AU2015374170B2 - Pyrrolo and pyrazolopyrimidines as ubiquitin-specific protease 7 inhibitors - Google Patents

Pyrrolo and pyrazolopyrimidines as ubiquitin-specific protease 7 inhibitors Download PDF

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AU2015374170B2
AU2015374170B2 AU2015374170A AU2015374170A AU2015374170B2 AU 2015374170 B2 AU2015374170 B2 AU 2015374170B2 AU 2015374170 A AU2015374170 A AU 2015374170A AU 2015374170 A AU2015374170 A AU 2015374170A AU 2015374170 B2 AU2015374170 B2 AU 2015374170B2
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methyl
pyrimidin
pyrazolo
alkyl
aryl
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AU2015374170A1 (en
Inventor
Alexandre Joseph Buckmelter
Ann-Marie Campbell
Justin A. Caravella
R. Bruce DIEBOLD
Anna Ericsson
Bruce Follows
David Joseph Guerin
Stephanos Ioannidis
JR. David R. LANCIA
Darby Rye Schmidt
Adam Charles Talbot
Minghua Wang
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Valo Early Discovery Inc
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Valo Early Discovery Inc
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Assigned to VALO EARLY DISCOVERY, INC. reassignment VALO EARLY DISCOVERY, INC. Request for Assignment Assignors: FORMA THERAPEUTICS, INC.
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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
    • 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
    • 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
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Hospice & Palliative Care (AREA)
  • Obesity (AREA)
  • Psychiatry (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
AU2015374170A 2014-12-30 2015-12-29 Pyrrolo and pyrazolopyrimidines as ubiquitin-specific protease 7 inhibitors Active AU2015374170B2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2021200346A AU2021200346A1 (en) 2014-12-30 2021-01-20 Pyrrolo and pyrazolopyrimidines as ubiquitin-specific protease 7 inhibitors

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201462098141P 2014-12-30 2014-12-30
US62/098,141 2014-12-30
PCT/US2015/067831 WO2016109515A1 (en) 2014-12-30 2015-12-29 Pyrrolo and pyrazolopyrimidines as ubiquitin-specific protease 7 inhibitors

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AU2015374170A1 AU2015374170A1 (en) 2017-07-27
AU2015374170B2 true AU2015374170B2 (en) 2020-10-22

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AU2021200346A Abandoned AU2021200346A1 (en) 2014-12-30 2021-01-20 Pyrrolo and pyrazolopyrimidines as ubiquitin-specific protease 7 inhibitors

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US (4) US9902728B2 (enExample)
EP (2) EP3240791B1 (enExample)
JP (1) JP6649388B2 (enExample)
KR (1) KR102581827B1 (enExample)
CN (1) CN107406451B (enExample)
AR (1) AR103297A1 (enExample)
AU (2) AU2015374170B2 (enExample)
CA (1) CA2972797C (enExample)
CL (1) CL2017001687A1 (enExample)
CO (1) CO2017006997A2 (enExample)
EA (1) EA038204B1 (enExample)
EC (1) ECSP17049010A (enExample)
ES (1) ES2768996T3 (enExample)
IL (1) IL252773A0 (enExample)
MA (1) MA40706A1 (enExample)
MX (2) MX373788B (enExample)
PH (1) PH12017501224A1 (enExample)
SA (1) SA517381839B1 (enExample)
SG (1) SG11201704897QA (enExample)
TW (2) TWI698436B (enExample)
WO (1) WO2016109515A1 (enExample)
