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

Info

Publication number
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
Authority
AU
Australia
Prior art keywords
compound
mmol
substituted
certain embodiments
alkylene
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.)
Active
Application number
AU2015342887A
Other languages
English (en)
Other versions
AU2015342887A1 (en
Inventor
Elyse Marie Josee Bourque
Andrew C. Good
Peter T. Lansbury
Renato T. Skerlj
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.)
Bial R&D Investments SA
Original Assignee
Bial R&D Investments SA
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 Bial R&D Investments SA filed Critical Bial R&D Investments SA
Publication of AU2015342887A1 publication Critical patent/AU2015342887A1/en
Assigned to BIAL – BioTech Investments, Inc. reassignment BIAL – BioTech Investments, Inc. Request for Assignment Assignors: LYSOSOMAL THERAPEUTICS INC.
Application granted granted Critical
Publication of AU2015342887B2 publication Critical patent/AU2015342887B2/en
Assigned to BIAL - R&D INVESTMENTS, S.A. reassignment BIAL - R&D INVESTMENTS, S.A. Request for Assignment Assignors: BIAL – BioTech Investments, Inc.
Active 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
    • 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

Landscapes

  • 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)
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

Publications (2)

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

Family

ID=55909884

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2015342887A Active AU2015342887B2 (en) 2014-11-06 2015-11-06 Substituted pyrazolo(1,5-a)pyrimidines and their use in the treatment of medical disorders

Country Status (21)

Country Link
US (5) US10570135B2 (cg-RX-API-DMAC10.html)
EP (2) EP3215511B1 (cg-RX-API-DMAC10.html)
JP (2) JP6734860B2 (cg-RX-API-DMAC10.html)
KR (1) KR102662215B1 (cg-RX-API-DMAC10.html)
CN (2) CN107001379B (cg-RX-API-DMAC10.html)
AU (1) AU2015342887B2 (cg-RX-API-DMAC10.html)
DK (1) DK3215511T3 (cg-RX-API-DMAC10.html)
EA (1) EA201790995A1 (cg-RX-API-DMAC10.html)
ES (1) ES2984482T3 (cg-RX-API-DMAC10.html)
FI (1) FI3215511T3 (cg-RX-API-DMAC10.html)
HR (1) HRP20240644T1 (cg-RX-API-DMAC10.html)
HU (1) HUE066864T2 (cg-RX-API-DMAC10.html)
IL (1) IL252053B2 (cg-RX-API-DMAC10.html)
LT (1) LT3215511T (cg-RX-API-DMAC10.html)
MX (1) MX394094B (cg-RX-API-DMAC10.html)
PL (1) PL3215511T3 (cg-RX-API-DMAC10.html)
PT (1) PT3215511T (cg-RX-API-DMAC10.html)
RS (1) RS65642B1 (cg-RX-API-DMAC10.html)
SI (1) SI3215511T1 (cg-RX-API-DMAC10.html)
SM (1) SMT202400187T1 (cg-RX-API-DMAC10.html)
WO (1) WO2016073895A1 (cg-RX-API-DMAC10.html)

Families Citing this family (23)

* 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
MX394094B (es) * 2014-11-06 2025-03-24 Bial R&D Invest S A PYRAZOLO [1, 5-a] PIRIMIDINAS SUSTITUIDAS Y SU USO EN EL TRATAMIENTO DE TRASTORNOS MÉDICOS.
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
US20180185368A1 (en) 2014-11-06 2018-07-05 Lysosomal Therapeutics Inc. Substituted pyrrolo[1,2-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
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
JP7034935B2 (ja) * 2016-04-06 2022-03-14 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
MX2018012211A (es) 2016-04-06 2019-03-28 Lysosomal Therapeutics Inc Compuestos de pirazol[1,5-a]pirimidinil carboxamida y su uso en el tratamiento de trastornos médicos.
JP7164774B2 (ja) 2016-05-05 2022-11-02 ビアル－アール・アンド・ディ・インベストメンツ・ソシエダーデ・アノニマ 置換イミダゾ［１，２－ｂ］ピリダジン、置換イミダゾ［１，５－ｂ］ピリダジン、関連化合物、および医学的障害の治療におけるその使用
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
CN109890829B (zh) 2016-11-02 2022-07-15 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
CA3048376A1 (en) 2016-12-27 2018-07-05 Riken Bmp-signal-inhibiting compound
JP7171057B2 (ja) 2016-12-29 2022-11-15 ミノリックス セラピューティクス エセ．エレ． ヘテロアリール化合物およびその使用
SG11201909735YA (en) 2017-05-22 2019-11-28 Hoffmann La Roche Therapeutic compounds and compositions, and methods of use thereof
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
US11459325B2 (en) 2018-01-31 2022-10-04 Takeda Pharmaceutical Company Limited Heterocyclic compound
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
CZ20022332A3 (cs) 2000-01-07 2003-01-15 Transform Pharmaceuticals, Inc. Sestava vzorků
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
ES2248616T3 (es) 2001-10-22 2006-03-16 Pfizer Inc. Compuestos imidazopiridina como moduladores del receptor 5-ht4.
KR20040087335A (ko) 2002-03-01 2004-10-13 야마노우치세이야쿠 가부시키가이샤 질소 함유 복소환 화합물
DOP2003000703A (es) 2002-09-20 2004-03-31 Pfizer Compuestos de imidazopiradina como agonistas del receptor 5-ht4
CA2499494A1 (en) 2002-09-20 2004-04-01 Pfizer Inc. N-substituted piperidinyl-imidazopyridine compounds as 5-ht4 receptor modulators
US7550470B2 (en) 2002-12-11 2009-06-23 Merck & Co. Inc. Substituted pyrazolo[1,5-A]pyrimidines as 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
BRPI0409592A (pt) 2003-04-21 2006-05-02 Pfizer compostos imidazopiridina tendo atividade agonìstica do receptor 5-ht4 e atividade antagonìstica do receptor 5-ht3
EP1682134A4 (en) 2003-11-12 2008-10-15 Amicus Therapeutics Inc GLUCOIMIDAZOLE AND POLYHYDROXYCYCLOHEXENYL-AMINE DERIVATIVES FOR THE TREATMENT OF GAUCHER DISEASE
GB0400812D0 (en) 2004-01-14 2004-02-18 Celltech R&D Ltd Novel compounds
JPWO2005077953A1 (ja) 2004-02-18 2007-10-18 萬有製薬株式会社 含窒素縮合ヘテロ芳香環誘導体
EP1753422B1 (en) 2004-05-14 2008-05-28 The Cleveland Clinic Foundation Small molecule inhibitors for mrp1 and other multidrug transporters
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
CA2568850A1 (en) 2004-08-02 2006-02-16 Schwarz Pharma Ag Indolizine carboxamides and the aza and diaza derivatives thereof
DE102004049363A1 (de) 2004-10-08 2006-04-13 Henkel Kgaa Mittel zum Färben von keratinhaltigen Fasern
