BR112021002479A2 - composto, composição farmacêutica, método para inibir a atividade de itk ou jak3 em uma população de células, método para tratar um distúrbio mediado por itk ou jak3 em um indivíduo necessitando do mesmo e uso de um composto - Google Patents

composto, composição farmacêutica, método para inibir a atividade de itk ou jak3 em uma população de células, método para tratar um distúrbio mediado por itk ou jak3 em um indivíduo necessitando do mesmo e uso de um composto Download PDF

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Publication number
BR112021002479A2
BR112021002479A2 BR112021002479-4A BR112021002479A BR112021002479A2 BR 112021002479 A2 BR112021002479 A2 BR 112021002479A2 BR 112021002479 A BR112021002479 A BR 112021002479A BR 112021002479 A2 BR112021002479 A2 BR 112021002479A2
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BR
Brazil
Prior art keywords
pyrrolo
amino
prop
pyrimidin
methylpiperidin
Prior art date
Application number
BR112021002479-4A
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English (en)
Portuguese (pt)
Inventor
Eric Jacobsen
David Anderson
James Blinn
Susan Hockerman
Richard HEIER
Paramita Mukherjee
Original Assignee
Aclaris Therapeutics, Inc.
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Filing date
Publication date
Application filed by Aclaris Therapeutics, Inc. filed Critical Aclaris Therapeutics, Inc.
Publication of BR112021002479A2 publication Critical patent/BR112021002479A2/pt

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    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • 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
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • 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
    • 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
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Dermatology (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
BR112021002479-4A 2018-08-10 2019-08-12 composto, composição farmacêutica, método para inibir a atividade de itk ou jak3 em uma população de células, método para tratar um distúrbio mediado por itk ou jak3 em um indivíduo necessitando do mesmo e uso de um composto BR112021002479A2 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201862717400P 2018-08-10 2018-08-10
US62/717,400 2018-08-10
PCT/US2019/046182 WO2020033955A1 (en) 2018-08-10 2019-08-12 Pyrrolopyrimidine itk inhibitors

Publications (1)

Publication Number Publication Date
BR112021002479A2 true BR112021002479A2 (pt) 2021-07-27

Family

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BR112021002479-4A BR112021002479A2 (pt) 2018-08-10 2019-08-12 composto, composição farmacêutica, método para inibir a atividade de itk ou jak3 em uma população de células, método para tratar um distúrbio mediado por itk ou jak3 em um indivíduo necessitando do mesmo e uso de um composto

Country Status (13)

Country Link
US (4) US11021482B2 (https=)
EP (1) EP3833350A4 (https=)
JP (2) JP7591500B2 (https=)
KR (1) KR102849047B1 (https=)
CN (2) CN119080779A (https=)
AU (1) AU2019317625B2 (https=)
BR (1) BR112021002479A2 (https=)
CA (1) CA3109192A1 (https=)
IL (1) IL280593A (https=)
MX (1) MX2021001558A (https=)
PH (1) PH12021550187A1 (https=)
SG (1) SG11202100525SA (https=)
WO (1) WO2020033955A1 (https=)

