CO2018009876A2 - Nuevos compuestos y sus composiciones farmacéuticas para el tratamiento de fibrosis - Google Patents

Nuevos compuestos y sus composiciones farmacéuticas para el tratamiento de fibrosis

Info

Publication number
CO2018009876A2
CO2018009876A2 CONC2018/0009876A CO2018009876A CO2018009876A2 CO 2018009876 A2 CO2018009876 A2 CO 2018009876A2 CO 2018009876 A CO2018009876 A CO 2018009876A CO 2018009876 A2 CO2018009876 A2 CO 2018009876A2
Authority
CO
Colombia
Prior art keywords
diseases
treatment
pharmaceutical compositions
fibrosis
new compounds
Prior art date
Application number
CONC2018/0009876A
Other languages
English (en)
Inventor
Christel Jeanne Marie Menet
Brigitte Allart
Oscar Mammoliti
Adeline Marie Elise Palisse
Caroline Martine Andrée-Marie Joannesse
Bkassiny Sandy El
Koen Karel Jansen
Original Assignee
Galapagos 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 Galapagos Nv filed Critical Galapagos Nv
Publication of CO2018009876A2 publication Critical patent/CO2018009876A2/es

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Classifications

    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • 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]
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • 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
    • 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
    • C07D403/04—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
    • 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
    • C07D403/14—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 three or more hetero rings
    • 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
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Rheumatology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

La presente invención describe compuestos de acuerdo con la Fórmula I: en donde R1a, R1b, R2a, R2b, R3, R4, R5, R6a, X, Cy1, Cy2, y los subíndices n y m son como se define en la presente. La presente invención se refiere a compuestos antagonistas del receptor de 1–fosfato de esfingosina (S1P), métodos para su producción, composiciones farmacéuticas que los comprenden, y métodos de tratamiento en los que se usan, para la profilaxis y/o el tratamiento de enfermedades que involucran enfermedades fibróticas, enfermedades inflamatorias, enfermedades autoinmunes, enfermedades metabólicas, enfermedades cardiovasculares y/o enfermedades proliferativas mediante la administración del compuesto de la invención.
CONC2018/0009876A 2016-03-04 2018-09-19 Nuevos compuestos y sus composiciones farmacéuticas para el tratamiento de fibrosis CO2018009876A2 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GBGB1603745.9A GB201603745D0 (en) 2016-03-04 2016-03-04 Novel compounds and pharmaceutical compositions thereof for the treatment of fibrosis
PCT/EP2017/054139 WO2017148787A1 (en) 2016-03-04 2017-02-23 Novel compounds and pharmaceutical compositions thereof for the treatment of fibrosis

Publications (1)

Publication Number Publication Date
CO2018009876A2 true CO2018009876A2 (es) 2018-10-10

Family

ID=55858990

Family Applications (1)

Application Number Title Priority Date Filing Date
CONC2018/0009876A CO2018009876A2 (es) 2016-03-04 2018-09-19 Nuevos compuestos y sus composiciones farmacéuticas para el tratamiento de fibrosis

Country Status (19)

Country Link
US (1) US20190388421A1 (es)
EP (1) EP3423445B1 (es)
JP (1) JP2019507766A (es)
KR (1) KR20180118752A (es)
CN (1) CN108699037A (es)
AR (1) AR107798A1 (es)
AU (1) AU2017227900A1 (es)
BR (1) BR112018067312A2 (es)
CA (1) CA3016185A1 (es)
CO (1) CO2018009876A2 (es)
GB (1) GB201603745D0 (es)
IL (1) IL261444A (es)
MX (1) MX2018010218A (es)
PH (1) PH12018501849A1 (es)
RU (1) RU2018134780A (es)
SG (1) SG11201807540UA (es)
TW (1) TW201734005A (es)
WO (1) WO2017148787A1 (es)
ZA (1) ZA201805601B (es)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2019091999A1 (en) 2017-11-08 2019-05-16 INSERM (Institut National de la Santé et de la Recherche Médicale) S1pr2 antagonists for treating diseases involving abnormal immune responses
KR20200088844A (ko) 2017-11-15 2020-07-23 갈라파고스 엔.브이. 섬유증성 질병 치료에서의 용도를 위한 화합물 및 그의 약학 조성물
US12024500B2 (en) * 2018-02-02 2024-07-02 Qingdao Kingagroot Chemical Compound Co., Ltd. Five-membered ring-substituted pyridazinol compounds and derivatives, preparation methods, herbicidal compositions and applications thereof
WO2019148850A1 (zh) 2018-02-02 2019-08-08 青岛清原化合物有限公司 吡啶环取代的哒嗪醇类化合物及其衍生物、制备方法、除草组合物和应用
CN110878086B (zh) * 2018-09-06 2024-06-07 青岛清原化合物有限公司 五元环取代的哒嗪醇类化合物及其衍生物、制备方法、除草组合物和应用
CN109053693B (zh) * 2018-09-20 2021-02-05 顺毅股份有限公司 哒嗪胺类化合物的制备及其应用
JP2022510691A (ja) * 2018-12-05 2022-01-27 バイキング・セラピューティクス・インコーポレイテッド 線維症及び炎症の処置のための組成物
CN110128457B (zh) * 2019-05-24 2022-05-03 宁波瑞奇医药科技有限公司 杂环小分子化合物的制备方法
US11465982B2 (en) * 2019-07-22 2022-10-11 Boehringer Ingelheim International Gmbh Pyridazines
US11485727B2 (en) 2019-07-22 2022-11-01 Boehringer Ingelheim International Gmbh N-methyl, n-(6-(methoxy)pyridazin-3-yl) amine derivatives as autotaxin (ATX) modulators
CN111777549A (zh) * 2020-07-07 2020-10-16 中瀚(齐河县)生物医药科技有限公司 一种2-甲氧基-3-溴-5-氟吡啶的合成工艺
EP4419508A2 (en) * 2021-10-22 2024-08-28 Carmot Therapeutics, Inc. Oxazole, oxadiazole, and indole derivatives for the inhibition of usp28

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2360305A1 (en) * 1999-02-09 2000-08-17 Bristol-Myers Squibb Company Lactam inhibitors of fxa and method
BRPI0817397A2 (pt) * 2007-09-24 2015-04-07 Allergan Inc Compostos indol contendo grupos arila ou heteroarila com atividade biológica do receptor de esfingosina-1-fosfato (sip)

Also Published As

Publication number Publication date
EP3423445B1 (en) 2020-04-01
KR20180118752A (ko) 2018-10-31
JP2019507766A (ja) 2019-03-22
US20190388421A1 (en) 2019-12-26
PH12018501849A1 (en) 2019-01-28
MX2018010218A (es) 2018-11-09
TW201734005A (zh) 2017-10-01
CN108699037A (zh) 2018-10-23
GB201603745D0 (en) 2016-04-20
WO2017148787A1 (en) 2017-09-08
AR107798A1 (es) 2018-06-06
SG11201807540UA (en) 2018-09-27
EP3423445A1 (en) 2019-01-09
IL261444A (en) 2018-10-31
ZA201805601B (en) 2019-06-26
RU2018134780A (ru) 2020-04-06
AU2017227900A1 (en) 2018-10-25
BR112018067312A2 (pt) 2018-12-26
CA3016185A1 (en) 2017-09-08

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