TWI606049B - 新穎激酶抑制劑 - Google Patents

新穎激酶抑制劑 Download PDF

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Publication number
TWI606049B
TWI606049B TW101114348A TW101114348A TWI606049B TW I606049 B TWI606049 B TW I606049B TW 101114348 A TW101114348 A TW 101114348A TW 101114348 A TW101114348 A TW 101114348A TW I606049 B TWI606049 B TW I606049B
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Taiwan
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pyrazolo
pyrimidin
phenyl
amine
amino
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TW101114348A
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English (en)
Chinese (zh)
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TW201245205A (en
Inventor
麥可 頌門
安德亞斯 塞姆
麥可 阿姆斯特
那丁 特勞伯
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原真股份有限公司
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    • 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
    • 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
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/02—Nasal agents, e.g. decongestants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/04—Antipruritics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/14—Decongestants or antiallergics
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Dermatology (AREA)
  • Hematology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Oncology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Biomedical Technology (AREA)
  • Urology & Nephrology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Transplantation (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Otolaryngology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
TW101114348A 2011-04-21 2012-04-23 新穎激酶抑制劑 TWI606049B (zh)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201161517582P 2011-04-21 2011-04-21

Publications (2)

Publication Number Publication Date
TW201245205A TW201245205A (en) 2012-11-16
TWI606049B true TWI606049B (zh) 2017-11-21

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Country Status (26)

Country Link
US (1) US9802937B2 (enExample)
EP (1) EP2699579B1 (enExample)
JP (1) JP6222776B2 (enExample)
KR (1) KR101649611B1 (enExample)
CN (1) CN103492389B (enExample)
AP (1) AP2013007253A0 (enExample)
AU (1) AU2012244550C1 (enExample)
BR (1) BR112013026521A2 (enExample)
CA (1) CA2831634C (enExample)
CL (1) CL2013003051A1 (enExample)
CO (1) CO6831982A2 (enExample)
CR (1) CR20130536A (enExample)
CU (1) CU20130143A7 (enExample)
EA (1) EA029040B1 (enExample)
EC (1) ECSP13012982A (enExample)
GT (1) GT201300255A (enExample)
IL (1) IL228968A (enExample)
MA (1) MA35124B1 (enExample)
MX (1) MX363696B (enExample)
PE (1) PE20140928A1 (enExample)
PH (1) PH12013502185A1 (enExample)
SG (1) SG194549A1 (enExample)
TN (1) TN2013000419A1 (enExample)
TW (1) TWI606049B (enExample)
WO (1) WO2012143144A1 (enExample)
ZA (1) ZA201307839B (enExample)

Families Citing this family (63)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20140020972A (ko) * 2011-03-28 2014-02-19 에프. 호프만-라 로슈 아게 티아졸로피리미딘 화합물
AU2012244550C1 (en) 2011-04-21 2017-06-22 Origenis Gmbh Pyrazolo [4, 3-d] pyrimidines useful as kinase inhibitors
MX2013012266A (es) 2011-04-21 2013-11-22 Gilead Sciences Inc Compuestos de benzotiazol y su uso farmaceutico.
US9376392B2 (en) 2012-01-04 2016-06-28 Gilead Sciences, Inc. 2-(tert-butoxy)-2-(7-methylquinolin-6-yl) acetic acid derivatives for treating AIDS
US9284323B2 (en) 2012-01-04 2016-03-15 Gilead Sciences, Inc. Naphthalene acetic acid derivatives against HIV infection
AR090650A1 (es) 2012-04-12 2014-11-26 Alcon Res Ltd Tratamiento para respuestas inflamatorias inducidas por microbios en el ojo
US20120323214A1 (en) * 2012-05-16 2012-12-20 Totada R Shantha Alzheimer's disease treatment with multiple therapeutic agents delivered to the olfactory region through a special delivery catheter and iontophoresis
EA025186B1 (ru) 2012-06-29 2016-11-30 Пфайзер Инк. НОВЫЕ 4-(ЗАМЕЩЕННЫЙ АМИНО)-7Н-ПИРРОЛО[2,3-d]ПИРИМИДИНЫ В КАЧЕСТВЕ ИНГИБИТОРОВ LRRK2
WO2014060112A1 (en) * 2012-10-19 2014-04-24 Origenis Gmbh Pyrazolo[4,3-d]pyrimidines as kinase inhibitors
US9440952B2 (en) 2013-03-04 2016-09-13 Merck Sharp & Dohme Corp. Compounds inhibiting leucine-rich repeat kinase enzyme activity
WO2014134774A1 (en) 2013-03-04 2014-09-12 Merck Sharp & Dohme Corp. Compounds inhibiting leucine-rich repeat kinase enzyme activity
WO2014134772A1 (en) 2013-03-04 2014-09-12 Merck Sharp & Dohme Corp. Compounds inhibiting leucine-rich repeat kinase enzyme activity
WO2014134776A1 (en) * 2013-03-04 2014-09-12 Merck Sharp & Dohme Corp. Compounds inhibiting leucine-rich repeat kinase enzyme activity
AR096654A1 (es) 2013-06-20 2016-01-27 Ab Science Derivados de benzimidazol como inhibidores selectivos de proteína quinasa
WO2015026683A1 (en) * 2013-08-22 2015-02-26 Merck Sharp & Dohme Corp. Compounds inhibiting leucine-rich repeat kinase enzyme activity
US10220034B2 (en) 2013-10-18 2019-03-05 Indiana University Research And Technology Corporation Hepatitis B viral assembly effectors
EP3083618B1 (en) 2013-12-17 2018-02-21 Pfizer Inc Novel 3,4-disubstituted-1h-pyrrolo[2,3-b]pyridines and 4,5-disubstituted-7h-pyrrolo[2,3-c]pyridazines as lrrk2 inhibitors
RU2016134751A (ru) * 2014-01-29 2018-03-02 Глэксосмитклайн Интеллекчуал Проперти Дивелопмент Лимитед Соединения
SG11201605342UA (en) 2014-01-29 2016-08-30 Glaxosmithkline Ip Dev Ltd Compounds
SG11201607990QA (en) 2014-04-25 2016-11-29 Pfizer Heteroaromatic compounds and their use as dopamine d1 ligands
EP3166637B1 (en) 2014-07-10 2020-01-29 The J. David Gladstone Institutes Compositions and methods for treating dengue virus infection
US10913744B2 (en) 2015-02-13 2021-02-09 Dana-Farber Cancer Institute, Inc. LRRK2 inhibitors and methods of making and using the same
WO2016168619A1 (en) 2015-04-17 2016-10-20 Indiana University Research And Technology Corporation Hepatitis b viral assembly effectors
JP2018518518A (ja) 2015-06-26 2018-07-12 カドモン コーポレイション,リミティド ライアビリティ カンパニー グルコース取り込み阻害剤
US10729691B2 (en) 2015-06-26 2020-08-04 Kadmon Corporation, Llc Treatment of infectious diseases with glucose uptake inhibitors
RU2722149C1 (ru) 2015-09-14 2020-05-27 Пфайзер Инк. Новые производные имидазо[4,5-c] хинолинов и имидазо[4,5-c][1,5] нафтиридинов в качестве ингибиторов LRRK2
US9762007B2 (en) 2016-02-10 2017-09-12 Dish Network L.L.C. Push on connector
US10280164B2 (en) 2016-09-09 2019-05-07 Incyte Corporation Pyrazolopyridone compounds and uses thereof
US20180072718A1 (en) 2016-09-09 2018-03-15 Incyte Corporation Pyrazolopyridine compounds and uses thereof
US20180072741A1 (en) 2016-09-09 2018-03-15 Incyte Corporation Pyrazolopyrimidine compounds and uses thereof
AR109596A1 (es) 2016-09-09 2018-12-26 Incyte Corp Compuestos pirazolopiridina y sus usos
CN109996546B (zh) 2016-09-30 2023-06-27 阿沙纳生物科学公司 P2x3和/或p2x2/3化合物及方法
CN106620315A (zh) * 2016-11-17 2017-05-10 郑州郑先医药科技有限公司 一种用于治疗风湿病的药物组合物
CN106667990A (zh) * 2016-11-17 2017-05-17 郑州郑先医药科技有限公司 一种治疗风湿病的药物
CN106580974A (zh) * 2016-12-06 2017-04-26 郑州郑先医药科技有限公司 一种治疗脊髓损伤的西药组合物及其应用
US20180153922A1 (en) 2016-12-06 2018-06-07 New York Society For The Ruptured And Crippled Maintaining The Hospital For Special Surgery Inhibition of expansion and function of pathogenic age-associated b cells and use for the prevention and treatment of autoimmune disease
US12539297B2 (en) 2017-02-07 2026-02-03 Oncocross Co., Ltd. Composition for inhibiting cancer metastasis and treating cancer
WO2018147612A1 (ko) * 2017-02-07 2018-08-16 주식회사 온코크로스 암의 전이 억제 및 치료용 조성물
WO2018152220A1 (en) 2017-02-15 2018-08-23 Incyte Corporation Pyrazolopyridine compounds and uses thereof
MX2019012431A (es) 2017-04-21 2020-08-03 Ikena Oncology Inc Inhibidores del receptor de hidrocarburos de arilo (ahr) de indol y usos de los mismos.
US10722495B2 (en) 2017-09-08 2020-07-28 Incyte Corporation Cyanoindazole compounds and uses thereof
CN108178760B (zh) * 2017-12-27 2020-02-18 安徽医科大学 一种嘧啶并吡唑杂环化合物、制备方法、用途
US10745388B2 (en) 2018-02-20 2020-08-18 Incyte Corporation Indazole compounds and uses thereof
DK3755703T3 (da) 2018-02-20 2022-06-27 Incyte Corp N-(phenyl)-2-(phenyl)pyrimidin-4-carboxamidderivater og relaterede forbindelser som hpk1-inhibitorer til behandling af kræft
US10752635B2 (en) 2018-02-20 2020-08-25 Incyte Corporation Indazole compounds and uses thereof
WO2019162964A1 (en) * 2018-02-23 2019-08-29 Indian Institute Of Science Anti-tubercular composition, and combinatorial implementations thereof
WO2019173500A1 (en) 2018-03-07 2019-09-12 Duquesne University Of The Holy Spirit PYRAZOLO[4,3-d]PYRIMIDINES AS ANTITUMOR AGENTS
US11299473B2 (en) 2018-04-13 2022-04-12 Incyte Corporation Benzimidazole and indole compounds and uses thereof
US10899755B2 (en) 2018-08-08 2021-01-26 Incyte Corporation Benzothiazole compounds and uses thereof
WO2020068729A1 (en) 2018-09-25 2020-04-02 Incyte Corporation Pyrazolo[4,3-d]pyrimidine compounds as alk2 abd/or fgfr modulators
CN109867800B (zh) * 2019-04-01 2021-04-09 江西理工大学 一种镉基金属-有机框架及其制备方法
MX2021014273A (es) * 2019-05-21 2022-01-06 Voronoi Inc Derivado de heteroarilo que contiene n y composicion farmaceutica que lo comprende como principio activo para la prevencion o el tratamiento de cancer.
WO2020247756A1 (en) * 2019-06-05 2020-12-10 Forcyte Biotechnologies, Inc. Small molecules to relax uterine smooth muscle contractions
US12533359B2 (en) 2019-07-05 2026-01-27 Icahn School Of Medicine At Mount Sinai Method for preventing hair loss
KR20220059480A (ko) 2019-08-06 2022-05-10 인사이트 코포레이션 고체 형태의 hpk1 억제제
CN110876752B (zh) * 2019-11-18 2021-04-30 暨南大学 长链非编码rna nron功能基序在制备抑制骨吸收及防治骨质疏松药物中的应用
AU2020394424A1 (en) 2019-11-26 2022-06-16 Ikena Oncology, Inc. Polymorphic carbazole derivatives and uses thereof
US12569481B2 (en) 2020-06-12 2026-03-10 Vanderbilt University Methods of treatment for gastrointestinal motility disorders
US20230392206A1 (en) * 2020-10-26 2023-12-07 Neuron23, Inc. Methods of treatment and diagnosis of parkinson's disease associated with wild-type lrrk2
KR20240055035A (ko) * 2021-08-31 2024-04-26 니뽄 다바코 산교 가부시키가이샤 6-아미노피라졸로피리미딘 화합물 및 그 의약 용도
WO2023076404A1 (en) 2021-10-27 2023-05-04 Aria Pharmaceuticals, Inc. Methods for treating systemic lupus erythematosus
JP2025539787A (ja) * 2022-11-16 2025-12-09 ヴァーンウィ セラピューティクス,インコーポレイテッド Tyk2阻害剤
WO2026123091A1 (pt) * 2024-12-12 2026-06-18 Centro Nacional De Pesquisa Em Energia E Materiais Compostos inibidores da adenosina quinase, composição farmacêutica e seus usos

