WO2016130818A1 - SUBSTITUTED PYRAZOLE COMPOUNDS AS RORgammaT INHIBITORS AND USES THEREOF - Google Patents

SUBSTITUTED PYRAZOLE COMPOUNDS AS RORgammaT INHIBITORS AND USES THEREOF Download PDF

Info

Publication number
WO2016130818A1
WO2016130818A1 PCT/US2016/017566 US2016017566W WO2016130818A1 WO 2016130818 A1 WO2016130818 A1 WO 2016130818A1 US 2016017566 W US2016017566 W US 2016017566W WO 2016130818 A1 WO2016130818 A1 WO 2016130818A1
Authority
WO
WIPO (PCT)
Prior art keywords
chloro
alkyl
tetrahydro
mmol
indazol
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.)
Ceased
Application number
PCT/US2016/017566
Other languages
English (en)
French (fr)
Inventor
Blair T. LAPOINTE
Peter H. FULLER
Hakan GUNAYDIN
Kun Liu
Nunzio Sciammetta
Benjamin Wesley TROTTER
Hongjun Zhang
Kenneth J. Barr
John K. F. MACLEAN
Danielle F. MOLINARI
Vladimir SIMOV
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Organon Pharma UK Ltd
Merck Sharp and Dohme LLC
Original Assignee
Merck Sharp and Dohme Ltd
Merck Sharp and Dohme LLC
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 Merck Sharp and Dohme Ltd, Merck Sharp and Dohme LLC filed Critical Merck Sharp and Dohme Ltd
Priority to CA2975997A priority Critical patent/CA2975997A1/en
Priority to US15/549,465 priority patent/US10221142B2/en
Priority to AU2016219183A priority patent/AU2016219183B2/en
Priority to JP2017541959A priority patent/JP2018510135A/ja
Priority to EP16749889.8A priority patent/EP3256450B1/en
Publication of WO2016130818A1 publication Critical patent/WO2016130818A1/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • C07D231/56Benzopyrazoles; Hydrogenated benzopyrazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/4151,2-Diazoles
    • A61K31/4161,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents
    • A61P33/02Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/14Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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
    • C07D405/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic 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
    • C07D413/06Heterocyclic 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 linked by a carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/06Peri-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/12Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains three hetero rings
    • C07D487/14Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04Ortho-condensed systems
    • C07D491/044Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/052Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being six-membered
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10Spiro-condensed systems
    • C07D491/107Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic 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
    • C07D495/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02ATECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Definitions

  • psoriasis One exemplary immune disorder in need of better therapy is psoriasis.
  • Various therapeutics have been developed in an attempt to treat psoriasis.
  • the traditional therapies for psoriasis often have toxic adverse effects.
  • An exemplary inflammatory disorder in need of better treatment is rheumatoid arthritis.
  • Numerous therapeutics have been developed in an attempt to treat this disorder.
  • some patients develop resistance to current therapies.
  • Another exemplary disorder in need of better therapy is cancer.
  • alkyl refers to an aliphatic hydrocarbon group having one of its hydrogen atoms replaced with a bond having the specified number of carbon atoms.
  • an alkyl group contains, for example, from 1 to 4 carbon atoms (C 1 - 4 )alkyl.
  • an alkyl group contains, for example, from 3 to 4 carbon atoms and is cyclic (C 3 - 4 )cycloalkyl.
  • alkoxy refers to a linear or branched alkyl group of indicated number of carbon atoms attached via its oxygen atom to the rest of the molecule, i.e. –O-alkyl, wherein an alkyl group is defined above; for example "(C 1-4 )alkoxy” includes, but is not limited to, -OCH 3 , -OCH 2 CH 3 , -OCH(CH 3 ) 2 , -OC(CH 3 ) 3 .
  • heteroalkyl refers to a linear or branched C 2-10 alkyl group in which at least one carbon atom has been replaced with an O or S atom.
  • the heteroalkyl may be, for example, an–O-C 1 -C 10 alkyl group, an -C 1 -C 6 alkylene-O-C 1 -C 6 alkyl group, or a C 1 -C 6 alkylene-OH group.
  • the“heteroalkyl” may be 2-8 membered heteroalkyl, indicating that the heteroalkyl contains from 2 to 8 atoms selected from the group consisting of carbon, oxygen, nitrogen, and sulfur.
  • the heteroalkyl may be a 2-6 membered, 4-8 membered, or a 5-8 membered heteroalkyl group (which may contain for example 1 or 2 heteroatoms selected from the group oxygen and nitrogen).
  • the heteroalkyl is an“alkyl” group in which 1-3 carbon atoms have been replaced with oxygen atoms.
  • One type of heteroalkyl group is an“alkoxyl” group.
  • purified refers to the physical state of a compound after the compound has been isolated through a synthetic process (e.g., from a reaction mixture), from a natural source, or a combination thereof.
  • purified also refers to the physical state of a compound after the compound has been obtained from a purification process or processes described herein or well-known to the skilled artisan (e.g., chromatography, recrystallization, and the like), in sufficient purity to be characterizable by standard analytical techniques described herein or well-known to the skilled artisan.
  • the present invention provides a compound according to Formula I-1:
  • R 2 is independently halogen, (C 1-4 )alkyl, CF 3 , CHF 2 , or (C 3-4 )cycloalkyl, wherein said alkyl and cycloalkyl are optionally substituted with one or more substituents independently selected from the group consisting of CN, (C 1-4 )haloalkyl, and halogen;
  • R 5 is independently OH, (C 0-4 )alkyl, or S(O) 2 R b ;
  • R 6 is independently (C 0-4 )alkyl
  • R 7 is independently (C 1-6 )alkyl
  • R 8 is independently (C 0-4 )alkyl, 2-8 membered heteroalkyl, or -(3-10 membered heterocyclyl optionally substituted by one or more R 9 );
  • N(R a ) 2 (C 1-4 )alkoxy, N(R a ) 2 , C(O)R 5 , C(O)N(R 5 ) 2 , wherein said alkyl is optionally substituted with one or more halogen;
  • the exact dose and regimen of administration of the active ingredient, or a pharmaceutical composition thereof may vary with the particular compound, the route of administration, and the age and condition of the individual subject to whom the medicament is to be administered.
  • a dosage for humans preferably contains 0.0001-100 mg per kg body weight.
  • the desired dose may be presented as one dose or as multiple subdoses administered at appropriate intervals throughout the day.
  • the dosage as well as the regimen of administration may differ between a female and a male recipient.
  • Step 3 Preparation of (R or S)-(6-amino-3-iodo-4,5,6,7-tetrahydro-1H-indazol-1-yl)(2-chloro- 6-cyclopropylphenyl)methanone (22A-3)

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Neurology (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Diabetes (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Transplantation (AREA)
  • Endocrinology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
PCT/US2016/017566 2015-02-11 2016-02-11 SUBSTITUTED PYRAZOLE COMPOUNDS AS RORgammaT INHIBITORS AND USES THEREOF Ceased WO2016130818A1 (en)

Priority Applications (5)

Application Number Priority Date Filing Date Title
CA2975997A CA2975997A1 (en) 2015-02-11 2016-02-11 Substituted pyrazole compounds as rorgammat inhibitors and uses thereof
US15/549,465 US10221142B2 (en) 2015-02-11 2016-02-11 Substituted pyrazole compounds as RORgammaT inhibitors and uses thereof
AU2016219183A AU2016219183B2 (en) 2015-02-11 2016-02-11 Substituted pyrazole compounds as RORgammaT inhibitors and uses thereof
JP2017541959A JP2018510135A (ja) 2015-02-11 2016-02-11 RORγT阻害剤としての置換ピラゾール化合物及びその使用
EP16749889.8A EP3256450B1 (en) 2015-02-11 2016-02-11 Substituted pyrazole compounds as ror-gamma-t inhibitors and uses thereof

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201562114854P 2015-02-11 2015-02-11
US62/114,854 2015-02-11

Publications (1)

Publication Number Publication Date
WO2016130818A1 true WO2016130818A1 (en) 2016-08-18

Family

ID=56614908

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2016/017566 Ceased WO2016130818A1 (en) 2015-02-11 2016-02-11 SUBSTITUTED PYRAZOLE COMPOUNDS AS RORgammaT INHIBITORS AND USES THEREOF

Country Status (6)

Country Link
US (1) US10221142B2 (https=)
EP (1) EP3256450B1 (https=)
JP (1) JP2018510135A (https=)
AU (1) AU2016219183B2 (https=)
CA (1) CA2975997A1 (https=)
WO (1) WO2016130818A1 (https=)

Cited By (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2017075178A1 (en) * 2015-10-27 2017-05-04 Merck Sharp & Dohme Corp. SUBSTITUTED BICYCLIC PYRAZOLE COMPOUNDS AS RORgammaT INHIBITORS AND USES THEREOF
WO2017075182A1 (en) * 2015-10-27 2017-05-04 Merck Sharp & Dohme Corp. Substituted indazole compounds as rorgammat inhibitors and uses thereof
WO2017075185A1 (en) * 2015-10-27 2017-05-04 Merck Sharp & Dohme Corp. Heteroaryl substituted benzoic acids as rorgammat inhibitors and uses thereof
US10221142B2 (en) 2015-02-11 2019-03-05 Merck Sharp & Dohme Corp. Substituted pyrazole compounds as RORgammaT inhibitors and uses thereof
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
US11993574B2 (en) 2018-06-15 2024-05-28 Reata Pharmaceuticals, Inc Pyrazole and imidazole compounds for inhibition of IL-17 and RORgamma
US12398097B2 (en) 2019-07-29 2025-08-26 Vanderbilt University WDR5-MYC inhibitors

