AU2015342887B2 - Substituted pyrazolo(1,5-a)pyrimidines and their use in the treatment of medical disorders - Google Patents

Substituted pyrazolo(1,5-a)pyrimidines and their use in the treatment of medical disorders Download PDF

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AU2015342887B2
AU2015342887B2 AU2015342887A AU2015342887A AU2015342887B2 AU 2015342887 B2 AU2015342887 B2 AU 2015342887B2 AU 2015342887 A AU2015342887 A AU 2015342887A AU 2015342887 A AU2015342887 A AU 2015342887A AU 2015342887 B2 AU2015342887 B2 AU 2015342887B2
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compound
mmol
substituted
certain embodiments
alkylene
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AU2015342887A1 (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
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Diabetes (AREA)
  • Psychiatry (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pain & Pain Management (AREA)
  • Epidemiology (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Hospice & Palliative Care (AREA)
  • Emergency Medicine (AREA)
  • Psychology (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
AU2015342887A 2014-11-06 2015-11-06 Substituted pyrazolo(1,5-a)pyrimidines and their use in the treatment of medical disorders Active AU2015342887B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201462076062P 2014-11-06 2014-11-06
US62/076,062 2014-11-06
PCT/US2015/059541 WO2016073895A1 (en) 2014-11-06 2015-11-06 Substituted pyrazolo(1,5-a)pyrimidines and their use in the treatment of medical disorders

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AU2015342887A1 AU2015342887A1 (en) 2017-06-15
AU2015342887B2 true AU2015342887B2 (en) 2020-09-10

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CN (2) CN107001379B (cg-RX-API-DMAC7.html)
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Families Citing this family (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9353117B2 (en) 2010-12-08 2016-05-31 The United States Of America As Represented By The Secretary, Dept. Of Health And Human Services Substituted pyrazolopyrimidines as glucocerebrosidase activators
WO2016073891A1 (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
US20170333435A1 (en) 2014-11-06 2017-11-23 Lysosomal Therapeutics Inc. Substituted imidazo[1,5-a]pyrimidines and their use in the treatment of medical disorders
CN108473498B (zh) * 2015-12-22 2021-11-02 豪夫迈·罗氏有限公司 作为IRAK4调节剂的吡唑并[1,5a]嘧啶衍生物
EP3429590A4 (en) * 2016-03-16 2020-02-19 Lysosomal Therapeutics Inc. METHOD AND COMPOSITIONS FOR THE TREATMENT OF A NEURODEGENERATIVE DISEASE IN A SUBJECT CARRIING THE SPHINGOLIPIDOSIS GENE
EP3440083A4 (en) 2016-04-06 2019-09-18 Lysosomal Therapeutics Inc. IMIDAZO [1,5-A] PYRIMIDINYL-CARBOXAMIDE COMPOUNDS AND THEIR USE IN THE TREATMENT OF MEDICAL DISORDER
JP7038063B2 (ja) 2016-04-06 2022-03-17 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 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
EP3440081A4 (en) 2016-04-06 2019-09-18 Lysosomal Therapeutics Inc. PYRROLO [1,2-A] PYRIMIDINYL-CARBOXAMIDE COMPOUNDS AND THEIR USE IN THE TREATMENT OF MEDICAL DISORDER
AU2017261291C1 (en) 2016-05-05 2022-05-26 Bial - R&D Investments, S.A. Substituted imidazo[1,2-b]pyridazines, substituted imidazo[1,5-b]pyridazines, related 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
EP3535273A1 (en) 2016-11-02 2019-09-11 H. Hoffnabb-La Roche Ag PYRAZOLO[1,5a]PYRIMIDINE DERIVATIVES AS IRAK4 MODULATORS
WO2018124001A1 (ja) 2016-12-27 2018-07-05 国立研究開発法人理化学研究所 Bmpシグナル阻害化合物
EP3562811B1 (en) 2016-12-29 2022-03-16 Minoryx Therapeutics S.L. Heteroaryl compounds and their use
CA3061236A1 (en) 2017-05-22 2018-11-29 F. Hoffmann-La Roche Ag Therapeutic compounds and compositions, and methods of use thereof
US12064414B2 (en) * 2017-12-20 2024-08-20 Aizant Drug Research Solutions Private Limited. Stable amorphous Eliglustat premix and process for the preparation thereof
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
JP7317721B2 (ja) 2018-01-31 2023-07-31 武田薬品工業株式会社 複素環化合物
IT201800006067A1 (it) * 2018-06-06 2019-12-06 Nuovi inibitori della diidroortato deidrogenasi umana (hDHODH) e loro uso mirato sul differenziamento mieloide.
AU2019360941B2 (en) 2018-10-15 2025-02-27 Takeda Pharmaceutical Company Limited TYK2 inhibitors and uses thereof
CN111217816B (zh) * 2018-11-27 2022-08-16 中国科学院上海药物研究所 一类flt3激酶抑制剂及其制备和应用
GB202211999D0 (en) * 2022-08-17 2022-09-28 Mironid Ltd Compounds and their use as PDE4 activators
WO2025198486A1 (en) 2024-03-22 2025-09-25 BIAL – R&D Investments, S.A. Process for preparing a pyrazolo[1,5-a]pyrimidinyl carboxamide compound

