JP2016532715A5 - - Google Patents
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- Publication number
- JP2016532715A5 JP2016532715A5 JP2016540455A JP2016540455A JP2016532715A5 JP 2016532715 A5 JP2016532715 A5 JP 2016532715A5 JP 2016540455 A JP2016540455 A JP 2016540455A JP 2016540455 A JP2016540455 A JP 2016540455A JP 2016532715 A5 JP2016532715 A5 JP 2016532715A5
- Authority
- JP
- Japan
- Prior art keywords
- optionally substituted
- bicyclic
- alkyl
- monocyclic
- membered
- 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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- 125000002950 monocyclic group Chemical group 0.000 claims 75
- 125000002619 bicyclic group Chemical group 0.000 claims 68
- 125000000753 cycloalkyl group Chemical group 0.000 claims 15
- 150000003839 salts Chemical class 0.000 claims 14
- 150000001875 compounds Chemical class 0.000 claims 13
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 12
- 125000003118 aryl group Chemical group 0.000 claims 10
- 125000005843 halogen group Chemical group 0.000 claims 10
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 9
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 8
- 125000001072 heteroaryl group Chemical group 0.000 claims 8
- 125000001424 substituent group Chemical group 0.000 claims 8
- -1 Oxapyrrolidinyl Chemical group 0.000 claims 6
- 125000000217 alkyl group Chemical group 0.000 claims 6
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 6
- 229910052717 sulfur Inorganic materials 0.000 claims 5
- 125000005059 halophenyl group Chemical group 0.000 claims 4
- 229910052760 oxygen Inorganic materials 0.000 claims 4
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 3
- 125000005842 heteroatom Chemical group 0.000 claims 3
- 229910052757 nitrogen Inorganic materials 0.000 claims 3
- 125000004043 oxo group Chemical group O=* 0.000 claims 3
- 125000003830 C1- C4 alkylcarbonylamino group Chemical group 0.000 claims 2
- 125000003342 alkenyl group Chemical group 0.000 claims 2
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims 2
- 125000004802 cyanophenyl group Chemical group 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 208000030159 metabolic disease Diseases 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 239000012453 solvate Substances 0.000 claims 2
- 125000006624 (C1-C6) alkoxycarbonylamino group Chemical group 0.000 claims 1
- 125000006650 (C2-C4) alkynyl group Chemical group 0.000 claims 1
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 1
- 208000023275 Autoimmune disease Diseases 0.000 claims 1
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims 1
- 150000001204 N-oxides Chemical class 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 125000004949 alkyl amino carbonyl amino group Chemical group 0.000 claims 1
- 125000004457 alkyl amino carbonyl group Chemical group 0.000 claims 1
- 125000004448 alkyl carbonyl group Chemical group 0.000 claims 1
- 125000005196 alkyl carbonyloxy group Chemical group 0.000 claims 1
- 208000026935 allergic disease Diseases 0.000 claims 1
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 claims 1
- 125000004104 aryloxy group Chemical group 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- 125000002393 azetidinyl group Chemical group 0.000 claims 1
- 125000001584 benzyloxycarbonyl group Chemical group C(=O)(OCC1=CC=CC=C1)* 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 1
- 125000002433 cyclopentenyl group Chemical group C1(=CCCC1)* 0.000 claims 1
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000016097 disease of metabolism Diseases 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000001188 haloalkyl group Chemical group 0.000 claims 1
- 125000005222 heteroarylaminocarbonyl group Chemical group 0.000 claims 1
- 125000005223 heteroarylcarbonyl group Chemical group 0.000 claims 1
- 150000004677 hydrates Chemical class 0.000 claims 1
- 229910052739 hydrogen Inorganic materials 0.000 claims 1
- ORTFAQDWJHRMNX-UHFFFAOYSA-N hydroxidooxidocarbon(.) Chemical group O[C]=O ORTFAQDWJHRMNX-UHFFFAOYSA-N 0.000 claims 1
- 150000008624 imidazolidinones Chemical class 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 125000002757 morpholinyl group Chemical group 0.000 claims 1
- ZFLIKDUSUDBGCD-UHFFFAOYSA-N parabanic acid Chemical class O=C1NC(=O)C(=O)N1 ZFLIKDUSUDBGCD-UHFFFAOYSA-N 0.000 claims 1
- UYWQUFXKFGHYNT-UHFFFAOYSA-N phenylmethyl ester of formic acid Natural products O=COCC1=CC=CC=C1 UYWQUFXKFGHYNT-UHFFFAOYSA-N 0.000 claims 1
- 125000004193 piperazinyl group Chemical group 0.000 claims 1
- 125000003386 piperidinyl group Chemical group 0.000 claims 1
- NDGRWYRVNANFNB-UHFFFAOYSA-N pyrazolidin-3-one Chemical class O=C1CCNN1 NDGRWYRVNANFNB-UHFFFAOYSA-N 0.000 claims 1
- 125000003072 pyrazolidinyl group Chemical group 0.000 claims 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 1
- 125000003107 substituted aryl group Chemical group 0.000 claims 1
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims 1
- 150000004867 thiadiazoles Chemical class 0.000 claims 1
- 125000001544 thienyl group Chemical group 0.000 claims 1
- 0 *C(*1*C1)C(C(*)*c1cc(C(*)(*)*)ccc11)N1S(*)(=O)=O Chemical compound *C(*1*C1)C(C(*)*c1cc(C(*)(*)*)ccc11)N1S(*)(=O)=O 0.000 description 1
- XRKJOVOGIOIHOQ-ALCCZGGFSA-N CC(N1CC/C=C\CCCCCCC1)=O Chemical compound CC(N1CC/C=C\CCCCCCC1)=O XRKJOVOGIOIHOQ-ALCCZGGFSA-N 0.000 description 1
- BXOFMBYDOREPNM-UHFFFAOYSA-N CC1=CC2SC=NC2C=C1 Chemical compound CC1=CC2SC=NC2C=C1 BXOFMBYDOREPNM-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361875220P | 2013-09-09 | 2013-09-09 | |
| US61/875,220 | 2013-09-09 | ||
| PCT/US2014/054489 WO2015035278A1 (en) | 2013-09-09 | 2014-09-08 | RORγ MODULATORS |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016532715A JP2016532715A (ja) | 2016-10-20 |
| JP2016532715A5 true JP2016532715A5 (en:Method) | 2017-10-19 |
| JP6407285B2 JP6407285B2 (ja) | 2018-10-17 |
Family
ID=51541401
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016540455A Expired - Fee Related JP6407285B2 (ja) | 2013-09-09 | 2014-09-08 | ＲＯＲγ調節因子 |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US9663469B2 (en:Method) |
| EP (1) | EP3044219A1 (en:Method) |
| JP (1) | JP6407285B2 (en:Method) |
| CN (1) | CN105705501B (en:Method) |
| WO (1) | WO2015035278A1 (en:Method) |
Families Citing this family (28)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105705501B (zh) | 2013-09-09 | 2019-04-19 | 百时美施贵宝公司 | RORγ调节剂 |
| JP6397488B2 (ja) | 2013-09-20 | 2018-09-26 | ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ | ＲＯＲγ調節因子 |
| ES2713681T3 (es) | 2014-01-06 | 2019-05-23 | Bristol Myers Squibb Co | Moduladores de ROR gamma de sulfona carbocíclica |
| JP6548664B2 (ja) | 2014-01-06 | 2019-07-24 | ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ | シクロヘキシルスルホンＲＯＲγ調節因子 |
| US9637455B2 (en) | 2014-01-06 | 2017-05-02 | Bristol-Myers Squibb Company | Heterocyclic sulfone RORγ modulators |
| JOP20200117A1 (ar) | 2014-10-30 | 2017-06-16 | Janssen Pharmaceutica Nv | كحولات ثلاثي فلوروميثيل كمُعدلات للمستقبل النووي جاما تي المرتبط بحمض الريتيونَويك ROR?t |
| CN107108598B (zh) | 2014-10-30 | 2020-11-17 | 詹森药业有限公司 | 作为Rorγt调节剂的噻唑 |
| SI3212642T1 (sl) | 2014-10-30 | 2020-01-31 | Janssen Pharmaceutica Nv | Amid substituirani tiazoli kot modulatorji RORGAMMAt |
| MX2017014189A (es) | 2015-05-07 | 2018-04-13 | Squibb Bristol Myers Co | Sulfonas triciclicas como moduladores del receptor huerfano relacionado con retinoide gamma (ror gamma). |
| 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 |
| CN104892546B (zh) * | 2015-07-01 | 2017-03-01 | 中国科学院南海海洋研究所 | 一类(2h)1,4‑苯并噻嗪类化合物及其制备方法和应用 |
| WO2017006953A1 (ja) * | 2015-07-07 | 2017-01-12 | 塩野義製薬株式会社 | ＴｒｋＡ阻害活性を有する複素環誘導体 |
| TW201803869A (zh) | 2016-04-27 | 2018-02-01 | 健生藥品公司 | 作為ＲＯＲγＴ調節劑之６－胺基吡啶－３－基噻唑 |
| EP3458449B1 (en) | 2016-05-20 | 2025-03-05 | Xenon Pharmaceuticals Inc. | Benzenesulfonamide compounds and their use as therapeutic agents |
