JP2015517495A5 - - Google Patents
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- Publication number
- JP2015517495A5 JP2015517495A5 JP2015511553A JP2015511553A JP2015517495A5 JP 2015517495 A5 JP2015517495 A5 JP 2015517495A5 JP 2015511553 A JP2015511553 A JP 2015511553A JP 2015511553 A JP2015511553 A JP 2015511553A JP 2015517495 A5 JP2015517495 A5 JP 2015517495A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- alkylene
- compound according
- haloalkyl
- halogen
- Prior art date
- Legal status (The legal status 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 status listed.)
- Granted
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- 150000001875 compounds Chemical class 0.000 claims description 32
- 150000003839 salts Chemical class 0.000 claims description 4
- 125000000217 alkyl group Chemical group 0.000 claims 58
- 229910052736 halogen Inorganic materials 0.000 claims 20
- 150000002367 halogens Chemical class 0.000 claims 20
- 125000003545 alkoxy group Chemical group 0.000 claims 18
- 229910052739 hydrogen Inorganic materials 0.000 claims 18
- 239000001257 hydrogen Substances 0.000 claims 18
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 17
- 125000001424 substituent group Chemical group 0.000 claims 16
- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 claims 14
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 12
- 125000006577 C1-C6 hydroxyalkyl group Chemical group 0.000 claims 10
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 10
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 claims 8
- 150000002431 hydrogen Chemical class 0.000 claims 8
- 206010059176 Juvenile idiopathic arthritis Diseases 0.000 claims 6
- 230000000366 juvenile effect Effects 0.000 claims 6
- 239000008194 pharmaceutical composition Substances 0.000 claims 6
- 208000003456 Juvenile Arthritis Diseases 0.000 claims 5
- 201000004681 Psoriasis Diseases 0.000 claims 5
- 201000002215 juvenile rheumatoid arthritis Diseases 0.000 claims 5
- 125000003118 aryl group Chemical group 0.000 claims 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
- 125000000623 heterocyclic group Chemical group 0.000 claims 4
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 4
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 4
- 208000019069 chronic childhood arthritis Diseases 0.000 claims 3
- 208000035475 disorder Diseases 0.000 claims 3
- 125000001188 haloalkyl group Chemical group 0.000 claims 3
- 208000002574 reactive arthritis Diseases 0.000 claims 3
- 206010003253 Arthritis enteropathic Diseases 0.000 claims 2
- 206010003267 Arthritis reactive Diseases 0.000 claims 2
- 206010039710 Scleroderma Diseases 0.000 claims 2
- 206010047115 Vasculitis Diseases 0.000 claims 2
- 125000002947 alkylene group Chemical group 0.000 claims 2
- 125000003710 aryl alkyl group Chemical group 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- 201000001981 dermatomyositis Diseases 0.000 claims 2
- 230000000694 effects Effects 0.000 claims 2
- 230000036566 epidermal hyperplasia Effects 0.000 claims 2
- 125000001072 heteroaryl group Chemical group 0.000 claims 2
- 208000026278 immune system disease Diseases 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 2
- 125000004043 oxo group Chemical group O=* 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 239000012453 solvate Substances 0.000 claims 2
- 125000003107 substituted aryl group Chemical group 0.000 claims 2
- 208000011580 syndromic disease Diseases 0.000 claims 2
- 201000000596 systemic lupus erythematosus Diseases 0.000 claims 2
- -1 —N (R 4 ) (R 5 ) Chemical group 0.000 claims 2
- 208000026872 Addison Disease Diseases 0.000 claims 1
- 206010002556 Ankylosing Spondylitis Diseases 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 206010003827 Autoimmune hepatitis Diseases 0.000 claims 1
- 208000023328 Basedow disease Diseases 0.000 claims 1
- 206010008609 Cholangitis sclerosing Diseases 0.000 claims 1
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 1
- 208000015943 Coeliac disease Diseases 0.000 claims 1
- 206010009900 Colitis ulcerative Diseases 0.000 claims 1
- 208000011231 Crohn disease Diseases 0.000 claims 1
- 201000004624 Dermatitis Diseases 0.000 claims 1
- 206010012438 Dermatitis atopic Diseases 0.000 claims 1
- 206010015278 Erythrodermic psoriasis Diseases 0.000 claims 1
- 206010072579 Granulomatosis with polyangiitis Diseases 0.000 claims 1
- 208000015023 Graves' disease Diseases 0.000 claims 1
- 206010021245 Idiopathic thrombocytopenic purpura Diseases 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 1
- 208000012528 Juvenile dermatomyositis Diseases 0.000 claims 1
- 208000000112 Myalgia Diseases 0.000 claims 1
- 208000020410 Psoriasis-related juvenile idiopathic arthritis Diseases 0.000 claims 1
- 201000001263 Psoriatic Arthritis Diseases 0.000 claims 1
- 208000036824 Psoriatic arthropathy Diseases 0.000 claims 1
- 206010037549 Purpura Diseases 0.000 claims 1
- 241001672981 Purpura Species 0.000 claims 1
- 206010037575 Pustular psoriasis Diseases 0.000 claims 1
- 108091008773 RAR-related orphan receptors γ Proteins 0.000 claims 1
- 208000012322 Raynaud phenomenon Diseases 0.000 claims 1
- 208000033464 Reiter syndrome Diseases 0.000 claims 1
- 208000034189 Sclerosis Diseases 0.000 claims 1
- 208000021386 Sjogren Syndrome Diseases 0.000 claims 1
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 1
- 201000006704 Ulcerative Colitis Diseases 0.000 claims 1
- 208000024340 acute graft versus host disease Diseases 0.000 claims 1
- 206010003230 arteritis Diseases 0.000 claims 1
- 206010003246 arthritis Diseases 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- 201000008937 atopic dermatitis Diseases 0.000 claims 1
- 201000003710 autoimmune thrombocytopenic purpura Diseases 0.000 claims 1
- 210000000988 bone and bone Anatomy 0.000 claims 1
- 210000000845 cartilage Anatomy 0.000 claims 1
- 230000015556 catabolic process Effects 0.000 claims 1
- 201000010415 childhood type dermatomyositis Diseases 0.000 claims 1
- 201000001352 cholecystitis Diseases 0.000 claims 1
- 208000017760 chronic graft versus host disease Diseases 0.000 claims 1
- 208000025302 chronic primary adrenal insufficiency Diseases 0.000 claims 1
- 238000006731 degradation reaction Methods 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 201000004990 juvenile ankylosing spondylitis Diseases 0.000 claims 1
- 210000004698 lymphocyte Anatomy 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 206010028417 myasthenia gravis Diseases 0.000 claims 1
- 201000008482 osteoarthritis Diseases 0.000 claims 1
- 230000001717 pathogenic effect Effects 0.000 claims 1
- 201000006292 polyarteritis nodosa Diseases 0.000 claims 1
- 230000001185 psoriatic effect Effects 0.000 claims 1
- 201000000306 sarcoidosis Diseases 0.000 claims 1
- 208000010157 sclerosing cholangitis Diseases 0.000 claims 1
- 230000001732 thrombotic effect Effects 0.000 claims 1
- 0 *C(CC(C1=C2*)S(C/C3=C\CCC/C=C/C3)(=*)=O)OC1=I**=C2N(*)I* Chemical compound *C(CC(C1=C2*)S(C/C3=C\CCC/C=C/C3)(=*)=O)OC1=I**=C2N(*)I* 0.000 description 3
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261644143P | 2012-05-08 | 2012-05-08 | |
| US61/644,143 | 2012-05-08 | ||
| PCT/US2013/039422 WO2013169588A1 (en) | 2012-05-08 | 2013-05-03 | BICYCLIC SULFONE COMPOUNDS FOR INHIBITION OF RORy ACTIVITY AND THE TREATMENT OF DISEASE |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015517495A JP2015517495A (ja) | 2015-06-22 |
| JP2015517495A5 true JP2015517495A5 (enExample) | 2017-11-02 |
| JP6236067B2 JP6236067B2 (ja) | 2017-11-22 |
Family
ID=49551169
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015511553A Expired - Fee Related JP6236067B2 (ja) | 2012-05-08 | 2013-05-03 | ＲＯＲγ活性を阻害し疾患を治療するための二環式スルホン化合物 |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US9266827B2 (enExample) |
| EP (1) | EP2846794B1 (enExample) |
| JP (1) | JP6236067B2 (enExample) |
| KR (1) | KR20150013500A (enExample) |
| CN (1) | CN104284657A (enExample) |
| AU (1) | AU2013259904A1 (enExample) |
| BR (1) | BR112014028023A2 (enExample) |
| CA (1) | CA2871504C (enExample) |
| IN (1) | IN2014DN08025A (enExample) |
| MX (1) | MX363350B (enExample) |
| RU (1) | RU2014149149A (enExample) |
| WO (1) | WO2013169588A1 (enExample) |
Families Citing this family (37)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX367341B (es) | 2012-05-08 | 2019-08-14 | Merck Sharp & Dohme | Tetrahidronaftiridina y compuestos biciclicos relacionados para la inhibicion de la actividad de rorgamma y el tratamiento de enfermedades. |
| WO2013169864A2 (en) | 2012-05-08 | 2013-11-14 | Lycera Corporation | TETRAHYDRO[1,8]NAPHTHYRIDINE SULFONAMIDE AND RELATED COMPOUNDS FOR USE AS AGONISTS OF RORƴ AND THE TREATMENT OF DISEASE |
| WO2015095788A1 (en) | 2013-12-20 | 2015-06-25 | Merck Sharp & Dohme Corp. | 2-ACYLAMIDOMETHYL AND SULFONYLAMIDOMETHYL BENZOXAZINE CARBAMATES FOR INHIBITION OF RORgamma ACTIVITY AND THE TREATMENT OF DISEASE |
| WO2015095792A1 (en) | 2013-12-20 | 2015-06-25 | Merck Sharp & Dohme Corp. | Carbamate benzoxaxine propionic acids and acid derivatives for modulation of rorgamma activity and the treatment of disease |
| WO2015095795A1 (en) | 2013-12-20 | 2015-06-25 | Merck Sharp & Dohme Corp. | TETRAHYDRONAPHTHYRIDINE, BENZOXAZINE, AZA-BENZOXAZINE, AND RELATED BICYCLIC COMPOUNDS FOR INHIBITION OF RORgamma ACTIVITY AND THE TREATMENT OF DISEASE |
| WO2015103509A1 (en) * | 2014-01-06 | 2015-07-09 | Bristol-Myers Squibb Company | Pyrrolidinyl sulfone derivatives and their use as ror gamma modulators |
| EP3092221B1 (en) * | 2014-01-06 | 2018-10-17 | Bristol-Myers Squibb Company | Heterocyclic sulfones as ror-gamma modulators |
| US9771320B2 (en) | 2014-01-06 | 2017-09-26 | Bristol-Myers Squibb Company | Carbocyclic sulfone RORγ modulators |
| ES2704460T3 (es) * | 2014-01-06 | 2019-03-18 | Bristol Myers Squibb Co | Moduladores de ROR gamma de ciclohexilsulfona |
| JP6466461B2 (ja) | 2014-02-03 | 2019-02-06 | ヴァイティー ファーマシューティカルズ，インコーポレイテッド | Ｒｏｒガンマのジヒドロピロロピリジン阻害剤 |
| CA2939305A1 (en) | 2014-02-27 | 2015-09-03 | Lycera Corporation | Adoptive cellular therapy using an agonist of retinoic acid receptor-related orphan receptor gamma & related therapeutic methods |
| EP3140291A4 (en) * | 2014-05-05 | 2018-01-10 | Lycera Corporation | Tetrahydroquinoline sulfonamide and related compounds for use as agonists of rory and the treatment of disease |
| EP3209641A4 (en) | 2014-05-05 | 2018-06-06 | Lycera Corporation | Benzenesulfonamido and related compounds for use as agonists of ror and the treatement of disease |
| EP3207043B3 (en) | 2014-10-14 | 2019-10-02 | Vitae Pharmaceuticals, LLC | Dihydropyrrolopyridine inhibitors of ror-gamma |
| US9845308B2 (en) | 2014-11-05 | 2017-12-19 | Vitae Pharmaceuticals, Inc. | Isoindoline inhibitors of ROR-gamma |
| US9663515B2 (en) | 2014-11-05 | 2017-05-30 | Vitae Pharmaceuticals, Inc. | Dihydropyrrolopyridine inhibitors of ROR-gamma |
| WO2016130818A1 (en) | 2015-02-11 | 2016-08-18 | Merck Sharp & Dohme Corp. | SUBSTITUTED PYRAZOLE COMPOUNDS AS RORgammaT INHIBITORS AND USES THEREOF |
| US10039727B2 (en) | 2015-04-21 | 2018-08-07 | Commissariat A L'energie Atomique Et Aux Energies Alternatives | Adamantane or pinene derivatives for use in the treatment of chlamydiales infections |
| JP2018515491A (ja) * | 2015-05-05 | 2018-06-14 | リセラ・コーポレイションＬｙｃｅｒａ Ｃｏｒｐｏｒａｔｉｏｎ | ＲＯＲγの作動薬及び疾患の療法として使用するジヒドロ−２Ｈ−ベンゾ［ｂ］［１，４］オキサジンスルホンアミド及び関連化合物 |
| WO2016179460A1 (en) * | 2015-05-07 | 2016-11-10 | Bristol-Myers Squibb Company | Tricyclic sulfones as rorϒ modulators |
| EP3845526A1 (en) | 2015-05-15 | 2021-07-07 | Aurigene Discovery Technologies Limited | Method for the preparation of tetrahydroquinolinone compounds having ror-gamma modulating activity |
| EP3101006A1 (en) * | 2015-06-05 | 2016-12-07 | Lead Pharma Cel Models IP B.V. | Ror gamma (rory) modulators |
| CA2987289A1 (en) | 2015-06-11 | 2016-12-15 | Lycera Corporation | Aryl dihydro-2h-benzo[b][1,4]oxazine sulfonamide and related compounds for use as agonists of ror.gamma. and the treatment of disease |
| DK3331876T3 (da) | 2015-08-05 | 2021-01-11 | Vitae Pharmaceuticals Llc | Modulators of ror-gamma |
| EP3368535B1 (en) | 2015-10-27 | 2020-12-02 | Merck Sharp & Dohme Corp. | Heteroaryl substituted benzoic acids as rorgammat inhibitors and uses thereof |
| JP2018531957A (ja) | 2015-10-27 | 2018-11-01 | メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋ Ｓｈａｒｐ ＆ Ｄｏｈｍｅ Ｃｏｒｐ． | ＲＯＲγＴ阻害薬としての置換二環式ピラゾール化合物及びその使用 |
| JP2018535958A (ja) | 2015-10-27 | 2018-12-06 | メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋ Ｓｈａｒｐ ＆ Ｄｏｈｍｅ Ｃｏｒｐ． | ＲＯＲγＴ阻害薬としての置換インダゾール化合物及びその使用 |
| EP3377482B1 (en) | 2015-11-20 | 2021-05-12 | Vitae Pharmaceuticals, LLC | Modulators of ror-gamma |
| TWI757266B (zh) | 2016-01-29 | 2022-03-11 | 美商維它藥物有限責任公司 | ＲＯＲ－γ調節劑 |
| US9481674B1 (en) | 2016-06-10 | 2016-11-01 | Vitae Pharmaceuticals, Inc. | Dihydropyrrolopyridine inhibitors of ROR-gamma |
| FR3063079B1 (fr) | 2017-02-17 | 2019-03-22 | Galderma Research & Development | Derives sulfonamides hydroxyles en tant qu'agonistes inverses du recepteur gamma orphelin associe aux retinoides ror gamma (t) |
| CN108503584B (zh) * | 2017-02-27 | 2021-05-04 | 复旦大学 | 一种1,2,3,4-四氢喹啉磺酰胺类化合物及其应用 |
| FR3065000A1 (fr) | 2017-04-06 | 2018-10-12 | Galderma Research & Development | Derives pyrazoles en tant qu'agonistes inverses du recepteur gamma orphelin associe aux retinoides ror gamma (t) |
| WO2019018975A1 (en) | 2017-07-24 | 2019-01-31 | Vitae Pharmaceuticals, Inc. | INHIBITORS OF ROR GAMMA |
| BR112020001246A2 (pt) | 2017-07-24 | 2020-07-21 | Vitae Pharmaceuticals, Llc | inibidores de rory |
| WO2019063015A1 (zh) * | 2017-09-30 | 2019-04-04 | 正大天晴药业集团股份有限公司 | 作为RORγ抑制剂的磺酰基取代的双环化合物 |
| ES2929140T3 (es) * | 2018-06-18 | 2022-11-25 | Janssen Pharmaceutica Nv | Imidazoles sustituidos con fenilo y piridinilo como moduladores de RORgammat |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP3414433B2 (ja) * | 1993-03-01 | 2003-06-09 | 日本化薬株式会社 | 電子写真用トナー |
| ES2379098T3 (es) * | 2005-09-01 | 2012-04-20 | Janssen Pharmaceutica Nv | Derivados de benzopirano novedosos como abridores del canal de potasio |
| US7799933B2 (en) | 2006-12-21 | 2010-09-21 | Hoffman-La Roche Inc. | Sulfonamide derivatives |
| WO2010017827A1 (en) | 2008-08-14 | 2010-02-18 | European Molecular Biology Laboratory | 6-substituted 1-sulfonyl-2, 3-dihydro-indole derivatives for the treatment of proliferative diseases |
| EP2181710A1 (en) * | 2008-10-28 | 2010-05-05 | Phenex Pharmaceuticals AG | Ligands for modulation of orphan receptor-gamma (NR1F3) activity |
| CN101580874B (zh) * | 2009-03-17 | 2012-03-21 | 江苏大学 | 一种人外周血RORγt转录本荧光定量PCR检测方法 |
-
2013
- 2013-05-03 IN IN8025DEN2014 patent/IN2014DN08025A/en unknown
- 2013-05-03 US US14/398,068 patent/US9266827B2/en active Active
- 2013-05-03 AU AU2013259904A patent/AU2013259904A1/en not_active Abandoned
- 2013-05-03 CN CN201380023864.9A patent/CN104284657A/zh active Pending
- 2013-05-03 WO PCT/US2013/039422 patent/WO2013169588A1/en not_active Ceased
- 2013-05-03 CA CA2871504A patent/CA2871504C/en not_active Expired - Fee Related
- 2013-05-03 JP JP2015511553A patent/JP6236067B2/ja not_active Expired - Fee Related
- 2013-05-03 KR KR1020147031134A patent/KR20150013500A/ko not_active Ceased
- 2013-05-03 BR BR112014028023A patent/BR112014028023A2/pt not_active IP Right Cessation
- 2013-05-03 MX MX2014013554A patent/MX363350B/es unknown
- 2013-05-03 EP EP13787211.5A patent/EP2846794B1/en active Active
- 2013-05-03 RU RU2014149149A patent/RU2014149149A/ru unknown
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