SG11201803627XA - N-substituted indole derivatives as pge2 receptor modulators - Google Patents
N-substituted indole derivatives as pge2 receptor modulatorsInfo
- Publication number
- SG11201803627XA SG11201803627XA SG11201803627XA SG11201803627XA SG11201803627XA SG 11201803627X A SG11201803627X A SG 11201803627XA SG 11201803627X A SG11201803627X A SG 11201803627XA SG 11201803627X A SG11201803627X A SG 11201803627XA SG 11201803627X A SG11201803627X A SG 11201803627XA
- Authority
- SG
- Singapore
- Prior art keywords
- gewerbestrasse
- allschwil
- actelion
- pharmaceuticals
- iii
- Prior art date
Links
- 102000008866 Prostaglandin E receptors Human genes 0.000 title abstract 2
- 108010088540 Prostaglandin E receptors Proteins 0.000 title abstract 2
- 229940054051 antipsychotic indole derivative Drugs 0.000 title abstract 2
- -1 N-substituted indole Chemical class 0.000 title 1
- 239000003814 drug Substances 0.000 abstract 5
- GJPICJJJRGTNOD-UHFFFAOYSA-N bosentan Chemical compound COC1=CC=CC=C1OC(C(=NC(=N1)C=2N=CC=CN=2)OCCO)=C1NS(=O)(=O)C1=CC=C(C(C)(C)C)C=C1 GJPICJJJRGTNOD-UHFFFAOYSA-N 0.000 abstract 4
- 229960003065 bosentan Drugs 0.000 abstract 4
- 239000003795 chemical substances by application Substances 0.000 abstract 2
- 102220240796 rs553605556 Human genes 0.000 abstract 2
- SIKJAQJRHWYJAI-UHFFFAOYSA-N Indole Chemical class C1=CC=C2NC=CC2=C1 SIKJAQJRHWYJAI-UHFFFAOYSA-N 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 230000008520 organization Effects 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 150000003180 prostaglandins Chemical class 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
-
- 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
-
- 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
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
- C07D403/12—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 linked by a chain containing hetero atoms as chain links
-
- 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
- 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
- C07D413/14—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
- C07D417/00—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
- C07D417/14—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 three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Indole Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 26 May 2017(26.05.2017) WIPOIPCT (10) International Publication Number WO 2017/085198 A1 (51) International Patent Classification: (30) (71) (72) C07D 403/12 (2006.01) C07D 413/14 (2006.01) C07D 403/14 (2006.01) C07D 409/14 (2006.01) C07D 417/14 (2006.01) A61K31/506 (2006.01) A61P 35/00 (2006.01) A61P 25/00 (2006.01) A61P9/00 (2006.01) A61P11/00 (2006.01) A61P15/00 (2006.01) (21) International Application Number: PCT/EP2016/078028 (22) International Filing Date: (25) Filing Language: (26) Publication Language 17 November 2016 (17.11.2016) English English Priority Data: PCT/EP2015/077269 20 November 2015 (20.11.2015) EP Applicant: ACTELION PHARMACEUTICALS LTD [CH/CH]; Gewerbestrasse 16, 4123 Allschwil (CH). Inventors: FRETZ, Heinz; c/o Actelion Pharmaceuticals Ltd, Gewerbestrasse 16, 4123 Allschwil (CH). LYOTHI- ER, Isabelle; c/o Actelion Pharmaceuticals Ltd, Gewerbe strasse 16, 4123 Allschwil (CH). POTHIER, Julien; c/o Actelion Pharmaceuticals Ltd, Gewerbestrasse 16, 4123 Allschwil (CH). RICHARD-BILDSTEIN, Sylvia; c/o Ac telion Pharmaceuticals Ltd, Gewerbestrasse 16, 4123 All schwil (CH). SIFFERLEN, Thierry; c/o Actelion Phar maceuticals Ltd, Gewerbestrasse 16, 4123 Allschwil (CH). WYDER PETERS, Lorenza; c/o Actelion Pharmaceutic als Ltd, Gewerbestrasse 16, 4123 Allschwil (CH). POZZI, Davide; c/o Actelion Pharmaceuticals Ltd, Gewerbestrasse 16, 4123 Allschwil (CH). CORMINBOEUF, Olivier; c/o Actelion Pharmaceuticals Ltd, Gewerbestrasse 16, 4123 Allschwil (CH). (74) Agent: VELKER, Jorg; c/o Actelion Pharmaceuticals Ltd, Gewerbestrasse 16, 4123 Allschwil (CH). (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, 