SG11201809342YA - Pyrimidine compounds as jak kinase inhibitors - Google Patents
Pyrimidine compounds as jak kinase inhibitorsInfo
- Publication number
- SG11201809342YA SG11201809342YA SG11201809342YA SG11201809342YA SG11201809342YA SG 11201809342Y A SG11201809342Y A SG 11201809342YA SG 11201809342Y A SG11201809342Y A SG 11201809342YA SG 11201809342Y A SG11201809342Y A SG 11201809342YA SG 11201809342Y A SG11201809342Y A SG 11201809342YA
- Authority
- SG
- Singapore
- Prior art keywords
- california
- international
- compounds
- avenue
- pct
- Prior art date
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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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
- C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
- C07D451/04—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
- C07D451/14—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing 9-azabicyclo [3.3.1] nonane ring systems, e.g. granatane, 2-aza-adamantane; Cyclic acetals thereof
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Dermatology (AREA)
- Epidemiology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic 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 111111101111 0 DOI 010111110101111 0 111 01111101111111010111011111110 HOE lil Organization International Bureau (10) International Publication Number (43) International Publication Date .....0\"\"\" WO 2017/189822 Al 02 November 2017 (02.11.2017) W I PO I PCT (51) International Patent Classification: SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, C07D 451/14 (2006.01) A61K 31/506 (2006.01) TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. C07D 451/04 (2006.01) (84) Designated States (unless otherwise indicated, for every (21) International Application Number: kind of regional protection available): ARIPO (BW, GH, PCT/US2017/029796 GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, (22) International Filing Date: UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, 27 April 2017 (27.04.2017) 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, (25) Filing Language: English MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, (26) Publication Language: English TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG). (30) Priority Data: 62/328,737 28 April 2016 (28.04.2016) US Published: (71) — Applicant: THERAVANCE BIOPHARMA R&D IP, with international search report (Art. 21(3)) LLC [US/US]; 901 Gateway Boulevard, South San Fran- cisco, California 94080 (US). (72) Inventors: HUDSON, Ryan; 1454 Walbrook Drive, San Jose, California 95129 (US). KOZAK, Jennifer; 771 _ Prairie Creek Drive, Pacifica, California 94044 (US). FLEURY, Melissa; 47D Joy Avenue, Brisbane, California — 94005 (US). FATHEREE, Paul R.; 921 Minnesota Street, San Francisco, California 94107 (US). BEAUSOLEIL, Anne-Marie; 600 Brewster Avenue, Apt. 306, Redwood = =_ City, California 94063 (US). PODESTO, Dante D.; 1122 = Trinity Avenue, Modesto, California 95350 (US). HUANG, Xiaojun; 513 Granger Terrace, Sunnyvale, California 94087 (US). = (74) Agent: HAGENAH, Jeffrey A. et al.; THERAVANCE BIOPHARMA US, INC., 901 Gateway Boulevard, South = — _ San Francisco, California 94080 (US). (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, = = (54) Title: PYRIMIDINE COMPOUNDS AS JAK KINASE INHIBITORS _ 1-1 (57) : The invention provides compounds of formula (I): wherein the variables are defined HO R1 in the specification, or a pharmaceutically-acceptable salt thereof,that are inhibitors of JAK kinases. I .4 HN N fl The invention also provides pharmaceutical compositions comprising such compounds, methods of ei ei N , , \ using such compounds to treat gastrointestinal and other inflammatory diseases, and processes and intermediates useful for preparing such compounds. GC 01 HN,_ ; ,,N., N, R 2 GC 1 i 11 • --).„ N 0 O