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2015095795A1 (en) 2013-12-20 2015-06-25 Merck Sharp & Dohme Corp. TETRAHYDRONAPHTHYRIDINE, BENZOXAZINE, AZA-BENZOXAZINE, AND RELATED BICYCLIC COMPOUNDS FOR INHIBITION OF RORgamma ACTIVITY AND THE TREATMENT OF DISEASE
WO2020117715A1 (en) 2018-12-03 2020-06-11 Board Of Regents, The University Of Texas System Oligo-benzamide analogs and their use in cancer treatment
JP2024501520A (ja) * 2020-12-22 2024-01-12 メルク・シャープ・アンド・ドーム・エルエルシー 新規ジアシルグリセリドo-アシルトランスフェラーゼ2阻害薬としてのテトラヒドロインダゾール誘導体の調製

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012106995A1 (en) * 2011-02-11 2012-08-16 Merck Sharp & Dohme Corp. Rorgammat inhibitors
WO2014026329A1 (en) * 2012-08-15 2014-02-20 Merck Sharp & Dohme Corp. N-alkylated indole and indazole compounds as rorgammat inhibitors and uses thereof
WO2014026327A1 (en) * 2012-08-15 2014-02-20 Merck Sharp & Dohme Corp. 4-heteroaryl substituted benzoic acid compounds as rorgammat inhibitors and uses thereof
WO2015008234A1 (en) * 2013-07-17 2015-01-22 Glenmark Pharmaceuticals S.A. Bicyclic heterocyclic compounds as ror gamma modulators

