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1,3,4-OXADIAZOLE SULFAMIDE DERIVATIVE COMPOUNDS AS HISTONE DEACETYLASE 6 INHIBITOR, AND THE PHARMACEUTICAL COMPOSITION COMPRISING THE SAME

The present invention relates to novel compounds having histone deacetylase 6 (HDAC6) inhibitory activity, stereoisomers thereof or pharmaceutically acceptable salts thereof, the use thereof for the preparation of therapeutic medicaments, pharmaceutical compositions containing the same, a method for treating diseases using the composition, and methods for preparing the novel compounds. The novel compounds, stereoisomers thereof or pharmaceutically acceptable salts thereof according to the present invention have histone deacetylase (HDAC) inhibitory activity and are effective for the prevention or treatment of HDAC6-mediated diseases, including infectious diseases; neoplasms; endocrine, nutritional and metabolic diseases; mental and behavioral disorders; neurological diseases; diseases of the eye and adnexa; cardiovascular diseases; respiratory diseases; digestive diseases; diseases of the skin and subcutaneous tissue; diseases of the musculoskeletal system and connective tissue; or congenital malformations, deformations and chromosomal abnormalities.

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

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Anilinoquinazoline inhibitors of the RET kinase domain – Elaboration of the 7-position

We have previously reported a series of anilinoquinazoline derivatives as potent and selective biochemical inhibitors of the RET kinase domain. However, these derivatives displayed diminished cellular potency. Herein we describe further optimisation of the series through modification of their physicochemical properties, delivering improvements in cell potency. However, whilst cellular selectivity against key targets could be maintained, combining cell potency and acceptable pharmacokinetics proved challenging.

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ANTIMICROBIAL COMPOUNDS AND METHODS OF MAKING AND USING THE SAME

The present invention relates generally to the field of antimicrobial compounds and to methods of making and using them. These compounds are useful for treating, preventing, and reducing the risk of microbial infections in humans and animals.

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HETEROCYCLIC COMPOUND

Provided is a compound or a salt thereof, which has an excellent JAK inhibitory action, and is useful as a prophylactic or therapeutic agent for autoimmune diseases (rheumatoid arthritis, psoriasis, inflammatory bowel disease, Sjogren’s syndrome, Behcet’s syndrome, multiple sclerosis, systemic lupus erythematosus, etc.), cancer (leukemia, uterine leiomyosarcoma, prostate cancer, multiple myeloma, cachexia, myelofibrosis, etc.) and the like. The present invention relates to a compound represented by the formula (I) wherein each symbol is as defined in the present specification, or a salt thereof.

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Synthetic Route of 39093-93-1, 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 some cases, the catalyzed mechanism may include additional steps.In a article, 39093-93-1, molcular formula is C4H9NO2S, introducing its new discovery.

TRICYCLIC HETEROCYCLIC COMPOUNDS AS PHOSPHOINOSITIDE 3-KINASE INHIBITORS

The invention relates to a compound of formula I: (I) or a pharmaceutically acceptable salt thereof and/or stereoisomers thereof. The compounds of the invention are useful in therapy.

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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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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

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C-3 NOVEL TRITERPENONE WITH C-28 REVERSE AMIDE DERIVATIVES AS HIV INHIBITORS

Formula (I) The invention relates to C-3 novel triterpenone with C-28 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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PYRROLIDINE DERIVATIVES AS DUAL NK1/NK3 RECEPTOR ANTAGONISTS

The invention relates to pyrrolidine derivatives of formulawherein R1,R2,R3,n, and o are defined in the specification and to pharmaceutically active acid-addition salts thereof. Compounds of formula I have a high affinity simultaneously to both the NK1 and the NK3 receptors (dual NK1/NK3 receptor antagonists), useful in the treatment of schizophrenia.

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

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The proportionality constant is the rate constant for the particular unimolecular reaction. the reaction rate is directly proportional to the concentration of the reactant. I hope my blog about 39093-93-1 is helpful to your research. Product Details of 39093-93-1

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PROCESS FOR THE PREPARATION OF ISOXAZOLYL-METHOXY-NICOTINIC ACIDS

The present invention relates to a process for the preparation of a compound of formula (I) which is useful as an intermediate in the preparation of active pharmaceutical compounds from a compound of formula (IV) wherein R1 and R2 are as defined herein,.

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Thiomorpholine – Wikipedia,
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4- (4-(HETEROCYCLYLALKOXY}PHENYL)-1-(HETEROCYCLYL-CARBONYL)PIPERIDINE DERIVATIVES AND RELATED COMPOUNDS AS HISTAMINE H3 ANTAGONISTS FOR THE TREATMENT OF NEUROLOGICAL DISEASES SUCH AS ALZHEIMER’S

The present invention provides, in a first aspect, a compound of formula (I) or a pharmaceutically acceptable salt thereof wherein: R1 represents-C1-6 alkyl-O-C1-6 alkyl,-C3-8 cycloalkyl, aryl, heterocyclyl, heteroaryl and other groups; X represents a bond, O, CO, OCH2, CH2 O or SO2; Z represents CO, CONR10 or SO2; R10 represents hydrogen, C1-6 alkyl,-C3-8 cycloalkyl, aryl, heterocyclyl, heteroaryl; A represents a single or a double bond; m and n independently represent 0, 1 or 2; R2 represents hydrogen, C1-6 alkyl or C1-6 alkoxy; R3 represents halogen, C1-6 alkyl, hydroxy, C1-6 alkoxy, cyano, amino,-COC1-6 alkyl,-SO2C1-6 alkyl or trifluoromethyl; R4 represents-(CH2)q-NR11R12 or a group of formula (i) wherein all the other substituents are as defined in claim 1. Compounds of formula (I) and their pharmaceutically acceptable salts have affinity for and are antagonists and/or inverse agonists of the histamine H3 receptor and are believed to be of potential use in the treatment of neurological diseases including Alzheimer’s disease.

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem