摘要:
The invention relates to novel small molecule compounds having a basic structure as depicted by formula (A), where in particular exemplary embodiments R1 is -OH, R2 is -NO2 and R3 is H, R4 and R5 are H, one of R6 and R7 is selected from H, -CONH2, and -CONR9 2, and the other one is selected from -CONR9 2 and -CONR11R9, wherein R9 and R11 are (possibly multiply) substituted alkyl and H or alkyl, respectively. The compounds of the invention inhibit the enzyme Catechol-O-methyltransferase (COMT) and exhibit a low off- target profile. The compounds are provided for use as a medicament, in particular for use in prevention or treatment of Parkinson's disease.
摘要:
Novel thermolatent bases and their use as catalysts for the preparation of polyurethanes or epoxy resins are disclosed herein. A process for the preparation of polyurethanes or epoxy resins in the presence of the catalyst is also disclosed.
摘要:
The invention relates to the compounds of formula I and formula II or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I or formula II; and methods for treating or preventing inflammatory bowel disease may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of gastrointestinal diseases and inflammation such as inflammatory bowel disease, ulcerative colitis, mild-to-moderate Crohn's disease, rheumatoid arthritis, inflammatory arthritis, psoriatic arthritis, liver cirrhosis and idiopathic urticaria.
摘要:
In one aspect, the invention relates to a compound of the structure: or a pharmaceutically acceptable salt thereof, and a crystalline form of this compound, having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising this compound; methods of using this compound; and processes for preparing this compound.
摘要:
The invention relates to a composition, in the form of an aqueous solution, comprising insulin in hexameric form, at least one substituted anionic compound having a non-saccharide structure and at least one polyanionic compound different from the substituted anionic compound.
摘要:
The present invention provides a compound represented by general formula I or a pharmaceutical acceptable salt thereof, the preparation method therefor and the use thereof in preparing a medicine for treating a neurological disease, such as epilepsy, convulsion, neuropathic pain, acute ischemic stroke, and a neurodegenerative disease. The compound according to present invention has a better absorption in brain tissue when compared with RTG. In addition, the compound provided by present invention has not only a greatly enhanced efficacy, but also a neurotoxicity greatly lower than that of RTG, and thus possesses a wider safety window.
摘要:
The present invention provides a compound of formula I';
or a pharmaceutically acceptable salt thereof, wherein R 1 , R 2 , R 3 , X and n are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
摘要:
Described herein are a series of compounds having the structure of Formula I for use in the inhibition of MAO and uses thereof for the treatment of a barrier disease, obesity, solid epithelial cell tumor metastasis, diabetes, an auto-immune and inflammatory disease or a cardiometabolic disorder.
摘要:
Analgesic compounds for treatment of pain or fever that include a bicyclopentane moiety linked to an amine, combinations of the compounds with opioid analgesic drugs, and methods for treating pain or fever by administering a compound described herein.
摘要:
Control or repellency of bed bugs is accomplished by bringing the bed bugs into contact with at least one of the compounds of the structure (I) Wherein R is selected from -OH, -OC(O)R 4 , -OR 6 , -(OR 6 ) 2 , wherein each R 6 is independently selected from an alkyl group containing from 1 to 4 carbon atoms and R 4 is a branched or straight chain saturated or unsaturated hydrocarbyl group with zero to two double bonds and from 1 to 15 carbon atoms; X is O or CH 2 , with the proviso that when X is O R can only be =O; each Z is independently selected from (CH) and (CH 2 ) y is a numeral selected from 1 and 2; R 1 is selected from H or a branched or straight chain saturated or unsaturated hydrocarbyl group with zero to two double bonds and from 1 to 15 carbon atoms. R 2 is selected from H and a branched or straight chain saturated or unsaturated hydrocarbyl group with zero to three double bonds and from 1 to 15 carbon atoms. R 3 is selected from H, a branched or straight chain, saturated or unsaturated hydrocarbyl group with zero to three double bonds and from 1 to 15 carbon atoms, -(CH 2 ) n OH, -C(O)OR 5 , -CH 2 C(O)OR 7 ,-CH 2 C(O)R 8 , -C(O)NR 9 R 10 , -CH 2 C(O)NR 11 R 12 where each of R 5 , R 7 , R 8 , R 9 , R 10 , R 11 and R 12 is independently selected from H and a branched or straight chain, saturated or unsaturated hydrocarbyl group with zero to three double bonds and from 1 to 15 carbon atoms, and n is an integer of from 1 to 12; and the bond between the 2 and 3 positions in the ring structure may be a single or a double bond, and wherein the compounds of structure (1) contain from 11 to 20 total carbon atoms, except where R is =O, X = CH 2 and y is 1 the compounds of structure (I) contain from 13 to 20 total carbon atoms in the compounds. wherein the compounds of structure (1) contain from 11 to 20 total carbon atoms, except where R is =O, X = CH 2 and y is 1 the compounds of structure (I) contain from 13 to 20 total carbon atoms in the compounds. wherein the compounds of structure (1) contain from 11 to 20 total carbon atoms, except where R is =O, X = CH 2 and y is 1 the compounds of structure (I) contain from 13 to 20 total carbon atoms in the compounds.