Families Citing this family (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20190043437A (ko) 2017-10-18 2019-04-26 씨제이헬스케어 주식회사 단백질 키나제 억제제로서의 헤테로고리 화합물
KR102821964B1 (ko) 2017-11-03 2025-06-19 어클라리스 쎄라퓨틱스, 인코포레이티드 치환된 피롤로피리미딘 jak 억제제 및 이의 제조 및 사용 방법
CN119080779A (zh) * 2018-08-10 2024-12-06 阿克拉瑞斯治疗股份有限公司 吡咯并嘧啶itk抑制剂
KR102195348B1 (ko) 2018-11-15 2020-12-24 에이치케이이노엔 주식회사 단백질 키나제 억제제로서의 신규 화합물 및 이를 포함하는 약제학적 조성물
CA3138544A1 (en) 2019-05-02 2020-11-05 Aclaris Therapeutics, Inc. Substituted pyrrolopyridines as jak inhibitors
CA3152752A1 (en) 2019-10-01 2021-04-08 Thomas Henley Genetic engineering of fungi to modulate tryptamine expression
CN115867272A (zh) * 2020-05-14 2023-03-28 施万生物制药研发Ip有限责任公司 肠道选择性jak3抑制剂的给药
KR102560138B1 (ko) * 2020-06-15 2023-07-27 경북대학교 산학협력단 신경교세포 표현형 기반의 siRNA 다중 스크리닝을 통해 선별된 신경교세포 인산화효소의 신경염증 조절 용도
CN114887080B (zh) * 2020-12-08 2023-10-31 深圳瑞吉生物科技有限公司 一种mRNA剂型的免疫抑制剂及其在制备肿瘤治疗药物中的应用
CN113350346B (zh) * 2021-06-01 2023-06-27 广西医科大学第一附属医院 长春新碱在预防或治疗心肌纤维化中的应用
KR20230019801A (ko) * 2021-08-02 2023-02-09 한국화학연구원 신규한 피롤로 피리미딘 유도체 화합물, 이의 제조방법, 및 이를 유효성분으로 포함하는 대사성 간질환의 예방 또는 치료용 약학적 조성물
CN113571191A (zh) * 2021-08-31 2021-10-29 复旦大学附属中山医院 免疫检查点抑制剂相关mace发生风险的预测方法
WO2023110843A1 (en) * 2021-12-15 2023-06-22 Almirall, S.A. Heterobicyclic derivatives as itk inhibitors
CN118984868A (zh) 2021-12-31 2024-11-19 恩派瑞安神经科学公司 用于产生精神药物生物碱的遗传修饰的生物体
WO2024102778A1 (en) * 2022-11-08 2024-05-16 Aclaris Therapeutics, Inc. Pyrrolopyrimidine compositions for treatment of itk mediated conditions
CN116115760A (zh) * 2022-12-15 2023-05-16 浙江大学 Eed抑制剂在制备治疗神经免疫性疾病药物中的应用
WO2025144781A1 (en) * 2023-12-28 2025-07-03 Aclaris Therapeutics, Inc. Crystalline polymorph of an itk inhibitor
WO2025144783A1 (en) * 2023-12-28 2025-07-03 Aclaris Therapeutics, Inc. Methods of synthesizing substituted pyrrolopyrimidine compounds
CN117982685B (zh) * 2024-01-26 2025-05-30 北京大学人民医院 用于骨肉瘤检测的光学分子成像探针及其制备方法和应用
WO2025181247A1 (en) * 2024-02-28 2025-09-04 Almirall, S.A. Heterobicyclic derivatives as itk inhibitors
WO2025235366A1 (en) * 2024-05-07 2025-11-13 Aclaris Therapeutics, Inc. Pyrrolopyrimidine compositions for treatment of atopic dermatitis

Family Cites Families (40)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE69422306T4 (de) 1993-11-30 2000-09-07 G.D. Searle & Co., Chicago Substituierte pyrazolyl-benzolsulfonamide zur behandlung von entzündungen
PA8474101A1 (es) 1998-06-19 2000-09-29 Pfizer Prod Inc Compuestos de pirrolo [2,3-d] pirimidina
WO2000000202A1 (en) 1998-06-30 2000-01-06 Parker Hughes Institute Method for inhibiting c-jun expression using jak-3 inhibitors
US7135575B2 (en) 2003-03-03 2006-11-14 Array Biopharma, Inc. P38 inhibitors and methods of use thereof
SE0301372D0 (sv) 2003-05-09 2003-05-09 Astrazeneca Ab Novel compounds
AR054416A1 (es) 2004-12-22 2007-06-27 Incyte Corp Pirrolo [2,3-b]piridin-4-il-aminas y pirrolo [2,3-b]pirimidin-4-il-aminas como inhibidores de las quinasas janus. composiciones farmaceuticas.
EP2354140A1 (en) 2005-05-20 2011-08-10 Vertex Pharmaceuticals Incorporated Pyrrolopyridines useful as inhibitors of protein kinase
CN102127078A (zh) 2005-07-14 2011-07-20 安斯泰来制药株式会社 Janus激酶3的杂环类抑制剂
WO2007007919A2 (en) 2005-07-14 2007-01-18 Astellas Pharma Inc. Heterocyclic janus kinase 3 inhibitors
SG10202003901UA (en) 2005-12-13 2020-05-28 Incyte Holdings Corp Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as janus kinase inhibitors
US8071779B2 (en) 2006-12-18 2011-12-06 Inspire Pharmaceuticals, Inc. Cytoskeletal active rho kinase inhibitor compounds, composition and use
AR064879A1 (es) 2007-01-12 2009-04-29 Astellas Pharma Inc Compuesto de piridina condensado
KR20150036210A (ko) 2007-06-13 2015-04-07 인사이트 코포레이션 야누스 키나제 억제제(R)―3―(4―(7H―피롤로[2,3-d]피리미딘―4―일)―1H―피라졸―1―일)―3―사이클로펜틸프로판니트릴의 염
CL2009001884A1 (es) 2008-10-02 2010-05-14 Incyte Holdings Corp Uso de 3-ciclopentil-3-[4-(7h-pirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il)propanonitrilo, inhibidor de janus quinasa, y uso de una composición que lo comprende para el tratamiento del ojo seco.
AR076794A1 (es) 2009-05-22 2011-07-06 Incyte Corp Derivados de n-(hetero)aril-pirrolidina de pirazol-4-il-pirrolo [2,3-d]pirimidinas y pirrol-3-il-pirrolo [2,3-d ]pirimidinas como inhibidores de la quinasa janus y composiciones farmaceuticas que los contienen
SI2432472T1 (sl) 2009-05-22 2019-11-29 Incyte Holdings Corp 3-(4-(7H-pirolo(2,3-d)pirimidin-4-il)-1H-pirazol-1-il)oktan- ali heptan-nitril kot inhibitorji JAK
WO2012058645A1 (en) 2010-10-29 2012-05-03 Biogen Idec Ma Inc. Heterocyclic tyrosine kinase inhibitors
PE20140146A1 (es) 2010-11-19 2014-02-06 Incyte Corp Derivados de pirrolopiridina y pirrolopirimidina sustituidos con ciclobutilo como inhibidores de jak
AU2012295802B2 (en) 2011-08-12 2017-03-30 Nissan Chemical Industries, Ltd. Tricyclic heterocyclic compounds and JAK inhibitors
EP2788000B1 (en) 2011-12-06 2018-05-30 Merck Sharp & Dohme Corp. Pyrrolopyrimidines as janus kinase inhibitors
PT3889181T (pt) 2012-09-07 2024-05-29 Regeneron Pharma Um anticorpo antagonista de il-4r para utilização no tratamento da dermatite atópica por administração
US9206188B2 (en) * 2013-04-18 2015-12-08 Arrien Pharmaceuticals Llc Substituted pyrrolo[2,3-b]pyridines as ITK and JAK inhibitors
GB2515785A (en) * 2013-07-03 2015-01-07 Redx Pharma Ltd Compounds
SI3077395T1 (en) * 2013-12-05 2018-03-30 Pfizer Inc. Pyrrolo(2,3-d)pyrimidinyl, pyrrolo(2,3-b)pyrazinyl and pyrrolo(2,3-d)pyridinyl acrylamides
EP2924026A1 (en) 2014-03-28 2015-09-30 Novartis Tiergesundheit AG Aminosulfonylmethylcyclohexanes as JAK inhibitors
KR20170002623A (ko) 2014-05-14 2017-01-06 화이자 인코포레이티드 피라졸로피리딘 및 피라졸로피리미딘
CN105777756B (zh) * 2014-07-02 2019-03-01 广东东阳光药业有限公司 杂芳化合物及其在药物中的应用
CN105712998B (zh) * 2014-12-05 2019-12-13 上海润诺生物科技有限公司 氮杂吲哚类衍生物、其制备方法及其在医药上的应用
EP3247353A4 (en) * 2015-01-23 2018-07-04 Confluence Life Sciences, Inc. Heterocyclic itk inhibitors for treating inflammation and cancer
EP3288943B1 (en) * 2015-05-01 2022-09-28 Pfizer Inc. Pyrrolo[2,3-b]pyrazinyl acrylamides and epoxides thereof as inhibitors of janus kinase
ES2830446T3 (es) 2015-12-11 2021-06-03 Sichuan Kelun Biotech Biopharmaceutical Co Ltd Derivado de azetidina, método de preparación del mismo y uso del mismo
MX388591B (es) * 2016-06-30 2025-03-20 Daewoong Pharmaceutical Co Ltd Derivados de pirazolopirimidina como inhibidor de cinasa.
TW201811795A (zh) * 2016-08-24 2018-04-01 美商亞闊股份有限公司 胺基-吡咯并嘧啶酮化合物及其用途
WO2019090143A1 (en) 2017-11-03 2019-05-09 Aclaris Therapeutics, Inc. Pyrazolyl pyrrolo[2,3-b]pyrimidine-5-carboxylate analogs and methods of making the same
KR102821964B1 (ko) 2017-11-03 2025-06-19 어클라리스 쎄라퓨틱스, 인코포레이티드 치환된 피롤로피리미딘 jak 억제제 및 이의 제조 및 사용 방법
CN119080779A (zh) * 2018-08-10 2024-12-06 阿克拉瑞斯治疗股份有限公司 吡咯并嘧啶itk抑制剂
JP7624922B2 (ja) 2018-12-19 2025-01-31 インサイト・コーポレイション 胃腸疾患の治療のためのjak1経路阻害剤
CA3138544A1 (en) 2019-05-02 2020-11-05 Aclaris Therapeutics, Inc. Substituted pyrrolopyridines as jak inhibitors
JP7532511B2 (ja) 2019-06-10 2024-08-13 インサイト・コーポレイション Jak阻害剤による尋常性白斑の局所治療
US20220235043A1 (en) 2019-07-31 2022-07-28 Aclaris Therapeutics, Inc. Substituted sulfonamide pyrrolopyridines as jak inhibitors

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Publication number Publication date
US20240132505A1 (en) 2024-04-25
EP3833350A1 (en) 2021-06-16
AU2019317625A1 (en) 2021-02-18
JP7591500B2 (ja) 2024-11-28
US20200048262A1 (en) 2020-02-13
JP2025037892A (ja) 2025-03-18
SG11202100525SA (en) 2021-02-25
CN119080779A (zh) 2024-12-06
KR20210044822A (ko) 2021-04-23
MX2021001558A (es) 2021-04-28
CN112823005A (zh) 2021-05-18
US11820775B2 (en) 2023-11-21
AU2019317625B2 (en) 2025-02-27
US11021482B2 (en) 2021-06-01
CN112823005B (zh) 2024-08-20
PH12021550187A1 (en) 2022-02-14
EP3833350A4 (en) 2022-05-18
WO2020033955A1 (en) 2020-02-13
US20260035373A1 (en) 2026-02-05
JP2021534244A (ja) 2021-12-09
IL280593A (en) 2021-03-25
CA3109192A1 (en) 2020-02-13
US20220348579A1 (en) 2022-11-03
KR102849047B1 (ko) 2025-08-22
US12297203B2 (en) 2025-05-13

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