ZA (1) ZA201704746B (enExample)

Families Citing this family (67)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20230038593A (ko) 2011-09-02 2023-03-20 인사이트 홀딩스 코포레이션 Ｐｉ３ｋ 억제제로서 헤테로시클릴아민
WO2015191677A1 (en) 2014-06-11 2015-12-17 Incyte Corporation Bicyclic heteroarylaminoalkyl phenyl derivatives as pi3k inhibitors
WO2016040554A1 (en) 2014-09-10 2016-03-17 Temple University-Of The Commonwealth System Of Higher Education Novel 5-hydroxytryptamine receptor 7 activity modulators and their method of use
MA41291A (fr) 2014-12-30 2017-11-07 Forma Therapeutics Inc Dérivés de la pyrrolotriazinone et de l'imidazotriazinone en tant qu'inhibiteurs de la protéase spécifique de l'ubiquitine n° 7 (usp7) pour le traitement d'un cancer
AR103297A1 (es) 2014-12-30 2017-05-03 Forma Therapeutics Inc Pirrolo y pirazolopirimidinas como inhibidores de la proteasa 7 específica de ubiquitina
JP2018504431A (ja) 2015-02-05 2018-02-15 フォーマ セラピューティクス，インコーポレイテッド ユビキチン特異的プロテアーゼ７阻害物質としてのチエノピリミジノン
HK1248221A1 (zh) 2015-02-05 2018-10-12 Forma Therapeutics, Inc. 异噻唑啉酮类，吡唑并嘧啶酮类和吡咯并嘧啶酮作为泛蛋白特异性蛋白酶7抑制剂
JP2018504430A (ja) 2015-02-05 2018-02-15 フォーマ セラピューティクス，インコーポレイテッド ユビキチン特異的プロテアーゼ７阻害物質としてのキナゾリノン及びアザキナゾリノン
PH12017501538B1 (en) 2015-02-27 2024-02-14 Incyte Holdings Corp Salts of p13k inhibitor and processes for their preparation
CA3012560A1 (en) * 2016-02-25 2017-08-31 Asceneuron S.A. Glycosidase inhibitors
WO2017201683A1 (en) 2016-05-25 2017-11-30 Merck Sharp & Dohme Corp. Substituted tetrahydroisoquinoline compounds useful as gpr120 agonists
FR3052452B1 (fr) * 2016-06-10 2018-06-22 Les Laboratoires Servier Nouveaux derives de piperidinyle, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
FR3061177B1 (fr) * 2016-12-28 2019-09-27 Les Laboratoires Servier Nouveaux derives piperidinyles hetero(aryle)-substitues, procede pour leur preparation et compositions pharmaceutiques les contenant
MD3468971T2 (ro) 2016-06-10 2020-06-30 Servier Lab Noi derivați de piperidinil (hetero)aril-substituiţi, procedeu de obţinere a acestora și compoziții farmaceutice care îi conțin
EP3481803B1 (en) 2016-07-08 2020-09-02 Mayo Foundation for Medical Education and Research Methods and materials for treating cancer
GB201612938D0 (en) * 2016-07-26 2016-09-07 Almac Discovery Ltd Pharmaceutical compounds
GB201617758D0 (en) 2016-10-20 2016-12-07 Almac Discovery Limited Pharmaceutical compounds
AU2017348322B8 (en) 2016-10-28 2021-12-23 Icahn School Of Medicine At Mount Sinai Compositions and methods for treating EZH2-mediated cancer
TW201822637A (zh) 2016-11-07 2018-07-01 德商拜耳廠股份有限公司 用於控制動物害蟲的經取代磺醯胺類
AU2017370694A1 (en) 2016-12-08 2019-07-25 Icahn School Of Medicine At Mount Sinai Compositions and methods for treating CDK4/6-mediated cancer
CN108239082B (zh) * 2016-12-26 2021-01-05 成都先导药物开发股份有限公司 一种抑制rock的化合物及其应用
EP3600290B1 (en) * 2017-03-21 2025-06-04 Temple University - Of The Commonwealth System of Higher Education Novel modulators of the sigma-2 receptor and their method of use
EP3600289A4 (en) 2017-03-21 2020-08-05 Temple University - Of The Commonwealth System of Higher Education 5-HYDROXYTRYPTAMINE RECEPTOR 7 MODULATORS AND THE USE OF THESE AS THERAPEUTIC AGENTS
JP7158393B2 (ja) 2017-09-14 2022-10-21 第一三共株式会社 環状構造を有する化合物
