Abstract: The invention relates to the R-enantiomer of N-carbamoylmethyl-4-phenyl-2-pyrrolidinone (R-Carphedon) of pharmacological value. The method of its preparation includes the N-alkylation of 4(R)-phenyl-2-pyrrolidinone with ethyl bromoacetate in the presence of a strong base and the treatment of intermediate N-ethoxycarbonylmethyl-4(R)-phenyl-2-pyrrolidinone with ammonia.

Abstract: The invention relates to the R-enantiomer of N-carbamoylmethyl-4-phenyl-2-pyrrolidinone (R-Carphedon) of pharmacological value. The method of its preparation includes the N-alkylation of 4(R)-phenyl-2-pyrrolidinone with ethyl bromoacetate in the presence of a strong base and the treatment of intermediate N-ethoxycarbonylmethyl-4(R)-phenyl-2-pyrrolidinone with ammonia.

Abstract: The invention relates to the R-enantiomer of N-carbamoylmethyl-4-phenyl-2-pyrrolidinone (R-Carphedon) of pharmacological value. The method of its preparation includes the N-alkylation of 4(R)-phenyl-2-pyrrolidinone with ethyl bromoacetate in the presence of a strong base and the treatment of intermediate N-ethoxycarbonylmethyl-4(R)-phenyl-2-pyrrolidinone with ammonia.

Abstract: The present invention provides a method for regeneration of chiral 2,2?-cyclopropylidene-bis(oxazolines), such as (3&R,3?aR,8aS,8?aS)-2,2?-cyclopropylidenebis-[3a,8a]-dihydro-8H-indeno-[1,2-d]-oxazole and (45,4?5,5R,5?R)-2,2?-cyclopropylidenebis-4,5-diphenyldihydro-4,5-oxazole, used as a part of complex catalysts for e.g. stereoselective addition reactions, from the reaction mixtures, by selective sorption of 2,2?-cyclopropylidene-bis(oxazolines) on a sorbent, such as silica gel, isolation of the sorbent from reaction mixture, desorption of 2,2?-cyclopropylidene-bis(oxazolines) from the sorbent with suitable organic solvent and final recovery of 2,2?-cyclopropylidene-bis(oxazolines) from the organic solvent used for desorption process. Catalytic quality of recovered compounds does not differ from those in freshly prepared catalysts.

Abstract: New compounds of 2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylic acid ester type having general formula I wherein R is a lower alkyl group, which is methyl or ethyl R1 and R2 is sodium carboxylate-methyl ester, having synergistic cytotoxic effect combined with 5-fluorouracil.

Abstract: A method for preparation of 6-[3-(1-adamantyl)-4-methoxyphenyl]-2-naphthoic acid is disclosed based on “one pot” synthesis approach including a direct synthesis of boronic acid derivative from 2-(1-adamantyl)-4-bromoanisole and cycloboranes with a subsequent Suzuki-Miyaura coupling with 6-halonaphtenoates and basic hydrolysis of the reaction product in ethylene glycol or 1,2-propanediol.

Abstract: New compounds of 2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylic acid ester type having general formula I wherein R is a lower alkyl group, which is methyl or ethyl R1 and R2 is sodium carboxylate-methyl ester, having synergistic cytotoxic effect combined with 5-fluorouracil.

Abstract: This invention pertains to certain carbamic acid compounds of the following formula, which inhibit HDAC (histone deacetylase) activity wherein: A is independently an unsubstituted or substituted bicyclic C9-10heteroaryl group (e.g., quinolinyl; quinoxalinyl; benzoxazolyl; benzothiazolyl); Q is an acid leader group, and is independently an unsubstituted or substituted, saturated or unsaturated C1-7alkylene group having a backbone length of 4 or less; with the proviso that if A is unsubstituted benzothiazol-2-yl, then Q is an unsaturated group; and with the proviso that if A is unsubstituted quinolin-6-yl, then Q is unsubstituted at the ?-position; and with the proviso that A is not benzimidazol-2-yl; and pharmaceutically acceptable salts, solvates, amides, esters, ethers, chemically protected forms, and prodrugs thereof.

Abstract: This invention pertains to certain carbamic acid compounds which inhibit HDAC (histone deacetylase) activity of the following formula: The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit HDAC, and in the treatment of conditions mediated by HDAC, cancer, proliferative conditions, psoriasis, etc.

Abstract: The present invention provides a method for regeneration of chiral 2,2?-cyclopropylidene-bis(oxazolines), such as (3&R, 3?aR,8aS,8?aS)-2,2?-cyclopropylidenebis-[3a,8a]-dihydro-8H-indeno-[1,2-d]-oxazole and (45,4?5,5R,5?R)-2,2?-cyclopropy-lidenebis-4,5-diphenyldihydro-4,5-oxazole, used as a part of complex catalysts for e.g. stereoselective addition reactions, from the reaction mixtures, by selective sorption of 2,2?-cyclopropylidene-bis(oxazolines) on a sorbent, such as silica gel, isolation of the sorbent from reaction mixture, desorption of 2,2?-cyclopropylidene-bis(oxazolines) from the sorbent with suitable organic solvent and final recovery of 2,2?-cyclopropylidene-bis(oxazolines) from the organic solvent used for desorption process. Catalytic quality of recovered compounds does not differ from those in freshly prepared catalysts.

