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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

Info

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

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic 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
    • C07D239/28Heterocyclic 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
    • C07D239/32One oxygen, sulfur or nitrogen atom
    • C07D239/42One nitrogen atom
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/08Bronchodilators
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic 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
    • C07D239/28Heterocyclic 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
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48Two nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic 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
    • C07D239/28Heterocyclic 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
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/50Three nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic 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
    • C07D239/28Heterocyclic 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
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/60Three or more oxygen or sulfur 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
    • C07D401/04Heterocyclic 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
    • 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
    • C07D403/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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
    • C07D405/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-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 (30)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102558155A (zh) 2003-01-14 2012-07-11 阿伦纳药品公司 作为代谢调节剂的芳基和杂芳基衍生物及其所涉及的疾病如糖尿病和高血糖症的预防和治疗
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
TW200946526A (en) 2008-02-06 2009-11-16 Glaxo Group Ltd Dual pharmacophores-PDE4-muscarinic antagonistics
UY31637A1 (es) 2008-02-06 2009-08-03 Farmacoforos duales-antagonistas muscarinicos de pde4
UY31636A1 (es) 2008-02-06 2009-08-03 Farmacoforos duales-antagonistas muscarinicos de pde4
EP2361242B1 (en) 2008-10-17 2018-08-01 Oryzon Genomics, S.A. Oxidase inhibitors and their use
WO2010084160A1 (en) 2009-01-21 2010-07-29 Oryzon Genomics S.A. Phenylcyclopropylamine derivatives and their medical use
JP5699152B2 (ja) 2009-09-25 2015-04-08 オリゾン・ジェノミックス・ソシエダッド・アノニマOryzon Genomics S.A. リジン特異的デメチラーゼ−1阻害剤およびその使用
EP2486002B1 (en) 2009-10-09 2019-03-27 Oryzon Genomics, S.A. Substituted heteroaryl- and aryl- cyclopropylamine acetamides and their use
WO2011106573A2 (en) 2010-02-24 2011-09-01 Oryzon Genomics, S.A. Lysine demethylase inhibitors for diseases and disorders associated with hepadnaviridae
WO2011106105A2 (en) 2010-02-24 2011-09-01 Oryzon Genomics, S.A. Inhibitors for antiviral use
DK2560947T3 (en) 2010-04-19 2016-11-21 Oryzon Genomics Sa LYSINE-SPECIFIC demethylase-1 INHIBITORS AND THEIR USE
RU2611437C2 (ru) 2010-07-29 2017-02-22 Оризон Дженомикс С.А. Ингибиторы деметилазы lsd1 на основе арилциклопропиламина и их применение в медицине
WO2012013727A1 (en) 2010-07-29 2012-02-02 Oryzon Genomics S.A. Cyclopropylamine derivatives useful as lsd1 inhibitors
EA201390421A1 (ru) 2010-09-22 2013-09-30 Арена Фармасьютикалз, Инк. Модуляторы рецептора gpr119 и лечение связанных с ним нарушений
US9061966B2 (en) 2010-10-08 2015-06-23 Oryzon Genomics S.A. Cyclopropylamine inhibitors of oxidases
EP2630145A1 (en) * 2010-10-20 2013-08-28 Chiesi Farmaceutici S.p.A. Carbonate derivatives for the treatment of cough
WO2012072713A2 (en) 2010-11-30 2012-06-07 Oryzon Genomics, S.A. Lysine demethylase inhibitors for diseases and disorders associated with flaviviridae
EP3981395A1 (en) 2011-02-08 2022-04-13 Oryzon Genomics, S.A. Lysine demethylase inhibitors for myeloproliferative disorders
WO2012156531A2 (en) * 2011-05-19 2012-11-22 Oryzon Genomics, S.A. Lysine demethylase inhibitors for inflammatory diseases or conditions
EP2763672B1 (en) 2011-10-06 2016-08-10 Merck Sharp & Dohme Corp. 1,3-substituted azetidine pde10 inhibitors
IN2014CN03337A (es) 2011-10-20 2015-07-03 Oryzon Genomics Sa
EP3736265A1 (en) 2011-10-20 2020-11-11 Oryzon Genomics, S.A. (hetero)aryl cyclopropylamine compounds as lsd1 inhibitors
PL3030565T3 (pl) * 2013-08-09 2017-12-29 Grünenthal GmbH Nowe podstawione skondensowane związki pirymidynowe
CN106573928B (zh) 2014-08-26 2020-04-14 安斯泰来制药株式会社 2-氨基噻唑衍生物或其盐
EP4445956A3 (en) 2015-01-06 2024-12-04 Arena Pharmaceuticals, Inc. Compound for use in treating conditions related to the s1p1 receptor
PL3310760T3 (pl) 2015-06-22 2023-03-06 Arena Pharmaceuticals, Inc. Krystaliczna sól L-argininy kwasu (R)-2-(7-(4-cyklopentylo-3-(trifluorometylo)benzyloksy)- 1,2,3,4-tetrahydrocyklo-penta[b]indol-3-ilo)octowego do zastosowania w zaburzeniach związanych z receptorem S1P1
CN110520124A (zh) 2017-02-16 2019-11-29 艾尼纳制药公司 用于治疗原发性胆汁性胆管炎的化合物和方法
CA3102136A1 (en) 2018-06-06 2019-12-12 Arena Pharmaceuticals, Inc. Methods of treating conditions related to the s1p1 receptor

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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
IL87149A (en) * 1987-07-20 1994-05-30 Merck & Co Inc 6-Piperazinyl derivatives of purine and its 3- and 9-deaza isosteres, their preparation and pharmaceutical compositions containing them

Also Published As

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

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