IL265564A - Calpain modulators and their medical uses - Google Patents

Calpain modulators and their medical uses

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Publication number
IL265564A
IL265564A IL265564A IL26556419A IL265564A IL 265564 A IL265564 A IL 265564A IL 265564 A IL265564 A IL 265564A IL 26556419 A IL26556419 A IL 26556419A IL 265564 A IL265564 A IL 265564A
Authority
IL
Israel
Prior art keywords
therapeutic uses
calpain modulators
calpain
modulators
therapeutic
Prior art date
Application number
IL265564A
Other languages
English (en)
Hebrew (he)
Inventor
Brad Owen Buckman
John Beamond Nicholas
Shendong Yuan
Marc Adler
Kumaraswamy Emayan
Jingyuang Ma
Original Assignee
Brad Owen Buckman
John Beamond Nicholas
Shendong Yuan
Marc Adler
Kumaraswamy Emayan
Jingyuang Ma
Blade 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 Brad Owen Buckman, John Beamond Nicholas, Shendong Yuan, Marc Adler, Kumaraswamy Emayan, Jingyuang Ma, Blade Therapeutics Inc filed Critical Brad Owen Buckman
Publication of IL265564A publication Critical patent/IL265564A/en

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    • C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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Families Citing this family (46)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2017292646A1 (en) 2016-07-05 2019-02-07 Blade Therapeutics, Inc. Calpain modulators and therapeutic uses thereof
DK3512846T3 (da) 2016-09-16 2024-11-11 Lighthouse Pharmaceuticals Inc Ketonhæmmere af lysin-gingipain
SG10201912574WA (en) 2016-09-28 2020-02-27 Blade Therapeutics Inc Calpain modulators and therapeutic uses thereof
AU2018289434A1 (en) * 2017-06-23 2020-01-16 Blade Therapeutics, Inc. Calpain modulators and therapeutic uses thereof
AU2018300150A1 (en) 2017-07-11 2020-01-30 Vertex Pharmaceuticals Incorporated Carboxamides as modulators of sodium channels
CA3095164A1 (en) * 2018-03-28 2019-10-03 Blade Therapeutics, Inc. Calpain modulators and therapeutic uses thereof
SG11202008773PA (en) * 2018-03-28 2020-10-29 Blade Therapeutics Inc Method of treating fibrotic disease
US11528907B2 (en) 2018-04-25 2022-12-20 Bayer Aktiengesellschaft Heteroaryl-triazole and heteroaryl-tetrazole compounds as pesticides
MX2021000154A (es) * 2018-06-28 2021-04-19 Blade Therapeutics Inc Metodos de tratamiento de fibrosis hepatica que usan inhibidores de calpaina.
EP3873897B1 (en) 2018-10-30 2024-08-14 Gilead Sciences, Inc. N-benzoyl-phenylalanine derivatives as alpha4beta7 integrin inhibitors for treating inflammatory diseases
KR20240015737A (ko) 2018-10-30 2024-02-05 길리애드 사이언시즈, 인코포레이티드 알파4베타7 인테그린 억제제로서의 퀴놀린 유도체
EP3873900B1 (en) 2018-10-30 2025-01-08 Gilead Sciences, Inc. Imidazo[1,2-a]pyridine derivatives as alpha4beta7 integrin inhibitors for the treatment of inflammatory diseases
CN112969504B (zh) 2018-10-30 2024-04-09 吉利德科学公司 用于抑制α4β7整合素的化合物
WO2020146682A1 (en) 2019-01-10 2020-07-16 Vertex Pharmaceuticals Incorporated Carboxamides as modulators of sodium channels
WO2020146612A1 (en) 2019-01-10 2020-07-16 Vertex Pharmaceuticals Incorporated Esters and carbamates as modulators of sodium channels
CN111825653A (zh) * 2019-04-19 2020-10-27 安道麦马克西姆有限公司 取代吡唑类化合物的制备及其作为邻氨基苯甲酰胺前体的用途
CA3148216A1 (en) 2019-07-23 2021-01-28 Bayer Aktiengesellschaft Novel heteroaryl-triazole compounds as pesticides
ES3013685T3 (en) 2019-07-23 2025-04-14 Bayer Ag Novel heteroaryl-triazole compounds as pesticides
BR112022001660A2 (pt) * 2019-07-31 2022-05-03 Blade Therapeutics Inc Inibidores de calpaína e usos dos mesmos para o tratamento de distúrbios neurológicos
KR20220047323A (ko) 2019-08-14 2022-04-15 길리애드 사이언시즈, 인코포레이티드 알파 4 베타 7 인테그린의 저해용 화합물
CN110604735B (zh) * 2019-09-18 2022-10-25 华东师范大学 一种治疗肝纤维化、硬皮病的化合物及其应用
HRP20241695T1 (hr) 2019-12-06 2025-02-14 Vertex Pharmaceuticals Incorporated Supstituirani tetrahidrofurani kao modulatori natrijevih kanala
CA3162405A1 (en) * 2019-12-26 2021-07-01 Xiangyang Chen Crystalline forms of (s) -1- (1-acryloylpyrrolidin-3-yl) -3- ( (3, 5-dimethoxyphenyl) ethynyl) -5- (methylamino) -1h-pyrazole-4-carboxamide
US11952365B2 (en) 2020-06-10 2024-04-09 Aligos Therapeutics, Inc. Anti-viral compounds
WO2022017975A1 (en) 2020-07-18 2022-01-27 Syngenta Crop Protection Ag Pesticidally active heterocyclic derivatives with sulfur containing substituents
EP4635972A2 (en) 2020-07-20 2025-10-22 Enanta Pharmaceuticals, Inc. Functionalized peptides as antiviral agents
CN111718326B (zh) * 2020-07-23 2023-04-07 河南中医药大学 一种含喹啉结构的nnn型嘧啶腙钴(ii)配合物及其制备方法和应用
US11384090B2 (en) 2020-11-23 2022-07-12 Enanta Pharmaceuticals, Inc. Spiropyrrolidine derived antiviral agents
US11352363B1 (en) 2020-11-23 2022-06-07 Enanta Pharmaceuticals, Inc. Spiropyrrolidine derived antiviral agents
US11976084B2 (en) 2020-11-23 2024-05-07 Enanta Pharmaceuticals, Inc. Spiropyrrolidine derived antiviral agents
US11970502B2 (en) 2021-05-04 2024-04-30 Enanta Pharmaceuticals, Inc. Macrocyclic antiviral agents
US12398147B2 (en) 2021-05-11 2025-08-26 Enanta Pharmaceuticals, Inc. Macrocyclic spiropyrrolidine derived antiviral agents
US11319325B1 (en) 2021-05-11 2022-05-03 Enanta Pharmaceuticals, Inc. Macrocyclic spiropyrrolidine derived antiviral agents
KR20240031300A (ko) 2021-06-04 2024-03-07 버텍스 파마슈티칼스 인코포레이티드 나트륨 채널 조절제로서의 n-(하이드록시알킬 (헤테로)아릴) 테트라하이드로푸란 카르복스아미드
US11851422B2 (en) 2021-07-09 2023-12-26 Aligos Therapeutics, Inc. Anti-viral compounds
US11325916B1 (en) 2021-07-29 2022-05-10 Enanta Pharmaceuticals, Inc. Spiropyrrolidine derived antiviral agents
US11339170B1 (en) 2021-07-23 2022-05-24 Enanta Pharmaceuticals, Inc. Spiropyrrolidine derived antiviral agents
US12479854B2 (en) 2021-07-29 2025-11-25 Enanta Pharmaceuticals, Inc. Spiropyrrolidine derived antiviral agents
CN113651762B (zh) * 2021-09-03 2023-12-26 上海晋鲁医药科技有限公司 一种1-甲基-1h-1,2,4-三氮唑-3-甲酸甲酯的制备方法
US12065428B2 (en) 2021-09-17 2024-08-20 Aligos Therapeutics, Inc. Anti-viral compounds
US12145941B2 (en) 2021-12-08 2024-11-19 Enanta Pharmaceuticals, Inc. Heterocyclic antiviral agents
WO2023107419A1 (en) 2021-12-08 2023-06-15 Enanta Pharmaceuticals, Inc. Saturated spirocyclics as antiviral agents
WO2023118434A1 (en) * 2021-12-22 2023-06-29 Globachem Nv Pesticidally active amide compounds
US20250064789A1 (en) * 2022-03-01 2025-02-27 Westvac Biopharma Co., Ltd. Ketoamide derivatives and pharmaceutical uses thereof
TW202409000A (zh) * 2022-08-29 2024-03-01 美商富曼西公司 用於製備３－鹵代－４，５－二氫－１ｈ－吡唑之高效新方法
KR102844743B1 (ko) * 2024-06-03 2025-08-12 주식회사 에이켐바이오 신규 피롤 또는 신규 이미다졸 유도체와 그것의 폐섬유화증 개선 용도

Family Cites Families (136)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1984003506A1 (en) 1983-03-08 1984-09-13 Commw Serum Lab Commission Antigenically active amino acid sequences
NZ207394A (en) 1983-03-08 1987-03-06 Commw Serum Lab Commission Detecting or determining sequence of amino acids
JPS60500673A (ja) 1983-03-08 1985-05-09 コモンウエルス　セラム　ラボラトリ−ズ　コミツシヨン 抗原活性を有するアミノ酸配列
US4863940A (en) 1984-07-26 1989-09-05 Rohm And Haas N-acetonyl-substituted amides and phytopathogenic fungicidal use thereof
NZ215865A (en) 1985-04-22 1988-10-28 Commw Serum Lab Commission Method of determining the active site of a receptor-binding analogue
US4783443A (en) 1986-03-03 1988-11-08 The University Of Chicago Amino acyl cephalosporin derivatives
US5571689A (en) 1988-06-16 1996-11-05 Washington University Method of N-acylating peptide and proteins with diheteroatom substituted analogs of myristic acid
US5223409A (en) 1988-09-02 1993-06-29 Protein Engineering Corp. Directed evolution of novel binding proteins
US5663143A (en) 1988-09-02 1997-09-02 Dyax Corp. Engineered human-derived kunitz domains that inhibit human neutrophil elastase
WO1990007329A1 (en) 1989-01-06 1990-07-12 The Regents Of The University Of California Selection method for pharmacologically active compounds
IE910847A1 (en) 1990-03-13 1991-09-25 Fisons Plc Immunosuppressive macrocyclic compounds
DE69130831T2 (de) 1990-11-21 1999-09-16 Iterex Pharmaceuticals Ltd. Partnership, San Diego Synthese äquimolarer mischungen vielzähliger oligomere, speziell oligopeptidmischungen
CA2095633C (en) 1990-12-03 2003-02-04 Lisa J. Garrard Enrichment method for variant proteins with altered binding properties
US5331573A (en) 1990-12-14 1994-07-19 Balaji Vitukudi N Method of design of compounds that mimic conformational features of selected peptides
US5145684A (en) 1991-01-25 1992-09-08 Sterling Drug Inc. Surface modified drug nanoparticles
