AR039399A1 - Compuestos quimicos con actividad doble, procedimientos para su preparacion y composiciones farmaceuticas - Google Patents

Compuestos quimicos con actividad doble, procedimientos para su preparacion y composiciones farmaceuticas

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Publication number
AR039399A1
AR039399A1 ARP030101223A ARP030101223A AR039399A1 AR 039399 A1 AR039399 A1 AR 039399A1 AR P030101223 A ARP030101223 A AR P030101223A AR P030101223 A ARP030101223 A AR P030101223A AR 039399 A1 AR039399 A1 AR 039399A1
Authority
AR
Argentina
Prior art keywords
alkyl
cycloalkyl
halogen
hydrogen
formula
Prior art date
Application number
ARP030101223A
Other languages
English (en)
Original Assignee
Ucb Sa
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 Ucb Sa filed Critical Ucb Sa
Publication of AR039399A1 publication Critical patent/AR039399A1/es

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/42—One nitrogen atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/08—Bronchodilators
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48—Two nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/50—Three nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/60—Three or more oxygen or sulfur 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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D403/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Pulmonology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

El presente se refiere a compuestos químicos que combinan una afinidad y un antagonismo contra el receptor muscarínico m3 humano con una actividad como agentes inhibidores selectivos de la fosfodiesterasa IV (PDE IV), a procedimientos para prepararlos, a composiciones farmacéuticas que los contienen y a su uso como productos farmacéuticos. Reivindicación 1: Un compuesto que tiene la fórmula (1), o una de sus sales farmacéuticamente aceptables, en el que: Y es -NH-R2 o un grupo de fórmula (2); R1 es cicloalquilo o alquilo sin sustituir; R2 es cicloalquilo; R3 es halógeno, alquilo, halógeno, hidroxi, alcoxi o amino; o R2R3 es un grupo de puente de alquileno; Ra es hidrógeno, alquilo, alquenilo, alquinilo, halógeno, hidroxi, alcoxi, amino, alquilamino, alquilsulfoniloxi, ciano, carboxi, éster o amido; Rb es hidrógeno, alquil o halógeno; o RaRb es carbonilo; R4 es hidrógeno o alquilo; R5 es cicloalquilo, arilalquilo o heterociclil-alquilo; o NR4R5 es un heterociclilo, que puede estar sustituido, que contiene solamente un heteroátomo que es un átomo de nitrógeno, o que contiene dos heteroátomos de los que uno es un átomo de nitrógeno y el otro es un átomo de azufre no oxidado, con la condición de que cuando Y es -NHR2 y R2R3 es un grupo de puente de alquileno o cuando Y es un grupo de fórmula (2); R1 ha de ser un cicloalquilo.
ARP030101223A 2002-04-18 2003-04-08 Compuestos quimicos con actividad doble, procedimientos para su preparacion y composiciones farmaceuticas AR039399A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP02008706 2002-04-18

Publications (1)

Publication Number Publication Date
AR039399A1 true AR039399A1 (es) 2005-02-16

Family

ID=29225591

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP030101223A AR039399A1 (es) 2002-04-18 2003-04-08 Compuestos quimicos con actividad doble, procedimientos para su preparacion y composiciones farmaceuticas

Country Status (7)

Country Link
US (1) US7544675B2 (es)
EP (1) EP1499598A1 (es)
AR (1) AR039399A1 (es)
AU (1) AU2003222786A1 (es)
CO (1) CO5450245A1 (es)
TW (1) TW200306832A (es)
WO (1) WO2003087064A1 (es)

Families Citing this family (29)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20110010824A (ko) 2003-01-14 2011-02-07 아레나 파마슈티칼스, 인크. 대사 조절제로서의 １,２,３-삼치환된 아릴 및 헤테로아릴 유도체, 및 당뇨병 및 고혈당증을 비롯한 이에 관련된 장애의 예방 및 치료
AR045047A1 (es) * 2003-07-11 2005-10-12 Arena Pharm Inc Derivados arilo y heteroarilo trisustituidos como moduladores del metabolismo y de la profilaxis y tratamiento de desordenes relacionados con los mismos
AR051095A1 (es) 2004-09-20 2006-12-20 Xenon Pharmaceuticals Inc Derivados heterociclicos y su uso comoinhibidores de la estearoil-coa desaturasa
UY31636A1 (es) 2008-02-06 2009-08-03 Farmacoforos duales-antagonistas muscarinicos de pde4
PE20091552A1 (es) 2008-02-06 2009-10-25 Glaxo Group Ltd Farmacoforos duales - antagonistas muscarinicos de pde4
AR070564A1 (es) 2008-02-06 2010-04-21 Glaxo Group Ltd Derivados de 1h-pirazolo[3,4-b]piridin-5-ilo,inhibidores de fosfodiesterasas pde4 y antagonistas de receptores muscarinicos de acetilcolina(machr), utiles en el tratamiento y/o profilaxis de enfermedades respiratorias y alergicas,y composiciones farmaceuticas que los comprenden
WO2010043721A1 (en) 2008-10-17 2010-04-22 Oryzon Genomics, S.A. Oxidase inhibitors and their use
US8993808B2 (en) 2009-01-21 2015-03-31 Oryzon Genomics, S.A. Phenylcyclopropylamine derivatives and their medical use
MX338041B (es) 2009-09-25 2016-03-30 Oryzon Genomics Sa Inhibidores de demetilasa-1 especificos de lisina y su uso.
US8946296B2 (en) 2009-10-09 2015-02-03 Oryzon Genomics S.A. Substituted heteroaryl- and aryl-cyclopropylamine acetamides and their use
US9186337B2 (en) 2010-02-24 2015-11-17 Oryzon Genomics S.A. Lysine demethylase inhibitors for diseases and disorders associated with Hepadnaviridae
WO2011106574A2 (en) 2010-02-24 2011-09-01 Oryzon Genomics, S.A. Inhibitors for antiviral use
ES2607081T3 (es) 2010-04-19 2017-03-29 Oryzon Genomics, S.A. Inhibidores de desmetilasa específica de lisina-1 y su uso
LT2598482T (lt) 2010-07-29 2018-07-10 Oryzon Genomics, S.A. Demetilazės lsd1 inhibitoriai arilciklopropilamino pagrindu ir jų medicininis panaudojimas
EP2598480B1 (en) 2010-07-29 2019-04-24 Oryzon Genomics, S.A. Cyclopropylamine derivatives useful as lsd1 inhibitors
US10894787B2 (en) 2010-09-22 2021-01-19 Arena Pharmaceuticals, Inc. Modulators of the GPR119 receptor and the treatment of disorders related thereto
WO2012045883A1 (en) 2010-10-08 2012-04-12 Oryzon Genomics S.A. Cyclopropylamine inhibitors of oxidases
KR20130140672A (ko) * 2010-10-20 2013-12-24 키에시 파르마슈티시 엣스. 피. 에이. 기침 치료용 카보네이트 유도체
WO2012072713A2 (en) 2010-11-30 2012-06-07 Oryzon Genomics, S.A. Lysine demethylase inhibitors for diseases and disorders associated with flaviviridae
WO2012107498A1 (en) 2011-02-08 2012-08-16 Oryzon Genomics S.A. Lysine demethylase inhibitors for myeloproliferative disorders
EP2741741A2 (en) * 2011-05-19 2014-06-18 Oryzon Genomics, S.A. Lysine demethylase inhibitors for inflammatory diseases or conditions
WO2013052395A1 (en) * 2011-10-06 2013-04-11 Merck Sharp & Dohme Corp. 1,3-substituted azetidine pde10 inhibitors
BR112014009306B1 (pt) 2011-10-20 2021-07-20 Oryzon Genomics S.A. Compostos de (hetero)aril ciclopropilamina como inibidores de lsd1
CA2849564C (en) 2011-10-20 2020-10-20 Oryzon Genomics, S.A. (hetero)aryl cyclopropylamine compounds as lsd1 inhibitors
HUE035967T2 (hu) 2013-08-09 2018-06-28 Gruenenthal Gmbh Új helyettesített kondenzált pirimidinvegyületek
PL3196200T3 (pl) * 2014-08-26 2019-09-30 Astellas Pharma Inc. Pochodne 2-aminotiazolu lub jego sól jako ligandy muskarynowe m3 do leczenia chorób pęcherza moczowego
MX2021011472A (es) 2015-01-06 2022-08-17 Arena Pharm Inc Metodos de condiciones de tratamiento relacionadas con el receptor s1p1.
KR102603199B1 (ko) 2015-06-22 2023-11-16 아레나 파마슈티칼스, 인크. Ｓ1ｐ1 수용체-관련 장애에서의 사용을 위한 (ｒ)-2-(7-(4-시클로펜틸-3-(트리플루오로메틸)벤질옥시)-1,2,3,4-테트라히드로시클로-펜타[ｂ]인돌-3-일)아세트산 (화합물 1)의 결정성 ｌ-아르기닌 염
WO2018151873A1 (en) 2017-02-16 2018-08-23 Arena Pharmaceuticals, Inc. Compounds and methods for treatment of primary biliary cholangitis

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1143167A (en) * 1967-01-25 1969-02-19 Ucb Sa Derivatives of pyrimidine
JPH062751B2 (ja) 1986-07-14 1994-01-12 チッソ株式会社 ２−（トランス−４−アルキルシクロヘキシル）−５−アルコキシピリミジン
NZ225447A (en) * 1987-07-20 1991-12-23 Merck & Co Inc Piperazinyl derivatives of purine and purine isosteres and pharmaceutical compositions

Also Published As

Publication number Publication date
TW200306832A (en) 2003-12-01
US20060074068A1 (en) 2006-04-06
WO2003087064A1 (en) 2003-10-23
AU2003222786A1 (en) 2003-10-27
CO5450245A1 (es) 2004-10-29
US7544675B2 (en) 2009-06-09
EP1499598A1 (en) 2005-01-26

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