Category: 114525-81-4

114525-81-4, An article , which mentions 114525-81-4, molecular formula is C10H17NO4S. The compound – (R)-4-(tert-Butoxycarbonyl)thiomorpholine-3-carboxylic acid played an important role in people’s production and life.

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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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

In an article, published in an article,authors is Blizzard, Timothy A., once mentioned the application of 114525-81-4, Name is (R)-4-(tert-Butoxycarbonyl)thiomorpholine-3-carboxylic acid,molecular formula is C10H17NO4S, is a conventional compound. this article was the specific content is as follows. 114525-81-4

Heterocyclic core analogs of a direct thrombin inhibitor

Thrombin is a serine protease that plays a key role in blood clotting. Pyrrolidine 1 is a potent thrombin inhibitor discovered at Merck several years ago. Seven analogs (2-8) of 1 in which the pyrrolidine core was replaced with various heterocycles were prepared and evaluated for activity against thrombin, clotting factors VIIa, IXa, Xa, and XIIa, and trypsin. The thiomorpholine analog 6 was the most active, essentially matching the thrombin inhibitory activity of 1 with slightly improved selectivity over trypsin.

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Chemistry is the experimental and theoretical study of materials on their properties at both the macroscopic and microscopic levels. 114525-81-4. In a patent£¬Which mentioned a new discovery about 114525-81-4, molcular formula is C10H17NO4S, introducing its new discovery.

MODULATORS OF THE G PROTEIN-COUPLED MAS RECEPTOR AND THE TREATMENT OF DISORDERS RELATED THERETO

The present invention relates to compounds of Formula (I) and pharmaceutically acceptable salts, solvates, and hydrates thereof that are useful in methods of treatment and alleviation of diseases and disorders of the heart, brain, kidney, immune, and reproductive system resulting from ischemia, or reperfusion subsequent to ischemia, and any downstream complication(s) related thereto. The present invention further relates to methods of treatment and alleviation of diseases and disorders of the vasculature resulting from vasoconstriction or hypertension and any downstream complications resulting from elevated blood pressure and/or reduced tissue perfusion

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

114525-81-4, 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, 114525-81-4, name is (R)-4-(tert-Butoxycarbonyl)thiomorpholine-3-carboxylic acid, introducing its new discovery.

Inhibitors of &alpha4&beta1 mediated cell adhesion

The present invention relates to compound of formula (I), that are potent inhibitors of alpha4beta1 mediated adhesion to either VCAM or CS-1 and which could be useful for the treatment of inflammatory diseases. Specifically, the molecules of the present invention can be used for treating or preventing alpha4beta1 adhesion mediated conditions in a mammal such as a human. This method may comprise administering to a mammal or a human patient an effective amount of the compound or composition as explained in the present specification.

Note that a catalyst decreases the activation energy for both the forward and the reverse reactions and hence accelerates both the forward and the reverse reactions.114525-81-4, you can also check out more blogs about114525-81-4

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Thiomorpholine – Wikipedia,
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114525-81-4, Chemistry is the science of change. But why do chemical reactions take place? Why do chemicals react with each other? The answer is in thermodynamics and kinetics.In a document type is Article, the author is Gong, Hongwei and a compound is mentioned, 114525-81-4, (R)-4-(tert-Butoxycarbonyl)thiomorpholine-3-carboxylic acid, introducing its new discovery.

Design and synthesis of a series of pyrido[2,3-d]pyrimidine derivatives as CCR4 antagonists

A series of pyrido[2,3-d]pyrimidine derivatives were designed and synthesized based on known CC chemokine receptor 4 (CCR4) antagonists. The activities of all the newly synthesized compounds were evaluated using a chemotaxis inhibition assay. Compound 6b was proven to be a potent CCR4 antagonist that can block cell chemotaxis induced by macrophage-derived chemokine (MDC), thymus and activation regulated chemokine (TARC), and CKLF1, the natural ligands of CCR4. In addition, compound 6b is more effective than budesonide in the murine rhinitis model. The intravenous injection LD 50 of compound 6b is 175 mg/kg and the oral LD50 is greater than 2,000 mg/kg.

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114525-81-4, Chemistry is the science of change. But why do chemical reactions take place? Why do chemicals react with each other? The answer is in thermodynamics and kinetics.In a document type is Article, the author is Gopalakrishnan, Ranganath and a compound is mentioned, 114525-81-4, (R)-4-(tert-Butoxycarbonyl)thiomorpholine-3-carboxylic acid, introducing its new discovery.

