SG11201811107WA - Heteroaromatic modulators of the retinoid-related orphan receptor gamma - Google Patents
Heteroaromatic modulators of the retinoid-related orphan receptor gammaInfo
- 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
Links
- 125000001072 heteroaryl group Chemical group 0.000 title abstract 3
- 102100023421 Nuclear receptor ROR-gamma Human genes 0.000 title abstract 2
- 108091008773 RAR-related orphan receptors γ Proteins 0.000 title abstract 2
- 125000000217 alkyl group Chemical group 0.000 abstract 9
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 abstract 4
- 150000001875 compounds Chemical class 0.000 abstract 4
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 3
- 125000001188 haloalkyl group Chemical group 0.000 abstract 2
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 125000005843 halogen group Chemical group 0.000 abstract 2
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 2
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 239000000543 intermediate Substances 0.000 abstract 1
- 230000008520 organization Effects 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 102220240796 rs553605556 Human genes 0.000 abstract 1
- 238000002560 therapeutic procedure Methods 0.000 abstract 1
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 or sparfloxacin
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Dermatology (AREA)
- Rheumatology (AREA)
- Epidemiology (AREA)
- Pain & Pain Management (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pulmonology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Transplantation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Hydrogenated Pyridines (AREA)
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)
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)
| Country | Link |
|---|---|
| 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) | MX383770B (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) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BR112019000486A2 (en) * | 2016-07-13 | 2019-04-24 | Leo Pharma A/S | compound, pharmaceutical composition, and method for preventing, treating or ameliorating psoriasis |
| 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 |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| UA95071C2 (en) * | 2005-04-04 | 2011-07-11 | Аб Сьянс | 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 |
| PE20151144A1 (en) | 2012-12-06 | 2015-08-02 | Glaxo Group Ltd | RETINOID RELATED GAMMA RECEPTOR ORPHAN MODULATORS (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 |
| JP6759110B2 (en) * | 2014-05-28 | 2020-09-23 | グラクソスミスクライン、インテレクチュアル、プロパティー、ディベロップメント、リミテッドＧｌａｘｏｓｍｉｔｈｋｌｉｎｅ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ Ｄｅｖｅｌｏｐｍｅｎｔ Ｌｉｍｉｔｅｄ | New compound |
| ES2716966T3 (en) | 2014-05-28 | 2019-06-18 | Glaxosmithkline Ip Dev Ltd | Piperazine derivatives as ROR-gamma modulators |
| BR112019000486A2 (en) * | 2016-07-13 | 2019-04-24 | Leo Pharma A/S | compound, pharmaceutical composition, and method for preventing, treating or ameliorating psoriasis |
-
2017
- 2017-07-11 BR BR112019000486-6A patent/BR112019000486A2/en active Search and Examination
- 2017-07-11 ES ES17737284T patent/ES2834009T3/en active Active
- 2017-07-11 MX MX2019000361A patent/MX383770B/en unknown
- 2017-07-11 EP EP17737284.4A patent/EP3484880B1/en active Active
- 2017-07-11 PT PT177372844T patent/PT3484880T/en unknown
- 2017-07-11 WO PCT/EP2017/067390 patent/WO2018011201A1/en not_active Ceased
- 2017-07-11 AU AU2017294969A patent/AU2017294969B2/en not_active Ceased
- 2017-07-11 MY MYPI2018002824A patent/MY196990A/en unknown
- 2017-07-11 CN CN201780043425.2A patent/CN109476653B/en not_active Expired - Fee Related
- 2017-07-11 SG SG11201811107WA patent/SG11201811107WA/en unknown
- 2017-07-11 KR KR1020197003804A patent/KR102490140B1/en active Active
- 2017-07-11 CA CA3030370A patent/CA3030370A1/en active Pending
- 2017-07-11 DK DK17737284.4T patent/DK3484880T3/en active
- 2017-07-11 RU RU2019103883A patent/RU2771280C2/en active
- 2017-07-11 JP JP2019501569A patent/JP7016344B2/en not_active Expired - Fee Related
- 2017-07-11 UA UAA201901406A patent/UA123330C2/en unknown
- 2017-07-11 US US16/317,655 patent/US10662181B2/en active Active
- 2017-07-11 PL PL17737284T patent/PL3484880T3/en unknown
-
2018
- 2018-12-13 ZA ZA2018/08436A patent/ZA201808436B/en unknown
-
2019
- 2019-01-08 IL IL264141A patent/IL264141B/en unknown
- 2019-01-13 SA SA519400868A patent/SA519400868B1/en unknown
-
2020
- 2020-05-15 US US16/874,961 patent/US10934282B2/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| MX383770B (en) | 2025-03-14 |
| NZ749301A (en) | 2021-03-26 |
| DK3484880T3 (en) | 2020-11-09 |
| US10934282B2 (en) | 2021-03-02 |
| RU2019103883A (en) | 2020-08-13 |
| AU2017294969A1 (en) | 2019-01-17 |
| BR112019000486A2 (en) | 2019-04-24 |
| EP3484880B1 (en) | 2020-09-02 |
| IL264141A (en) | 2019-02-28 |
| CN109476653A (en) | 2019-03-15 |
| RU2019103883A3 (en) | 2020-09-23 |
| US20190284177A1 (en) | 2019-09-19 |
| KR20190026872A (en) | 2019-03-13 |
| PT3484880T (en) | 2020-12-07 |
| US10662181B2 (en) | 2020-05-26 |
| SA519400868B1 (en) | 2022-06-13 |
| WO2018011201A1 (en) | 2018-01-18 |
| CN109476653B (en) | 2022-04-22 |
| JP7016344B2 (en) | 2022-02-04 |
| PL3484880T3 (en) | 2021-04-06 |
| JP2019521137A (en) | 2019-07-25 |
| MX2019000361A (en) | 2019-05-23 |
| EP3484880A1 (en) | 2019-05-22 |
| UA123330C2 (en) | 2021-03-17 |
| US20200291010A1 (en) | 2020-09-17 |
| ES2834009T3 (en) | 2021-06-16 |
| MY196990A (en) | 2023-05-17 |
| AU2017294969B2 (en) | 2021-03-25 |
| RU2771280C2 (en) | 2022-04-29 |
| IL264141B (en) | 2021-09-30 |
| ZA201808436B (en) | 2020-05-27 |
| CA3030370A1 (en) | 2018-01-18 |
| KR102490140B1 (en) | 2023-01-19 |
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