Abstract: The present invention relates to cryptophycin compounds of formula (I): The invention also relates to cryptophycin payloads, to cryptophycin conjugates, to compositions containing them and to their therapeutic use, especially as anticancer agents. The invention also relates to the process for preparing these conjugates.

Abstract: The present invention relates to cryptophycin compounds of formula (I). The invention also relates to cryptophycin payloads, to cryptophycin conjugates, to compositions containing them and to their therapeutic use, especially as anticancer agents. The invention also relates to the process for preparing these conjugates.

Abstract: The present invention relates to cryptophycin compounds of formula (I). The invention also relates to cryptophycin payloads, to cryptophycin conjugates, to compositions containing them and to their therapeutic use, especially as anticancer agents. The invention also relates to the process for preparing these conjugates.

Abstract: The present invention relates to a process for the preparation of a compound of the formula I, which comprises reacting a compound of the formula IV with an oxalic acid diester and to novel intermediate compounds used therein.

Abstract: The invention relates to a method for preparing an activated ester of the formula (I), where R is a (C1-C6) alkyl, aryl, heteroaryl, cycloalkyl, or heterocycloalkyl group, and ALK is a (C1-C6) alkylene group, said method consisting of reacting the dicyclohexylamine P1 salt and the disuccinimidyl carbonate (DSC) in a solvent in which the dicyclohexylamine salt of the N-hydroxysuccinimide P2 is precipitated. The invention also relates to products of the formula P1.

Abstract: The present invention relates to a process for the preparation of a compound of the formula I, which comprises reacting a compound of the formula IV with an oxalic acid diester and to novel intermediate compounds used therein.

Abstract: This disclosure relates to methods for preparing an enantiomerically enriched N-carboxyanhydride of an amino alpha acid of the formula (IIIa) or (IIIb): from a compound of the formula (IIa) or (IIb), respectively: wherein R1, R2, and R3 are as defined in the disclosure.

Abstract: This invention discloses and claims an industrial method for the production of azetidine derivatives, such as, N-(1-benzhydrylazetidin-3-yl)-N-phenylmethylsulphonamide.

Abstract: This disclosure relates to methods for preparing an enantiomerically enriched N-carboxyanhydride of an amino alpha acid of the formula (IIIa) or (IIIb): from a compound of the formula (IIa) or (IIb), respectively: wherein R1, R2, and R3 are as defined in the disclosure.

Abstract: The invention relates to a method for preparing an activated ester of the formula (I), where R is a (C1-C6) alkyl, aryl, heteroaryl, cycloalkyl, or heterocycloalkyl group, and ALK is a (C1-C6) alkylene group, said method consisting of reacting the dicyclohexylamine P1 salt and the disuccinimidyl carbonate (DSC) in a solvent in which the dicyclohexylamine salt of the N-hydroxysuccinimide P2 is precipitated. The invention also relates to products of the formula P1.

Abstract: The invention relates to compounds of formula (I) wherein the groups have stated meanings, and to their physiologically compatible salts. Said compounds are suitable, for example, as anti-obesity drugs and for treating cardiometabolic syndrome.

Abstract: This invention discloses and claims an industrial method for the production of azetidine derivatives, such as, N-(1-benzhydrylazetidin-3-yl)-N-phenylmethylsulphonamide.

Abstract: Compounds of formula (I), wherein R1 and R3 have the meanings given in the description, said compounds being in all isomeric forms; and salts thereof; processes for the preparation of the compounds and intermediates; compositions containing them, and the use thereof as medicaments, particularly as anti-cancer agents.

Abstract: This disclosure relates to methods for preparing an enantiomerically enriched N-carboxyanhydride of an amino alpha acid of the formula (IIIa) or (IIIb): from a compound of the formula (IIa) or (IIb), respectively: wherein R1, R2, and R3 are as defined in the disclosure.

