公开(公告)号：US20230043159A1

公开(公告)日：2023-02-09

申请号：US17282176

申请日：2019-10-02

申请人： DISC MEDICINE, INC.

发明人： Srikanth Venkatraman ,  Subhendu Mukherjee ,  Rajeev Goswami ,  Venkateshwar Rao Gummadi ,  A. Bharathi Raja ,  Martuza Hadianawala

IPC分类号： C07D471/04 ,  C07D401/12 ,  C07D403/12 ,  C07D401/14 ,  C07D209/42 ,  C07D403/14 ,  C07D413/10 ,  C07D417/12 ,  C07D409/12 ,  C07D413/14 ,  C07D409/06 ,  C07D405/12 ,  C07D233/28 ,  C07D417/04 ,  C07D413/04 ,  C07D401/06 ,  C07D471/08

摘要： The present invention provides compounds for inhibiting matriptase 2, or a mutant thereof, and compositions and methods of use thereof.

公开(公告)号：US20210275499A1

公开(公告)日：2021-09-09

申请号：US17258273

申请日：2019-07-05

申请人： METRION BIOSCIENCES LIMITED

发明人： Marc ROGERS ,  Robert KIRBY ,  Gakujun SHOMI ,  Takuya MATSUO ,  Satoru KOBAYASHI ,  Junichiro KANAZAWA ,  Nobutaka YAMAOKA ,  Makoto TORIZUKA ,  Koichi SUZAWA

IPC分类号： A61K31/4164 ,  C07D233/28 ,  C07D405/12 ,  C07D403/06 ,  C07D401/06 ,  C07D401/12 ,  C07D471/08 ,  C07D403/12 ,  C07D235/02 ,  C07D491/107 ,  A61K31/4178 ,  C07D409/12 ,  A61K31/454 ,  A61K31/4439 ,  A61K31/46 ,  A61K31/439 ,  A61K31/55 ,  A61K31/5377

摘要： The invention relates to heterocyclic sulfonamide derivatives and their use in the treatment and prophylaxis of autoimmune, inflammatory, cardiovascular, neuronal, auditory, renal and metabolic mediated diseases, and to compositions containing said derivatives and processes for their preparation.

公开(公告)号：US10981878B2

公开(公告)日：2021-04-20

申请号：US16548444

申请日：2019-08-22

申请人： Government of the United States as Represented by the Secretary of the Air Force

发明人： Rusty L. Blanski ,  Robert H. Grubbs

IPC分类号： C07D233/28 ,  C07F15/00

摘要： Backfunctionalized imidazolinium salts and methods of synthesizing the same and NHC carbene-metal complexes therefrom. For backfunctionalized imidazolinium salts of the formula: Wherein R1 is selected from the group consisting of an ester group, an amide group, and an aromatic group; R2 is selected from the group consisting of hydrogen, an ester group, an amide group, and an aromatic group; R3 and R4 are each an aliphatic group; and X is an anion; the method comprises cyclization of a halogenated acrylate with Hünig's base in a solvent.

公开(公告)号：US20200002286A1

公开(公告)日：2020-01-02

申请号：US16548419

申请日：2019-08-22

申请人： Government of the United States as Represented by the Secretary of the Air Force

发明人： Rusty L. Blanski ,  Robert H. Grubbs

IPC分类号： C07D233/28 ,  C07F15/00

摘要： Backfunctionalized imidazolinium salts and methods of synthesizing the same and NHC carbene-metal complexes therefrom. For backfunctionalized imidazolinium salts of the formula: Wherein R1 is selected from the group consisting of an ester group, an amide group, and an aromatic group; R2 is selected from the group consisting of hydrogen, an ester group, an amide group, and an aromatic group; R3 and R4 are each an aliphatic group; and X is an anion; the method comprises cyclization of a halogenated acrylate with Hünig's base in a solvent.

公开(公告)号：US20190023663A1

公开(公告)日：2019-01-24

申请号：US16049679

申请日：2018-07-30

申请人： Saint Louis University

发明人： Peter G. Ruminski ,  David W. Griggs

IPC分类号： C07D239/14 ,  C07D239/16 ,  C07D239/02 ,  C07D401/12 ,  C07D233/28

摘要： The present disclosure provides pharmaceutical agents of the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such pharmaceutical agents. Methods of using the pharmaceutical agents for the treatment of a variety of diseases and disorders are also provided.

公开(公告)号：US20150259306A1

公开(公告)日：2015-09-17

申请号：US14722422

申请日：2015-05-27

申请人： FerroKin BioSciences, Inc.

发明人： James W. Malecha, JR.

IPC分类号： C07D263/16 ,  C07D231/14 ,  C07D233/28

CPC分类号： C07D263/16 ,  C07D231/14 ,  C07D233/28 ,  C07D277/12 ,  C07D277/56

摘要： Disclosed herein are new compounds of desazadesferrothiocin polyether (DADFT-PE) analogues, as well as pharmaceutical compositions comprising them and their application as metal chelation agents for the treatment of disease. Methods of chelation of iron and other metals in a human or animal subject are also provided for the treatment of metal overload and toxicity.

摘要翻译： 本文公开了新型的脱氮铁硫代聚醚（DADFT-PE）类似物的化合物，以及包含它们的药物组合物及其作为用于治疗疾病的金属螯合剂的应用。 还提供了人或动物受试者中铁和其他金属的螯合方法用于治疗金属过载和毒性。

公开(公告)号：US08420687B2

公开(公告)日：2013-04-16

申请号：US13362545

申请日：2012-01-31

申请人： Yasushi Murakami ,  Naoko Kobayashi ,  Azuma Nishio ,  Nobuo Kubota

发明人： Yasushi Murakami ,  Naoko Kobayashi ,  Azuma Nishio ,  Nobuo Kubota

IPC分类号： A01N43/52 ,  A61K31/415 ,  C07D233/28 ,  C07D233/91

CPC分类号： A61K31/4168 ,  A61K9/0019 ,  A61K47/12 ,  A61K47/18 ,  A61K47/22

摘要： To provide a pharmaceutical composition which can enhance the storage stability of 1-(1-hydroxymethyl-2,3-dihydroxypropyloxymethyl)-2-nitroimidazole without impairing the effect of the compound.The pharmaceutical composition includes 1-(1-hydroxymethyl-2,3-dihydroxypropyloxymethyl)-2-nitroimidazole, which is represented by formula (1): and a compound having chelating ability.

公开(公告)号：US20110312996A1

公开(公告)日：2011-12-22

申请号：US13108211

申请日：2011-05-16

申请人： Brad Buckman ,  John B. Nicholas ,  Vladimir Serebryany ,  Scott D. Seiwert

发明人： Brad Buckman ,  John B. Nicholas ,  Vladimir Serebryany ,  Scott D. Seiwert

IPC分类号： A61K31/4709 ,  C07D401/12 ,  C07D233/28 ,  C07D403/12 ,  C07D403/14 ,  C07D417/14 ,  C07D409/14 ,  C07D413/14 ,  C07D405/14 ,  C07D401/14 ,  C07D487/04 ,  C07D471/04 ,  A61K31/4184 ,  A61K31/4178 ,  A61K31/428 ,  A61K31/423 ,  A61P31/14 ,  A61P1/16 ,  C07D403/04

CPC分类号： C07D403/04 ,  A61K31/4025 ,  A61K31/4178 ,  A61K31/4184 ,  A61K31/423 ,  A61K31/428 ,  A61K31/4365 ,  A61K31/437 ,  A61K31/439 ,  A61K31/4985 ,  A61K31/506 ,  A61K31/517 ,  A61K31/519 ,  A61K31/55 ,  A61K31/558 ,  A61K31/5585 ,  C07D207/16 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04 ,  C07D513/04

摘要： The embodiments provide compounds of the general Formulae VI, VII, VIII, IX, X, XI, XII, XIII, XIV, and XV as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.

摘要翻译： 实施方案提供了通式VI，VII，VIII，IX，X，XI，XII，XIII，XIV和XV的化合物以及包含主题化合物的组合物，包括药物组合物。 实施方案还提供治疗方法，包括治疗丙型肝炎病毒感染的方法和治疗肝纤维化的方法，所述方法通常涉及向有需要的个体施用有效量的主题化合物或组合物。

公开(公告)号：US20110178292A1

公开(公告)日：2011-07-21

申请号：US13003862

申请日：2009-07-16

申请人： George Lentzen ,  Thorsten Neuhaus

发明人： George Lentzen ,  Thorsten Neuhaus

IPC分类号： C07D243/04 ,  C07D239/06 ,  C07D233/28 ,  C12P13/00

CPC分类号： C07D233/26 ,  C07D239/06 ,  C07D243/04

摘要： The invention relates to an innovative method for synthesis of cyclic amidines. The synthesis starts from a β-, γ- or δ-lactone which is twofold brominated. After esterification of the carboxyl function, the bromine atoms are nucleophilically substituted and the corresponding diamino compound is obtained. The ring closure to the cyclic amidine is accomplished subsequently by reaction with orthoester, imidate or thioimidate. Owing to interposing additional steps for recovery of the diamino compound in enantiomerically pure form, the enantiomers of the cyclic amidines can be stereoselectively synthesized.

摘要翻译： 本发明涉及一种用于合成环脒的创新方法。 合成开始于二溴溴化的β-，γ-或δ-内酯。 羧基官能团酯化后，溴原子被亲核取代，得到相应的二氨基化合物。 随后通过与原酸酯，亚胺酯或硫代亚氨酸酯反应来完成环脒的闭环。 由于以对映体纯的形式介入了二氨基化合物的回收步骤，可以立体选择性地合成环脒的对映异构体。

公开(公告)号：US20100076043A1

公开(公告)日：2010-03-25

申请号：US12565347

申请日：2009-09-23

申请人： Michael Farber

发明人： Michael Farber

IPC分类号： A61K31/4164 ,  C07C203/02 ,  C07D233/28 ,  C07D207/08 ,  A61K31/215 ,  A61K31/401 ,  A61K31/405 ,  C07D209/04 ,  A61K9/48 ,  A61P21/00

CPC分类号： C07D207/16 ,  A23L33/175 ,  A61K31/215 ,  A61K31/401 ,  A61K31/405 ,  A61K31/4164 ,  C07C229/02 ,  C07C229/08 ,  C07D209/20 ,  C07D233/64

摘要： There is provided novel amino acid ester compounds comprising at least one nitric oxide releasing group and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one amino acid ester compound comprising at least one nitric oxide releasing group, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. Also provided are compositions for increasing nitric oxide physiological levels in a subject, methods for increasing nitric oxide physiological levels in a subject, methods for improving a subject's muscle strength, athletic performances and/or lean body mass gain and or performance in a subject.

摘要翻译： 提供了包含至少一种一氧化氮释放基团及其药学上可接受的盐的新型氨基酸酯化合物和包含至少一种包含至少一种一氧化氮释放基团的至少一种氨基酸酯化合物和任选的至少一种硝酸 氧化物供体和/或至少一种治疗剂。 还提供了用于增加受试者中的一氧化氮生理水平的组合物，用于增加受试者的一氧化氮生理水平的方法，用于改善受试者的肌肉力量的方法，运动表现和/或瘦体重增加和/或受试者的表现。