WO1992013549A1 (en) 1991-02-07 1992-08-20 Research Corporation Technologies, Inc. Inhibition of cell proliferation by hydrophobic peptides
SE9102462D0 (sv) 1991-08-28 1991-08-28 Astra Ab New isosteric peptides
EP0541946B1 (de) 1991-10-07 1996-07-17 Hoechst Aktiengesellschaft Verfahren zur diastereoselektiven reduktiven Pinakol-Kupplung von homochiralen alpha-Aminoaldehyden
US5644048A (en) 1992-01-10 1997-07-01 Isis Pharmaceuticals, Inc. Process for preparing phosphorothioate oligonucleotides
CA2138124A1 (en) 1992-06-24 1994-01-06 David D. Eveleth, Jr. Use of calpain inhibitors in the inhibition and treatment of medical conditions associated with increased calpain activity
US5658885A (en) 1993-04-27 1997-08-19 The Dupont Merck Pharmaceutical Company Amidino and guanidino substituted boronic acid inhibitors of trypsin-like enzymes
WO1995009859A1 (en) 1993-10-07 1995-04-13 The Du Pont Merck Pharmaceutical Company Boropeptide inhibitors of thrombin which contain a substituted pyrrolidine ring
ATE377006T1 (de) 1995-11-28 2007-11-15 Cephalon Inc Aus d-aminosäuren abgeleitete cystein- und serinproteasehemmer
DE19642591A1 (de) 1996-10-15 1998-04-16 Basf Ag Neue Piperidin-Ketocarbonsäure-Derivate, deren Herstellung und Anwendung
JP2002514192A (ja) 1996-11-13 2002-05-14 セフアロン・インコーポレーテツド ベンゾチアゾおよび関連の複素環基を含有するシステインおよびセリンプロテアーゼ阻害剤
DE19648793A1 (de) 1996-11-26 1998-05-28 Basf Ag Neue Benzamide und deren Anwendung
US5952322A (en) 1996-12-05 1999-09-14 Pfizer Inc. Method of reducing tissue damage associated with non-cardiac ischemia using glycogen phosphorylase inhibitors
DE19650975A1 (de) 1996-12-09 1998-06-10 Basf Ag Neue heterocyclisch substituierte Benzamide und deren Anwendung
SK282680B6 (sk) 1996-12-11 2002-11-06 Basf Aktiengesellschaft Ketobenzamidy, farmaceutické prípravky s ich obsahom a ich použitie na potlačenie chorôb
DE69826881T2 (de) 1997-03-14 2005-12-01 Smithkline Beecham Corp. Neue indolcarboxamide, pharmazeutische zusammensetzungen und methoden zur hemmung von calpain
DE69824582T2 (de) * 1997-03-14 2005-07-07 Smithkline Beecham Corp. Neuartige Chinolin- und Naphthalincarboxamide, pharmazeutische Zusammensetzungen und Verfahren zum Inhibieren von Calpain
US6083944A (en) 1997-10-07 2000-07-04 Cephalon, Inc. Quinoline-containing α-ketoamide cysteine and serine protease inhibitors
US6150378A (en) 1997-10-07 2000-11-21 Cephalon, Inc. Peptidyl-containing α-ketoamide cysteine and serine protease inhibitors
US6506559B1 (en) 1997-12-23 2003-01-14 Carnegie Institute Of Washington Genetic inhibition by double-stranded RNA
AUPP249298A0 (en) 1998-03-20 1998-04-23 Ag-Gene Australia Limited Synthetic genes and genetic constructs comprising same I
WO1999050264A1 (en) 1998-03-30 1999-10-07 Kyowa Hakko Kogyo Co., Ltd. Quinazoline derivatives
KR20010042839A (ko) 1998-04-20 2001-05-25 스타르크, 카르크 시스테인 프로테아제를 억제하는 효과를 나타내고헤테로시클릭 치환체가 있는 신규 아미드
DE19817461A1 (de) 1998-04-20 1999-10-21 Basf Ag Neue substituierte Benzamide, deren Herstellung und Anwendung
AU3927699A (en) 1998-04-20 1999-11-08 Basf Aktiengesellschaft New substituted amides, their production and their use
DE19818614A1 (de) 1998-04-20 1999-10-21 Basf Ag Neue substituierte Amide, deren Herstellung und Anwendung
EP1082308B1 (de) 1998-04-20 2009-04-01 Abbott GmbH & Co. KG Heterocyclisch substituierte amide als calpainhemmer
DE19817459A1 (de) * 1998-04-20 1999-10-21 Basf Ag Neue heterozyklische substituierte Amide, Herstellung und Anwendung
US6482832B1 (en) 1998-05-25 2002-11-19 Abbott Laboratories Heterocyclically substituted amides, their production and their use
US6335155B1 (en) 1998-06-26 2002-01-01 Sunesis Pharmaceuticals, Inc. Methods for rapidly identifying small organic molecule ligands for binding to biological target molecules
US6280946B2 (en) 1998-08-07 2001-08-28 Boston Probes, Inc. PNA probes, probe sets, methods and kits pertaining to the universal detection of bacteria and eucarya
WO2000039585A1 (en) 1998-12-28 2000-07-06 Sunesis Pharmaceuticals, Inc. Identifying small organic molecule ligands for binding
EP1159260A1 (en) 1999-03-15 2001-12-05 Axys Pharmaceuticals, Inc. Novel compounds and compositions as protease inhibitors
ES2215626T3 (es) * 1999-03-15 2004-10-16 Axys Pharmaceuticals, Inc. N-cianomethil amidas como inhibidores de proteasas.
EP1165490B1 (en) 1999-03-16 2006-08-16 Cytovia, Inc. Substituted 2-aminobenzamide caspase inhibitors and the use thereof
DE50010931D1 (de) 1999-06-23 2005-09-15 Aventis Pharma Gmbh Substituierte benzimidazole
KR20020067702A (ko) 2000-01-26 2002-08-23 오노 야꾸힝 고교 가부시키가이샤 질소 함유 5원환 화합물 및 이러한 화합물을 유효성분으로서 함유하는 약제
EP1283728A2 (en) 2000-05-23 2003-02-19 Amersham Health AS Contrast agents
US6582827B1 (en) 2000-11-27 2003-06-24 The Trustees Of Columbia University In The City Of New York Specialized substrates for use in sequential lateral solidification processing
DE10114762A1 (de) 2001-03-26 2002-10-02 Knoll Gmbh Verwendung von Cysteinprotease-Inhibitoren
PT2280070E (pt) 2001-07-23 2015-10-29 Univ Leland Stanford Junior Métodos e composições para inibição mediada por iarn da expressão génica em mamíferos
WO2003024955A2 (en) 2001-09-18 2003-03-27 Sunesis Pharmaceuticals, Inc. Small molecule inhibitors of caspases
US20030167490A1 (en) 2001-11-26 2003-09-04 Hunter Craig P. Gene silencing by systemic RNA interference
TW200301698A (en) 2001-12-21 2003-07-16 Bristol Myers Squibb Co Acridone inhibitors of IMPDH enzyme
PL369772A1 (en) 2002-01-31 2005-05-02 Morphochem Aktiengesellschaft Für Kombinatorischechemie Compounds that inhibit factor xa activity
