JP7038063B2 - ピラゾロ［１，５－ａ］ピリミジニルカルボキサミド化合物および医学的障害の処置におけるその使用 - Google Patents

ピラゾロ［１，５－ａ］ピリミジニルカルボキサミド化合物および医学的障害の処置におけるその使用 Download PDF

Info

Publication number
JP7038063B2
JP7038063B2 JP2018552683A JP2018552683A JP7038063B2 JP 7038063 B2 JP7038063 B2 JP 7038063B2 JP 2018552683 A JP2018552683 A JP 2018552683A JP 2018552683 A JP2018552683 A JP 2018552683A JP 7038063 B2 JP7038063 B2 JP 7038063B2
Authority
JP
Japan
Prior art keywords
alkyl
substituted
cycloalkyl
alkoxyl
certain embodiments
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.)
Expired - Fee Related
Application number
JP2018552683A
Other languages
English (en)
Japanese (ja)
Other versions
JP2019510790A5 (OSRAM
JP2019510790A (ja
Inventor
レナート・ティ・スケルリ
エリーズ・マリー・ジョゼ・ブルク
ピーター・ティ・ランズベリー
アンドリュー・シー・グッド
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.)
Lysosomal Therapeutics Inc
Original Assignee
Lysosomal Therapeutics Inc
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 Lysosomal Therapeutics Inc filed Critical Lysosomal Therapeutics Inc
Publication of JP2019510790A publication Critical patent/JP2019510790A/ja
Publication of JP2019510790A5 publication Critical patent/JP2019510790A5/ja
Application granted granted Critical
Publication of JP7038063B2 publication Critical patent/JP7038063B2/ja
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • 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
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/08—Antiepileptics; Anticonvulsants
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P25/22—Anxiolytics
    • 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
    • A61P25/24—Antidepressants
    • 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
    • A61P25/28—Drugs 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
    • 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
    • A61P27/06—Antiglaucoma agents or miotics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • 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
    • A61P7/06—Antianaemics

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Psychiatry (AREA)
  • Diabetes (AREA)
  • Hospice & Palliative Care (AREA)
  • Ophthalmology & Optometry (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Pain & Pain Management (AREA)
  • Reproductive Health (AREA)
  • Psychology (AREA)
  • Epidemiology (AREA)
  • Obesity (AREA)
  • Emergency Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
JP2018552683A 2016-04-06 2017-04-06 ピラゾロ［１，５－ａ］ピリミジニルカルボキサミド化合物および医学的障害の処置におけるその使用 Expired - Fee Related JP7038063B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201662318929P 2016-04-06 2016-04-06
US62/318,929 2016-04-06
PCT/US2017/026280 WO2017176960A1 (en) 2016-04-06 2017-04-06 Pyrazolo[1,5-a]pyrimidinyl carboxamide compounds and their use in the treatment of medical disorders

Publications (3)

Publication Number Publication Date
JP2019510790A JP2019510790A (ja) 2019-04-18
JP2019510790A5 JP2019510790A5 (OSRAM) 2021-11-04
JP7038063B2 true JP7038063B2 (ja) 2022-03-17

Family

ID=60001526

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2018552683A Expired - Fee Related JP7038063B2 (ja) 2016-04-06 2017-04-06 ピラゾロ［１，５－ａ］ピリミジニルカルボキサミド化合物および医学的障害の処置におけるその使用

Country Status (12)