Abstract: Substituted pyrazolopyrimidine derivatives of formula (I) wherein Y1, Y2, Y3, Y4 represent N or C—, whereby at least two of the groups Y1 to Y4 represent a carbon atom, R1 represents chloro or bromo, R2 to R7 represent e.g. hydrogen, methyl or ethyl; and R10 and R11 independently represent e.g. hydrogen or C1-C6alkyl, are potent mGluR5 modulators and are useful for the prevention of acute and chronic neurological disorders.

Abstract: Substituted pyrazolopyrimidine derivatives of formula (I) wherein Y1, Y2, Y3, Y4 represent N or C—, whereby at least two of the groups Y1 to Y4 represent a carbon atom, R1 represents chloro or bromo, R2 to R7 represent e.g. hydrogen, methyl or ethyl; and R10 and R11 independently represent e.g. hydrogen or C1-C6alkyl, are potent mGluR5 modulators and are useful for the prevention of acute and chronic neurological disorders.

Abstract: This invention pertains to certain carbamic acid compounds which inhibit HDAC (histone deacetylase) activity of the following formula: The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit HDAC, and in the treatment of conditions mediated by HDAC, cancer, proliferative conditions, psoriasis, etc.

Abstract: The invention relates to pyrazolopyrimidine derivatives of formula (I) wherein Y1, Y2 and Y3 independently are e.g. CR10, NH, S or O, whereby at least one of Y1, Y2 and Y3 represents CR10; R1 represents chloro or bromo; R2, R3, R4, R5, R6 and R7 represent e.g. hydrogen or C1-C6-alkyl, and R10 represents e.g. hydrogen, halogen or phenyl; which are potent mGluR5 modulators and are e.g. useful for the treatment of various neurological disorders.

Abstract: This invention pertains to certain active carbamic acid compounds which inhibit HDAC activity and which have the following formula: wherein: A is a C5-20heteroaryl or C5-20carboaryl group and is optionally substituted; Q1 is a C2-7alkylene group having a backbone of at least 2 carbon atoms, and is optionally substituted; J is —N(R1)C(?O)— or —C(?O)N(R1)—; R1 is hydrogen, C1-7alkyl, C3-20heterocyclyl, or C5-20aryl; and, Q2 is C1-7alkylene, C5-20arylene, C5-20arylene-C1-7alkylene, or C1-7alkylene-C5-20arylene having a backbone of at least 3 carbon atoms, and is optionally substituted; and pharmaceutically acceptable salts thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit HDAC, and, e.g., to treat proliferative conditions, such as cancer and psoriasis.

Abstract: The present invention relates to highly effective treatment of ischemic heart disease with 3-(2,2,2-trimethylhydrazinium) propionate hydrogen fumarate, and 3-(2,2,2-trimethylhydrazinium) propionate dihydrogen phosphate.

Abstract: This invention pertains to certain active carbamic acid compounds which inhibit HDAC activity and which have the formula (1) wherein: A is an aryl group; Q1 is an aryl leader group having a backbone of at least 2 carbon atoms; J is an amide linkage selected from: —NR1C(?O)— and —C(?O)NR1—; R1 is an amido substituent; and, Q2 is an acid leader group; and pharmaceutically acceptable salts, solvates, amides, esters, ethers, chemically protected forms, and prodrugs thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit HDAC, and, e.g., to inhibit proliferative conditions, such as cancer and psorias.

Abstract: This invention pertains generally to the field of therapeutic compounds, and more particularly, to certain bicyclosulfonyl acid (BCSA) compounds which act as inhibitors of Tumour Necrosis Factor-? Converting Enzyme (TACE). The compounds are useful in the treatment of conditions mediated by TNF-?, such as rheumatoid arthritis; inflammation; psoriasis; septic shock; graft rejection; cachexia; anorexia; congestive heart failure; post ischaemic reperfusion injury; inflammatory disease of the central nervous system; inflammatory bowel disease; insulin resistance; HIV infection; cancer; chronic obstructive pulmonary disease (COPD); and asthma. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, in the inhibition of TACE, and in the treatment of conditions that are ameliorated by the inhibition of TACE.

Abstract: Certain 1-aminoalkylcyclohexanes are systematically-active 5HT3 and nicotinic receptor antagonists and are useful in the inhibition of progression of or alleviation of conditions resulting from disturbances of serotoninergic or nicotinergic transmission giving them a wide range of utility in the treatment of CNS-disorders. Pharmaceutical compositions thereof for such purpose and method of making same, as well as a method-of-treating conditions which are alleviated by the employment of a 5HT3 or neuronal nicotinic receptor antagonist.

Abstract: This invention pertains to certain active carbamic acid compounds which inhibit HDAC activity and which have the formula (1) wherein: A is an aryl group; Q1 is an aryl leader group having a backbone of at least 2 carbon atoms; J is an amide linkage selected from: —NR1C(?O)— and —C(?O)NR1—; R1 is an amido substituent; and, Q2 is an acid leader group; and pharmaceutically acceptable salts, solvates, amides, esters, ethers, chemically protected forms, and prodrugs thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit HDAC, and, e.g.