MX2020002963A - Pirrolo y pirazolopirimidinas como inhibidores de la proteasa 7 especifica de ubiquitina. - Google Patents

Pirrolo y pirazolopirimidinas como inhibidores de la proteasa 7 especifica de ubiquitina.

Info

Publication number
MX2020002963A
MX2020002963A MX2020002963A MX2020002963A MX2020002963A MX 2020002963 A MX2020002963 A MX 2020002963A MX 2020002963 A MX2020002963 A MX 2020002963A MX 2020002963 A MX2020002963 A MX 2020002963A MX 2020002963 A MX2020002963 A MX 2020002963A
Authority
MX
Mexico
Prior art keywords
sub
inhibitors
diseases
pyrazolopyrimidines
ubiquitin
Prior art date
Application number
MX2020002963A
Other languages
English (en)
Inventor
Justin A Caravella
Stephanos Ioannidis
R Bruce Diebold
Anna Ericsson
Adam Charles Talbot
Bruce Follows
Alexandre Joseph Buckmelter
Minghua Wang
Darby Rye Schmidt
David Joseph Guerin
Jr David R Lancia
Ann-Marie Campbell
Original Assignee
Forma Therapeutics Inc
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 Forma Therapeutics Inc filed Critical Forma Therapeutics Inc
Publication of MX2020002963A publication Critical patent/MX2020002963A/es

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
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (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)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Cardiology (AREA)
  • Emergency Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Endocrinology (AREA)
  • Hospice & Palliative Care (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

La invención se relaciona con inhibidores de los inhibidores de USP7 útiles en el tratamiento de cánceres, enfermedades neurodegenerativas, alteraciones inmunológicas, alteraciones inmunológicas alteraciones inflamatorias, enfermedades cardiovasculares, enfermedades isquémicas, enfermedades e infecciones virales y enfermedades e infecciones bacterianas, con la fórmula: (ver formula) donde X1, X2, R1-R5, y R6 se describen en el presente.
MX2020002963A 2014-12-30 2017-06-27 Pirrolo y pirazolopirimidinas como inhibidores de la proteasa 7 especifica de ubiquitina. MX2020002963A (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201462098141P 2014-12-30 2014-12-30

Publications (1)

Publication Number Publication Date
MX2020002963A true MX2020002963A (es) 2020-07-22

Family

ID=55310894

Family Applications (2)

Application Number Title Priority Date Filing Date
MX2017008604A MX2017008604A (es) 2014-12-30 2015-12-29 Pirrolo y pirazolopirimidinas como inhibidores de la proteasa 7 especifica de ubiquitina.
MX2020002963A MX2020002963A (es) 2014-12-30 2017-06-27 Pirrolo y pirazolopirimidinas como inhibidores de la proteasa 7 especifica de ubiquitina.

Family Applications Before (1)

Application Number Title Priority Date Filing Date
MX2017008604A MX2017008604A (es) 2014-12-30 2015-12-29 Pirrolo y pirazolopirimidinas como inhibidores de la proteasa 7 especifica de ubiquitina.

Country Status (22)

Country Link
US (4) US9902728B2 (es)
EP (2) EP3240791B1 (es)
JP (1) JP6649388B2 (es)
KR (1) KR102581827B1 (es)
CN (1) CN107406451B (es)
AR (1) AR103297A1 (es)
AU (2) AU2015374170B2 (es)
CA (1) CA2972797C (es)
CL (1) CL2017001687A1 (es)
CO (1) CO2017006997A2 (es)
EA (1) EA038204B1 (es)
EC (1) ECSP17049010A (es)
ES (1) ES2768996T3 (es)
HK (1) HK1246284A1 (es)
IL (1) IL252773A0 (es)
MA (1) MA40706A1 (es)
MX (2) MX2017008604A (es)
PH (1) PH12017501224A1 (es)
SA (1) SA517381839B1 (es)
SG (1) SG11201704897QA (es)
TW (2) TWI770525B (es)
WO (1) WO2016109515A1 (es)

Families Citing this family (49)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BR122019020716B1 (pt) 2011-09-02 2021-02-17 Incyte Holdings Corporation heterociclilaminas como inibidores de pi3k e composição farmacêutica que as compreende
US10544117B2 (en) 2014-09-10 2020-01-28 Temple University—Of the Commonwealth System of Higher Education 5-hydroxytryptamine receptor 7 activity modulators and their method of use
TWI770525B (zh) 2014-12-30 2022-07-11 美商瓦洛健康公司 作為泛素特異性蛋白酶７抑制劑之吡咯并及吡唑并嘧啶
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
EP3253765A1 (en) 2015-02-05 2017-12-13 Forma Therapeutics, Inc. Thienopyrimidinones as ubiquitin-specific protease 7 inhibitors
WO2016126926A1 (en) 2015-02-05 2016-08-11 Forma Therapeutics, Inc. Quinazolinones and azaquinazolinones as ubiquitin-specific protease 7 inhibitors
US9938300B2 (en) 2015-02-05 2018-04-10 Forma Therapeutics, Inc. Isothiazolopyrimidinones, pyrazolopyrimidinones, and pyrrolopyrimidinones as ubiquitin-specific protease 7 inhibitors
US11612599B2 (en) * 2016-02-25 2023-03-28 Asceneuron Sa Glycosidase inhibitors
WO2017201683A1 (en) * 2016-05-25 2017-11-30 Merck Sharp & Dohme Corp. Substituted tetrahydroisoquinoline compounds useful as gpr120 agonists
DK3468971T3 (da) 2016-06-10 2020-05-18 Servier Lab Nye (hetero)aryl-substituterede piperidinyl-derivativer, en fremgangsmåde til deres fremstilling og farmaceutiske sammensætninger indeholdende dem
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
WO2018009812A1 (en) 2016-07-08 2018-01-11 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
MX2019004950A (es) 2016-10-28 2019-09-26 Icahn School Med Mount Sinai Composiciones y metodos para tratar el cancer mediado por el potenciador del homologo zeste 2.
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
CA3045037A1 (en) 2016-12-08 2018-06-14 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
WO2018175190A1 (en) * 2017-03-21 2018-09-27 Temple University-Of The Commonwealth System Of Higher Education 5-hydroxytryptamine receptor 7 modulators and their use as therapeutic agents
JP7365237B2 (ja) 2017-03-21 2023-10-19 テンプル・ユニバーシティ－オブ・ザ・コモンウェルス・システム・オブ・ハイアー・エデュケイション シグマ－２受容体の新規調節物質およびその使用方法
KR102616949B1 (ko) 2017-09-14 2023-12-22 다이이찌 산쿄 가부시키가이샤 고리형 구조를 갖는 화합물
WO2019084030A1 (en) 2017-10-24 2019-05-02 Genentech, Inc. (4-HYDROXYPYRROLIDIN-2-YL) -HYDROXAMATE COMPOUNDS AND METHODS OF USE
