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(Azetidin-1-ylalkyl) lactams as tachykinin antagonists

The present invention provides compounds of formula (I) and the pharmaceutically acceptable salts thereof, wherein R is C3 -C7 cycloalkyl, aryl or C1 -C6 alkyl, said C1 -C6 alkyl, said C1 -C6 alkyl being optionally substituted by fluoro, COOH, –COO(C1 -C4 alkyl), C3 -C7 cycloalkyl, adamantyl, aryl or het1, and said C3 -C7 cycloalkyl being optionally substituted by 1 or 2 substituents each independently selected from C1 -C4 alkyl, C3 -C7 cycloalkyl, C1 -C4 alkoxy, hydroxy, fluoro, fluoro (C1 -C4) alkyl and fluoro (C1 -C4) Alkoxy; R1 is phenyl, naphthyl, thienyl, benzothienyl or indolyl, each optionally substituted by 1 or 2 substituents each independently selected from C1 -C4 alkyl, C1 -C4 alkoxy, halo and trifluormethyl; R2 is –CO2 H, –CONR3 R4, –CONR5 (C3 -C7 cycloalkyl), –NR5 (C2 -C5 alkanoyl), –NR3 R4, –NR5 CONR5 R6, (C3 -C7 cycloalkyl-C1 -C4 alkyl)R5 N–, –NR5 COCF3, –NR5 SO2 CF3, –NR5 (SO2 C1 -C4 alkyl), –NR5 SO2 NR5 R6, –NR5 (SO2 aryl), –N(aryl) (SO2 C1 -C4 alkyl), –OR5, –O(C3 -C7 cycloalkyl), –SO2 NR5 R6, het3 or a group of formulas: (a), (b), (c), (d), (e), (f), (g) or (h); X is C1 -C4 alkylene; X1 is a direct link or C1 -C6 alkylene; X2 is a direct link, CO, SO2, or NR5 CO; and m is 0, 1 or 2; together with intermediates used in the preparation of compositions containing and the use as tachykinin angatonists of such derivatives. STR1

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Reference£º
Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

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PERIPHERALLY RESTRICTED DIPHENYL PURINE DERIVATIVES

The invention provides compounds capable o f acting as antagonists at cannabanoid receptors according to the following formula: Such compounds may be used to treat conditions for which the cannabinoid receptor system has been implicated, such as obesity, liver disease, diabetes, pain, and inflammation

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

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Discovery of novel chalcone-dithiocarbamates as ROS-mediated apoptosis inducers by inhibiting catalase

Novel chalcone-dithiocarbamate hybrids were designed, synthesized and evaluated for antiproliferative activity against selected cancer cell lines (MGC803, MCF7, and PC3). Among these analogues, (E)-2-oxo-2-((4-(3-(3,4,5-trimethoxyphenyl)acryloyl)phenyl)amino)ethyl-4-(2-hydroxyethyl)piperazine-1-carbodithioate (12d) showed the best inhibitory activity against PC3 cells (IC50 = 1.05 muM). Cellular mechanism studies elucidated 12d could inhibit colony formation, arrest cell cycle at G2/M phase and induce DNA damage against PC3 cells. Compound 12d also induced mitochondrial apoptosis by caspase activation, MMP decrease, ROS production and catalase (CAT) inhibition. Importantly, 12d inhibited epithelial-mesenchymal transition (EMT) process by regulating EMT-related proteins (E-cadherin, N-cadherin, Vimentin, MMP2, MMP9). These results indicated that 12d is a promising lead compound and deserves further investigation for prevention and treatment of human prostate cancer.

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

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We¡¯ll also look at important developments in the pharmaceutical industry because understanding organic chemistry is important in understanding health, medicine, the role of 39093-93-1, and how the biochemistry of the body works.Product Details of 39093-93-1

In homogeneous catalysis, the catalyst is in the same phase as the reactant. The number of collisions between reactants and catalyst is at a maximum.In a patent, 39093-93-1, name is Thiomorpholine 1,1-dioxide, introducing its new discovery. Product Details of 39093-93-1

4-SUBSTITUTED PYRROLO- AND PYRAZOLO-DIAZEPINES

BET protein-inhibitory, especially BRD2-, BRD3- and BRD4-inhibitory, 4-substituted pyrrolo- and pyrazolodiazepines of the general formula I are described, in which X, Y, n, m, p, R1, R2, R3, R4 and R5 are each as defined in the description, as are pharmaceutical compositions comprising the inventive compounds, and the prophylactic and therapeutic use thereof in the case of hyperproliferative disorders, especially in the case of neoplastic disorders. Also described is the use of the inventive compounds as BET protein inhibitors in benign hyperplasias, in atherosclerotic disorders, in sepsis, in autoimmune disorders, in vascular disorders, in viral infections, in neurodegenerative disorders, in inflammatory disorders and in male fertility control.

