AR104880A1 - MODULADORES DE ROR GAMMA (RORg) - Google Patents

MODULADORES DE ROR GAMMA (RORg)

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Publication number
AR104880A1
AR104880A1 ARP160101634A ARP160101634A AR104880A1 AR 104880 A1 AR104880 A1 AR 104880A1 AR P160101634 A ARP160101634 A AR P160101634A AR P160101634 A ARP160101634 A AR P160101634A AR 104880 A1 AR104880 A1 AR 104880A1
Authority
AR
Argentina
Prior art keywords
alkyl
cycloalkyl
optionally substituted
heterocycloalkyl
heteroaryl
Prior art date
Application number
ARP160101634A
Other languages
English (en)
Original Assignee
Lead Pharma Cel Models Ip B V
Sanofi Sa
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 Cel Models Ip B V, Sanofi Sa filed Critical Lead Pharma Cel Models Ip B V
Publication of AR104880A1 publication Critical patent/AR104880A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81—Amides; Imides
    • 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
    • A61K31/166—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the carbon of a carboxamide group directly attached to the aromatic ring, e.g. procainamide, procarbazine, metoclopramide, labetalol
    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • 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
    • A61K31/42—Oxazoles
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/22—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound oxygen atoms
    • C07C311/23—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound oxygen atoms having the sulfur atoms of the sulfonamide groups bound to acyclic carbon atoms
    • C07C311/27—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound oxygen atoms having the sulfur atoms of the sulfonamide groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/30—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/45—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups at least one of the singly-bound nitrogen atoms being part of any of the groups, X being a hetero atom, Y being any atom, e.g. N-acylaminosulfonamides
    • C07C311/46—Y being a hydrogen or a carbon atom
    • C—CHEMISTRY; METALLURGY
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
    • C07D261/02—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
    • C07D261/06—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members
    • C07D261/08—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/02—Systems containing only non-condensed rings with a three-membered ring

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pyridine Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

Los compuestos pueden usarse como inhibidores de RORg y son útiles para el tratamiento de enfermedades mediadas por RORg. Reivindicación 1: Un compuesto de acuerdo con la fórmula (1), o una sal farmacéuticamente aceptable del mismo en donde: A¹¹ - A¹⁴ son N o CR¹¹, CR¹², CR¹³, CR¹⁴, respectivamente, con la condición de que no más que dos de las cuatro posiciones A pueden ser simultáneamente N; R¹ es alquilo C₂₋₆, cicloalquilo C₃₋₆, cicloalquilo C₃₋₆-alquilo C₁₋₃, (di)cicloalquil C₃₋₆amino o (di)(cicloalquil C₃₋₆-alquil C₁₋₃)-amino, con todos los átomos de carbono de los grupos alquilo opcionalmente sustituidos con uno o más F y todos los átomos de carbono de los grupos cicloalquilo opcionalmente sustituidos con uno o más F o metilo; R² y R³ son independientemente H, F, metilo, etilo, hidroxi, metoxi o R² y R³ juntos es carbonilo, todos los grupos alquilo, si están presentes, estando sustituidos opcionalmente con uno o más F; R⁴ es H o alquilo C₁₋₆; R⁵ es H, hidroxietilo, metoxietilo, alquilo C₁₋₆, arilo C₆₋₁₀, aril C₆₋₁₀-alquilo C₁₋₃, heteroarilo C₁₋₉, heteroaril C₁₋₉-alquilo C₁₋₃, cicloalquilo C₃₋₆, cicloalquil C₃₋₆-alquilo C₁₋₃, heterocicloalquilo C₂₋₅ o heterocicloalquil C₂₋₅-alquilo C₁₋₃, todos los grupos opcionalmente sustituidos con uno o más F, Cl, alquilo C₁₋₂, alcoxi C₁₋₂ o ciano; el grupo sulfonilo con R¹ se representa por uno de R⁷, R⁸ o R⁹; el resto R⁶ - R¹⁴ son independientemente H, halógeno, amino, alcoxi C₁₋₃, (di)alquil C₁₋₃-amino o alquilo C₁₋₆, todos los grupos alquilo opcionalmente sustituidos con uno o más F; R¹⁵ es H, alquilo C₁₋₆, cicloalquilo C₃₋₆, cicloalquil C₃₋₆-alquilo C₁₋₃, arilo C₆₋₁₀, aril C₆₋₁₀-alquilo C₁₋₃, heteroarilo C₁₋₉, heteroaril C₁₋₉-alquilo C₁₋₃, heterocicloalquilo C₂₋₅ o heterocicloalquil C₂₋₅-alquilo C₁₋₃, todos los grupos opcionalmente sustituidos con uno o más F, Cl, alquilo C₁₋₂, alcoxi C₁₋₂ o ciano; y R¹⁶ es alquilo C₁₋₆, cicloalquilo C₃₋₆, cicloalquil C₃₋₆-alquilo C₁₋₃, arilo C₆₋₁₀, aril C₆₋₁₀-alquilo C₁₋₃, heteroarilo C₁₋₉, heteroaril C₁₋₉-alquilo C₁₋₃, heterocicloalquilo C₂₋₅ o heterocicloalquil C₂₋₅-alquilo C₁₋₃, todos los grupos opcionalmente sustituidos con uno o más F, Cl, alquilo C₁₋₂, alcoxi C₁₋₂ o ciano.
ARP160101634A 2015-06-05 2016-06-02 MODULADORES DE ROR GAMMA (RORg) AR104880A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP15170765.0A EP3101009A1 (en) 2015-06-05 2015-06-05 Ror gamma (rory) modulators

Publications (1)

Publication Number Publication Date
AR104880A1 true AR104880A1 (es) 2017-08-23

Family

ID=53284143

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP160101634A AR104880A1 (es) 2015-06-05 2016-06-02 MODULADORES DE ROR GAMMA (RORg)

Country Status (15)

Country Link
US (1) US10556866B2 (es)
EP (2) EP3101009A1 (es)
JP (1) JP6754777B2 (es)
KR (1) KR102576004B1 (es)
CN (1) CN108430974B (es)
AR (1) AR104880A1 (es)
AU (1) AU2016273353B2 (es)
CA (1) CA2988002C (es)
ES (1) ES2783824T3 (es)
IL (1) IL256038B (es)
MX (1) MX2017015740A (es)
PL (1) PL3303293T3 (es)
PT (1) PT3303293T (es)
RU (1) RU2735546C2 (es)
WO (1) WO2016193461A1 (es)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2927631T3 (es) 2015-12-15 2022-11-08 Astrazeneca Ab Compuestos de isoindol
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
BR112019000603A2 (pt) 2016-07-14 2019-04-30 Cadila Healthcare Limited composto, composição farmacêutica, método para o tratamento de doenças e uso do composto
AR110481A1 (es) 2016-12-05 2019-04-03 Lead Pharma Holding Bv MODULADORES DE ROR g (RORg)
JP2020524660A (ja) 2017-06-14 2020-08-20 アストラゼネカ・アクチエボラーグＡｓｔｒａｚｅｎｅｃａ Ａｋｔｉｅｂｏｌａｇ Ｒｏｒ−ガンマモジュレーターとして有用な２，３−ジヒドロイソインドール−１−カルボキサミド
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
CN109593068B (zh) * 2017-09-30 2022-12-27 广东东阳光药业有限公司 一种RORγ抑制剂的中间体及其制备方法
CN108840800A (zh) * 2018-05-28 2018-11-20 上海华堇生物技术有限责任公司 一种苯基硝基乙酮的新制备方法
CN113166061B (zh) * 2018-11-27 2023-11-21 正大天晴药业集团股份有限公司 含有磺酰基结构的RORγ抑制剂
CN117384004B (zh) * 2023-12-11 2024-03-29 山东国邦药业有限公司 一种2,4-二氯氟苯的合成方法

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MX2008013194A (es) 2006-04-11 2008-12-01 Vertex Pharma Composiciones utiles como inhibidores de canales de sodio regulados por voltaje.
WO2012028100A1 (en) * 2010-09-01 2012-03-08 Glaxo Group Limited Novel compounds
US9512111B2 (en) * 2010-11-08 2016-12-06 Lycera Corporation N-sulfonylated tetrahydroquinolines and related bicyclic compounds for inhibition of RORγ activity and the treatment of disease
WO2013029338A1 (en) * 2011-09-01 2013-03-07 Glaxo Group Limited Novel compounds
BR112014026266A2 (pt) * 2012-04-24 2017-06-27 Chugai Pharmaceutical Co Ltd derivado de quinazolidinadiona
SG11201407919WA (en) * 2012-05-31 2014-12-30 Phenex Pharmaceuticals Ag Carboxamide or sulfonamide substituted thiazoles and related derivatives as modulators for the orphan nuclear receptor ror[gamma]
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WO2013171729A2 (en) * 2013-01-08 2013-11-21 Glenmark Pharmaceuticals S.A. Aryl and heteroaryl amide compounds as rorgamat modulator
WO2014125426A1 (en) 2013-02-15 2014-08-21 Aurigene Discovery Technologies Limited Trisubstituted heterocyclic derivatives as ror gamma modulators
CA2942871A1 (en) * 2014-03-27 2015-10-01 Piramal Enterprises Limited Ror-gamma modulators and uses thereof
EP3101008A1 (en) 2015-06-05 2016-12-07 Lead Pharma Cel Models IP B.V. Ror gamma (rory) modulators
EP3101005A1 (en) 2015-06-05 2016-12-07 Lead Pharma Cel Models IP B.V. Ror gamma (rory) modulators
EP3101006A1 (en) 2015-06-05 2016-12-07 Lead Pharma Cel Models IP B.V. Ror gamma (rory) modulators
EP3101007A1 (en) 2015-06-05 2016-12-07 Lead Pharma Cel Models IP B.V. Ror gamma (rory) modulators
AR110481A1 (es) 2016-12-05 2019-04-03 Lead Pharma Holding Bv MODULADORES DE ROR g (RORg)

Also Published As

Publication number Publication date
US10556866B2 (en) 2020-02-11
PT3303293T (pt) 2020-04-09
RU2017145930A3 (es) 2019-09-27
KR102576004B1 (ko) 2023-09-06
EP3101009A1 (en) 2016-12-07
ES2783824T3 (es) 2020-09-18
CN108430974A (zh) 2018-08-21
JP2018518480A (ja) 2018-07-12
AU2016273353A1 (en) 2018-01-04
RU2735546C2 (ru) 2020-11-03
EP3303293A1 (en) 2018-04-11
IL256038A (en) 2018-01-31
RU2017145930A (ru) 2019-07-09
US20180162815A1 (en) 2018-06-14
KR20180040559A (ko) 2018-04-20
EP3303293B1 (en) 2020-02-05
CN108430974B (zh) 2021-09-17
WO2016193461A1 (en) 2016-12-08
CA2988002A1 (en) 2016-12-08
CA2988002C (en) 2023-08-08
IL256038B (en) 2021-02-28
MX2017015740A (es) 2018-04-24
PL3303293T3 (pl) 2020-10-05
JP6754777B2 (ja) 2020-09-16
BR112017026223A2 (pt) 2018-09-11
AU2016273353B2 (en) 2020-08-27

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