SURFACE RELIEF MICROSTRUCTURES, RELATED DEVICES AND METHOD OF MAKING THEM

The present invention relates to a method for the replication of a patterned surface relief microstructure, comprising the steps of generation of a first layer with a patterned surface relief microstructure, generation of a master, by copying the microstructure of the first layer into a second layer, thereby involving at least one dry or wet etching step, characterized by an additional step, in which the microstructure of the master is brought into contact with a replica material, such that the microstructure of the master is reproduced in the replica. 1. Method for the replication of a patterned surface relief microstructure , comprising the steps ofgeneration of a first layer with a patterned surface relief microstructure on top of a second layer, the first layer comprising a first material and the second layer comprising a second materialgeneration of a master, by copying the microstructure of the first layer into the second layer, thereby involving at least one dry or wet etching step,characterized by an additional step, in which the microstructure of the master is brought into contact with a replica material, such that the microstructure of the master is reproduced in the replica material with an inverse surface relief profile as compared to that of the master.2. Method according to claim 1 , wherein in one of the etching steps the thickness of the first layer is reduced until the material in the lower zones of the surface relief microstructure is cleared away and parts of the underlying second layer are set free.3. Method according to claim 1 , wherein the depth of the copied microstructure is larger than that of the original microstructure.4. Method according to claim 1 , wherein the depth of the copied microstructure is different in different areas.5. Method according to claim 1 , wherein there is at least one area of the pattern claim 1 , which comprises an anisotropic microstructure.6. Method according to claim 1 , wherein the pattern comprises at least ...

Combination therapy with parp inhibitors

The present invention describes benzimidazole derivatives of Formula (I) which constitute potent PARP inhibitors in combination with radiotherapy or in combination with other chemotherapeutic agents.

NOVEL CARBOXYLIC ACID DERIVATIVES, THEIR PREPARATION AND USE

1. A carboxylic acid derivative of the formula I{'sup': '2', 'sub': 2', '1', '4', '1', '4', '2', '1', '4', '1', '4', '1', '4', '1', '4', '1', '4, 'Rhydrogen, hydroxyl, NHNH (C-C-alkyl), N(C-C-alkyl), halogen, C-Calkyl, C-C-haloalkyl, C-C-alkoxy, C-C-haloalkoxy or C-C-alkylthio;'}{'sup': 14', '14', '14', '3, 'sub': 1', '5', '1', '4', '1', '4, 'x nitrogen or CRwhere Ris hydrogen or C--alkyl, or CRforms together with CRa 5- or 6-membered alkylene or alkenylene ring which can be substituted by one or two C--alkyl groups and in which in each case a methylene group can be replaced by oxygen, sulfur, —NH or —NC--alkyl;'}{'sup': '3', 'sub': 2', '1', '4', '1', '4', '2', '1', '4', '1', '4', '1', '4', '1', '4', '1', '4', '1', '4', '3', '14, 'Rhydrogen, hydroxyl, NH, NH(C-C-Alkyl), N (C-C-alkyl), halogen, C-C-alkyl, C-C-haloalkyl, C-C-alkoxy, C-C-haloalkoxy, —NH—O—C--alkyl, C-C-alkylthio or CRis linked to CRas indicated above to give a 5- or 6-membered ring;'}{'sup': 4', '5, 'claim-text': [{'sub': 1', '4', '1', '4', '1', '4', '1', '4', '1', '4', '1', '4', '1', '4, 'phenyl or naphthyl, which can be substituted by one or more of the following radicals: halogen, nitro, cyano, hydroxyl, C-C-alkyl, C-C-haloalkyl, C-C-alkoxy, C-C-haloalkoxy, phenoxy, C-C-alkylthio, amino, C-C-alkylamino or C-C-dialkylamino; or'}, {'sub': 2', '3', '7, 'phenyl or naphthyl, which are connected together in the ortho positions via a direct linkage, a methylene, ethylene or ethenylene group, an oxygen or sulfur atom or an SO, NH or N-alkyl group or C-C-cycloalkyl;'}], 'Rand R(which can be identical or different){'sub': 1', '8', '3', '6', '3', '6', '3', '8', '1', '4', '3', '6', '3', '6', '1', '4', '1', '4', '1', '4', '1', '4', '3-8', '1', '4', '1', '4', '1', '4', '1', '4', '1', '4', '1', '4', '1', '4, 'claim-text': [{'sub': 1', '4', '1', '4', '1', '4', '1', '4', '1', '4', '1', '4', '1', '4, 'phenyl or naphthyl, each of which can be substituted by one or more of the following radicals: halogen, nitro, cyano ...

SUBSTITUTED OXINDOLE DERIVATIVES, MEDICAMENTS CONTAINING THE LATTER AND USE THEREOF

The invention relates to novel oxindole derivatives of general formula (I), in which the substituents A, B, R, Rand Rare defined as cited in claim , to medicaments containing said derivatives and to the use of the latter for the prophylaxis and/or treatment of vasopressin-dependent and/or oxytocin-dependent diseases. 7. A compound according to any of to , having a binding affinity Ki for the vasopressin V1b receptor subtype of less than about 100 nM.8. A compound according to any of to , having a selectivity for the vasopressin V1b receptor subtype vis-à-vis the vasopressin V1a receptor subtype , the quotient of Ki(V1a)/Ki(V1b) being greater than 1.9. A compound according to any of to , having a selectivity for the vasopressin V1b receptor subtype vis-à-vis the vasopressin V2 receptor subtype , the quotient of Ki(V2)/Ki(V1b) being greater than 1.10. A compound according to any of to , having a selectivity for the vasopressin V1b receptor subtype vis-à-vis the oxytocin (OT) receptor , the quotient of Ki(OT)/Ki(V1b) being greater than 1.11. A compound according to any of to , having a binding affinity Ki for the vasopressin V1b receptor subtype of less than 100 nM and a selectivity for the vasopressin V1b receptor subtype vis-à-vis the vasopressin V1a receptor subtype , the quotient of Ki(V1a)/Ki(V1b) being greater than 1.12. A compound according to any of to , having a binding affinity Ki for the vasopressin V1b receptor subtype of less than 100 nM and a selectivity for the vasopressin V1b receptor subtype vis-à-vis the vasopressin V2 receptor subtype , the quotient of Ki(V2)/Ki(V1b) being greater than 1.13. A compound according to any of to , having a binding affinity Ki for the vasopressin V1b receptor subtype of less than 100 nM and a selectivity for the vasopressin V1b receptor subtype vis-à-vis the oxytocin (OT) receptor , the quotient of Ki(OT)/Ki(V1b) being greater than 1.14. A compound according to any of to , having a binding affinity Ki for the vasopressin ...

QUINOLINE COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE SEROTONIN-5-HT6 RECEPTOR

The present invention relates to novel quinoline compounds of the formula (I) and to the salts thereof. The compounds possess valuable therapeutic properties and are particularly suitable, for treating diseases that respond to modulation of the serotonin 5-HTreceptor. In formula (I) R is a moiety of the formula (R) wherein * indicates the binding site to the quinolinyl radical and wherein A, B, X′, Y, Q, R, R, R, R, R, m, n, p, q, R, R, X and Ar are as defined in claim . 132-. (canceled)34. The method of claim 33 , wherein the variables x and y of the moiety R are 0 claim 33 , 1 or 2 claim 33 , provided that x+y is 1 claim 33 , 2 or 3.35. The method of claim 33 , wherein the variables a and b of the moiety R are 0 claim 33 , 1 or 2 claim 33 , provided that a+b is 1 claim 33 , 2 or 3.36. The method of claim 33 , wherein Q is N.37. The method of claim 33 , wherein the variable q of the moiety R is 0.38. The method of claim 33 , wherein the variable p of the moiety R is 0.39. The method of claim 33 , wherein Ris hydrogen.40. The method of claim 33 , wherein Rand Rare hydrogen.42. The method of claim 41 , wherein the moiety R is selected from a radical selected from the group consisting of the formulae R-1 claim 41 , R-3 claim 41 , R-5 claim 41 , R-6 claim 41 , R-8 claim 41 , R-9 claim 41 , R-10 claim 41 , R-11 claim 41 , R-12 claim 41 , R-13 claim 41 , R-15 claim 41 , R-17 claim 41 , R-21 claim 41 , R-22 claim 41 , R-24 claim 41 , R-25 claim 41 , R-27 claim 41 , R-28 claim 41 , R-29 claim 41 , R-34 claim 41 , R-35 claim 41 , R-36 claim 41 , R-37 claim 41 , R-38 and R44.43. The method of claim 33 , wherein X is SO.44. The method of claim 33 , wherein X is CH.45. The method of claim 33 , wherein X is C(O).46. The method of claim 33 , wherein X is located in the 3-position of the quinolinyl moiety.47. The method of claim 33 , wherein X is located in the 4-position of the quinolinyl moiety.48. The method of claim 33 , wherein Ar is phenyl claim 33 , naphthyl claim 33 , ...

SUBSTITUTED OXINDOLE DERIVATIVES, MEDICAMENTS CONTAINING SAID DERIVATIVES AND USE THEREOF

The invention relates to novel oxindole derivatives of general formula (I), wherein the substituents R, R, A, B, and Y are defined as in Claim . The invention further relates to medicaments containing said derivatives, and use thereof for the prevention and/or treatment of vasopressin-dependent diseases. 190-. (canceled)92. The method of characterized in that the patient is a mammal.93. A method for preparing at least one compound of general formula (I) characterized in that said compound may be prepared by a competent person skilled in the art and having knowledge of the technical teaching of the invention for carrying out and/or analogously carrying out method steps known as such. The present invention relates to novel substituted oxindole derivatives, medicaments containing same, and use thereof for the treatment of diseases.Vasopressin (AVP) is an endogenous hormone which has various effects on organs and tissues. Vasopressin is related to oxytocin (OT), and therefore both peptides are combined into a vasopressin/oxytocin family. It is suspected that the vasopressin/oxytocin system plays a role in various medical conditions. Currently, three vasopressin receptors (V1, V1or V3, and V2 receptors) and one oxytocin receptor (OT receptor) are known which mediate the effects of vasopressin and oxytocin. Antagonists of these receptors, in particular antagonists which bind specifically to only one of the above receptors, represent novel therapeutic approaches to the treatment of diseases (M. Thibonnier, Exp. Opin. Invest. Drugs 1998, 7(5), 729-740). For example, it has been found that a selective antagonist of the vasopressin V1 b receptor has anxiolytic and antidepressive effects in animal models (Griebel et al., PNAS 2002, 99, 6370; Serradeil-Le Gal et al., J. Pharm. Exp. Ther. 2002, 300, 1122). Since the described models have a certain predictive capability for the anticipated clinical effects, antagonists of the V1b receptor are of special interest for the treatment ...

Novel carboxylic acid derivatives, their preparation and use

Carboxylic acid derivatives where R—R 6 , X, Y and Z have the meanings stated in the description, and the preparation thereof, are described. The novel compounds are suitable for controlling diseases.

