SG11201809342YA - Pyrimidine compounds as jak kinase inhibitors - Google Patents

Pyrimidine compounds as jak kinase inhibitors

Info

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
Application number
SG11201809342YA
Inventor
Ryan Hudson
Jennifer Kozak
Melissa Fleury
Paul R Fatheree
Anne-Marie Beausoleil
Dante D Podesto
Xiaojun Huang
Original Assignee
Theravance Biopharma R&D Ip Llc
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 Theravance Biopharma R&D Ip Llc filed Critical Theravance Biopharma R&D Ip Llc
Publication of SG11201809342YA publication Critical patent/SG11201809342YA/en

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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

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
SG11201809342YA 2016-04-28 2017-04-27 Pyrimidine compounds as jak kinase inhibitors SG11201809342YA (en)

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)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT3303348T (en) 2015-05-28 2019-11-15 Theravance Biopharma R&D Ip Llc Naphthyridine compounds as jak kinase inhibitors
DK3371185T3 (en) 2015-11-03 2020-11-30 Topivert Pharma Ltd 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 CHINASE INHIBITORS
EP3712152B1 (en) 2015-11-03 2021-01-13 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
US10028960B2 (en) 2016-04-28 2018-07-24 Theravance Biopharma R&D Ip, Llc Pyrimidine compounds as JAK kinase inhibitors
JP7218364B2 (en) 2017-10-27 2023-02-06 セラヴァンス バイオファーマ アール＆ディー アイピー， エルエルシー Pyrimidine compounds as JAK kinase inhibitors
WO2019246273A1 (en) 2018-06-20 2019-12-26 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
TWI741423B (en) * 2018-11-30 2021-10-01 大陸商江蘇豪森藥業集團有限公司 Heteroaromatic derivative regulator, its preparation method and application
AR118768A1 (en) 2019-04-24 2021-10-27 Theravance Biopharma R&D Ip Llc PYRIMIDINE DERIVATIVES AS INHIBITORS OF JAK KINASES
US11439641B2 (en) 2019-04-24 2022-09-13 Theravance Biopharma R&D Ip, Llc Pyrimidine JAK inhibitors for the treatment of skin diseases
JP2023528239A (en) * 2020-05-14 2023-07-04 テラバンス バイオファーマ アールアンドディー アイピー リミテッド ライアビリティ カンパニー Administration of intestinal selective JAK3 inhibitor
WO2022083687A1 (en) * 2020-10-21 2022-04-28 南京明德新药研发有限公司 Selenium heterocyclic compounds 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)

* Cited by examiner, † Cited by third party
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
BR0116411A (en) 2000-12-21 2003-11-11 Vertex Pharma 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
CA2629781A1 (en) 2005-11-16 2007-05-24 Vertex Pharmaceuticals Incorporated Aminopyrimidines useful as kinase inhibitors
AU2007263655A1 (en) 2006-06-30 2008-01-03 Astrazeneca Ab Pyrimidine derivatives useful in the treatment of cancer
US8222256B2 (en) 2006-07-05 2012-07-17 Exelixis, Inc. Methods of using IGFIR 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
PT3303348T (en) 2015-05-28 2019-11-15 Theravance Biopharma R&D Ip Llc Naphthyridine compounds as jak kinase inhibitors
US10028960B2 (en) * 2016-04-28 2018-07-24 Theravance Biopharma R&D Ip, Llc Pyrimidine compounds as JAK kinase inhibitors

Also Published As

Publication number Publication date
AU2017258186B2 (en) 2020-09-17
US11110095B2 (en) 2021-09-07
US20180303836A1 (en) 2018-10-25
PT3433253T (en) 2020-04-30
CA3020506A1 (en) 2017-11-02
ZA201807179B (en) 2019-08-28
IL262386B (en) 2021-08-31
EP3433253B1 (en) 2020-02-12
US10028960B2 (en) 2018-07-24
CL2018003060A1 (en) 2018-12-14
EA201892436A1 (en) 2019-04-30
WO2017189822A1 (en) 2017-11-02
EA035226B1 (en) 2020-05-19
DK3433253T3 (en) 2020-04-06
KR20190002591A (en) 2019-01-08
AU2017258186A1 (en) 2018-11-15
JP6881879B2 (en) 2021-06-02
TW201739747A (en) 2017-11-16
CO2018011408A2 (en) 2018-11-13
KR102244257B1 (en) 2021-04-26
ES2779880T3 (en) 2020-08-20
US20200046709A1 (en) 2020-02-13
IL262386A (en) 2018-11-29
JP2019514903A (en) 2019-06-06
CN109071529B (en) 2021-08-06
TWI726094B (en) 2021-05-01
US10485803B2 (en) 2019-11-26
EP3433253A1 (en) 2019-01-30
BR112018072168A2 (en) 2019-02-12
CN109071529A (en) 2018-12-21
MX2018013191A (en) 2019-02-13
US20170312280A1 (en) 2017-11-02

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