cas 17583-10-7, 2-AMINO-5,6-DIHYDRO-1,3-BENZOTHIAZOL-7(4H)-ONE

Articles about 17583-10-7Total 19 be found

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Hydrogen Peroxide-Mediated Rapid Room Temperature Metal-Free C(sp2)-H Thiocyanation of Amino Pyrazoles, Amino Uracils, and Enamines
A rapid metal-and additive-free room temperature method for C(sp2)-H thiocyanation of aminopyrazoles, aminoisoxazole, aminoisothiazole, amino uracils, and aliphatic enamines has been developed in an aqueous medium using hydrogen peroxide as a benign oxidant and ammonium thiocyanate as a thiocyanating agent. On the other hand, the reaction of hydrogen peroxide and ammonium thiocyanate followed by one-pot addition of NaOH provides the corresponding disulfides in the case of amino azoles, and pyrimidine-fused 2-amino thiazoles were observed in the case of aminouracils. The salient features of this method are the use of an eco-friendly oxidant, reaction tunability to access different products, wide substrate scope, and good to very good yields.
Ali, Danish,Panday, Anoop Kumar,Choudhury, Lokman H.
p. 13610 - 13620
(2020/11/27)

Copper-Catalyzed Thiolation of Terminal Alkynes Employing Thiocyanate as the Sulfur Source Leading to Enaminone-Based Alkynyl Sulfides under Ambient Conditions
A highly efficient protocol for copper-catalyzed thio-alkynylation of enaminone-based thiocyanates with terminal alkynes under mild conditions has been developed. This scalable amino group-directed thio-alkynylation proceeds in the open air with a broad substrate scope and an excellent yield. The demonstrated synthetic transformation creates the opportunity for a wide variety of sulfur-containing useful materials. Gram-scale synthesis and further synthetic transformations of alkynyl sulfides highlight the potential utility of the method.
Chandran,Pise, Ashwini,Shah, Suraj Kumar,Rahul,Suman,Tiwari, Keshri Nath
supporting information
p. 6557 - 6561
(2020/08/24)

Piperazinyl tetrahydrobenzothiazole oxime ether derivative and application thereof
The invention relates to a piperazinyl tetrahydrobenzothiazole oxime ether derivative shown as a general formula (I) and application of the piperazinyl tetrahydrobenzothiazole oxime ether derivative as a bactericide. The compound represents a novel bacter
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Paragraph 0048-0049

(2020/10/04)

Synthesis of novel derivatives of 7,8-dihydro-6H-imidazo[2,1-b][1,3]benzothiazol-5-one and their virus-inhibiting activity against influenza A virus
Influenza remains a highly pathogenic and hardly controlled human infection. The ability of selecting drug-resistant variants necessitates the search and development of novel anti-influenza drugs. Herein, we describe the synthesis and evaluation of a seri
Galochkina, Anastasia V.,Bollikanda, Rakesh K.,Zarubaev, Vladimir V.,Tentler, Dmitry G.,Lavrenteva, Irina N.,Slita, Alexander V.,Chirra, Nagaraju,Kantevari, Srinivas
(2018/12/13)

Discovery of cycloalkyl-fused N-thiazol-2-yl-benzamides as tissue non-specific glucokinase activators: Design, synthesis, and biological evaluation
Glucokinase (GK) activators are being developed for the treatment of type 2 diabetes mellitus (T2DM). However, existing GK activators have risks of hypoglycemia caused by over-activation of GK in islet cells and dyslipidemia caused by over-activation of intrahepatic GK. In the effort to mitigate risks of hypoglycemia and dyslipidemia while maintaining the promising efficacy of GK activator, we investigated a series of cycloalkyl-fused N-thiazol-2-yl-benzamides as tissue non-specific partial GK activators, which led to the identification of compound 72 that showed a good balance between in vitro potency and enzyme kinetic parameters, and protected β-cells from streptozotocin-induced apoptosis. Chronic treatment of compound 72 demonstrated its potent activity in regulation of glucose homeostasis and low risk of dyslipidemia with diabetic db/db mice in oral glucose tolerance test (OGTT). Moreover, acute treatment of compound 72 did not induce hypoglycemia in C57BL/6J mice even at 200 mg/kg via oral administration.
Wang, Zhengyu,Shi, Xiaofan,Zhang, Huan,Yu, Liang,Cheng, Yanhua,Zhang, Hefeng,Zhang, Huibin,Zhou, Jinpei,Chen, Jing,Shen, Xu,Duan, Wenhu
p. 128 - 152
(2017/08/10)

FUSED THIOPHENE AND THIAZOLE DERIVATIVES AS ROR GAMMA MODULATORS
The present invention provides fused thiophene and thiazole derivatives of formula (I), which may be therapeutically useful, more particularly as RORγ modulators; in which R1, R2, R3, R4, R5, R6, R7, X1, X2, L, m, n and ring A have the meanings given in the specification, and pharmaceutically acceptable salts thereof that are useful in the treatment and prevention of diseases or disorders, in particular their use in disease(s) or disorder(s) where there is an advantage in modulating RORγ receptor. The present invention also provides preparation of the compounds and pharmaceutical formulations comprising at least one of the fused thiophene and thiazole derivatives of formula (I), together with a pharmaceutically acceptable carrier, diluent or excipient therefor.
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(2015/07/16)

Identification and optimisation of 4,5-dihydrobenzo[1,2-d:3,4-d]bisthiazole and 4,5-dihydrothiazolo[4,5-h]quinazoline series of selective phosphatidylinositol-3 kinase alpha inhibitors
Abstract A cyclisation within a 4′,5-bisthiazole (S)-proline-amide-urea series of selective PI3Kα inhibitors led to a novel 4,5-dihydrobenzo[1,2-d:3,4-d]bisthiazole tricyclic sub-series. The synthesis and optimisation of this 4,5-dihydrobenzo[1,2-d:3,4-d]bisthiazole sub-series and the expansion to a related tricyclic 4,5-dihydrothiazolo[4,5-h]quinazoline sub-series are described. From this work analogues including 11, 12, 19 and 23 were identified as potent and selective PI3Kα inhibitor in vivo tool compounds.
Fairhurst, Robin A.,Gerspacher, Marc,Imbach-Weese, Patricia,Mah, Robert,Caravatti, Giorgio,Furet, Pascal,Fritsch, Christine,Schnell, Christian,Blanz, Joachim,Blasco, Francesca,Desrayaud, Sandrine,Guthy, Daniel A.,Knapp, Mark,Arz, Dorothee,Wirth, Jasmin,Roehn-Carnemolla, Esther,Luu, Van Huy
p. 3575 - 3581
(2015/08/06)

Discovery of imidazo[2,1- b ]thiazole HCV NS4B inhibitors exhibiting synergistic effect with other direct-acting antiviral agents
The design, synthesis, and SAR studies of novel inhibitors of HCV NS4B based on the imidazo[2,1-b]thiazole scaffold were described. Optimization of potency with respect to genotype 1b resulted in the discovery of two potent leads 26f (EC50 = 16
Wang, Ning-Yu,Xu, Ying,Zuo, Wei-Qiong,Xiao, Kun-Jie,Liu, Li,Zeng, Xiu-Xiu,You, Xin-Yu,Zhang, Li-Dan,Gao, Chao,Liu, Zhi-Hao,Ye, Ting-Hong,Xia, Yong,Xiong, Ying,Song, Xue-Jiao,Lei, Qian,Peng, Cui-Ting,Tang, Hong,Yang, Sheng-Yong,Wei, Yu-Quan,Yu, Luo-Ting
p. 2764 - 2778
(2015/04/14)

