AU2017246455B2 - Pyrazolo[1,5-a]pyrimidinyl carboxamide compounds and their use in the treatment of medical disorders - Google Patents

Pyrazolo[1,5-a]pyrimidinyl carboxamide compounds and their use in the treatment of medical disorders Download PDF

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Publication number
AU2017246455B2
AU2017246455B2 AU2017246455A AU2017246455A AU2017246455B2 AU 2017246455 B2 AU2017246455 B2 AU 2017246455B2 AU 2017246455 A AU2017246455 A AU 2017246455A AU 2017246455 A AU2017246455 A AU 2017246455A AU 2017246455 B2 AU2017246455 B2 AU 2017246455B2
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alkyl
cycloalkyl
membered
alkoxyl
halogen
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AU2017246455A1 (en
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Elyse Marie Josee Bourque
Andrew C. Good
Peter T. Lansbury
Renato T. Skerlj
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Bial R&D Investments SA
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    • 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
    • A61K31/505Pyrimidines; 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
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • A61P27/06Antiglaucoma agents or miotics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06Antianaemics

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  • 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)
AU2017246455A 2016-04-06 2017-04-06 Pyrazolo[1,5-a]pyrimidinyl carboxamide compounds and their use in the treatment of medical disorders Ceased AU2017246455B2 (en)

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 (2)

Publication Number Publication Date
AU2017246455A1 AU2017246455A1 (en) 2018-10-25
AU2017246455B2 true AU2017246455B2 (en) 2021-09-30

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AU2017246455A Ceased AU2017246455B2 (en) 2016-04-06 2017-04-06 Pyrazolo[1,5-a]pyrimidinyl carboxamide compounds and their use in the treatment of medical disorders

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

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 (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007048066A2 (en) * 2005-10-21 2007-04-26 Exelixis, Inc. Pyrazolo-pyrimidines as casein kinase ii (ck2) modulators
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 (98)

* 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
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
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
NZ551424A (en) 2004-05-14 2009-10-30 Childrenaes Cancer Inst Austra Small molecule inhibitors for MRP1 and other multidrug transporters
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
DE102005007534A1 (de) 2005-02-17 2006-08-31 Bayer Cropscience Ag Pyrazolopyrimidine
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
WO2010086040A1 (en) 2009-01-29 2010-08-05 Biomarin Iga, Ltd. Pyrazolo-pyrimidines for treatment of duchenne muscular dystrophy
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 (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007048066A2 (en) * 2005-10-21 2007-04-26 Exelixis, Inc. Pyrazolo-pyrimidines as casein kinase ii (ck2) modulators
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 (12)

* Cited by examiner, † Cited by third party
Title
AHMETAJ, S. et al., "Parallel synthesis of7-heteroaryl-pyrazolo[1,5-a]pyrimidine-3- carboxamides", Molecular Diversity, (2013-01-01), vol. 17, no. 4, doi:10.1007/s11030-013-9469-3, ISSN 1381-1991, pages 731 - 743 *
CAS Registry Number 1022459-94-4 ; STN Entry Date 25 May 2008; 5-(2-furanyl)-N-[(4-methylphenyl)methyl]-7-(trifluoromethyl)- pyrazolo[1,5-a]pyrimidine-3-carboxamide *
CAS Registry Number 1090443-11-0 ; STN Entry Date 26 December 2008; N-(dicyclopropylmethyl)-5,7-dimethyl-pyrazolo[1,5-a]pyrimidine-3-carboxamide *
CAS Registry Number 1099976-59-6; STN Entry Date 3 February 2009; N-(1-cyclopropyl-4-piperidinyl)-5,7-dimethyl-pyrazolo[1,5-a]pyrimidine-3-carboxamide *
CAS Registry Number 1224940-28-6; STN Entry Date 24 May 2010; N-cyclohexyl-5-methoxy-pyrazolo[1,5-a]pyrimidine-3-carboxamide *
CAS Registry Number 1224940-60-6; STN Entry Date 24 May 2010; N-cyclohexyl-5-(ethylamino)-pyrazolo[1,5-a]pyrimidine-3-carboxamide *
CAS Registry Number 1355610-51-3; STN Entry Date 7 February 2012; (2-Cyclopentyl-1-pyrrolidinyl)(5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methanone *
CAS Registry Number 1355851-51-2; STN Entry Date 8 February 2012; (2-Cyclohexyl-1-pyrrolidinyl)pyrazolo[1,5-a]pyrimidin-3-ylmethanone *
CAS Registry Number 1424084-03-6; STN Entry Date 15 March 2013; (4-bicyclo[2.2.1]hept-2-yl-1-piperazinyl)(2-methylpyrazolo[1,5-a]pyrimidin-3-yl)methanone *
CAS Registry Number 1624709-79-0; STN Entry Date 23 September 2014; 4-cyclopentyl-1-piperazinyl)(2-methylpyrazolo[1,5-a]pyrimidin-3-yl)methanone *
CAS Registry Number 696640-82-1; STN Entry Date 21 June 2004; 7-(difluoromethyl)-5-(4-methoxyphenyl)-N-(tricyclo[3.3.1.13,7]dec-1-ylmethyl)-pyrazolo[1,5-a]pyrimidine-3-carboxamide *
CAS Registry Number 895779-11-0; STN Entry Date 25 July 2006; 5-(4-bromophenyl)-N-[(4-methoxyphenyl)methyl]-7-(trifluoromethyl)-pyrazolo[1,5-a]pyrimidine-3-carboxamide *

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