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

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Identification of novel 1,2,3,6-tetrahydropyridyl-substituted benzo[d]thiazoles: Lead generation and optimization toward potent and orally active EP1 receptor antagonists

Herein we described the design, synthesis and evaluation of a novel series of benzo[d]thiazole derivatives toward an orally active EP1 antagonist. Lead generation studies provided benzo[d]thiazole core from the four designed scaffolds. Optimization of this scaffold in terms of EP1 antagonist potency and ligand-lipophilicity efficiency (LLE; pIC50-clogP) led to a 1,2,3,6-tetrahydropyridyl-substituted benzo[d]thiazole derivative, 7r (IC50 1.1?nM; LLE 4.7), which showed a good pharmacological effect when administered intraduodenally in a 17-phenyl trinor-PGE2 (17-PTP)-induced overactive bladder model in rats.

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

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HETEROARYL SUBSTITUTED PYRROLOTRIAZINE AMINE COMPOUNDS AS PI3K INHIBITORS

Disclosed are compounds of Formula (I); or a salt thereof; wherein Qi is (i) C1, Br, I, -CN, -CH3, or -CF3; or (ii) pyrazole, triazole, or pyridinyl, each substituted with R1; Q2 is pyridinyl, indazolyl, isoquinolinyl, or benzo[d]imidazolyl substituted with R2 and R3; and R1, R2, and R3 are defined herein. Also disclosed are methods of using such compounds as modulators of PI3K, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing inflammatory and autoimmune diseases.

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

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Challenges in the Development of a Thiol-Based Broad-Spectrum Inhibitor for Metallo-beta-Lactamases

Pathogens, expressing metallo-beta-lactamases (MBLs), become resistant against most beta-lactam antibiotics. Besides the dragging search for new antibiotics, development of MBL inhibitors would be an alternative weapon against resistant bacterial pathogens. Inhibition of resistance enzymes could restore the antibacterial activity of beta-lactams. Various approaches to MBL inhibitors are described; among others, the promising motif of a zinc coordinating thiol moiety is very popular. Nevertheless, since the first report of a thiol-based MBL inhibitor (thiomandelic acid) in 2001, no steps in development of thiol based MBL inhibitors were reported that go beyond clinical isolate testing. In this study, we report on the synthesis and biochemical characterization of thiol-based MBL inhibitors and highlight the challenges behind the development of thiol-based compounds, which exhibit good in vitro activity toward a broad spectrum of MBLs, selectivity against human off-targets, and reasonable activity against clinical isolates.

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

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NOVEL COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS THEREOF FOR THE TREATMENT OF DISEASES

The present invention discloses compounds aceording to Formula I: wherein R1,R2a,X,Y,and Z are as defined herein. The present invention relates to compounds,methods for their production,pharmaceutical compositions comprising the same,and methods of treatment using the same,for the prophylaxis and/or treatment of inflammatory diseases,autoinflammatory diseases,autoimmune diseases,proliferative diseases,fibrotic diseases,transplantation rejection,diseases involving impairment of cartilage turnover,congenital cartilage malformation,diseases involving impairment of bone turnover,diseases associated with hypersecretion of IL-6,diseases associated with hypersecretion of TNFalpha,interferons,IL-12 and/or IL-23,respiratory diseases,endocrine and/or metabolic diseases,cardiovascular diseases,dermatological diseases,and/or abnormal angiogenesis associated diseases by administering the compound of the invention.

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

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HETEROCYCLIC MODULATORS OF HIF ACTIVITY FOR TREATMENT OF DISEASE

The present invention relates to compounds and methods which may be useful as inhibitors of HIF pathway activity for the treatment or prevention of cancer and other hypoxia-mediated diseases.

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

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BRIDGED HETEROCYCLIC COMPOUNDS AND METHODS OF USE

This disclosure relates to new compounds that may be used to modulate a histamine receptor in an individual. Novel compounds are described, including new bridged heterocyclic [4,3-b]indole compounds. Pharmaceutical compositions are also provided. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem