AR072118A1 - Derivados de pirrolidina como antagonistas de receptor de nk2 - Google Patents

Derivados de pirrolidina como antagonistas de receptor de nk2

Info

Publication number
AR072118A1
AR072118A1 ARP090102130A ARP090102130A AR072118A1 AR 072118 A1 AR072118 A1 AR 072118A1 AR P090102130 A ARP090102130 A AR P090102130A AR P090102130 A ARP090102130 A AR P090102130A AR 072118 A1 AR072118 A1 AR 072118A1
Authority
AR
Argentina
Prior art keywords
lower alkyl
alkyl
halogen
hydrogen
substituted
Prior art date
Application number
ARP090102130A
Other languages
English (en)
Inventor
Caterina Bissantz
Philippe Jablonski
Anja Limberg
Claus Riemer
Matthias Nettekoven
Henner Knust
Hasane Ratni
Andreas Koblet
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 AR072118A1 publication Critical patent/AR072118A1/es

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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
    • C07D207/10—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
    • 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
    • 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
    • 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
    • C07D401/12—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 chain containing hetero atoms as chain links
    • 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
    • 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
    • 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
    • C07D403/12—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 chain containing hetero atoms as chain links
    • 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
    • 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
    • C07D405/12—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 chain containing hetero atoms as chain links
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings

Landscapes

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

Abstract

Proceso medicamento y uso para preparar medicamentos para tratar depresion, ansiedad y esquizofrenia. Reivindicacion 1: Un compuesto de la formula (1) en la que R1 es hidrogeno, halogeno, ciano o alquilo inferior; n es el numero 1, 2 o 3; R2 es hidrogeno o alquilo inferior; R3 es un anillo arilo o heteroarilo, dichos anillos est n opcionalmente sustituidos por uno o dos sustituyentes R'; R' se elige entre hidrogeno, halogeno, alquilo inferior, alcoxi inferior, alquilo inferior sustituido por halogeno, alcoxi inferior sustituido por halogeno, -S(O)-alquilo inferior, CN, -NR4R5, -C(O)-alquilo inferior, heterociclilo o heteroarilo; R4/R5 con independencia entre s¡ son hidrogeno, -(CO)CF3, o alquilo inferior o es Un grupo heteroc¡clico no arom tico de formula (2) en el que X es N o CH; Y es -CH(R7)-; -N(R7')-, u O o puede ser SO2; R6 es hidrogeno, alquilo inferior o hidroxi; R7 es hidrogeno, hidroxi, =O, alquilo interior, alcoxi inferior, -S(O)2-alquilo inferior, -C(O)-alquilo inferior, -C(O)CH 2O-alquilo inferior, -CH2CN, -C(O)CH2CN, -C(O)-cicloalquilo, dicho grupo cicloalquilo est  opcionalmente sustituido por ciano, alquilo inferior, uno o dos  tomos de halogeno, =O o por amino, o es -C(O)O-alquilo inferior, -NH-alquilo inferior, -NRC(O)O-alquilo inferior, -NRC(O)-alquilo inferior o -CH2O-alquilo inferior; y R7' es hidrogeno, alquilo inferior, -(CH2)q-S(O)2-alquilo inferior, -(CH2)q-S(O)2-cicloalquilo, -C(O)-alquilo inferior, -(CH2)q-cicloalquilo, -C(O)CH2-O-alquilo inferior, -(CH2)qCN, -C(O)CN, -O(O)CH2CN, alquilo inferior sustituido por halogeno, alquenilo inferior sustituido por halogeno, -C(O)-cicloalquilo, dicho grupo cicloalquilo est  opcionalmente sustituido por ciano, alquilo inferior, uno o dos  tomos de halogeno, =O o por amino, o es -C(O)O-alquilo inferior o -(CH2)qO-alquilo inferior y q es un numero 0-3; o R6 y R7 junto con los  tomos de carbono a los que est n unidos pueden formar un anillo no arom tico de cinco o seis eslabones o R6 y R7' junto con el nitrogeno y los  tomos de carbono a los que est n unidos pueden formar un anillo no arom tico de cinco o seis eslabones; p es el numero 0, 1 o 2; Ar es arilo o heteroariio, dichos anillos est n opcionalmente sustituidos por uno o dos sustituyentes R''; R'' se elige entre hidrogeno, halogeno, alquilo inferior, alquilo inferior sustituido por halogeno, alcoxi inferior, alcoxi inferior sustituido por halogeno, -OCH2-cicloalquilo, -NR4R5, -CN, -CH(CH3)CN, -CH2O-alquilo inferior o pirrolilo; m es el numero 0, 1 o 2 y o es el numero 0; o es el numero 0, 1 o 2 y m es el numero 1, o sus sales farmaceuticamente activas, mezclas racemicas, enantiomeros, isomeros opticos o formas tautomeras.
ARP090102130A 2008-06-16 2009-06-12 Derivados de pirrolidina como antagonistas de receptor de nk2 AR072118A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP08158326 2008-06-16

Publications (1)

Publication Number Publication Date
AR072118A1 true AR072118A1 (es) 2010-08-04

Family

ID=40843342

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP090102130A AR072118A1 (es) 2008-06-16 2009-06-12 Derivados de pirrolidina como antagonistas de receptor de nk2

Country Status (13)

Country Link
US (2) US20090312327A1 (es)
EP (1) EP2297098A1 (es)
JP (1) JP2011524397A (es)
KR (1) KR20110010781A (es)
CN (1) CN102066321A (es)
AR (1) AR072118A1 (es)
AU (1) AU2009259493A1 (es)
BR (1) BRPI0914779A2 (es)
CA (1) CA2728054A1 (es)
IL (1) IL209266A0 (es)
MX (1) MX2010013311A (es)
TW (1) TW201002684A (es)
WO (1) WO2009153179A1 (es)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8592454B2 (en) 2008-09-19 2013-11-26 Takeda Pharmaceutical Company Limited Nitrogen-containing heterocyclic compound and use of same
EP2331500A1 (en) * 2008-10-09 2011-06-15 F. Hoffmann-La Roche AG Pyrrolidine n-benzyl derivatives
US20110144081A1 (en) * 2009-12-15 2011-06-16 Henner Knust Pyrrolidine derivatives
US20110152233A1 (en) * 2009-12-18 2011-06-23 Henner Knust Pyrrolidine compounds
BR112013029201B1 (pt) 2011-05-13 2022-08-09 Array Biopharma Inc Compostos de pirrolidinil ureia e pirrolidinil tioureia, seu processo de preparação, seu uso e composições farmacêuticas
JP6633618B2 (ja) 2014-08-21 2020-01-22 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ｒｏｃｋ阻害剤としてのタイドバックのベンズアミド誘導体
WO2020107189A1 (en) * 2018-11-27 2020-06-04 Legion Pharma Co. Ltd Pyrrolidine compounds for the treatment of malaria

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3446713A1 (de) 1984-12-21 1986-06-26 Boehringer Mannheim Gmbh, 6800 Mannheim N-substituierte aziridin-2-carbonsaeurederivate, verfahren zu deren herstellung sowie diese substanzen enthaltende arzneimittel
AUPQ570100A0 (en) 2000-02-17 2000-03-09 Fujisawa Pharmaceutical Co., Ltd. Beta-alanine derivatives and their use as receptor antagonists
US7514441B2 (en) * 2002-08-26 2009-04-07 Takeda Pharmaceutical Company Limited Substituted pyrazolo [1,5-A]pyrimidines as calcium receptor modulating agents
EP1670476A4 (en) * 2003-09-30 2009-05-27 Merck & Co Inc ANTAGONISTS OF TACHYKININ RECEPTOR BASED ON PHENYL PYRROLIDINE ETHER
WO2005068427A1 (ja) * 2004-01-14 2005-07-28 Takeda Pharmaceutical Company Limited カルボキサミド誘導体およびその用途
JP2008520711A (ja) * 2004-11-22 2008-06-19 メルク エンド カムパニー インコーポレーテッド シクロアルキルケトピペリジンタキキニン受容体拮抗剤
WO2007002457A2 (en) * 2005-06-27 2007-01-04 Merck & Co., Inc. Hydroisoindoline tachykinin receptor antagonists
AU2007284927A1 (en) * 2006-08-09 2008-02-21 Banyu Pharmaceutical Co., Ltd. Process for making lactam tachykinin receptor antagonists
EP1975165A1 (de) * 2007-03-27 2008-10-01 Boehringer Ingelheim Pharma GmbH & Co. KG Substituierte Pyrrolidinamide, deren Herstellung und deren Verwendung als Arzneimittel
CL2008003595A1 (es) * 2007-12-03 2009-11-20 Takeda Pharmaceuticals Co Compuestos heterociclicos nitrogenados, antagonistas del receptor de taquiquinina; agente farmaceutico que comprende el compuesto; y uso en la profilaxis o el tratamiento de una enfermedad del tracto urinario inferior, una enfermedad gastrointestinal o una enfermedad del sistema nervioso central.

Also Published As

Publication number Publication date
TW201002684A (en) 2010-01-16
EP2297098A1 (en) 2011-03-23
IL209266A0 (en) 2011-01-31
US20120208803A1 (en) 2012-08-16
JP2011524397A (ja) 2011-09-01
AU2009259493A1 (en) 2009-12-23
US8404679B2 (en) 2013-03-26
CA2728054A1 (en) 2009-12-23
KR20110010781A (ko) 2011-02-07
MX2010013311A (es) 2010-12-21
BRPI0914779A2 (pt) 2015-10-20
US20090312327A1 (en) 2009-12-17
CN102066321A (zh) 2011-05-18
WO2009153179A1 (en) 2009-12-23

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