Family Cites Families (119)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4670447A (en) 1983-08-22 1987-06-02 Hoechst-Roussel Pharmaceuticals Inc. Antipsychotic 3-(piperidinyl)- and 3-(pyrrolidinyl)-1H-indazoles
GB8607294D0 (en) 1985-04-17 1986-04-30 Ici America Inc Heterocyclic amide derivatives
PT95899A (pt) 1989-11-17 1991-09-13 Glaxo Group Ltd Processo para a preparacao de derivados indole
TW263508B (https=) 1991-02-12 1995-11-21 Pfizer
JP3414433B2 (ja) 1993-03-01 2003-06-09 日本化薬株式会社 電子写真用トナー
US5639780A (en) 1995-05-22 1997-06-17 Merck Frosst Canada, Inc. N-benzyl indol-3-yl butanoic acid derivatives as cyclooxygenase inhibitors
DE19523446A1 (de) 1995-06-28 1997-01-02 Bayer Ag Benzotriazole
US6037367A (en) 1995-07-14 2000-03-14 Smithkline Beecham Corporation Substituted-pent-4-ynoic acids
IL122944A (en) 1995-08-10 2001-11-25 Bayer Ag Halogenobenzimidazoles, their preparation and microbicidal compositions containing them
AU722514B2 (en) 1995-12-28 2000-08-03 Fujisawa Pharmaceutical Co., Ltd. Benzimidazole derivatives
CA2258728C (en) 1996-06-19 2011-09-27 Rhone Poulenc Rorer Limited Substituted azabicylic compounds and their use as inhibitors of the production of tnf and cyclic amp phosphodiesterase
DE69728688T2 (de) 1996-11-19 2004-08-19 Amgen Inc., Thousand Oaks Aryl und heteroaryl substituierte kondensierte pyrrole als entzündunghemmende mittel
US6828344B1 (en) 1998-02-25 2004-12-07 Genetics Institute, Llc Inhibitors of phospholipase enzymes
US6133290A (en) 1998-07-31 2000-10-17 Eli Lilly And Company 5-HT1F agonists
CA2344262A1 (en) 1998-09-18 2000-03-30 Basf Aktiengesellschaft 4-aminopyrrolopyrimidines as kinase inhibitors
US6348032B1 (en) 1998-11-23 2002-02-19 Cell Pathways, Inc. Method of inhibiting neoplastic cells with benzimidazole derivatives
AU6762400A (en) 1999-08-12 2001-03-13 Cor Therapeutics, Inc. Inhibitors of factor xa
EP1218336A2 (en) 1999-09-20 2002-07-03 Takeda Chemical Industries, Ltd. Melanin concentrating hormone antagonist
GB0117577D0 (en) 2001-02-16 2001-09-12 Aventis Pharm Prod Inc Novel heterocyclic substituted carbonyl derivatives and their use as dopamine D receptor ligands
TWI239942B (en) 2001-06-11 2005-09-21 Dainippon Pharmaceutical Co N-arylphenylacetamide derivative and pharmaceutical composition containing the same
WO2003014075A2 (en) 2001-08-03 2003-02-20 Schering Corporation Novel gamma secretase inhibitors
US7355042B2 (en) 2001-10-16 2008-04-08 Hypnion, Inc. Treatment of CNS disorders using CNS target modulators
DE10229777A1 (de) 2002-07-03 2004-01-29 Bayer Ag Indolin-Phenylsulfonamid-Derivate
FR2845382A1 (fr) 2002-10-02 2004-04-09 Sanofi Synthelabo Derives d'indazolecarboxamides, leur preparation et leur utilisation en therapeutique
UA80171C2 (en) 2002-12-19 2007-08-27 Pfizer Prod Inc Pyrrolopyrimidine derivatives
JP4601038B2 (ja) 2003-03-26 2010-12-22 第一三共株式会社 インドリルマレイミド類
SI1668014T1 (sl) * 2003-09-17 2009-06-30 Janssen Pharmaceutica Nv Kondenzirane heterociklične spojine kot modulatorji serotoninskih receptorjev
KR20060070572A (ko) 2003-09-18 2006-06-23 콘포마 세러퓨틱스 코포레이션 Hsp90-저해제로서의 신규 헤테로시클릭 화합물
SE0302760D0 (sv) 2003-10-20 2003-10-20 Biovitrum Ab New compounds
US7420059B2 (en) 2003-11-20 2008-09-02 Bristol-Myers Squibb Company HMG-CoA reductase inhibitors and method
US7569571B2 (en) 2003-12-23 2009-08-04 Novartis Ag Substituted pyrazolo [3,4-d]pyrimidines as cytokine modulators
EP1771204A4 (en) 2004-07-01 2008-08-13 Univ New York COMPOSITIONS AND METHOD FOR MODULATING ROR-GAMMA-T
JP2008509138A (ja) 2004-08-03 2008-03-27 ワイス 心臓血管疾患の治療に有用なインダゾール類
US20070010537A1 (en) 2004-08-20 2007-01-11 Kazumasa Hamamura Fused pyramidine derivative and use thereof
US7605168B2 (en) 2004-09-03 2009-10-20 Plexxikon, Inc. PDE4B inhibitors
SE0402762D0 (sv) 2004-11-11 2004-11-11 Astrazeneca Ab Indazole sulphonamide derivatives
CN100516049C (zh) 2004-11-16 2009-07-22 永信药品工业股份有限公司 抗血管生成药n2-(取代的芳基甲基)-3-(取代的苯基)吲唑的合成
AR051780A1 (es) 2004-11-29 2007-02-07 Japan Tobacco Inc Compuestos en anillo fusionados que contienen nitrogeno y utilizacion de los mismos
EP1828180A4 (en) 2004-12-08 2010-09-15 Glaxosmithkline Llc 1H-pyrrolo [2,3-BETA] PYRIDINE
US8003624B2 (en) 2005-08-25 2011-08-23 Schering Corporation Functionally selective ALPHA2C adrenoreceptor agonists
BRPI0615307A2 (pt) 2005-08-25 2009-08-04 Schering Corp agonistas de adrenorreceptor alfa2c
JP2009509928A (ja) 2005-09-01 2009-03-12 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ カリウムチャンネル開口剤としての新規ベンゾピラン誘導体
JP4843040B2 (ja) 2005-09-15 2011-12-21 エフ.ホフマン−ラ ロシュ アーゲー 肝カルニチンパルミトイルトランスフェラーゼのインヒビターとして有用な新規ヘテロ二環式誘導体
JP4949413B2 (ja) 2006-02-13 2012-06-06 エフ.ホフマン−ラ ロシュ アーゲー 糖尿病の処置用のヘテロ二環式スルホンアミド誘導体