GUANIDINE COMPOUNDS, AND USE THEREOF AS BINDING PARTNERS FOR 5-HT5 RECEPTORS

The present invention relates to guanidine compounds of the general formula I 3. Guanadine compound according to or , wherein the given moieties have the following definition:W: W1;{'sub': 3', '2', '3', '2, 'claim-text': [{'sub': 1', '6', '2', '6, 'each optionally substituted C-C-alkyl or C-C-alkenyl,'}, {'sub': 2', 'A', 'A', 'A', 'A', 'A', 'A', 'A', 'A', 'A, 'sup': 1', '1', '1', '2', '3', '4', '1', '4', '1, 'O—CH—COO—R, O—R, S—R, NRR, NR—CO—Ror CO—NRR;'}], 'A: halogen, OH, CN, CF, CHF, OCF, OCHF, or'}{'sub': A', '1', '4', '3', '7, 'sup': '1', 'R: each optionally substituted C-C-alkyl, C-C-cycloalkyl, phenyl or benzyl;'}{'sub': 'A', 'sup': '2', 'claim-text': {'sub': 1', '4', '1', '4', '1', '4', '2', '1', '4', '2', '2', '2', '1', '4, 'each optionally substituted C-C-alkyl, phenyl, benzyl, phenethyl, CO—C-C-alkyl, CO-aryl, CO—O—C-C-alkyl, SO—C-C-alkyl, SO-aryl, SO-hetaryl or SO—C-C-alkylene-aryl;'}, 'R: hydrogen, or'}{'sub': A', '1', '4', '1', '4', '1', '4', '2', '1', '4', '2', '2', '2', '1', '4, 'sup': '3', 'claim-text': {'sub': A', 'A, 'sup': 2', '3, 'or the moieties Rand Rtogether form an optionally substituted 5- or 6-membered saturated or unsaturated ring, which can contain up to two identical or different heteroatoms from the group O and N;'}, 'R: each optionally substituted C-C-alkyl, phenyl, benzyl, phenethyl, CO—C-C-alkyl, CO-aryl, CO—O—C-C-alkyl, SO—C-C-alkyl, SO-aryl, SO-hetaryl, or SO—C-C-alkylene-aryl;'}{'sub': A', '1', '4, 'sup': '4', 'R: hydrogen or an optionally substituted C-C-alkyl moiety;'}B: hydrogen or as moiety A is defined;{'sub': W', '3', '3, 'sup': '1', 'claim-text': {'sub': 1', '4', '1', '6', '1', '6, 'each optionally substituted C-C-alkyl, aryl, C-C-alkylamino or C-C-dialkylamino;'}, 'R: hydrogen, F, Cl, CN, CF, O—CF, or'}in the formula Z1 the sum of a, b and c is 1, 2 or 3;{'sub': Z', 'Z', 'Z', 'Z, 'sup': 1', '2', '3', '4, 'claim-text': {'sub': 1', '6, 'hydrogen, halogen, OH, optionally substituted C-C-alkyl;'}, 'R, R, R, Rindependently of ...

GUANIDINE COMPOUNDS AND USE THEREOF AS BINDING PARTNERS FOR 5-HT5 RECEPTORS

The present invention relates to guanidine compounds of the general formula I 3. Guanadine compound according to or , wherein the given moieties have the following definition:W: W1;{'sub': 3', '2', '3', '2, 'claim-text': {'sub': 1', '6', '2', '6', '2', 'A', 'A', 'A', 'A', 'A', 'A', 'A', 'A', 'A, 'sup': 1', '1', '1', '2', '3', '4', '1', '4', '1, 'each optionally substituted C-C-alkyl or C-C-alkenyl, O—CH—COO—R, O—R, S—R, NRR, NR—CO—Ror CO—NRR;'}, 'A: halogen, OH, CN, CF, CHF, OCF, OCHF, or'}{'sub': A', '1', '4', '3', '7, 'sup': '1', 'R: each optionally substituted C-C-alkyl, C-C-cycloalkyl, phenyl or benzyl;'}{'sub': 'A', 'sup': '2', 'claim-text': {'sub': 1', '4', '1', '4', '1', '4', '2', '1', '4', '2', '2', '2', '1', '4, 'each optionally substituted C-C-alkyl, phenyl, benzyl, phenethyl, CO—C-C-alkyl, CO-aryl, CO—O—C-C-alkyl, SO—C-C-alkyl, SO-aryl, SO-hetaryl or SO—C-C-alkylene-aryl;'}, 'R: hydrogen, or'}{'sub': A', '1', '4', '1', '4', '1', '4', '2', '1', '4', '2', '2', '2', '1', '4, 'sup': '3', 'claim-text': {'sub': A', 'A, 'sup': 2', '3, 'or the moieties Rand Rtogether form an optionally substituted 5- or 6-membered saturated or unsaturated ring, which can contain up to two identical or different heteroatoms from the group O and N;'}, 'R: each optionally substituted C-C-alkyl, phenyl, benzyl, phenethyl, CO—C-C-alkyl, CO-aryl, CO—O—C-C-alkyl, SO—C-C-alkyl, SO-aryl, SO-hetaryl, or SO—C-C-alkylene-aryl;'}{'sub': A', '1', '4, 'sup': '4', 'R: hydrogen or an optionally substituted C-C-alkyl moiety;'}B: hydrogen or as moiety A is defined;{'sub': w', '3', '3, 'sup': '1', 'claim-text': {'sub': 1', '4', '1', '6', '1', '6, 'each optionally substituted C-C-alkyl, aryl, C-C-alkylamino or C-C-dialkylamino;'}, 'R: hydrogen, F, Cl, CN, CF, O—CF, or'}in the formula Z1 the sum of a, b and c is 1, 2 or 3;{'sub': Z', 'Z', 'Z', 'Z, 'sup': 1', '2', '3', '4, 'claim-text': {'sub': 1', '6, 'hydrogen, halogen, OH, optionally substituted C-C-alkyl;'}, 'R, R, R, Rindependently of one another ...

HETEROARYL-SUBSTITUTED 1,3-DIHYDROINDOL-2-ONE DERIVATIVES AND MEDICAMENTS CONTAINING THEM

The present invention relates to novel 1,3-dihydroindol-2-one (oxindole) derivatives of the formula (I) 2. The compound of claim 1 , wherein A is selected from the group consisting of aromatic heteromonocyclic and aromatic heterobicyclic systems comprising 1 or 2 heteroatoms claim 1 , where one of the 2 heteroatoms is nitrogen.3. The compound of claim 1 , wherein A is selected from the group consisting of benzothiazole claim 1 , pyrimidine claim 1 , pyridine claim 1 , pyridazine claim 1 , pyrazine claim 1 , isoquinoline claim 1 , quinoline claim 1 , thiazole claim 1 , benzimidazole claim 1 , imidazole claim 1 , benzoxazole claim 1 , benzothiophene claim 1 , thiophene claim 1 , benzofuran and furan.5. The compound of claim 4 , wherein B is selected from the group consisting of thiophene claim 4 , furan claim 4 , pyrrole claim 4 , pyrazole claim 4 , isoxazole claim 4 , pyridine claim 4 , pyrimidine claim 4 , quinoline claim 4 , isoquinoline claim 4 , tetrahydroisoquinoline claim 4 , benzothiophene claim 4 , benzofuran claim 4 , indole claim 4 , thiazole claim 4 , imidazothiazole claim 4 , benzooxazine and quinoxaline.7. The compound of claim 6 , wherein D is selected from the group consisting of aromatic heteromonocyclic and aromatic heterobicyclic systems comprising 1 or 2 heteroatoms claim 6 , where one of the 2 heteroatoms is nitrogen.8. The compound of claim 6 , wherein D is selected from the group consisting of benzothiazole claim 6 , pyrimidine claim 6 , pyridine claim 6 , pyridazine claim 6 , pyrazine claim 6 , isoquinoline claim 6 , quinoline claim 6 , thiazole claim 6 , benzimidazole claim 6 , imidazole claim 6 , benzoxazole claim 6 , benzothiophene claim 6 , thiophene claim 6 , benzofuran and furan.9. The compound of any of claim 6 , wherein G is selected from the group consisting of thiophene claim 6 , furan claim 6 , pyrrole claim 6 , pyrazole claim 6 , isoxazole claim 6 , pyridine claim 6 , pyrimidine claim 6 , quinoline claim 6 , isoquinoline claim 6 , ...

HETEROARYL-SUBSTITUTED 1,3-DIHYDROINDOL-2-ONE DERIVATIVES AND MEDICAMENTS CONTAINING THEM

The present invention relates to novel 1,3-dihydroindol-2-one (oxindole) derivatives of the formula (I) 2. The compound of claim 1 , wherein A is selected from the group consisting of aromatic heteromonocyclic and aromatic heterobicyclic systems comprising 1 or 2 heteroatoms claim 1 , where one of the 2 heteroatoms is nitrogen.3. The compound of claim 1 , wherein A is selected from the group consisting of benzothiazole claim 1 , pyrimidine claim 1 , pyridine claim 1 , pyridazine claim 1 , pyrazine claim 1 , isoquinoline claim 1 , quinoline claim 1 , thiazole claim 1 , benzimidazole claim 1 , imidazole claim 1 , benzoxazole claim 1 , benzothiophene claim 1 , thiophene claim 1 , benzofuran and furan.5. The compound of claim 4 , wherein B is selected from the group consisting of thiophene claim 4 , furan claim 4 , pyrrole claim 4 , pyrazole claim 4 , isoxazole claim 4 , pyridine claim 4 , pyrimidine claim 4 , quinoline claim 4 , isoquinoline claim 4 , tetrahydroisoquinoline claim 4 , benzothiophene claim 4 , benzofuran claim 4 , indole claim 4 , imidazole claim 4 , thiazole claim 4 , imidazothiazole claim 4 , benzooxazine and quinoxaline.7. The compound of claim 6 , wherein D is selected from the group consisting of aromatic heteromonocyclic and aromatic heterobicyclic systems comprising 1 or 2 heteroatoms claim 6 , where one of the 2 heteroatoms is nitrogen.8. The compound of claim 6 , wherein D is selected from the group consisting of benzothiazole claim 6 , pyrimidine claim 6 , pyridine claim 6 , pyridazine claim 6 , pyrazine claim 6 , isoquinoline claim 6 , quinoline claim 6 , thiazole claim 6 , benzimidazole claim 6 , imidazole claim 6 , benzoxazole claim 6 , benzothiophene claim 6 , thiophene claim 6 , benzofuran and furan.9. The compound of any of to claim 6 , wherein G is selected from the group consisting of thiophene claim 6 , furan claim 6 , pyrrole claim 6 , pyrazole claim 6 , isoxazole claim 6 , pyridine claim 6 , pyrimidine claim 6 , quinoline claim 6 , ...

