KR102662215B1 - 치환된 피라졸로(1,5-a)피리미딘 및 의학적 장애의 치료에서의 그의 용도 - Google Patents

치환된 피라졸로(1,5-a)피리미딘 및 의학적 장애의 치료에서의 그의 용도 Download PDF

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KR102662215B1
KR102662215B1 KR1020177015300A KR20177015300A KR102662215B1 KR 102662215 B1 KR102662215 B1 KR 102662215B1 KR 1020177015300 A KR1020177015300 A KR 1020177015300A KR 20177015300 A KR20177015300 A KR 20177015300A KR 102662215 B1 KR102662215 B1 KR 102662215B1
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pyrimidine
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레나토 티. 스컬리
피터 티. 랜스버리
앤드류 씨. 굿
엘리제 마리 조제 부르크
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비알 - 알&디 인베스트먼츠, 에스.에이.
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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
    • 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
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Diabetes (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Ophthalmology & Optometry (AREA)
  • Epidemiology (AREA)
  • Emergency Medicine (AREA)
  • Psychology (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Urology & Nephrology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
KR1020177015300A 2014-11-06 2015-11-06 치환된 피라졸로(1,5-a)피리미딘 및 의학적 장애의 치료에서의 그의 용도 Active KR102662215B1 (ko)

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

Publications (2)

Publication Number Publication Date
KR20170082577A KR20170082577A (ko) 2017-07-14
KR102662215B1 true KR102662215B1 (ko) 2024-05-02

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US (5) US10570135B2 (enExample)
EP (2) EP4406616A3 (enExample)
JP (2) JP6734860B2 (enExample)
KR (1) KR102662215B1 (enExample)
CN (2) CN107001379B (enExample)
AU (1) AU2015342887B2 (enExample)
DK (1) DK3215511T3 (enExample)
EA (1) EA201790995A1 (enExample)
ES (1) ES2984482T3 (enExample)
FI (1) FI3215511T3 (enExample)
HR (1) HRP20240644T1 (enExample)
HU (1) HUE066864T2 (enExample)
IL (1) IL252053B2 (enExample)
LT (1) LT3215511T (enExample)
MX (1) MX394094B (enExample)
PL (1) PL3215511T3 (enExample)
PT (1) PT3215511T (enExample)
RS (1) RS65642B1 (enExample)
SI (1) SI3215511T1 (enExample)
SM (1) SMT202400187T1 (enExample)
WO (1) WO2016073895A1 (enExample)

Families Citing this family (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RS63320B1 (sr) 2010-12-08 2022-07-29 The U S A As Represented By The Secretary Department Of Health And Human Services Supstituisani pirazolopirimidini kao aktivatori glukocerebrozidaze
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
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
JP6895439B2 (ja) * 2015-12-22 2021-06-30 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ ＩＲＡＫ４調節因子としてのピラゾロ［１，５ａ］ピリミジン誘導体
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
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
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
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
WO2018083085A1 (en) 2016-11-02 2018-05-11 F. Hoffmann-La Roche Ag PYRAZOLO[1,5a]PYRIMIDINE DERIVATIVES AS IRAK4 MODULATORS
CA3048376A1 (en) 2016-12-27 2018-07-05 Riken Bmp-signal-inhibiting compound
US11174242B2 (en) 2016-12-29 2021-11-16 Minoryx Therapeutics S.L. Heteroaryl compounds and their use
TW201902896A (zh) 2017-05-22 2019-01-16 瑞士商赫孚孟拉羅股份公司 治療化合物及組合物及其使用方法
WO2019123476A1 (en) * 2017-12-20 2019-06-27 Sarudbhava Formulations 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
WO2019151269A1 (ja) 2018-01-31 2019-08-08 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.
US11414431B2 (en) 2018-10-15 2022-08-16 Nimbus Lakshmi, Inc. Substituted pyrazolo[1,5-a]pyrimidines as TYK2 inhibitors
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 (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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

Family Cites Families (102)

* 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
DOP2003000703A (es) 2002-09-20 2004-03-31 Pfizer Compuestos de imidazopiradina como agonistas del receptor 5-ht4
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
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
JP5376950B2 (ja) * 2005-10-21 2013-12-25 エクセリクシス， インク． カゼインキナーゼｉｉ（ｃｋ２）モジュレーターとしてのピリミジオン類
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
WO2012075393A2 (en) 2010-12-02 2012-06-07 President And Fellows Of Harvard College Activators of proteasomal degradation and uses thereof
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
WO2014141129A2 (en) 2013-03-14 2014-09-18 Grueneberg Dorre A Novel 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
WO2015012328A1 (ja) 2013-07-24 2015-01-29 武田薬品工業株式会社 複素環化合物
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
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
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
WO2015073267A1 (en) 2013-11-15 2015-05-21 Calitor Sciences, Llc Substituted heteroaryl compounds and methods of use
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
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
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
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
WO2017004405A1 (en) 2015-07-01 2017-01-05 Northwestern University Substituted quinazoline 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
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
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
EP3452045A1 (en) 2016-05-04 2019-03-13 Lysosomal Therapeutics Inc. Methods of treatment and combination therapies using gcase activator heterobicyclic and related compounds
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
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
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 (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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

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