AR112348A1 - Compuestos bicíclicos de pirazolo y triazolo como inhibidores de quinasas jak - Google Patents

Compuestos bicíclicos de pirazolo y triazolo como inhibidores de quinasas jak

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Publication number
AR112348A1
AR112348A1 ARP180102151A AR112348A1 AR 112348 A1 AR112348 A1 AR 112348A1 AR P180102151 A ARP180102151 A AR P180102151A AR 112348 A1 AR112348 A1 AR 112348A1
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Argentina
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group
alkyl
independently selected
optionally
alkoxy
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English (en)
Inventor
Miroslav Rapta
Venkat R Thalladi
Marta Dabros
Jerry Nzerem
Breena Fraga
Diana Jin Wang
Anthony Francesco Palermo
Robert Murray Mkinnell
Mandy Loo
Tom M Lam
Erik Fenster
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Theravance Biopharma R&D Ip Llc
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Application filed by Theravance Biopharma R&D Ip Llc filed Critical Theravance Biopharma R&D Ip Llc
Publication of AR112348A1 publication Critical patent/AR112348A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/12—Heterocyclic 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
    • 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
    • A61K31/415—1,2-Diazoles
    • A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
    • 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
    • A61K31/495—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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A61K31/535—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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • 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
    • A61P35/00—Antineoplastic agents
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D401/12—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 chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • 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
    • C07D413/12—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 linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Dermatology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Reivindicación 1: Un compuesto caracterizado porque tiene la fórmula (1), o una sal farmacéuticamente aceptable del mismo, en donde: X¹ y X² se seleccionan, cada uno independientemente, entre N y CH; X³ se selecciona entre el grupo que consiste en N, CH, C-CH₃, C-CF₃, C-CHF₂, C-CH₂-O-CH₃, C-SMe, C-NMe₂, C-NH-CH₃, C-Cl, C-CN, y C-OMe; el resto de fórmula (2) se selecciona entre el grupo que consiste en los compuestos del grupo de fórmulas (3); Rᵃ, Rᵇ, Rᶜ, y Rᶠ se seleccionan, cada uno independientemente, entre el grupo que consiste en H y alquilo C₁₋₃; Rᵈ, Rᵉ, Rᵍ, Rʰ, Rⁱ, Rʲ, Rˡ, Rᵐ, Rⁿ y Rᵒ se seleccionan, cada uno independientemente, entre el grupo que consiste en H y alquilo C₁₋₃, en donde el grupo alquilo C₁₋₃ puede estar opcionalmente sustituido con 1 a 3 halógenos; opcionalmente, Rᵈ y Rᵉ pueden unirse para formar un anillo de ciclopropilo; A se selecciona entre el grupo que consiste en: (a) un grupo heterocíclico monocíclico de 4 a 10 miembros que contiene un átomo de nitrógeno y que opcionalmente contiene un heteroátomo adicional seleccionado entre N, S, S(O)₂ y O, y (b) un grupo heterocíclico multicíclico de 6 a 10 miembros que contiene un átomo de nitrógeno y que opcionalmente contiene un heteroátomo adicional seleccionado entre N, S, y O, en donde L está ligado a un átomo de carbono en A, y A está opcionalmente sustituido con 1 a 3 grupos Rᵏ; cada Rᵏ se selecciona independientemente entre el grupo que consiste en F, CN, alcoxi C₁₋₃, ciclopropilo, y alquilo C₁₋₃, en donde el grupo alquilo C₁₋₃ puede estar opcionalmente sustituido con OH, OMe o 1 a 3 halógenos; R¹ se selecciona entre el grupo que consiste en los compuestos del grupo de fórmulas (4), en donde Rᵖ y Rq se seleccionan, cada uno independientemente, entre el grupo que consiste en H, cicloalquilo C₃₋₅ y alquilo C₁₋₆, en donde el grupo alquilo C₁₋₆ puede estar opcionalmente sustituido con 1 a 3 sustituyentes independientemente seleccionados entre el grupo que consiste en alcoxi C₁₋₃ y -S-alquilo C₁₋₃, o Rᵖ y Rq forman un grupo heterocíclico monocíclico de 4 a 6 miembros que contiene un átomo de nitrógeno y que opcionalmente contiene un heteroátomo adicional seleccionado entre N, S, y O, en donde el grupo heterocíclico monocíclico de 4 a 6 miembros está opcionalmente sustituido con 1 a 3 sustituyentes independientemente seleccionados entre el grupo que consiste en alquilo C₁₋₆, alcoxi C₁₋₃, -S-alquilo C₁₋₃ y alquilo C₁₋₃-alcoxi C₁₋₃; R² se selecciona entre el grupo que consiste en H, Cl, OMe, Me y F; R³ se selecciona entre el grupo que consiste en H y F; R⁴ se selecciona entre el grupo que consiste en H y F; y R⁵ se selecciona entre el grupo que consiste en H, Me y F.
ARP180102151 2017-08-01 2018-07-31 Compuestos bicíclicos de pirazolo y triazolo como inhibidores de quinasas jak AR112348A1 (es)

