Abstract: The present invention is related to compounds of structure (I) as heme oxygenase 1 (HMOX 1) inducers. The present invention is also related a method of controlling the activity or the amount, or both the activity and the amount, of heme-oxygenase 1 in a mammalian subject. The definitions of the variables are provided herein.
Type:
Grant
Filed:
April 8, 2020
Date of Patent:
September 8, 2020
Assignee:
Mitobridge Inc.
Inventors:
Margaret Biddle, Arthur Kluge, Sanjita Sasmal, Bharat Lagu, Xinyuan Wu, Takashi Ogiyama, Eric Bell
Abstract: The invention describes an aryl-2,2?-tandem bisthiazole compound and a preparation method and the use thereof. In particular, disclosed in the present invention are an aryl-2,2?-tandem bisthiazole compound with the structure as shown in general formula I and the preparation method thereof and use thereof as a histone deacetylase inhibitor in the preparation of antitumor drugs.
Type:
Grant
Filed:
August 24, 2017
Date of Patent:
September 8, 2020
Assignee:
Shanghai Institute of Materia Medica, Chinese Academy of Sciences
Abstract: Described herein are compounds of Formula I, methods of making such compounds, pharmaceutical compositions and medicaments containing such compounds, and methods of using such compounds to treat or prevent diseases or conditions associated with the enzyme glucosylceramide synthase (GCS).
Abstract: The present disclosure relates to C-glycoside derivatives having a fused phenyl ring or pharmaceutical acceptable salts thereof, a method for preparing the same, a pharmaceutical composition comprising the same, a use thereof and a method for dual inhibition of SGLT1 and SGLT2 using the same. A novel compound of the present disclosure has a dual inhibitory activity against SGLT1 and SGLT2, thus being valuably used as a diabetes therapeutic agent.
Type:
Grant
Filed:
January 3, 2017
Date of Patent:
August 25, 2020
Assignee:
Je II Pharmaceutical Co., Ltd.
Inventors:
Joon Woo Nam, Jong Yup Kim, Kyung Hoon Kim, Jung Mee Lee, Ji Yoon Kim, Ji Seon Park, Joseph Kim, Yoon Sun Park, Jeong Min Kim
Abstract: The present invention relates to a novel family of covalent kinases inhibitors, compounds of this class have been found to have inhibitory activity against members of the TEC kinase family, particularly ITK and/or TXK, BTK, TEC and/or combinations thereof. The present invention is directed to a compound of Formula I or pharmaceutically acceptable salt, solvate, solvates of salt, stereoisomer, tautomer, isotope, prodrug, complex or biologically active metabolite thereof, for use in therapy.
Abstract: The disclosure provides for methods for preparing 2-cyanoimino-1,3-thiazolidine, which is an important building block for the preparation of crop protection active ingredients and pharmaceuticals. To this end, the disclosure provides for more efficient and improved methods of preparing 2-cyanoimino-1,3-thiazolidine.
Abstract: The present invention provides compounds for the treatment of a bacterial infection. Additionally, the present invention provides compositions and methods for using these compounds and compositions in the treatment of a bacterial infection in a subject.
Abstract: The present disclosure provides solid forms, including a salt or co-crystal, of Compound I: which exhibits Acetyl-CoA carboxylase (“ACC”) inhibitory activity and may be useful in treating ACC mediated diseases. Also provided herein are processes or steps for the preparation of a Compound I and intermediates useful for the processes or steps described herein.
Abstract: Provided herein are therapeutic and/or prophylactic compounds for mitochondrial or oxidative stress diseases such as cancer, amyotrophic lateral sclerosis, Creutzfeldt-Jakob disease, Machado-Joseph disease, spinocerebellar ataxia, Huntington disease, Parkinson disease, Alzheimer disease, myocardial infarction, cerebral infarction, diseases related to aging, diabetes, alcoholic liver injury, chronic obstructive pulmonary disease, mitochondrial myopathy, encephalopathy, lactic acidosis, and stroke-like episodes (MELAS), and the like, wherein the compound is represented by formula (1), or reduced forms thereof, or pharmaceutically acceptable salts thereof.
Abstract: The present disclosure relates to a method for preparing various physiologically active pharmaceutical ingredients, such as a 1,1-diaryl compound and a 1,1-diheteroaryl compound (specifically, a 1,1-diaryl carbonyl compound), in an economical and convenient manner under mild conditions without using an expensive transition metal catalyst by activating an alkyne compound (e.g., an ynamide) using a Brønsted acid as a catalyst to induce a reaction of the activated alkyne compound and a N—O bond oxidant to form an adduct intermediate and then inducing a coupling reaction of the adduct intermediate with various nucleophilic organic compounds (e.g., a nucleophilic arene compound).