EP3700901A1 (en) 2017-10-24 2020-09-02 Genentech, Inc. (4-hydroxypyrrolidin-2-yl)-heterocyclic compounds and methods of use thereof
EP3717482A1 (en) 2017-11-29 2020-10-07 Les Laboratoires Servier SAS New piperidinyl derivatives as inhibitors of ubiquitin specific protease 7
KR20200099557A (ko) 2017-12-15 2020-08-24 피라미드 바이오사이언스, 인크. 암을 치료하기 위한 Trk 키나제 저해제로서의 5-(2-(2,5-다이플루오로페닐)피롤리딘-1-일)-3-(1H-피라졸-1-일)피라졸로[1,5-a]피리미딘 유도체 및 관련 화합물
BR112020012651A2 (pt) 2017-12-22 2020-12-01 Ravenna Pharmaceuticals, Inc. compostos derivados de aril-bipiridina amina como inibidores da fosfatidilinositol fosfato quinase, composição farmacêutica compreendendo os mesmos e usos terapêuticos dos ditos compostos
GB201801562D0 (en) * 2018-01-31 2018-03-14 Almac Diagnostics Ltd Pharmaceutical compounds
CN112154146A (zh) 2018-03-06 2020-12-29 西奈山伊坎医学院 丝氨酸苏氨酸激酶(akt)降解/破坏化合物和使用方法
WO2019183523A1 (en) 2018-03-23 2019-09-26 Genentech, Inc. Hetero-bifunctional degrader compounds and their use as modulators of targeted ubiquination (vhl)
CN111918865B (zh) 2018-03-30 2023-10-27 住友化学株式会社 杂环化合物和含有该杂环化合物的有害节肢动物防除组合物
SG11202010068VA (en) 2018-04-25 2020-11-27 Bayer Ag Novel heteroaryl-triazole and heteroaryl-tetrazole compounds as pesticides
UY38291A (es) * 2018-07-05 2020-06-30 Servier Lab Nuevos derivados de amino-pirimidonilo un proceso para su preparación y composiciones farmacéuticas
CN113365696A (zh) * 2018-12-06 2021-09-07 阿尔麦克探索有限公司 药物化合物和其作为泛素特异性蛋白酶19(usp19)抑制剂的用途
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
WO2020142559A1 (en) 2018-12-31 2020-07-09 Biomea Fusion, Llc Inhibitors of menin-mll interaction
SG11202106304RA (en) 2018-12-31 2021-07-29 Biomea Fusion Llc Irreversible inhibitors of menin-mll interaction
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
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
IL296921A (en) * 2020-04-15 2022-12-01 Pyramid Biosciences Inc Methods for making receptor tyrosine kinase inhibitors
US20230174470A1 (en) * 2020-04-27 2023-06-08 Autotac Inc. Compound as a ubr box domain ligand
AR123313A1 (es) * 2020-08-24 2022-11-16 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
WO2023003973A1 (en) * 2021-07-20 2023-01-26 Dana-Farber Cancer Institute, Inc. Inhibitors targeting ubiquitin specific protease 7 (usp7)
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