UREA DERIVATIVE HAVING PI3K INHIBITORY ACTIVITY
Provided is a compound or a pharmaceutically acceptable salt thereof which inhibits the activity of PI3K to regulate many biological processes including the growth, differentiation, survival, proliferation, migration, metabolism, and the like of cells and is therefore useful for the prophylaxis/therapy of diseases including inflammatory diseases, arteriosclerosis, vascular/circulatory diseases, cancer/tumors, immune system diseases, cell proliferative diseases, infectious diseases, and the like. The above problem was solved by providing a urea derivative shown in the present specification, or a pharmaceutically acceptable salt thereof.
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(2012/03/26)

Convenient and simple synthesis of 2-aminothiazoles by the reaction of α-halo ketone carbonyls with ammonium thiocyanate in the presence of N-methylimidazole
Substituted 2-aminothiazole derivatives were obtained as a result of N-methylimidazole catalyzed cyclization of α-halo ketone carbonyls with ammonium thiocyanate in water-alcoholic media. The generality of the method has been demonstrated by screening a series of aromatic/heteroaromatic/aliphatic α-halo ketones, α-halo β-diketones, and α-halo β-ketoesters. The developed method is simple, mild, and general route for the preparation of diversely functionalized 2-aminothiazoles in good to moderate yields from readily available starting materials.
Meshram,Thakur, Pramod B.,Madhu Babu,Bangade, Vikas M.
p. 5265 - 5269
(2012/10/30)

Design, synthesis, and evaluation of 2-methyl- and 2-amino-N-aryl-4,5- dihydrothiazolo[4,5-h]quinazolin-8-amines as ring-constrained 2-anilino-4-(thiazol-5-yl)pyrimidine cyclin-dependent kinase inhibitors
Following the recent discovery and development of 2-anilino-4-(thiazol-5- yl)pyrimidine cyclin dependent kinase (CDK) inhibitors, a program was initiated to evaluate related ring-constrained analogues, specifically, 2-methyl- and 2-amino-N-aryl-4,5-dihydr
McIntyre, Neil A.,McInnes, Campbell,Griffiths, Gary,Barnett, Anna L.,Kontopidis, George,Slawin, Alexandra M. Z.,Jackson, Wayne,Thomas, Mark,Zheleva, Daniella I.,Wang, Shudong,Blake, David G.,Westwood, Nicholas J.,Fischer, Peter M.
supporting information; experimental part
p. 2136 - 2145
(2010/08/07)

THIAZOLYL-DIHYDRO-QUINAZOLINE
Disclosed are thiazolyl-dihydro-quinazolines of general formula (I) wherein the groups R1 to R4 have the meanings given in the claims and specification, the isomers thereof, and processes for preparing these compounds and their use as pharmaceutical compositions.
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(2008/06/13)

THIAZOLYL-DIHYDRO-CHINAZOLINE
Disclosed are compounds of general formula (I), wherein the groups A, R1, R2, Ra and Rb have the meanings given in the claims and specification, the tautomers, racemates, enantiomers, diastereomers and the mixtures thereof, and optionally the pharmacologically acceptable acid addition salts, solvates and hydrates thereof, and processes for preparing these thiazolyl-dihydro-quinazolines and the use thereof as pharmaceutical compositions.
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Page/Page column 27

(2008/06/13)

PI3 KINASES
The invention relates to the novel compounds of formula (1), which, due to their pharmaceutical effect as PI3 kinase modulators, are suitable for use in the therapy and treatment of inflammatory or allergic diseases. Examples of these diseases are inflammatory and allergic respiratory diseases, inflammatory diseases of the gastro-intestinal system and of the locomotor apparatus, inflammatory and allergic skin diseases, inflammatory ophthalmic diseases, diseases of the nasal mucosa, inflammatory or allergic autoimmune reactive conditions, or renal inflammations.
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Page/Page column 129

(2008/06/13)

THIAZOLO-, OXAZALO AND IMIDAZOLO-QUINAZOLINE COMPOUNDS CAPABLE OF INHIBITING PROTEIN KINASES
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Page/Page column 36

(2008/06/13)

Benzothiazole derivatives
The present invention is directed to a compound of formula (I), racemic-diastereomeric mixtures thereof, optical isomers thereof, prodrugs thereof, isotopes thereof or pharmaceutically-acceptable salts of said compound, isomers, prodrugs and isotopes, wherein the variables are defined herein. The compounds of this invention are useful as inhibitors of serine/threonine and tyrosine kinases. In particular, compounds of this invention are useful as inhibitors of tyrosine kinases that are important in hyperproliferative diseases, especially in cancer and in the process of angiogenesis.
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(2008/06/13)

Heterocycle-fused thiazole derivatives
PCT No. PCT/KR96/00082 Sec. 371 Date Jul. 3, 1997 Sec. 102(e) Date Jul. 3, 1997 PCT Filed Jun. 1, 1996 PCT Pub. No. WO97/03076 PCT Pub. Date Jan. 30, 1997A thiazole compound represented by general formula (I), wherein R is hydrogen atom, a hydroxy group, a straight or branched C1-C6 lower alkyl group, a C1-C4 lower alkoxy group, phenyl group, a phenyl group having one to three substituents selected from a group consisting of a C1-C4 lower alkyl group, a C1-C4 lower alkoxy group, fluorine, chlorine, bromine and an amino group, a C1-C5 alkylphenyl group, a phenyl group having one to three substituents selected from a group consisting of a C1-C4 lower alkyl group, a C1-C4 lower alkoxy group, fluorine, chlorine, bromine and an amino group, a substituted or unsubstituted guanidino group, or an amino group having a general formula: NR3R4 in which R3 and R4, identical to or different from each other, represent independently a hydrogen atom, a C1-C6 lower alkyl group, a C3-C6 cycloalkyl group, a substituted or unsubstituted pyridyl group, a phenyl group having one to three substituents selected from a group consisting of a C1-C4 lower alkyl group, a C1-C4 lower alkoxy group, a halogen atom, an amino group, a cyano group and a nitro group, a piperidine group or C1-C4 alkylpiperidine group; R1 and R2, identical to or different from each other, are independently a hydrogen atom, a hydroxy group, a C1-C6 lower alkyl group, phenyl group, a phenyl group having one substituent selected from a group consisting of a C1-C4 lower alkyl group, a C1-C4 lower alkoxy group, a halogen atom, a nitro and a cyano group, a C1-C5 alkylphenyl group, or a pyridine group; R5, R6, R7 and R8, identical to or different from each other, are independently a hydrogen atom, a hydroxy group, a C1-C4 lower alkyl group, a C1-C4 lower alkoxy group, phenyl group, or a phenyl group substituted with a C1-C4 alkyl group, a C1-C4 alkoxy group or a halogen atom, or a C1-C3 alkylphenyl group; Het is a 3-, 4- or 5-membered unsaturated monocyclic group, or 6- to 12-membered unsaturated fused cyclic group, said monocyclic and fused cyclic group being comprised of one or more hetero atoms selected from oxygen, oxidative nitrogen and oxidative sulfur atom are disclosed. These compounds show excellent anti-ulcer activity.
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(2008/06/13)

A New Heteroannulation Method to 2-Cyclohexenone, Mediated by Phosphonate Auxiliaries. Synthesis of 4,5,6,7-Tetrahydrobenzothiazole Derivatives
Dimethyl (1,2-epoxy-3-oxocyclohex-1-yl)phosphonate 7, easily available from 2-cyclohexen-1-one, affords the new (tetrahydrobenzothiazolyl)phosphonates 10 upon reaction with thiocarboxamides 8.This cyclocondensation proceeds with regioselective conjunction
Oehler, E.
p. 763 - 774
(2007/10/02)

SYNTHESIS AND ANTIBACTERIAL ACTIVITY OF DERIVATIVES OF BENZOTHIAZOLONE, THIAZOLOAZEPINONE, AND FURAZANOAZEPINONE
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Ivanov, E. I.,Konup, I. P.,Konup, L. A.,Stepanov, D. E.,Grishchuk, L. V.,Vysotskaya, V. V.
p. 500 - 503
(2007/10/02)