Country Link
US (4) US11192892B2 (OSRAM)
EP (1) EP3440080A4 (OSRAM)
JP (1) JP7038063B2 (OSRAM)
KR (2) KR20180133461A (OSRAM)
CN (1) CN109311887B (OSRAM)
AU (1) AU2017246455B2 (OSRAM)
BR (1) BR112018070586A8 (OSRAM)
CA (1) CA3020287A1 (OSRAM)
IL (1) IL262177B (OSRAM)
MX (1) MX2018012211A (OSRAM)
SG (1) SG11201808830YA (OSRAM)
WO (1) WO2017176960A1 (OSRAM)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2958391T3 (es) 2014-11-06 2024-02-08 Bial R&D Invest S A Imidazo[1,5-a]pirimidinas sustituidas y su uso en el tratamiento de trastornos médicos
DK3215511T3 (da) 2014-11-06 2024-05-13 Bial R&D Invest S A Substituerede pyrazolo(1,5-a)pyrimidiner og deres anvendelse i behandlingen af medicinske lidelser
CA2966581A1 (en) 2014-11-06 2016-05-12 Lysosomal Therapeutics Inc. Substituted pyrrolo[1,2-a]pyrimidines and their use in the treatment of medical disorders
JP7046827B2 (ja) * 2016-04-06 2022-04-04 リソソーマル・セラピューティクス・インコーポレイテッド イミダゾ［１，５－ａ］ピリミジニルカルボキサミド化合物および医学的障害の処置におけるその使用
WO2017176960A1 (en) 2016-04-06 2017-10-12 Lysosomal Therapeutics Inc. Pyrazolo[1,5-a]pyrimidinyl carboxamide compounds and their use in the treatment of medical disorders
WO2017176962A1 (en) 2016-04-06 2017-10-12 Lysosomal Therapeutics, Inc. Pyrrolo[1,2-a]pyrimidinyl carboxamide compounds and their use in the treatment of medical disorders
US11345698B2 (en) 2016-05-05 2022-05-31 Bial—R&D Investments, S.A. Substituted imidazo[1,2-a]pyridines, substituted imidazo[1,2-a]pyrazines, related compounds, and their use in the treatment of medical disorders
BR112018072552A8 (pt) 2016-05-05 2023-03-14 Lysosomal Therapeutics Inc Compostos de imidazo [1,2-b]piridazinas e imidazo [1,5-b] piridazinas substituídas, composição farmacêutica que os compreende e seu uso no tratamento de distúrbios médicos
CN110698484B (zh) * 2019-06-05 2021-11-05 陕西理工大学 含吡唑并[1,5-a]嘧啶的衍生物、药用组合物及应用
CN115108972A (zh) * 2022-08-29 2022-09-27 北京迪泰医药科技有限公司 一种2-甲基-3-氟-5-溴吡啶的合成方法
WO2025014639A2 (en) * 2023-07-07 2025-01-16 The Johns Hopkins University Neutral sphingomyelinase inhibitors
WO2025146216A1 (zh) * 2024-01-05 2025-07-10 成都赜灵生物医药科技有限公司 六并五氮杂环酰胺类化合物及其用途
CN118184599A (zh) * 2024-02-29 2024-06-14 重庆药友制药有限责任公司 一种阿莫奈韦中间体的制备方法

Citations (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2004277337A (ja) 2003-03-14 2004-10-07 Sumitomo Pharmaceut Co Ltd ピラゾロ［１，５−ａ］ピリミジン誘導体
WO2005113004A2 (en) 2004-05-14 2005-12-01 The Cleveland Clinic Founfation Small molecule inhibitors for mrp1 and other multidrug transporters
WO2007048066A2 (en) 2005-10-21 2007-04-26 Exelixis, Inc. Pyrazolo-pyrimidines as casein kinase ii (ck2) modulators
JP2008530155A (ja) 2005-02-17 2008-08-07 バイエル・クロツプサイエンス・アクチエンゲゼルシヤフト ピラゾロピリミジン類
WO2010086040A1 (en) 2009-01-29 2010-08-05 Biomarin Iga, Ltd. Pyrazolo-pyrimidines for treatment of duchenne muscular dystrophy
WO2012075393A2 (en) 2010-12-02 2012-06-07 President And Fellows Of Harvard College Activators of proteasomal degradation and uses thereof
WO2012078855A1 (en) 2010-12-08 2012-06-14 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Substituted pyrazolopyrimidines as glucocerebrosidase activators
WO2014141129A2 (en) 2013-03-14 2014-09-18 Grueneberg Dorre A Novel methods, compounds, and compositions for inhibition of ros
WO2015012328A1 (ja) 2013-07-24 2015-01-29 武田薬品工業株式会社 複素環化合物
WO2015073267A1 (en) 2013-11-15 2015-05-21 Calitor Sciences, Llc Substituted heteroaryl compounds and methods of use

Family Cites Families (94)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4838925A (en) 1986-04-25 1989-06-13 E. I. Du Pont De Nemours And Company Heterocyclic acyl sulfonamides
JP3763997B2 (ja) 1999-05-13 2006-04-05 富士写真フイルム株式会社 感熱記録材料
JP4331823B2 (ja) 1999-05-21 2009-09-16 富士フイルム株式会社 ピロロ［１，２−ａ］−１，３，５−トリアジン−４−オン系化合物
AU2930501A (en) 2000-01-07 2001-07-24 Transform Pharmaceuticals, Inc. High-throughput formation, identification, and analysis of diverse solid-forms
TWI243164B (en) 2001-02-13 2005-11-11 Aventis Pharma Gmbh Acylated indanyl amines and their use as pharmaceuticals
JP4070966B2 (ja) 2001-06-28 2008-04-02 株式会社カネボウ化粧品 新規ガラクトシルセラミド類縁体及び用途
DE60206952T2 (de) 2001-10-22 2006-06-22 Pfizer Inc. Imidazopyridinverbindungen als 5-ht4-rezeptormodulatoren
CN1281606C (zh) 2002-03-01 2006-10-25 安斯泰来制药有限公司 含氮杂环化合物
JP2006502180A (ja) 2002-09-20 2006-01-19 ファイザー株式会社 ５−ｈｔ４レセプターモジュレーターとしてのｎ−置換されたピペリジニル−イミダゾピリジン化合物
DOP2003000703A (es) 2002-09-20 2004-03-31 Pfizer Compuestos de imidazopiradina como agonistas del receptor 5-ht4
WO2004052315A2 (en) 2002-12-11 2004-06-24 Merck & Co., Inc. Tyrosine kinase inhibitors
MXPA05011270A (es) 2003-04-21 2006-01-24 Pfizer Compuestos de imidazopiridina que tienen actividad agonista del receptor 5-ht4 y actividad antagonista del receptor 5-ht3.
AU2004289327A1 (en) 2003-11-12 2005-05-26 Amicus Therapeutics Inc. Glucoimidazole and polyhydroxycyclohexenyl amine derivatives to treat Gaucher disease
GB0329214D0 (en) 2003-12-17 2004-01-21 Glaxo Group Ltd Novel compounds
GB0400812D0 (en) 2004-01-14 2004-02-18 Celltech R&D Ltd Novel compounds
CN1922183B (zh) 2004-02-18 2010-05-26 万有制药株式会社 含氮的稠合杂芳环衍生物
RU2378277C2 (ru) 2004-06-21 2010-01-10 Ф. Хоффманн-Ля Рош Аг Производные пиразолпиримидина
ATE390424T1 (de) 2004-08-02 2008-04-15 Sanol Arznei Schwarz Gmbh Carboxamide des indolizins und seiner aza- und diazaderivate
DE102004049363A1 (de) 2004-10-08 2006-04-13 Henkel Kgaa Mittel zum Färben von keratinhaltigen Fasern
CA2593264C (en) 2005-01-19 2012-09-25 Merck & Co., Inc. Bicyclic pyrimidines as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes
JP4708438B2 (ja) * 2005-02-11 2011-06-22 エフ．ホフマン−ラ ロシュ アーゲー ｍＧｌｕＲ２アンタゴニストとしてのピラゾロピリミジン誘導体
TW200720231A (en) 2005-04-21 2007-06-01 Dainippon Sumitomo Pharma Co An n-substituted phenylacetamide derivative and a pharmaceutical composition thereof
JP5079500B2 (ja) 2005-04-28 2012-11-21 協和発酵キリン株式会社 ２−アミノキナゾリン誘導体
US7632837B2 (en) 2005-06-17 2009-12-15 Bristol-Myers Squibb Company Bicyclic heterocycles as cannabinoid-1 receptor modulators
US7723336B2 (en) 2005-09-22 2010-05-25 Bristol-Myers Squibb Company Fused heterocyclic compounds useful as kinase modulators
TW200745128A (en) 2005-10-06 2007-12-16 Schering Corp Pyrazolopyrimidines as protein kinase inhibitors
TWI372760B (en) * 2005-10-21 2012-09-21 Mitsubishi Tanabe Pharma Corp A pyrazolo[1,5-a]pyrimidine compound
WO2007065664A2 (en) 2005-12-08 2007-06-14 Novartis Ag Pyrazolo[1,5-a]pyridine-3-carboxylic acids as ephb and vegfr2 kinase inhibitors