WO2019084030A1 (en) 2017-10-24 2019-05-02 Genentech, Inc. (4-HYDROXYPYRROLIDIN-2-YL) -HYDROXAMATE COMPOUNDS AND METHODS OF USE
WO2019084026A1 (en) 2017-10-24 2019-05-02 Genentech, Inc. (4-HYDROXYPYRROLIDIN-2-YL) -HETEROCYCLIC COMPOUNDS AND METHODS OF USE
EA202091260A1 (ru) 2017-11-29 2020-09-07 Ле Лаборатуар Сервье Новые пиперидинильные производные в качестве ингибиторов убиквитин-специфической протеазы 7
JP7321183B2 (ja) 2017-12-15 2023-08-04 ピラミッド バイオサイエンシズ インコーポレイテッド がんを治療するためのｔｒｋキナーゼ阻害物質としての、５－（２－（２，５－ジフルオロフェニル）ピロリジン－１－イル）－３－（１ｈ－ピラゾール－１－イル）ピラゾロ［１，５－ａ］ピリミジン誘導体及び関連する化合物
WO2019126733A1 (en) 2017-12-22 2019-06-27 Petra Pharma Corporation Aryl-bipyridine amine derivatives as phosphatidylinositol phosphate kinase inhibitors
GB201801562D0 (en) * 2018-01-31 2018-03-14 Almac Diagnostics Ltd Pharmaceutical compounds
WO2019173516A1 (en) 2018-03-06 2019-09-12 Icahn School Of Medicine At Mount Sinai Serine threonine kinase (akt) degradation / disruption compounds and methods of use
WO2019183523A1 (en) 2018-03-23 2019-09-26 Genentech, Inc. Hetero-bifunctional degrader compounds and their use as modulators of targeted ubiquination (vhl)
JP7301042B2 (ja) 2018-03-30 2023-06-30 住友化学株式会社 複素環化合物及びそれを含有する有害節足動物防除組成物
UA127065C2 (uk) 2018-04-25 2023-03-29 Баєр Акціенгезельшафт Нові гетероарил-триазольні та гетероарил-тетразольні сполуки як пестициди
CN112996518A (zh) 2018-06-21 2021-06-18 西奈山伊坎医学院 Wd40重复结构域蛋白5(wdr5)降解/破坏化合物和使用方法
UY38291A (es) * 2018-07-05 2020-06-30 Servier Lab Nuevos derivados de amino-pirimidonilo un proceso para su preparación y composiciones farmacéuticas
US20220016115A1 (en) * 2018-12-06 2022-01-20 Almac Discovery Limited Usp19 inhibitors for use in therapy
KR102712818B1 (ko) 2018-12-06 2024-09-30 한국화학연구원 Pde9a 저해 활성을 가지는 화합물 및 이들의 의약 용도
BR112021010644A2 (pt) * 2018-12-06 2021-09-28 Almac Discovery Limited Composto, estereoisômero, tautômero, hidrato, derivado de n-óxido ou sal farmaceuticamente aceitável, composição farmacêutica, métodos para tratamento de obesidade, resistência a insulina, diabetes tipo ii, atrofia muscular e câncer e para redução de perda de massa muscular em um indivíduo, e, inibidor de usp19
CN109666005A (zh) * 2018-12-14 2019-04-23 上海毕得医药科技有限公司 一种2-溴恶唑-5-甲酸乙酯的合成方法
US11174263B2 (en) 2018-12-31 2021-11-16 Biomea Fusion, Inc. Inhibitors of menin-MLL interaction
AU2019417833B2 (en) 2018-12-31 2024-11-07 Biomea Fusion, Inc. Irreversible inhibitors of menin-MLL interaction
US12479816B2 (en) 2019-02-08 2025-11-25 University of Pittsburgh—of the Commonwealth System of Higher Education 20-HETE formation inhibitors
EP3923987A1 (en) 2019-02-14 2021-12-22 Institut National de la Santé et de la Recherche Médicale (INSERM) Use of usp7 inhibitors for the treatment of acute myeloid leukemia (aml)
CN109912598B (zh) * 2019-03-27 2022-09-13 四川大学华西医院 防治炎症反应的核苷类衍生物及其应用
CN113423709B (zh) * 2019-04-11 2024-02-09 四川科伦博泰生物医药股份有限公司 三嗪酮并咪唑类化合物及其医药用途
WO2020227325A1 (en) 2019-05-06 2020-11-12 Icahn School Of Medicine At Mount Sinai Heterobifunctional compounds as degraders of hpk1
CN112608320B (zh) * 2020-01-16 2023-03-17 中国药科大学 哌啶类化合物及其制备方法和医药用途
GB202001980D0 (en) 2020-02-13 2020-04-01 Almac Discovery Ltd Therapeutic mentods
MX2022012437A (es) * 2020-04-15 2022-10-27 Pyramid Biosciences Inc Metodos para preparar inhibidores del receptor de la tirosina quinasa.
WO2021221445A1 (ko) * 2020-04-27 2021-11-04 주식회사 오토텍바이오 Ubr 박스 도메인 리간드로의 화합물
US12103924B2 (en) 2020-06-01 2024-10-01 Icahn School Of Medicine At Mount Sinai Mitogen-activated protein kinase kinase (MEK) degradation compounds and methods of use
UY39391A (es) * 2020-08-24 2022-03-31 Adama Makhteshim Ltd Proceso para la preparación de pirazoles sustituidos
WO2022159650A1 (en) * 2021-01-22 2022-07-28 Icahn School Of Medicine At Mount Sinai HETEROBIFUNCTIONAL COMPOUNDS AS DEGRADERS OF eEF1A2
PE20231987A1 (es) 2021-03-10 2023-12-12 Jnana Therapeutics Inc Inhibidores de molecula pequena de la funcion de slc6a19 de mamifero
CN117412973A (zh) * 2021-05-31 2024-01-16 上海瑛派药业有限公司 含氮稠合杂芳双环化合物作为usp1抑制剂及其应用
EP4373487A4 (en) * 2021-07-19 2025-10-29 Baylor College Medicine CORONAVIRUS MAJOR PROTEASE INHIBITORS AND THEIR METHODS OF USE
AU2022315201A1 (en) * 2021-07-20 2024-01-18 Dana-Farber Cancer Institute, Inc. Inhibitors targeting ubiquitin specific protease 7 (usp7)
CA3228627A1 (en) 2021-08-11 2023-02-16 Thomas Butler Covalent inhibitors of menin-mll interaction for diabetes mellitus
EP4387972A1 (en) 2021-08-20 2024-06-26 Biomea Fusion, Inc. Crystalline form of n-[4-[4-(4-morpholinyl)-7h-pyrrolo[2,3-d]pyrimidin-6-yl]phenyl]-4-[[3(r)-[(1-oxo -2-propen-1-yl)amino]-1-piperidinyl]methyl]-2-pyridinecarboxamide, an irreversible menin-mll inhibitor for the treatment of cancer
GB202200753D0 (en) * 2022-01-21 2022-03-09 Almac Discovery Ltd Pharmaceutical compounds
CN114957248B (zh) * 2022-05-09 2023-12-29 南开大学 一种吡咯并嘧啶化合物及其制备方法、药物组合物和应用
WO2024155710A1 (en) 2023-01-18 2024-07-25 Biomea Fusion, Inc. Crystalline forms of n-[4-[4-(4-morpholinyl)-7h-pyrrolo[2,3-d]pyrimidin-6- yl]phenyl]-4-[[3(r)-[(l-oxo-2-propen-l-yl)amino]-l-piperidinyl]methyl]-2-pyridinecarboxamide as a covalent inhibitor of menin-mll interaction
EP4467535A1 (en) 2023-05-25 2024-11-27 Basf Se Lactam pesticidal compounds
WO2024240859A1 (en) 2023-05-25 2024-11-28 Basf Se Lactam pesticidal compounds
WO2025038421A1 (en) * 2023-08-11 2025-02-20 Jnana Therapeutics Inc. Bicyclic heteroaryl-containing piperidine inhibitors of slc6a19 function
CN118496138B (zh) * 2024-07-10 2024-12-03 西北农林科技大学深圳研究院 一种l-氮杂环丁烷-2-羧酸的合成方法

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2565186A1 (en) * 2011-09-02 2013-03-06 Hybrigenics S.A. Selective and reversible inhibitors of ubiquitin specific protease 7

Family Cites Families (96)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5985863A (en) 1996-09-12 1999-11-16 Vertex Pharmaceuticals, Inc. Compositions and methods for decreasing IGIF and IFN-γ production by administering an ICE inhibitor
US6204261B1 (en) 1995-12-20 2001-03-20 Vertex Pharmaceuticals Incorporated Inhibitors of interleukin-1β Converting enzyme inhibitors
US6008217A (en) 1995-12-20 1999-12-28 Vertex Pharmaceuticals Incorporated Inhibitors of interleukin-1β converting enzyme
US5874424A (en) 1995-12-20 1999-02-23 Vertex Pharmaceuticals Incorporated Inhibitors of interleukin-1β converting enzyme