Abstract: The present invention relates to the novel isoindolone derivatives of the formula I in which R1 to R6 have the meanings stated in the claims. The inventive compounds are suitable as antiarrhythmic medicaments with a cardioprotective component for infarction prophylaxis and infarction treatment and for the treatment of angina pectoris. They also inhibit in a preventive manner the pathophysiological processes associated with the development of ischemia-induced damage, in particular in the triggering of ischemia-induced cardiac arrhythmias and of heart failure.

Abstract: The invention relates to epothilone analog represented by the formula I wherein (i) R2 is absent or oxygen; “a” can be either a single or double bond; “b” can be either absent or a single bond; and “c” can be either absent or a single bond, with the proviso that if R2 is oxygen then “b” and “c” are both a single bond and “a” is a single bond; if R2 is absent then “b” and “c” are absent and “a” is a double bond; and if “a” is a double bond, then R2, “b” and “c” are absent; R3 is a radical selected from the group consisting of hydrogen; lower alkyl; —CH?CH2; —C?CH; —CH2F; —CH2Cl; —CH2—OH; —CH2—O—(C1-C6-alkyl); and —CH2—S—(C1-C6-alkyl); R4 and R5 are independently selected from hydrogen, methyl or a protecting group; and R1 is as defined in the specification, or a salt of a compound of the formula I where a salt-forming group is present. A further aspect of the invention is related to the synthesis of epothilone E.

Abstract: The invention relates to 4-substituted quinoline derivatives of general formula: which are active as antimicrobials, in which: X1, X2, X3, X4 and X5 represent >C—R?1 to >C—R?5 respectively, or alternatively at most one represents nitrogen, Y represents CHR, CO, CROH, CRNH2, CRF or CF2, R being a hydrogen or alkyl, m is 0, 1 or 2 and n is 0 or 1, R2 represents a radical R, —CO2R, —CH2CO2R, —CH2—CH2CO2R, —CONH2, —CH2—CONH2, —CH2—CH2—CONH2, —CH2OH, —CH2—CH2OH, —CH2—NH2—CH2—CH2—NH2 or —CH2—CH2—CH2—NH2, R being as defined above, R3 represents phenyl, heteroaryl or alk-Ro3, where alk is alkyl and Ro3 represents various groups, where appropriate containing oxygen, sulfur or amine, in their enantiomeric or diastereoisomeric forms or their mixtures, and/or where appropriate in the syn or anti form or their mixtures, and their salts.

Abstract: Compounds of formula (I), wherein R1 and R3 have the meanings given in the description, said compounds being in all isomeric forms; and salts thereof; processes for the preparation of the compounds and intermediates; compositions containing them, and the use thereof as medicaments, particularly as anti-cancer agents.

Abstract: The present invention relates to compounds according to the general formula (I) wherein X is selected from the group consisting of wherein n and p are independently 0, 1, 2, or 3, provided that n+p is a least 1; and unsubstituted and at least monosubstituted C1-C10-alkylene-Y, C2-C10-alkylene-Y, C3-C10-cycloalkylene-Y and C3-C10-cycloalkenylene-Y; and R1, A, B, Q, T, Y, E and W have the meanings given in the description. These compounds are useful for the manufacture of a medicament for the treatment of insulin resistance, type 2 diabetes, metabolic syndrome, lipid disorders or cardiovasular disease or for providing an anti-lipolytic effect.

Abstract: The present invention relates to a process for preparing 2-amino-thiazoline derivatives of formula (II): in which either Y is a methylene (CH2) and X is chosen from the following groups: O, NH, (C1-C4) N-Alkyl, N-Bn, N-Ph, N-(2-Py), N-(3-Py), N-(4-Py), N-2-pyrimidyl, N-5-pyrimidyl, S, SO, SO2, CH2 or CHPh; or Y is a carbonyl (C?O) and X is chosen from the following groups: NH, N-Ph, N-(2-Py), N-(3-Py), N-(4-Py), N-2-pyrimidyl or N-5-pyrimidyl.