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CATHEPSIN CYSTEINE PROTEASE INHIBITORS

This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

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SUBSTITUTED PYRAZOLO[3,4-b]PYRIDIN-6-CARBOXYLIC ACIDS AND METHOD OF USE

The present invention provides for compounds of formula (I) wherein R1, R2, R3, and R4 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions mediated and modulated by CFTR, including cystic fibrosis, Sjoegren’s syndrome, pancreatic insufficiency, chronic obstructive lung disease, and chronic obstructive airway disease. Also provided are pharmaceutical compositions comprised of one or more compounds of formula (I).

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

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C-3 NOVEL TRITERPENONE WITH C-17 REVERSE AMIDE DERIVATIVES AS HIV INHIBITORS

The present invention relates to C-3 novel triterpenone with C-17 reverse amide compounds of Formula (I); and pharmaceutically acceptable salts thereof, wherein ring Formula (II), R1, R2, R3, R4, R5, R6, R7, ‘n’ and ‘m’ are as defined in Formula (I). The invention also relates to C-3 novel triterpenone with C-17 reverse amide derivatives, related compounds, and pharmaceutical compositions useful for the therapeutic treatment of viral diseases and particularly HIV mediated diseases.

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

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PYRROLOPYRIDINEAMINO DERIVATIVES AS MPS1 INHIBITORS

The present invention relates to the use of certain pyrrolopyridineamino derivatives (hereinafter referred to as “PPA derivatives”), particularly 1H-pyrrolo[3,2-c]pyridine-6-amino derivatives, to inhibit the spindle checkpoint function of Monospindle 1 (Mpsl also known as TTK) kinases either directly or indirectly via interaction with the Mps kinase itself. In particular, the present invention relates to PPA derivatives for use as therapeutic agents for the treatment and/or prevention of proliferative diseases, such as cancer. The present invention also relates to processes for the preparation of the PPA derivatives, and pharmaceutical compositions comprising them. Formula (1)

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

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HETEROCYCLIC COMPOUND

The present invention provide a heterocyclic compound having a HDAC inhibitory action, and useful for the treatment of autoimmune diseases and/or inflammatory diseases, graft versus host disease, cancers, central nervous diseases including neurodegenerative diseases, Charcot-Marie-Tooth disease and the like, and a pharmaceutical composition comprising the compound. The present invention relates to a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof.

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

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Inhibiting SSAO/VAP – 1 of amine compounds and their use in medicine (by machine translation)

The invention relates to a method for inhibiting semicarbazide-sensitive oxidase (SSAO) and/or vascular adhesion protein – 1 (VAP – 1) inhibitors of amine compounds and their use in medicine, further relates to the pharmaceutical composition. Said compound of the invention and pharmaceutical composition can be used for treating inflammation and/or inflammation-related diseases, diabetes and/or diabetes-related diseases, psychiatric disorders, ischemic disease, vascular disease, fibrosis or tissue transplant rejection. (by machine translation)

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

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Discovery and Optimization of 5-Amino-1,2,3-triazole-4-carboxamide Series against Trypanosoma cruzi

Chagas’ disease, caused by the protozoan parasite Trypanosoma cruzi, is the most common cause of cardiac-related deaths in endemic regions of Latin America. There is an urgent need for new safer treatments because current standard therapeutic options, benznidazole and nifurtimox, have significant side effects and are only effective in the acute phase of the infection with limited efficacy in the chronic phase. Phenotypic high content screening against the intracellular parasite in infected VERO cells was used to identify a novel hit series of 5-amino-1,2,3-triazole-4-carboxamides (ATC). Optimization of the ATC series gave improvements in potency, aqueous solubility, and metabolic stability, which combined to give significant improvements in oral exposure. Mitigation of a potential Ames and hERG liability ultimately led to two promising compounds, one of which demonstrated significant suppression of parasite burden in a mouse model of Chagas’ disease.

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

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COMPOSITIONS AND METHODS FOR MODULATING THE WNT SIGNALING PATHWAY

The present invention relates to compositions and methods for modulating the Wnt signaling pathway, using compounds having Formula (1) and (3): wherein A, B, Y and Z all represent rings, and R 1 , R 2 , R 3 are as defined herein.

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

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5H-PYRIDO[3,2-B]INDOLE COMPOUNDS AS ANTICANCER AGENTS

The present invention is directed to tricyclic compounds of formula (I), pharmaceutically acceptable compositions comprising compounds of the invention and said compositions for use in methods for the treatment of various disorders in particular cancer.

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

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Asymmetric Hydrogenation of Unfunctionalized Tetrasubstituted Acyclic Olefins

Asymmetric hydrogenation has evolved as one of the most powerful tools to construct stereocenters. However, the asymmetric hydrogenation of unfunctionalized tetrasubstituted acyclic olefins remains the pinnacle of asymmetric synthesis and an unsolved challenge. We report herein the discovery of an iridium catalyst for the first, generally applicable, highly enantio- and diastereoselective hydrogenation of such olefins and the mechanistic insights of the reaction. The power of this chemistry is demonstrated by the successful hydrogenation of a wide variety of electronically and sterically diverse olefins in excellent yield and high enantio- and diastereoselectivity.

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem