439 results about "Thiazole derivative" patented technology

A thiazole derivative of the formula (I): wherein R is a 1-optionally substituted-6-oxo-1,6-dihydro-3-pyridazinyl, R′ is an optionally substituted phenyl, and R² is hydrogen, a group of the formula (i): wherein R⁴ is hydrogen, lower alkyl or lower alkenyl, and R⁵ is hydrogen, optionally substituted lower alkyl, acyl, cyclo(lower)alkyl, lower alkenyl, optionally substituted aryl or heterocyclic, or a group of the formula (ii): wherein X is oxygen or sulfur, R⁸ is hydrogen or lower alkyl, R⁹ is hydrogen, optionally substituted lower alkyl, cyclo(lower)alkyl, lower alkoxy or mono- or di-lower alkylamino or R⁸ and R⁹ may combine together to form optionally substituted saturated N-containing heterocyclic, or a salt thereof.

The present invention relates to a compound represented by the following formula, a pharmacologically acceptable salt thereof, or a use thereof as a pharmaceutical:

wherein R¹ and R² are substituents adjacent to each other, and together with two carbon atoms to each of which they attach, form a 5- to 7-membered non-aromatic carbocyclic group or the like, which may be substituted by 1 to 4 substituents selected from (1) an oxo group, (2) a hydroxyl group, and the like; R³ represents a hydrogen atom or the like; and R⁶ represents a hydrogen atom or the like.

It is an object of the present invention to discover an agent for treating or preventing lower urinary tract symptoms, and particularly symptoms regarding urinary storage, which has a superior strength of binding to a 5-HT1A receptor and an antagonism to the receptor.

PCT No. PCT/JP97/02609 Sec. 371 Date Mar. 24, 1998 Sec. 102(e) Date Mar. 24, 1998 PCT Filed Jul. 29, 1997 PCT Pub. No. WO98/04536 PCT Pub. Date Feb. 5, 1998A thiazole compound of the formula: wherein T is lower alkylene; u is 0 or 1; R1 and R2 are the same or different and are each H, or lower alkyl, etc.; R3 is R4 is H or lower alkanoyloxy-lower alkyl, which shows inhibitory activity on protein kinase C (PKC, Ca2+/phospholipid-depending serine/threonine protein phosphatase), and are useful as a protein kinase C inhibitor.

A thiazolylimidazole derivative represented by the formula

or a pharmaceutically acceptable salt thereof, and an ALK5 inhibitor, an therapeutic agent for alopecia or a hair growth agent having the above as an active ingredient, wherein:

X¹ and X² are different from each other and represent a sulfur atom or a carbon atom; R¹ represents a phenyl group; a substituted phenyl group; a phenyl group condensed with a hetero aromatic ring; a pyridyl group; or a pyridyl group condensed with a hetero aromatic ring; R² represents a hydrogen atom, a halogen atom, an alkyl group having 1 to 6 carbon atoms, an alkyl group having 1 to 6 carbon atoms substituted with 1 to 5 halogen atoms, an alkoxy group having 1 to 6 carbon atoms, an alkanoyl group having 1 to 5 carbon atoms, or a hydroxyalkyl group having 1 to 6 carbon atoms, A represents a group which is represented by the formula.

The present invention provides an inhibitory substance against ALK5 which is a TGF-β type I receptor and provides a hair growth stimulant or a hair growth agent based on its novel activities.

The invention disclosed an aryl nitrile group thiazole derivative for inhibiting the activity of xanthine oxidase, a method for preparing the same and application thereof. In the aryl nitrile group thiazole, R1 is methyl, ethyl, propyl, isopropyl, isobutyl, methyl cyclopropane, methyl cyclobutane, isoamyl, methyl cyclopentane, methyl cyclohexane or aromatic ring methyl, R2 is methyl or trifluoromethyl, and R3 is formic acid, sodium formate, potassium formate, lithium formate, methyl formate, or ethyl formate. Simultaneously, the invention discloses a method for synthesizing the aryl nitrile group thiazole derivative by using inexpensive raw materials, which has the advantages of simple operation, high yield, easy purification of products, application to industrial production and the like, and can obtain an efficient compound with low toxicity through screening; besides, the effective compound is expected to be widely applied to inhibit the activity of the xanthine oxidase required on animals and humans, and to become a new generation of antigout drugs and hyperuricemia drugs with special effect.