WO2003091202A1 (en) 2002-04-25 2003-11-06 Ono Pharmaceutical Co., Ltd. Diketohydrazine derivative compounds and drugs contaiing the compounds as the active ingredient
CA2493008A1 (en) 2002-08-09 2004-02-19 Transtech Pharma, Inc. Aryl and heteroaryl compounds and methods to modulate coagulation
AU2004204760C1 (en) 2003-01-08 2010-08-19 Novartis Vaccines And Diagnostics, Inc. Antibacterial agents
US20040242542A1 (en) 2003-03-25 2004-12-02 The Regents Of The University Of California Compositions and methods for inducing CD81 dependent antiproliferation and for treating hepatitis C and other disorders
WO2005000793A1 (ja) 2003-06-26 2005-01-06 Taisho Pharmaceutical Co., Ltd. ２位置換シクロアルキルカルボン酸誘導体
EP1493739A1 (fr) 2003-07-03 2005-01-05 Warner-Lambert Company LLC Dérivés thiophényliques d'aminoacides, leur procédé de préparation et les compositions pharmaceutiques qui les contiennent
CN100406016C (zh) 2003-07-21 2008-07-30 诺瓦提斯公司 用于治疗骨转移瘤、肿瘤生长和肿瘤诱导的骨丢失的组织蛋白酶k抑制剂和二膦酸盐/酯的组合
US7459472B2 (en) 2003-08-08 2008-12-02 Transtech Pharma, Inc. Aryl and heteroaryl compounds, compositions, and methods of use
CN1835936A (zh) 2003-08-14 2006-09-20 默克公司 用于治疗阿尔茨海默氏病的大环β－分泌酶抑制剂
JPWO2005102381A1 (ja) 2004-04-26 2008-03-06 小野薬品工業株式会社 カテプシンｋ阻害薬およびｐｔｈ類を併用することを特徴とする骨密度増加剤
RU2007119427A (ru) 2004-11-09 2008-12-20 СмитКлайн Бичем Корпорейшн (US) Соединения, являющиеся ингибиторами гликогенфосфорилазы, и фармацевтические композиции на их основе
US8257931B2 (en) 2005-01-21 2012-09-04 President And Fellows Of Harvard College Regulation of protein synthesis
US20080311036A1 (en) * 2005-05-11 2008-12-18 University Of Florida Research Foundation, Inc. Imaging of Neural and Organ Injury or Damage
WO2007016476A2 (en) 2005-08-01 2007-02-08 Phenomix Corporation Hepatitis c serine protease inhibitors and uses therefor
US7964624B1 (en) 2005-08-26 2011-06-21 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases
AR055395A1 (es) 2005-08-26 2007-08-22 Vertex Pharma Compuestos inhibidores de la actividad de la serina proteasa ns3-ns4a del virus de la hepatitis c
EP1968568A4 (en) 2005-12-22 2011-04-13 Glaxosmithkline Llc HEMMER OF NUTS ACTIVITY
WO2007081530A2 (en) 2006-01-03 2007-07-19 Med Institute, Inc. Endoluminal medical device for local delivery of cathepsin inhibitors
US20090304631A1 (en) 2006-01-27 2009-12-10 David Alan Campbell Hepatitis c serine protease inhibitors and uses therefor
US20070207144A1 (en) 2006-02-16 2007-09-06 Lee Rubin Ubiquitin/proteasome inhibitors for the treatment of spinal muscular atrophy
NZ571280A (en) 2006-03-16 2011-10-28 Vertex Pharma Deuterated hepatitis C protease inhibitors
US20080045521A1 (en) 2006-06-09 2008-02-21 Astrazeneca Ab Phenylalanine derivatives
US8710178B2 (en) 2006-10-18 2014-04-29 Lincoln University Macrocyclic cysteine protease inhibitors and compositions thereof