Family Cites Families (97)

* 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
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
US6204261B1 (en) 1995-12-20 2001-03-20 Vertex Pharmaceuticals Incorporated Inhibitors of interleukin-1β Converting enzyme inhibitors
IN151496B (es) 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
US5716929A (en) 1994-06-17 1998-02-10 Vertex Pharmaceuticals, Inc. Inhibitors of interleukin-1β converting enzyme
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
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
WO1998049899A1 (en) 1997-05-08 1998-11-12 Agrevo Uk Limited Fungicides
US6444816B1 (en) 1997-10-27 2002-09-03 Dr. Reddy's Research Foundation Fused 7-oxo-pyrimidinyl compounds, preparation, composition and use thereof
DE69828445D1 (de) 1998-04-23 2005-02-03 Reddys Lab Ltd Dr Heterozyklische verbindungen,und deren verwendung in arzneimittel,verfahren zu deren herstellung und diese enthaltende pharmazeutische zusammenstellungen
US6844367B1 (en) 1999-09-17 2005-01-18 Millennium Pharmaceuticals, Inc. Benzamides and related inhibitors of factor Xa
US6720317B1 (en) 1999-09-17 2004-04-13 Millennium Pharmaceuticals, Inc. Inhibitors of factor Xa
US6632815B2 (en) 1999-09-17 2003-10-14 Millennium Pharmaceuticals, Inc. Inhibitors of factor Xa
US20060183776A9 (en) 2000-03-03 2006-08-17 Eisai Co., Ltd. Liquid dosage formulations of donepezil
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
ATE273980T1 (de) 2000-06-07 2004-09-15 Almirall Prodesfarma Sa 6-phenylpyrrolopyrimidindion derivate
JP2004501918A (ja) 2000-06-23 2004-01-22 ブリストル−マイヤーズ　スクイブ　ファーマ　カンパニー Ｘａ因子阻害剤としての１−（ヘテロアリール−フェニル）−縮合ピラゾール誘導体
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
AU2003212335B8 (en) 2002-03-13 2009-04-23 Janssen Pharmaceutica N.V. Aminocarbonyl-derivatives as novel 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
AU2003298514A1 (en) 2002-05-17 2004-05-04 Eisai Co., Ltd. Methods and compositions using cholinesterase inhibitors
WO2004014916A1 (en) 2002-08-13 2004-02-19 Warner-Lambert Company Llc Pyrimidine fused bicyclic metalloproteinase inhibitors
AU2003249477A1 (en) 2002-08-13 2004-02-25 Warner-Lambert Company Llc Heterobicylcic metalloproteinase inhibitors
AU2003301662A1 (en) 2002-10-21 2004-05-13 Bristol-Myers Squibb Company Quinazolinones and derivatives thereof as factor xa inhibitors
AU2003299791A1 (en) 2002-12-20 2004-07-22 Bayer Pharmaceuticals Corporation Substituted 3,5-dihydro-4h-imidazol-4-ones for the treatment of obesity
ES2289377T3 (es) 2003-03-18 2008-02-01 The Jordanian Pharmaceutical Manufacturing Co. Ltd. Nuevas pirazolopirimidonas y su uso como inhibidores de pde.
EP1646615B1 (en) 2003-06-06 2009-08-26 Vertex Pharmaceuticals Incorporated Pyrimidine derivatives as modulators of atp-binding cassette transporters
US7557113B2 (en) 2003-08-26 2009-07-07 Teijin Pharma Limited Substituted pyrrolo[3,2-d]pyrimidine derivatives
TW200509938A (en) 2003-08-26 2005-03-16 Teijin Pharma Ltd Pyrrolopyrimidine thion derivatives
US20050148534A1 (en) 2003-09-22 2005-07-07 Castellino Angelo J. Small molecule compositions and methods for increasing drug efficiency using compositions thereof
US20050187147A1 (en) 2003-09-22 2005-08-25 Newman Michael J. Compositions and methods for increasing drug efficiency
US7868205B2 (en) 2003-09-24 2011-01-11 Methylgene Inc. Inhibitors of histone deacetylase
WO2005087226A1 (en) 2004-03-05 2005-09-22 Eisai Co., Ltd. Cadasil treatment with cholinesterase inhibitors
US7253204B2 (en) 2004-03-26 2007-08-07 Methylgene Inc. Inhibitors of histone deacetylase
BRPI0508183B8 (pt) 2004-04-02 2021-05-25 Prana Biotechnology Ltd compostos neurologicamente ativos, seus usos, composição farmacêutica ou veterinária e processos para preparação dos mesmos
US20080045500A1 (en) 2004-07-01 2008-02-21 Eisai R&D Management Co., Ltd. Nerve Regeneration Stimulator
