BR112018012469A2 - quinolina-3-carboxamidas como inibidores da h-pgds - Google Patents

quinolina-3-carboxamidas como inibidores da h-pgds

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Publication number
BR112018012469A2
BR112018012469A2 BR112018012469A BR112018012469A BR112018012469A2 BR 112018012469 A2 BR112018012469 A2 BR 112018012469A2 BR 112018012469 A BR112018012469 A BR 112018012469A BR 112018012469 A BR112018012469 A BR 112018012469A BR 112018012469 A2 BR112018012469 A2 BR 112018012469A2
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BR
Brazil
Prior art keywords
pgds
compound
relates
carboxamides
quinoline
Prior art date
Application number
BR112018012469A
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English (en)
Other versions
BR112018012469B1 (pt
Inventor
L Larkin Andrew
Paul Hancock Ashley
Schulte Christie
J Price Daniel
Norman Deaton Dave
Saxty Gordon
Hobbs Heather
Edward David Smith Ian
Le Joelle
Wendell Wilson Joseph
T Schaller Lee
N Mortenson Paul
Cadilla Rodolfo
Teanby Hodgson Simon
Andrew Thomson Stephen
Original Assignee
Astex Therapeutics Ltd
Glaxosmithkline Ip Dev Ltd
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Publication date
Application filed by Astex Therapeutics Ltd, Glaxosmithkline Ip Dev Ltd filed Critical Astex Therapeutics Ltd
Publication of BR112018012469A2 publication Critical patent/BR112018012469A2/pt
Publication of BR112018012469B1 publication Critical patent/BR112018012469B1/pt

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    • C—CHEMISTRY; METALLURGY
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    • 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
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
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    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
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    • A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P27/02—Ophthalmic agents
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D215/20—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
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    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D215/48—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C07D215/54—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 3
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    • 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
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    • 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
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    • C07—ORGANIC CHEMISTRY
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    • 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
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    • 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
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    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
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    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/056—Ortho-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pulmonology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Neurology (AREA)
  • Dermatology (AREA)
  • Pain & Pain Management (AREA)
  • Immunology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Rheumatology (AREA)
  • Epidemiology (AREA)
  • Urology & Nephrology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Otolaryngology (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Quinoline Compounds (AREA)

Abstract

a presente invenção refere-se a compostos de fórmula (xi): (xi) em que r1a, r2a, r3a, r4a, r5a, r6a e aa são conforme definidos neste documento, e a sais farmaceuticamente aceitáveis dos mesmos. os compostos da presente invenção são inibidores da prostaglandina d sintase hematopoiética (h-pgds) e podem ser úteis no tratamento da distrofia muscular de duchenne. logo, a invenção também se refere a composições farmacêuticas que compreendem um composto da invenção. além do mais, a invenção também se refere a métodos para inibir a atividade da h-pgds e ao tratamento de transtornos associados a esta usando um composto da invenção ou uma composição farmacêutica compreendendo um composto da invenção.
BR112018012469-9A 2015-12-17 2016-12-15 compostos quinolina-3-carboxamidas como inibidores da h-pgds, composição farmacêutica compreendendo os ditos compostos e uso terapêutico dos mesmos. BR112018012469B1 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201562268630P 2015-12-17 2015-12-17
US62/268.630 2015-12-17
PCT/IB2016/057676 WO2017103851A1 (en) 2015-12-17 2016-12-15 Quinoline-3-carboxamides as h-pgds inhibitors

Publications (2)

Publication Number Publication Date
BR112018012469A2 true BR112018012469A2 (pt) 2018-12-18
BR112018012469B1 BR112018012469B1 (pt) 2020-11-24

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BR112018012469-9A BR112018012469B1 (pt) 2015-12-17 2016-12-15 compostos quinolina-3-carboxamidas como inibidores da h-pgds, composição farmacêutica compreendendo os ditos compostos e uso terapêutico dos mesmos.

Country Status (13)

Country Link
US (1) US20210238162A1 (pt)
EP (1) EP3390384B1 (pt)
JP (1) JP2019502691A (pt)
KR (1) KR20180095580A (pt)
CN (1) CN108430992A (pt)
AR (1) AR107044A1 (pt)
AU (1) AU2016370779B2 (pt)
BR (1) BR112018012469B1 (pt)
CA (1) CA3008358A1 (pt)
RU (1) RU2018126105A (pt)
TW (1) TW201733988A (pt)
UY (1) UY37028A (pt)
WO (1) WO2017103851A1 (pt)

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KR20230027059A (ko) 2020-06-19 2023-02-27 사토 세이야쿠 가부시키가이샤 H－pgds를 저해하는 축환 화합물
KR20240013784A (ko) * 2021-05-28 2024-01-30 머크 샤프 앤드 돔 엘엘씨 Btk 억제제 및 그의 중간체의 합성
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BR112018012469B1 (pt) 2020-11-24
AU2016370779B2 (en) 2019-07-25
CN108430992A (zh) 2018-08-21
JP2019502691A (ja) 2019-01-31
RU2018126105A (ru) 2020-01-17
KR20180095580A (ko) 2018-08-27
AU2016370779A1 (en) 2018-06-14
CA3008358A1 (en) 2017-06-22
UY37028A (es) 2017-07-31
EP3390384B1 (en) 2021-09-15
EP3390384A1 (en) 2018-10-24
TW201733988A (zh) 2017-10-01
WO2017103851A1 (en) 2017-06-22
AR107044A1 (es) 2018-03-14

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