JP2015517495A5 - - Google Patents
Download PDFInfo
- 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
Links
- 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 |
| US9663502B2 (en) | 2013-12-20 | 2017-05-30 | Lycera Corporation | 2-Acylamidomethyl and sulfonylamidomethyl benzoxazine carbamates for inhibition of RORgamma activity and the treatment of disease |
| US9809561B2 (en) | 2013-12-20 | 2017-11-07 | Merck Sharp & Dohme Corp. | Tetrahydronaphthyridine, benzoxazine, aza-benzoxazine and related bicyclic compounds 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 |
| EP3092221B1 (en) * | 2014-01-06 | 2018-10-17 | Bristol-Myers Squibb Company | Heterocyclic sulfones as ror-gamma modulators |
| EP3092215B1 (en) * | 2014-01-06 | 2018-10-17 | Bristol-Myers Squibb Company | Cyclohexyl sulfone ror gamma modulators |
| CA2936116A1 (en) * | 2014-01-06 | 2015-07-09 | Bristol-Myers Squibb Company | Pyrrolidinyl sulfone derivatives and their use as ror gamma modulators |
| US9771320B2 (en) | 2014-01-06 | 2017-09-26 | Bristol-Myers Squibb Company | Carbocyclic sulfone RORγ modulators |
| EP3527569B1 (en) | 2014-02-03 | 2021-08-25 | Vitae Pharmaceuticals, LLC | Dihydropyrrolopyridine inhibitors of ror-gamma for use in treating drye eye |
| AU2015222917A1 (en) | 2014-02-27 | 2016-09-15 | Lycera Corporation | Adoptive cellular therapy using an agonist of retinoic acid receptor-related orphan receptor gamma and related therapeutic methods |
| JP6728061B2 (ja) | 2014-05-05 | 2020-07-22 | リセラ・コーポレイションＬｙｃｅｒａ Ｃｏｒｐｏｒａｔｉｏｎ | ＲＯＲγアゴニストとして用いるテトラヒドロキノリンスルホンアミド及び関連化合物ならびに疾患の治療 |
| JP6523337B2 (ja) | 2014-05-05 | 2019-05-29 | リセラ・コーポレイションＬｙｃｅｒａ Ｃｏｒｐｏｒａｔｉｏｎ | ＲＯＲγのアゴニストとしての使用及び疾患治療のためのベンゼンスルホンアミド及び関連化合物 |
| TWI675032B (zh) | 2014-10-14 | 2019-10-21 | 美商維它藥物公司 | ＲＯＲ-γ之二氫吡咯并吡啶抑制劑 |
| US9663515B2 (en) | 2014-11-05 | 2017-05-30 | Vitae Pharmaceuticals, Inc. | Dihydropyrrolopyridine inhibitors of ROR-gamma |
| US9845308B2 (en) | 2014-11-05 | 2017-12-19 | Vitae Pharmaceuticals, Inc. | Isoindoline 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 |
| AU2016257997A1 (en) * | 2015-05-05 | 2017-11-09 | Lycera Corporation | Dihydro-2H-benzo[b][1,4]oxazine sulfonamide and related compounds for use as agonists of RORy and the treatment of disease |
| KR102114536B1 (ko) * | 2015-05-07 | 2020-05-22 | 브리스톨-마이어스 스큅 컴퍼니 | RORγ 조정제로서의 트리시클릭 술폰 |
| CU24487B1 (es) * | 2015-05-15 | 2020-11-30 | Aurigene Discovery Tech Ltd | Compuestos de tetrahidroquinolinona sustituidos como moduladores de gamma ror |
| EP3101006A1 (en) * | 2015-06-05 | 2016-12-07 | Lead Pharma Cel Models IP B.V. | Ror gamma (rory) modulators |
| US10611740B2 (en) | 2015-06-11 | 2020-04-07 | Lycera Corporation | Aryl dihydro-2H-benzo[b][1,4]oxazine sulfonamide and related compounds for use as agonists of RORγ and the treatment of disease |
| ES2856931T3 (es) | 2015-08-05 | 2021-09-28 | Vitae Pharmaceuticals Llc | Moduladores de ROR-gamma |
| WO2017075182A1 (en) | 2015-10-27 | 2017-05-04 | Merck Sharp & Dohme Corp. | Substituted indazole compounds as rorgammat inhibitors and uses thereof |
| US10344000B2 (en) | 2015-10-27 | 2019-07-09 | Merck Sharp & Dohme Corp. | Substituted bicyclic pyrazole compounds as RORgammaT inhibitors and uses thereof |
| WO2017075185A1 (en) | 2015-10-27 | 2017-05-04 | Merck Sharp & Dohme Corp. | Heteroaryl substituted benzoic acids as rorgammat inhibitors and uses thereof |
| EP3868750A1 (en) | 2015-11-20 | 2021-08-25 | Vitae Pharmaceuticals, LLC | Modulators of ror-gamma |
| TW202220968A (zh) | 2016-01-29 | 2022-06-01 | 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 |
| MA49685A (fr) | 2017-07-24 | 2021-04-14 | Vitae Pharmaceuticals Llc | INHIBITEURS DE ROR gamma |
| US11396503B2 (en) | 2017-09-30 | 2022-07-26 | Chia Tai Tianqing Pharmaceutical Group Co., Ltd. | Sulfonyl substituted bicyclic compound which acts as ROR inhibitor |
| CN112334450A (zh) * | 2018-06-18 | 2021-02-05 | 詹森药业有限公司 | 作为RORγt的调节剂的苯基和吡啶基取代的咪唑 |
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 |
| SI1937669T1 (sl) * | 2005-09-01 | 2012-05-31 | Janssen Pharmaceutica Nv | Novi derivati benzopirana kot odpiralci kalijevega kanala |
| 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 AU AU2013259904A patent/AU2013259904A1/en not_active Abandoned
- 2013-05-03 CA CA2871504A patent/CA2871504C/en not_active Expired - Fee Related
- 2013-05-03 KR KR1020147031134A patent/KR20150013500A/ko not_active Ceased
- 2013-05-03 JP JP2015511553A patent/JP6236067B2/ja not_active Expired - Fee Related
- 2013-05-03 MX MX2014013554A patent/MX363350B/es unknown
- 2013-05-03 US US14/398,068 patent/US9266827B2/en active Active
- 2013-05-03 RU RU2014149149A patent/RU2014149149A/ru unknown
- 2013-05-03 IN IN8025DEN2014 patent/IN2014DN08025A/en unknown
- 2013-05-03 BR BR112014028023A patent/BR112014028023A2/pt not_active IP Right Cessation
- 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 EP EP13787211.5A patent/EP2846794B1/en active Active