US20060135507A1 (en) 2004-08-13 2006-06-22 Osamu Yokoyama Therapeutic agent for overactive bladder involved in aging
US20060172992A1 (en) 2004-08-13 2006-08-03 Eisai Co., Ltd. Therapeutic agent for overactive bladder resulting from cerebral infarction
EP1789399A1 (en) 2004-08-31 2007-05-30 AstraZeneca AB Quinazolinone derivatives and their use as b-raf inhibitors
EP1811844A4 (en) 2004-09-14 2009-12-02 Minerva Biotechnologies Corp METHOD FOR THE 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
JPWO2006068163A1 (ja) 2004-12-24 2008-06-12 大日本住友製薬株式会社 二環性ピロール誘導体
EP1876179B1 (en) 2005-04-28 2015-03-25 Takeda Pharmaceutical Company Limited Thienopyrimidone compounds
GB0510204D0 (en) 2005-05-19 2005-06-22 Chroma Therapeutics Ltd Enzyme inhibitors
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
US8618115B2 (en) 2005-10-26 2013-12-31 Bristol-Myers Squibb Company Substituted thieno[3,2-d]pyrimidinones as MCHR1 antagonists and methods for using them
KR20080090446A (ko) 2005-12-23 2008-10-08 노파르티스 아게 Ｄｄｐ-ｉｖ 억제제로서 유용한 축합 헤테로시클릭 화합물
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
WO2008112715A2 (en) 2007-03-12 2008-09-18 Vm Discovery Inc. Novel agents of calcium ion channel modulators
CN101730703B (zh) 2007-03-16 2012-12-26 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
US20100184706A1 (en) * 2007-03-20 2010-07-22 Bachovchin William W Fap-activated chemotherapeutic compounds, and methods of use thereof
WO2008138126A1 (en) 2007-05-09 2008-11-20 Neuromed Pharmaceuticals Ltd. Bicyclic pyrimidine derivatives as calcium channel blockers
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
RU2345996C1 (ru) 2007-07-17 2009-02-10 Андрей Александрович Иващенко Аннелированные азагетероциклические амиды, включающие пиримидиновый фрагмент, способ их получения и применения
JP5498392B2 (ja) * 2007-11-30 2014-05-21 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング １，５−ジヒドロ−ピラゾロ［３，４−ｄ］ピリミジン−４−オン誘導体及びｃｎｓ障害の治療のためのｐｄｅ９ａモジュレーターとしてのそれらの使用
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
JP2011516496A (ja) 2008-04-04 2011-05-26 ギリアード サイエンシーズ， インコーポレイテッド ステアロイル−ＣｏＡデサチュラーゼの阻害剤として使用するためのピロロトリアジノン誘導体
JP2011530596A (ja) 2008-08-11 2011-12-22 プレジデント アンド フェロウズ オブ ハーバード カレッジ ｔＲＮＡ合成酵素の阻害のためのハロフジノン類似体およびそれらの使用
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
CN102316735A (zh) 2008-12-23 2012-01-11 哈佛大学校长及研究员协会 坏死性凋亡的小分子抑制剂
AU2010222289B2 (en) 2009-03-13 2013-07-11 Advinus Therapeutics Private Limited Substituted fused pyrimidine compounds
WO2011024873A1 (ja) 2009-08-26 2011-03-03 武田薬品工業株式会社 縮合複素環誘導体およびその用途
MX2012004289A (es) 2009-10-13 2012-06-12 Msd Oss Bv Derivados de azina condensada para el tratamiento de enfermedades relacionadas con el receptor de acetilcolina.
US20130085133A1 (en) 2010-02-08 2013-04-04 Sourthern Research Institute Office of Commercialization and Intellectual Prop. Anti-viral treatment and assay to screenfor 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
WO2012054332A1 (en) 2010-10-18 2012-04-26 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
WO2012096928A2 (en) * 2011-01-10 2012-07-19 Glaxosmithkline Llc Pyrimidinone derivatives as fatty acid synthase inhibitors
GB201107768D0 (en) 2011-05-10 2011-06-22 Univ Manchester Riboswitches
EP2565186A1 (en) 2011-09-02 2013-03-06 Hybrigenics S.A. Selective and reversible inhibitors of ubiquitin specific protease 7
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
TWI770525B (zh) * 2014-12-30 2022-07-11 美商瓦洛健康公司 作為泛素特異性蛋白酶７抑制劑之吡咯并及吡唑并嘧啶
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
US9938300B2 (en) 2015-02-05 2018-04-10 Forma Therapeutics, Inc. Isothiazolopyrimidinones, pyrazolopyrimidinones, and pyrrolopyrimidinones as ubiquitin-specific protease 7 inhibitors
EP3253765A1 (en) 2015-02-05 2017-12-13 Forma Therapeutics, Inc. Thienopyrimidinones as ubiquitin-specific protease 7 inhibitors
WO2016126926A1 (en) 2015-02-05 2016-08-11 Forma Therapeutics, Inc. Quinazolinones and azaquinazolinones as ubiquitin-specific protease 7 inhibitors