CA2637531A1 (en) 2006-02-17 2007-08-30 Memory Pharmaceuticals Corporation Compounds having 5-ht6 receptor affinity
ES2439948T3 (es) 2006-02-17 2014-01-27 Rigel Pharmaceuticals, Inc. Compuestos de 2,4-pirimidindiamina para el tratamiento o la prevención de enfermedades autoinmunitarias
JP4675801B2 (ja) 2006-03-06 2011-04-27 日本メナード化粧品株式会社 Ror活性化剤
BRPI0708615A2 (pt) 2006-03-07 2011-06-07 Array Biopharma Inc compostos de pirazol heterobicìclicos e métodos de uso
CA2651072A1 (en) 2006-05-01 2007-11-08 Pfizer Products Inc. Substituted 2-amino-fused heterocyclic compounds
US20080305169A1 (en) 2006-05-26 2008-12-11 Japan Tobacco Inc. Pharmaceutical Compositions Comprising Nitrogen-Containing Fused Ring Coumpounds
AU2007255042A1 (en) 2006-06-01 2007-12-13 Wyeth 1-sulfonylindazolylamine and -amide derivatives as 5-hydroxytryptamine-6 ligands
GB0611587D0 (en) 2006-06-12 2006-07-19 Glaxo Group Ltd Novel compounds
EP2046741B1 (en) 2006-07-03 2012-10-31 Proximagen Ltd. Indoles as 5-ht6 modulators
TWI315304B (en) 2006-08-31 2009-10-01 Univ Taipei Medical Indoline-sulfonamides compounds
US20090275586A1 (en) 2006-10-06 2009-11-05 Kalypsys, Inc. Heterocyclic inhibitors of pde4
WO2008062740A1 (fr) 2006-11-20 2008-05-29 Japan Tobacco Inc. Composé azoté à anneaux fusionnés et son utilisation
US7799933B2 (en) 2006-12-21 2010-09-21 Hoffman-La Roche Inc. Sulfonamide derivatives
US20080186971A1 (en) 2007-02-02 2008-08-07 Tarari, Inc. Systems and methods for processing access control lists (acls) in network switches using regular expression matching logic
MX2009011210A (es) 2007-04-16 2009-10-30 Abbott Lab Inhibidores de mcl1 de indol 7-no sustituido.
GB0708141D0 (en) 2007-04-26 2007-06-06 Syngenta Participations Ag Improvements in or relating to organic compounds
AR067326A1 (es) 2007-05-11 2009-10-07 Novartis Ag Imidazopiridinas y pirrolo -pirimidinas sustituidas como inhibidores de cinasa de lipido
WO2008150827A1 (en) 2007-05-29 2008-12-11 Smithkline Beecham Corporation Naphthyridine, derivatives as p13 kinase inhibitors
AR068046A1 (es) 2007-06-05 2009-11-04 Schering Corp Derivados policiclicos de indazol y su uso como inhibidores de erk para el tratamiento del cancer
US7776877B2 (en) 2007-06-22 2010-08-17 Chemocentryx, Inc. N-(2-(hetaryl)aryl) arylsulfonamides and N-(2-(hetaryl) hetaryl arylsulfonamides
US20100317863A1 (en) 2007-07-25 2010-12-16 Boehringer Ingelheim International Gmbh Glucocorticoid Mimetics, Methods of Making Them, Pharmaceutical Compositions and Uses Thereof
US20110190280A1 (en) 2007-08-29 2011-08-04 George Adjabeng Thiazole And Oxazole Kinase Inhibitors
US7960376B2 (en) 2007-09-14 2011-06-14 Cara Therapeutics, Inc. Benzo-fused heterocycles
RU2364597C1 (ru) 2007-12-14 2009-08-20 Андрей Александрович Иващенко ГЕТЕРОЦИКЛИЧЕСКИЕ ИНГИБИТОРЫ Hh-СИГНАЛЬНОГО КАСКАДА, ЛЕКАРСТВЕННЫЕ КОМПОЗИЦИИ НА ИХ ОСНОВЕ И СПОСОБ ЛЕЧЕНИЯ ЗАБОЛЕВАНИЙ, СВЯЗАННЫХ С АББЕРАНТНОЙ АКТИВНОСТЬЮ Hh СИГНАЛЬНОЙ СИСТЕМЫ
US7960377B2 (en) 2008-03-28 2011-06-14 Cara Therapeutics, Inc. Substituted pyridoxazines
US8658635B2 (en) 2008-06-05 2014-02-25 Glaxosmithkline Intellectual Property Development Limited Benzpyrazol derivatives as inhibitors of PI3 kinases
ES2566339T3 (es) 2008-06-05 2016-04-12 Glaxo Group Limited Derivados de 4-carboxamida indazol útiles como inhibidores de PI3-quinasas
ES2383246T3 (es) 2008-06-05 2012-06-19 Glaxo Group Limited 4-amino-indazoles
US8329725B2 (en) 2008-06-09 2012-12-11 Sanofi Annelated pyrrolidin sulfonamides with oxadiazolone headgroup, processes for their preparation and their use as pharmaceuticals
WO2009149819A1 (en) 2008-06-09 2009-12-17 Sanofi-Aventis Annelated pyrrolidin sulfonamides with oxadiazolone headgroup, processes for their preparation and their use as pharmaceuticals
JPWO2009157196A1 (ja) 2008-06-25 2011-12-08 武田薬品工業株式会社 アミド化合物
WO2010017827A1 (en) 2008-08-14 2010-02-18 European Molecular Biology Laboratory 6-substituted 1-sulfonyl-2, 3-dihydro-indole derivatives for the treatment of proliferative diseases
NZ592008A (en) 2008-10-02 2011-12-22 Taisho Pharmaceutical Co Ltd 7-piperidinoalkyl-3,4-dihydroquinolone derivative
EP2181710A1 (en) 2008-10-28 2010-05-05 Phenex Pharmaceuticals AG Ligands for modulation of orphan receptor-gamma (NR1F3) activity
WO2010050837A1 (ru) 2008-10-28 2010-05-06 Haskin Lev Yakovlevich Ветроэнергетическая установка
WO2010057101A2 (en) 2008-11-17 2010-05-20 Schering Corporation Compounds useful as hiv blockers
CN102281919A (zh) 2008-11-19 2011-12-14 先灵公司 二酰基甘油酰基转移酶的抑制剂
CA2744498C (en) 2008-11-25 2017-10-24 University Of Rochester Mlk inhibitors and methods of use
EP2376502B1 (en) 2008-12-19 2015-06-17 GlaxoSmithKline LLC Thiazolopyridine sirtuin modulating compounds
TW201030007A (en) 2009-02-06 2010-08-16 Gruenenthal Gmbh Substituted spiro-amides as b1r modulators