IN151496B (enExample) 1980-02-26 1983-05-07 Chamanlal Jagannath Shishoo
FI95572C (fi) 1987-06-22 1996-02-26 Eisai Co Ltd Menetelmä lääkeaineena käyttökelpoisen piperidiinijohdannaisten tai sen farmaseuttisen suolan valmistamiseksi
JP2777159B2 (ja) 1988-12-22 1998-07-16 エーザイ株式会社 環状アミン誘導体を含有する医薬
US5124335A (en) 1991-01-30 1992-06-23 Merck & Co., Inc. Substituted pyrollo-fused 6 membered heterocycles as angiotensin ii antagonists
US5262564A (en) 1992-10-30 1993-11-16 Octamer, Inc. Sulfinic acid adducts of organo nitroso compounds useful as retroviral inactivating agents anti-retroviral agents and anti-tumor agents
US5756466A (en) 1994-06-17 1998-05-26 Vertex Pharmaceuticals, Inc. Inhibitors of interleukin-1β converting enzyme
US6420522B1 (en) 1995-06-05 2002-07-16 Vertex Pharmaceuticals Incorporated Inhibitors of interleukin-1β converting enzyme
US5847135A (en) 1994-06-17 1998-12-08 Vertex Pharmaceuticals, Incorporated Inhibitors of interleukin-1β converting enzyme
US5716929A (en) 1994-06-17 1998-02-10 Vertex Pharmaceuticals, Inc. Inhibitors of interleukin-1β converting enzyme
US20120165319A1 (en) 1995-12-20 2012-06-28 Vertex Pharmaceuticals Incorporated Inhibitors of interleukin-1 beta converting enzyme
FR2750862B1 (fr) 1996-07-12 1998-10-16 Dupin Jean Pierre Utilisation d'heterocycles diazotes fusionnes avec un systeme aromatique ou heteroaromatique pour le traitement des maladies thrombo-emboliques
JP2001524121A (ja) 1997-05-08 2001-11-27 アグレボ・ユー・ケイ・リミテツド 殺菌剤
US6444816B1 (en) 1997-10-27 2002-09-03 Dr. Reddy's Research Foundation Fused 7-oxo-pyrimidinyl compounds, preparation, composition and use thereof
WO1999008501A2 (en) 1998-04-23 1999-02-25 Dr. Reddy's Research Foundation New heterocyclic compounds and their use in medicine, process for their preparation and pharmaceutical compositions containing them
US6632815B2 (en) 1999-09-17 2003-10-14 Millennium Pharmaceuticals, Inc. Inhibitors of factor Xa
US6720317B1 (en) 1999-09-17 2004-04-13 Millennium Pharmaceuticals, Inc. Inhibitors of factor Xa
US6844367B1 (en) 1999-09-17 2005-01-18 Millennium Pharmaceuticals, Inc. Benzamides and related inhibitors of factor Xa
US20030153598A1 (en) 2000-07-25 2003-08-14 Raymond Pratt Methods for treating Parkinson's disease with cholinesterase inhibitors
EP1311272B1 (en) 2000-03-03 2006-11-22 Eisai Co., Ltd. Novel methods using cholinesterase inhibitors
US20060183776A9 (en) 2000-03-03 2006-08-17 Eisai Co., Ltd. Liquid dosage formulations of donepezil
WO2001094350A1 (en) 2000-06-07 2001-12-13 Almirall Prodesfarma S.A. 6-phenylpyrrolopyrimidinedione derivatives
AU2001268712A1 (en) 2000-06-23 2002-01-08 Bristol-Myers Squibb Company 1 - (heteroaryl-phenyl) - condensed pyrazol derivatives as factor Xa inhibitors
JP2002105081A (ja) 2000-07-28 2002-04-10 Nikken Chem Co Ltd 新規チオフェンニ環化合物
PE20020394A1 (es) * 2000-08-18 2002-06-21 Agouron Pharma Compuestos de pirazol y composiciones farmaceuticas que los contienen, que modulan y/o inhiben la actividad de erab/hadh2
US20020169175A1 (en) 2001-02-05 2002-11-14 Dr. Reddy's Laboratories Ltd. Pharmaceutically acceptable salts of heterocyclic compounds
US6960595B2 (en) 2001-03-23 2005-11-01 Bristol-Myers Squibb Pharma Company 5-6 to 5-7 Heterobicycles as factor Xa inhibitors
WO2003024456A1 (en) 2001-09-20 2003-03-27 Eisai Co., Ltd. Methods for treating and preventing migraines
AU2002340232A1 (en) 2001-10-17 2003-04-28 Eisai Co., Ltd. Methods for treating substance abuse with cholinesterase inhibitors
WO2003076400A1 (en) 2002-03-13 2003-09-18 Janssen Pharmaceutica N.V. New inhibitors of histone deacetylase
WO2003092606A2 (en) 2002-05-01 2003-11-13 Eisai Co., Ltd. Cholinesterase inhibitors to prevent injuries caused by chemicals
US20070053976A1 (en) 2002-05-17 2007-03-08 Eisai R & D Management Co., Ltd. Novel combination of drugs as antidepressant
WO2004034963A2 (en) 2002-05-17 2004-04-29 Eisai Co., Ltd. Methods and compositions using cholinesterase inhibitors
AU2003253165A1 (en) 2002-08-13 2004-02-25 Warner-Lambert Company Llc Pyrimidine fused bicyclic metalloproteinase inhibitors
WO2004014908A1 (en) 2002-08-13 2004-02-19 Warner-Lambert Company Llc Heterobicylcic metalloproteinase inhibitors
WO2004037176A2 (en) * 2002-10-21 2004-05-06 Bristol-Myers Squibb Company Quinazolinones and derivatives thereof as factor xa inhibitors
WO2004058727A1 (en) 2002-12-20 2004-07-15 Bayer Pharmaceuticals Corporation Substituted 3,5-dihydro-4h-imidazol-4-ones for the treatment of obesity
ATE368666T1 (de) 2003-03-18 2007-08-15 Jordanian Pharmaceutical Mfg Pyrazolopyrimidinone und ihre verwendung als pde inhibitoren
ATE440825T1 (de) 2003-06-06 2009-09-15 Vertex Pharma Pyrimidin-derivate zur verwendung als modulatoren von atp-bindende kassette transportern
US7557113B2 (en) 2003-08-26 2009-07-07 Teijin Pharma Limited Substituted pyrrolo[3,2-d]pyrimidine derivatives
EP1661896A4 (en) 2003-08-26 2008-07-16 Teijin Pharma Ltd PYRROLOPYRIMIDINETHIONDERIVAT
US20050148534A1 (en) 2003-09-22 2005-07-07 Castellino Angelo J. Small molecule compositions and methods for increasing drug efficiency using compositions thereof
WO2005035003A2 (en) 2003-09-22 2005-04-21 Dihedron Corporation Compositions and methods for increasing drug efficiency
EP1663953A1 (en) 2003-09-24 2006-06-07 Methylgene, Inc. Inhibitors of histone deacetylase
US20080312189A1 (en) 2004-03-05 2008-12-18 Eisai Co., Ltd. Cadasil Treatment with Cholinesterase Inhibitors
US7253204B2 (en) 2004-03-26 2007-08-07 Methylgene Inc. Inhibitors of histone deacetylase
MXPA06011236A (es) 2004-04-02 2007-01-16 Prana Biotechnology Ltd Compuestos neurologicamente activos.
JPWO2006004201A1 (ja) 2004-07-01 2008-04-24 エーザイ・アール・アンド・ディー・マネジメント株式会社 神経再生促進剤
US20060172992A1 (en) 2004-08-13 2006-08-03 Eisai Co., Ltd. Therapeutic agent for overactive bladder resulting from cerebral infarction
US20060135507A1 (en) 2004-08-13 2006-06-22 Osamu Yokoyama Therapeutic agent for overactive bladder involved in aging
MX2007002434A (es) 2004-08-31 2007-05-04 Astrazeneca Ab Derivados de quinazolinona y su uso como inhibidores de b-raf.