5,6-DISUBSTITUTED OXINDOLE-DERIVATIVES AND USE THEREOF FOR TREATING VASOPRESSIN-DEPENDENT DISEASES

The present invention relates to novel 5,6-disubstituted oxindole derivatives, pharmaceutical compositions comprising them, and their use for the manufacture of a medicament. 247.-. (canceled)48. A method for the treatment of vasopressin-dependent diseases claim 1 , the method comprising administering a compound of or a pharmaceutically acceptable salt thereof to a subject in need thereof.49. A method for the treatment of diseases selected from hypertension claim 1 , pulmonary hypertension claim 1 , heart failure claim 1 , myocardial infarction claim 1 , coronary spasm claim 1 , unstable angina claim 1 , PTCA (percutaneous transluminal coronary angioplasty) claim 1 , ischemias of the heart claim 1 , impairments of the renal system claim 1 , edemas claim 1 , renal vasospasm claim 1 , necrosis of the renal cortex claim 1 , hyponatremia claim 1 , hypokalemia claim 1 , Schwartz-Bartter syndrome claim 1 , impairments of the gastrointestinal tract claim 1 , gastritic vasospasm claim 1 , hepatocirrhosis claim 1 , gastric and intestinal ulcers claim 1 , emesis claim 1 , emesis occurring during chemotherapy claim 1 , travel sickness claim 1 , diabetes claim 1 , insulin resistance claim 1 , nocturnal enuresis claim 1 , incontinence claim 1 , and diseases in which impairments of blood clotting occur claim 1 , and/or for delaying micturition claim 1 , the method comprising administering a compound of or a pharmaceutically acceptable salt thereof to a subject in need thereof.50. A method for the treatment of behavioral diseases selected from affective disorders claim 1 , depressive disorders claim 1 , psychoses claim 1 , psychotic disorders claim 1 , anxiety disorders claim 1 , stress-dependent anxiety disorders claim 1 , sleep disorders claim 1 , childhood onset mood disorders claim 1 , Cushing's syndrome claim 1 , memory impairment claim 1 , Alzheimer's disease claim 1 , vasomotor symptoms claim 1 , thermoregulatory dysfunctions claim 1 , schizophrenia claim 1 , and stress- ...

HETEROCYCLIC COMPOUNDS AND THEIR USE AS BINDING PARTNERS FOR 5-HT5 RECEPTORS

The invention relates to compounds of general formula (I), corresponding enantiomeric, diastereomeric and/or tautomeric forms thereof as well as pharmaceutically acceptable salts thereof and the prodrugs of said compounds. The invention also relates to the use of said compounds as binding partners for 5-HT5 receptors for treating diseases that are modulated by a 5-HT5 receptor activity, in particular, for treating neurodegenerative and neuropsychiatric disorders as well as signs, symptoms and dysfunctions. 2. A compound of general formula I according to claim 1 , corresponding enantiomeric claim 1 , diastereomeric and/or tautomeric forms thereof and/or the pharmaceutically acceptable salts thereof and/or the active ingredient precursors (prodrugs) thereof claim 1 , in which:{'sup': 1', '2, 'Rand Rindependently of one another denote'}hydrogen, a free electron pair, OH, CN or optionally substituted{'sub': 1', '6', '1', '6', '1', '6', '1', '6, 'O—C-Calkyl, C-Calkyl, CO—C-Calkyl, CO—OC-Calkyl.'}3. A one compound of general formula I according to claim 1 , corresponding enantiomeric claim 1 , diastereomeric and/or tautomeric forms thereof and/or the pharmaceutically acceptable salts thereof and/or the active ingredient precursors (prodrugs) thereof claim 1 , in which:{'sub': 1', '6', '3', '2', '1', '6', '1', '6', '2', '1', '6', '1', '6', '2', '1', '6', '1', '6, 'claim-text': {'sub': 1', '6', '2', '1', '6', '1', '4', '3', '2', '1', '4', '1', '4', '1', '4', '2', '3', '2', '1', '4', '2', '1', '4', '2', '1', '4', '1', '4, '—N(C-Calkyl)-SO—C-Calkyl, C-Calkylene-CO—N(CH), C-Calkylene-CO—N-piperidyl, C-Calkylene-CO—N-morpholinyl, C-Calkylene-SO—N(CH), C-Calkylene-SO—N-piperidyl, C-Calkylene, SO—N-morpholinyl or C-Calkyl-O—C-Calkyl and'}, 'A denotes OH, —O—C-Calkyl, —OCF, —OCHFor optionally substituted —NH—C-Calkyl, —NH—CO—C-Calkyl, —NH—SO—C-Calkyl, —N(C-Calkyl), piperidinyl, morpholinyl, —N(C-Calkyl)-CO—C-Calkyl or'}{'sub': 3', '3', '2', '2', '1', '6', '2', '6', '2', '6', '3', ...

5-HALOGEN-SUBSTITUTED OXINDOLE DERIVATIVES AND USE THEREOF FOR TREATING VASOPRESSIN-DEPENDENT DISEASES

The present invention relates to novel 5-halogen-substituted oxindole derivatives, pharmaceutical compositions comprising them, and their use for the treatment of vasopressin-dependent disorders. 2. A compound as claimed in claim 1 , in which Ris hydrogen or methoxy.3. A compound as claimed in claim 1 , in which Rand Rare methoxy.4. A compound as claimed in any of the preceding claims claim 1 , in which Ris hydrogen claim 1 , methyl or ethyl.5. A compound as claimed in any of the preceding claims claim 1 , in which Ris ethoxy and Ris H.6. A compound as claimed in any of to claim 1 , in which Ris ethoxy and Ris methyl.7. A compound as claimed in any of to claim 1 , in which Ris isopropoxy and Ris H.8. A compound as claimed in any of the preceding claims claim 1 , in which Ris Cl.9. A compound as claimed in any of to claim 1 , in which Ris F.10. A compound as claimed in any of the preceding claims claim 1 , in which Xis N and Xis CH.11. A compound as claimed in any of to claim 1 , in which Xis CH and Xis N.12. A compound as claimed in any of the preceding claims claim 1 , in which Xis O.13. A compound as claimed in any of to claim 1 , in which Xis NH.14. A compound as claimed in any of to claim 1 , in which Xis CH.15. A compound as claimed in any of the preceding claims claim 1 , in which{'sup': '1', 'Ris methoxy;'}{'sup': '2', 'Ris methoxy;'}{'sup': '3', 'Ris methyl;'}{'sup': '4', 'Ris ethoxy;'}{'sup': '5', 'Ris H;'}{'sup': '6', 'Ris Cl;'}{'sup': '1', 'Xis NH;'}{'sup': '2', 'Xis N; and'}{'sup': '3', 'Xis CH.'}16. A compound as claimed in any of to claim 1 , in which{'sup': '1', 'Ris methoxy;'}{'sup': '2', 'Ris methoxy;'}{'sup': '3', 'Ris methyl;'}{'sup': '4', 'Ris ethoxy;'}{'sup': '5', 'Ris methyl;'}{'sup': '6', 'Ris Cl;'}{'sup': '1', 'Xis NH;'}{'sup': '2', 'Xis N; and'}{'sup': '3', 'Xis CH.'}17. A compound as claimed in any of to claim 1 , in which{'sup': '1', 'Ris methoxy;'}{'sup': '2', 'Ris methoxy;'}{'sup': '3', 'Ris ethyl;'}{'sup': '4', 'Ris ethoxy;'}{'sup': '5 ...

5-RING HETEROAROMATIC COMPOUNDS AND THEIR USE AS BINDING PARTNERS FOR 5-HT5 RECEPTORS

The invention relates to 5-ring heteroaromatic compounds of general formula (I), their use for the treatment and/or prevention of diseases, and medicaments containing same. 2. A 5-ring heteroaromatic compound of general formula I according to , and/or corresponding enantiomeric , diastereomeric , and/or tautomeric forms thereof , and/or pharmaceutically acceptable salts thereof , and/or active substance precursors (“prodrugs”) thereof , wherein the radicals W , A , RRRR , B , Rw , D , Q , a b , c , R , R , R , R , V , R , R , R , R , X , Y , Z , unless stated otherwise below , have the same meaning as in , and the radicals below have the following definitions:{'sup': 4', '6, 'R, Rin each case independently stand for a radical selected from groups 1.), 3.), 4.), or 5.), which may be the same or different, and'}{'sup': 5', '7, 'R, Rin each case independently stand for a radical selected from groups 2.), 3.), 4.), or 5.), which may be the same or different,'}{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'wherein groups 1.)-5.) in each case have the meanings stated in .'}3. A 5-ring heteroaromatic compound of general formula I according to , and/or corresponding enantiomeric , diastereomeric , and/or tautomeric forms thereof , and/or pharmaceutically acceptable salts thereof , and/or active substance precursors (“prodrugs”) thereof , wherein the radicals W , A , R , R , R , R , B , R , D , R , R , R , X , Y , Z , R , R , R , R , R , R , R , R , R , R , R , R , unless stated otherwise below , have the same meaning stated in , and the radicals below have the following definitions:Q: Formula Q1 is the sum of a, b, and c and is equal to 1, 2, or 3;{'sub': Q', 'Q', 'Q', 'Q, 'sup': 1', '2', '3', '4, 'claim-text': {'sub': 1', '6, 'hydrogen, halogen, OH, or optionally substituted C-Calkyl;'}, 'R, R, R, Rindependently stand for{'sub': Q', 'Q', 'Q, 'sup': 5', '5, 'V: is —CO—, —CO—NR—, —NR—CO—, —O—, —S—;'}{'sub': Q', '3, 'sup': '5', 'R: is hydrogen, CH.'}4. A 5-ring ...

AMIDOMETHYL-SUBSTITUTED OXINDOLE DERIVATIVES AND THE USE THEREOF FOR THE TREATMENT OF VASOPRESSIN-DEPENDENT ILLNESSES

The present invention relates to novel amidomethyl-substituted oxindole derivatives, pharmaceutical compositions comprising them, and their use for the treatment of vasopressin-dependent disorders. 2. A compound as claimed in claim 1 , in which Ris hydrogen or methoxy.3. A compound as claimed in any of the preceding claims claim 1 , in which Ris hydrogen claim 1 , methyl or ethyl.4. A compound as claimed in any of the preceding claims claim 1 , in which Xis N and Xis CH.5. A compound as claimed in any of to claim 1 , in which Xis CH and Xis N.6. A compound as claimed in any of the preceding claims claim 1 , in which{'sup': '1', 'Ris methoxy;'}{'sup': '2', 'Ris methoxy;'}{'sup': '3', 'Ris methyl;'}{'sup': '1', 'Xis CH; and'}{'sup': '2', 'Xis N.'}7. A compound as claimed in any of to claim 1 , in which{'sup': '1', 'Ris methoxy;'}{'sup': '2', 'Ris methoxy;'}{'sup': '3', 'Ris methyl;'}{'sup': '1', 'Xis N; and'}{'sup': '2', 'Xis CH.'}8. A compound as claimed in any of to claim 1 , in which{'sup': '1', 'Ris methoxy;'}{'sup': '2', 'Ris methoxy;'}{'sup': '3', 'Ris methyl;'}{'sup': '1', 'Xis CH; and'}{'sup': '2', 'Xis CH.'}9. A compound as claimed in any of to claim 1 , in which{'sup': '1', 'Ris methoxy;'}{'sup': '2', 'Ris methoxy;'}{'sup': '3', 'Ris ethyl;'}{'sup': '1', 'Xis CH; and'}{'sup': '2', 'Xis N.'}10. A compound as claimed in any of to claim 1 , in which{'sup': '1', 'Ris methoxy;'}{'sup': '2', 'Ris methoxy;'}{'sup': '3', 'Ris ethyl;'}{'sup': '1', 'Xis N; and'}{'sup': '2', 'Xis CH.'}11. A compound as claimed in any of the preceding claims claim 1 , which is the (−) enantiomer in an enantiomeric purity of at least 50% ee.12. A compound as claimed in claim 11 , where the (−) enantiomer has an enantiomeric purity of at least 90% ee.13. A compound as claimed in any of to claim 11 , which is the racemate.14. A pharmaceutical composition comprising at least one compound of the formula I as defined in any of the preceding claims and/or at least one pharmaceutically ...