JP5656880B2 (ja) 2009-03-09 2015-01-21 グラクソ グループ リミテッドGlaxo Group Limited Pi3キナーゼの阻害剤としての4−オキサジアゾール−2−イル−インダゾール
TW201102391A (en) 2009-03-31 2011-01-16 Biogen Idec Inc Certain substituted pyrimidines, pharmaceutical compositions thereof, and methods for their use
WO2010123139A1 (ja) 2009-04-24 2010-10-28 持田製薬株式会社 スルファモイル基を有するアリールカルボキサミド誘導体
WO2010125082A1 (en) 2009-04-30 2010-11-04 Glaxo Group Limited Oxazole substituted indazoles as pi3-kinase inhibitors
WO2010150837A1 (ja) 2009-06-25 2010-12-29 第一三共株式会社 インドリン誘導体
WO2011014775A1 (en) 2009-07-31 2011-02-03 The Brigham And Women's Hospital, Inc. Modulation of sgk1 expression in th17 cells to modulate th17-mediated immune responses
WO2011019634A2 (en) 2009-08-10 2011-02-17 Taipei Medical University Aryl substituted sulfonamide compounds and their use as anticancer agents
US9556201B2 (en) 2009-10-29 2017-01-31 Glaxosmithkline Llc Bicyclic pyridines and analogs as sirtuin modulators
US20120245171A1 (en) 2009-12-03 2012-09-27 Glaxo Group Limited Benzpyrazole derivatives as inhibitors of pi3 kinases
EP2507226A1 (en) 2009-12-03 2012-10-10 Glaxo Group Limited Novel compounds
EP2507231A1 (en) 2009-12-03 2012-10-10 Glaxo Group Limited Indazole derivatives as pi 3 - kinase inhibitors
JP2013514385A (ja) 2009-12-18 2013-04-25 ヤンセン ファーマシューティカ エヌ.ベー. エストロゲン関連受容体αモジュレーターとしての置換アミノチアゾロンインダゾール
US9260382B2 (en) 2010-02-16 2016-02-16 Uwm Research Foundation Methods of reducing virulence in bacteria
MX2012010115A (es) 2010-03-01 2013-02-26 Gtx Inc Compuestos para el tratamiento de cancer.
WO2011146313A1 (en) 2010-05-19 2011-11-24 The University Of North Carolina At Chapel Hill Pyrazolopyrimidine compounds for the treatment of cancer
RS54286B1 (sr) 2010-09-08 2016-02-29 Glaxosmithkline Intellectual Property Development Limited Polimorfi i soli n-[5-[4-(5-{[(2r,6s)-2,6-dimetil-4-morfolinil]metil}-1,3-oksazol-2-il)-1h-indazol-6-il]-2(metiloksi)-3-piridinil]-metansulfonamida
US9326987B2 (en) 2010-09-08 2016-05-03 Glaxo Group Limited Indazole derivatives for use in the treatment of influenza virus infection
WO2012037108A1 (en) 2010-09-13 2012-03-22 Glaxosmithkline Llc Aminoquinoline derivatives as antiviral agents
CA2816753A1 (en) 2010-11-08 2012-05-18 Lycera Corporation N- sulfonylated tetrahydroquinolines and related bicyclic compounds inhibition of rory activity and the treatment of diseases
KR20120063283A (ko) 2010-12-07 2012-06-15 제일약품주식회사 신규한 피라졸로 피리딘 유도체 또는 이의 약학적으로 허용가능한 염, 이의 제조방법 및 이를 포함하는 약학적 조성물
RU2620376C2 (ru) 2010-12-22 2017-05-25 Людвиг-Максимилианс-Университэт Мюнхен Цинкорганические комплексы, способы их получения и применение
EP2511263A1 (en) 2011-04-14 2012-10-17 Phenex Pharmaceuticals AG Pyrrolo sulfonamide compounds for modulation of orphan nuclear receptor RAR-related orphan receptor-gamma (RORgamma, NR1F3) activity and for the treatment of chronic inflammatory and autoimmune diseases
JP2014166961A (ja) 2011-06-20 2014-09-11 Dainippon Sumitomo Pharma Co Ltd 新規インダゾール誘導体
MX363350B (es) 2012-05-08 2019-03-20 Merck Sharp & Dohme COMPUESTOS DE SULFONA BICÍCLICA PARA LA INHIBICIÓN DE LA ACTIVIDAD RORgamma Y EL TRATAMIENTO DE ENFERMEDADES.
AU2013259737A1 (en) 2012-05-08 2014-10-02 Lycera Corporation Tetrahydronaphthyridine and related bicyclic compounds for inhibition of RORgamma activity and the treatment of disease
WO2014026330A1 (en) 2012-08-15 2014-02-20 Merck Sharp & Dohme Corp. 3-AMINOCYCLOALKYL COMPOUNDS AS RORgammaT INHIBITORS AND USES THEREOF
WO2014026328A1 (en) 2012-08-15 2014-02-20 Merck Sharp & Dohme Corp. 3-cyclohexenyl substituted indole and indazole compounds as rorgammat inhibitors and uses thereof
TW201605797A (zh) 2013-12-10 2016-02-16 葛蘭馬克製藥公司 作為ror伽馬調節物的雙環雜芳基化合物
WO2015095795A1 (en) 2013-12-20 2015-06-25 Merck Sharp & Dohme Corp. TETRAHYDRONAPHTHYRIDINE, BENZOXAZINE, AZA-BENZOXAZINE, AND RELATED BICYCLIC COMPOUNDS FOR INHIBITION OF RORgamma ACTIVITY AND THE TREATMENT OF DISEASE
US9783511B2 (en) 2013-12-20 2017-10-10 Lycera Corporation Carbamate benzoxazine propionic acids and acid derivatives for modulation of RORgamma activity and the treatment of disease
US9663502B2 (en) 2013-12-20 2017-05-30 Lycera Corporation 2-Acylamidomethyl and sulfonylamidomethyl benzoxazine carbamates for inhibition of RORgamma activity and the treatment of disease
WO2015139621A1 (zh) * 2014-03-18 2015-09-24 北京韩美药品有限公司 4-杂芳基取代的苯甲酸或苯甲酰胺类化合物
JP2016141632A (ja) * 2015-01-30 2016-08-08 第一三共株式会社 縮合二環式ヘテロ環誘導体
EP3256450B1 (en) 2015-02-11 2020-12-02 Merck Sharp & Dohme Corp. Substituted pyrazole compounds as ror-gamma-t inhibitors and uses thereof
WO2016128908A1 (en) 2015-02-12 2016-08-18 Advinus Therapeutics Limited Bicyclic compounds, compositions and medicinal applications thereof

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012106995A1 (en) * 2011-02-11 2012-08-16 Merck Sharp & Dohme Corp. Rorgammat inhibitors
WO2014026329A1 (en) * 2012-08-15 2014-02-20 Merck Sharp & Dohme Corp. N-alkylated indole and indazole compounds as rorgammat inhibitors and uses thereof
WO2014028591A2 (en) * 2012-08-15 2014-02-20 Merck Sharp & Dohme Corp. N-ALKYLATED INDOLE AND INDAZOLE COMPOUNDS AS RORgammaT INHIBITORS AND USES THEREOF
WO2014026327A1 (en) * 2012-08-15 2014-02-20 Merck Sharp & Dohme Corp. 4-heteroaryl substituted benzoic acid compounds as rorgammat inhibitors and uses thereof
WO2014028589A2 (en) * 2012-08-15 2014-02-20 Merck Sharp & Dohme Corp. 4-HETEROARYL SUBSTITUTED BENZOIC ACID COMPOUNDS AS RORgammaT INHIBITORS AND USES THEREOF
WO2015008234A1 (en) * 2013-07-17 2015-01-22 Glenmark Pharmaceuticals S.A. Bicyclic heterocyclic compounds as ror gamma modulators

Cited By (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10221142B2 (en) 2015-02-11 2019-03-05 Merck Sharp & Dohme Corp. Substituted pyrazole compounds as RORgammaT inhibitors and uses thereof
WO2017075178A1 (en) * 2015-10-27 2017-05-04 Merck Sharp & Dohme Corp. SUBSTITUTED BICYCLIC PYRAZOLE COMPOUNDS AS RORgammaT INHIBITORS AND USES THEREOF
WO2017075182A1 (en) * 2015-10-27 2017-05-04 Merck Sharp & Dohme Corp. Substituted indazole compounds as rorgammat inhibitors and uses thereof
WO2017075185A1 (en) * 2015-10-27 2017-05-04 Merck Sharp & Dohme Corp. Heteroaryl substituted benzoic acids as rorgammat inhibitors and uses thereof
US10287272B2 (en) 2015-10-27 2019-05-14 Merck Sharp & Dohme Corp. Substituted indazole compounds as RORgammaT inhibitors and uses thereof
EP3368535A4 (en) * 2015-10-27 2019-06-19 Merck Sharp & Dohme Corp. HETEROARYL-SUBSTITUTED BENZOIC ACIDS AS ROR-GAMMA-T-HEMMER AND USES THEREOF
US10344000B2 (en) 2015-10-27 2019-07-09 Merck Sharp & Dohme Corp. Substituted bicyclic pyrazole compounds as RORgammaT inhibitors and uses thereof
US10584121B2 (en) 2015-10-27 2020-03-10 Merck Sharp & Dohme Corp. Heteroaryl substituted benzoic acids as RORgammaT inhibitors and uses thereof
US10689369B2 (en) 2015-10-27 2020-06-23 Merck Sharp & Dohme Corp. Substituted indazole compounds as RORgammaT inhibitors and uses thereof
US11993574B2 (en) 2018-06-15 2024-05-28 Reata Pharmaceuticals, Inc Pyrazole and imidazole compounds for inhibition of IL-17 and RORgamma
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
US12398097B2 (en) 2019-07-29 2025-08-26 Vanderbilt University WDR5-MYC inhibitors