TW200800997A (en) 2006-03-22 2008-01-01 Astrazeneca Ab Chemical compounds
AU2007260812B2 (en) 2006-06-23 2012-08-16 Amicus Therapeutics, Inc. Method for the treatment of neurological disorders by enhancing the activity of beta-glucocerebrosidase
AR061793A1 (es) 2006-07-05 2008-09-24 Mitsubishi Tanabe Pharma Corp Compuesto de pirazolo[1,5-a] pirimidina y composicion farmaceutica
US7553846B2 (en) 2006-08-07 2009-06-30 Albany Molecular Research, Inc. 2-alkylbenzoxazole carboxamides as 5-HT3 modulators
EP2102211A2 (en) 2006-11-20 2009-09-23 Alantos Pharmaceuticals Holding, Inc. Heterobicyclic metalloprotease inhibitors
AU2007321923A1 (en) 2006-11-20 2008-05-29 Alantos Pharmaceuticals Holding, Inc. Heterobicyclic matrix metalloprotease inhibitors
EP2137187A1 (en) 2007-03-28 2009-12-30 Inovacia AB Pyrazolo [1,5-a]pyrimidines as inhibitors of stearoyl-coa desaturase
AR067326A1 (es) 2007-05-11 2009-10-07 Novartis Ag Imidazopiridinas y pirrolo -pirimidinas sustituidas como inhibidores de cinasa de lipido
KR20100035635A (ko) 2007-06-21 2010-04-05 아이알엠 엘엘씨 단백질 키나제 억제제 및 그의 사용 방법
WO2009060835A1 (ja) 2007-11-05 2009-05-14 Kyoto University 新規ユビキリン結合性小分子
EP2217601A1 (en) 2007-11-08 2010-08-18 Centro Nacional de Investigaciones Oncológicas (CNIO) Imidazopyridazines for use as protein kinase inhibitors
CA2706946A1 (en) 2007-11-28 2009-06-04 Schering Corporation 2-fluoropyrazolo[1,5-a]pyrimidines as protein kinase inhibitors
WO2009100375A1 (en) 2008-02-06 2009-08-13 Bristol-Myers Squibb Company Substituted imidazopyridazines useful as kinase inhibitors
CA2718727A1 (en) 2008-03-25 2009-10-01 Takeda Pharmaceutical Company Limited Heterocyclic compound
CA2723135A1 (en) 2008-05-01 2009-11-05 Sirtris Pharmaceuticals, Inc. Quenolines and related analogs as sirtuin modulators
CN102245605B (zh) 2008-10-14 2016-01-27 阿斯利康(瑞典)有限公司 用于治疗细菌感染的稠合、螺环杂芳族化合物
EP2348860B1 (en) 2008-10-31 2015-05-27 Genentech, Inc. Pyrazolopyrimidine jak inhibitor compounds and methods
AR077468A1 (es) * 2009-07-09 2011-08-31 Array Biopharma Inc Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa
CN102573846B (zh) 2009-08-17 2015-10-07 因特利凯公司 杂环化合物及其用途
MX358682B (es) 2010-07-13 2018-08-31 Hoffmann La Roche Derivados de pirazolo [1,5a]pirimidina y de tieno[3,2b] pirimidina como moduladores de la cinasa asociada al receptor de la interleucina 4 (irak4).
WO2012034095A1 (en) 2010-09-09 2012-03-15 Irm Llc Compounds and compositions as trk inhibitors
TW201217312A (en) 2010-09-22 2012-05-01 Gruenenthal Gmbh Substituted benzamide compounds
US9127000B2 (en) 2011-02-23 2015-09-08 Intellikine, LLC. Heterocyclic compounds and uses thereof
US9169260B2 (en) 2011-03-22 2015-10-27 Merck Sharp & Dohme Corp. Amidopyrazole inhibitors of interleukin receptor-associated kinases
US9845327B2 (en) * 2011-06-22 2017-12-19 The General Hospital Corporation Treatment of proteinopathies
PT2746265E (pt) 2011-08-18 2016-03-11 Nippon Shinyaku Co Ltd Derivado heterocíclico como inibidor de pronstaglandina-sintase microssomal (mpge)
EA026701B1 (ru) 2011-09-02 2017-05-31 Байер Интеллектуэль Проперти Гмбх Замещенные аннелированные пиримидины, способ их получения, их применение и лекарственное средство для лечения и/или профилактики заболеваний
US8961959B2 (en) 2011-10-17 2015-02-24 The Regents Of The University Of Michigan Glucosylceramide synthase inhibitors and therapeutic methods using the same
CN104394869A (zh) * 2011-10-20 2015-03-04 葛兰素史密斯克莱有限责任公司 用作沉默调节蛋白调节剂的取代的双环氮杂杂环化合物和类似物
CN104125953A (zh) 2011-12-23 2014-10-29 诺华股份有限公司 用于抑制bcl2与结合配偶体相互作用的化合物
US9340549B2 (en) 2012-03-05 2016-05-17 Amgen Inc. Oxazolidinone compounds and derivatives thereof
HK1199814A1 (en) 2012-03-09 2015-07-24 Lexicon Pharmaceuticals, Inc. Inhibition of adaptor associated kinase 1 for the treatment of pain
EP2822559B1 (en) 2012-03-09 2018-05-02 Lexicon Pharmaceuticals, Inc. Imidazo[1,2-b]pyridazine-based compounds, compositions comprising them, and uses thereof
WO2013148333A1 (en) 2012-03-28 2013-10-03 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Salicylic acid derivatives useful as glucocerebrosidase activators
WO2013178591A1 (en) 2012-05-31 2013-12-05 F. Hoffmann-La Roche Ag Aminoquinazoline and pyridopyrimidine derivatives
JP6311603B2 (ja) 2012-06-22 2018-04-18 住友化学株式会社 縮合複素環化合物
WO2014025651A1 (en) 2012-08-06 2014-02-13 Amgen Inc. Chroman derivatives as trpm8 inhibitors
WO2014037340A1 (de) 2012-09-05 2014-03-13 Bayer Cropscience Ag Verwendung substituierter 2-amidobenzimidazole, 2-amidobenzoxazole und 2-amidobenzothiazole oder deren salze als wirkstoffe gegen abiotischen pflanzenstress
AU2013344716B2 (en) 2012-11-16 2018-03-01 University Health Network Pyrazolopyrimidine compounds
HK1215579A1 (zh) 2012-11-29 2016-09-02 Karyopharm Therapeutics, Inc. 被取代的2，3-二氫苯並呋喃基化合物和其用途
BR112015012454B1 (pt) 2012-12-07 2022-07-05 Vertex Pharmaceuticals Incorporated Compostos inibidores de atr quinase, seu uso e composição farmacêutica compreendendo os mesmos
KR20140086002A (ko) 2012-12-28 2014-07-08 한미약품 주식회사 Fms 키나아제 저해 활성을 갖는 피리다진 접합고리 유도체
EP2970266B1 (en) 2013-03-15 2018-01-31 Epizyme, Inc. 1-phenoxy-3-(alkylamino)-propan-2-ol derivatives as carm1 inhibitors and uses thereof
US20160199372A1 (en) 2013-08-20 2016-07-14 Bristol-Myers Squibb Company Imidazopyridazine kinase inhibitors useful to treating a disease or disorder mediated by aak1, such as alzheimer's disease, bipolar disorder, pain, schizophrenia
EA201690458A1 (ru) 2013-08-23 2016-07-29 Инсайт Корпорейшн Фуро- и тиенопиридинкарбоксамиды, используемые в качестве ингибиторов pim-киназы
AR097543A1 (es) 2013-09-06 2016-03-23 Lexicon Pharmaceuticals Inc COMPUESTOS BASADOS EN IMIDAZO[1,2-b]PIRIDAZINA, COMPOSICIONES QUE LOS COMPRENDEN Y SUS MÉTODOS DE USO
TW201542550A (zh) 2013-09-06 2015-11-16 Lexicon Pharmaceuticals Inc 吡唑并［１，５－ａ］嘧啶基化合物、包含彼之組合物以及使用彼之方法