The invention discloses 5-(4-chlorophenylmethyl)-4-tertiary butyl thiazole derivatives (I), which has the following structural formula as shown in the specification of the invention, wherein X1 in a formula I is selected from hydrogen, hydroxyl group, methoxy group, nitro group, amino group and chlorine; X2 is selected from hydrogen, nitro group, amino group, methoxy group, chlorine, bromine and iodine; X3 is selected from hydrogen, methyl group, ethyl group, nitro group, methoxy group, chlorine, bromine, amino group and dimethylamino group; and X4 is selected from hydrogen, nitro group, amino group, methoxy group, chlorine, bromine and iodine. The 5-(4-chlorophenylmethyl)-4-tertiary butyl thiazole derivatives (I) have favorable inhibition activity on human cervical cancer cells, human liver cancer cells, human nasal and oral cancer cells and the like and can be used for preparing anti-tumor medicines.

The present invention relates to a novel compound with thiazole ring having an inhibitory activity against sodium-dependent glucose cotransporter 2 (SGLT2) being present in the intestine and kidney, and a pharmaceutical composition comprising the same as an active ingredient, which is useful for preventing or treating metabolic disorders, particularly diabetes.

The present invention relates to compounds of formula (I)

wherein R¹, R², R³ and R⁴ are as defined in the description and claims, and pharmaceutically acceptable salts thereof, for use as therapeutically active substances. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with the modulation of CB1 receptors, including obesity.

Compounds of formula (I) are inhibitors of P13 kinase activity, and useful in treatment of, inter alia, autoimmune, inflammatory and proliferative diseases: wherein: s is 0 or 1; U is hydrogen or halogen; X is —(C═O), an optionally substituted divalent phenylene, pyridinylene, pyrimidinylene, or pyrazinylene radical, or a bond; P is optionally substituted C₁-C₆ alkyl and Z is —(CH₂)_Z—X₁-L₁-NHCHR₁R₂; or Z is optionally substituted C₁-C₆ alkyl and P is —(CH₂)_Z—X₁-L₁-NHCHR₁R₂; R₁ is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular carboxylesterase enzymes to a carboxylic acid group; R₂ is the side chain of a natural or non-natural alpha amino acid; X₁ is (i) a bond; —NR₄C(═O)NR₅— or —NR₄S(═O)₂—; or except when X is —(C═O)— (ii) —C(═O)—, —S(═O)₂—, or —S(═O)₂NR₄— wherein R₄ and R₅ are independently hydrogen or optionally substituted C₁-C₆ alkyl; and z and L1 are as defined in the specification.

Therapeutically active thiazole derivatives of formula (I) wherein R¹-R², X and X′ as are defined in the specification, processes for the preparation thereof, the use thereof in therapy, particularly in the treatment or prophylaxis of disorders characterised by overexpression of transforming growth factor • (TGF-•), and pharmaceutical compositions for use in such

therapy.

The invention discloses benzoselenadiazole derivatives with antitumor and antioxidation activities, and a preparation method and application thereof. The chemical structure of the benzoselenadiazole derivatives is disclosed as Formula I, wherein R1 is -H or -NO2, R2 is -H, -NO2 or a group shown in specification, and R1 and R2 can not be H at the same time. The benzoselenadiazole derivatives are synthesized by reacting ortho-diamine compounds with selenium dioxide in a liquid phase or solid phase. The benzoselenadiazole derivatives have favorable antitumor and antioxidation activities, and have the advantages of simple preparation method and high yield. The benzoselenadiazole derivatives disclosed by the invention can be used for preparing antitumor drugs and/or antioxidation drugs. Formula I is shown in the specification.

The invention belongs to the field of biochemistry and particularly relates to a substituted coumarin-thiazole orange derivative, a preparation method therefor and use of the substituted coumarin-thiazole orange derivative. The substituted coumarin-thiazole orange derivative provided by the invention has a structural formula represented by a formula I shown in the description. The invention also provides the preparation method for the substituted coumarin-thiazole orange derivative and use of the substituted coumarin-thiazole orange derivative in fluorescent recognition of G-quadruplex. The substituted coumarin-thiazole orange derivative provided by the invention has the advantages that the toxicity is low, the selectivity is good, the sensitivity is high, raw materials are simply and easily obtained, the whole synthesis route is high in operability, reaction conditions are relatively mild, the overall cost is relatively low, and the like, thereby undoubtedly having better market competitiveness compared with the existing inefficient G-quadruplex fluorescent probes.

The present invention provides 2-substituted-ethynylthiazole derivatives of formula (I):

wherein R¹, R² and X are as defined herein, or a pharmaceutically acceptable salt thereof; and pharmaceutical compositions and methods of using same.

The invention relates to a glaucocalyxin A (GLA) thiazole derivative. The structure II of the derivative is shown in the description, wherein R is hydrogen, alkyl, alkylene and aromatic hydrocarbon. Based on cytotoxic activity evaluation experiment, the GLA thiazole derivative disclosed by the invention has very strong human tumor cell proliferation inhibitory activity which is better than that of parent compound GLA.

The invention belongs to the fields of drugs and chemical industry, and discloses a quinazoline derivative and a preparation method thereof and an application of the quinazoline derivative used as an anticancer drug. The structural formula of the quinazoline derivative is shown in the specifications, wherein R1 is NH(CH2)mNR5 or NH(CH2)m-Ar; R2 is NHCO(CH2)n NR5, NHCO(CH2)n-Ar, NHCO(CH2)nNH(CH2)nNR5 or NHCO(CH2)nNH(CH2)n-Ar; R3 is F, Cl, Br, I, H, CH3, SO2CH3 or OCH3; R4 is H, NHCO(CH2)nNR5, NHCO(CH2)n-Ar, NHCO(CH2)nNH(CH2)nNR5 or NHCO(CH2)nNH(CH2)n-Ar; -Ar represents various aromatic rings comprising various aromatic heterocyclic rings; m is equal to 2, 3 or 4; n is equal to 1, 2, 3, 4 or 5; and R5 represents alkyl of C1-6, cycloalkyl of C3-6, piperidyl, morpholinyl, piperazinyl or quinoxalinyl. The invention simultaneously discloses the preparation method of the quinazoline derivative and the application of the quinazoline derivative used as the anticancer drug. The experiment proves that the quinazoline derivative of the invention has strong inhibiting effect on telomere DNA expression, has obvious inhibiting effect on various kinds of cancer cell strains, has low toxicity to normal cells, and has wide application prospects in preparation of anticancer drugs.

The invention discloses a method for preparing an imidazo[2,1-b]thiazole derivative by catalysis of a copper salt. In an environment of an organic solvent, the copper salt is taken as a catalyst, 1,1-dibromo-1-olefin or alkynyl bromide and a 2-mercaptoimidazole compound are taken as substrates to synthesize the imidazo[1,5-b]thiazole derivative under the action of alkali by one step, wherein the molar ratio of the 2-mercaptoimidazole compound to the 1,1-dibromo-1-olefin or alkynyl bromide is 1:1-1:5; the molar ratio of the 2-mercaptoimidazole compound to the alkali is 1:3-1:8; based on the 2-mercaptoimidazole compound, the using amount of the copper salt is 0.1 percent to 3.0 mol percent; the molar ratio of a ligand to the copper salt is 1:2-2:1; and the reaction temperature is 20 to 110 DEG C. The preparation method is simple and mild in reaction conditions, and has wide application prospect in fine chemical industry and pharmacy industry.