WO2006078676A2 (en) 2005-01-19 2006-07-27 Merck & Co., Inc. Bicyclic pyrimidines as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes
BRPI0607927A2 (pt) 2005-02-11 2009-10-20 Hoffmann La Roche derivados de pirazol-pirimidina
DE102005007534A1 (de) 2005-02-17 2006-08-31 Bayer Cropscience Ag Pyrazolopyrimidine
CA2605351A1 (en) 2005-04-21 2006-11-02 Dainippon Sumitomo Pharma Co., Ltd. N-substituted phenylacetamide derivative and pharmaceutical composition comprising the same
WO2006118256A1 (ja) 2005-04-28 2006-11-09 Kyowa Hakko Kogyo Co., Ltd. 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
JP5102212B2 (ja) 2005-10-06 2012-12-19 メルク・シャープ・アンド・ドーム・コーポレーション プロテインキナーゼインヒビターとしてのピラゾロピリミジン
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
EP1963316A2 (en) 2005-12-08 2008-09-03 Novartis AG Pyrazolo[1,5-a]pyridine-3-carboxylic acids as ephb and vegfr2 kinase inhibitors
EP2040548B1 (en) 2006-06-23 2012-05-02 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
AU2007321922A1 (en) 2006-11-20 2008-05-29 Alantos Pharmaceuticals Holding, Inc. Heterobicyclic matrix metalloprotease inhibitors
CA2670083A1 (en) 2006-11-20 2008-05-29 Alantos Pharmaceuticals Holding, Inc. Heterobicyclic 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
EA201000003A1 (ru) 2007-06-21 2010-06-30 Айрм Ллк Ингибиторы протеинкиназ и способы их применения
JP5479105B2 (ja) 2007-11-05 2014-04-23 国立大学法人佐賀大学 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
MX2010005950A (es) 2007-11-28 2010-06-17 Schering Corp 2-fluoropirazolo[1,5-a]pirimidinas como inhibidores de proteina quinasa.
US8389527B2 (en) 2008-02-06 2013-03-05 Bristol-Myers Squibb Company Substituted imidazopyridazines useful as kinase inhibitors
WO2009119088A1 (ja) 2008-03-25 2009-10-01 武田薬品工業株式会社 複素環化合物
EP2273992B1 (en) 2008-05-01 2016-05-25 Glaxosmithkline LLC Quinolines and related analogs as sirtuin modulators
BRPI0920180B1 (pt) 2008-10-14 2021-10-26 Entasis Therapeutics Limited Compostos herecíclicos substituídos, uso dos mesmos e composiçâo farmacêutica compreendendo os ditos compostos
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
PE20170003A1 (es) 2009-08-17 2017-03-15 Intellikine Llc Compuestos heterociclicos y usos de los mismos
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
WO2012116237A2 (en) 2011-02-23 2012-08-30 Intellikine, Llc Heterocyclic compounds and uses thereof
JP6061922B2 (ja) 2011-06-22 2017-01-18 ザ ジェネラル ホスピタル コーポレイション プロテイノパチーの処置方法
CN103857657B (zh) 2011-08-18 2016-04-20 日本新药株式会社 杂环衍生物及医药
JP6054967B2 (ja) 2011-09-02 2016-12-27 バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツングＢａｙｅｒ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ ＧｍｂＨ 置換アネレート化ピリミジンおよびその使用
US8961959B2 (en) 2011-10-17 2015-02-24 The Regents Of The University Of Michigan Glucosylceramide synthase inhibitors and therapeutic methods using the same
AU2012325909B2 (en) 2011-10-20 2016-06-09 Glaxosmithkline Llc Substituted bicyclic aza-heterocycles and analogues as sirtuin modulators
JP2015503519A (ja) 2011-12-23 2015-02-02 ノバルティス アーゲー Ｂｃｌ２と結合相手の相互作用を阻害するための化合物
US8969565B2 (en) 2012-03-09 2015-03-03 Lexicon Pharmaceuticals, Inc. Imidazo[1,2-b]pyridazine-based compounds, compositions comprising them, and methods of their use