EP3122726B1 (en) 2014-03-27 2018-08-29 Academisch Medisch Centrum N-(5-((aryl or heteroaryl)methyloxy)pentyl)-substituted iminosugars as inhibitors of glucosylceramide synthase
TW201613925A (en) 2014-07-10 2016-04-16 Incyte Corp Imidazopyrazines as LSD1 inhibitors
ES2958391T3 (es) 2014-11-06 2024-02-08 Bial R&D Invest S A Imidazo[1,5-a]pirimidinas sustituidas y su uso en el tratamiento de trastornos médicos
CA2966581A1 (en) 2014-11-06 2016-05-12 Lysosomal Therapeutics Inc. Substituted pyrrolo[1,2-a]pyrimidines and their use in the treatment of medical disorders
DK3215511T3 (da) 2014-11-06 2024-05-13 Bial R&D Invest S A Substituerede pyrazolo(1,5-a)pyrimidiner og deres anvendelse i behandlingen af medicinske lidelser
WO2017004405A1 (en) 2015-07-01 2017-01-05 Northwestern University Substituted quinazoline compounds and uses thereof for modulating glucocerebrosidase activity
WO2017004408A1 (en) 2015-07-01 2017-01-05 Northwestern University Substituted 4-methyl-pyrrolo[1.2-a]pyrimidine-8-carboxamide compounds and uses thereof for modulating glucocerebrosidase activity
EP3344632A4 (en) 2015-09-04 2019-03-20 Lysosomal Therapeutics Inc. Heterocyclic pyrimidine compounds and their use in the treatment of medical disorders
US10065963B2 (en) 2015-11-06 2018-09-04 Incyte Corporation Heterocyclic compounds as PI3K-γ inhibitors
EP3377496B1 (en) 2015-11-18 2020-09-16 Bristol-Myers Squibb Company Imidazopyridazine compounds useful as modulators of il-12, il-23 and/or ifn alpha responses
CN108473501B (zh) 2016-02-18 2021-07-16 豪夫迈·罗氏有限公司 治疗化合物、其组合物及使用方法
WO2017176962A1 (en) 2016-04-06 2017-10-12 Lysosomal Therapeutics, Inc. Pyrrolo[1,2-a]pyrimidinyl carboxamide compounds and their use in the treatment of medical disorders
WO2017176960A1 (en) 2016-04-06 2017-10-12 Lysosomal Therapeutics Inc. Pyrazolo[1,5-a]pyrimidinyl carboxamide compounds and their use in the treatment of medical disorders
JP7046827B2 (ja) 2016-04-06 2022-04-04 リソソーマル・セラピューティクス・インコーポレイテッド イミダゾ［１，５－ａ］ピリミジニルカルボキサミド化合物および医学的障害の処置におけるその使用
EP3452045A1 (en) 2016-05-04 2019-03-13 Lysosomal Therapeutics Inc. Methods of treatment and combination therapies using gcase activator heterobicyclic and related compounds
EP3452480A4 (en) 2016-05-05 2019-11-06 Lysosomal Therapeutics Inc. SUBSTITUTED PYRROLO [1,2-] TRIAZINES AND RELATED COMPOUNDS AND THEIR USE IN THE TREATMENT OF MEDICAL DISORDERS
BR112018072552A8 (pt) 2016-05-05 2023-03-14 Lysosomal Therapeutics Inc Compostos de imidazo [1,2-b]piridazinas e imidazo [1,5-b] piridazinas substituídas, composição farmacêutica que os compreende e seu uso no tratamento de distúrbios médicos
US11345698B2 (en) 2016-05-05 2022-05-31 Bial—R&D Investments, S.A. Substituted imidazo[1,2-a]pyridines, substituted imidazo[1,2-a]pyrazines, related compounds, and their use in the treatment of medical disorders
US20200339587A1 (en) 2017-12-21 2020-10-29 Lysosomal Therapeutics Inc. Crystalline substituted cyclohexyl pyrazolo[1,5-a]pyrimidinyl carboxamide compound and therapeutic uses thereof

