PE20180119A1 - Sulfonas triciclicas como moduladores del receptor huerfano relacionado con retinoide gamma (rorgamma) - Google Patents
Sulfonas triciclicas como moduladores del receptor huerfano relacionado con retinoide gamma (rorgamma)Info
- Publication number
- PE20180119A1 PE20180119A1 PE2017002385A PE2017002385A PE20180119A1 PE 20180119 A1 PE20180119 A1 PE 20180119A1 PE 2017002385 A PE2017002385 A PE 2017002385A PE 2017002385 A PE2017002385 A PE 2017002385A PE 20180119 A1 PE20180119 A1 PE 20180119A1
- Authority
- PE
- Peru
- Prior art keywords
- rorgamma
- retinoid
- modulators
- orphan receptor
- related orphan
- Prior art date
Links
- 108091008773 RAR-related orphan receptors γ Proteins 0.000 title abstract 3
- 102100023421 Nuclear receptor ROR-gamma Human genes 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 3
- 229910052739 hydrogen Inorganic materials 0.000 abstract 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- 125000001475 halogen functional group Chemical group 0.000 abstract 2
- 239000001257 hydrogen Substances 0.000 abstract 2
- 125000004435 hydrogen atom Chemical class [H]* 0.000 abstract 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 1
- 208000023275 Autoimmune disease Diseases 0.000 abstract 1
- 102000016978 Orphan receptors Human genes 0.000 abstract 1
- 108070000031 Orphan receptors Proteins 0.000 abstract 1
- 201000004681 Psoriasis Diseases 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 230000001363 autoimmune Effects 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 208000027866 inflammatory disease Diseases 0.000 abstract 1
- 201000006417 multiple sclerosis Diseases 0.000 abstract 1
- 150000004492 retinoid derivatives Chemical class 0.000 abstract 1
- 206010039073 rheumatoid arthritis Diseases 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 125000000547 substituted alkyl group Chemical group 0.000 abstract 1
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 abstract 1
Classifications
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- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6564—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms
- C07F9/6571—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and oxygen atoms as the only ring hetero atoms
- C07F9/6574—Esters of oxyacids of phosphorus
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
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- C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
- C07D493/08—Bridged systems
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- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—Ortho-condensed systems
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/08—Bridged systems
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Abstract
Referido a un compuesto de formula I, caracterizado porque X es -CR4R5-, -(CR4-R5)2, -OCR6R7-, -S(O)pCR6R7- o -NR6CR6R7-; V e Y son independientemente anillos aromaticos o heteroaromaticos de 5 o 6 elementos; R1 es H, halo, OCF3, CN, entre otros; R2 es H, CN, alquilo sustituido, entre otros; R4 y R5 son independientemente hidrogeno, halo, alquilo C1-6, entre otros; R6 y R7 son independientemente hidrogeno C(=O) alquilo C1-4, entre otro; m es 0 - 3; n es 0 - 2; p y q son 0 -2; t es 0 o 1. Dicho compuesto tiene estereoisomeros, tautomeros, sales de estos farmaceuticamente aceptable o solvatos. Estos compuestos son moduladores del receptor huerfano relacionado con retinoide (RORgamma) en una celula, son utiles para diagnosticar, prevenir o tratar a un sujeto que tiene una enfermedad o un trastorno en los que este se beneficiaria terapeuticamente de la modulacion de la actividad de RORgamma, tal es el caso de trastornos autoinmunitarios y/o inflamatorios como artritis reumatoide, psoriasis, esclerosis multiple, entre otros.