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662328737P | 2016-04-28 | 2016-04-28 | |
| PCT/US2017/029796 WO2017189822A1 (en) | 2016-04-28 | 2017-04-27 | Pyrimidine compounds as jak kinase inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| SG11201809342YA true SG11201809342YA (en) | 2018-11-29 |
Family
ID=58672793
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SG11201809342YA SG11201809342YA (en) | 2016-04-28 | 2017-04-27 | Pyrimidine compounds as jak kinase inhibitors |
Country Status (20)
| Country | Link |
|---|---|
| US (3) | US10028960B2 (en) |
| EP (1) | EP3433253B1 (en) |
| JP (1) | JP6881879B2 (en) |
| KR (1) | KR102244257B1 (en) |
| CN (1) | CN109071529B (en) |
| AU (1) | AU2017258186B2 (en) |
| BR (1) | BR112018072168A2 (en) |
| CA (1) | CA3020506A1 (en) |
| CL (1) | CL2018003060A1 (en) |
| CO (1) | CO2018011408A2 (en) |
| DK (1) | DK3433253T3 (en) |
| EA (1) | EA035226B1 (en) |
| ES (1) | ES2779880T3 (en) |
| IL (1) | IL262386B (en) |
| MX (1) | MX2018013191A (en) |
| PT (1) | PT3433253T (en) |
| SG (1) | SG11201809342YA (en) |
| TW (1) | TWI726094B (en) |
| WO (1) | WO2017189822A1 (en) |
| ZA (1) | ZA201807179B (en) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3303348B1 (en) | 2015-05-28 | 2019-08-07 | Theravance Biopharma R&D IP, LLC | Naphthyridine compounds as jak kinase inhibitors |
| EP3865481A1 (en) | 2015-11-03 | 2021-08-18 | Topivert Pharma Limited | 4,5,6,7-tetrahydro-1h-imidazo[4,5-c]pyridine and 1,4,5,6,7,8-hexahydroimidazo[4,5-d]azepine derivatives as janus kinase inhibitors |
| WO2017077288A1 (en) | 2015-11-03 | 2017-05-11 | Topivert Pharma Limited | 4,5,6,7-tetrahydro-1h-imidazo[4,5-c]pyridine and 1,4,5,6,7,8-hexahydroimidazo[4,5-d]azepine derivatives as janus kinase inhibitors |
| SG11201809342YA (en) | 2016-04-28 | 2018-11-29 | Theravance Biopharma R&D Ip Llc | Pyrimidine compounds as jak kinase inhibitors |
| SG11202001706RA (en) | 2017-10-27 | 2020-03-30 | Theravance Biopharma R&D Ip Llc | Pyrimidine compound as jak kinase inhibitor |
| EP3810094A1 (en) | 2018-06-20 | 2021-04-28 | Progenity, Inc. | Treatment of a disease of the gastrointestinal tract with a jak or other kinase inhibitor |
| TWI740288B (en) * | 2018-11-27 | 2021-09-21 | 大陸商江蘇豪森藥業集團有限公司 | Nitrogen-containing heteroaromatic derivative regulator, preparation method and application thereof |
| CA3121408A1 (en) * | 2018-11-30 | 2020-06-04 | Jiangsu Hansoh Pharmaceutical Group Co., Ltd. | Heteroaromatic derivatives for use as regulator, preparation method therefor and use thereof |
| TW202106682A (en) | 2019-04-24 | 2021-02-16 | 美商施萬生物製藥研發Ｉｐ有限責任公司 | Ester and carbonate pyrimidine compounds as jak kinase inhibitors |
| AR118767A1 (en) | 2019-04-24 | 2021-10-27 | Theravance Biopharma R&D Ip Llc | PYRIMIDINES SUBSTITUTED AS JAK INHIBITORS AND THEIR USE FOR THE TREATMENT OF INFLAMMATORY OR AUTOIMMUNE SKIN DISEASES |
| CN115867272A (en) * | 2020-05-14 | 2023-03-28 | 施万生物制药研发Ip有限责任公司 | Administration of an enterically selective JAK3 inhibitor |
| CN116390922A (en) * | 2020-10-21 | 2023-07-04 | 南京明德新药研发有限公司 | Selenium heterocyclic compound and application thereof |
| WO2023011359A1 (en) * | 2021-08-05 | 2023-02-09 | 南京明德新药研发有限公司 | Bridged ring compound and use thereof |
| CN113883920B (en) * | 2021-10-25 | 2024-01-23 | 安徽华铂再生资源科技有限公司 | Method for reducing outlet temperature of air cooling tower of air separation device |
| WO2023202706A1 (en) * | 2022-04-21 | 2023-10-26 | 南京明德新药研发有限公司 | Salt form and crystal form of selenium heterocyclic compound and application thereof |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6660731B2 (en) | 2000-09-15 | 2003-12-09 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
| EP2264028A1 (en) | 2000-12-21 | 2010-12-22 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