WO2013134336A2 (en) 2012-03-09 2013-09-12 Lexicon Pharmaceuticals, Inc. Inhibition of adaptor associated kinase 1 for the treatment of pain
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
BR112014029404A2 (pt) 2012-05-31 2017-06-27 Hoffmann La Roche compostos , composição farmacêutica, utilização de um composto, método para o tratamento ou profilaxia do cancêr e invenção
EP2865671B1 (en) 2012-06-22 2017-11-01 Sumitomo Chemical Company, Ltd Fused heterocyclic compound
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
JP6377068B2 (ja) 2012-11-16 2018-08-22 ユニバーシティ・ヘルス・ネットワーク ピラゾロピリミジン化合物
EP2925750A1 (en) 2012-11-29 2015-10-07 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
WO2014141129A2 (en) 2013-03-14 2014-09-18 Grueneberg Dorre A Novel methods, compounds, and compositions for inhibition of ros
WO2014144455A1 (en) 2013-03-15 2014-09-18 Epizyme, Inc. 1 -phenoxy-3-(alkylamino)-propan-2-ol derivatives as carm1 inhibitors and uses thereof
US20160159808A1 (en) 2013-07-24 2016-06-09 Takeda Pharmaceutical Company Limited Heterocyclic compound
WO2015026574A1 (en) 2013-08-20 2015-02-26 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
MX2016002367A (es) 2013-08-23 2016-10-28 Incyte Corp Compuestos de carboxamida de furo y tienopiridina utiles como inhibidores de cinasas pim.
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
WO2015147639A1 (en) 2014-03-27 2015-10-01 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
US20180185368A1 (en) 2014-11-06 2018-07-05 Lysosomal Therapeutics Inc. Substituted pyrrolo[1,2-a]pyrimidines and their use in the treatment of medical disorders
MX394094B (es) 2014-11-06 2025-03-24 Bial R&D Invest S A PYRAZOLO [1, 5-a] PIRIMIDINAS SUSTITUIDAS Y SU USO EN EL TRATAMIENTO DE TRASTORNOS MÉDICOS.
EP3317265A4 (en) 2015-07-01 2019-04-17 Northwestern University SUBSTITUTED CHINAZOLIN COMPOUNDS AND USES THEREOF FOR MODULATING GLUCOCEREBROSIDASE ACTIVITY
JP2018522872A (ja) 2015-07-01 2018-08-16 ノースウェスタン ユニバーシティ 置換４−メチルピロロ［１，２−ａ］ピリミジン−８−カルボキサミド化合物及びグルコセレブロシダーゼ活性の調節のためのその使用
WO2017040877A1 (en) 2015-09-04 2017-03-09 Lysosomal Therapeutics Inc. Heterobicyclic pyrimidinone compounds and their use in the treatment of medical disorders
TWI824309B (zh) 2015-11-06 2023-12-01 美商英塞特公司 作為PI3K-γ抑制劑之雜環化合物
JP6843135B2 (ja) 2015-11-18 2021-03-17 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ ＩＬ−１２、ＩＬ−２３および／またはＩＦＮα応答のモジュレーターとして有用なイミダゾピリダジン化合物
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
JP7034935B2 (ja) 2016-04-06 2022-03-14 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
MX2018012211A (es) 2016-04-06 2019-03-28 Lysosomal Therapeutics Inc Compuestos de pirazol[1,5-a]pirimidinil carboxamida y su uso en el tratamiento de trastornos médicos.
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
JP7164774B2 (ja) 2016-05-05 2022-11-02 ビアル－アール・アンド・ディ・インベストメンツ・ソシエダーデ・アノニマ 置換イミダゾ［１，２－ｂ］ピリダジン、置換イミダゾ［１，５－ｂ］ピリダジン、関連化合物、および医学的障害の治療におけるその使用
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
WO2017192929A1 (en) 2016-05-05 2017-11-09 Lysosomal Therapeutics Inc. SUBSTITUTED PYRROLO[1,2-α]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. *