US20080064680A1 (en) 2004-09-14 2008-03-13 Bamdad Cynthia C Methods for Diagnosis and Treatment of Cancer
JP2006176503A (ja) 2004-11-26 2006-07-06 Tohoku Univ 脳血管障害を伴うアルツハイマー病治療薬
BRPI0518651A2 (pt) 2004-12-24 2008-12-02 Dainippon Sumitomo Pharma composto, uma prà-droga do mesmo, ou um sal do composto ou prà-droga farmaceuticamente aceitÁvel, composiÇço farmacÊutica, inibidor de dipeptidil peptidase iv, uso de um composto, uma prà-droga do mesmo ou um sal do composto ou prà-droga farmaceuticamente aceitÁvel, e, mÉtodo para tratar diabetes
US7989445B2 (en) 2005-04-28 2011-08-02 Takeda Pharmaceutical Company Limited Thienopyrimidone compound
GB0510204D0 (en) 2005-05-19 2005-06-22 Chroma Therapeutics Ltd Enzyme inhibitors
AR056155A1 (es) 2005-10-26 2007-09-19 Bristol Myers Squibb Co Antagonistas del receptor 1 de la hormona de concentracion de melanina no basica
US7745447B2 (en) 2005-10-26 2010-06-29 Bristol-Myers Squibb Company Substituted thieno[3,2-D]pyrimidines as non-basic melanin concentrating hormone receptor-1 antagonists
EP1966215A1 (en) 2005-12-23 2008-09-10 Novartis AG Condensed heterocyclic compounds useful as dpp-iv inhibitors
WO2008024978A2 (en) 2006-08-24 2008-02-28 Serenex, Inc. Tetrahydroindolone and tetrahydroindazolone derivatives
AR065081A1 (es) 2007-01-29 2009-05-13 Xenon Pharmaceuticals Inc Compuestos de quinazolinona y pirimidona fusionados y composicion farmaceutica
CN101686952A (zh) 2007-03-12 2010-03-31 Vm生物医药公司 新型钙离子通道调节剂
CN103087043A (zh) 2007-03-16 2013-05-08 中国人民解放军军事医学科学院放射与辐射医学研究所 具有抗增殖活性的苯甲酰胺类衍生物及其药用制剂
WO2008116053A2 (en) * 2007-03-20 2008-09-25 Trustees Of Tufts College Fap-activated chemotherapeutic compounds, and methods of use thereof
CA2685753A1 (en) 2007-05-09 2008-11-20 Neuromed Pharmaceuticals Ltd. Bicyclic pyrimidine derivatives as calcium channel blockers
RU2345996C1 (ru) 2007-07-17 2009-02-10 Андрей Александрович Иващенко Аннелированные азагетероциклические амиды, включающие пиримидиновый фрагмент, способ их получения и применения
RU2341527C1 (ru) 2007-07-17 2008-12-20 Общество С Ограниченной Ответственностью "Исследовательский Институт Химического Разнообразия" Аннелированные азагетероциклы, включающие пиримидиновый фрагмент, способ их получения и ингибиторы pi3k киназ
US8648085B2 (en) * 2007-11-30 2014-02-11 Boehringer Ingelheim International Gmbh 1, 5-dihydro-pyrazolo (3, 4-D) pyrimidin-4-one derivatives and their use as PDE9A mudulators for the treatment of CNS disorders
UA105362C2 (en) * 2008-04-02 2014-05-12 Бьорингер Ингельхайм Интернациональ Гмбх 1-heterocyclyl-1, 5-dihydro-pyrazolo [3, 4-d] pyrimidin-4-one derivatives and their use as pde9a modulators
WO2009124259A1 (en) 2008-04-04 2009-10-08 Cv Therapeutics, Inc. Pyrrolotriazinone derivatives for use as stearoyl coa desaturase inhibitors
CA2737219C (en) 2008-08-11 2017-02-28 Tracy Keller Halofuginone analogs for inhibition of trna synthetases and uses thereof
US20110082158A1 (en) 2008-10-01 2011-04-07 Aleem Gangjee Selective proton coupled folate transporter and folate receptor, and garftase and/or other folate metabolizing enzymes inhibitor compounds and methods of using the same