SUBSTITUTED OXINDOLE DERIVATIVES, MEDICAMENTS CONTAINING SAID DERIVATIVES AND USE THEREOF

The invention relates to novel oxindole derivatives of general formula (I), wherein the substituents R, R, A, B, and Y are defined as in Claim . The invention further relates to medicaments containing said derivatives, and use thereof for the prevention and/or treatment of vasopressin-dependent diseases. 766. Compound of general formula (I) according to one of through , wherein the radicals A , B , Y , R , and Rin each case independently have one of the meanings stated in through , and wherein the Rradical is bonded at the 6-position of the oxindole ring structure.1413. Compound of general formula (I) or (I.a) according to one of through claims 1 , wherein the Y radical on the C atom bearing the Rradical has the S configuration claims 1 , and the carbon atom in the 3-position on the oxindol-2-one structure has either the R or the S configuration.1514. Compound of general formula (I) or (I.a) according to one of through claims 1 , wherein the compound is present in the form of the levorotatory stereoisomer with respect to the free base.1615. Compound of general formula (I) or (I.a) according to one of through claims 1 , wherein the compounds have a binding affinity Ki for the vasopressin receptor subtype V1b of less than approximately 100 nM claims 1 , preferably between approximately 10 nM and approximately 100 nM claims 1 , particularly preferably less than or equal to approximately 10 nM.1716. Compound of general formula (I) or (I.a) according to one of through for use as a medicament.1816. Medicament containing at least one compound of general formula (I) or (I.a) according to one of through .1916. Use of at least one compound of general formula (I) or (I.a) according to one of through for the treatment and/or prevention of at least one vasopressin-dependent disease claims 1 , and/or for producing a medicament for the treatment and/or prevention of at least one vasopressin-dependent disease.2016. Use of at least one compound of general formula (I) or (I.a) ...

Substituted oxindole-derivatives and the use thereof for the treatment of vasopressin-dependent illnesses

The present invention relates to novel substituted oxindole derivatives of the formula (I), pharmaceutical agents containing said derivatives, and the use thereof for the treatment of vasopressin-dependent illnesses.

CARBAMATE-SUBSTITUTED OXINDOLE DERIVATIVES AND USE THEREOF FOR THE TREATMENT OF VASOPRESSIN-DEPENDENT DISEASES

The present invention relates to novel carbamate-substituted oxindole derivatives, pharmaceutical compositions comprising them, and their use for the treatment of vasopressin-dependent disorders. 2. A compound as claimed in claim 1 , in which Ris hydrogen or methoxy.3. A compound as claimed in any of the preceding claims claim 1 , in which Ris hydrogen claim 1 , methyl or ethyl.4. A compound as claimed in any of the preceding claims claim 1 , in which Xis N and Xis CH.5. A compound as claimed in any of to claim 1 , in which Xis CH and Xis N.6. A compound as claimed in any of to claim 1 , in which Xis CH and Xis CH.7. A compound as claimed in any of to and claim 1 , in which{'sup': '1', 'Ris methoxy;'}{'sup': '2', 'Ris methoxy;'}{'sup': '3', 'Ris methyl or ethyl;'}{'sup': '1', 'Xis CH; and'}{'sup': '2', 'Xis N.'}8. A compound as claimed in any of to and claim 1 , in which{'sup': '1', 'Ris methoxy;'}{'sup': '2', 'Ris H;'}{'sup': '3', 'Ris methyl or ethyl;'}{'sup': '1', 'Xis CH; and'}{'sup': '2', 'Xis N.'}9. A compound as claimed in any of to and claim 1 , in which{'sup': '1', 'Ris H;'}{'sup': '2', 'Ris methoxy;'}{'sup': '3', 'Ris methyl or ethyl;'}{'sup': '1', 'Xis CH; and'}{'sup': '2', 'Xis N.'}10. A compound as claimed in any of to and claim 1 , in which{'sup': '1', 'Ris H;'}{'sup': '2', 'Ris H;'}{'sup': '3', 'Ris methyl or ethyl;'}{'sup': '1', 'Xis CH; and'}{'sup': '2', 'Xis N.'}11. A compound as claimed in any of to claim 1 , in which{'sup': '1', 'Ris methoxy;'}{'sup': '2', 'Ris methoxy;'}{'sup': '3', 'Ris methyl or ethyl;'}{'sup': '1', 'Xis N; and'}{'sup': '2', 'Xis CH.'}12. A compound as claimed in any of to claim 1 , in which{'sup': '1', 'Ris methoxy;'}{'sup': '2', 'Ris H;'}{'sup': '3', 'Ris methyl or ethyl;'}{'sup': '1', 'Xis N; and'}{'sup': '2', 'Xis CH.'}13. A compound as claimed in any of to claim 1 , in which{'sup': '1', 'Ris H;'}{'sup': '2', 'Ris methoxy;'}{'sup': '3', 'Ris methyl or ethyl;'}{'sup': '1', 'Xis N; and'}{'sup': '2', 'Xis CH.'}{'claim-ref': ...

SUBSTITUTED OXINDOLE DERIVATIVES AND THEIR USE AS VASOPRESSIN RECEPTOR LIGANDS

The present invention relates to novel oxindole derivatives of the general formula (I) to medicaments comprising them and to their use for the prophylaxis and/or treatment of diseases vasopressin dependent. 2. Compounds according to claim 1 , in which R5 is hydrogen or methoxy.3. Compounds according to claim 1 , in which R7 is hydrogen claim 1 , methyl or ethyl.4. Compounds according to any of to claim 1 , in whichR5 is hydrogen or methoxy;R7 is hydrogen, methyl or ethyl;X1 is —NH—;X2 is N; andX3 is CH.5. Compounds according to any of to claim 1 , in whichR5 is hydrogen or methoxy;R7 is hydrogen, methyl or ethyl;X1 is —NH—;X2 is CH; andX3 is N.6. Compounds according to any of to claim 1 , in whichR5 is methoxy;R6 is methoxyR7 is methyl or ethyl;X1 is —NH—;X2 is CH and X3 is NorX2 is N and X3 is CH.7. Compounds according to any of to claim 1 , in whichR5 is methoxy;R6 is methoxy;R7 is methyl;X1 is —NH—;X2 is N; andX3 is CH.8. Compounds according to any of to claim 1 , in whichR5 is methoxy;R6 is methoxy;R7 is methyl;X1 is —NH—;X2 is CH; andX3 is N.9. Compounds according to any of to claim 1 , in whichR5 is methoxy;R6 is methoxy;R7 is ethyl;X1 is —NH—;X2 is CH; andX3 is N.10. Compounds of the general formula (I) according to any of to claim 1 , characterized in that they are present in optically active form and that they are the (laevorotatory) (−)-enantiomer claim 1 , which rotates the plane of polarization of linear polarized light to the left claim 1 , of the compound of the general formula (I) in question in the form of the free base claim 1 , and the pharmaceutically acceptable salts claim 1 , tautomeric forms and/or prodrugs thereof.12. Compounds of the general formula (I) according to in optically active form claim 10 , characterized in that the corresponding laevorotatory (−)-enantiomer is present in an optical purity (enantiomeric excess claim 10 , ee) of greater than 50% claim 10 , and the pharmaceutically acceptable salts claim 10 , tautomeric forms and ...

SUBSTITUTED OXINDOLE DERIVATIVES AND THEIR USE AS VASOPRESSIN RECEPTOR LIGANDS

The present invention relates to novel oxindole derivatives of the general formula (I) to medicaments comprising them and to their use for the prophylaxis and/or treatment of diseases vasopressin dependent. 151.-. (canceled)53. The method according to claim 52 , in which R5 is hydrogen or methoxy.54. The method according to claim 52 , in which R7 is hydrogen claim 52 , methyl or ethyl.55. The method according to claim 52 , in whichR5 is hydrogen or methoxy;R7 is hydrogen, methyl or ethyl;X1 is —NH—;X2 is N; andX3 is CH.56. The method according to claim 52 , in whichR5 is hydrogen or methoxy;R7 is hydrogen, methyl or ethyl;X1 is —NH—;X2 is CH; andX3 is N.57. The method according to claim 52 , in whichR5 is methoxy;R6 is methoxy;R7 is methyl or ethyl;X1 is —NH—; andX2 is CH and X3 is N orX2 is N and X3 is CH.58. The method according to claim 52 , in whichR5 is methoxy;R6 is methoxy;R7 is methyl;X1 is —NH—;X2 is N; andX3 is CH.59. The method according to claim 52 , in whichR5 is methoxy;R6 is methoxy;R7 is methyl;X1 is —NH—;X2 is CH; andX3 is N.60. The method according to claim 52 , in whichR5 is methoxy;R6 is methoxy;R7 is ethyl;X1 is —NH—;X2 is CH; andX3 is N.61. The method according to claim 52 , wherein the compound of the general formula (I) claim 52 , or a pharmaceutically acceptable salt thereof claim 52 , or a tautomeric form thereof claim 52 , is present in optically active form as the (laevorotatory) (−)-enantiomer claim 52 , which rotates the plane of polarization of linear polarized light to the left.63. The method according to claim 61 , characterized in that the corresponding laevorotatory (−)-enantiomer is present in an optical purity (enantiomeric excess claim 61 , ee) of greater than 50% claim 61 , a pharmaceutically acceptable salt thereof claim 61 , or a tautomeric form thereof.64. The method according to claim 62 , characterized in that the enantiomer having the preferred absolute configuration at the C-3 ring carbon atom is present in an optical ...

