Abstract: The invention concerns a process for the preparation of N-aryl-aza-heterocycles of the general formula I by reaction of aza-heterocycles with activated aryl halides with use of caesium carbonate without addition of further catalysts at room temperature.

Abstract: The invention concerns a process for the preparation of N-aryl-aza-heterocycles of the general formula I 1

Abstract: Methods and materials for preparing irreversible inhibitors of tyrosine kinases of general Formula 1 are disclosed. Such inhibitors, which include N-[4-(3-chloro-4-floro-phenylamino)-7-(3-morpholin-4-yl-propoxy)-quinazolin-6-yl]-acrylamide, are useful for treating cancer, restenosis, atherosclerosis, endometriosis and psoriasis. The disclosed methods employ protecting schemes to minimize undesirable diacryloylamino-quinazoline side products.

Abstract: The invention concerns a process for the preparation of N-aryl-aza-heterocycles of the general formula I by reaction of aza-heterocycles with activated aryl halides with use of caesium carbonate without addition of further catalysts at room temperature.

Abstract: Process for the preparation of symmetrical and asymmetrical carbonates of the general formula I by reaction of alcohols of the general formula II and alkyl or aryl halides of the general formula III, R—OH  II R′—HAL  III with carbon dioxide and caesium carbonate at room temperature in dipolar aprotic solvents.

Abstract: There are described polymorphic forms/hydrates of N-[4-(3-chloro-4-fluorophenylamino)-7-(3-morpholin-4-yl-propoxy)-quinazolin-6-yl]-acrylamide dihydrochloride, processes for their preparation, as well as the use of the same for the preparation of medicaments with irreversible tyrosine kinase inhibiting action.

Abstract: The invention concerns a one-pot reaction for the preparation of (3-chloro-4-fluorophenyl)-[7-(3-morpholin-4-yl-propoxy)-6-nitroquinazolin-4-yl]-amine (I) or of (3-chloro-4-fluorophenyl)-[7-(3-morpholino-4-yl-propoxy)-6-aminoquinazolin-4-yl]-amine (VII)

Abstract: The invention concerns a one-pot reaction for the preparation of (3-chloro-4-fluorophenyl)-[7-(3-morpholin-4-yl-propoxy)-6-nitroquinazolin-4-yl]-amine (I) 1

Abstract: The invention relates to a method of producing heterocyclic carbamates of the general formula (I) by reacting aza-heterocyclic compounds with alkyl- or aryl-halides in the presence of carbon dioxide and alkali carbonate, and to new compounds of the general formula (I).

Abstract: The invention concerns a one-pot reaction for the preparation of (3-chloro-4-fluorophenyl)-[7-(3-morpholin-4-yl-propoxy)-6-nitroquinazolin-4-yl]-amine (I) 1

Abstract: The present invention is concerned with the use of indolocarbazole imides of the general formula (I): ##STR1## for the preparation of pharmaceutical compositions for the treatment and/or prevention of cancer, virus diseases (for example HIV infections), heart and blood vessel diseases (for example high blood pressure, thromboses, heart rhythm disturbances and atheroscleroses), bronchopulmonary diseases, degenerative diseases of the central nervous system (for example Alzheimer's disease), inflammatoryl diseases (for example rheumatism and arthritis), diseases of the immune system (for example allergies), as well as psoriasis and for use as immune suppressives; as well as new compounds of general formula (I).

Abstract: The present invention is concerned with the use of indolocarbazole imides of the general formula (I): ##STR1## for the preparation of pharmaceutical compositions for the treatment and/or prevention of cancer, virus diseases (for example HIV infections), heart and blood vessel diseases (for example high blood pressure, thromboses, heart rhythm disturbances and atheroscleroses), bronchopulmonary diseases, degenerative diseases of the central nervous system (for example Alzheimer's disease), inflammatory diseases (for example rheumatism and arthritis), diseases of the immune system (for example allergies), as well as psoriasis and for use as immune suppressives; as well as new compounds of general formula (I).