CA2772760A1 (en) 2008-12-23 2010-07-01 President And Fellows Of Harvard College Small molecule inhibitors of necroptosis
EP2405917B1 (en) 2009-03-13 2014-04-23 Advinus Therapeutics Private Limited Substituted fused pyrimidine compounds
US8927718B2 (en) 2009-08-26 2015-01-06 Takeda Pharmaceutical Company Limited Fused heterocyclic ring derivative and use thereof
BR112012008518A2 (pt) 2009-10-13 2016-04-05 Msd Oss Bv derivado heterocíclico, e, composição farmacêutica
WO2011097607A1 (en) 2010-02-08 2011-08-11 Southern Research Institute Anti-viral treatment and assay to screen for anti-viral agent
US8575114B2 (en) 2010-03-23 2013-11-05 Albany Molecular Research, Inc. SGLT-2 inhibitors, methods of making them, and uses thereof
US8765773B2 (en) 2010-10-18 2014-07-01 Millennium Pharmaceuticals, Inc. Substituted hydroxamic acids and uses thereof
WO2012075393A2 (en) 2010-12-02 2012-06-07 President And Fellows Of Harvard College Activators of proteasomal degradation and uses thereof
EP2663311A2 (en) 2011-01-10 2013-11-20 GlaxoSmithKline LLC Pyrimidinone derivatives as fatty acid synthase inhibitors
GB201107768D0 (en) 2011-05-10 2011-06-22 Univ Manchester Riboswitches
US20130116241A1 (en) 2011-11-09 2013-05-09 Abbvie Inc. Novel inhibitor compounds of phosphodiesterase type 10a
US9394297B2 (en) 2012-02-28 2016-07-19 Amgen Inc. Amides as pim inhibitors
GB201205164D0 (en) 2012-03-23 2012-05-09 Almac Discovery Ltd Pharmaceutical compounds
EP2938610A2 (en) 2012-12-28 2015-11-04 The U.S.A. as represented by the Secretary, Department of Health and Human Services Inhibitors of the usp1/uaf1 deubiquitinase complex and uses thereof
KR101446680B1 (ko) 2013-02-08 2014-10-07 한국과학기술연구원 ｍＧｌｕＲ1 길항제로 작용하는 사이에노피리미디논 유도체
CN103833646A (zh) 2014-02-28 2014-06-04 广东工业大学 一种脂肪氨基取代喹唑啉酮衍生物及其制备方法和应用
MA41291A (fr) 2014-12-30 2017-11-07 Forma Therapeutics Inc Dérivés de la pyrrolotriazinone et de l'imidazotriazinone en tant qu'inhibiteurs de la protéase spécifique de l'ubiquitine n° 7 (usp7) pour le traitement d'un cancer
AR103297A1 (es) 2014-12-30 2017-05-03 Forma Therapeutics Inc Pirrolo y pirazolopirimidinas como inhibidores de la proteasa 7 específica de ubiquitina
JP2018504431A (ja) 2015-02-05 2018-02-15 フォーマ セラピューティクス，インコーポレイテッド ユビキチン特異的プロテアーゼ７阻害物質としてのチエノピリミジノン
HK1248221A1 (zh) 2015-02-05 2018-10-12 Forma Therapeutics, Inc. 异噻唑啉酮类，吡唑并嘧啶酮类和吡咯并嘧啶酮作为泛蛋白特异性蛋白酶7抑制剂
JP2018504430A (ja) 2015-02-05 2018-02-15 フォーマ セラピューティクス，インコーポレイテッド ユビキチン特異的プロテアーゼ７阻害物質としてのキナゾリノン及びアザキナゾリノン

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2565186A1 (en) * 2011-09-02 2013-03-06 Hybrigenics S.A. Selective and reversible inhibitors of ubiquitin specific protease 7

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
BENEDIKT M KESSLER, "Selective and reversible inhibitors of ubiquitin-specific protease 7: a patent evaluation (WO2013030218)", EXPERT OPINION ON THERAPEUTIC PATENTS., 2014, Vol. 24(5), pages 597 - 602 *
WOLFGANG SIPPL ET AL, "Ubiquitin-specific proteases as cancer drug targets", FUTURE ONCOLOGY - FUTURE MEDICINE, 2011, Vol. 7(5), pages 619 - 632 *

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