CARBAMATE-SUBSTITUTED OXINDOLE DERIVATIVES AND USE THEREOF FOR THE TREATMENT OF VASOPRESSIN-DEPENDENT DISEASES

The present invention relates to novel carbamate-substituted oxindole derivatives, pharmaceutical compositions comprising them, and their use for the treatment of vasopressin-dependent disorders. 2. A compound as claimed in claim 1 , in which Ris hydrogen or methoxy.3. A compound as claimed in any of the preceding claims claim 1 , in which Ris hydrogen claim 1 , methyl or ethyl.4. A compound as claimed in any of the preceding claims claim 1 , in which Xis N and Xis CH.5. A compound as claimed in any of to claim 1 , in which Xis CH and Xis N.6. A compound as claimed in any of to claim 1 , in which Xis CH and Xis CH.7. A compound as claimed in any of to and claim 1 , in which{'sup': '1', 'Ris methoxy;'}{'sup': '2', 'Ris methoxy;'}{'sup': '3', 'Ris methyl or ethyl;'}{'sup': '1', 'Xis CH; and'}{'sup': '2', 'Xis N.'}8. A compound as claimed in any of to and claim 1 , in which{'sup': '1', 'Ris methoxy;'}{'sup': '2', 'Ris H;'}{'sup': '3', 'Ris methyl or ethyl;'}{'sup': '1', 'Xis CH; and'}{'sup': '2', 'Xis N.'}9. A compound as claimed in any of to and claim 1 , in which{'sup': '1', 'Ris H;'}{'sup': '2', 'Ris methoxy;'}{'sup': '3', 'Ris methyl or ethyl;'}{'sup': '1', 'Xis CH; and'}{'sup': '2', 'Xis N.'}10. A compound as claimed in any of to and claim 1 , in which{'sup': '1', 'Ris H;'}{'sup': '2', 'Ris H;'}{'sup': '3', 'Ris methyl or ethyl;'}{'sup': '1', 'Xis CH; and'}{'sup': '2', 'Xis N.'}11. A compound as claimed in any of to claim 1 , in which{'sup': '1', 'Ris methoxy;'}{'sup': '2', 'Ris methoxy;'}{'sup': '3', 'Ris methyl or ethyl;'}{'sup': '1', 'Xis N; and'}{'sup': '2', 'Xis CH.'}12. A compound as claimed in any of to claim 1 , in which{'sup': '1', 'Ris methoxy;'}{'sup': '2', 'Ris H;'}{'sup': '3', 'Ris methyl or ethyl;'}{'sup': '1', 'Xis N; and'}{'sup': '2', 'Xis CH.'}13. A compound as claimed in any of to claim 1 , in which{'sup': '1', 'Ris H;'}{'sup': '2', 'Ris methoxy;'}{'sup': '3', 'Ris methyl or ethyl;'}{'sup': '1', 'Xis N; and'}{'sup': '2', 'Xis CH.'}14. A compound ...

Substituted oxindol derivatives, drugs containing said derivatives and the use thereof

The invention relates to novel oxindol derivative of general formula (I), wherein substituents R1, R2, A, B and Y are such as defined in a claim 1. Drugs containing said derivatives and the use thereof for preventing and/or treating vassopress-and/or oxytocin-dependent-diseases are also disclosed.

Poly(9,9'-spirobisfluorenes), their production and their use

Soluble poly(bis-9,9′-fluorenes) comprise identical or different structural repeating units of the formula I, where the two R 1 s are, independently of one another, H, C 1 -C 18 alkyl, C 6 -C 14 aryl, C 7 -C 15 aralkyl, C 1 -C 18 alkoxy, R 2 —(O—C n H 2n ) m —O—, C 1 -C 18 alkylthio, C 1 -C 18 dialkylamino, —C(O)OH, —C(O)O—C 1 -C 18 alkyl, —C(O)—N(C 1 -C 18 alkyl) 2 , —SO 3 H, —SO 3 —C 1 -C 18 alkyl, —SO 2 —N(C 1 -C 18 alkyl) 2 , C 1 -C 17 alkyl-C(O)—O— or C 1 -C 17 alkyl-C(O)—, R 2 is H or C 1 -C 12 alkyl, n is from 2 to 6 and m is from 1 to 12. The polymers can be used either alone or in admixture with at least one additional fluorophore whose absorption band overlaps the emission band (fluorescent emission) of the polymer of the formula I as active radiative layer for light-emitting diodes, VDUs and display elements.

Poly(9,9′-spirobisfluorenes), their production and their use

Soluble poly(bis-9,9′-fluorenes) comprise identical or different structural repeating units of the formula I, where the two R 1 s are, independently of one another, H, C 1 -C 18 alkyl, C 8 -C 14 aryl, C 7 -C 15 aralkyl, C 1 -C 18 alkoxy, R 2 —(O—C n H 2n ) m —O—, C 1 -C 18 alkylthio, C 1 -C 18 dialkylamino, —C(O)OH, —C(O)O—C 1 -C 18 alkyl, —C(O)—N(C 1 -C 18 alkyl) 2 , —SO 3 H, —SO 3 —C 1 -C 18 alkyl, —SO 2 —N(C 1 -C 18 alkyl) 2 , C 1 -C 17 -alkyl-C(O)—O— or C 1 -C 17 alkyl-C(O)—, R 2 is H or C 1 -C 12 alkyl, n is from 2 to 6 m is from 1 to 12. The polymers can be used either alone or in admixture with at least one additional fluorophore whose absorption band overlaps the emission band (fluorescent emission) of the polymer of the formula I as active radiative layer for light-emitting diodes, VDUs and display elements.

Combination therapy with parp inhibitors

The present invention describes benzimidazole derivatives of Formula (I) which constitute potent PARP inhibitors in combination with radiotherapy or in combination with other chemotherapeutic agents.

Substituted naphthacen-5,12-diones and their use.

Heteroaryl-substituted 1,3-dihydroindol-2-one derivatives and medicaments containing them

The present invention relates to novel 1,3-di-hydroindol-2-one (oxindole) derivatives of the formula (I) in which A, R 3, R 4, R 5 R 6 and R 7 are defined according to claim 1, and to medicaments containing them for the treatment of diseases. In particular, the novel oxindole derivaties can be used for the control and/or prophylaxis of various vasopressin-dependent or oxytocin-dependent diseases.

Quinoline compounds suitable for treating disorders that respond to modulation of the serotonin 5-HT6 receptor

Combination therapy with parp inhibitors

Inhibitor PARP-a ili njegova terapijski prihvatljiva so, pri čemu je inhibitor PARP-a 2-[(2R)-2-metilpirolidin-2-il]-1 H-benzimidazol-4-karboksamid, za korišćenje u lečenju raka ili inhibiciji tumorskog rasta kod sisara, pri čemu je maligna bolest tumor CNS-a, i pri čemu bi se navedeni inhibitor PARP-a primenjivao u kombinaciji sa radioterapijom. A PARP inhibitor or a therapeutically acceptable salt thereof, wherein the PARP inhibitor is 2 - [(2R) -2-methylpyrrolidin-2-yl] -1H-benzimidazole-4-carboxamide, for use in the treatment of cancer or the inhibition of tumor growth in a mammal, wherein the malignant disease is a CNS tumor, and wherein said PARP inhibitor would be administered in combination with radiotherapy.

Copolyimides, their preparation and the use thereof

Mixtures of salts of organic dicarboxylic acids and organic compounds of non-salt character, dissolved in a C 1 -C 4 alkanol, can be concentrated or separated with a semipermeable membrane made from a copolyimide which contains a first aromatic diamine radical (1) and a second aromatic diamine radical (2) which carries --SO 3 M groups, wherein M is H⊕, a mono- to trivalent metal cation or an ammonium cation. The first amine radical (1) and/or the second diamine radical (2) contains C 1 -C 4 alkyl groups in both o-positions to at least one amino group. These copolyamides are also radiation-sensitive (self-crosslinking) and can be used for the production of protective layers or relief images, development being carried out in an aqueous alkaline medium.

Carbamate-substituted oxindole derivatives and use thereof for the treatment of vasopressin-dependent diseases

The present invention relates to novel carbamate-substituted oxindole derivatives, pharmaceutical compositions comprising them, and their use for the treatment of vasopressin-dependent disorders.

New carboxylic acid derivatives, their preparation and their use

Carboxylic acid derivatives have the formula (I), in which R to R6, X, Y, and Z have the meanings given in the description. Also disclosed is their preparation. These new compounds are useful for controlling diseases.

Quinoline compounds suitable for treating disorders that respond to modulation of the serotonin 5-ht6 receptor

The present invention relates to novel quinoline compounds. The compounds possess valuable therapeutic properties and are particularly suitable, for treating diseases that respond to modulation of the serotonin 5-HT6 receptor. formula (I) wherein R is a moiety of the formula (R) wherein A, R1 to R4 are as defined in the claims and the specification, n is 0, 1 or 2; m is 0, 1, 2 or 3; Ra, Rb are independently selected from the group consisting of halogen, CN, C1-C4-alkyl, C1-C4-haloalkyl, C1-C4-alkoxy, C1-C4-haloalkoxy, C(O)Raa, C(O)NRccRbb and NRccRbb; X is CH2, C(O), S, S(O) or S(O)2; which is located in the 3- or 4-position of the quinoline ring; Ar is a radical Ar1, Ar2-Ar3 or Ar2-O-Ar3, wherein Ar1, Ar2 and Ar3 are each independently selected from the group consisting of aryl or hetaryl wherein aryl or hetaryl moieties may be unsubstituted or may carry 1, 2, 3 substituents Rx, wherein and physiologically tolerated acid addition salts and the N-oxides thereof.

The use of carboxylic acid derivatives as drugs

The invention concerns the use of carboxylic acid derivatives of formula I (I) in which R means a formyl group, a CO2H group or a residue which can be hydrolysed to form COOH; X means nitrogen or CR14, wherein R14 means hydrogen or, together with R3, forms a 3- to 4-member alkylene or alkenylene chain in each of which a methyl group can be replaced by oxygen; Y means sulphur or oxygen or a single bond; Z means sulphur or oxygen; and the other substituents have the meanings given in the description. These derivatives can be used for preparing medicaments.

Substituted benzimidazolone derivatives, medicaments comprising them and their use for treating vasopressin-dependent disease

The present invention relates to novel benzimidazolone derivatives of the general formula (I) in which the substituents R1, R2, R3, A1, A2, and B are as defined in claim 1, medicaments comprising these, and the use thereof for the prophylaxis and/or treatment of vasopressin-dependent diseases.

Heteroaryl derivatives of 1,3-dihydroindol-2-one derivatives and medicaments containing them

Η παρούσα εφεύρεση αφορά σε νέα παράγωγα 1,3-διυδροϊνδολ-2-όνης (οξινδόλης) του τύπου (I) όπου A, R3, R4, R5, R6 και R7 ορίζονται σύμφωνα προς την αξίωση 1, και σε φάρμακα που περιέχουν αυτά για θεραπεία ασθενειών. Ιδιαιτέρως, τα νέα παράγωγα οξινδολίου μπορεί να χρησιμοποιηθούν για τον έλεγχο ή/και την προφύλαξη διαφόρων εξαρτώμενων από αγγειοπιεσίνη ή εξαρτώμενων από οξυτοκίνη ασθενειών. The present invention relates to novel 1,3-dihydroindol-2-one (oxindole) derivatives of formula (I) wherein A, R3, R4, R5, R6 and R7 are defined according to claim 1, and medicaments containing them for treatment of diseases. In particular, novel oxindole derivatives may be used to control and / or prevent various angiopressin-dependent or oxytocin-dependent diseases.

Substituted oxindole derivative and its use as a vasopressin receptor ligand

Carboxylic acid derivatives, their preparation and use

Carboxylic acid derivatives where R-R 6 , X, Y and Z have the meanings stated in the description, and the preparation thereof, are described. The novel compounds are suitable for controlling diseases.