Type:
Grant
Filed:
March 19, 2018
Date of Patent:
August 11, 2020
Assignee:
Industry-University Cooperation Foundation Hanyang University
Inventors:
Seunghoon Shin, Dilip V. Patil, Seung Woo Kim, Quynh H. Nguyen
Abstract: The invention relates to 1,3-diaza-spiro-[3.4]-octane derivatives, their preparation and use in medicine, particularly in various neurological disorders, including but not limited to pain, neurodegenerative disorders, neuroinflammatory disorders, neuropsychiatric disorders, substance abuse/dependence.
Type:
Grant
Filed:
August 29, 2019
Date of Patent:
August 11, 2020
Assignee:
GRÜNENTHAL GMBH
Inventors:
Paul Ratcliffe, Ingo Konetzki, Nikolay Sitnikov, Thomas Koch, Ruth Jostock
Abstract: The present invention relates to a novel compound having an effect of inhibiting platelet aggregation and a salt thereof and, more specifically, to: a novel platelet aggregation inhibitor specifically inhibiting shear stress-induced platelet aggregation; a pharmaceutical composition containing the same as an active ingredient; and a preparation method therefor.
Type:
Grant
Filed:
September 2, 2016
Date of Patent:
August 4, 2020
Assignee:
Shin Poong Pharmaceutical Co., Ltd.
Inventors:
Jei Man Ryu, Dong Won Lee, Kang Hyeok Lee, Jin Hun Park, Geum Sil Cho, Ki Sung Lee, Jin Ho Chung, Woo Ile Park, Jae Young Lee
Abstract: The present invention discloses a pyrido-azacyclic compound represented by formula I, an isomer thereof, a pharmaceutically acceptable salt or a pharmaceutically acceptable solvate thereof, a preparation process thereof and a composition comprising the compound, and a use thereof as a multi-target protein kinase inhibitor in the preparation of a medicament for the treatment of diseases that are associated with protein kinase, especially c-Met, such as cancer and the like. The compound represented by formula I has potent inhibitory activity on tumor cells with overexpression of c-Met kinase, can effectively target c-Met-mediated signaling pathway, and can be used in the treatment of diseases such as cancer and the like that is caused by the overexpression of c-Met kinase.
Type:
Grant
Filed:
May 23, 2016
Date of Patent:
July 14, 2020
Assignee:
SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES
Inventors:
Yaqiu Long, Meiyu Geng, Zhongliang Xu, Jing Ai
Abstract: A novel type of water-soluble isatin derivatives, and manufacturing method and application thereof. An isatin derivative comprising a phenolic hydroxy group is used as the substrates. A dimethylaminomethylene group is introduced to an ortho position of the phenolic hydroxy group to significantly improve the water solubility of a class of compounds provided by the invention. An antitumor activity study showed that the activity of the class of compounds was not reduced, and even improved. The class of compounds has great prospects for applications in developing an antitumor pharmaceutical product.
Type:
Grant
Filed:
July 28, 2016
Date of Patent:
July 7, 2020
Assignee:
Tianjin University of Science & Technology
Abstract: The present invention relates to a method for preparing substituted 3-(2-anilino-1-cyclohexyl-1H-benzimidazol-5-yl)propanoic acid derivatives of the general formula (I) in which R1 represents a hydrogen atom or R1 represents a group selected from the series of C1-C3-alkyl-, C1-C3-alkoxy-, C1-C3-haloalkyl- and C1-C3-haloalkoxy-, R2 represents a hydrogen atom or a C1-C3-alkyl group, R3 represents a hydrogen atom or a C1-C3-alkyl group, R4 represents a cyclohexyl group, which is optionally singly or multiply substituted by a C1-C3-alkyl group, and R5 represents a hydrogen atom or a C1-C6-alkyl group; and also intermediates which may be used to prepare substituted 3-(2-anilino-1-cyclohexyl-1H-benzimidazol-5-yl)propanoic acid derivatives.
Abstract: Disclosed herein is a compound of formula (I) and/or a pharmaceutically acceptable salt thereof that can serve as Erk inhibitors. They are potentially useful in the treatment of diseases treatable by inhibition of Erk, such as cancers. Also disclosed herein is a pharmaceutical composition, comprising a compound of formula I and/or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier.