AU2013302644A1 - 3-cyclohexenyl and cyclohexyl substituted indole and indazole compounds as RORgammaT inhibitors and uses thereof - Google Patents

3-cyclohexenyl and cyclohexyl substituted indole and indazole compounds as RORgammaT inhibitors and uses thereof Download PDF

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Publication number
AU2013302644A1
AU2013302644A1 AU2013302644A AU2013302644A AU2013302644A1 AU 2013302644 A1 AU2013302644 A1 AU 2013302644A1 AU 2013302644 A AU2013302644 A AU 2013302644A AU 2013302644 A AU2013302644 A AU 2013302644A AU 2013302644 A1 AU2013302644 A1 AU 2013302644A1
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Prior art keywords
chloro
trifluoromethyl
indazol
benzoyl
cyclohex
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Abandoned
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AU2013302644A
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English (en)
Inventor
Brian Andresen
Neville Anthony
Kenneth Jay BARR
Richard Thomas Beresis
Blair LAPOINTE
John Maclean
Nunzio Sciammetta
Dongshan Zhang
Hongjun Zhang
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Merck Sharp and Dohme LLC
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Merck Sharp and Dohme Ltd
Merck Sharp and Dohme LLC
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Publication of AU2013302644A1 publication Critical patent/AU2013302644A1/en
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • C07D231/56—Benzopyrazoles; Hydrogenated benzopyrazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
    • A61K31/40—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
    • A61K31/404—Indoles, e.g. pindolol
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    • 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
    • A61K31/415—1,2-Diazoles
    • A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
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    • 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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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    • 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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • A—HUMAN NECESSITIES
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    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/18—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D209/26—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with an acyl radical attached to the ring nitrogen atom
    • C—CHEMISTRY; METALLURGY
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    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
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    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
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    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
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    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
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  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
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  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
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  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
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  • Physical Education & Sports Medicine (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Endocrinology (AREA)
  • Dermatology (AREA)
  • Diabetes (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Pain & Pain Management (AREA)
  • Neurosurgery (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
AU2013302644A 2012-08-15 2013-08-14 3-cyclohexenyl and cyclohexyl substituted indole and indazole compounds as RORgammaT inhibitors and uses thereof Abandoned AU2013302644A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
AUPCT/CN2012/080133 2012-08-15
PCT/CN2012/080133 WO2014026328A1 (en) 2012-08-15 2012-08-15 3-cyclohexenyl substituted indole and indazole compounds as rorgammat inhibitors and uses thereof
PCT/US2013/054902 WO2014028597A2 (en) 2012-08-15 2013-08-14 3-CYCLOHEXENYL AND CYCLOHEXYL SUBSTITUTED INDOLE AND INDAZOLE COMPOUNDS AS RORgammaT INHIBITORS AND USES THEREOF

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AU2013302644A1 true AU2013302644A1 (en) 2015-03-05

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AU2013302644A Abandoned AU2013302644A1 (en) 2012-08-15 2013-08-14 3-cyclohexenyl and cyclohexyl substituted indole and indazole compounds as RORgammaT inhibitors and uses thereof

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US (1) US9487490B2 (enExample)
EP (1) EP2884976B1 (enExample)
JP (1) JP6232429B2 (enExample)
KR (1) KR20150041800A (enExample)
CN (1) CN104822376A (enExample)
AU (1) AU2013302644A1 (enExample)
BR (1) BR112015003332A2 (enExample)
CA (1) CA2881696A1 (enExample)
CY (1) CY1122272T1 (enExample)
DK (1) DK2884976T3 (enExample)
ES (1) ES2749713T3 (enExample)
HR (1) HRP20191654T1 (enExample)
HU (1) HUE045379T2 (enExample)
LT (1) LT2884976T (enExample)
ME (1) ME03579B (enExample)
PL (1) PL2884976T3 (enExample)
PT (1) PT2884976T (enExample)
RS (1) RS59364B1 (enExample)
RU (1) RU2015108898A (enExample)
SI (1) SI2884976T1 (enExample)
SM (1) SMT201900580T1 (enExample)
WO (2) WO2014026328A1 (enExample)

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WO2014026327A1 (en) 2012-08-15 2014-02-20 Merck Sharp & Dohme Corp. 4-heteroaryl substituted benzoic acid compounds as rorgammat inhibitors and uses thereof
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UA121309C2 (uk) 2014-02-03 2020-05-12 Вітае Фармасьютікалс, Ллс Дигідропіролопіридинові інгібітори ror-гамма
US10532088B2 (en) 2014-02-27 2020-01-14 Lycera Corporation Adoptive cellular therapy using an agonist of retinoic acid receptor-related orphan receptor gamma and related therapeutic methods
US9896441B2 (en) 2014-05-05 2018-02-20 Lycera Corporation Tetrahydroquinoline sulfonamide and related compounds for use as agonists of RORγ and the treatment of disease
EP3209641A4 (en) 2014-05-05 2018-06-06 Lycera Corporation Benzenesulfonamido and related compounds for use as agonists of ror and the treatement of disease
US20170217956A1 (en) * 2014-07-25 2017-08-03 Innov17 Llc Azaindole retinoic acid receptor-related orphan receptor modulators and uses thereof
US20160024057A1 (en) * 2014-07-25 2016-01-28 Innov17 Llc Indazole retinoic acid receptor-related orphan receptor modulators and uses thereof
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WO2016014910A1 (en) * 2014-07-25 2016-01-28 Innov17 Llc Sulfonamide retinoic acid receptor-related orphan receptor modulators and uses thereof
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BR112017007460A2 (pt) 2014-10-14 2017-12-19 Vitae Pharmaceuticals Inc inibidores de di-hidropirrolopiridina de ror-gama
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