KR101578674B1 (ko) 2006-12-29 2015-12-18 아비에 도이치란트 게엠베하 운트 콤파니 카게 카복스아미드 화합물 및 칼페인 억제제로서의 이의 용도
EP2134717A2 (en) 2007-02-27 2009-12-23 Vertex Pharmceuticals Incorporated Inhibitors of serine proteases
CN107021895A (zh) 2007-06-12 2017-08-08 尔察祯有限公司 抗菌剂
EP2014657A1 (de) 2007-06-21 2009-01-14 Bayer Schering Pharma Aktiengesellschaft Diaminopyrimidine als Modulatoren des EP2-Rezeptors
TWI453019B (zh) 2007-12-28 2014-09-21 Abbvie Deutschland 甲醯胺化合物
WO2010023609A1 (en) 2008-08-25 2010-03-04 Piramal Life Sciences Limited Oxazole, oxadiazole and thiazole derivatives as diacylglycerol acyltranferase inhibitors
JP5583694B2 (ja) 2009-01-05 2014-09-03 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 Ｃｂ２受容体を調節するピロリジン化合物
GB2467561A (en) 2009-02-06 2010-08-11 Summit Corp Plc Dual calpain-ROS inhibitors
TWI519530B (zh) 2009-02-20 2016-02-01 艾伯維德國有限及兩合公司 羰醯胺化合物及其作為鈣蛋白酶（ｃａｌｐａｉｎ）抑制劑之用途
US8236798B2 (en) 2009-05-07 2012-08-07 Abbott Gmbh & Co. Kg Carboxamide compounds and their use as calpain inhibitors
US9051304B2 (en) 2009-12-22 2015-06-09 AbbVie Deutschland GmbH & Co. KG Carboxamide compounds and their use as calpain inhibitors V
US8598211B2 (en) 2009-12-22 2013-12-03 Abbvie Inc. Carboxamide compounds and their use as calpain inhibitors IV
TW201134825A (en) 2009-12-30 2011-10-16 Avila Therapeutics Inc Ligand-directed covalent modification of protein
WO2011133346A1 (en) 2010-04-21 2011-10-27 Pharmacofore, Inc. Peripheral opioid agonists and peripheral opioid antagonists
US9725479B2 (en) 2010-04-22 2017-08-08 Ionis Pharmaceuticals, Inc. 5′-end derivatives
WO2011159781A2 (en) 2010-06-17 2011-12-22 Senomyx, Inc. Bitter taste modulators
US20120010235A1 (en) 2010-07-12 2012-01-12 Xin-Jie Chu N-substituted pyrrolidines
WO2012021788A2 (en) 2010-08-13 2012-02-16 Banyan Biomarkers Dipeptide calpain inhibitors
CN103201262B (zh) 2010-08-20 2016-06-01 艾米拉医药股份有限公司 自分泌运动因子抑制剂及其用途
WO2012040242A1 (en) 2010-09-22 2012-03-29 Intermune, Inc. Substituted proline inhibitors of hepatitis c virus replication
CA2819087A1 (en) 2010-12-09 2012-06-14 AbbVie Deutschland GmbH & Co. KG Carboxamide compounds and their use as calpain inhibitors v
WO2012122420A2 (en) 2011-03-09 2012-09-13 Pharmacofore, Inc. Opioid prodrugs with heterocyclic linkers
BR112013022946A2 (pt) 2011-03-09 2017-07-18 Signature Therapeutics Inc pró-fármacos de agentes ativos com ligantes heterocíclocos
CA2833082C (en) 2011-04-15 2019-12-31 New World Laboratories, Inc. Selective cysteine protease inhibitors and uses thereof
ES2929179T3 (es) 2011-08-30 2022-11-25 Tufts College Inhibidores del proteasoma activados por FAP para el tratamiento de tumores sólidos
KR20140102253A (ko) 2011-11-25 2014-08-21 에프. 호프만-라 로슈 아게 카텝신의 억제제로서의 피롤리딘 유도체
MX352654B (es) 2012-01-11 2017-12-04 Hoffmann La Roche Amidas macrociclicas como inhibidores de proteasas.