Patent Citations (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2004277337A (ja) 2003-03-14 2004-10-07 Sumitomo Pharmaceut Co Ltd ピラゾロ［１，５−ａ］ピリミジン誘導体
WO2005113004A2 (en) 2004-05-14 2005-12-01 The Cleveland Clinic Founfation Small molecule inhibitors for mrp1 and other multidrug transporters
JP2008530155A (ja) 2005-02-17 2008-08-07 バイエル・クロツプサイエンス・アクチエンゲゼルシヤフト ピラゾロピリミジン類
WO2007048066A2 (en) 2005-10-21 2007-04-26 Exelixis, Inc. Pyrazolo-pyrimidines as casein kinase ii (ck2) modulators
WO2010086040A1 (en) 2009-01-29 2010-08-05 Biomarin Iga, Ltd. Pyrazolo-pyrimidines for treatment of duchenne muscular dystrophy
WO2012075393A2 (en) 2010-12-02 2012-06-07 President And Fellows Of Harvard College Activators of proteasomal degradation and uses thereof
WO2012078855A1 (en) 2010-12-08 2012-06-14 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Substituted pyrazolopyrimidines as glucocerebrosidase activators
WO2014141129A2 (en) 2013-03-14 2014-09-18 Grueneberg Dorre A Novel methods, compounds, and compositions for inhibition of ros
WO2015012328A1 (ja) 2013-07-24 2015-01-29 武田薬品工業株式会社 複素環化合物
WO2015073267A1 (en) 2013-11-15 2015-05-21 Calitor Sciences, Llc Substituted heteroaryl compounds and methods of use