Also Published As

Publication number Publication date
EP4406616A3 (en) 2024-11-06
US11932645B2 (en) 2024-03-19
US20250066364A1 (en) 2025-02-27
KR102662215B1 (ko) 2024-05-02
US11091492B2 (en) 2021-08-17
US9732089B2 (en) 2017-08-15
US10570135B2 (en) 2020-02-25
LT3215511T (lt) 2024-06-25
ES2984482T3 (es) 2024-10-29
US20170183354A1 (en) 2017-06-29
CN107001379A (zh) 2017-08-01
HRP20240644T1 (hr) 2024-08-02
JP2017533968A (ja) 2017-11-16
RS65642B1 (sr) 2024-07-31
MX394094B (es) 2025-03-24
US20200385390A1 (en) 2020-12-10
NZ731897A (en) 2023-11-24
EP3215511A1 (en) 2017-09-13
MX2017005940A (es) 2018-01-11
IL252053B2 (en) 2024-04-01
FI3215511T3 (fi) 2024-05-16
SI3215511T1 (sl) 2024-07-31
EP3215511A4 (en) 2018-02-28
WO2016073895A1 (en) 2016-05-12
AU2015342887A1 (en) 2017-06-15
PT3215511T (pt) 2024-05-22
SMT202400187T1 (it) 2024-07-09
EP4406616A2 (en) 2024-07-31
IL252053A0 (en) 2017-07-31
JP2020183410A (ja) 2020-11-12
JP6734860B2 (ja) 2020-08-05
US20170334916A1 (en) 2017-11-23
DK3215511T3 (da) 2024-05-13
US20220169652A1 (en) 2022-06-02
IL252053B1 (en) 2023-12-01
CN115925711A (zh) 2023-04-07
JP7519221B2 (ja) 2024-07-19
BR112017009276A2 (pt) 2017-12-19
EA201790995A1 (ru) 2017-10-31
KR20170082577A (ko) 2017-07-14
BR112017009276A8 (pt) 2023-03-14
PL3215511T3 (pl) 2024-08-12
EP3215511B1 (en) 2024-04-17
HUE066864T2 (hu) 2024-09-28
CN107001379B (zh) 2022-11-01
CA2966583A1 (en) 2016-05-12

Similar Documents

Publication Publication Date Title
AU2015342887B2 (en) Substituted pyrazolo(1,5-a)pyrimidines and their use in the treatment of medical disorders
AU2015342883B2 (en) Substituted pyrrolo(1,2-a)pyrimidines and their use in the treatment of medical disorders
WO2017192841A1 (en) Methods of treatment and combination therapies using gcase activator heterobicyclic and related compounds
CA2898650C (en) Quinoline and quinoxaline amides as modulators of sodium channels
CA3133753A1 (en) Novel small molecule inhibitors of tead transcription factors
CA3020310A1 (en) Pyrrolo[1,2-a]pyrimidinyl carboxamide compounds and their use in the treatment of medical disorders
EP3215510B1 (en) Substituted imidazo[1,5-a]pyrimidines and their use in the treatment of medical disorders
EP3452455A1 (en) Substituted imdazo[1,2- ]pyridines, substituted imidazo[1,2- ]pyrazines, related compounds, and their use in the treatment of medical disorders
WO2017192929A1 (en) SUBSTITUTED PYRROLO[1,2-α]TRIAZINES AND RELATED COMPOUNDS AND THEIR USE IN THE TREATMENT OF MEDICAL DISORDERS
WO2017040877A1 (en) Heterobicyclic pyrimidinone compounds and their use in the treatment of medical disorders
CA3178647A1 (en) Substituted tricyclic amides, analogues thereof, and methods using same
CA2937656A1 (en) Novel heterobicyclic compounds as kappa opioid agonists
CA2966583C (en) Substituted pyrazolo[1,5-a]pyrimidines and their use in the treatment of medical disorders
BR112017009276B1 (pt) Pirazolo[1,5-a]pirimidinas substituídas, composição farmacêutica e seus usos
HK1242700B (en) Substituted pyrazolo(1,5-a)pyrimidines and their use in the treatment of medical disorders
HK1242700A1 (en) Substituted pyrazolo(1,5-a)pyrimidines and their use in the treatment of medical disorders

Legal Events

Date Code Title Description
PC1 Assignment before grant (sect. 113)

Owner name: BIAL - BIOTECH INVESTMENTS, INC.

Free format text: FORMER APPLICANT(S): LYSOSOMAL THERAPEUTICS INC.

FGA Letters patent sealed or granted (standard patent)
PC Assignment registered

Owner name: BIAL - R&D INVESTMENTS, S.A.

Free format text: FORMER OWNER(S): BIAL - BIOTECH INVESTMENTS, INC.