- BICYCLIC HETEROAROMATIC AMIDE COMPOUNDS AND USES THEREOF
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The present invention features compounds useful in the treatment of neurological disorders. The compounds of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing neurological disorders.
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Page/Page column 74-75
(2021/12/29)
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- BTK Inhibitors and uses thereof
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The invention discloses a bruton's tyrosine kinase (BTK) inhibitor and use thereof. Specifically, the invention provides heteroaromatic compounds or stereoisomers, geometrical isomers, tautomers, racemates, nitrogen oxides, hydrates, solvates, metabolites and pharmaceutically acceptable salts or prodrugs thereof, and pharmaceutical compositions containing the heteroaromatic compounds; the invention also discloses use of the heteroaromatic compounds or the pharmaceutical compositions containing the heteroaromatic compounds in preparation of medicines; the medicines can be used for treating autoimmune diseases, inflammatory diseases or proliferative diseases.
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Paragraph 0475-0480; 1510-1515
(2020/05/02)
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- IMIDAZO-PYRIDINE COMPOUNDS AS PAD INHIBITORS
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Heterocyclic compounds of Formula (I), (II), and (III) are described herein along with their polymorphs, stereoisomers, prodrugs, solvates, co-crystals, intermediates, pharmaceutically acceptable salts, and metabolites thereof. The compounds described herein, their polymorphs, stereoisomers, prodrugs, solvates, co-crystals, intermediates, pharmaceutically acceptable salts, and metabolites thereof are PAD4 inhibitors and may be useful in the treatment of various disorders, for example rheumatoid arthritis, vasculitis, systemic lupus erythematosis, cutaneous lupus erythematosis, ulcerative colitis, cancer, cystic fibrosis, asthma, multiple sclerosis and psoriasis. The process of preparation of the compounds of Formula (I), (II), and (III), their polymorphs, stereoisomers, prodrugs, solvates, co-crystals, intermediates, pharmaceutically acceptable salts, and metabolites thereof, along with a pharmaceutical composition comprising a compound of Formula (I), Formula (II), Formula (III), or a pharmaceutically acceptable salt thereof have also been described.
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Paragraph 000133; 000344
(2019/05/10)
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- Low-temperature catalytic hydrogenation of bio-based furfural and relevant aldehydes using cesium carbonate and hydrosiloxane
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Selective hydrogenation of unsaturated compounds is mainly carried out by using high-pressure hydrogen in the presence of a precious or transition metal catalyst. Here, we describe a benign approach to efficiently catalyze the hydrogenation of furfural (FUR) to furfuryl alcohol (FFA) over commercially available cesium carbonate using nontoxic and cheap polymethylhydrosiloxane (PMHS) as hydrogen source. Good to excellent FFA yields (≥90%) could be obtained at 25-80 °C by appropriate control of the catalyst dosage, reaction time, and the hydride amount. FUR-to-FFA hydrogenation was clarified to follow a pseudo-first order kinetics with low apparent activation energy of 20.6 kJ mol-1. Mechanistic insights manifested that PMHS was redistributed to H3SiMe, which acted as the active silane for the hydrogenation reactions. Importantly, this catalytic system was able to selectively reduce a wide range of aromatic aldehydes to the corresponding alcohols in good yields of 81-99% at 25-80 °C in 2-6 h.
- Long, Jingxuan,Zhao, Wenfeng,Xu, Yufei,Wu, Weibo,Fang, Chengjiang,Li, Hu,Yang, Song
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p. 3063 - 3071
(2019/02/10)
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- HEPATITIS B CORE PROTEIN MODULATORS
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The present disclosure provides, in part, compounds having allosteric effector properties against Hepatitis B virus Cp. Also provided herein are methods of treating viral infections, such as hepatitis B, comprising administering to a patient in need thereof a disclosed compound of formula:
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Page/Page column 108; 109
(2018/04/13)
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- QUINAZOLINE DERIVATIVE
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Provided are a quinazoline derivative, a pharmaceutical composition containing the same, a method for preparation of said derivative, and an application of same as an anti-cancer drug.
