Abstract: There are described 7H-pyrrolo[2,3-d]pyrimidine derivatives of the formula I in which the substituents are as defined in claim 1. These compounds inhibit the tyrosine kinase activity of the receptor for the epidermal growth factor (EGF) and c-erbB2 kinase and can be used as anti-tumor agents.

Abstract: Tetrahydroisoquinoline 3-carboxamide derivatives of formula and pharmaceutically acceptable salts thereof wherein: X is (a) CH2; (b) S (c) O; or (d) C(CH3)2; R1 and R2 are independently (a) hydrogen; (b) hydroxy; (c) alkyl; (d) alkoxy; (e) aralkoxy; or (f) halogen. Compounds of formula I inhibit DPP-IV (dipeptidyl-peptidase-IV) activity. They are therefore useful in the treatment of conditions mediated by DPP-IV, such as non-insulin-dependent diabetes mellitus, arthritis, obesity, osteoporosis and further conditions of impaired glucose tolerance.

Abstract: Compounds of formula I wherein R1, R2, R3, R4 and R5 are as defined in the description, are useful as pharmaceuticals.

Abstract: The present invention relates to a compound of formula (I) ##STR1## wherein R is substituted adamantyl; and n is 0 to 3; in free form or in acid addition salt form. Compounds of formula I inhibit DPP-IV (dipeptidyl-peptidase-IV) activity. They are therefore indicated for use as pharmaceuticals in inhibiting DPP-IV and in the treatment of conditions mediated by DPP-IV, such as non-insulin-dependent diabetes mellitus, arthritis, obesity, osteoporosis and further conditions of impaired glucose tolerance.

Abstract: A process for preparing the d-threo isomer of methylphenidate hydrochloride comprising converting d,l-threo methylphenidate hydrochloride to the free base form in a first step, resolving the free base prepared in the first step with (R)-(-)-1,1'-binaphthyl-2,2'-diyl hydrogen phosphate to obtain the phosphate salt enriched with the d-threo isomer of methylphenidate in a second step, basifying the phosphate salt to obtain the free base form of the d-threo isomer of methylphenidate in a third step, converting the free base to the hydrochloride salt form of the d-threo isomer of methylphenidate in high optical purity in a fourth step, and recrystallizing the hydrochloride salt form to obtain the desired d-threo isomer in a higher optical purity. An alternative embodiment relates to the preparation of the d-threo isomer of methylphenidate hydrochloride utilizing the hydrochloride salt form of the racemic mixture of threo-methylphenidate directly.

Abstract: The invention relates on the one hand to a novel preparation of compounds of the formula (I) ##STR1## in which R.sub.1 is an aromatic or heteroaromatic radical, aromatic-aliphatic or heteroaromatic-aliphatic radical, a heterocyclic radical, a cycloaliphatic radical, a cycloaliphatic-aliphatic radical or an aliphatic radical,and on the other hand to novel compounds of the formula (I).

Abstract: The present invention relates to the use of fluorinated triazoles in treating affective disorders.

Abstract: The invention relates to a process for the production of epothilones and intermediate products within the process.Epothilones A and B are natural substances, which can be produced by microorganisms, and the taxols have similar properties and are thus of particular interest in pharmaceutical chemistry.

Abstract: There are described compounds of formula I ##STR1## wherein R.sub.1 and R.sub.2 are as defined in the description, Q is heterocyclyl boned via a ring nitrogen atom and having the formula IA ##STR2## wherein R.sub.3 and R.sub.4 and m and n are as defined in the description, the ring marked A is a heterocyclyl having 5 to 9 ring atoms and having at least one saturated bond, it being possible for a further ring hetero atom selected from O and S to be present in addition to the bonding nitrogen atom, the ring system marked B is a free or benzo-, thieno-, furo-, pyrrolo- or dihydropyrrolo-fused carbocyclic ring having from 5 to 9 carbon atoms that is fused to the ring A and may be unsaturated, partially saturated or fully saturated, and the bond marked by a parallel dotted line between the ring systems marked A and B is either a single bond or a double bond, and a salt thereof where at least one salt-forming group is present.

Abstract: Described are 7H-pyrrolo[2,3-d]pyrimidine derivatives of formula I ##STR1## wherein the symbols are as defined in claim 1. Those compounds inhibit tyrosine protein kinase and can be used in the treatment of hyperproliferative diseases, for example tumour diseases.

Abstract: N-(N'-substituted glycyl)-2-cyanopyrrolidines of formula I ##STR1## wherein R is as defined herein. Compounds of formula I inhibit DPP-IV (dipeptidyl-peptidase-IV) activity. They are therefore indicated for use as pharmaceuticals in inhibiting DPP-IV and in the treatment of conditions mediated by DPP-IV, such as non-insulin-dependent diabetes mellitus, arthritis, obesity, osteoporosis and further conditions of impaired glucose tolerance.

