cas 494769-34-5, (4-Formylthiazol-2-yl)carbamic acid tert-butyl ester

Articles about 494769-34-5Total 12 be found

4,6-Substituted-1H-Indazoles as potent IDO1/TDO dual inhibitors
Indoleamine 2,3-dioxygenase 1 (IDO1) and tryptophan 2,3-dioxygenase (TDO) are constitutively overexpressed in many types of cancer cells and exert important immunosuppressive functions. In this article, a series of 4,6-substituted-1H-indazole derivatives were synthesized and evaluated the inhibitory activities against IDO1 and TDO, as well as their structure-activity relationships (SARs). Among these, compound 35 displayed the most IDO1 inhibitory potency with an IC50 value of 0.74 μM in an enzymatic assay and 1.37 μM in HeLa cells. Quantitative analysis of the Western blot results indicated that 35 significantly decreased the INFγ-induced IDO1 expression in a concentration-dependent manner. In addition, 35 showed promising TDO inhibition with an IC50 value of 2.93 μM in the enzymatic assay and 7.54 μM in A172 cells. Moreover, compound 35 exhibited in vivo antitumor activity in the CT26 xenograft model. These findings suggest that 1H-indazole derivative 35 is a potent IDO1/TDO dual inhibitor, and has the potential to be developed for IDO1/TDO-related cancer treatment.
Yang, Lingling,Chen, Yang,He, Junlin,Njoya, Emmanuel Mfotie,Chen, Jianjun,Liu, Siyan,Xie, Congqiang,Huang, Wenze,Wang, Fei,Wang, Zhouyu,Li, Yuzhi,Qian, Shan
p. 1087 - 1098
(2019/02/19)

SPIROCYCLIC HAT INHIBITORS AND METHODS FOR THEIR USE
Compounds having a structure of Formula (IX) or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof, wherein R1, R2a, R2b, R3a, R3b, R4a, R4b, Q1----Q2, R6, R7, A, B, W, x, and y are as defined herein and are provided. Pharmaceutical compositions comprising such compounds and methods for treating various HAT-related conditions or diseases, including cancer, by administration of such compounds are also provided.
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(2016/04/10)

Novel 6-amino acid heteroaryldihydropyrimidines for the treatment and prophylaxis of hepatitis B virus infection
The invention provides novel compounds having the general formula: wherein R1, R2, R3, R4 and A are as described herein, compositions including the compounds and methods of using the compounds.
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Paragraph 0439; 0443

(2015/02/19)

TRICYCLIC PIPERIDINE COMPOUNDS
The present invention relates to compounds of the formula (I), wherein R, R1a, R1b, R2, R3, and X are as described in the description, to their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of formula (I), to methods for the preparation of such compounds of formula (I), and especially to their use as TPH modulators.
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(2015/06/08)

6-AMINO ACID HETEROARYLDIHYDROPYRIMIDINES FOR THE TREATMENT AND PROPHYLAXIS OF HEPATITIS B VIRUS INFECTION
The invention provides novel compounds having the general formula:, wherein R1, R2, R3, R4 and A are as described herein, compositions including the compounds and methods of using the compounds.
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Page/Page column 126

(2014/03/26)

1-[M-CARBOXAMIDO(HETERO)ARYL-METHYL]-HETEROCYCLYL-CARBOXAMIDE DERIVATIVES
The present invention relates to 1-[m-carboxamido(hetero)aryl-methyl]-heterocycyl- carboxamide compounds of formula (I) wherein X, Ar1, R1, R2, R3, R4, R5a, R5b and p are as described in the description, to their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of formula (I), and especially to their use as CXCR7 receptor modulators.
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Page/Page column 55-56

(2014/01/09)

1-[M-CARBOXAMIDO(HETERO)ARYL-METHYL]-PIPERIDINE-4-CARBOXAMIDE DERIVATIVES
The present invention relates to 1-[m-Carboxamido(hetero)aryl-methyl]-piperidine-4-carboxamide derivatives of formula (I) wherein X, Ar1, R1, R2, R3, R4, R5 and p are as described in the description, to their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of formula (I), and especially to their use as CXCR7 receptor modulators.
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Paragraph 0579

(2014/02/15)

TRICYCLIC SPIROCYCLE DERIVATIVES AND METHODS OF USE
The present invention relates to novel Tricyclic Spirocycle Derivatives, pharmaceutical compositions comprising the Tricyclic Spirocycle Derivatives and the use of these compounds for treating or preventing allergy, an allergy-induced airway response, congestion, a cardiovascular disease, an inflammatory disease, a gastrointestinal disorder, a neurological disorder, a metabolic disorder, obesity or an obesity-related disorder, diabetes, a diabetic complication, impaired glucose tolerance or aired fasting glucose.
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Page/Page column 41

(2011/07/29)

NOVEL GLUCOKINASE ACTIVATORS AND METHODS OF USING SAME
Compounds are provided which are phosphonate and phosphinate activators and thus are useful in treating diabetes and related diseases and have the structure wherein is a heteroaryl ring; R4 is —(CH2)n-Z-(CH2)m—PO(OR7)(OR8), —(CH2)nZ-(CH2)m—PO(OR7)Rg, —(CH2)n-Z-(CH2)m—OPO(OR7)Rg, —(CH2)nZ—(CH2)m—OPO(R9)(R10), or —(CH2)nZ—(CH2)m—PO(R9)(R10);R5 and R6 are independently selected from H, alkyl and halogen;Y is R7(CH2)s or is absent; andX, n, Z, m, R4, R5, R6, R7, and s are as defined herein; or a pharmaceutically acceptable salt thereof. A method for treating diabetes and related diseases employing the above compounds is also provided.
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Page/Page column 60

(2008/06/13)

Naphthyridin derivatives
The present invention relates to heterocyclic derivatives of formula I wherein R1, R2 and R3 are as defined in the description and claims, which compounds are metabotropic glutamate receptor 5 antagonists.
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Page/Page column 32

(2008/06/13)

Substituted heteroaryl amide modulators of glucocorticoid receptor, AP-1, and/or NF-kB activity and use thereof
The present invention relates to new class of non-steroidal compounds which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-κB activity including obesity, diabetes, inflammatory- and immune-associ
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Page/Page column 38

(2008/06/13)

Seleno compounds containing nitrone moiety, their preparation and their therapeutic uses
The present invention provides novel seleno compounds containing nitrone moiety, a process for preparing the same, the use of the novel compounds as therapeutics for treating and/or preventing various medical dysfunctions and diseases arising from reactiv
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(2008/06/13)