Substituted oxindole derivatives and their use as vasopressin receptor ligands

The present invention relates to novel oxindole derivatives of the general formula (I) to medicaments comprising them and to their use for the prophylaxis and/or treatment of diseases vasopressin dependent.

Substituted oxindole derivatives, medicaments containing said derivatives and use thereof

The invention relates to novel oxindole derivatives of general formula (I), wherein substituents A, B, X and Y are defined as in Claim I, medicaments containing said derivatives, and the use thereof in the prophylaxis and/or treatment of vasopressin-dependent and/or oxytocin-dependent diseases.

New carboxylic acid derivatives and their use

Heterocyclyl-substd. propanoic acids and their derivs., of formula (I), are new. R = formyl, tetrazolyl, nitrile, COOH or a gp. that can be hydrolysed to COOH; X = N or CR14; R2 = H, OH, NH2, alkylamino, dialkylamino, halo, alkyl, haloalkyl, alkoxy, haloalkoxy or alkylthio; R14 = H or 1-5 C alkyl; R3 = R2 or alkoxyimino; or CR3 + CR14 = 5 or 6 membered alkylene or alkenyl ring (opt. substd. by 1-2 alkyl) in which a methylene can be replaced by O, S, NH or alkylamino; R4, R5 = phenyl or naphthyl (both opt. substd. by one or more halo, NO2, CN, OH, alkyl, haloalkyl, alkoxy, haloalkyloxy, phenoxy, alkylthio, NH2, alkylamine or dialkylamino) or 3-7 C cycloalkyl; or the phenyl or naphthyl gps. are opt. bonded at the O- position (by a bond, CH2, O, S, SO2, ethylene, ethenylene or opt. alkylated amino); R6 = H, 1-8 C alkyl, 2-6 C alkenyl, 3-6 C alkynyl, 3-8 C cycloalkyl (all opt. substd. by 1 or more halo, NO2, CN, alkoxy 3-6 C alkenyloxy, 3-6 C alkynyloxy, alkylthio, haloalkoxy, alkylcarbonyl, alkoxycarbonyl, 3-8 C alkylcarbonylalkyl, alkylamino, dialkylamino, phenyl, Ph or OPh), Ar or Het; Y = S, O or bond; Q = S, O, SO, SO2 or bond; Ph = substd. phenyl, where substits. are halo, NO2, CN, alkyl, haloalkyl, alkoxy, haloalkoxy or alkylthio; Ar = phenyl or naphthyl (both opt. substd. by 1 or more halo, NO2, CN, OH, NH2, alkylamino, dialkylamino or OCH2CH2O); Het = 5 or 6 membered heteroaromatic with 1-3 N atoms and/or one S or O (opt. substd. by 1-4 halo and/or 1 or 2 alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio, phenyl, phenoxy or phenyl carbonyl (where the phenyl is opt. substd. by 1-5 halo and/or 1-3 alkyl, haloalkyl, alkoxy, haloalkoxy and/or alkylthio)); alkyl and alkoxy have 1-4 C unless otherwise stated; provided that R6 is not H when Q = bond.

Combination therapy with parp inhibitors

The present invention describes benzimidazole derivatives of Formula (I) which constitute potent PARP inhibitors in combination with radiotherapy or in combination with other chemotherapeutic agents.

Bicyclic derivatives, their production and use

Substituted oxindole derivatives and their use as vasopressin receptor ligands

The present invention relates to novel oxindole derivatives of the general formula (I) to medicaments comprising them and to their use for the prophylaxis and/or treatment of diseases vasopressin dependent.

NEW CARBOXYLIC ACID DERIVATIVES ITS PREPARATION AND UTILIZATION

Substituted oxindole-derivatives and the use thereof for the treatment of vasopressin-dependent illnesses

Disclosed is a compound of formula (I) as depicted where the substituents are as disclosed in the specification. Examples of compounds of formula (I) are 5-Cyano-1-(2,4-dimethoxypheriylsulfonyl)-3-(2-ethoxypyridin-3-yl)-2-oxo-2,3-dihydro-1H-indol-3-yI 4-(4-methylpiperazin-1-yI)benzoate; N-[5-Cyano-3-(2-ethoxypyridin-3-yl)-1-(4-methoxyphenylsulfonyl)-2-oxo-2, 3-dihydro-1H-indol-3-yl]-4-(4-methylpiperazin-1 -yl)benzamide; N-[5-Cyano-3-(2-ethoxypyridin-3-yl)-1-(4-methoxyphenylsulfonyl)-2-oxo-2, 3-dihydro-1H-indol-3-yl]-4-(4-ethylpiperazin-1-yI)benzamide. Also disclosed is a pharmaceutical composition comprising a compound of formula (I) and the use of a compound of formula (I) in the manufacture of a medicament for treatment and/or prophylaxis of vasopressin-dependent diseases such as diabetes, insulin resistance, nocturnal enuresis, incontinence; hypertension, pulmonary hypertension, heart failure, myocardial infarction, coronary spasm, unstable angina; affective disorders; anxiety disorders and stress-dependent anxiety disorders; impairments and Alzheimer's disease; psychoses and psychotic disorders; Cushing's syndrome and other stress-dependent diseases; sleep disorders; depressive disorders; childhood onset mood disorders; symptoms and/or thermoregulatory dysfunctions; drug or pharmaceutical dependencies and schizophrenia.

Substituted oxindole derivatives, medicaments containing said derivatives and use thereof

The invention relates to novel oxindole derivatives of general formula (I), wherein substituents A, B, X and Y are defined as in Claim I, medicaments containing said derivatives, and the use thereof in the prophylaxis and/or treatment of vasopressin-dependent and/or oxytocin-dependent diseases.

Substituted oxindole derivatives and their use as vasopressin receptor ligands

The present invention relates to novel oxindole derivatives of the general formula (I) to medicaments comprising them and to their use for the prophylaxis and/or treatment of diseases vasopressin dependent.

The use of carboxylic acid derivatives as medicaments

Amidomethyl-substituted oxindole derivatives and the use thereof for the treatment of vasopressin-dependent illnesses

The present invention relates to novel amidomethyl-substituted oxindole derivatives of formula (I), pharmaceutical agents containing same, and the use thereof for the treatment of vasopressin-dependent illnesses. In formula (I), R1 is hydrogen, methoxy or ethoxy; R2 is hydrogen or methoxy; R3 is hydrogen, methyl, ethyl, n-propyl or isopropyl; and X1 and X2 are N or CH, with the proviso that X1 and X2 are not both N at the same time.

The use of carboxylic acid derivatives as drugs

The invention concerns the use of carboxylic acid derivatives of formula I (I) in which R means a formyl group, a CO2H group or a residue which can be hydrolysed to form COOH; X means nitrogen or CR14, wherein R14 means hydrogen or, together with R3, forms a 3- to 4-member alkylene or alkenylene chain in each of which a methyl group can be replaced by oxygen; Y means sulphur or oxygen or a single bond; Z means sulphur or oxygen; and the other substituents have the meanings given in the description. These derivatives can be used for preparing medicaments.

Poly(9,9'-Spirobisfluorenes), their production and their use

Soluble poly(bis-9,9′-fluorenes) comprise identical or different structural repeating units of the formula 1, where the two R 1 s are, independently of one another, H, C 1 -C 18 alkyl, C 8 -C 14 aryl, C 7 -C 15 aralkyl, C 1 -C 18 alkoxy, R 2 —(O—C n H 2n ) m —O—, C 1 -C 18 alkylthio, C 1 -C 18 dialkylamino, —C(O)OH, —C(O)O— C 1 -C 18 alkyl, —C(O)—N(C 1 -C 18 alkyl) 2 , —SO 3 H, —SO 3 —C 1 -C 18 alkyl, —SO 2 N(C 1 -C 18 alkyl) 2 , C 1 -C 17 -alkyl—C(O)—O— or C 1 -C 17 alkyl—C(O)—, R 2 is H or C 1 -C 12 alkyl, n is from 2 to 6 and m is from 1 to 12 . The polymers can be used either alone or in admixture with at least one additional fluorophore whose absorption band overlaps the emission band (fluorescent emission) of the polymer of the formula I as active radiative layer for light-emitting diodes, VDUs and display elements.

Substituted oxindole-derivatives and the use thereof for the treatment of vasopressin-dependent illnesses

Substituted oxindole derivatives, medicinal products containing them, and use thereof

The invention relates to novel oxindole derivatives of general formula (I), in which the substituents R1, R2, A, B and Y are defined as per claim 1, to medicaments containing said derivatives and to their use for the prophylaxis and/or treatment of vasopressin-dependent and/or oxytocin-dependent diseases.

Sulfated vinylphenol polymers, compositions containing sulfated vinylphenol polymers and the use thereof

Polymers containing, based on the polymer, from 5 to 100 mol% of identical or different structural units of the formula I <IMAGE> and from 0 to 95 mol% of identical or different structural units of the formula II -Z- (II), in which n is 0 or the number 1 or 2, R1 is H or methyl, M<(+)> is H<(+)>, an alkali metal cation or an ammonium cation, X is C1-C4-alkyl, C1-C4-alkoxy, Cl or Br, and Z is the radical of an olefin monomer other than (I). The polymers can be used as polyanions in electroconductive compositions with polycations comprising anilines or heteroaromatic compounds, for example pyrrole, which can be used as fillers for plastics or as electrodes.

Poly(9,9'-spiro-bisfluorenes), the production and use of same

Hetaryl-substituted guanidine compounds and use thereof as binding partners for 5-HT5-receptors

The invention relates to the hetaryl-substituted guanidine compounds of general formula (I), enantiomeres, diastereomeres and/or tautomeres thereof, in addition to the pharmaceutically acceptable salts thereof and the prodrugs of the known compounds. The invention also relates to the use of said hetaryl-substituted guanidine compounds as binding partners for 5-HT5-receptors for treating and/or for the prophylaxis of illnesses which are modulated by a 5-HT5-receptor activity, in particular, for treating and/or for the prophylaxis of neurodegenerative and neuropsychiatric disorders, and signs, symptoms and dysfunctions associated with said disorders.

5,6-disubstituted oxindole-derivatives and use thereof for treating vasopressine-dependent diseases

The invention relates to novel 5,6-disubstituted oxindole derivatives of formula (I) (see formula I) to pharmaceutical agents containing said components and to the use thereof for producing a medicament. In formula (I), R1 and R2 are independently of one another hydrogen, C1-C3-alkyl, C1-C3-fluoroalkyl, C1-C3-alkoxy, C1-C3-fluoroalkoxy, halogen or CN; R3 is hydrogen or C1-C4-alkyl; R4 is ethoxy, fluorinated ethoxy or isopropoxy; R5 is hydrogen or methyl; R6 is Br, Cl, F or CN; R7 is Cl, F or CN; R8 and R9 are independently of one another C1-C3-alkyl or C1-C3-fluoroalkyl; X1 is O, NH or CH2; X2 and X3 are N or CH, with the proviso that X2 and X3 are not simultaneously N; X4 is N or CH; a and b are independently of one another 0, 1 or 2; and m, n, o and p are independently of one another 1, 2 or 3.

METHOD FOR PRODUCING POLY (HETEROAROMATS) AND FILM-SHAPED PRODUCTS OBTAINED BY THIS METHOD

New oxindole derivatives useful for treating vasopressin- or oxytocin-dependent diseases

Oxindole derivatives (I) are new. Oxindole derivatives of formula (I) are new. A : optionally substituted 6-10C aryl; B' : an optionally substituted 6-10C monocyclic or fused bicyclic aromatic or partially aromatic group; R 1>, R 2>H, halo, ACN, CN, 1-6C haloalkyl, 1-6C haloalkoxy, NO 2, AORx1, ORx1, OAAr, OAr, AAr, R, R', OR', 1-4C alkylthio, ANRx2Rx3, NRx2Rx3, ACORx1, CORx1, SO 2Rx1, ACOORx1, COORx1, OACOORx1, ASRx1, SRx1, AAr', Ar', AOCORx1, OCORx1, ASO 2NRx2Rx3, ACONRx2Rx3, CONRx2Rx2, AOCONRx2Rx3, ASORx1, ASO 2Rx1, NHCOOAr, NHCOOAAr or NHCOOAr; or R 1>, R 2>= H or heteroaryl optionally substituted with Rx1; A : 1-4C alkylene; R : 1-6C alkyl; R' : 2-6C alkenyl or alkynyl; Ar : 6-10C aryl or heteroaryl; Ar' : 3-7C cycloalkyl, 3-7C heterocycloalkyl or 3-7C heterocycloalkenyl; Rx1 : H, R, R', (1-4C)alkoxy(1-5C)alkyl, ANHR, ANRR, ACOR,, Ar, AAr, Ar', AAr'; Rx2, Rx3 : Rx1, SO 2Rx1, COORx1, CONRx1Rx1 or CORx1, or Rx2+Rx3 forms a ring; Y : -Ry-Z-; Ry : -NRy1-(CRy2Ry3) n-N((CRy4Ry5) mRy6)-; Ry1-Ry6 : H, 1-6C alkyl or 3-7C cycloalkyl, or pairs of Ry1-Ry6 can form rings; n : 1-3; m : 0-3; Z : optionally substituted 5- or 6-membered heterocyclyl or heteroaryl. [Image] ACTIVITY : Urotropic; Hemostatic; Anticoagulant; Hypotensive; Cardiant; Vasotropic; Nephrotropic; Antiinflammatory; Hepatotropic; Antiulcer; Antiemetic; Antidepressant; Tranquilizer; Nootropic; Neuroprotective; Neuroleptic. MECHANISM OF ACTION : Vasopressin V1b receptor antagonist. 5-Chloro-1-(2,4-dimethoxyphenylsulfonyl)-3-(2-methoxyphenyl)-3-(4-(4-pyridyl)-1-piperazinyl)-1,3-dihydro-2-indolinone had an affinity constant of less than 50 nM for human V1b receptor.

Substituted benzimidazolone derivatives, medicaments comprising them and their use

The present invention relates to novel benzimidazolone derivatives of the general formula (I) in which the substituents R 1 , R 2 , R 3 , A 1 , A 2 , and B are as defined in claim 1 , medicaments comprising these, and the use thereof for the prophylaxis and/or treatment of vasopressin-dependent diseases.

New substituted oxindole derivatives are vasopressin receptor binders useful to treat e.g. diabetes insipidus, enuresis nocturna, incontinence, hypertonia, heart failure, myocardial infarction, coronary spasm and renal disorders

Substituted oxindole derivatives (I) and their tautomers, enantiomers, diastereomers, prodrugs and salts, are new. Substituted oxindole derivatives of formula (I) and their tautomers, enantiomers, diastereomers, prodrugs and salts, are new. A : (hetero)aromatic or partially-(hetero)aromatic 2-10C mono- or bicyclic ring comprising 0-4 N atoms or 0-2 of O-atoms and 0-2 of S-atoms and substituted with R a 1> and with 1-3 residues of R a 1> 1>, R a 1> 2> or R a 1> 3>; R a 1> 1>, R a 1> 2>, R a 1> 3>H, Cl, Br, I, F, CN, CF 3, OCF 3, OCNF 2, CO-NH 2, CO-NH (1-4C alkyl), CO-N-(1-4C alkyl) (1-4C alkyl), NH 2, NH (1-4C alkyl), N(1-4C alkyl)(1-4C alkyl), NHCHO, NH-CO-NH 2, NH-CO (1-4C alkyl), NO 2, OH, O-1-4C alkyl, O-(0-4C alkylene)-phenyl, phenyl, 1-6C alkyl, 1-6C haloalkyl, 2-6C alkenyl or 2-6C alkynyl; R a 1>R a 2>-(1-4C alkylene)-R a 4>; R a 2>(0-4C-alkylene)-O, (0-4C alkylene)-NR a 5>, (0-4C alkylene)-S, (0-4C-alkylene)-SO, (0-4C-alkylene)-SO 2, (0-4C-alkylene)-CO, (0-4C-alkylene)-NR a 5>-CO, (0-4C-alkylene)-CO-NR a 5>, (0-4C-alkylene)-CO-O, (0-4C-alkylene)-NR a 5>-SO 2, (0-4C alkylene)-SO 2-NR a 5>, (0-4C-alkylene)-NR a 5>-CO-NR a 6>, (0-4C-alkylene)-O-CO-NR a 5>, (0-4C-alkylene)-NR a 5>-CO-O or single bond; R a 4>NH 2, NH(1-4C-alkyl), N(1-4C-alkyl)(1-4C-alkyl), NH(1-4C-alkylene-O-1-4C-alkyl), N(1-4C-alkyl) (1-4C-alkylene-O-1-4C-alkyl), NH-CHO, N(1-4C-alkyl)-CHO, NH-CO-NH 2, N(1-4C alkyl)-CO-NH 2, NH-CO-1-4C-alkyl, N(1-4C-alkyl)-CO-1-4C-alkyl, NH-SO 2-1-4C-alkyl, N(1-4C-alkyl)-SO 2-1-4C-alkyl or ring R a 8>; R a 5>, R a 6>, R a 9>H, 1-4C-alkyl or 1-4C-haloalkyl; R a 8>e.g. -azetidine, -pyrrolidine, -piperidine, -morpholine or -thiomorpholine; B 1>2-10C (hetero)aromatic or partially-(hetero)aromatic mono- or bicyclic ring comprising 0-4 N atoms, 0-2 O atoms and/or 0-2 S atoms and 1-3 residues of R b 1>, R b 2> or R b 3>; R b 1>-R b 3>F, CN, CF 3, OCF 3, OCHF ...

OXINDOL DERIVATIVES REPLACED, MEDICINES THAT UNDERSTAND AND USE THEMSELVES

Nuevos derivados de ixindol de la formula general (I) medicamentos que los comprenden, y su uso para la profilaxis y/o el tratamiento de enfermedades. New derivatives of ixindole of the general formula (I) medicines that comprise them, and their use for the prophylaxis and / or treatment of diseases.

Sheet-like heating elements and preparation thereof

Sheet-like heating elements thereof Abstract A sheet-like heating element using an electrically conductive polymer complex consisting of a) a polycation of polyheteroaromatic compound; and b) a polyanion of thermoplastic polymer, containing a sulfated alcohol group in the repeating structural unit, having film-forming properties.

5,6-disubstituted oxindole-derivatives and use thereof for treating vasopressine-dependent diseases

The invention relates to novel 5,6-disubstituted oxindole derivatives, to pharmaceutical agents containing said components and to the use thereof for producing a medicament.

Quinoline compounds suitable for treating disorders that respond to modulation of the serotonin 5-ht6 receptor

The present invention relates to novel quinoline compounds of the formula (I) and to the salts thereof. The compounds possess valuable therapeutic properties and are particularly suitable, for treating diseases that respond to modulation of the serotonin 5-HT6 receptor. In formula (I) R is a moiety of the formula (R) wherein * indicates the binding site to the quinolinyl radical and wherein A, B, X', Y, Q, R1, R2, R3, R4, R5, m, n, p, q, Ra, Rb, X and Ar are as defined in claim 1.

REPLACED OXINDOL DERIVATIVES AND THEIR USE AS VASOPRESSIN RECEIVER LINKS

Quinoline compounds suitable for treating disorders that respond to modulation of the serotonin 5-ht6 receptor

The present invention relates to novel quinoline compounds. The compounds possess valuable therapeutic properties and are particularly suitable, for treating diseases that respond to modulation of the serotonin 5-HT6 receptor. formula (I) wherein R is a moiety of the formula (R) wherein A, R1 to R4 are as defined in the claims and the specification, n is 0, 1 or 2; m is 0, 1, 2 or 3; Ra, Rb are independently selected from the group consisting of halogen, CN, C1-C4-alkyl, C1-C4-haloalkyl, C1-C4-alkoxy, C1-C4-haloalkoxy, C(O)Raa, C(O)NRccRbb and NRccRbb; X is CH2, C(O), S, S(O) or S(O)2; which is located in the 3- or 4-position of the quinoline ring; Ar is a radical Ar1, Ar2-Ar3 or Ar2-O-Ar3, wherein Ar1, Ar2 and Ar3 are each independently selected from the group consisting of aryl or hetaryl wherein aryl or hetaryl moieties may be unsubstituted or may carry 1, 2, 3 substituents Rx, wherein and physiologically tolerated acid addition salts and the N-oxides thereof.

Surface relief microstructures, related devices and method of making them

The present invention relates to a method for the replication of a patterned surface relief microstructure, comprising the steps of generation of a first layer with a patterned surface relief microstructure, generation of a master, by copying the microstructure of the first layer into a second layer, thereby involving at least one dry or wet etching step, characterized by an additional step, in which the microstructure of the master is brought into contact with a replica material, such that the microstructure of the master is reproduced in the replica. The invention further relates to the elements made as a replica according to the method. The surface relief microstructures are suitable to display images with a positive- negative and/or color image flip. The elements according to the invention are particularly useful for securing documents and articles against counterfeiting and falsification.

Carboxylic acid derivatives, their preparation and use

Carboxylic acid derivatives where R–R 6 , X, Y and Z have the meanings stated in the description, and the preparation thereof, are described. The novel compounds are suitable for controlling diseases.

Dibenzodiazepine derivates, their preparation and use

The invention relates to compounds of the formula (I) and their tautomeric forms, possible enantiomeric and diastereomeric forms and their prodrugs, an d to their preparation and use, where A, B, R1 and X1 have the meanings given in the description.

New carboxylic acid derivatives, their production and use

Substituted oxindole derivatives and medicaments containing the same

The present invention relates to novel oxindole derivatives of the general formula (I), wherein the substitutes A, B, R 1 , R 2 and R 3 are as defined in Claim 1 , and medicaments containing the same for the prophylaxis and/or treatment of vasopressin-dependent or oxytocin-dependent diseases.

New carboxylic acid derivatives, their preparation and their use

Carboxylic acid derivatives have the formula (I), in which R to R6, X, Y, and Z have the meanings given in the description. Also disclosed is their preparation. These new compounds are useful for controlling diseases.

