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TETRAZOLE COMPOUNDS AS CALCIUM CHANNEL BLOCKERS

The present invention relates to novel tetrazole compounds; to processes for their preparation; to pharmaceutical compositions containing the compounds; and to the use of the compounds in therapy to treat diseases for which blocking the Cav2.2 calcium channels is beneficial. Formula (I) wherein A is: (II) or (III)

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Thiomorpholine | C4H9NS – PubChem

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NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A

The present invention relates to novel compounds of the formula I which are inhibitors of phosphodiesterase type 10A and to their use for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders

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As cell necrosis inhibitors of the indole compounds (by machine translation)

The invention relates to chemical formula (1) indole compounds, or its pharmaceutically acceptable salt or isomer, and in containing the same as the characteristic, as an active ingredient for the prevention or treatment of cell necrosis and its associated disease composition and method of manufacturing. (by machine translation)

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Synthesis and Biological Evaluation of Novel Thiomorpholine 1,1-Dioxide Derived 1,2,3-Triazole Hybrids as Potential Anticancer Agents

In this report, we describe the synthesis and biological evaluation of a new series of (4-((1-(aryl)-1H-1,2,3-triazol-4-yl)methoxy)phenyl)(1,1-dioxidothiomorpholino)methanone derivatives (6 a-6 n). All the new derivatives were well analyzed by 1H NMR, 13C NMR, FTIR, mass spectral and elemental data. The synthesized compounds were screened for in vitro anticancer activity against three cancer cell lines (MCF-7, HeLa, and HEK293) and compared with standard drug cisplatin. Three (6 b, 6 g and 6 i) out of fourteen derivatives exhibited potent anticancer activity against MCF-7, HeLa, and HEK293. Two (6 b and 6 g) potent hybrids were screened for in vivo studies against EAC bearing mice and found to possess potential anticancer activity.

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PYRAZOLO[3,4-b]PYRIDINE AND PYRROLO[2,3-b]PYRIDINE INHIBITORS OF BRUTON’S TYROSINE KINASE

Disclosed are pyrazolo[3,4-b]pyridine and pyrrolo[2,3-b]pyridine inhibitors of Bruton’s tyrosine kinase (Btk). Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are described, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.

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JAK2 INHIBITORS AND THEIR USE FOR THE TREATMENT OF MYELOPROLIFERATIVE DISEASES AND CANCER

The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof. The formula (I) compounds inhibit tyrosine kinase activity of JAK2, thereby making them useful as antiproliferative agents for the treatment of cancer and other diseases.

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NOVEL SALTS AND PHARMACEUTICAL COMPOSITIONS THEREOF FOR THE TREATMENT OF INFLAMMATORY DISORDERS

The present invention discloses salts of a Compound 1: useful in the prophylaxis and/or treatment of inflammatory conditions, autoimmune diseases, proliferative diseases, allergy, transplant rejection, diseases involving degradation and/or disruption of cartilage homeostasis, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or interferons.

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Synthetic Route of 114525-81-4, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.114525-81-4, Name is (R)-4-(tert-Butoxycarbonyl)thiomorpholine-3-carboxylic acid, molecular formula is C10H17NO4S. In a Article£¬once mentioned of 114525-81-4

Design of Gut-Restricted Thiazolidine Agonists of G Protein-Coupled Bile Acid Receptor 1 (GPBAR1, TGR5)

Bile acid signaling and metabolism in the gastrointestinal tract have wide-ranging influences on systemic disease. G protein-coupled bile acid receptor 1 (GPBAR1, TGR5) is one of the major effectors in bile acid sensing, with demonstrated influence on metabolic, inflammatory, and proliferative processes. The pharmacologic utility of TGR5 agonists has been limited by systemic target-related effects such as excessive gallbladder filling and blockade of gallbladder emptying. Gut-restricted TGR5 agonists, however, have the potential to avoid these side effects and consequently be developed into drugs with acceptable safety profiles. We describe the discovery and optimization of a series of gut-restricted TGR5 agonists that elicit a potent response in mice, with minimal gallbladder-related effects. The series includes 12 (TGR5 EC50: human, 143 nM; mouse, 1.2 nM), a compound with minimal systemic availability that may have therapeutic value to patients with type 2 diabetes mellitus, nonalcoholic steatohepatitis, or inflammatory bowel disease.

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CHEMOKINE CXCR4 RECEPTOR MODULATORS AND USES RELATED THERETO

The disclosure relates to chemokine CXCR4 receptor modulators and uses related thereto. The receptor modulators can be formulated to form pharmaceutical compositions comprising the disclosed compounds or pharmaceutically acceptable salts or prodrugs thereof. The compositions may be used for managing CXCR4 related conditions, typically prevention or treatment of viral infections abnormal cellular proliferation, retinal degeneration, inflammatory diseases, or as an immunostimulant or immunosuppressant or for managing cancer and may be administered with another active ingredient such as an antiviral agent or chemotherapeutic agent.

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ANTIBACTERIAL QUINOLINE DERIVATIVES

The present invention relates to novel subst ituted quinoline derivatives according to the general Formula (Ia) or Formula (Ib): including any stereochemically isomeric form thereof, a pharmaceutically acceptable salt thereof, a N-oxide form thereof or a solvate thereof. The claimed compounds are useful for the treatment of a bacterial infection. Also claimed is a composition comprising a pharmaceutically acceptable carrier and, as active ingredient, a therapeutically effective amount of the claimed compounds, the use of the claimed compounds or composit ions for the manufacture of a medicament for the treatment of a bacterial infection and a process for preparing the claimed compounds.

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Thiomorpholine – Wikipedia,
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