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). Declarations under Rule 4.17: — as to applicant's entitlement to apply for and be granted a patent (Rule 4.17(H)) [Continued on next page] (54) Title: N - SUB STITUTED INDOLE DERIVATIVES AS PGE2 RECEPTOR MODULATORS 00 ON ICi 00 n O Ar 1 (I) (57) : The present invention relates to derivativesof formula (I) wherein (R*)n, R2, R3, R4a, R4b, R5a, R5b and Ar1 are as de scribed in the description, to their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of formula (I), and especially to their use as modulators of the prostaglandin 2 receptors EP2 and/or EP4. WO 2017/085198 A11II III IIII III III III 11II III Hill lllll lllll II lllll III mill llll Ill III Published: — with international search report (Art. 21(3))
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP2015077269 | 2015-11-20 | ||
| PCT/EP2016/078028 WO2017085198A1 (en) | 2015-11-20 | 2016-11-17 | N-substituted indole derivatives as pge2 receptor modulators |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| SG11201803627XA true SG11201803627XA (en) | 2018-06-28 |
Family
ID=57326428
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SG11201803627XA SG11201803627XA (en) | 2015-11-20 | 2016-11-17 | N-substituted indole derivatives as pge2 receptor modulators |
Country Status (34)
| Country | Link |
|---|---|
| US (2) | US11241431B2 (en) |
| EP (2) | EP3377483B9 (en) |
| JP (2) | JP2018534328A (en) |
| KR (1) | KR102352022B1 (en) |
| CN (1) | CN108349949B (en) |
| AU (1) | AU2016358242B2 (en) |
| BR (1) | BR112018010291B1 (en) |
| CA (1) | CA3002610C (en) |
| CL (1) | CL2018001325A1 (en) |
| CO (1) | CO2018005715A2 (en) |
| CR (1) | CR20180323A (en) |
| CY (1) | CY1124913T1 (en) |
| DK (2) | DK3928836T3 (en) |
| EA (1) | EA037953B1 (en) |
| ES (2) | ES2994636T3 (en) |
| FI (1) | FI3928836T3 (en) |
| HR (2) | HRP20211678T1 (en) |
| HU (2) | HUE056679T2 (en) |
| IL (1) | IL259424B (en) |
| LT (2) | LT3928836T (en) |
| MA (2) | MA43251B1 (en) |
| MX (1) | MX375978B (en) |
| MY (1) | MY195888A (en) |
| PE (1) | PE20181304A1 (en) |
| PH (1) | PH12018501077B1 (en) |
| PL (2) | PL3377483T3 (en) |
| PT (2) | PT3928836T (en) |
| RS (2) | RS62598B1 (en) |
| SA (1) | SA518391588B1 (en) |
| SG (1) | SG11201803627XA (en) |
| SI (2) | SI3928836T1 (en) |
| TW (2) | TWI719078B (en) |
| UA (1) | UA123441C2 (en) |
| WO (1) | WO2017085198A1 (en) |
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| CR20180323A (en) * | 2015-11-20 | 2018-08-06 | Idorsia Pharmaceuticals Ltd | DERIVATIVES OF INDOL N-SUBSTITUTES AS MODULATORS OF PGE2 RECEIVERS |
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| LT3625222T (en) | 2017-05-18 | 2021-11-10 | Idorsia Pharmaceuticals Ltd | PHENYL DERIVATIVES AS PGE2 RECEPTOR MODULATORS |
| CN110621671A (en) | 2017-05-18 | 2019-12-27 | 爱杜西亚药品有限公司 | Benzofuran and benzothiophene derivatives as PGE2 receptor modulators |
| PT3625228T (en) | 2017-05-18 | 2021-09-16 | Idorsia Pharmaceuticals Ltd | Pyrimidine derivatives as pge2 receptor modulators |
| CN109678780A (en) * | 2017-10-19 | 2019-04-26 | 中国石油化工股份有限公司 | A method of preparing 3- alkyl-indol derivative |
| CA3084581A1 (en) | 2017-11-20 | 2019-05-23 | Icahn School Of Medicine At Mount Sinai | Kinase inhibitor compounds and compositions and methods of use |
| EP3735419A4 (en) | 2018-01-05 | 2021-09-15 | Icahn School of Medicine at Mount Sinai | Method of increasing proliferation of pancreatic beta cells, treatment method, and composition |
| AU2019240065A1 (en) | 2018-03-20 | 2020-09-24 | Icahn School Of Medicine At Mount Sinai | Kinase inhibitor compounds and compositions and methods of use |
| US20220064146A1 (en) * | 2018-12-31 | 2022-03-03 | Icahn School Of Medicine At Mount Sinai | Kinase inhibitor compounds and compositions and methods of use |
| EP3693359A1 (en) | 2019-02-08 | 2020-08-12 | Medibiofarma, S.L. | New n-benzyl-2-phenoxybenzamide derivatives as prostaglandin e2 (pge2) receptors modulators |
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