Abstract: The instant invention is a compound of formulaA--X--Y--E.sub.n --R.sup.5in which A is a bis-indolylmaleinimide or indolopyrrolocarbazole useful in the treatment and/or prevention of cancer, viral diseases, thrombosis, heart rhythm disturbances, atherosclerosis, bronchopulmonary diseases, degenerative diseases of the central nervous system, inflammatory diseases, diseases of the immune system, psoriasis, and immune suppression. A pharmaceutical composition and methods of preparing the compounds are also included.

Abstract: The present invention provides bis-(1H-indol-3-yl)maleinimide derivatives and the pharmacologically acceptable salts thereof, processes for the preparation of these compounds, and pharmaceutical compositions containing them for the treatment of heart and blood vessel diseases, such as thromboses, arteriosclerosis, hypertension, of inflammatory processes, allergies, cancer, and certain degenerative damages of the central nervous system, as well as of diseases of the immune system and viral diseases.

Abstract: New indolocarbazoles of formula: ##STR1## or a pharmaceutically acceptable salt thereof, processes for their preparation, compositions containing, and methods for using the composition for the inhibition of protein kinases, such as protein kinase C, for the prevention and/or treatment of heart and blood vessel diseases such as thromboses, arterioscleroses, hypertension, or for inflammatory processes, allergies, cancers, viral diseases, and certain degenerative damages of the central nervous system are disclosed.

Abstract: The present invention provides bis-(1H-indol-3-yl)maleinimide derivatives and the pharmacologically acceptable salts thereof, processes for the preparation of these compounds, and pharmaceutical compositions containing them for the treatment of heart and blood vessel diseases, such as thromboses, arteriosclerosis, hypertension, of inflammatory processes, allergies, cancer, and certain degenerative damages of the central nervous system, as well as of diseases of the immune system and viral diseases.

Abstract: 1,2,4-Benzothiadiazine oxide derivatives of the general Formula I ##STR1## in which R.sup.1 represents an unsubstituted or substituted aryl radical;R.sup.2 and R.sup.5, which may be the same or different, and represent hydrogen, halogen, or a nitro group, andR.sup.3 represents a hydrogen atom or a hydroxy radical, an alkyl, alkoxy alkyl or alkoxy carbonyl radical with up to four carbon atoms, unsubstituted or substituted by halogen, hydroxy, amino, alkyl amino or dialkyl amino radicals, or a phenyl radical, unsubstituted or substituted by halogen,are described as having anxiolytic effects on the central nervous system.

Abstract: The present invention provides compounds of the general formula I ##STR1## wherein R.sup.1 and R.sup.2, which are the same or different, are unsubstituted or substituted aromatic rings, Alk is a straight-chained or branched lower hydrocarbon chain and Z is a hydrogen atom, with the proviso that when Alk is a straight-chained hydrocarbon chain, Z can also be a lower alkylamino radical of the general formula II ##STR2## in which R.sup.3 and R.sup.4 are the same or different and are hydrogen atoms or straight-chained or branched lower alkyl radicals or R.sup.3 and R.sup.4, together with the nitrogen atom to which they are attached, can also form a ring optionally containing further hetero atoms; and the pharmacologically acceptable salts thereof.The present invention also provides an inventive process for preparing these compounds, as well as pharmaceutical compositions containing them. The compounds I may be used in the therapy of inflammations and they are free of gastrointestinal side effects.

Abstract: 4-Thioxobenzopyrano[2,3-d]-pyrimidine derivatives of the general formulae Ia or Ib ##STR1## are described. Compounds Ia and Ib are tautomers and are valuable intermediates for the preparation of 5H-[1]-benzopyrano[2,3-d]pyrimidine derivatives having ulcer-protective action without inhibition of secretion.

Abstract: The invention relates to 5H-[1]benzopyrano-[2,3-d]pyrimidine derivatives of the general formula I ##STR1## which may be prepared by means of a new chemical process and have a protective effect similar to that of cimetidine, but do not exhibit the undesired side effects of antisecretory agents. The invention is based on a new mucoprotective mode of action which prevents lesions of the mucous membrane epithelium to arise.