SG11201807540UA - Novel compounds and pharmaceutical compositions thereof for the treatment of fibrosis - Google Patents
Novel compounds and pharmaceutical compositions thereof for the treatment of fibrosisInfo
- Publication number
- SG11201807540UA SG11201807540UA SG11201807540UA SG11201807540UA SG11201807540UA SG 11201807540U A SG11201807540U A SG 11201807540UA SG 11201807540U A SG11201807540U A SG 11201807540UA SG 11201807540U A SG11201807540U A SG 11201807540UA SG 11201807540U A SG11201807540U A SG 11201807540UA
- Authority
- SG
- Singapore
- Prior art keywords
- wittelaan
- mechelen
- galapagos
- generaal
- international
- Prior art date
Links
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
WO 17 / 1487 87 Al (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (10) International Publication Number (43) International Publication Date WO 2017/148787 Al 8 September 2017 (08.09.2017) WIPO I PCT 1111111111111101110111111111110101111101110101111111101111111101111111111111110111111 (51) International Patent Classification: C07D 401/14 (2006.01) A61P 35/00 (2006.01) C07D 403/04 (2006.01) (21) International Application Number: PCT/EP2017/054139 (22) International Filing Date: 23 February 2017 (23.02.2017) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 1603745.9 4 March 2016 (04.03.2016) GB (71) Applicant: GALAPAGOS NV [BE/BE]; Generaal De Wittelaan L11/A3, 2800 Mechelen (BE). (81) Designated States (unless otherwise indicated, for every kind of national protection available): AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KH, KN, KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. (84) Designated States (unless otherwise indicated, for every kind of regional protection available): ARIPO (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG). arations under Rule 4.17: as to applicant's entitlement to apply for and be granted a patent (Rule 4.17(11)) of inventorship (Rule 4.17(iv)) Published: with international search report (Art. 21(3)) (72) Inventors: MAMMOLITI, Oscar; Galapagos NV Gener- aal De Wittelaan Ll l/A3, 2800 Mechelen (BE). JANSEN, Koen, Karel; Galapagos NV Generaal De Wittelaan Ll l/A3, 2800 Mechelen (BE). PALISSE, Adeline, Marie, Elise; Galapagos NV Generaal De Wittelaan L11/A3, 2800 Mechelen (BE). JOANNESSE, Caroline, Martine, An- Decl dree-Marie; Galapagos NV Generaal De Wittelaan Ll l/A3, 2800 Mechelen (BE). MENET, Christel, Jeanne, Marie; Confo Therapeutics Pleinlaan 2, Building E, 7th floor, E7.6, 1050 Brussels (BE). ALLART, Brigitte; Galapagos NV Generaal De Wittelaan L11/A3, 2800 Mechelen (BE). EL BKASSINY, Sandy; Galapagos NV Generaal De Wittelaan L11/A3, 2800 Mechelen (BE). (74) Agent: BAR, Gregory, Louis, Joseph; Galapagos NV Generaal De Wittelaan L11/A3, 2800 Mechelen (BE). (54) Title: NOVEL COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS THEREOF FOR THE TREATMENT OF FIBROSIS Ia (R 5 ) rin (57) : The present invention discloses compounds according to Formula I, wherein Rla, R 1b , R 2a , R 2b , R, R 3 4 , R 5 , R6a , c yl, Cy2, and the subscript n and m are as defined herein. The present invention relates to antagonists compounds of sphingosine 1-phos- phate (SIP) receptor, methods for their production, pharmaceutical compositions comprising the same, and methods of treatment us - ing the same, for the prophylaxis and/or treatment of diseases involving fibrotic diseases, inflammatory diseases, autoimmune dis - eases, metabolic diseases, cardiovascular diseases, and/or proliferative diseases by administering the compound of the invention.
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 |
|---|---|
| SG11201807540UA true SG11201807540UA (en) | 2018-09-27 |
Family
ID=55858990
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SG11201807540UA SG11201807540UA (en) | 2016-03-04 | 2017-02-23 | Novel compounds and pharmaceutical compositions thereof for the treatment of fibrosis |
Country Status (19)
| Country | Link |
|---|---|
| US (1) | US20190388421A1 (en) |
| EP (1) | EP3423445B1 (en) |
| JP (1) | JP2019507766A (en) |
| KR (1) | KR20180118752A (en) |
| CN (1) | CN108699037A (en) |
| AR (1) | AR107798A1 (en) |
| AU (1) | AU2017227900A1 (en) |
| BR (1) | BR112018067312A2 (en) |
| CA (1) | CA3016185A1 (en) |
| CO (1) | CO2018009876A2 (en) |
| GB (1) | GB201603745D0 (en) |
| IL (1) | IL261444A (en) |
| MX (1) | MX2018010218A (en) |
| PH (1) | PH12018501849A1 (en) |
| RU (1) | RU2018134780A (en) |
| SG (1) | SG11201807540UA (en) |
| TW (1) | TW201734005A (en) |
| WO (1) | WO2017148787A1 (en) |
| ZA (1) | ZA201805601B (en) |
Families Citing this family (11)
| 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 |
| MX2020004810A (en) | 2017-11-15 | 2020-08-13 | Galapagos Nv | Compounds and pharmaceutical compositions thereof for use in the treatment of fibrotic diseases. |
| WO2019148851A1 (en) * | 2018-02-02 | 2019-08-08 | 青岛清原化合物有限公司 | Five-membered ring-substituted pyridazinol compound and derivatives thereof, preparation method, herbicidal composition, and application |
| CN110878086B (en) * | 2018-09-06 | 2024-06-07 | 青岛清原化合物有限公司 | Five-membered ring substituted pyridazinol compound and derivative, preparation method, weeding composition and application thereof |
| CN109053693B (en) * | 2018-09-20 | 2021-02-05 | 顺毅股份有限公司 | Preparation and application of pyridazine amine compound |
| WO2020117962A1 (en) * | 2018-12-05 | 2020-06-11 | Viking Therapeutics, Inc. | Compositions for the treatment of fibrosis and inflammation |
| CN110128457B (en) * | 2019-05-24 | 2022-05-03 | 宁波瑞奇医药科技有限公司 | Preparation method of heterocyclic small molecule compound |
| 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 (en) * | 2020-07-07 | 2020-10-16 | 中瀚(齐河县)生物医药科技有限公司 | Synthesis process of 2-methoxy-3-bromo-5-fluoropyridine |
| 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 |
| BRPI0817397A2 (en) * | 2007-09-24 | 2015-04-07 | Allergan Inc | Indole compounds containing aryl or heteroaryl groups with sphingosine-1-phosphate receptor (sip) biological activity |
-
2016
- 2016-03-04 GB GBGB1603745.9A patent/GB201603745D0/en not_active Ceased
-
2017
- 2017-02-23 JP JP2018546507A patent/JP2019507766A/en active Pending
- 2017-02-23 SG SG11201807540UA patent/SG11201807540UA/en unknown
- 2017-02-23 WO PCT/EP2017/054139 patent/WO2017148787A1/en active Application Filing
- 2017-02-23 KR KR1020187028440A patent/KR20180118752A/en unknown
- 2017-02-23 AU AU2017227900A patent/AU2017227900A1/en not_active Abandoned
- 2017-02-23 CN CN201780015118.3A patent/CN108699037A/en active Pending
- 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 MX MX2018010218A patent/MX2018010218A/en unknown
- 2017-02-23 BR BR112018067312A patent/BR112018067312A2/en not_active Application Discontinuation
- 2017-02-23 RU RU2018134780A patent/RU2018134780A/en not_active Application Discontinuation
- 2017-02-23 EP EP17706783.2A patent/EP3423445B1/en active Active
- 2017-03-03 TW TW106107104A patent/TW201734005A/en unknown
- 2017-03-03 AR ARP170100536A patent/AR107798A1/en 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/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| AU2017227900A1 (en) | 2018-10-25 |
| IL261444A (en) | 2018-10-31 |
| US20190388421A1 (en) | 2019-12-26 |
| BR112018067312A2 (en) | 2018-12-26 |
| CA3016185A1 (en) | 2017-09-08 |
| JP2019507766A (en) | 2019-03-22 |
| WO2017148787A1 (en) | 2017-09-08 |
| ZA201805601B (en) | 2019-06-26 |
| EP3423445B1 (en) | 2020-04-01 |
| CO2018009876A2 (en) | 2018-10-10 |
| RU2018134780A (en) | 2020-04-06 |
| CN108699037A (en) | 2018-10-23 |
| TW201734005A (en) | 2017-10-01 |
| KR20180118752A (en) | 2018-10-31 |
| AR107798A1 (en) | 2018-06-06 |
| MX2018010218A (en) | 2018-11-09 |
| PH12018501849A1 (en) | 2019-01-28 |
| EP3423445A1 (en) | 2019-01-09 |
| GB201603745D0 (en) | 2016-04-20 |
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