| WO2017213210A1 (ja) * | 2016-06-10 | 2017-12-14 | 武田薬品工業株式会社 | 複素環化合物 |
| AU2017371674B2 (en) | 2016-12-09 | 2021-07-22 | Xenon Pharmaceuticals Inc. | Benzenesulfonamide compounds and their use as therapeutic agents |
| US10822318B2 (en) * | 2017-05-24 | 2020-11-03 | Regents Of The University Of Minnesota | Lactone-based probes and methods of use thereof |
| JP2020142989A (ja) * | 2017-06-21 | 2020-09-10 | Ｍｅｉｊｉ Ｓｅｉｋａファルマ株式会社 | イミダゾール誘導体及びそれを含有する医薬 |
| US11230555B2 (en) | 2018-03-12 | 2022-01-25 | Escalier Biosciences B.V. | Bicyclic RORγ modulators |
| CN112118841A (zh) * | 2018-03-12 | 2020-12-22 | 爱思凯利尔生物科学私人有限责任公司 | 螺环ROR-γ调节剂 |
| UA127024C2 (uk) | 2018-06-13 | 2023-03-15 | Ксенон Фармасьютікалз Інк. | Бензолсульфонамідні сполуки та їх застосування як терапевтичних агентів |
| CN112292183A (zh) | 2018-06-18 | 2021-01-29 | 詹森药业有限公司 | 作为RORγt的调节剂的6-氨基吡啶-3-基吡唑 |
| WO2019243999A1 (en) | 2018-06-18 | 2019-12-26 | Janssen Pharmaceutica Nv | Phenyl substituted pyrazoles as modulators of roryt |
| WO2019244000A1 (en) | 2018-06-18 | 2019-12-26 | Janssen Pharmaceutica Nv | Phenyl and pyridinyl substituted imidazoles as modulators of roryt |
| CN112292373A (zh) | 2018-06-18 | 2021-01-29 | 詹森药业有限公司 | 作为RORγt的调节剂的吡啶基吡唑类 |
| WO2020011086A1 (zh) * | 2018-07-13 | 2020-01-16 | 四川科伦博泰生物医药股份有限公司 | 苯并二氮杂环类化合物、其制备方法及用途 |
| MA53488A (fr) | 2018-08-31 | 2021-12-08 | Xenon Pharmaceuticals Inc | Composés de sulfonamide substitués par hétéroaryle et leur utilisation en tant qu'inhibiteurs de canaux sodiques |
| BR112021000209A2 (pt) | 2018-08-31 | 2021-08-24 | Xenon Pharmaceuticals Inc. | Compostos de sulfonamida substituída por heteroarila e seu uso como agentes terapêuticos |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ITMI20012060A1 (it) * | 2001-10-05 | 2003-04-05 | Recordati Chem Pharm | Nuovi eterocilcli n-acilati |
| US7741317B2 (en) * | 2005-10-21 | 2010-06-22 | Bristol-Myers Squibb Company | LXR modulators |
| EP2368886A1 (en) * | 2010-03-01 | 2011-09-28 | Phenex Pharmaceuticals AG | Novel compounds for modulation of orphan nuclear receptor RAR-related orphan receptor-gamma (ROR gamma, NR1F3) activity and for the treatment of chronic inflammatory and autoimmune desease |
| JP6063870B2 (ja) * | 2010-11-08 | 2017-01-18 | ライセラ・コーポレイション | ＲＯＲγ活性の阻害用のＮ−スルホニル化テトラヒドロキノリンおよび関連二環化合物および病気の治療 |
| WO2013064231A1 (en) * | 2011-10-31 | 2013-05-10 | Phenex Pharmaceuticals Ag | SEVEN-MEMBERED SULFONAMIDES AS MODULATORS OF RAR-RELATED ORPHAN RECEPTOR-GAMMA (RORγ, NR1F3) |
| CN105209453B (zh) | 2012-10-16 | 2017-06-20 | 詹森药业有限公司 | ROR‑γ‑T的亚甲基连接的喹啉基调节剂 |
| WO2014062938A1 (en) | 2012-10-19 | 2014-04-24 | Bristol-Myers Squibb Company | Rory modulators |
| CN105705501B (zh) | 2013-09-09 | 2019-04-19 | 百时美施贵宝公司 | RORγ调节剂 |
| JP6397488B2 (ja) | 2013-09-20 | 2018-09-26 | ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ | ＲＯＲγ調節因子 |
| JP6548664B2 (ja) | 2014-01-06 | 2019-07-24 | ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ | シクロヘキシルスルホンＲＯＲγ調節因子 |
| US9637455B2 (en) | 2014-01-06 | 2017-05-02 | Bristol-Myers Squibb Company | Heterocyclic sulfone RORγ modulators |
| ES2713681T3 (es) | 2014-01-06 | 2019-05-23 | Bristol Myers Squibb Co | Moduladores de ROR gamma de sulfona carbocíclica |
| MX369347B (es) | 2014-01-06 | 2019-11-06 | Bristol Myers Squibb Co | Derivados de pirrolidinilsulfona y su uso como moduladores del receptor huerfano relacionado con retinoide gamma (ror gamma). |
-
2014
- 2014-09-08 CN CN201480061168.1A patent/CN105705501B/zh not_active Expired - Fee Related
- 2014-09-08 WO PCT/US2014/054489 patent/WO2015035278A1/en not_active Ceased
- 2014-09-08 US US14/917,420 patent/US9663469B2/en active Active
- 2014-09-08 EP EP14766373.6A patent/EP3044219A1/en not_active Withdrawn
- 2014-09-08 JP JP2016540455A patent/JP6407285B2/ja not_active Expired - Fee Related
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