Citations (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005058837A1 (en) * 2003-12-17 2005-06-30 Glaxo Group Limited Benzazepine derivatives as histamine h3 antagonists
WO2007108750A1 (en) * 2006-03-22 2007-09-27 Astrazeneca Ab Pyridopyrimidine derivatives and their use as pde4 inhibitors
WO2010051549A1 (en) * 2008-10-31 2010-05-06 Genentech, Inc. Pyrazolopyrimidine jak inhibitor compounds and methods
WO2012007375A1 (en) * 2010-07-13 2012-01-19 F. Hoffmann-La Roche Ag Pyrazolo [1, 5a] pyrimidine and thieno [3, 2b] pyrimidine derivatives as irak4 modulators
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
WO2012129258A1 (en) * 2011-03-22 2012-09-27 Merck Sharp & Dohme Corp. Amidopyrazole inhibitors of interleukin receptor-associated kinases
WO2013134079A1 (en) * 2012-03-05 2013-09-12 Amgen Inc. Oxazolidinone compounds and derivatives thereof
WO2014025651A1 (en) * 2012-08-06 2014-02-13 Amgen Inc. Chroman derivatives as trpm8 inhibitors
WO2014089379A1 (en) * 2012-12-07 2014-06-12 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase

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
NZ519984A (en) 2000-01-07 2004-03-26 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
WO2003035649A1 (en) 2001-10-22 2003-05-01 Pfizer Japan Inc. Imidazopyridine compounds as 5-ht4 receptor modulators
US20050096322A1 (en) 2002-03-01 2005-05-05 Susumu Igarashi Nitrogen-containing heterocyclic compound
DOP2003000703A (es) 2002-09-20 2004-03-31 Pfizer Compuestos de imidazopiradina como agonistas del receptor 5-ht4
EP1543004A1 (en) 2002-09-20 2005-06-22 Pfizer Inc. N-substituted piperidinyl-imidazopyridine compounds as 5-ht4 receptor modulators
AU2003299651A1 (en) 2002-12-11 2004-06-30 Merck And 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.
WO2005046611A2 (en) 2003-11-12 2005-05-26 Amicus Therapeutics Inc. Glucoimidazole and polyhydroxycyclohexenyl amine derivatives to treat gaucher disease
GB0400812D0 (en) 2004-01-14 2004-02-18 Celltech R&D Ltd Novel compounds
CA2556404A1 (en) 2004-02-18 2005-08-25 Banyu Pharmaceutical Co., Ltd. Nitrogenous fused heteroaromatic ring derivative
ATE396725T1 (de) 2004-05-14 2008-06-15 Cleveland Clinic Foundation Kleinmolekülige hemmer für mrp1 und andere multiarzneimitteltransporter
JP4608542B2 (ja) 2004-06-21 2011-01-12 エフ.ホフマン−ラ ロシュ アーゲー ピラゾロピリミジン誘導体
US20080051409A1 (en) 2004-08-02 2008-02-28 Peter Gmeiner Indolizine Carboxamides and Aza and Diaza Derivatives Thereof
DE102004049363A1 (de) 2004-10-08 2006-04-13 Henkel Kgaa Mittel zum Färben von keratinhaltigen Fasern
DE602006010320D1 (de) 2005-01-19 2009-12-24 Merck & Co Inc Bicyclische pyrimidine als dipeptidylpeptidase-iv-hemmer zur behandlung bzw. prävention von diabetes
RU2402553C2 (ru) 2005-02-11 2010-10-27 Ф. Хоффманн-Ля Рош Аг ПРОИЗВОДНЫЕ ПИРАЗОЛ-ПИРИМИДИНА В КАЧЕСТВЕ АНТАГОНИСТОВ mGluR2
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
CA2624500A1 (en) 2005-10-06 2007-04-19 Schering Corporation Pyrazolopyrimidines as protein kinase inhibitors
US8372851B2 (en) 2005-10-21 2013-02-12 Exelixis, Inc. Pyrazolo pyrimidines as casein kinase II (CK2) modulators
RU2008127263A (ru) 2005-12-08 2010-01-20 Новартис АГ (CH) ПИРАЗОЛ [1,5-a] ПИРИДИН-3-КАРБОНОВЫЕ КИСЛОТЫ В КАЧЕСТВЕ ИНГИБИТОРОВ EphB-И VEGFR2-КИНАЗЫ
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
WO2008019363A2 (en) 2006-08-07 2008-02-14 Albany Molecular Research, Inc. 2-alkylbenzoxazole carboxamides as 5ht3 modulators
AU2007321924A1 (en) 2006-11-20 2008-05-29 Alantos Pharmaceuticals Holding, Inc. Heterobicyclic metalloprotease inhibitors