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Paragraph 0091
(2017/07/04)
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- PROTEIN KINASE INHIBITORS
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The present invention relates to a novel family of inhibitors of protein kinases. In particular, the present invention relates to inhibitors of the members of the Tec and Src protein kinase families.
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Paragraph 0172
(2015/07/15)
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- PROTEIN KINASE INHIBITORS
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The present invention relates to a novel family of inhibitors o f protein kinase of formula 1 and process for their production and pharmaceutical compositions thereof. In particular, the present invention relates to inhibitors of the members of the Tec, Src and Btk protein kinase families
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Page/Page column 23; 24
(2014/01/18)
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- PROTEIN KINASE INHIBITORS
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The present invention relates to a novel family of inhibitors of protein kinases. In particular, the present invention relates to inhibitors of the members of the Tec and Src protein kinase families, more particularly Btk, having the general formula (1): A-Y-E-W-Z (1.)
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Page/Page column 22; 23
(2014/03/25)
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- GLYCOSIDASE INHIBITORS
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Compounds of formula (I) wherein X1, X2, W, R1 to R5, L and m have the meaning according to the claims, are glucosidase inhibitors, and can be employed, inter alia, for the treatment of Alzheimer's disease.
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Page/Page column 58
(2014/10/15)
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- PROTEIN KINASE INHIBITORS
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The present invention relates to a novel family of inhibitors of protein kinases. In particular, the present invention relates to inhibitors of the members of the Tec and Src protein kinase families.
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Page/Page column 40-41
(2014/01/07)
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- BENZAZEPINE DERIVATIVES, PROCESS FOR THE PREPARATION OF THE SAME AND USES THEREOF
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Compounds of the general formula (I): or salts thereof, which exhibit CCR5 antagonism and exert preventive and therapeutic effects against HIV infections: wherein R1 is a 5- to 6-membered aromatic ring which bears a substituent represented by the general formula: R-Z1-X-Z2- (wherein R1 is hydrogen or optionally substituted hydrocarbyl; X is optionally substituted alkylene; and Z1 and Z2 are each a heteroatom) and may be further substituted, with R being optionally bonded to the aromatic ring to form another ring; Y is optionally substituted imino; and R2 and R3 are each optionally substituted aliphatic hydrocarbyl or an optionally substituted hetero-alicyclic group.
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- RETROVIRAL PROTEASE INHIBITING PIPERAZINE COMPOUNDS
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Retroviral protease inhibiting compounds of the formula: STR1 are disclosed.
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- Cyclophanes. 14. Synthesis, Structure Assignment, and Conformational Properties of (2,5)Oxazolo- and Thiazolophanes
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The first synthesis of cyclophanes containing aromatic nuclei with two heteroatoms is described.A Hoffman pyrolytic route was used.Two isomeric (2,5)oxazolophanes (6a and 6b) and two isomeric (2,5)thiazolophanes (13a and 13b) were isolated.In both cases the isomers were found to have the anti-anti and the anti-syn structure.The assignments were made by spectral analysis and variable-temperature nuclear magnetic resonance spectroscopy in the oxazolophane case and on the basis of NMR spectral comparisons between normal (13a and 13b) and deuterated derivatives (14a and 14b) in the thiazolophane case.While the aromatic nuclei in the thiazolophanes were found to be conformationally rigid on the NMR time scale, those in the oxazolophanes were found to be conformationally mobile with a rotational barrier of 17.8 kcal/mol.
- Mashraqui, Sabir H.,Keehn, Philip M.
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p. 4461 - 4465
(2007/10/02)
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- Novel thiazole derivatives
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Novel substituted thiazoles of the formula STR1 wherein R is alkyl of 1 to 5 carbon atoms and R1 is selected from the group consisting of --NH2, -- NH-AlK, STR2 PHENYLAMINO AND DIPHENYLAMINO, AlK is alkyl of 1 to 4 carbon atoms and n
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