Substituted oxindole derivatives, medicaments containing the latter and use thereof.

La invencion se refiere a derivados de oxindol novedosos de formula general (I), en la que los sustituyentes R1, R2, R3, Y1, Y2, m, n, W, X, B y Z se definen como se establece en la reivindicacion 1, a medicamentos que comprenden dichos derivados y al uso de estos mismos para la profilaxis y/o tratamiento de enfermedades dependientes de vasopresina y/o dependientes de oxitocina. (ver formula (I)).

5-ring heteroaromatic compounds and their use as binding partners for 5-ht5 receptors

The invention relates to 5-ring heteroaromatic compounds of general formula (I), their use for treating and/or preventing diseases, and to medicaments containing them.

Pyrimidine or triazine carboxylic acid derivatives for use as medicaments

Solid electrolytic capacitors and process for producing the same

A solid electrolytic capacitor having a solid electrolyte layer, which layer comprises an electrically conductive thermoplastic organic polymer complex having an electric conductivity of 0.1 Scm -1 or more and a glass transition temperature of -100 to 150°C formed on a valve metal foil through a dielectric film. A small and larege-capacity solid electrolytic capacitor having excellent highfrequency characteristic and long-term stability is provided.

Guanidine compounds, and use thereof as binding partners for 5-ht5 receptors

The invention relates to guanidine compounds of general formula (I), corresponding enantiomeric, diastereomeric, and/or tautomeric forms thereof, and pharmaceutically acceptable salts thereof. The invention further relates to the use of guanidine compounds as binding partners for 5-HT5 receptors in order to treat diseases modulated by 5-HT5 receptor activity, especially treat neurodegenerative and neuropsychiatric disorders and the signs, symptoms, and malfunctions associated therewith.

Substituted oxindole-derivatives and the use thereof for the treatment of vasopressin-dependent illnesses

The present invention relates to novel substituted oxindole derivatives of the formula (l) (see formula I) in which X1, X2, X3, X4, A, R1, R2, R3, R4, R5, R6, R7, R8,R9, a, m, and n are as defined in the specification. The present invention also relates to pharmaceutical agents containing said derivatives, and the use thereof for the treatment of vasopressin-dependent illnesses.

Carboxylic acid derivatives, their preparation and use

Carboxylic acid derivatives where R-R 6 , X, Y and Z have the meanings stated in the description, and the preparation thereof, are described. The novel compounds are suitable for controlling diseases.

Heteroaryl-substituted 1,3-dihydroindol-2-one derivatives and medicaments containing them 13--2-

Substituted oxindole derivative and its use as a vasopressin receptor modulator

The present invention relates to novel oxindole derivatives of the formula (I) to medicaments comprising them and to their use for the prophylaxis and/or treatment of diseases vasopressin dependent.

Quinoline compounds suitable for treating disorders that respond to modulation of the serotonin 5-HT6 receptor

Solid electrolytic capacitors and process for producing the same

Solid electrolytic capacitors and process for producing the same Abstract A solid electrolytic capacitor having a solid electrolyte layer, which layer comprises an electrically conductive thermoplastic organic polymer complex having an electricconductivity of 0.1 Scm-1 or more and a glass transition temperature of -100 to 150°C formed on a valve metal foil through a dielectric film. A small and larege-capacity solid electrolytic capacitor having excellent highfrequency characteristic and long-term stability is provided.

Substituted oxindole derivatives, medicaments containing the latter and use thereof

The invention relates to novel oxindole derivatives of general formula (I), in which the substituents R1, R2, R3, Y1, Y2, m, n, W, X, B and Z are defined as cited in claim 1, to medicaments containing said derivatives and to the use of the latter for the prophylaxis and/or treatment of vasopressin-dependent and/or oxytocin-dependent diseases.

Guanidine compounds, and use thereof as binding partners for 5-ht5 receptors

The invention relates to guanidine compounds of general formula (I), corresponding enantiomeric, diastereomeric, and/or tautomeric forms thereof, and pharmaceutically acceptable salts thereof. The invention further relates to the use of guanidine compounds as binding partners for 5-HT5 receptors in order to treat diseases modulated by 5-HT5 receptor activity, especially treat neurodegenerative and neuropsychiatric disorders and the signs, symptoms, and malfunctions associated therewith.

Quinoline compounds suitable for treating disorders that respond to modulation of the serotonin-5-HT6 receptor

The present invention relates to novel quinoline compounds of the formula (I) and to the salts thereof. The compounds possess valuable therapeutic properties and are particularly suitable, for treating diseases that respond to modulation of the serotonin 5-HT 6 receptor. In formula (I) R is a moiety of the formula (R) wherein * indicates the binding site to the quinolinyl radical and wherein A, B, X′, Y, Q, R 1 , R 2 , R 3 , R 4 , R 5 , m, n, p, q, R a , R b , X and Ar are as defined in claim 1.

5,6-disubstituted oxindole-derivatives and use thereof for treating vasopressine-dependent diseases.

La presente invención se refiere a derivados novedosos de oxindol 5,6-disubstituidos, a agentes farmacéuticos que contienen dichos componentes y al uso de los mismos para la producción de un medicamento.

Substituted oxindole derivatives and medicaments containing the same

The present invention relates to novel oxindole derivatives of the general formula (I), (see formula I) wherein the substitutes A, B, R1, R2 and R3 are as defined in Claim 1, and medicaments containing the same for the prophylaxis and / or treatment of vasopressin-dependent or oxytocin-dependent diseases.

5-halogen-substituted oxindole derivatives and use thereof for treating vasopressine-dependent diseases

Quinoline compounds suitable for treating disorders that respond to modulation of the serotonin 5-ht6 receptor

Heteroaryl-substituted 1,3-dihydroindol-2-one derivatives and medicaments containing the derivatives

【課題】新規な１，３−ジヒドロインドール−２−オン（オキシインドール）誘導体、および、様々な疾患を処置するための、これらを含有する医薬品の提供。 【解決手段】式（Ｉ）の新規なオキシインドール誘導体は、様々なバソプレッシン依存性疾患またはオキシトシン依存性疾患の抑制および／または予防のために使用。 【選択図】なし

Substituted bisacyloxynaphthacenes

Compounds of the formula I ##STR1## in which R 1 to R 8 independently of one another are H and at least one of R 1 to R 8 is a substituent belonging to the group --F, --Si(C 1 -C 4 alkyl) 3 or --COOR 10 ; or each pair of adjacent radicals of R 1 to R 8 is --CO--O--CO--; or at least one of R 1 to R 8 is C 1 -C 20 alkyl--(X) p --, C 2 -C 20 alkenyl--(X) p --, C 2 -C 20 -alkynyl--(X) p --, C 3 -C 8 cycloalkyl--(X) p --, (C 1 -C 12 alkyl--C 3 -C 8 cycloalkyl--(X) p --, C 3 -C 8 -cycloalkyl--CH 2 --(X) p --, C 1 -C 12 alkyl--C 3 -C 8 cycloalkyl--CH 2 --(X) p --, C 6 -C 10 aryl--X--, C 7 -C 20 alkaryl--X--, C 7 -C 12 aralkyl--(X) p -- or C 8 -C 20 --alkaralkyl--(X) p -- or --Y--(C m H 2m --O)-- n R 10 each of which is unsubstituted or substituted by --F, --OH, --CN, C 1 -C 12 alkoxy, C 1 -C 12 acyloxy or --COOR 10 ; R 10 is H or C 1 -C 18 alkyl, X is --O--, --S--, --SO-- or --SO 2 -- and Y is --O-- or --S--, and p is 0 or 1, m is a number from 2 to 6 and n is a number from 2 to 20; and R 9 is C 1 -C 4 acyl which is unsubstituted or substituted by --F. The compounds are intermediates for the preparation of 5,6,11,12-tetrathiotetracenes which form electrically conducting charge-transfer complexes with electron donors.

Combination therapy with parp inhibitors

The present invention describes benzimidazole derivatives of Formula (I) which constitute potent PARP inhibitors in combination with radiotherapy or in combination with other chemotherapeutic agents.

Benzenesulfonanilide compounds suitable for treating disorders that respond to modulation of the serotonin 5-ht6 receptor

Disclosed are benzenesulfonanilide compounds of formulae I and I' and physiologically tolerated acid addition salts and the N-oxides thereof, wherein the substituents are as described with the specification. An example of a compound of formulae I and I' includes 3-Difluoromethoxy-N-(4-methoxy-3-piperazin-1-yl-phenyI)-benzenesulfonamide. Further disclosed is pharmaceutical composition comprising a compound of formula I or I', and the use of a compound of formulae I or I' for preparing a pharmaceutical composition for the treatment of a medical disorder selected from diseases of the central nervous system, addiction diseases or obesity.

Quinoline compounds suitable for treating disorders that respond to modulation of the serotonin 5-ht6 receptor

The present invention relates to novel quinoline compounds. The compounds possess valuable therapeutic properties and are particularly suitable, for treating diseases that respond to modulation of the serotonin 5-HT 6 receptor. wherein R is a moiety of the formula wherein A, R 1 to R 4 are as defined in the claims and the specification, n is 0, 1 or 2; m is 0, 1, 2 or 3; R a , R b are independently selected from the group consisting of halogen, CN, C 1 -C 4 -alkyl, C 1 -C 4 -haloalkyl, C 1 -C 4 -alkoxy, C 1 -C 4 -haloalkoxy, C(O)R aa , C(O)NR cc R bb and NR cc R bb ; X is CH 2 , C(O), S, S(O) or S(O) 2 ; which is located in the 3- or 4-position of the quinoline ring; Ar is a radical Ar 1 , Ar 2 —Ar 3 or Ar 2 —O—Ar 3 , wherein Ar 1 , Ar 2 and Ar 3 are each independently selected from the group consisting of aryl or hetaryl wherein aryl or hetaryl moieties may be unsubstituted or may carry 1, 2, 3 substituents R x , wherein and physiologically tolerated acid addition salts and the N-oxides thereof.

Novel carboxylic acid derivatives, their preparation and use

Carboxylic acid derivatives where R—R 6 , X, Y and Z have the meanings stated in the description, and the preparation thereof, are described. The novel compounds are suitable for controlling diseases.

Hetaryl-substituted guanidine compounds and use thereof as binding partners for 5-ht5-receptors

Die vorliegende Erfindung betrifft Hetaryl-substituierte Guanidinverbindungen der allgemeinen Formel (I), die enantiomeren, diastereomeren und/oder tautomeren Formen davon sowie die pharmazeutisch annehmbaren Salze davon sowie die Prodrugs der genannten Verbindungen. Weiterhin betrifft die vorliegende Verbindung die Verwendung von Hetaryl-substituierten Guanidinverbindungen als Bindungspartner für 5-HT5-Rezeptoren zur Behandlung und/oder Prophylaxe von Krankheiten, die durch eine 5-HT5-Rezeptoraktivität moduliert werden, insbesondere zur Behandlung und/oder Prophylaxe von neurodegenerativen und neuropsychiatrischen Störungen sowie den damit zusammenhängenden Anzeichen, Symptomen und Fehlfunktionen.