Also Published As

Publication number Publication date
US10221142B2 (en) 2019-03-05
EP3256450A4 (en) 2018-05-30
AU2016219183B2 (en) 2020-06-11
US20180016239A1 (en) 2018-01-18
CA2975997A1 (en) 2016-08-18
EP3256450A1 (en) 2017-12-20
JP2018510135A (ja) 2018-04-12
EP3256450B1 (en) 2020-12-02
AU2016219183A1 (en) 2017-08-24

Similar Documents

Publication Publication Date Title
US10221142B2 (en) Substituted pyrazole compounds as RORgammaT inhibitors and uses thereof
ES2749713T3 (es) Compuestos de indol e indazol sustituidos con 3-ciclohexenilo y ciclohexilo como inhibidores de RORgammaT y usos de los mismos
CN108431007B (zh) 用于治疗癌症的作为btk抑制剂的吡唑并嘧啶衍生物
JP6411345B2 (ja) RORγT阻害剤としてのN−アルキル化インドールおよびインダゾール化合物およびそれらの使用
EP2487159A1 (en) RorgammaT inhibitors
CN104822657A (zh) 作为RORγT抑制剂的3-氨基环烷基化合物及其用途
CN105051047A (zh) 化学个体
EP3368539B1 (en) Substituted indazole compounds as ror gamma t inhibitors and uses thereof
EP3368516B1 (en) SUBSTITUTED BICYCLIC PYRAZOLE COMPOUNDS AS RORgammaT INHIBITORS AND USES THEREOF
EP3368535B1 (en) Heteroaryl substituted benzoic acids as rorgammat inhibitors and uses thereof
HK1259662A1 (en) Substituted indazole compounds as rorgammat inhibitors and uses thereof

Legal Events

Date Code Title Description
121 Ep: the epo has been informed by wipo that ep was designated in this application

Ref document number: 16749889

Country of ref document: EP

Kind code of ref document: A1

ENP Entry into the national phase

Ref document number: 2975997

Country of ref document: CA

WWE Wipo information: entry into national phase

Ref document number: 15549465

Country of ref document: US

ENP Entry into the national phase

Ref document number: 2017541959

Country of ref document: JP

Kind code of ref document: A

NENP Non-entry into the national phase

Ref country code: DE

ENP Entry into the national phase

Ref document number: 2016219183

Country of ref document: AU

Date of ref document: 20160211

Kind code of ref document: A

REEP Request for entry into the european phase

Ref document number: 2016749889

Country of ref document: EP