 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
    • C07D405/02—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 two hetero rings
    • C07D405/06—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 two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/10—Spiro-condensed systems

Landscapes

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

Abstract

La invención se refiere a derivados de pirrolidina de la fórmula (I) en donde R1 es hidrógeno, halógeno o alquilo inferior; R2 es hidrógeno, halógeno, alcoxi inferior o alquilo inferior sustituido por halógeno; R3 es -(CH2)p-heterociclilo opcionalmente sustituido por a Ref. 09-188 halógeno, -S(O)2-alquilo inferior, -C(O)-alquilo inferior, -C(O)O-alquilo inferior, hidroxi, alquilo inferior sustituido por hidroxi, -(CH2)p-O-alquilo inferior, -NHCO-alquilo inferior, o es cicloalquilo de C3-6 opcionalmente sustituido por =O, -(CH2)p-O-alquilo inferior o alquinilo inferior, o arilo o heteroarilo sustituido o sin sustituir, en donde los sustituyentes se seleccionan del grupo que consiste de alquilo inferior, CN, -S(O)2-alquilo inferior, halógeno, -C(O)-alquilo inferior, hidroxi, alcoxi inferior o alcoxi inferior sustituido por halógeno; o es -(CH2)p-NR4R5 R4/R5 son independientemente entre sí hidrógeno, alquilo inferior, -(CRR')p-alquilo inferior sustituido por hidroxi, -(CRR')p-O-alquilo inferior, -(CRR')p-S-alquilo inferior, -(CRR')p-O- alquilo inferior sustituido por hidroxi o cicloalquilo de C3-6; R/R' son independientemente entre sí hidrógeno, alquilo inferior o alquilo inferior sustituido por hidroxilo; n es 1 ó 2; o es 1 ó 2; P es 0, 1, 2, 3 ó 4; o sus sales de adición de ácido farmacéuticamente aceptables.
MX2009011051A 2007-04-20 2008-04-09 Derivados de pirrolidina como antagonistas del receptor nk1/nk3 doble. MX2009011051A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP07106666 2007-04-20
PCT/EP2008/054261 WO2008128891A1 (en) 2007-04-20 2008-04-09 Pyrrolidine derivatives as dual nk1/nk3 receptor antagonists

Publications (1)

Publication Number Publication Date
MX2009011051A true MX2009011051A (es) 2009-10-30

Family

ID=39563424

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2009011051A MX2009011051A (es) 2007-04-20 2008-04-09 Derivados de pirrolidina como antagonistas del receptor nk1/nk3 doble.

Country Status (14)

Country Link
US (1) US7893062B2 (es)
EP (1) EP2148857B1 (es)
JP (1) JP5203449B2 (es)
KR (1) KR101163847B1 (es)
CN (1) CN101657418B (es)
AT (1) ATE475645T1 (es)
AU (1) AU2008240804B2 (es)
BR (1) BRPI0810402A2 (es)
CA (1) CA2682506C (es)
DE (1) DE602008001983D1 (es)
ES (1) ES2348002T3 (es)
IL (1) IL201317A0 (es)
MX (1) MX2009011051A (es)
WO (1) WO2008128891A1 (es)

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Publication number Priority date Publication date Assignee Title
EP2336105B9 (en) 2008-09-19 2014-09-17 Takeda Pharmaceutical Company Limited Nitrogen-containing heterocyclic compound and use of same
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
US8022099B2 (en) * 2008-11-03 2011-09-20 Hoffmann-La Roche Inc. N-benzyl pyrrolidine derivatives
US8318759B2 (en) * 2009-02-18 2012-11-27 Hoffmann-La Roche Inc. Pyrrolidine derivatives as NK3 receptor antagonists
US20110144081A1 (en) * 2009-12-15 2011-06-16 Henner Knust Pyrrolidine derivatives
US20110152233A1 (en) 2009-12-18 2011-06-23 Henner Knust Pyrrolidine compounds
US8507535B2 (en) 2010-07-07 2013-08-13 Hoffmann-La Roche Inc. Methyl-pyrrolidine ether 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
JP6609253B2 (ja) * 2014-08-06 2019-11-20 キッセイ薬品工業株式会社 シアノチオフェン誘導体
KR102704783B1 (ko) 2015-05-18 2024-09-10 칸디 테라퓨틱스 리미티드 성-호르몬 의존성 질환의 치료를 위한 이중 nk-1/nk-3 수용체 길항제
EA202092131A1 (ru) 2018-03-14 2020-11-27 Кэнди Терапьютикс Лимитед Новый фармацевтический препарат, содержащий двойные антагонисты рецептора nk-1/nk-3
WO2019186358A1 (en) * 2018-03-26 2019-10-03 Novartis Ag 3-hydroxy-n-(3-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)phenyl)pyrrolidine-1-carboxamide derivatives
WO2020107189A1 (en) * 2018-11-27 2020-06-04 Legion Pharma Co. Ltd Pyrrolidine compounds for the treatment of malaria
US12533358B1 (en) 2025-05-14 2026-01-27 Bayer Consumer Care Ag Methods of treatment with elinzanetant

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AU506399B2 (en) 1975-12-30 1980-01-03 Showa Denko Kabushiki Kaisha 3-(2-aryl-2-propyl) ureas
IL111960A (en) 1993-12-17 1999-12-22 Merck & Co Inc Morpholines and thiomorpholines their preparation and pharmaceutical compositions containing them
CN1067683C (zh) 1993-12-29 2001-06-27 默克·夏普-道姆公司 取代的吗啉衍生物及其作为治疗剂的用途
TW385308B (en) 1994-03-04 2000-03-21 Merck & Co Inc Prodrugs of morpholine tachykinin receptor antagonists
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EP1192952A3 (en) 2000-09-28 2003-03-26 Pfizer Products Inc. Combination, for treating depression and anxiety, containing an NK-3 receptor antagonist and a CNS penetrant NK-1 receptor antagonist
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US7138423B2 (en) * 2004-07-20 2006-11-21 Bristol-Myers Squibb Company Arylpyrrolidine derivatives as NK-1 /SSRI antagonists
US20060030600A1 (en) * 2004-08-06 2006-02-09 Patrick Schnider Dual NK1/NK3 receptor antagonists for the treatment of schizophrenia
JP2008509179A (ja) * 2004-08-09 2008-03-27 グラクソ グループ リミテッド グルタミン酸受容体を強化する化合物および医学におけるその使用
JP2007008913A (ja) * 2004-09-17 2007-01-18 Tanabe Seiyaku Co Ltd ピペリジン化合物およびその製法
KR100939347B1 (ko) 2005-07-20 2010-01-29 (주)카이로드 광학적으로 순수한 (ｓ)-3-히드록시 피롤리딘의 제조방법

Also Published As

Publication number Publication date
AU2008240804B2 (en) 2013-02-21
IL201317A0 (en) 2010-05-31
ATE475645T1 (de) 2010-08-15
CN101657418A (zh) 2010-02-24
AU2008240804A1 (en) 2008-10-30
KR101163847B1 (ko) 2012-07-09
EP2148857B1 (en) 2010-07-28
WO2008128891A1 (en) 2008-10-30
BRPI0810402A2 (pt) 2014-11-04
CA2682506C (en) 2016-05-24
KR20090130317A (ko) 2009-12-22
EP2148857A1 (en) 2010-02-03
JP5203449B2 (ja) 2013-06-05
US7893062B2 (en) 2011-02-22
DE602008001983D1 (de) 2010-09-09
CA2682506A1 (en) 2008-10-30
ES2348002T3 (es) 2010-11-26
US20080275021A1 (en) 2008-11-06
CN101657418B (zh) 2012-05-30
JP2010524880A (ja) 2010-07-22

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