Applications Claiming Priority (1)

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US201762539642P 2017-08-01 2017-08-01

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AR112348A1 true AR112348A1 (es) 2019-10-16

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US (4) US10392368B2 (es)
EP (1) EP3652169A1 (es)
JP (2) JP7098716B2 (es)
KR (1) KR20200036004A (es)
CN (1) CN111032646B (es)
AR (1) AR112348A1 (es)
AU (1) AU2018312349A1 (es)
BR (1) BR112020002265A2 (es)
CA (1) CA3069990A1 (es)
CL (1) CL2020000283A1 (es)
CO (1) CO2020001469A2 (es)
EA (1) EA038912B1 (es)
IL (1) IL272031A (es)
MA (1) MA49570A (es)
MX (1) MX2020001170A (es)
MY (1) MY200629A (es)
PE (1) PE20201028A1 (es)
PH (1) PH12020500201A1 (es)
SG (1) SG11202000602YA (es)
TW (1) TW201920150A (es)
UA (1) UA125318C2 (es)
WO (1) WO2019027960A1 (es)
ZA (1) ZA202000561B (es)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN111032646B (zh) 2017-08-01 2023-01-03 施万生物制药研发Ip有限责任公司 作为jak激酶抑制剂的吡唑并和三唑并双环化合物
JP2022518741A (ja) 2019-01-23 2022-03-16 セラヴァンス バイオファーマ アール＆ディー アイピー， エルエルシー ＪＡＫキナーゼ阻害剤としてのイミダゾ［１，５－ａ］ピリジン、１，２，４－トリアゾロ［４，３－ａ］ピリジンおよびイミダゾ［１，５－ａ］ピラジン
JP2022541013A (ja) * 2019-07-15 2022-09-21 ノバルティス アーゲー 肝臓ｘ受容体アゴニストでマイボーム腺機能不全を治療するための方法
EP4149462A4 (en) * 2020-05-14 2024-04-24 Theravance Biopharma R&D IP, LLC ADMINISTRATION OF A GUT SELECTIVE JAK3 INHIBITOR
CN114075221B (zh) * 2020-08-13 2024-08-23 广东东阳光药业股份有限公司 取代的杂芳基化合物及其组合物和用途
CN114075220A (zh) * 2020-08-13 2022-02-22 广东东阳光药业有限公司 取代的杂芳基化合物及其组合物和用途
WO2022053000A1 (zh) * 2020-09-10 2022-03-17 四川海思科制药有限公司 一种碳环酰胺衍生物及其在医药上的应用
WO2022199599A1 (zh) * 2021-03-23 2022-09-29 凯复(苏州)生物医药有限公司 丙烯酰基取代的化合物、包含其的药物组合物及其用途
EP4313974A1 (en) * 2021-03-29 2024-02-07 Bristol-Myers Squibb Company Crystal forms of 6-(cyclopropanecarboxamido)-4-((2-methoxy-3-(1-methyl-1h-1,2,4-triazol-3-yl)phenyl)amino)-n-(methyl-d3)pyridazine-3-carboxamide
CN113061137B (zh) * 2021-04-02 2022-08-02 广西医科大学 含氮杂环衍生物或其药学上可接受的盐和用途
US20220378746A1 (en) * 2021-05-03 2022-12-01 Incyte Corporation Jak1 pathway inhibitors for the treatment of prurigo nodularis
WO2023116748A1 (zh) * 2021-12-23 2023-06-29 广东东阳光药业有限公司 取代的杂芳基化合物及其组合物和用途
WO2023165562A1 (zh) * 2022-03-02 2023-09-07 南京明德新药研发有限公司 含氮杂环类化合物及其应用
GB202213164D0 (en) 2022-09-08 2022-10-26 Cambridge Entpr Ltd Novel compounds, compositions and therapeutic uses thereof
GB202213163D0 (en) 2022-09-08 2022-10-26 Cambridge Entpr Ltd Novel compounds, compositions and therapeutic uses thereof

Family Cites Families (56)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AR034588A1 (es) 2001-04-20 2004-03-03 Wyeth Corp Derivados heterociclilalcoxi-, -alquiltio- y -alquilamino-benzazol como ligandos de 5-hidroxitriptamina-6, un proceso para su preparacion, intermediarios, composiciones farmaceuticas y el uso de dichos derivados para la manufactura de medicamentos
FR2836915B1 (fr) 2002-03-11 2008-01-11 Aventis Pharma Sa Derives d'aminoindazoles, procede de preparation et intermediaires de ce procede a titre de medicaments et compositions pharmaceutiques les renfermant
US20030139427A1 (en) 2002-08-23 2003-07-24 Osi Pharmaceuticals Inc. Bicyclic pyrimidinyl derivatives and methods of use thereof
KR100976076B1 (ko) 2003-05-22 2010-08-17 아보트 러보러터리즈 인다졸, 벤즈이속사졸 및 벤즈이소티아졸 키나제 억제제
EP1647549A1 (en) 2004-10-14 2006-04-19 Laboratoire Theramex Indazoles, benzisoxazoles and benzisothiazoles as estrogenic agents
WO2007050574A1 (en) 2005-10-25 2007-05-03 Abbott Laboratories Formulation comprising a drug of low water solubility and method of use thereof
JP2009532375A (ja) 2006-03-30 2009-09-10 タケダ サン ディエゴ インコーポレイテッド キナーゼ阻害剤
KR100834758B1 (ko) 2006-07-05 2008-06-05 삼성전자주식회사 컴퓨터 시스템 보안 장치 및 방법
JP2009007342A (ja) 2007-06-01 2009-01-15 Mitsubishi Tanabe Pharma Corp 医薬組成物
US8648069B2 (en) 2007-06-08 2014-02-11 Abbvie Inc. 5-substituted indazoles as kinase inhibitors
EP2280959B1 (en) 2008-06-05 2012-04-04 Glaxo Group Limited 4-amino-indazoles
ES2526966T3 (es) 2008-06-05 2015-01-19 Glaxo Group Limited Compuestos novedosos
US8658635B2 (en) 2008-06-05 2014-02-25 Glaxosmithkline Intellectual Property Development Limited Benzpyrazol derivatives as inhibitors of PI3 kinases
WO2010012121A1 (zh) 2008-07-28 2010-02-04 江苏国华投资有限公司 芳烷基哌啶（嗪）衍生物及其在治疗精神分裂症中的应用
TW201111385A (en) 2009-08-27 2011-04-01 Biocryst Pharm Inc Heterocyclic compounds as janus kinase inhibitors
FR2951172B1 (fr) 2009-10-13 2014-09-26 Pf Medicament Derives pyrazolopyridines en tant qu'agent anticancereux
JP2013512878A (ja) 2009-12-03 2013-04-18 グラクソ グループ リミテッド 新規化合物
WO2011067365A1 (en) 2009-12-03 2011-06-09 Glaxo Group Limited Benzpyrazole derivatives as inhibitors of p13 kinases
TW201200518A (en) 2010-03-10 2012-01-01 Kalypsys Inc Heterocyclic inhibitors of histamine receptors for the treatment of disease
PT2635299T (pt) 2010-11-02 2019-10-14 Univ Columbia Métodos de tratamento de distúrbios de perda de cabelo
WO2013037390A1 (en) 2011-09-12 2013-03-21 Sanofi 6-(4-hydroxy-phenyl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
US8846712B2 (en) 2011-09-12 2014-09-30 Sanofi 6-(4-hydroxy-phenyl)-3-styryl-1H-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
EP2567959B1 (en) 2011-09-12 2014-04-16 Sanofi 6-(4-hydroxy-phenyl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
CN102993201A (zh) * 2011-09-14 2013-03-27 赛诺菲 作为激酶抑制剂的6-(4-羟基-苯基)-3-苯乙烯基-1H-吡唑并[3，4-b]吡啶-4-羧酸酰胺衍生物
EP2760862B1 (en) 2011-09-27 2015-10-21 Sanofi 6-(4-hydroxy-phenyl)-3-alkyl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
US20130102601A1 (en) 2011-10-21 2013-04-25 F. Hoffmann-La Roche Ltd Pyrimidin-4-one derivatives and their use in the treatment, amelioration or prevention of a viral disease
WO2013060636A1 (en) 2011-10-25 2013-05-02 Sanofi 6-(4-hydroxy-phenyl)-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
US8993756B2 (en) * 2011-12-06 2015-03-31 Merck Sharp & Dohme Corp. Pyrrolopyrimidines as janus kinase inhibitors
US8377946B1 (en) * 2011-12-30 2013-02-19 Pharmacyclics, Inc. Pyrazolo[3,4-d]pyrimidine and pyrrolo[2,3-d]pyrimidine compounds as kinase inhibitors
CN104334191A (zh) 2012-03-29 2015-02-04 纽约市哥伦比亚大学托管会 治疗毛发脱落疾病的方法
WO2013167403A1 (en) * 2012-05-09 2013-11-14 Sanofi Substituted 6-(4-hydroxy-phenyl)-1h-pyrazolo[3,4-b]pyridine derivatives as kinase inhibitors
TWI629275B (zh) 2013-03-13 2018-07-11 賽諾菲公司 Ｎ－（４－（氮雜吲唑－６－基）－苯基）－磺醯胺及其作為醫藥之用途
JP2016113366A (ja) * 2013-03-29 2016-06-23 大鵬薬品工業株式会社 アセトアミド基を有する１，２，４−トリアジン−６−カルボキサミド誘導体
CN106061973B (zh) 2013-12-05 2019-07-09 辉瑞公司 吡咯并[2,3-d]嘧啶基、吡咯并[2,3-b]吡嗪基和吡咯并[2,3-d]吡啶基丙烯酰胺
CA2937111A1 (en) 2014-01-24 2015-07-30 Abbvie Inc. 6-phenyl- or 6-(pyridin-3-yl)indazole derivatives and methods of use
AU2015222865B2 (en) * 2014-02-28 2019-06-20 Takeda Pharmaceutical Company Limited TYK2 inhibitors and uses thereof
WO2015173683A1 (en) 2014-05-14 2015-11-19 Pfizer Inc. Pyrazolopyridines and pyrazolopyrimidines
US10519160B2 (en) 2014-07-18 2019-12-31 The General Hospital Corporation Imaging agents for neural flux
US10590086B2 (en) 2014-11-03 2020-03-17 Iomet Pharma Ltd. Pharmaceutical compound
CN105837574B (zh) 2015-02-02 2018-03-02 四川大学 N‑(3‑哌啶基)‑芳香胺衍生物及其制备方法和用途
CA2984183C (en) 2015-05-01 2021-11-09 Pfizer Inc. Pyrrolo[2,3-d]pyrimidinyl, pyrrolo[2,3-b]pyrazinyl, pyrrolo[2,3-b]pyridinyl acrylamides and epoxides thereof
EP3291794A4 (en) 2015-05-07 2019-02-13 The Trustees of Columbia University in the City of New York METHODS AND COMPOSITIONS FOR PROMOTING HAIR GROWTH
EP3865481A1 (en) 2015-11-03 2021-08-18 Topivert Pharma Limited 4,5,6,7-tetrahydro-1h-imidazo[4,5-c]pyridine and 1,4,5,6,7,8-hexahydroimidazo[4,5-d]azepine derivatives as janus kinase inhibitors
US10973913B2 (en) 2016-02-16 2021-04-13 Washington University JAK inhibitors and uses thereof
SG11201811470PA (en) 2016-06-30 2019-01-30 Daewoong Pharmaceutical Co Ltd Pyrazolopyrimidine derivatives as kinase inhibitor
WO2018049174A1 (en) 2016-09-08 2018-03-15 Synergistic Therapeutics, Llc Topical hair growth formulation
JP7082120B2 (ja) 2016-10-21 2022-06-07 ニンバス ラクシュミ， インコーポレイテッド Ｔｙｋ２阻害剤およびその使用
US20180117148A1 (en) 2016-10-28 2018-05-03 Andrew J. Holman Compounds, pharmaceutical compositions and methods of treatments of immune related diseases and disorders
KR102032418B1 (ko) * 2017-06-15 2019-10-16 한국화학연구원 접합 피리미딘 유도체, 이의 제조방법 및 이를 유효성분으로 포함하는 브루톤티로신 키나제 활성 관련 질환의 예방 또는 치료용 약학적 조성물
CN111032646B (zh) 2017-08-01 2023-01-03 施万生物制药研发Ip有限责任公司 作为jak激酶抑制剂的吡唑并和三唑并双环化合物
AU2018360059B2 (en) 2017-11-03 2023-07-13 Aclaris Therapeutics, Inc. Substituted pyrrolopyrimidine JAK inhibitors and methods of making and using the same
KR102577241B1 (ko) 2017-12-28 2023-09-11 주식회사 대웅제약 카이네이즈 저해제로서의 아미노-플루오로피페리딘 유도체
HRP20221043T1 (hr) 2017-12-28 2022-11-11 Daewoong Pharmaceutical Co., Ltd. Derivat oksi-fluoropiperidina kao inhibitor kinaze
KR102577242B1 (ko) 2017-12-28 2023-09-11 주식회사 대웅제약 카이네이즈 저해제로서의 아미노-메틸피페리딘 유도체
JP2022518741A (ja) * 2019-01-23 2022-03-16 セラヴァンス バイオファーマ アール＆ディー アイピー， エルエルシー ＪＡＫキナーゼ阻害剤としてのイミダゾ［１，５－ａ］ピリジン、１，２，４－トリアゾロ［４，３－ａ］ピリジンおよびイミダゾ［１，５－ａ］ピラジン
EP4149462A4 (en) * 2020-05-14 2024-04-24 Theravance Biopharma R&D IP, LLC ADMINISTRATION OF A GUT SELECTIVE JAK3 INHIBITOR

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