CO2018009876A2 - Nuevos compuestos y sus composiciones farmacéuticas para el tratamiento de fibrosis - Google Patents
Nuevos compuestos y sus composiciones farmacéuticas para el tratamiento de fibrosisInfo
- 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
Links
- 150000001875 compounds Chemical class 0.000 title abstract 4
- 238000011282 treatment Methods 0.000 title abstract 3
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 2
- 206010016654 Fibrosis Diseases 0.000 title 1
- 230000004761 fibrosis Effects 0.000 title 1
- 201000010099 disease Diseases 0.000 abstract 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 3
- 102000011011 Sphingosine 1-phosphate receptors Human genes 0.000 abstract 2
- 108050001083 Sphingosine 1-phosphate receptors Proteins 0.000 abstract 2
- 238000000034 method Methods 0.000 abstract 2
- 208000023275 Autoimmune disease Diseases 0.000 abstract 1
- 208000024172 Cardiovascular disease Diseases 0.000 abstract 1
- 239000005557 antagonist Substances 0.000 abstract 1
- 230000003176 fibrotic effect Effects 0.000 abstract 1
- 208000027866 inflammatory disease Diseases 0.000 abstract 1
- 208000030159 metabolic disease Diseases 0.000 abstract 1
- 230000002062 proliferating effect Effects 0.000 abstract 1
- 238000011321 prophylaxis Methods 0.000 abstract 1
- DUYSYHSSBDVJSM-KRWOKUGFSA-N sphingosine 1-phosphate Chemical compound CCCCCCCCCCCCC\C=C\[C@@H](O)[C@@H](N)COP(O)(O)=O DUYSYHSSBDVJSM-KRWOKUGFSA-N 0.000 abstract 1
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)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Epidemiology (AREA)
- Transplantation (AREA)
- Heart & Thoracic Surgery (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Cardiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (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.
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 (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20210038502A1 (en) | 2017-11-08 | 2021-02-11 | INSERM (Institut National de la Santé et de la Recherche Médicale) | S1pr2 antagonists for treating diseases involving abnormal immune responses |
| CN111343986A (zh) | 2017-11-15 | 2020-06-26 | 加拉帕戈斯股份有限公司 | 用于治疗纤维化疾病的化合物及其药物组合物 |
| 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 |
| 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 |
| CA3094167A1 (en) | 2018-03-22 | 2019-09-26 | Viking Therapeutics, Inc. | Crystalline forms and methods of producing crystalline forms of a compound |
| 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 |
| WO2020117962A1 (en) * | 2018-12-05 | 2020-06-11 | Viking Therapeutics, Inc. | Compositions for the treatment of fibrosis and inflammation |
| 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 |
| DK4003978T3 (da) | 2019-07-22 | 2024-07-22 | Boehringer Ingelheim Int | N-methyl, n-(6-(methoxy)pyridazin-3-yl) aminderivater som autotaxin (atx) modulatorer til behandlingen af inflammatoriske luftvejs- eller fibrotiske sygdomme |
| 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 |
| US11465982B2 (en) * | 2019-07-22 | 2022-10-11 | Boehringer Ingelheim International Gmbh | Pyridazines |
| 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 |
| WO2023069721A2 (en) * | 2021-10-22 | 2023-04-27 | Carmot Therapeutics, Inc. | Oxazole, oxadiazole, and indole derivatives for the inhibition of usp28 |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6297233B1 (en) * | 1999-02-09 | 2001-10-02 | Bristol-Myers Squibb Company | Lactam inhibitors of FXa and method |
| CN101918360A (zh) * | 2007-09-24 | 2010-12-15 | 阿勒根公司 | 具有1-磷酸-鞘氨醇(s1p)受体生物学活性的带芳基或者杂芳基基团的吲哚化合物 |
-
2016
- 2016-03-04 GB GBGB1603745.9A patent/GB201603745D0/en not_active Ceased
-
2017
- 2017-02-23 MX MX2018010218A patent/MX2018010218A/es unknown
- 2017-02-23 EP EP17706783.2A patent/EP3423445B1/en active Active
- 2017-02-23 JP JP2018546507A patent/JP2019507766A/ja active Pending
- 2017-02-23 RU RU2018134780A patent/RU2018134780A/ru not_active Application Discontinuation
- 2017-02-23 US US16/081,797 patent/US20190388421A1/en not_active Abandoned
- 2017-02-23 CA CA3016185A patent/CA3016185A1/en not_active Abandoned
- 2017-02-23 SG SG11201807540UA patent/SG11201807540UA/en unknown
- 2017-02-23 AU AU2017227900A patent/AU2017227900A1/en not_active Abandoned
- 2017-02-23 BR BR112018067312A patent/BR112018067312A2/pt not_active Application Discontinuation
- 2017-02-23 CN CN201780015118.3A patent/CN108699037A/zh active Pending
- 2017-02-23 KR KR1020187028440A patent/KR20180118752A/ko not_active Withdrawn
- 2017-02-23 WO PCT/EP2017/054139 patent/WO2017148787A1/en not_active Ceased
- 2017-03-03 AR ARP170100536A patent/AR107798A1/es unknown
- 2017-03-03 TW TW106107104A patent/TW201734005A/zh unknown
-
2018
- 2018-08-22 ZA ZA2018/05601A patent/ZA201805601B/en unknown
- 2018-08-29 IL IL261444A patent/IL261444A/en unknown
- 2018-08-30 PH PH12018501849A patent/PH12018501849A1/en unknown
- 2018-09-19 CO CONC2018/0009876A patent/CO2018009876A2/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| IL261444A (en) | 2018-10-31 |
| EP3423445A1 (en) | 2019-01-09 |
| AU2017227900A1 (en) | 2018-10-25 |
| CA3016185A1 (en) | 2017-09-08 |
| MX2018010218A (es) | 2018-11-09 |
| TW201734005A (zh) | 2017-10-01 |
| EP3423445B1 (en) | 2020-04-01 |
| SG11201807540UA (en) | 2018-09-27 |
| AR107798A1 (es) | 2018-06-06 |
| WO2017148787A1 (en) | 2017-09-08 |
| RU2018134780A (ru) | 2020-04-06 |
| JP2019507766A (ja) | 2019-03-22 |
| US20190388421A1 (en) | 2019-12-26 |
| GB201603745D0 (en) | 2016-04-20 |
| PH12018501849A1 (en) | 2019-01-28 |
| KR20180118752A (ko) | 2018-10-31 |
| CN108699037A (zh) | 2018-10-23 |
| BR112018067312A2 (pt) | 2018-12-26 |
| ZA201805601B (en) | 2019-06-26 |
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