Also Published As

Publication number Publication date
CO2017006997A2 (es) 2017-10-20
KR20170106981A (ko) 2017-09-22
TW202115067A (zh) 2021-04-16
KR102581827B1 (ko) 2023-09-25
BR112017013692A2 (pt) 2018-01-09
EA038204B1 (ru) 2021-07-22
EP3240791A1 (en) 2017-11-08
JP2018500376A (ja) 2018-01-11
EP3240791B1 (en) 2019-11-06
TWI770525B (zh) 2022-07-11
US20210332052A1 (en) 2021-10-28
CA2972797A1 (en) 2016-07-07
US10377760B2 (en) 2019-08-13
WO2016109515A1 (en) 2016-07-07
SA517381839B1 (ar) 2022-05-30
AU2015374170B2 (en) 2020-10-22
US9902728B2 (en) 2018-02-27
CN107406451B (zh) 2019-12-17
IL252773A0 (en) 2017-08-31
EA201791507A1 (ru) 2018-01-31
SG11201704897QA (en) 2017-07-28
AR103297A1 (es) 2017-05-03
AU2015374170A1 (en) 2017-07-27
MX2017008604A (es) 2017-11-15
TW201639847A (zh) 2016-11-16
MA40706A1 (fr) 2018-02-28
US10934299B2 (en) 2021-03-02
ECSP17049010A (es) 2017-11-30
US20180339988A1 (en) 2018-11-29
CA2972797C (en) 2023-12-05
PH12017501224A1 (en) 2018-01-15
HK1246284A1 (zh) 2018-09-07
ES2768996T3 (es) 2020-06-24
US20190367525A1 (en) 2019-12-05
CN107406451A (zh) 2017-11-28
AU2021200346A1 (en) 2021-03-18
JP6649388B2 (ja) 2020-02-19
EP3623372A1 (en) 2020-03-18
CL2017001687A1 (es) 2018-03-23
US20160185785A1 (en) 2016-06-30
TWI698436B (zh) 2020-07-11

Similar Documents

Publication Publication Date Title
MX2020002963A (es) Pirrolo y pirazolopirimidinas como inhibidores de la proteasa 7 especifica de ubiquitina.
WO2016109480A8 (en) Pyrrolotriazinone and imidasotriazinone derivatives as obiquitin-specific protease 7 cusp? ) inhibitors for the treatment of cancer and other usp7 mediated diseases
MX2021001186A (es) Purinonas como inhibidores de proteasa especifica de ubiquitina 1.
PH12021550418A1 (en) Macrocycles with hetrocyclic p2` groups as factor xia inhibitors
PH12020500195A1 (en) Pyrimidinones as factor xia inhibitors
WO2018226758A3 (en) METHODS FOR ENHANCED PRODUCTION AND ISOLATION OF CELL ORIGIN VESICLES AND TREATMENT OF INFLAMMATION AND NEUROLOGICAL DAMAGE
PH12017500408B1 (en) Heteroaryl compounds as btk inhibitors and uses thereof
TW201613925A (en) Imidazopyrazines as LSD1 inhibitors
WO2016127179A3 (en) Immunomodulatory agents
MX2015011898A (es) Compuestos de pirazolo y usos de los mismos.
AU2015287674B2 (en) Topical antiviral compositions and methods of using the same
MX2021014663A (es) Il-23a y tnf-alfa orientados y compuesto y sus usos.
MX2019001011A (es) Compuestos farmaceuticos.
MX2017010357A (es) Derivados novedosos de n-acil-arilsulfonamida como inhibidores de aminoacil acido ribonucleico de transferencia (arnt) sintetasa.
WO2014145035A8 (en) Methods of making cancer compositions
EA201691620A1 (ru) Циклопропиламины в качестве ингибиторов lsd1