Abstract: Compounds of the formula I ##STR1## in which R.sub.1 is hydroxyl or an aliphatic, araliphatic or aromatic radical,X is a divalent aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, araliphatic, heteroarylaliphatic or aromatic radical,R.sub.2 is hydrogen or an aliphatic or araliphatic radical, alk is lower alkylidene andR.sub.3, R.sub.4 and R.sub.5 independently of one another are hydrogen, lower alkyl, halogen, trifluoromethyl, cyano or nitro,and their salts can be used for the treatment of pathological conditions which respond to blockage of excitatory amino acid receptors, and for the production of pharmaceutical preparations.

Abstract: The invention discloses certain N-(substituted glycyl)-4-cyanothiazolidines, pharmaceutical compositions containing said compounds as an active ingredient thereof, and the use of said compounds in inhibiting dipeptidyl peptidase-IV.

Abstract: The invention discloses certain N-(substituted glycyl)-thiazolidines, pharmaceutical compositions containing said compounds as an active ingredient thereof, and the use of said compounds in inhibiting dipeptidyl peptidase-IV.

Abstract: A process for preparing the d-threo isomer of methylphenidate hydrochloride comprising resolving the racemic mixture of threo methylphenidate hydrochloride with dibenzoyl-D-tartaric acid to obtain a dibenzoyl-D-tartrate salt enriched with the d-threo isomer of methylphenidate in a first step, basifying the tartrate salt to obtain the free base form of the d-threo isomer of methylphenidate in a second step, converting the free base to the hydrochloride salt form of the d-threo isomer of methylphenidate in high optical purity in a third step, and recrystallizing the hydrochloride salt form to obtain the desired d-threo isomer in a higher optical purity.

Abstract: A compound which is a dinucleotide analogue of formula ##STR1## or a salt thereof, where B.sup.1 and B.sup.2 are each independently a monovalent nucleoside base radical,R.sup.1 is hydrogen or Y.sup.1,R.sup.2 and R.sup.3 are each independently hydrogen, halogen, hydroxy or --OY.sup.2,R.sup.4 is hydrogen, halogen, hydroxy, --OY.sup.3 or R.sup.7,R.sup.5 is hydrogen, halogen or R.sup.8,R.sup.6 is hydrogen, Y.sup.4 or a phosphoramidyl group,Z is a group of formula II, III or IV ##STR2## where R.sup.9 is hydrogen, halogen, hydroxy, --OY.sup.5 or R.sup.13, R.sup.10 is hydrogen, halogen or R.sup.14, R.sup.11 is hydroxy, R.sup.15 or --OR.sup.15 where R.sup.15 is a C.sub.1 to C.sub.10 aliphatic group, a C.sub.3 to C.sub.8 cycloaliphatic group, a C.sub.6 to C.sub.10 aromatic group or a C.sub.7 to C.sub.13 araliphatic group, and R.sup.12 is hydrogen, R.sup.12.sub.a or --OCOR.sup.12.sub.a where R.sup.12.sub.a is a C.sub.1 to C.sub.10 aliphatic group, a C.sub.3 to C.sub.8 cycloaliphatic group, a C.sub.6 to C.sub.

Abstract: 2,3-Dioxo-1,2,3,4-tetrahydro-quinoxalinyl derivatives of formula (I), ##STR1## wherein one of the radicals R.sub.1, and R.sub.2 is a group R.sub.5 and the other is a group of formula --CH(R.sub.6)--alk--R.sub.7 (Ia), --alk--CH(R.sub.6 -R.sub.7 (Ib), --alk--N(R.sub.8)--X--R.sub.7 (Ic), --alk--N.sup.+ (R.sub.8)(R.sup.9)--X--R.sub.7 A.sup.- (Id), --alk--O--X--R.sub.7 (Ie) or --alk--S--X--R.sub.7 (If), R.sub.3, R.sub.4 and R.sub.5 are each independently of the others hydrogen, lower alkyl, halogen, trifluoromethyl, cyano or nitro, R.sub.6 is unsubstituted or lower alkylated and/or lower alkanoylated amino, R.sub.

Abstract: The present invention relates to the use of fluorinated triazoles in treating neuropathic pain.

Abstract: The invention relates to a process for the production of epothilones and intermediate products within the process.Epothilones A and B are natural substances, which can be produced by microorganisms, and the taxols have similar properties and are thus of particular interest in pharmaceutical chemistry.

Abstract: N-(N'-substituted glycyl)-2-cyanopyrrolidines of formula I ##STR1## Compounds of formula I inhibit DPP-IV (dipeptidyl-peptidase-IV) activity. They are therefore indicated for use as pharmaceuticals in inhibiting DPP-IV and in the treatment of conditions mediated by DPP-IV, such as non-insulin-dependent diabetes mellitus, arthritis, obesity, osteoporosis and further conditions of impaired glucose tolerance.