AU2007321923A1 (en) 2006-11-20 2008-05-29 Alantos Pharmaceuticals Holding, Inc. Heterobicyclic matrix metalloprotease inhibitors
CA2682016A1 (en) 2007-03-28 2008-10-02 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
EA201000003A1 (ru) 2007-06-21 2010-06-30 Айрм Ллк Ингибиторы протеинкиназ и способы их применения
WO2009060835A1 (ja) 2007-11-05 2009-05-14 Kyoto University 新規ユビキリン結合性小分子
US20110046127A1 (en) 2007-11-08 2011-02-24 Paolo Pevarello Imidazopyridazines for Use as Protein Kinase Inhibitors
EP2225247A1 (en) 2007-11-28 2010-09-08 Schering Corporation 2-fluoropyrazolo[1,5-a]pyrimidines as protein kinase inhibitors
EP2240488B1 (en) 2008-02-06 2016-11-02 Bristol-Myers Squibb Company Substituted imidazopyridazines useful as kinase inhibitors
CA2718727A1 (en) 2008-03-25 2009-10-01 Takeda Pharmaceutical Company Limited Heterocyclic compound
SG190603A1 (en) 2008-05-01 2013-06-28 Sirtris Pharmaceuticals Inc Quinolines and related analogs as sirtuin modulators
AU2009305203B2 (en) 2008-10-14 2013-03-07 Entasis Therapeutics Limited Fused, spirocyclic heteroaromatic compounds for the treatment of bacterial infections
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
AU2010284254B2 (en) 2009-08-17 2015-09-17 Intellikine, Llc Heterocyclic compounds and uses thereof
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
WO2012075393A2 (en) 2010-12-02 2012-06-07 President And Fellows Of Harvard College Activators of proteasomal degradation and uses thereof
EP2678016B1 (en) 2011-02-23 2016-08-10 Intellikine, LLC Heterocyclic compounds and uses thereof
EP2723384B1 (en) 2011-06-22 2018-08-29 The General Hospital Corporation Treatment of proteinopathies
HUE026671T2 (en) 2011-08-18 2016-07-28 Nippon Shinyaku Co Ltd Heterocyclic derivatives as microsomal prostaglandin E synthetase inhibitors (mPGEs)
EP2751106B1 (de) 2011-09-02 2017-10-18 Bayer Intellectual Property GmbH Substituierte annellierte pyrimidine und ihre verwendung
WO2013059119A1 (en) 2011-10-17 2013-04-25 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
BR112014015339A8 (pt) 2011-12-23 2017-06-13 Novartis Ag compostos para inibição da interação de bcl2 com parceiros de ligação
EP3235499A3 (en) 2012-03-09 2018-01-17 Lexicon Pharmaceuticals, Inc. Inhibition of adaptor associated kinase 1 for the treatment of pain
MX347917B (es) 2012-03-09 2017-05-17 Lexicon Pharmaceuticals Inc Compuestos a base de imidazo[1,2-b]piridazina, composiciones que los comprenden, y metodos para su uso.
EP2831039A1 (en) 2012-03-28 2015-02-04 The U.S.A. as represented by the Secretary, Department of Health and Human Services Salicylic acid derivatives useful as glucocerebrosidase activators
CA2870407A1 (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
JP2015532650A (ja) 2012-09-05 2015-11-12 バイエル・クロップサイエンス・アクチェンゲゼルシャフト 非生物的植物ストレスに対する活性物質としての置換された2−アミドベンズイミダゾール類、2−アミドベンゾオキサゾール類および2−アミドベンゾチアゾール類またはそれらの塩の使用
EP2920181B1 (en) 2012-11-16 2019-01-09 University Health Network Pyrazolopyrimidine compounds
US9938258B2 (en) 2012-11-29 2018-04-10 Karyopharm Therapeutics Inc. Substituted 2,3-dihydrobenzofuranyl compounds and uses thereof
KR20140086002A (ko) 2012-12-28 2014-07-08 한미약품 주식회사 Fms 키나아제 저해 활성을 갖는 피리다진 접합고리 유도체
US9963452B2 (en) 2013-03-14 2018-05-08 Augusta Pharmaceuticals Inc. Methods, compounds, and compositions for inhibition of ROS
EP2970266B1 (en) 2013-03-15 2018-01-31 Epizyme, Inc. 1-phenoxy-3-(alkylamino)-propan-2-ol derivatives as carm1 inhibitors and uses thereof
EP3026051A4 (en) 2013-07-24 2017-03-08 Takeda Pharmaceutical Company Limited Heterocyclic compound
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
WO2015027124A1 (en) 2013-08-23 2015-02-26 Incyte Corporation Furo- and thieno-pyridine carboxamide compounds useful as pim kinase inhibitors
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
WO2015073267A1 (en) 2013-11-15 2015-05-21 Calitor Sciences, Llc Substituted heteroaryl compounds and methods of use
ES2895490T3 (es) 2014-03-27 2022-02-21 Acad Medisch Ct Iminoazúcares N-(5-(bifen-4-ilmetiloxi)pentil)-sustituidos como inhibidores de glucosilceramida sintasa
TW201613925A (en) 2014-07-10 2016-04-16 Incyte Corp Imidazopyrazines as LSD1 inhibitors
WO2016073891A1 (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
US20170333435A1 (en) 2014-11-06 2017-11-23 Lysosomal Therapeutics Inc. Substituted imidazo[1,5-a]pyrimidines and their use in the treatment of medical disorders
CN108290855A (zh) 2015-07-01 2018-07-17 西北大学 被取代的喹唑啉化合物及其调节葡糖脑苷脂酶活性的用途
US9802942B2 (en) 2015-07-01 2017-10-31 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
PT3371190T (pt) 2015-11-06 2022-07-08 Incyte Corp Compostos heterocíclicos como inibidores de pi3k-gamma
US10479793B2 (en) 2015-11-18 2019-11-19 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
EP3440081A4 (en) 2016-04-06 2019-09-18 Lysosomal Therapeutics Inc. PYRROLO [1,2-A] PYRIMIDINYL-CARBOXAMIDE COMPOUNDS AND THEIR USE IN THE TREATMENT OF MEDICAL DISORDER
EP3440083A4 (en) 2016-04-06 2019-09-18 Lysosomal Therapeutics Inc. IMIDAZO [1,5-A] PYRIMIDINYL-CARBOXAMIDE COMPOUNDS AND THEIR USE IN THE TREATMENT OF MEDICAL DISORDER
JP7038063B2 (ja) 2016-04-06 2022-03-17 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 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
EP3452045A1 (en) 2016-05-04 2019-03-13 Lysosomal Therapeutics Inc. Methods of treatment and combination therapies using gcase activator heterobicyclic and related compounds
AU2017261291C1 (en) 2016-05-05 2022-05-26 Bial - R&D Investments, S.A. Substituted imidazo[1,2-b]pyridazines, substituted imidazo[1,5-b]pyridazines, related 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
US20190389865A1 (en) 2016-05-05 2019-12-26 Lysosomal Therapeutics Inc. SUBSTITUTED PYRROLO[1,2-a]TRIAZINES AND 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 (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005058837A1 (en) * 2003-12-17 2005-06-30 Glaxo Group Limited Benzazepine derivatives as histamine h3 antagonists
WO2007108750A1 (en) * 2006-03-22 2007-09-27 Astrazeneca Ab Pyridopyrimidine derivatives and their use as pde4 inhibitors
WO2010051549A1 (en) * 2008-10-31 2010-05-06 Genentech, Inc. Pyrazolopyrimidine jak inhibitor compounds and methods
WO2012007375A1 (en) * 2010-07-13 2012-01-19 F. Hoffmann-La Roche Ag Pyrazolo [1, 5a] pyrimidine and thieno [3, 2b] pyrimidine derivatives as irak4 modulators
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
WO2012129258A1 (en) * 2011-03-22 2012-09-27 Merck Sharp & Dohme Corp. Amidopyrazole inhibitors of interleukin receptor-associated kinases
WO2013134079A1 (en) * 2012-03-05 2013-09-12 Amgen Inc. Oxazolidinone compounds and derivatives thereof
WO2014025651A1 (en) * 2012-08-06 2014-02-13 Amgen Inc. Chroman derivatives as trpm8 inhibitors
WO2014089379A1 (en) * 2012-12-07 2014-06-12 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
Robb, Graeme R., et al. "Design of pyrazolo-pyrimidines as 11β-HSD1 inhibitors through optimisation of molecular electrostatic potential." MedChemComm 6.5 (2015): 926-934. *
Wang, Xiaojing, et al. "Discovery of novel pyrazolo [1, 5-a] pyrimidines as potent pan-Pim inhibitors by structure-and property-based drug design." Bioorganic & medicinal chemistry letters 23.11 (2013): 3149-3153. *

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