BR112017026224A2 - moduladores de ror gama (rory) - Google Patents

moduladores de ror gama (rory)

Info

Publication number
BR112017026224A2
BR112017026224A2 BR112017026224-0A BR112017026224A BR112017026224A2 BR 112017026224 A2 BR112017026224 A2 BR 112017026224A2 BR 112017026224 A BR112017026224 A BR 112017026224A BR 112017026224 A2 BR112017026224 A2 BR 112017026224A2
Authority
BR
Brazil
Prior art keywords
formula
rory
methyl
present
substituted
Prior art date
Application number
BR112017026224-0A
Other languages
English (en)
Inventor
Maria Gerardus Barbara Cals Joseph
De Kimpe Vera
Bernardus Nabuurs Sander
Damiano Cadicamo Cosimo
Gerardus Henricus LEMMERS Jaap
Original Assignee
Lead Pharma Holding B.V.
Sanofi
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Lead Pharma Holding B.V., Sanofi filed Critical Lead Pharma Holding B.V.
Publication of BR112017026224A2 publication Critical patent/BR112017026224A2/pt

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    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C317/00—Sulfones; Sulfoxides
    • C07C317/26—Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton
    • C07C317/32—Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
    • 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
    • A61K31/095—Sulfur, selenium, or tellurium compounds, e.g. thiols
    • A61K31/10—Sulfides; Sulfoxides; Sulfones
    • 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
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • A61K31/167—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
    • 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
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/18—Sulfonamides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/33—Heterocyclic compounds
    • A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
    • A61K31/381—Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/33—Heterocyclic compounds
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
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    • A61K31/421—1,3-Oxazoles, e.g. pemoline, trimethadione
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    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4436—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom
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    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
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    • C07C311/20—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Heterocyclic Compounds Containing Sulfur Atoms (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

moduladores de ror gama (rory). a presente invenção está relacionada a compostos de acordo com a fórmula i: (fórmula i) ou seu sal aceitável farmaceuticamente em que a1 é nr1 ou cr1, com r1 sendo h ou metil, com metil, se presente, opcionalmente sendo substituído por um ou mais f; a porção de ciclopropil pode ser opcionalmente substituída por um ou mais metil e um ou mais f; a2-a5 são n ou cr2-cr5, respectivamente, com a condição de que não mais de duas das quatro posições a em a2-a5possam ser simultaneamente n; r2-r5 são independentemente h, halógeno, amino, c (1-3) alcóxi, (di)c(1-3)alquilamino ou c (1-6) alquil; r6 e r7 são independentemente h, f, metil, etil, hidroxil ou metóxi ou r2 e r3 em conjunto são carbonil, todos os grupos de alquil, se presentes, opcionalmente sendo substituídos por um ou mais f; r8 é h ou c(1-6)alquil; r9 é selecionado do grupo que consiste nas fórmulas ii, iii, iv e v (fórmula ii) (fórmula iii) (fórmula iv) (fórmula v) os compostos podem ser usados como inibidores de rory e são úteis para o tratamento de doenças mediadas por rory.
BR112017026224-0A 2015-06-05 2016-06-03 moduladores de ror gama (rory) BR112017026224A2 (pt)

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EP3101009A1 (en) 2015-06-05 2016-12-07 Lead Pharma Cel Models IP B.V. Ror gamma (rory) modulators
EP3390396B1 (en) 2015-12-15 2022-07-06 Astrazeneca AB Isoindole compounds
TW201815388A (zh) 2016-07-14 2018-05-01 印度商卡迪拉保健有限公司 作為ＲＯＲγ調節劑之新穎化合物
JP2019520400A (ja) 2016-07-14 2019-07-18 カディラ ヘルスケア リミティド 新規シクロプロピル誘導体
AR110481A1 (es) 2016-12-05 2019-04-03 Lead Pharma Holding Bv MODULADORES DE ROR g (RORg)
JP6953538B2 (ja) * 2017-02-09 2021-10-27 ▲復▼旦大学Ｆｕｎｄａｎ Ｕｎｉｖｅｒｓｉｔｙ ビアリール化合物、その製造方法及び用途
US11034654B2 (en) 2017-06-14 2021-06-15 Astrazeneca Ab 2,3-dihydroisoindole-1-carboxamides useful as ROR-gamma modulators
CN113666853B (zh) * 2020-05-15 2023-04-18 上海辉启生物医药科技有限公司 可用作RORγ调节剂的联芳基类化合物
CN111658651B (zh) * 2020-06-08 2021-08-03 重庆医科大学附属第一医院 CQMU151在制备治疗Th17细胞介导自身免疫病药物中的应用

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