SG11201811107WA - Heteroaromatic modulators of the retinoid-related orphan receptor gamma - Google Patents

Heteroaromatic modulators of the retinoid-related orphan receptor gamma

Info

Publication number
SG11201811107WA
SG11201811107WA SG11201811107WA SG11201811107WA SG11201811107WA SG 11201811107W A SG11201811107W A SG 11201811107WA SG 11201811107W A SG11201811107W A SG 11201811107WA SG 11201811107W A SG11201811107W A SG 11201811107WA SG 11201811107W A SG11201811107W A SG 11201811107WA
Authority
SG
Singapore
Prior art keywords
alkyl
cycloalkyl
ballerup
membered
international
Prior art date
Application number
SG11201811107WA
Inventor
Alan Stuart Jessiman
Patrick Stephen Johnson
Kristoffer Maansson
Morten Dahl Sørensen
Original Assignee
Leo Pharma As
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 Leo Pharma As filed Critical Leo Pharma As
Publication of SG11201811107WA publication Critical patent/SG11201811107WA/en

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Classifications

    • 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
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • 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
    • 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
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • 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
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/04—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • 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

Abstract

INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 18 January 2018 (18.01.2018) W I PO I PCT omit VIII °nolo III m OH VIII O II oimIE (10) International Publication Number WO 2018/011201 Al (51) International Patent Classification: CO7D 413/14 (2006.01) CO7D 417/14 (2006.01) CO7D 241/04 (2006.01) A61K 31/496 (2006.01) C07D 413/12 (2006.01) A61P 17/06 (2006.01) (21) International Application Number: PCT/EP2017/067390 (22) International Filing Date: (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 16020268.5 13 July 2016 (13.07.2016) EP (71) Applicant: LEO PHARMA A/S [DK/DK]; Industriparken 55, 2750 Ballerup (DK). (72) Inventors: JESSIMAN, Alan Stuart; c/o LEO Pharma A/S, Industriparken 55, 2750 Ballerup (DK). JOHNSON, Patrick Stephen; c/o LEO Pharma A/S, Industriparken 55, 2750 Ballerup (DK). MAANSSON, Kristoffer; c/o LEO Pharma A/S, Industriparken 55, 2750 Ballerup (DK). SORENSEN, Morten Dahl; c/o LEO Pharma A/S, Indus- triparken 55, 2750 Ballerup (DK). (74) Agent: LEO PHARMA A/S; Patent Department, Industri- parken 55, 2750 Ballerup (DK). (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, JO, 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). 11 July 2017 (11.07.2017) Published: — with international search report (Art. 21(3)) W O 20 18/0 1120 1 Al (54) Title: HETEROAROMATIC MODULATORS OF THE RETINOID-RELATED ORPHAN RECEPTOR GAMMA (57) : The present invention relates to a compound according to gen- es R3 eral formula (I) wherein X represents N or CH; R1 is -CN, (Ci-C6)alkyl, (C3- C 7 )cycloalkyl, (3-7 membered)heterocycloalkyl, (5-6 membered)heteroaryl, (C 3 - X- N C7)cycloalkyl(Ci-C4)alkyl, (3-7 membered)heterocycloalkyl-(Ci-C4)alkyl or (5-6 membered)heteroaryl- (Ci-C4)alkyl; R2 is halogen, cyano, (Ci-C4)alkyl or (C3- C 7 )cycloalkyl; R3 is halogen, cyano, (Ci-C4)alkyl, (Ci-C4)haloalkyl or (C3- C7)cycloalkyl; R4 is (Ci-C4)alkyl or (Ci-C4)haloalkyl; R5 is (Ci-C6)alkyl, (C3- C7)cycloalkyl, (Ci-C6)alkyl-(C3-C7)cycloalkyl, (C3-C7)cycloalkyl-(Ci-C6)alkyl, (3-7 membered)heterocycloalkyl, phenyl, (5-6 membered)heteroaryl or -0R a . The invention further relates to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds and to intermediates for preparation of said compounds. (I)
SG11201811107WA 2016-07-13 2017-07-11 Heteroaromatic modulators of the retinoid-related orphan receptor gamma SG11201811107WA (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP16020268 2016-07-13
PCT/EP2017/067390 WO2018011201A1 (en) 2016-07-13 2017-07-11 Heteroaromatic modulators of the retinoid-related orphan receptor gamma

Publications (1)

Publication Number Publication Date
SG11201811107WA true SG11201811107WA (en) 2019-01-30

Family

ID=56511303

Family Applications (1)

Application Number Title Priority Date Filing Date
SG11201811107WA SG11201811107WA (en) 2016-07-13 2017-07-11 Heteroaromatic modulators of the retinoid-related orphan receptor gamma

Country Status (21)

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US (2) US10662181B2 (en)
EP (1) EP3484880B1 (en)
JP (1) JP7016344B2 (en)
KR (1) KR102490140B1 (en)
CN (1) CN109476653B (en)
AU (1) AU2017294969B2 (en)
BR (1) BR112019000486A2 (en)
CA (1) CA3030370A1 (en)
DK (1) DK3484880T3 (en)
ES (1) ES2834009T3 (en)
IL (1) IL264141B (en)
MX (1) MX2019000361A (en)
MY (1) MY196990A (en)
PL (1) PL3484880T3 (en)
PT (1) PT3484880T (en)
RU (1) RU2771280C2 (en)
SA (1) SA519400868B1 (en)
SG (1) SG11201811107WA (en)
UA (1) UA123330C2 (en)
WO (1) WO2018011201A1 (en)
ZA (1) ZA201808436B (en)

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX2019000361A (en) * 2016-07-13 2019-05-23 Leo Pharma As Heteroaromatic modulators of the retinoid-related orphan receptor gamma.
CN111825654A (en) * 2019-04-19 2020-10-27 北京酷瓴生物技术有限公司 Phenylmethylene piperidine derivatives, preparation method, intermediates and uses thereof
CN112898292A (en) * 2019-12-03 2021-06-04 微境生物医药科技(上海)有限公司 Novel aurora kinase inhibitor and use thereof

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CS244821B2 (en) * 1983-06-16 1986-08-14 Boehringer Ingelheim Ltd Production method of new substituted phenylalkyl(piperazinyl or homopiperazinyle)-prpylureas or thioureas
WO2004073612A2 (en) 2003-02-13 2004-09-02 Merck & Co. Inc. Estrogen receptor modulators
FR2879381B1 (en) 2004-12-15 2008-12-26 Thales Sa QUANTUM QUANTUM DISTRIBUTION SYSTEM OF CONTINUOUSLY VARIABLE ENCRYPTION KEY
EP1874305B1 (en) * 2005-04-04 2014-08-27 AB Science Substituted oxazole derivatives and their use as tyrosine kinase inhibitors
EP2511275A1 (en) 2011-04-12 2012-10-17 Bioprojet Novel piperidinyl monocarboxylic acids as S1P1 receptor agonists
LT2928885T (en) * 2012-12-06 2017-05-25 Glaxo Group Limited Modulators of the retinoid-related orphan receptor gamma (ror-gamma) for use in the treatment of autoimmune and inflammatory diseases
CA2929194A1 (en) * 2013-11-05 2015-05-14 F. Hoffmann-La Roche Ag 5,6,7,8-tetrahydro-5,8-methanocinnoline derivatives as rorc modulators for the treatment of autoimmune diseases
KR20170012388A (en) * 2014-05-28 2017-02-02 글락소스미스클라인 인털렉츄얼 프로퍼티 디벨로프먼트 리미티드 Novel compounds
KR20170008852A (en) * 2014-05-28 2017-01-24 글락소스미스클라인 인털렉츄얼 프로퍼티 디벨로프먼트 리미티드 Novel compounds
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JP2019521137A (en) 2019-07-25
AU2017294969B2 (en) 2021-03-25
BR112019000486A2 (en) 2019-04-24
KR102490140B1 (en) 2023-01-19
PL3484880T3 (en) 2021-04-06
EP3484880A1 (en) 2019-05-22
NZ749301A (en) 2021-03-26
IL264141B (en) 2021-09-30
AU2017294969A1 (en) 2019-01-17
CA3030370A1 (en) 2018-01-18
US20200291010A1 (en) 2020-09-17
US10662181B2 (en) 2020-05-26
SA519400868B1 (en) 2022-06-13
US20190284177A1 (en) 2019-09-19
EP3484880B1 (en) 2020-09-02
CN109476653A (en) 2019-03-15
ZA201808436B (en) 2020-05-27
MX2019000361A (en) 2019-05-23
ES2834009T3 (en) 2021-06-16
RU2019103883A3 (en) 2020-09-23
JP7016344B2 (en) 2022-02-04
RU2771280C2 (en) 2022-04-29
PT3484880T (en) 2020-12-07
WO2018011201A1 (en) 2018-01-18
KR20190026872A (en) 2019-03-13
DK3484880T3 (en) 2020-11-09
MY196990A (en) 2023-05-17
RU2019103883A (en) 2020-08-13
CN109476653B (en) 2022-04-22
US10934282B2 (en) 2021-03-02
UA123330C2 (en) 2021-03-17
IL264141A (en) 2019-02-28

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