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2276610A1 (en) * 1996-12-31 1998-07-09 Neurogen Corporation 3-aryl substituted pyrazolo[4,3-d]pyrimidine derivatives; corticotropin-releasing factor receptor (crf1) specific ligands
WO2002074774A1 (en) * 2001-03-16 2002-09-26 Pfizer Limited Cyclic guanosine 3',5'-monophosphate phosphodiesterase inhibitors
US6531475B1 (en) * 1998-11-12 2003-03-11 Neurocrine Biosciences, Inc. CRF receptor antagonists and methods relating thereto
EP1348707A1 (en) * 2002-03-28 2003-10-01 Ustav Experimentalni Botaniky AV CR (Institute of Experimental Botany Academy of Sciences of the Czech Republic) Pyrazolo[4,3-d]pyrimidines, processes for their preparation and methods for therapy

Family Cites Families (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4469868A (en) * 1982-05-24 1984-09-04 Warner-Lambert Company Alkylimidazo[1,2-c]pyrazolo[3,4-e]pyrimidines
GB8306481D0 (en) * 1983-03-09 1983-04-13 Beecham Group Plc Compounds
US5360720A (en) 1993-10-08 1994-11-01 Alcon Laboratories, Inc. Method of preparing human conjunctival mast cells for mast cell stabilization assays
DE19942474A1 (de) * 1999-09-06 2001-03-15 Merck Patent Gmbh Pyrazolo[4,3-d]pyrimidine
DE10113710A1 (de) 2001-03-16 2002-09-26 Joerg Rademann Oxoammoniumsalze sowie deren Verwendung
US20030139427A1 (en) * 2002-08-23 2003-07-24 Osi Pharmaceuticals Inc. Bicyclic pyrimidinyl derivatives and methods of use thereof
US7226919B2 (en) 2002-12-18 2007-06-05 Vertex Pharmaceuticals Inc. Compositions useful as inhibitors of protein kinases
MEP8409A (en) * 2004-06-02 2011-12-20 Fused heterocyclic compound
PT1881985E (pt) 2005-05-12 2011-02-01 Pfizer Formas cristalinas anidras de n-[1-(2-etoxietil)-5-(n- -etil-n-metilamino)-7-(4-metilpiridin-2-il-amino)-1h- -pirazolo[4,3-d]pirimidino-3-carbonil]metanossulfonamida
JPWO2006126718A1 (ja) 2005-05-27 2008-12-25 田辺三菱製薬株式会社 ピラゾロピリミジン誘導体
JP2007055940A (ja) 2005-08-24 2007-03-08 Astellas Pharma Inc ピラゾロピリミジン誘導体
NL2000291C2 (nl) 2005-11-10 2009-02-17 Pfizer Prod Inc 1-(1-(2-ethoxyethyl)-3-ethyl-7-(4-methylpyridin-2-ylamino)-1H- pyrazool(4,3-d)pyrimidine-5-yl)piperidine-4-carbonzuur en zouten daarvan.
CN101611035A (zh) * 2006-12-28 2009-12-23 大正制药株式会社 吡唑并嘧啶化合物
JP5496915B2 (ja) 2008-02-13 2014-05-21 シージーアイ ファーマシューティカルズ,インコーポレーテッド 6−アリール−イミダゾ[1,2−a]ピラジン誘導体、その製造方法、及びその使用方法
PE20120121A1 (es) 2008-12-08 2012-02-20 Gilead Connecticut Inc Derivados de imidazopirazina como inhibidores de syk
WO2010118367A2 (en) 2009-04-10 2010-10-14 Progenics Pharmaceuticals, Inc. Antiviral pyrimidines
KR101705158B1 (ko) 2009-05-05 2017-02-09 다나-파버 캔서 인스티튜트 인크. Egfr 억제제 및 질환 치료방법
AU2012244550C1 (en) 2011-04-21 2017-06-22 Origenis Gmbh Pyrazolo [4, 3-d] pyrimidines useful as kinase inhibitors
AR090650A1 (es) 2012-04-12 2014-11-26 Alcon Res Ltd Tratamiento para respuestas inflamatorias inducidas por microbios en el ojo

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2276610A1 (en) * 1996-12-31 1998-07-09 Neurogen Corporation 3-aryl substituted pyrazolo[4,3-d]pyrimidine derivatives; corticotropin-releasing factor receptor (crf1) specific ligands
US6531475B1 (en) * 1998-11-12 2003-03-11 Neurocrine Biosciences, Inc. CRF receptor antagonists and methods relating thereto
WO2002074774A1 (en) * 2001-03-16 2002-09-26 Pfizer Limited Cyclic guanosine 3',5'-monophosphate phosphodiesterase inhibitors
EP1348707A1 (en) * 2002-03-28 2003-10-01 Ustav Experimentalni Botaniky AV CR (Institute of Experimental Botany Academy of Sciences of the Czech Republic) Pyrazolo[4,3-d]pyrimidines, processes for their preparation and methods for therapy

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Yuan et al, Bioorganic & Medicinal Chemistry Letters, 2002, 12, p2133-2136 *

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