AR101132A1 - Derivados de pirazina agonistas del gpr40 para el tratamiento de la diabetes tipo ii - Google Patents

Derivados de pirazina agonistas del gpr40 para el tratamiento de la diabetes tipo ii

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Publication number
AR101132A1
AR101132A1 ARP150102181A ARP150102181A AR101132A1 AR 101132 A1 AR101132 A1 AR 101132A1 AR P150102181 A ARP150102181 A AR P150102181A AR P150102181 A ARP150102181 A AR P150102181A AR 101132 A1 AR101132 A1 AR 101132A1
Authority
AR
Argentina
Prior art keywords
alkyl
cycloalkyl
methoxy
heterocyclyl
phenyl
Prior art date
Application number
ARP150102181A
Other languages
English (en)
Original Assignee
Janssen Pharmaceutica Nv
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 Janssen Pharmaceutica Nv filed Critical Janssen Pharmaceutica Nv
Publication of AR101132A1 publication Critical patent/AR101132A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/12—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/12—Antidiuretics, e.g. drugs for diabetes insipidus
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/14—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three 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
    • C07D241/18—Oxygen or sulfur atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/14—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three 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
    • C07D241/20—Nitrogen 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
    • C07D409/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms 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
    • C07D413/04—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 directly linked by a ring-member-to-ring-member bond

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Diabetes (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Child & Adolescent Psychology (AREA)
  • Cardiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Reivindicación 1: Un compuesto de fórmula (1) caracterizado porque R¹ se selecciona del grupo que consiste en fenilo, piridin-4-ilo, y tiofenilo; caracterizado porque R¹ está opcionalmente sustituido independientemente con uno o dos sustituyentes que son alquilo C₁₋₄, metoxi, fluoro, ciano, o trifluorometilo; siempre y cuando el fenilo de R¹ está sustituido con no más de un sustituyente metoxi; G se selecciona del grupo que consiste en alquilo C₁₋₆; alcoxi C₁₋₆; cicloalquilo C₃₋₇; 2,2,6,6-tetrametiltetrahidro-2H-piran-4-iloxi; oxetan-3-iloxi; alq C₂₋₆-1-en-1-ilo; 3,3,3-trifluoropropiloxi; 1,1,1-trifluoroprop-2-ilo; (alquil C₁₋₆)tiofen-2-ilo; fenilo opcionalmente sustituido con uno a dos sustituyentes alquilo C₁₋₄; (alquil C₁₋₆)amino; di(alquil C₁₋₆)amino; heterociclilo donde dicho heterociclilo está unido al anillo del núcleo pirazina a través de un átomo de nitrógeno y dicho heterociclilo está opcionalmente espirofusionado a un grupo cicloalquilo C₃₋₇; anillo de fórmula (2); cicloalquiloxi C₃₋₇; y cicloalquil C₃₋₇-metoxi; en donde la porción cicloalquiloxi C₃₋₇ y cicloalquilo C₃₋₇; del cicloalquilo-metoxi C₃₋₇ están opcionalmente sustituidos con uno a cuatro sustituyentes metilo; R² es cicloalquilo C₃₋₅, alquilo C₁₋₆, o ciano; o un enantiómero, diastereómero, o forma de sal farmacéuticamente aceptable de estos.
ARP150102181A 2014-07-09 2015-07-08 Derivados de pirazina agonistas del gpr40 para el tratamiento de la diabetes tipo ii AR101132A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201462022257P 2014-07-09 2014-07-09

Publications (1)

Publication Number Publication Date
AR101132A1 true AR101132A1 (es) 2016-11-23

Family

ID=53761519

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP150102181A AR101132A1 (es) 2014-07-09 2015-07-08 Derivados de pirazina agonistas del gpr40 para el tratamiento de la diabetes tipo ii

Country Status (5)

Country Link
US (1) US9688642B2 (es)
AR (1) AR101132A1 (es)
TW (1) TW201613878A (es)
UY (1) UY36209A (es)
WO (1) WO2016007714A1 (es)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2019019124A (ja) * 2017-07-19 2019-02-07 日本化薬株式会社 ピラジン化合物
EP3709995A4 (en) * 2017-11-16 2021-04-14 Merck Sharp & Dohme Corp. BICYCLIC ANTIDIABETIC COMPOUNDS
CN118084940A (zh) 2018-02-13 2024-05-28 吉利德科学公司 Pd-1/pd-l1抑制剂
CA3093130C (en) 2018-04-19 2023-10-17 Gilead Sciences, Inc. Pd-1/pd-l1 inhibitors
CR20210013A (es) 2018-07-13 2021-02-26 Gilead Sciences Inc Inhibidores de pd-1/pd-l1
CA3117199C (en) 2018-10-24 2024-03-19 Gilead Sciences, Inc. Pd-1/pd-l1 inhibitors
CN115867536A (zh) * 2020-02-28 2023-03-28 卡尔优普公司 Gpr40激动剂
IL295825A (en) * 2020-02-28 2022-10-01 Kallyope Inc gpr40 agonists

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1295880A4 (en) * 2000-06-28 2004-05-06 Ssp Co Ltd IMIDAZOLE DERIVATIVES OR SALTS THEREOF, AND MEDICINAL PRODUCTS CONTAINING DERIVATIVES OR SALTS
WO2014078608A1 (en) * 2012-11-16 2014-05-22 Bristol-Myers Squibb Company Dihydropyrazole gpr40 modulators
MA38170B1 (fr) 2012-11-28 2017-04-28 Boehringer Ingelheim Int Nouveaux acides indanyloxydihydrobenzofuranylacétiques

Also Published As

Publication number Publication date
US9688642B2 (en) 2017-06-27
UY36209A (es) 2016-01-29
TW201613878A (en) 2016-04-16
US20160009662A1 (en) 2016-01-14
WO2016007714A1 (en) 2016-01-14

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