56 results about "Thienopyridine Derivatives" patented technology

The invention provides a novel tetrahydro thienopyridine derivative. The dosage of one or more active compounds in the novel tetrahydro thienopyridine derivative is 0.1-20mg/kg body weight, and the preferable dosage is 0.1-5mg/kg body weight. The novel tetrahydro thienopyridine derivative can be used for producing medicines for preventing and/or treating diseases induced by thrombosis or thromboembolism.

The present invention relates to compounds of formula I

wherein R¹, R², R³, R⁴, and R⁵ are as defined in the specification. Compounds of the invention are active on the GABAB receptor and are useful for treating a variety of CNS disorders, including anxiety, depression, epilepsy, schizophrenia, cognitive disorders, spasticity-and skeletal muscle rigidity, spinal cord injury, multiple sclerosis, amyotrophic lateral sclerosis, cerebral palsy, neuropathic pain and craving associated with cocaine and nicotine, psychosis, panic disorder, posttraumatic stress disorders and gastrointestinal disorders.

Methods and pharmaceutical compositions for treating viral infections, by administering certain thienopyridine derivative compounds in therapeutically effective amounts are disclosed. Methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment of viral infections such as caused by flavivirus is disclosed, i.e., including but not limited to, Dengue virus, West Nile virus, yellow fever virus, Japanese encephalitis virus, and tick-borne encephalitis virus.

The invention provides an optically active 2-hydroxyltetrahydrothienopyridine derivative shown by formula I, or a pharmaceutically acceptable salt, solvate, polycrystal, enantiomer or racemization mixture thereof, wherein in the formula I, R1 is F, Cl, Br or I; m is 0 or 1; n is an integer from 1 to 6; R2 or R3 is independently hydrogen, C1-C6 alkyl or optionally substituted C1-6 alkyl; R4 or R5 is independently hydrogen, C1-C10 alkyl, C1-C10 alkenyl, C1-10 alkoxy, C1-10 aryl, halogen, acylamino, sulfmidyl, acyloxy or C(O)R', and R' is hydrogen, C1-C10 alkyl, C1-C10 alkenyl, C1-10 alkoxy, C1-10 aryl, halogen, acylamino, sulfmidyl or acyloxy. The compound has obvious platelet agglomeration resistance action, and the bioavailability of the compound is obviously higher than that of clopidogrel. The invention further provides a preparation method of the compound, a pharmaceutical composition containing the compound, and a pharmaceutical use of the compound and the pharmaceutical composition.

[Problem to be Solved]The present invention provides a compound promoting osteogenesis. [Solution]

The present invention provides a compound having the following general formula (I)

wherein R¹ is H or alkyl,

• R² is R^aS—, R^aO—, R^aNH—, R^a(R^b)N— or cyclic amino, and
• R^a and R^b are alkyl which may be substituted, cycloalkyl which may be substituted, or the like, or a pharmacologically acceptable salt thereof.

PCT No. PCT/JP97/01413 Sec. 371 Date Jun. 26, 1997 Sec. 102(e) Date Jun. 26, 1997 PCT Filed Apr. 23, 1997 PCT Pub. No. WO97/40050 PCT Pub. Date Oct. 30, 1997There is disclosed a compound of the formula (A): wherein W is C-G or C-G' (G is optionally esterified carboxyl; and G' is halogen); X is oxygen, optionally oxidized sulfur or -(CH2)q- (q is 0 to 5); R is optionally substituted amino or heterocyclic group; the ring B is optionally substituted nitrogen-containing 5- to 7-membered ring; L is hydrogen, optionally substituted hydrocarbon residue, optionally substituted acyl, optionally substituted carbamoyl, optionally substituted thiocarbamoyl or optionally substituted sulfonyl provided that, when W is C-G, L is hydrogen, optionally substituted acyl, optionally substituted carbamoyl, optionally substituted alkoxycarbonyl, optionally substituted thiocarbamoyl or optionally substituted sulfonyl; n is 0 or 1; the ring A may have a substituent. A process for producing the compound (A) and a pharmaceutical composition containing the compound (A) are also disclosed. The pharmaceutical composition is useful for an anti-inflammatory drug, particularly, a drug for preventing or treating arthritis, a drug for inhibiting bone resorption, immunosuppressant or the like.

The invention relates to the field of pharmacy and specifically relates to water-soluble 2-hydroxyl tetrahydrothienopyridine derivatives as well as a preparation method of the derivatives and application of the derivatives in pharmacy, and specifically relates to application of the water-soluble 2-hydroxyl tetrahydrothienopyridine derivatives in preparation of drugs for preventing or treating thrombus and embolism related diseases, and in particular to application of the water-soluble 2-hydroxyl tetrahydrothienopyridine derivatives in prevention and treatment of acute ST segment elevation type myocardial infarction as injections.

The invention belongs to the field of pharmaceutical chemistry technology, and particularly discloses thienopyridine derivatives, and preparation methods and a medical use thereof. Through structural modification of clopidogrel and prasugrel, a series of new thienopyridine derivative compounds are synthesized and mainly include derivatives esterified with ligustrazine formic acid and shikimic acid; the compounds go into a body, then are rapidly metabolized into effective metabolites and ligustrazine formic acid or shikimic acid, successfully keep away from metabolism of CYP2C19 enzyme, can be directly metabolized into active compounds to play a pharmacological function, thereby solving the clopidogrel resistance problem, effectively improving the compound antithrombotic activity, and also having no significant effect on hemorrhage risk; and the compounds have relatively ideal protective function on liver and kidney, and also have potential therapeutic significance for other cardiovascular diseases.

The invention relates to the field of medicines, in particular to a novel metabolin marker and application of the metabolin marker to develop or prepare a medicine containing the 2-hydroxyl radical tetrahydro-thiophene pyridine derivative with the optical activity. The medicines can be used for preventing or treating diseases caused by thrombus. The invention further provides a preparation method of the novel metabolin marker.

The invention relates to novel thienopyridine derivatives of formula (I), where R<1>, R<2>, R<3> and Y have the meanings given in claim 1, which are HSP90 inhibitors and can be used for the production of a medicament for the treatment of diseases in which the inhibition, regulation and/or modulation of HSP90 play a role.

The present invention relates to methods of treatment of hepatitis C using prasugrel. The methods of the present invention can be used in patients with hepatitis C administering prasugrel in combination with one or more anti-hepatitis C drugs.

The invention discloses a tetrahydrothienopyridine deuterated derivative as well as a preparation method and pharmaceutical application thereof. The derivative can be used for preparing medicines for preventing or treating thrombus-related diseases. The thienopyridine derivative can balance and optimize the safety and effectiveness of a medicine, the thienopyridine derivative is prevented from being hydrolyzed too fast in the gastrointestinal tract, and a better treatment effect is achieved on the premise that the bleeding risk of a patient is not increased.

The invention discloses polysubstituted thieno[2,3-b]pyridine derivatives, and a preparation method and an application thereof. The structural formula of the derivatives are represented by formula I shown in the description. A compound for inhibiting a urea transporter is screened by using an erythrocyte model. Experimental results show that the compounds (represented by formula I-1) can inhibit the permeation of a urea transporter UT-B mediated erythrocyte membrane to urea, and the effect of the compounds has a dose-dependent relationship; the compounds represented by the formula I-1 have nocytotoxic effect on MDCK cells within an effective dose range, so the effect of the compounds represented by the formula I-1 on inhibiting cell permeation urea is irrelevant to the cytotoxicity of thecompounds; the inhibition effect of the compounds represented by the formula I-1 on the urea transporter UT-B is gradually enhanced; the inhibiting effect of the compounds represented by the formulaI-1 on the UT-B is reversible; and in-vivo test results show that the compounds represented by the formula I-1 can significantly increase the urination volume of rats, reduce the concentration of ureain rat urine and reduce the osmotic pressure, so that the compounds represented by the formula I-1 generate a urea selective diuresis effect in vivo.

The invention discloses a bi-thienopyridine type derivative and a preparation method thereof. The bi-thienopyridine derivative disclosed by the invention adopts a rigid near plane structure, a skeleton structure is the combination of thiophthene and pyridine, a conjugation system is larger, and the double-thienopyridine derivative belongs to the technical field of synthesis. The general formula of a preparation reaction is shown as follows. The coordination compound uses 3, 4-diamino thieno [2, 3-b] thiophene -2, 5- denitrile as a raw material, under the induction of a catalyst, the raw material and ketone or aldehyde generate a Friedlander reaction, and a series of bi-thienopyridine derivatives are synthesized in a one-pot method. The operation process is simple, the atom economy is high, the reaction conditions are mild, and the yield is high. The material of the derivative can be used as a luminescent material, and can be used as the material of a luminous layer in a light emitting device. The synthetic method is one of the manners of magnetic stirring, hydrothermal reactions, microwaves, solid phase synthesis and the like. Through the adoption of the preparation method disclosed by the invention, different substrates can be used for synthesizing various bi-thienopyridine type derivatives which are not reported in literatures.

The present invention provides thienopyridine derivatives, which are useful as anti-inflammatory drugs, particularly as remedies for arthritis; processes for producing them, and pharmaceutical compositions containing them. The thienopyridine derivatives are represented by the formula (I): wherein G is a halogen atom, hydroxyl group, an optionally substituted amino group, etc.; alk is an optionally substituted lower alkylene group; X is O, S, -(CH2)q-, etc.; R is an optionally substituted amino group, etc.; ring B is an optionally substituted Y-containing 5- to 8-membered ring whose ring constituent atoms contain no nitrogen atom; Y is O, S, a group of (wherein Ra, Rb and Rc are the same or different and, each is H, a halogen atom, an optionally substituted hydrocarbon group, etc.), etc.; and ring A may be substituted.

The invention relates to synthesis of a pyrazolo[3,4-b]thieno[2,3-e]pyridine derivative, in particular to synthesis of pyrazolo[3,4-b]thieno[2,3-e]pyridine. The pyrazolo[3,4-b]thieno[2,3-e]pyridine derivative is generated by taking aromatic aldehyde, 1-phenyl-3-methyl-5-aminopyrazole and 3-oxosulfolane as raw materials in one step under a solvent-free and catalyst-free condition with a three-component one-pot process. According to the method, a synthesis process has a simple and convenient route, conditions are mild, and the total yield is over 78 percent.