Non-Patent Citations (4)

* Cited by examiner, † Cited by third party
Title
AHMETAJ,Sizana，Parallel synthesis of 7-heteroaryl-pyrazolo[1,5-a]pyrimidine-3-carboxamides，Mol.Divers，2013年，17，731-743
DALINGER, IGOR L.，Liquid-phase synthesis of combinatorial libraries based on 7-trifluoromethyl-substituted pyrazolo[1,5-a]pyrimidine scaffold，Journal of Conbinatorial Chemistry [ONLINE]，2005年，7(2)，236-245
PATNAIK, S.，Discovery, Structure-Activity Relationship, and Biological Evaluation of Noninhibitory Small Molecul，Journal of Medicinal Chemistry，2012年，55(12)，5734-5748
WANG, X.，Discovery of novel pyrazolo[1,5-a]pyrimidines as potent pan-Pim inhibitors by structure- and propert，Bioorganic & Medicinal Chemistry Letters，2013年，23(11)，3149-3153

Also Published As

Publication number Publication date
RU2018138688A (ru) 2020-05-19
KR20230104752A9 (ko) 2024-11-15
US20200017507A1 (en) 2020-01-16
IL262177A (en) 2018-11-29
SG11201808830YA (en) 2018-11-29
CN109311887A (zh) 2019-02-05
EP3440080A4 (en) 2020-01-22
RU2018138688A3 (OSRAM) 2020-08-31
US10934298B2 (en) 2021-03-02
MX2018012211A (es) 2019-03-28
US9840510B1 (en) 2017-12-12
CA3020287A1 (en) 2017-10-12
KR20180133461A (ko) 2018-12-14
CN109311887B (zh) 2022-09-13
EP3440080A1 (en) 2019-02-13
KR20230104752A (ko) 2023-07-10
BR112018070586A8 (pt) 2023-03-14
US20190330213A1 (en) 2019-10-31
IL262177B (en) 2022-06-01
AU2017246455A1 (en) 2018-10-25
US12116369B2 (en) 2024-10-15
US11192892B2 (en) 2021-12-07
US20230098494A1 (en) 2023-03-30
JP2019510790A (ja) 2019-04-18
US20170349598A1 (en) 2017-12-07
WO2017176960A1 (en) 2017-10-12
BR112018070586A2 (pt) 2019-02-05
AU2017246455B2 (en) 2021-09-30

Similar Documents

Publication Publication Date Title
JP7038063B2 (ja) ピラゾロ［１，５－ａ］ピリミジニルカルボキサミド化合物および医学的障害の処置におけるその使用
JP2019510790A5 (OSRAM)
JP7046827B2 (ja) イミダゾ［１，５－ａ］ピリミジニルカルボキサミド化合物および医学的障害の処置におけるその使用
JP6291103B2 (ja) 抗ウイルス処置のための化合物および方法
AU2022200478B2 (en) Inhibitors of KEAP1-Nrf2 protein-protein interaction
JP6445560B2 (ja) Ｔｎｆ活性のモジュレーターとしての縮合三環式イミダゾール誘導体
JP7034935B2 (ja) ピロロ［１，２－ａ］ピリミジニルカルボキサミド化合物および医学的障害の処置におけるその使用
KR20190003738A (ko) 치환된 이미다조[1,2-b]피리다진, 치환된 이미다조[1,5-b]피리다진, 관련 화합물, 및 의학적 장애의 치료에서의 그의 용도
CA2926830C (en) Thiazolopyrimidinones as modulators of nmda receptor activity
US10202378B2 (en) Therapeutic compounds and uses thereof
EP4051680B1 (en) Condensed bi-heterocycles as inhibiting agents for bruton's tyrosine kinase
JP2022508953A (ja) Ｈｂｖの処置のための５員のヘテロアリールカルボキサミド化合物
KR20240026911A (ko) 골수성 세포 2 작용제 상에서 발현되는 유발 수용체로서의 헤테로고리 화합물 및 사용 방법
JP2023523241A (ja) Ｈｂｖの処置のための５員のヘテロアリールカルボキサミド化合物
TWI508968B (zh) 用於治療呼吸道融合性病毒感染的化合物
MX2012008644A (es) Inhibidores de cinasa de pirazolopiridinas.
KR20140051998A (ko) 디벤조옥세핀 유도체
JP2023546742A (ja) Ｌｐａ受容体活性に付随する症状を治療するための化合物および組成物
RU2799332C2 (ru) Пиразоло[1,5-a]пиримидинилкарбоксамиды и их применение для лечения патологических состояний
JP2025186437A (ja) Ｈｂｖの処置のための５員のヘテロアリールカルボキサミド化合物

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20200406

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20200406

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20210316

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20210615

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20210805

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20210915

A524 Written submission of copy of amendment under article 19 pct

Free format text: JAPANESE INTERMEDIATE CODE: A524

Effective date: 20210915

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20220105

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20220201

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20220307

R150 Certificate of patent or registration of utility model

Ref document number: 7038063

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

S111 Request for change of ownership or part of ownership

Free format text: JAPANESE INTERMEDIATE CODE: R313113

R350 Written notification of registration of transfer

Free format text: JAPANESE INTERMEDIATE CODE: R350

LAPS Cancellation because of no payment of annual fees