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)
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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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Publication of AR112348A1 publication Critical patent/AR112348A1/es

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    • 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
    • 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
    • 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
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • 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
    • A61P35/00Antineoplastic agents
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
    • 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
    • C07D413/12Heterocyclic 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
    • 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
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (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)

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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 (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BR112020002265A2 (pt) 2017-08-01 2020-07-28 Theravance Biopharma R&D Ip, Llc compostos pirazólicos e triazólicos bicíclicos como inibidores de jak quiinase
WO2020154350A1 (en) * 2019-01-23 2020-07-30 Theravance Biopharma R&D Ip, Llc Imidazo[1,5-a]pyridine, 1,2,4-triazolo[4,3-a]pyridine and imidazo[1,5-a]pyrazine as jak inhibitors
WO2021231272A1 (en) * 2020-05-14 2021-11-18 Theravance Biopharma R&D Ip, Llc Administration of gut-selective jak3 inhibitor
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
WO2022033544A1 (zh) * 2020-08-13 2022-02-17 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
US20240190845A1 (en) * 2021-03-29 2024-06-13 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
CA3219092A1 (en) * 2021-05-03 2022-11-10 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
BR0209047A (pt) 2001-04-20 2004-08-10 Wyeth Corp Derivados de heterociclilalcóxi-, -alquiltio- e -alquilaminobenzazol como ligantes de 5-hidroxitriptamina-6
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
ATE469888T1 (de) 2003-05-22 2010-06-15 Abbott Lab Indazol-, benzisoxazol- und benzisothiazol- kinaseinhibitoren
EP1647549A1 (en) 2004-10-14 2006-04-19 Laboratoire Theramex Indazoles, benzisoxazoles and benzisothiazoles as estrogenic agents
US20070104780A1 (en) 2005-10-25 2007-05-10 Lipari John M Formulation comprising a drug of low water solubility and method of use thereof
US20090247554A1 (en) 2006-03-30 2009-10-01 Takeda San Diego, Inc. Kinase inhibitors
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
JP5508400B2 (ja) 2008-06-05 2014-05-28 グラクソ グループ リミテッド Pi3キナーゼの阻害剤としてのベンズピラゾール誘導体
JP5502076B2 (ja) 2008-06-05 2014-05-28 グラクソ グループ リミテッド 新規化合物
ATE552255T1 (de) 2008-06-05 2012-04-15 Glaxo Group Ltd 4-aminoindazole
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
WO2011067365A1 (en) 2009-12-03 2011-06-09 Glaxo Group Limited Benzpyrazole derivatives as inhibitors of p13 kinases
EP2507226A1 (en) 2009-12-03 2012-10-10 Glaxo Group Limited Novel compounds
TW201200518A (en) 2010-03-10 2012-01-01 Kalypsys Inc Heterocyclic inhibitors of histamine receptors for the treatment of disease
WO2012061537A2 (en) 2010-11-02 2012-05-10 The Trustees Of Columbia University In The City Of New York Methods for treating hair loss disorders
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
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
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
EP2771340B1 (en) 2011-10-25 2016-04-13 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
PL2830662T3 (pl) 2012-03-29 2019-02-28 The Trustees Of Columbia University In The City Of New York Sposoby leczenia zaburzeń utraty włosów
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
JP6192839B2 (ja) 2013-12-05 2017-09-06 ファイザー・インク ピロロ[2,3−d]ピリミジニル、ピロロ[2,3−b]ピラジニル、およびピロロ[2,3−d]ピリジニルアクリルアミド
US20160376240A1 (en) 2014-01-24 2016-12-29 Abbvie Inc. 6 Phenyl or 6 Pyridin 3 YL Indazole Derivatives and Methods of Use
WO2015131080A1 (en) * 2014-02-28 2015-09-03 Nimbus Lakshmi, Inc. 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
AU2015341913B2 (en) 2014-11-03 2020-07-16 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
ES2928757T3 (es) * 2015-05-01 2022-11-22 Pfizer Acrilamidas de pirrolo[2,3-b]pirazinilo y epóxidos de las mismas como inhibidores de la Janus Quinasa
JP2018515501A (ja) 2015-05-07 2018-06-14 ザ トラスティーズ オブ コロンビア ユニバーシティ イン ザ シティ オブ ニューヨークThe Trustees Of Columbia University In The City Of New York 発毛を促進する方法及び組成物
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
WO2017143014A1 (en) 2016-02-16 2017-08-24 Brian Kim Jak inhibitors and uses thereof
JP2019519579A (ja) 2016-06-30 2019-07-11 デウン ファーマシューティカル カンパニー リミテッド キナーゼ阻害剤としてのピラゾロピリミジン誘導体
EP3509572A4 (en) 2016-09-08 2020-05-13 Synergistic Therapeutics, LLC TOPICAL FORMULATION FOR HAIR GROWTH
WO2018075937A1 (en) 2016-10-21 2018-04-26 Nimbus Lakshmi, Inc. Tyk2 inhibitors and uses thereof
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
BR112020002265A2 (pt) 2017-08-01 2020-07-28 Theravance Biopharma R&D Ip, Llc compostos pirazólicos e triazólicos bicíclicos como inibidores de jak quiinase
CN111566095B (zh) 2017-11-03 2024-09-27 阿克拉瑞斯治疗股份有限公司 被取代的吡咯并吡啶jak抑制剂及其制造方法和使用方法
TN2020000082A1 (en) 2017-12-28 2022-01-06 Dae Woong Pharma Oxy-fluoropiperidine derivative as kinase inhibitor
KR102577242B1 (ko) 2017-12-28 2023-09-11 주식회사 대웅제약 카이네이즈 저해제로서의 아미노-메틸피페리딘 유도체
KR102577241B1 (ko) 2017-12-28 2023-09-11 주식회사 대웅제약 카이네이즈 저해제로서의 아미노-플루오로피페리딘 유도체
WO2020154350A1 (en) * 2019-01-23 2020-07-30 Theravance Biopharma R&D Ip, Llc Imidazo[1,5-a]pyridine, 1,2,4-triazolo[4,3-a]pyridine and imidazo[1,5-a]pyrazine as jak inhibitors
WO2021231272A1 (en) * 2020-05-14 2021-11-18 Theravance Biopharma R&D Ip, Llc Administration of gut-selective jak3 inhibitor

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