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US201562158178P | 2015-05-07 | 2015-05-07 |
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EP (1) | EP3292101B1 (es) |
JP (1) | JP6553746B2 (es) |
KR (1) | KR102114536B1 (es) |
CN (1) | CN107709295B (es) |
AR (1) | AR104555A1 (es) |
AU (1) | AU2016258087B2 (es) |
BR (1) | BR112017023780A2 (es) |
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EA (1) | EA033345B1 (es) |
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ES2887087T3 (es) * | 2015-05-07 | 2021-12-21 | Bristol Myers Squibb Co | Sulfonas tricíclicas como moduladores ROR gamma |
SG10201609616TA (en) * | 2016-09-06 | 2018-04-27 | Apple Inc | Electronic device with cooling fan |
CN110072848A (zh) * | 2016-10-10 | 2019-07-30 | 百时美施贵宝公司 | 作为γ调节剂的三环砜 |
WO2018071620A1 (en) * | 2016-10-13 | 2018-04-19 | Bristol-Myers Squibb Company | Heterocyclic sulfones as ror gamma modulators |
DE102017010487A1 (de) * | 2016-12-02 | 2018-06-07 | Merck Patent Gmbh | Monofluorierte cyclohexane |
KR20210009357A (ko) * | 2018-05-17 | 2021-01-26 | 브리스톨-마이어스 스큅 컴퍼니 | Ror 감마 조정제로서의 트리시클릭 술폰 화합물 |
EP3807265A1 (en) * | 2018-06-15 | 2021-04-21 | Reata Pharmaceuticals, Inc. | Pyrazole and imidazole compounds for inhibition of il-17 and rorgamma |
MX2021003158A (es) | 2018-09-18 | 2021-07-16 | Nikang Therapeutics Inc | Derivados de anillo tricíclico condensado como inhibidores de la fosfatasa de homología a src 2. |
US20230295087A1 (en) * | 2019-05-13 | 2023-09-21 | Bristol-Myers Squibb Company | AGONISTS OF ROR GAMMAt |
KR20220131962A (ko) * | 2020-01-24 | 2022-09-29 | 브리스톨-마이어스 스큅 컴퍼니 | Ror 감마 조정제로서의 트리시클릭 술폰 |
US11332442B2 (en) | 2020-08-12 | 2022-05-17 | Bristol-Myers Squibb Company | Synthetic process |
WO2023232870A1 (en) | 2022-05-31 | 2023-12-07 | Immunic Ag | Rorg/rorgt modulators for the treatment of virus infections like covid-19 |
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MXPA06011722A (es) | 2004-04-13 | 2007-01-25 | Incyte Corp | Derivados de piperazinilpiperidina como antagonistas del receptor de quimiocina. |
US20070155738A1 (en) | 2005-05-20 | 2007-07-05 | Alantos Pharmaceuticals, Inc. | Heterobicyclic metalloprotease inhibitors |
CN102702044A (zh) * | 2006-01-20 | 2012-10-03 | 先灵公司 | 作为γ分泌酶抑制剂的碳环和杂环芳基砜化合物 |
CN101970445A (zh) * | 2007-07-17 | 2011-02-09 | 先灵公司 | 苯磺酰基-色满、硫代色满、四氢萘和相关γ分泌酶抑制剂 |
KR20150013500A (ko) * | 2012-05-08 | 2015-02-05 | 머크 샤프 앤드 돔 코포레이션 | Ror감마 활성의 억제를 위한 비시클릭 술폰 화합물 및 질환의 치료 |
EP2669286A1 (en) | 2012-05-31 | 2013-12-04 | Ares Trading S.A. | Spiro tetrahydro-benzothiophen derivatives useful for the treatment of neurodegenerative diseases |
WO2014062938A1 (en) | 2012-10-19 | 2014-04-24 | Bristol-Myers Squibb Company | Rory modulators |
PE20151794A1 (es) | 2013-03-08 | 2015-12-03 | Amgen Inc | Compuestos de 1,3-oxazin-2-amina fusionados con ciclopropilo perfluorado como inhibidores de beta-secretasa y metodos de uso |
US9663469B2 (en) | 2013-09-09 | 2017-05-30 | Bristol-Myers Squibb Company | RORγ modulators |
CN105555768B (zh) * | 2013-09-20 | 2018-10-16 | 百时美施贵宝公司 | RORγ调节剂 |
ES2704460T3 (es) | 2014-01-06 | 2019-03-18 | Bristol Myers Squibb Co | Moduladores de ROR gamma de ciclohexilsulfona |
US9637455B2 (en) | 2014-01-06 | 2017-05-02 | Bristol-Myers Squibb Company | Heterocyclic sulfone RORγ modulators |
EP3092216B1 (en) | 2014-01-06 | 2018-12-12 | Bristol-Myers Squibb Company | Carbocyclic sulfone ror gamma modulators |
ES2669208T3 (es) | 2014-01-06 | 2018-05-24 | Bristol-Myers Squibb Company | Derivados de pirrolidinilsulfona y su uso como moduladores de ROR gamma |
ES2887087T3 (es) * | 2015-05-07 | 2021-12-21 | Bristol Myers Squibb Co | Sulfonas tricíclicas como moduladores ROR gamma |
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