| EP1841760B1 (en) * | 2004-12-30 | 2011-08-10 | Exelixis, Inc. | Pyrimidine derivatives as kinase modulators and method of use |
| WO2007059299A1 (en) | 2005-11-16 | 2007-05-24 | Vertex Pharmaceuticals Incorporated | Aminopyrimidines useful as kinase inhibitors |
| EP2044063A1 (en) | 2006-06-30 | 2009-04-08 | Astra Zeneca AB | Pyrimidine derivatives useful in the treatment of cancer |
| WO2008005538A2 (en) | 2006-07-05 | 2008-01-10 | Exelixis, Inc. | Methods of using igf1r and abl kinase modulators |
| CN104011050A (en) | 2011-12-22 | 2014-08-27 | 霍夫曼-拉罗奇有限公司 | 2, 4-diamine-pyrimidine derivative as serine/threonine kinase inhibitors |
| WO2015094803A1 (en) * | 2013-12-16 | 2015-06-25 | Calitor Sciences, Llc | Substituted heteroaryl compounds and methods of use |
| NO2721710T3 (en) * | 2014-08-21 | 2018-03-31 | ||
| EP3303348B1 (en) | 2015-05-28 | 2019-08-07 | Theravance Biopharma R&D IP, LLC | Naphthyridine compounds as jak kinase inhibitors |
| SG11201809342YA (en) | 2016-04-28 | 2018-11-29 | Theravance Biopharma R&D Ip Llc | Pyrimidine compounds as jak kinase inhibitors |
-
2017
- 2017-04-27 SG SG11201809342YA patent/SG11201809342YA/en unknown
- 2017-04-27 AU AU2017258186A patent/AU2017258186B2/en not_active Ceased
- 2017-04-27 PT PT177223245T patent/PT3433253T/en unknown
- 2017-04-27 BR BR112018072168-9A patent/BR112018072168A2/en not_active Application Discontinuation
- 2017-04-27 WO PCT/US2017/029796 patent/WO2017189822A1/en active Application Filing
- 2017-04-27 EP EP17722324.5A patent/EP3433253B1/en active Active
- 2017-04-27 TW TW106114033A patent/TWI726094B/en not_active IP Right Cessation
- 2017-04-27 EA EA201892436A patent/EA035226B1/en unknown
- 2017-04-27 CN CN201780026437.4A patent/CN109071529B/en not_active Expired - Fee Related
- 2017-04-27 DK DK17722324.5T patent/DK3433253T3/en active
- 2017-04-27 KR KR1020187034319A patent/KR102244257B1/en active IP Right Grant
- 2017-04-27 CA CA3020506A patent/CA3020506A1/en not_active Abandoned
- 2017-04-27 US US15/498,803 patent/US10028960B2/en not_active Expired - Fee Related
- 2017-04-27 MX MX2018013191A patent/MX2018013191A/en active IP Right Grant
- 2017-04-27 JP JP2018555938A patent/JP6881879B2/en active Active
- 2017-04-27 ES ES17722324T patent/ES2779880T3/en active Active
-
2018
- 2018-06-21 US US16/014,233 patent/US10485803B2/en active Active
- 2018-10-15 IL IL262386A patent/IL262386B/en unknown
- 2018-10-25 CO CONC2018/0011408A patent/CO2018011408A2/en unknown
- 2018-10-26 ZA ZA2018/07179A patent/ZA201807179B/en unknown
- 2018-10-26 CL CL2018003060A patent/CL2018003060A1/en unknown
-
2019
- 2019-10-18 US US16/656,927 patent/US11110095B2/en active Active
Also Published As
| Publication number | Publication date |
|---|---|
| US10485803B2 (en) | 2019-11-26 |
| AU2017258186A1 (en) | 2018-11-15 |
| EA201892436A1 (en) | 2019-04-30 |
| US20200046709A1 (en) | 2020-02-13 |
| DK3433253T3 (en) | 2020-04-06 |
| EP3433253B1 (en) | 2020-02-12 |
| CO2018011408A2 (en) | 2018-11-13 |
| CN109071529B (en) | 2021-08-06 |
| CL2018003060A1 (en) | 2018-12-14 |
| US20180303836A1 (en) | 2018-10-25 |
| KR102244257B1 (en) | 2021-04-26 |
| IL262386A (en) | 2018-11-29 |
| IL262386B (en) | 2021-08-31 |
| US11110095B2 (en) | 2021-09-07 |
| AU2017258186B2 (en) | 2020-09-17 |
| CN109071529A (en) | 2018-12-21 |
| EA035226B1 (en) | 2020-05-19 |
| EP3433253A1 (en) | 2019-01-30 |
| CA3020506A1 (en) | 2017-11-02 |
| ES2779880T3 (en) | 2020-08-20 |
| BR112018072168A2 (en) | 2019-02-12 |
| JP2019514903A (en) | 2019-06-06 |
| US10028960B2 (en) | 2018-07-24 |
| TWI726094B (en) | 2021-05-01 |
| KR20190002591A (en) | 2019-01-08 |
| US20170312280A1 (en) | 2017-11-02 |
| ZA201807179B (en) | 2019-08-28 |
| PT3433253T (en) | 2020-04-30 |
| JP6881879B2 (en) | 2021-06-02 |
| MX2018013191A (en) | 2019-02-13 |
| WO2017189822A1 (en) | 2017-11-02 |
| TW201739747A (en) | 2017-11-16 |
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