RU2014144285A (ru) 2012-04-03 2016-05-27 Эббви Дойчланд Гмбх Унд Ко. Кг Карбоксамидные соединения и их применение в качестве ингибиторов кальпаина v
US9309284B2 (en) 2012-05-02 2016-04-12 Kansas State University Reasearch Foundation Macrocyclic and peptidomimetic compounds as broad-spectrum antivirals against 3C or 3C-like proteases of picornaviruses, caliciviruses and coronaviruses
JP2016501848A (ja) 2012-11-16 2016-01-21 アデレード リサーチ アンド イノヴェーション プロプライエタリー リミテッド 大環状化合物及びその使用
CN105492444B (zh) 2013-07-02 2018-09-07 百时美施贵宝公司 作为rock抑制剂的三环吡啶-甲酰胺衍生物
UY35834A (es) 2013-11-14 2015-05-29 Bristol Myers Squibb Company Una Corporación Del Estado De Delaware Piperazinas de pirazolo sustituido como inhibidores de caseína quinasa 1 delta y epsilon
EP3107952B1 (en) 2014-02-19 2018-09-26 ETH Zurich Method for the generation of chemical libraries
WO2015140199A1 (de) 2014-03-21 2015-09-24 Bayer Pharma Aktiengesellschaft Cyano-substituierte imidazo[1,2-a]pyridincarboxamide und ihre verwendung
US10392422B2 (en) 2014-05-20 2019-08-27 Rqx Pharmaceuticals, Inc. Macrocyclic broad spectrum antibiotics
WO2015196086A1 (en) * 2014-06-20 2015-12-23 The University of Montana, Missoula, MT NOVEL INHIBITORS OF SYSTEM Xc(-)
WO2016027284A2 (en) 2014-08-22 2016-02-25 Alkem Laboratories Ltd. Piperidine ureas as cathepsin cysteine protease inhibitors
EP3189047B1 (en) 2014-09-04 2018-12-26 Bristol-Myers Squibb Company Diamide macrocycles that are fxia inhibitors
US11219670B2 (en) 2014-09-05 2022-01-11 The Johns Hopkins University Targeting CAPN9/CAPNS2 activity as a therapeutic strategy for the treatment of myofibroblast differentiation and associated pathologies
WO2016089648A1 (en) 2014-12-01 2016-06-09 Vtv Therapeutics Llc Bach 1 inhibitors in combination with nrf2 activators and pharmaceutical compositions thereof
RU2732405C2 (ru) 2015-07-02 2020-09-16 Тёрнинг Поинт Терапьютикс, Инк. Хиральные диарильные макроциклы в качестве модуляторов протеинкиназ
MX2018006856A (es) 2015-12-07 2018-08-01 Plexxikon Inc Compuestos y metodos para modulacion de la quinasa, e indicaciones de los mismos.
CN105669520B (zh) 2016-01-12 2018-10-30 山东大学 含有色氨酸基本骨架的邻苯二胺类选择性组蛋白去乙酰化酶抑制剂及其制备方法和应用
AU2017229591B2 (en) 2016-03-09 2021-08-19 Blade Therapeutics Pty Ltd Calpain modulators and methods of production and use thereof
EP3426674A4 (en) 2016-03-09 2019-08-14 Blade Therapeutics, Inc. CYCLIC KETO AMID COMPOUNDS AS CALPAIN MODULATORS AND METHOD FOR THE PRODUCTION AND USE THEREOF
US11560356B2 (en) 2016-06-29 2023-01-24 The Regents Of The University Of California Compounds and compositions for the treatment of cancer
AU2017292646A1 (en) 2016-07-05 2019-02-07 Blade Therapeutics, Inc. Calpain modulators and therapeutic uses thereof
SG10201912574WA (en) 2016-09-28 2020-02-27 Blade Therapeutics Inc Calpain modulators and therapeutic uses thereof
AU2018289434A1 (en) 2017-06-23 2020-01-16 Blade Therapeutics, Inc. Calpain modulators and therapeutic uses thereof
SG11202008773PA (en) 2018-03-28 2020-10-29 Blade Therapeutics Inc Method of treating fibrotic disease
CA3095164A1 (en) 2018-03-28 2019-10-03 Blade Therapeutics, Inc. Calpain modulators and therapeutic uses thereof
US20210253642A1 (en) 2018-05-09 2021-08-19 Blade Therapeutics, Inc. Calpain modulators and therapeutic uses thereof background
MX2021000154A (es) 2018-06-28 2021-04-19 Blade Therapeutics Inc Metodos de tratamiento de fibrosis hepatica que usan inhibidores de calpaina.
WO2020006177A1 (en) 2018-06-29 2020-01-02 Blade Therapeutics, Inc. Vascular adhesion protein-1 (vap-1) modulators and therapeutic uses thereof

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