Evaluation of synthetic FK506 analogues as ligands for the FK506-binding proteins 51 and 52

The FK506-binding proteins (FKBP) 51 and 52 are cochaperones that modulate the signal transduction of steroid hormone receptors. Both proteins have been implicated in prostate cancer. Furthermore, single nucleotide polymorphisms in the gene encoding FKBP51 have been associated with a variety of psychiatric disorders. Rapamycin and FK506 are two macrocyclic natural products that bind to these proteins indiscriminately but with nanomolar affinity. We here report the cocrystal structure of FKBP51 with a simplified alpha-ketoamide analogue derived from FK506 and the first structure-activity relationship analysis for FKBP51 and FKBP52 based on this compound. In particular, the tert-pentyl group of this ligand was systematically replaced by a cyclohexyl ring system, which more closely resembles the pyranose ring in the high-affinity ligands rapamycin and FK506. The interaction with FKBPs was found to be surprisingly tolerant to the stereochemistry of the attached cyclohexyl substituents. The molecular basis for this tolerance was elucidated by X-ray cocrystallography.

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Chemistry is traditionally divided into organic and inorganic chemistry. 114525-81-4, The former is the study of compounds containing at least one carbon-hydrogen bonds.In a patent£¬Which mentioned a new discovery about 114525-81-4

INHIBITORS OF HCV NS5A

Provided herein are compounds, pharmaceutical compositions and combination therapies for inhibition of hepatitis C.

One of the oldest and most widely used commercial enzyme inhibitors is aspirin, 114525-81-4, which selectively inhibits one of the enzymes involved in the synthesis of molecules that trigger inflammation. you can also check out more blogs about 114525-81-4

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Thiomorpholine | C4H9NS – PubChem

Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In a patent, 114525-81-4, molecular formula is C10H17NO4S, introducing its new discovery. 114525-81-4

INHIBITORS OF HCV NS5A

Provided herein are compounds, pharmaceutical compositions and combination therapies for inhibition of hepatitis C.

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

Each compound has different characteristics, and only by selecting the characteristics of the compound suitable for a specific situation can the compound be applied on a large scale. 114525-81-4, name is (R)-4-(tert-Butoxycarbonyl)thiomorpholine-3-carboxylic acid. This compound has unique chemical properties. The synthetic route is as follows. 114525-81-4

To a 25 mL round bottom flask, Intermediate 7 (540 mg, 1.45 mmol), Intermediate 9 (359 mg, 1.45 mmol), EDCI (418 mg, 2.18 mmol), HOBt (294 mg, 2.18 mmol), DIEA (374 mg, 2.9 mmol) and tetrahydrofuran (9 mL) were added, and stirred at room temperature overnight. Thereafter, the reaction product was subjected to vacuum distillation for removal of solvent, dissolved with water, and extracted 3 times with ethyl acetate. The extracts were combined, washed 3 times with saturated brine, concentrated, and separated through a silica gel column (eluent: petroleum ether/ethyl acetate), to give 688 mg of a white foamy solid product, yield 78.8%.1H-NMR (400 MHz, CDCl3) delta ppm: 7.42 (1H, d, J=1.12 Hz), 7.27 (2H, m), 5.75 (1H, s), 5.19 (1H, s), 4.58 (2H, s), 3.95-3.44 (10H, brm), 3.12 (1H, m), 2.82 (2H, m), 2.43 (2H, m), 1.92 (9H, s); EI-MS (m/z): 601.1 [M+H]+.

While traditionally a conservative industry, chemical producers will need to modernize their PR strategies to stay relevant. 114525-81-4, we look forward to future research findings about .

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Patent; Li, Song; Wang, Ying; Xiao, Junhai; Ma, Dalong; Gong, Hongwei; Qi, Hui; Wang, Lili; Ling, Xiaomei; Zheng, Zhibing; Zhang, Yang; Zhong, Wu; Li, Meina; Xie, Yunde; Xu, Enquan; Li, Xingzhou; Ma, Jing; Zhao, Guoming; Zhou, Xinbo; Wang, Xiaokui; Liu, Hongying; US2015/126500; (2015); A1;,
Thiomorpholine – Wikipedia
Thiomorpholine | C4H9NS – PubChem

Each compound has different characteristics, and only by selecting the characteristics of the compound suitable for a specific situation can the compound be applied on a large scale. 114525-81-4, name is (R)-4-(tert-Butoxycarbonyl)thiomorpholine-3-carboxylic acid. This compound has unique chemical properties. The synthetic route is as follows. 114525-81-4

Referring to Scheme 5-2, a mixture of compound 17 (667 mg, 2.4 mmol), (R)-N-Boc-thiomorpholine-3-carboxylic acid (594 mg, 2.4 mmol) and Et3N (486 mg, 4.8 mmol) in EtOAc (20 mL) was stirred at rt for 2h. Subsequently, the reaction mixture was concentrated and the residue was dried in vacuo to give crude compound 19, which was used for the next step without further purification. LC-MS (ESI): m/z 466.0 (M+Na)+.

While traditionally a conservative industry, chemical producers will need to modernize their PR strategies to stay relevant. 114525-81-4, we look forward to future research findings about .

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Patent; PRESIDIO PHARMACEUTICALS, INC.; LI, Leping; ZHONG, Min; WO2011/150243; (2011); A1;,
Thiomorpholine – Wikipedia
Thiomorpholine | C4H9NS – PubChem