Aminotetraline and aminoindane derivatives, pharmaceutical compositions containing them, and their use in therapy

The present invention relates to aminotetraline and aminoindane derivatives of the formula (I) 119.-. (canceled)22. The method of claim 20 , wherein Ris C-C-alkyl claim 20 , C-C-cycloalkyl-C-C-alkyl claim 20 , or C-C-cycloalkyl.23. The method of claim 20 , wherein W is a bond and Ais a bond.24. The method of claim 20 , wherein Q is —S(O)— and Y is —NR—.25. The method of claim 20 , wherein at least one of n1 and n2 is 1 claim 20 , 2 claim 20 , or 3 and the sum of n1+n2 is 2 claim 20 , 3 claim 20 , or 4.26. The method of claim 20 , wherein Xis >N— claim 20 , n1 is 1 claim 20 , and n2 is 1; or Xis >CH— claim 20 , n1 is 1 claim 20 , and n2 is 1.27. The method of claim 20 , wherein Ris hydrogen claim 20 , C-C-alkyl claim 20 , or two radicals Rtogether with the carbon atom to which they are attached form a carbonyl group.29. The method of claim 20 , wherein Ris hydrogen or halogen.30. The method of claim 20 , wherein Ris hydrogen or C-C-alkyl.31. The method of claim 20 , wherein Yis a bond.32. The method of claim 20 , wherein Ris hydrogen claim 20 , C-C-alkyl claim 20 , optionally substituted C-C-cycloalkyl claim 20 , C-C-cycloalkyl-C-C-alkyl claim 20 , or M-M-heterocyclyl and Ris hydrogen or C-C-alkyl; or wherein R claim 20 , Rtogether are optionally substituted C-C-alkylene claim 20 , wherein one —CH— of C-C-alkylene may be replaced by an oxygen atom.33. The method of claim 20 , wherein Xis >CRR claim 20 , Xis a bond claim 20 , and Ris hydrogen or C-C-alkyl and Ris hydrogen or C-C-alkyl.35. The method of claim 20 , wherein m is 1.36. The method of claim 20 , whereinA is a benzene ring;{'sup': '1', 'sub': 1', '6', '3', '12', '1', '4', '3', '12, 'Ris C-C-alkyl, C-C-cycloalkyl-C-C-alkyl, or optionally substituted M-Mheterocyclyl;'}W is a bond;{'sup': '1', 'Ais a bond;'}{'sub': '2', 'Q is —S(O)—;'}{'sup': '8', 'Y is —NR—;'}n1 is 1 or 2;n2 is 1 or 2;{'sup': 6', '6, 'sub': 1', '6, 'Ris hydrogen, C-C-alkyl, or two radicals Rtogether with the carbon atom to which they are ...

Pyrrolidine derivatives, pharmaceutical compositions containing them, and their use in therapy

The present invention relates to pyrrolidine derivatives of the formula (I), or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such pyrrolidine derivatives, and the use of such pyrrolidine derivatives for therapeutic purposes. The pyrrolidine derivatives are GlyT1 inhibitors.

Pyrrolidine derivatives, pharmaceutical compositions containing them, and their use in therapy

The present invention relates to pyrrolidine derivatives of the formula (I), or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such pyrrolidine derivatives, and the use of such pyrrolidine derivatives for therapeutic purposes. The pyrrolidine derivatives are GlyT1 inhibitors.

Carboxamide compounds and their use as calpain inhibitors v

The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. The carboxamide compounds are compounds of the general formula (I) in which R1, R2, R3 R4, X, m and n have the meanings mentioned in the claims and the description, the tautomers thereof, the hydrates thereof and the pharmaceutically suitable salts thereof. Of these compounds those are preferred wherein R1 is optionally substituted benzyl or hetaryl-methyl, X is a single bond or an oxygen atom, R2 is C1-C4- alkyl, C1-C4-haloalkyl, C2-C4-alkenyl, C3-C6-cycloalkyl, C3-C6-cycloalkyl-C1-C2-alkyl, C3-C6-heterocycloalkyl-C1-C2-alkyl, phenyl, phenyl-C1-C3-alkyl, pyridin-2-yl-C1-C3-alkyl or CH2-C(O)OCH3,R3 and R4 independently of one another are halogen ...

Carboxamide compounds and their use as calpain inhibitors

The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. The carboxamide compounds are compounds of the general formula I in which R1, R2, R3 R4, R5, m and n have the meanings mentioned in the claims and the description, the tautomers thereof, the hydrates thereof and the pharmaceutically suitable salts thereof. Of these compounds those are preferred wherein R1 is optionally substituted phenyl-C1-C2-alkyl or hetaryl-C1-C2-alkyl, R2 is optionally substituted aryl, hetaryl, aryl-C1-C6-alkyl, aryl-C2-C6-alkenyl or hetaryl-C1-C4-alkyl, R3 is C1-C3-alkyl, C1-C3-haloalkyl, C2-C4-alkenyl, C3-C6-cycloalkyl, C3-C6-cycloalkyl-C1-C2-alkyl, or phenyl-C1-C3-alkyl, R4 and R5 independently of one another are halogen ...

Aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives, pharmaceutical compositions containing them, and their use in therapy

The present invention relates to aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives of the formula (I) 119.-. (canceled)22. The method of claim 20 , wherein Ris C-C-alkyl claim 20 , C-C-cycloakyl-C-C-alkyl claim 20 , or C-C-cycloalkyl.23. The method of claim 20 , wherein W is a bond and Ais a bond.24. The method of claim 20 , wherein Q is —S(O)—.25. The method of claim 20 , wherein at least one of n1 and n2 is 1 claim 20 , 2 claim 20 , or 3 and the sum of n1+n2 is 2 claim 20 , 3 claim 20 , or 4.26. The method of claim 20 , wherein Xis >N— claim 20 , n1 is 1 claim 20 , and n2 is 1; or Xis >CH— claim 20 , n1 is 1 claim 20 , and n2 is 1.27. The method of claim 20 , wherein Ris hydrogen or C-C-alkyl claim 20 , or two radicals Rtogether with the carbon atom to which they are attached form a carbonyl group.29. The method of claim 20 , wherein Ris hydrogen or halogen.30. The method of claim 20 , wherein Ais —O—.31. The method of claim 20 , wherein Ris hydrogen or C-C-alkyl.32. The method of claim 20 , wherein Yis a bond.33. The method of claim 20 , wherein Ris hydrogen claim 20 , C-C-alkyl claim 20 , optionally substituted C-C-cycloalkyl claim 20 , C-C-cycloalkyl-C-C-alkyl claim 20 , or M-M-heterocyclyl and Ris hydrogen or C-C-alkyl; or wherein R claim 20 , Rtogether are optionally substituted C-C-alkylene claim 20 , wherein one —CH— of C-C-alkylene may be replaced by an oxygen atom.34. The method of claim 20 , wherein Xis >RR claim 20 , Xis a bond claim 20 , and Ris hydrogen or C-C-alkyl and Ris hydrogen or C-C-alkyl.36. The method of claim 20 , whereinA is a benzene ring;{'sup': '1', 'sub': 1', '6', '3', '12', '1', '4', '3', '12, 'Ris C-C-alkyl, C-C-cycloakyl-C-C-alkyl, or an optionally substituted M-M-heterocyclyl;'}W is a bond;{'sup': '1', 'Ais a bond;'}{'sub': '2', 'Q is —S(O)—;'}{'sup': '8', 'Y is —NR—;'}n1 is 1;n2 is 1;{'sup': '6', 'Ris hydrogen;'}{'sup': '1', 'Xis →N— or >CH—;'}{'sup': '2', 'Ris hydrogen or halogen;'}{'sup': '2', ' ...

Carbidopa and L-dopa prodrugs and methods of use

The present disclosure relates to (a) carbidopa prodrugs, (b) pharmaceutical combinations and compositions comprising a carbidopa prodrug and/or an L-dopa prodrug, and (c) methods of treating Parkinson's disease and associated conditions comprising administering a carbidopa prodrug and an L-dopa prodrug to a subject with Parkinson's disease.

Aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives, pharmaceutical compositions containing them, and their use in therapy

The present invention relates to aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives, and the use of such aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives for therapeutic purposes. The aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives are GlyT1 inhibitors.

4,5-dihydropyrazole derivatives, pharmaceutical compositions containing them, and their use in therapy

The present invention relates to 4,5-dihydropyrazole derivatives of the formula (I) and physiologically tolerated salts thereof which are GlyT1 inhibitors. The invention further relates to pharmaceutical compositions comprising such 4,5-dihydropyrazole derivatives, and the use of such 4,5-dihydropyrazole derivatives for therapeutic purposes.

Aminotetraline and aminoindane derivatives, pharmaceutical compositions containing them, and their use in therapy

The present invention relates to aminotetraline and aminoindane derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminotetraline and aminoindane derivatives, and the use of such aminotetraline and aminoindane derivatives for therapeutic purposes. The aminotetraline and aminoindane derivatives are GlyT1 inhibitors.

Carboxamide compounds and their use as calpain inhibitors iv

The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. The carboxamide compounds are compounds of the general formula I in which R1, R2, R3 R4, R5,, m and n have the meanings mentioned in the claims and the description, the tautomers thereof, the hydrates thereof and the pharmaceutically suitable salts thereof. Of these compounds those are preferred wherein R1 is optionally substituted phenyl-C1-C2-alkyl or hetaryl-C1-C2-alkyl, R2 is optionally substituted aryl, hetaryl, aryl-C1-C6-alkyl, aryl-C2-C6-alkenyl or hetaryl-C1-C4-alkyl, R3 is C3-C4-alkyl, C1-C4-haloalkyl, C2-C4-alkenyl, C3-C6-cycloalkyl, C3-C6-cycloalkyl-C1-C2-alkyl, C3-C6- heterocycloalkyl-C1-C2-alkyl, phenyl-C1-C3-alkyl, pyridin-2- ...

N-PHENYL-(PIPERAZINYL OR HOMOPIPERAZINYL)-BENZENESULFONAMIDE OR BENZENESULFONYL-PHENYL-(PIPERAZINE OR HOMOPIPERAZINE) COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE SEROTONIN 5-HT6 RECEPTOR

The present invention relates to N-phenyl-(piperazinyl or homopiperazinyl)-benzenesulfonamide or benzenesulfonyl-phenyl-(piperazine or homopiperazine) compounds, pharmaceutical compositions containing them, and their use in therapy. The compounds possess valuable therapeutic properties and are particularly suitable for treating diseases that respond to modulation of the serotonin 5-HTreceptor. 2. The compound as claimed in claim 1 , wherein Ris hydrogen claim 1 , fluorine claim 1 , C-Calkyl claim 1 , fluorinated C-Calkyl claim 1 , C-Calkoxy or fluorinated C-Calkoxy3. The compound of claim 1 , where Ris hydrogen.4. The compound of claim 1 , wherein Ris hydrogen.5. The compound of claim 1 , wherein Ris methyl.6. The compound of claim 1 , wherein X is a group N—R.7. The compound of claim 1 , wherein n is 1.8. The compound of claim 1 , wherein Ris methyl or methoxy.9. The compound of claim 1 , wherein Ris hydrogen or fluorine.10. The compound of claim 1 , wherein Ris hydrogen claim 1 , C-Calkyl or cyclopropylmethyl.11. The compound of claim 1 , wherein Ris hydrogen.12. The compound of claim 1 , wherein Ris hydrogen.13. The compound of claim 1 , wherein Ris methyl claim 1 , methoxy or difluoromethoxy.14. The compound of claim 1 , wherein Ris chlorine or fluorine.15. The compound of claim 1 , wherein Ris hydrogen.16. The compound of claim 1 , wherein Rand Rare hydrogen claim 1 , Ris selected from the group consisting of C-Calkyl and CCalkoxy claim 1 , and Ris selected from the group consisting of hydrogen claim 1 , C-Calkyl claim 1 , or cyclopropylmethyl.17. The compound of claim 1 , wherein{'sup': '4', 'X is a bond or a group N—R;'}{'sup': '1', 'Ris hydrogen or methyl;'}{'sup': '2', 'Ris hydrogen;'}{'sup': '3', 'sub': 1', '2', '1', '2, 'Ris hydrogen, C-Calkyl, C-Calkoxy;'}{'sup': '4', 'Ris hydrogen, methyl, ethyl, n-propyl, isopropyl or cyclopropylmethyl;'}{'sup': '5', 'Ris hydrogen, methyl or methoxy;'}{'sup': '6', 'Ris hydrogen; and'}n is 1 or 2.18. The compound of ...

N-PHENYL-(PIPERAZINYL OR HOMOPIPERAZINYL)-BENZENESULFONAMIDE OR BENZENESULFONYL-PHENYL-(PIPERAZINE OR HOMOPIPERAZINE) COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE SEROTONIN 5-HT6 RECEPTOR

The present invention relates to N-phenyl-(piperazinyl or homopiperazinyl)-benzenesulfonamide or benzenesulfonyl-phenyl-(piperazine or homopiperazine) compounds, pharmaceutical compositions containing them, and their use in therapy. The compounds possess valuable therapeutic properties and are particularly suitable for treating diseases that respond to modulation of the serotonin 5-HTreceptor. 130-. (canceled)32. The method of claim 31 , wherein the addictive disease is caused by the abuse of a psychotropic substance.33. The method of claim 32 , wherein the psychotropic substance is a sedative claim 32 , an anxiolytic claim 32 , a hypnotic claim 32 , or a narcotic.34. The method of claim 32 , wherein the psychotropic substance is an opioid claim 32 , cocaine claim 32 , nicotine claim 32 , alcohol claim 32 , a substance which interacts with the GABA chloride channel complex claim 32 , a sedative claim 32 , a hypnotic claim 32 , a tranquilizer claim 32 , lysergic acid diethylamide claim 32 , a cannabinoid claim 32 , a psychomotor stimulant claim 32 , an amphetamine or amphetamine-like substance claim 32 , or caffeine.35. The method of claim 31 , wherein the addictive disease is an addiction to gaming.36. The method of claim 31 , wherein the addictive disease is an addiction to gambling claim 31 , a computer or video game addiction claim 31 , or an internet addiction.37. The method of claim 31 , wherein X is a group N—R.38. The method of claim 31 , wherein n is 1.39. The method of claim 31 , wherein Ris methyl or methoxy.40. The method of claim 31 , wherein Ris hydrogen.41. The method of claim 31 , wherein Ris methyl claim 31 , methoxy or difluoromethoxy.42. The method of claim 31 , wherein Ris hydrogen.43. The method of claim 31 , wherein{'sup': '4', 'X is a bond or a group N—R;'}{'sup': '1', 'Ris hydrogen or methyl;'}{'sup': '2', 'Ris hydrogen;'}{'sup': '3', 'sub': 1', '2', '1', '2, 'Ris hydrogen, C-Calkyl, or C-Calkoxy;'}{'sup': '4', 'Ris hydrogen, methyl, ethyl, n- ...

CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS V

The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. The carboxamide compounds are compounds of the general formula (I) in which R, R, R, R, X, m and n have the meanings mentioned in the claims and the description, the tautomers thereof, the hydrates thereof and the pharmaceutically suitable salts thereof. Of these compounds those are preferred wherein Ris optionally substituted benzyl or hetaryl-methyl, X is a single bond or an oxygen atom, Ris C-C-alkyl, C-C-haloalkyl, C-C-alkenyl, C-C-cycloalkyl, C-C-cycloalkyl-C-C-alkyl, C-C-heterocycloalkyl-C-C-alkyl, phenyl, phenyl-C-C-alkyl, pyridin-2-yl-C-C-alkyl or CH—C(O)OCH, Rand Rindependently of one another are halogen, CN, CF, CHF, CHF, C-C-alkyl or C-C-alkoxy, and m and n independently of one another are 0 or 1. 2. The carboxamide compound as claimed in claim 1 , in which X is oxygen.3. The carboxamide compound as claimed in claim 1 , in which X indicates a single bond.4. The carboxamide compound as claimed in claim 1 , in which Ris selected from C-C-alkyl claim 1 , C-C-haloalkyl claim 1 , C-C-alkenyl claim 1 , C-C-alkynyl claim 1 , C-C-cycloalkyl claim 1 , C-C-cycloalkyl-C-C-alkyl claim 1 , C-C-heterocycloalkyl-C-C-alkyl claim 1 , (C-C-alkylene)-COOR claim 1 , C-C-alkoxy-C-C-alkyl claim 1 , phenyl claim 1 , phenyl-C-C-alkyl claim 1 , hetaryl and hetaryl-C-C-alkyl claim 1 , where phenyl and hetaryl in the last four mentioned radicals is unsubstituted or carries 1 claim 1 , 2 or 3 substituents Rand where Rand Rare as defined in .5. The carboxamide compound as claimed in claim 4 , in which Ris selected from C-C-alkyl claim 4 , C-C-alkenyl claim 4 , C-C-alkynyl claim 4 , C-C-cycloalkyl claim 4 , C-C-cycloalkyl-methyl claim 4 , ...

CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS V

The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. The carboxamide compounds are compounds of the general formula (I) in which R, Rand n have the meanings mentioned in the claims and the description, Y is a radical of the formulae (Y1) or (Y2) where # indicates the point of attachment of Y to the pyridine ring, R, R, R, Rand m have the meanings mentioned in the claims and the description, A is (CH)with p being 1, 2, 3 or 4, where one or two hydrogen atoms may be replaced by a radical R, where A is attached to the 3- or 4-position of the pyrazole radical and Rhas the meaning mentioned in the claims and the description; Ais (CH)q with q being 0, 1, 2 or 3, where one or two hydrogen atoms may be replaced by halogen or C-C-alkyl; and Ais (CH)r with r being 0, 1, 2 or 3, where one or two hydrogen atoms may be replaced by halogen or C-C-alkyl, provided that that r+q is 2, 3, 4, 5 or 6; their tautomers, the hydrates thereof, the pharmaceutically suitable salts of the carbox-amide compounds (I), the prodrugs of (I) and the pharmaceutically suitable salts of the prodrugs, tautomers or hydrates of (I). 2. The carboxamide compound of claim 1 , wherein Ris selected from the group consisting of:{'sub': 1', '10, 'sup': '1a', 'C-C-alkyl, which may be partly or completely halogenated and/or have 1, 2 or 3 substituents selected from R, and'}{'sub': 3', '7, 'sup': 1b', '1c, 'C-C-cycloalkyl-methyl, where the cycloalkyl moiety may have 1, 2, 3 or 4 radicals selected from the group consisting of R, benzyl, and hetaryl-methyl, where phenyl and hetaryl in the last 2 radicals mentioned may be unsubstituted or carry 1, 2, 3 or 4 identical or different radicals selected from R.'}3. The ...

4,5- dihydropyrazole derivatives, pharmaceutical compositions containing them, and their use in therapy

The present invention relates to 4,5-dihydropyrazole derivatives of the formula (I) and physiologically tolerated salts thereof which are GlyT1 inhibitors. The invention further relates to pharmaceutical compositions comprising such 4,5-dihydropyrazole derivatives, and the use of such 4,5-dihydropyrazole derivatives for therapeutic purposes.

Carbidopa and L-Dopa Prodrugs and Methods of use

The present disclosure relates to (a) carbidopa prodrugs, (b) pharmaceutical combinations and compositions comprising a carbidopa prodrug and/or an L-dopa prodrug, and (c) methods of treating Parkinson's disease and associated conditions comprising administering a carbidopa prodrug and an L-dopa prodrug to a subject with Parkinson's disease. 130-. (canceled)32. A method of treating Parkinson's disease comprising administering to a subject in need thereof a therapeutically effective amount of the pharmaceutical composition according to .33. The method of claim 32 , further comprising administering another anti-Parkinson's agent to the subject.34. A kit comprising the pharmaceutical composition of . The present disclosure relates to (a) carbidopa prodrugs, (b) L-dopa prodrugs, (c) pharmaceutical combinations and compositions comprising a carbidopa prodrug and/or an L-dopa prodrug, and (d) methods of treating Parkinson's disease and associated conditions comprising administering a carbidopa prodrug and an L-dopa prodrug to a subject with Parkinson's disease.Parkinson's disease is a chronic and progressive neurodegenerative condition characterized by reduced levels in the brain of the neurotransmitter dopamine (i.e., 3,4-dihydroxyphenethylamine). Administration of L-dopa (i.e., L-3,4-dihydroxyphenylalanine) currently is the most effective therapy for treating a patient with Parkinson's disease. L-dopa, which unlike dopamine can cross the blood-brain barrier, is enzymatically converted in the brain to dopamine resulting in an increase in dopamine levels:The conversion of L-dopa to dopamine is catalyzed by aromatic L-amino acid decarboxylase, a ubiquitous enzyme that promotes central as well as peripheral metabolism of L-dopa to dopamine. Due to the peripheral metabolism of L-dopa, a relatively large dose of L-dopa is required to achieve therapeutically effective dopamine levels in the brain. Administration of such large L-dopa doses results in elevated peripheral ...

CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS IV

The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. 2. The carboxamide compound of claim 1 , in which m is 0 or 1 and claim 1 , when m=1 claim 1 , Ris selected from F claim 1 , Cl claim 1 , CN claim 1 , CF claim 1 , C-C-alkyl and C-C-alkoxy.3. The carboxamide compound of claim 1 , in which n is 0 or 1 and claim 1 , when n=1 claim 1 , Ris selected from F claim 1 , Cl claim 1 , CN claim 1 , CF claim 1 , C-C-alkyl and C-C-alkoxy.4. The carboxamide compound of claim 1 , in which Ris selected from C-C-alkyl claim 1 , C-C-haloalkyl claim 1 , C-C-alkenyl claim 1 , C-C-alkynyl claim 1 , C-C-cycloalkyl claim 1 , C-C-cycloalkyl-C-C-alkyl claim 1 , C-C-heterocycloalkyl-C-C-alkyl claim 1 , (C-C-alkylene)-COOR claim 1 , C-C-alkoxy-C-C-alkyl claim 1 , aryl claim 1 , aryl-C-C-alkyl claim 1 , hetaryl and hetaryl-C-C-alkyl claim 1 , where aryl and heteraly in the last four mentioned radicals is unsubstituted or carries 1 claim 1 , 2 or 3 substituents Rand where Rand Rare as defined in .5. The carboxamide compound of claim 4 , in which Ris selected from C-C-alkyl claim 4 , C-C-alkenyl claim 4 , C-C-cycloalkyl claim 4 , C-C-cycloalkyl-methyl claim 4 , morpholin-4-yl-C-C-alkyl claim 4 , (C-C-alkylene)-COO—C-C-alkyl claim 4 , phenyl-C-C-alkyl claim 4 , pyridinyl-C-C-alkyl claim 4 , thiazol-2-yl claim 4 , thiazol-2-yl-C-C-alkyl claim 4 , benzo[b]imidazol-2-yl-C-C-alkyl claim 4 , oxazol-2-yl-C-C-alkyl and benzoxazolyl-C-C-alkyl.6. The carboxamide compound of claim 5 , in which Ris selected from propyl claim 5 , butyl claim 5 , propenyl claim 5 , cyclopropyl claim 5 , cyclobutyl claim 5 , cyclopropyl-methyl claim 5 , morpholin-4-yl-propyl claim 5 , benzyl claim 5 , phenyl-ethyl claim 5 , ...

Carbidopa and L-Dopa Prodrugs and Methods of Use

The present disclosure relates to (a) carbidopa prodrugs, (b) pharmaceutical combinations and compositions comprising a carbidopa prodrug and/or an L-dopa prodrug, and (c) methods of treating Parkinson's disease and associated conditions comprising administering a carbidopa prodrug and an L-dopa prodrug to a subject with Parkinson's disease. 2. The pharmaceutical combination of claim 1 , wherein the first compound or pharmaceutically acceptable salt thereof claim 1 , and the second compound or pharmaceutically acceptable salt thereof are present in separate pharmaceutical compositions.3. The pharmaceutical combination of claim 1 , wherein the first compound or pharmaceutically acceptable salt thereof claim 1 , and the second compound or pharmaceutically acceptable salt thereof are present in a same pharmaceutical composition.9. The pharmaceutical combination of claim 1 , wherein a weight ratio of the first compound or pharmaceutically acceptable salt thereof to the second compound or pharmaceutically acceptable salt thereof is from about 1:4 to about 1:10.10. The pharmaceutical combination of claim 1 , wherein the combination is an aqueous combination suitable for intragastric claim 1 , subcutaneous claim 1 , intramuscular claim 1 , intrajejunum claim 1 , oral claim 1 , intranasal or intravenous administration.11. The pharmaceutical combination of claim 1 , wherein the combination is an aqueous combination suitable for subcutaneous administration.12. The pharmaceutical combination of claim 1 , wherein the first compound or pharmaceutically acceptable salt thereof has a solubility of at least about 200 mg/ml in aqueous solution at about neutral pH claim 1 , and the second compound or pharmaceutically acceptable salt thereof has a solubility of at least about 400 mg/ml in aqueous solution at about neutral pH.14. The compound or pharmaceutically acceptable salt of claim 13 , wherein Rand Rare each independently selected from the group consisting of hydrogen claim 13 , ...

Aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives, pharmaceutical compositions containing them, and their use in therapy

The present invention relates to aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives of the formula (I) or a physiologically tolerated salt thereof The invention relates to pharmaceutical compositions comprising such aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives, and the use of such aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquin oline derivatives for therapeutic purposes. The aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives are GlyT1 inhibitors.

Aminotetraline and aminoindane derivatives, pharmaceutical compositions containing them, and their use in therapy

The present invention relates to aminotetraline and aminoindane derivatives of the formula (I) 3. Compound as claimed in claim 1 , wherein Ris C-C-alkyl claim 1 , C-C-cycloalkyl-C-C-alkyl claim 1 , or C-C-cycloalkyl.4. Compound as claimed in claim 1 , wherein W is a bond and Ais a bond.5. Compound as claimed in claim 1 , wherein Q is —S(O)— and Y is —NR—.6. Compound as claimed in claim 1 , wherein at least one of n1 and n2 is 1 claim 1 , 2 claim 1 , or 3 and the sum of n1+n2 is 2 claim 1 , 3 claim 1 , or 4.7. Compound as claimed in claim 1 , wherein Xis >N— claim 1 , n1 is 1 claim 1 , and n2 is 1; or Xis >CH— claim 1 , n1 is 1 claim 1 , and n2 is 1.8. Compound as claimed in claim 1 , wherein Ris hydrogen claim 1 , C-C-alkyl claim 1 , or two radicals Rtogether with the carbon atom to which they are attached form a carbonyl group.10. Compound as claimed in claim 1 , wherein Ris hydrogen or halogen.11. Compound as claimed in claim 1 , wherein Ris hydrogen or C-C-alkyl.12. Compound as claimed in claim 1 , wherein Yis a bond.13. Compound as claimed in claim 1 , wherein Ris hydrogen claim 1 , C-C-alkyl claim 1 , optionally substituted C-C-cycloalkyl claim 1 , C-C-cycloalkyl-C-C-alkyl claim 1 , or M-M-heterocyclyl and Ris hydrogen or C-C-alkyl; or wherein R claim 1 , Rtogether are optionally substituted C-C-alkylene claim 1 , wherein one —CH— of C-C-alkylene may be replaced by an oxygen atom.14. Compound as claimed in claim 1 , wherein Xis >CRR claim 1 , Xis a bond claim 1 , and Ris hydrogen or C-C-alkyl and Ris hydrogen or C-C-alkyl.16. Compound as claimed in claim 1 , wherein m is 1.17. Compound as claimed in claim 1 , whereinA is a benzene ring;{'sup': '1', 'sub': 1', '6', '3', '12', '1', '4', '3', '12, 'Rwhere is C-C-alkyl, C-C-cycloalkyl-C-C-alkyl, or optionally substituted M-Mheterocyclyl;'}W is a bond;{'sup': '1', 'Ais a bond'}{'sub': '2', 'Q is —S(O)—;'}{'sup': '8', 'Y is —NR—;'}n1 is 1 or 2;n2 is 1 or 2;{'sup': 6', '6, 'sub': 1', '6, 'Ris hydrogen, C-C-alkyl, or ...

PYRROLIDINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM, AND THEIR USE IN THERAPY

The present invention relates to pyrrolidine derivatives of the formula (I), 2. The compound as claimed in claim 1 , wherein Ris optionally substituted 1 claim 1 ,3-diazolyl.3. The compound as claimed in claim 1 , wherein Ris optionally substituted 1 claim 1 ,2 claim 1 ,3-triazolyl.4. The compound as claimed in claims 1 , wherein Ris hydrogen claims 1 , halogen or C-C-alkyl claims 1 , and Ris hydrogen.5. The compound as claimed in claim 1 , wherein Ris C-C-aryl optionally substituted with 1 claim 1 , 2 claim 1 , or 3 substituents independently selected from the group consisting of halogen claim 1 , C-C-alkyl and C-C-alkoxy.6. The compound as claimed in claim 1 , wherein Ris C-C-heterocyclyl optionally substituted with 1 claim 1 , 2 claim 1 , or 3 substituents independently selected from the group consisting of halogen claim 1 , C-C-alkyl and C-C-cycloalkyl.7. The compound as claimed in claim 1 , wherein Ris hydrogen.8. The compound as claimed in claim 1 , wherein Yis >CR— and Ris hydrogen claim 1 , methyl claim 1 , benzyl claim 1 , hydroxy-methyl claim 1 , or hydroxy.9. The compound as claimed in claims 1 , wherein Ris hydrogen claims 1 , halogen or C-C-alkyl claims 1 , and Ris hydrogen.12. The compound as claimed in claim 11 , wherein{'sup': '1', 'Ris an optionally substituted 5-membered heterocyclic ring containing at least 1 N atom and optionally 1 or 2 further heteroatoms selected from N, O and S;'}{'sup': 2a', '2b, 'claim-text': 'are hydrogen;', 'R, R'}{'sup': '3a', 'sub': 3', '12', '6', '12', '1', '6', '3', '12', '1', '4', '2', '6', '6', '12', '1', '4', '6', '12', '3', '12, 'Ris C-C-cycloalkyl, optionally substituted C-C-aryl, hydroxy, C-C-alkoxy, C-C-cycloalkyl-C-C-alkoxy, C-C-alkenyloxy, C-C-aryl-C-C-alkoxy, optionally substituted C-C-aryloxy, or optionally substituted C-C-heterocyclyl;'}{'sup': '3b', 'Ris hydrogen or hydroxy;'}{'sup': 1', '6, 'Yis >CR;'}{'sup': '6', 'sub': 1', '6', '1', '6, 'Ris hydrogen, C-C-alkyl, or hydroxy-C-C-alkyl'}{'sup': '8a', 'sub ...

Pyrrolidine derivatives, pharmaceutical compositions containing them, and their use in therapy

The present invention relates to pyrrolidine derivatives of the formula (I), or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such pyrrolidine derivatives, and the use of such pyrrolidine derivatives for therapeutic purposes. The pyrrolidine derivatives are GlyT1 inhibitors.

CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS V

The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. 2. The carboxamide compound of claim 1 , in which m is 0 or 1 and claim 1 , when m=1 claim 1 , Ris selected from F claim 1 , Cl claim 1 , CN claim 1 , CF claim 1 , C-C-alkyl and C-C-alkoxy.3. The carboxamide compound of claim 1 , in which n is 0 or 1 and claim 1 , when n=1 claim 1 , Ris selected from F claim 1 , Cl claim 1 , CN claim 1 , CF claim 1 , C-C-alkyl and C-C-alkoxy.4. The carboxamide compound of claim 1 , in which Ris selected from C-C-alkyl claim 1 , C-C-haloalkyl claim 1 , C-C-alkenyl claim 1 , C-C-alkynyl claim 1 , C-C-cycloalkyl claim 1 , C-C-cycloalkyl-C-C-alkyl claim 1 , C-C-heterocycloalkyl-C-C-alkyl claim 1 , C-C-alkoxy-C-C-alkyl claim 1 , aryl and aryl-C-C-alkyl.5. The carboxamide compound of claim 4 , in which Ris selected from methyl claim 4 , ethyl claim 4 , n-propyl claim 4 , isopropyl claim 4 , propenyl claim 4 , but-2-enyl claim 4 , but-3-enyl claim 4 , propinyl claim 4 , cyclopropyl claim 4 , cyclobutyl claim 4 , cyclopentyl claim 4 , cyclopropyl-methyl and 2-(morpholin-4-yl)ethyl.6. The carboxamide compound of claim 4 , in which Ris selected from C-C-alkyl claim 4 , C-C-haloalkyl claim 4 , C-C-alkenyl claim 4 , C-C-alkynyl claim 4 , C-C-cycloalkyl claim 4 , C-C-alkoxy-C-C-alkyl claim 4 , aryl and aryl-C-C-alkyl.7. The carboxamide compound of claim 6 , in which Ris selected from methyl claim 6 , ethyl claim 6 , propenyl claim 6 , but-2-enyl claim 6 , but-3-enyl claim 6 , propinyl claim 6 , cyclopropanyl claim 6 , cyclopropanyl-methyl claim 6 , phenyl and benzyl.8. The carboxamide compound of claim 1 , in which Ris selected from C-C-alkyl which may be partly or completely halogenated and/or have ...

Carbidopa prodrugs

The present disclosure relates to (a) carbidopa prodrugs, (b) pharmaceutical combinations and compositions comprising a carbidopa prodrug and/or an L-dopa prodrug, and (c) methods of treating Parkinson's disease and associated conditions comprising administering a carbidopa prodrug and an L-dopa prodrug to a subject with Parkinson's disease.

Aminotetraline and aminoindane derivatives, pharmaceutical compositions containing them, and their use in therapy

The present invention relates to aminotetraline and aminoindane derivatives of the formula (I) 3. Compound as claimed in claim 1 , wherein Ris C-C-alkyl claim 1 , C-C-cycloalkyl-C-C-alkyl claim 1 , or C-C-cycloalkyl.4. Compound as claimed in claim 1 , wherein W is a bond and Ais a bond.5. Compound as claimed in claim 1 , wherein Q is —S(O)— and Y is —NR—.6. Compound as claimed in claim 1 , wherein at least one of n1 and n2 is 1 claim 1 ,2 claim 1 , or 3 and the sum of n1+n2 is 2 claim 1 ,3 claim 1 , or 4.7. Compound as claimed in claim 1 , wherein Xis >N— claim 1 , n1 is 1 claim 1 , and n2 is 1; or Xis >CH— claim 1 , n1 is 1 claim 1 , and n2 is 1.8. Compound as claimed in claim 1 , wherein Ris hydrogen claim 1 , C-C-alkyl claim 1 , or two radicals Rtogether with the carbon atom to which they are attached form a carbonyl group.10. Compound as claimed in claim 1 , wherein Ris hydrogen or halogen.11. Compound as claimed in claim 1 , wherein Ris hydrogen or C-C-alkyl.12. Compound as claimed in claim 1 , wherein Yis a bond.13. Compound as claimed in claim 1 , wherein Ris hydrogen claim 1 , C-C-alkyl claim 1 , optionally substituted C-C-cycloalkyl claim 1 , C-C-cycloalkyl-C-C-alkyl claim 1 , or M-M-heterocyclyl and Ris hydrogen or C-C-alkyl; or wherein R claim 1 , Rtogether are optionally substituted C-C-alkylene claim 1 , wherein one —CH— of C-C-alkylene may be replaced by an oxygen atom.14. Compound as claimed in claim 1 , wherein Xis >CRR claim 1 , Xis a bond claim 1 , and Ris hydrogen or C-C-alkyl and Ris hydrogen or C-C-alkyl.16. Compound as claimed in claim 1 , wherein m is 1.17. Compound as claimed in claim 1 , whereinA is a benzene ring;{'sup': '1', 'sub': 1', '6', '3', '12', '1', '4', '3', '12, 'Ris C-C-alkyl, C-C-cycloalkyl-C-C-alkyl, or optionally substituted M-Mheterocyclyl;'}W is a bond;{'sup': '1', 'Ais a bond;'}{'sub': '2', 'Q is —S(O)—;'}{'sup': '8', 'Y is —NR—;'}n1 is 1 or 2;n2 is 1 or 2;{'sup': 6', '6, 'sub': 1', '6, 'Ris hydrogen, C-C-alkyl, or two ...

Aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives, pharmaceutical compositions containing them, and their use in therapy

The present invention relates to aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives of the formula (I) 3. Compound as claimed in claim 1 , wherein Ris C-C-alkyl claim 1 , C-C-cycloalkyl-C-C-alkyl claim 1 , or C-C-cycloalkyl.4. Compound as claimed in claim 1 , wherein W is a bond and Ais a bond.5. Compound as claimed in claim 1 , wherein Q is —S(O)—.6. Compound as claimed in claim 1 , wherein at least one of n1 and n2 is 1 claim 1 , 2 claim 1 , or 3 and the sum of n1+n2 is 2 claim 1 , 3 claim 1 , or 4.7. Compound as claimed in claim 1 , wherein Xis >N— claim 1 , n1 is 1 claim 1 , and n2 is 1; or Xis >CH— claim 1 , n1 is 1 claim 1 , and n2 is 1.8. Compound as claimed in claim 1 , wherein Ris hydrogen or C-C-alkyl claim 1 , or two radicals Rtogether with the carbon atom to which they are attached form a carbonyl group.10. Compound as claimed in claim 1 , wherein Ris hydrogen or halogen.11. Compound as claimed in claim 1 , wherein Ais —O—.12. Compound as claimed in claim 1 , wherein Ris hydrogen or C-C-alkyl.13. Compound as claimed in claim 1 , wherein Yis a bond.14. Compound as claimed in claim 1 , wherein Ris hydrogen claim 1 , C-C-alkyl claim 1 , optionally substituted C-C-cycloalkyl claim 1 , C-C-cycloalkyl-C-C-alkyl claim 1 , or M-M-heterocyclyl and Ris hydrogen or C-C-alkyl; or wherein R claim 1 , Rtogether are optionally substituted C-C-alkylene claim 1 , wherein one —CH— of C-C-alkylene may be replaced by an oxygen atom.15. Compound as claimed in wherein Xis >CRR claim 1 , Xis a bond claim 1 , and Ris hydrogen or C-C-alkyl and Ris hydrogen or C-C-alkyl.17. Compound as claimed in claim 1 , whereinA is a benzene ring;{'sup': '1', 'sub': 1', '6', '3', '12', '1', '4', '3', '12, 'Ris C-C-alkyl, C-C-cycloalkyl-C-C-alkyl, or an optionally substituted M-M-heterocyclyl;'}W is a bond;{'sup': '1', 'Ais a bond;'}{'sub': '2', 'Q is —S(O)—;'}{'sup': '8', 'Y is —NR—;'}n1 is 1;n2 is 1;{'sup': '6', 'Ris hydrogen;'}{'sup': '1', 'Xis ->N— or >CH ...

Carbidopa And L-Dopa Prodrugs And Methods Of Use

The present disclosure relates to (a) carbidopa prodrugs, (b) pharmaceutical combinations and compositions comprising a carbidopa prodrug and/or an L-dopa prodrug, and (c) methods of treating Parkinson's disease and associated conditions comprising administering a carbidopa prodrug and an L-dopa prodrug to a subject with Parkinson's disease. 130-. (canceled)31. A crystalline polymorph of L-dopa 4′-monophosphate identified by powder X-ray diffraction wherein the crystalline polymorph is:crystalline L-dopa 4′-monophosphate anhydrate (i) demonstrating at least one characteristic peak in the powder X-ray diffraction pattern at values of two theta of 10.261±0.20, 12.053±0.20, 13.759±0.20, 14.932±0.20, 16.147±0.20, 16.718±0.20, 17.34±0.20, 19.254±0.20, 20.654±0.20, 22.078±0.20, 23.599±0.20, 24.198±0.20, 25.898±0.20, 26.338±0.20, and 27.117±0.20; orcrystalline L-dopa 4′-monophosphate anhydrate (ii) demonstrating at least one characteristic peak in the powder X-ray diffraction pattern at values of two theta of 8.468±0.20, 10.234±0.20, 11.821±0.20, 13.084±0.20, 13.503±0.20, 15.48±0.20, 15.848±0.20, 16.513±0.20, 18.447±0.20, 19.346±0.20, 20.239±0.20, 21.139±0.20, 24.221±0.20, 24.865±0.20, 25.647±0.20.32. A crystalline L-dopa 3′-monophosphate demonstrating at least one characteristic peak in the powder X-ray diffraction pattern at values of two theta of 8.662±0.20 , 11.286±0.20 , 15.079±0.20 , 15.678±0.20 , 16.786±0.20 , 17.288±0.20 , 18.438±0.20 , 19.682±0.20 , 20.946±0.20 , 22.188±0.20 , 22.671±0.20 , 23.088±0.20 , 24.144±0.20 , 24.744±0.20 , and 25.383±0.20.33. A crystalline L-dopa 3′4-diphosphate trihydrate demonstrating at least one characteristic peak in the powder X-ray diffraction pattern at values of two theta of 7.118±0.20 , 10.342±0.20 , 11.355±0.20 , 12.161±0.20 , 14.201±0.20 , 17.36±0.20 , 17.632±0.20 , 19.196±0.20 , 19.444±0.20 , 20.83±0.20 , 21.504±0.20 , 22.491±0.20 , 23.085±0.20 , 24.487±0.20 , and 25.11±0.20.34. A crystalline polymorph of carbidopa 4′- ...

Carbidopa Prodrug

The present disclosure relates to (a) carbidopa prodrugs, (b) pharmaceutical combinations and compositions comprising a carbidopa prodrug and/or an L-dopa prodrug, and (c) methods of treating Parkinson's disease and associated conditions comprising administering a carbidopa prodrug and an L-dopa prodrug to a subject with Parkinson's disease. 130-. (canceled) The present disclosure relates to (a) carbidopa prodrugs, (b) L-dopa prodrugs, (c) pharmaceutical combinations and compositions comprising a carbidopa prodrug and/or an L-dopa prodrug, and (d) methods of treating Parkinson's disease and associated conditions comprising administering a carbidopa prodrug and an L-dopa prodrug to a subject with Parkinson's disease.Parkinson's disease is a chronic and progressive neurodegenerative condition characterized by reduced levels in the brain of the neurotransmitter dopamine (i.e., 3,4-dihydroxyphenethylamine). Administration of L-dopa (i.e., L-3,4-dihydroxyphenylalanine) currently is the most effective therapy for treating a patient with Parkinson's disease. L-dopa, which unlike dopamine can cross the blood-brain barrier, is enzymatically converted in the brain to dopamine resulting in an increase in dopamine levels:The conversion of L-dopa to dopamine is catalyzed by aromatic L-amino acid decarboxylase, a ubiquitous enzyme that promotes central as well as peripheral metabolism of L-dopa to dopamine. Due to the peripheral metabolism of L-dopa, a relatively large dose of L-dopa is required to achieve therapeutically effective dopamine levels in the brain. Administration of such large L-dopa doses results in elevated peripheral dopamine levels that can cause nausea in some patients. To overcome these problems, L-dopa generally is co-administered with a peripheral aromatic L-amino acid decarboxylase inhibitor such as carbidopa (i.e., (2S)-3-(3,4-dihydroxyphenyl)-2-hydrazino-2-methylpropanoic acid):Co-administration of carbidopa with L-dopa inhibits the peripheral metabolism ...

Carbidopa and l-dopa prodrugs and method of use thereof

【課題】パーキンソン病および関連状態の治療するための組成物の提供。【解決手段】式（I-a)等のカルビドパプロドラッグと式（II-a)等のＬ−ドーパプロドラッグを含む医薬組み合わせ及び組成物。【選択図】なし

Aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives, pharmaceutical compositions containing them, and their use in therapy

The present invention relates to aminochromane, aminothiochromane and amino-1,2,3,4- tetrahydroquinoline derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminochromane, aminothio-chromane and amino-1,2,3,4-tetrahydroquinoline derivatives, and the use of such aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives for therapeutic purposes. The aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives are GlyT1 inhibitors.

carboxamide compounds and their use as calpain inhibitors

compostos de carboxamida e seu uso como inibidores de calpaína. a presente invenção refere-se a novos compostos de carboxamida e seu uso para a fabricação de um medicamento. os compostos de carboxamida são inibidores de calpaína (proteases de cisteína dependentes de cálcio). a invenção, portanto, também se refere á utilização destes compostos de carboxamida para o tratamento de um distúrbio associado a uma elevada atividade de calpaína. os compostos de carboxamida são compostoes da fórmula geral i em que r^ 1^, r^ 2^, r^ 3^, r^ 4^, r^ 5^, m e n tem os significados mencionados nas reivindicações e a descrição, os tautômeros do mesmos, os hidratos dos mesmos e os sais farmaceuticamente aceitáveis dos mesmos. destes compostos, são preferidos aqueles em que r^ 1^ é fenil-c~ 1~-c~ 2~-alquila ou hetaril-c~ 1~-c~ 2~alquila opcionalmente substituído, r^ 2^ é arila opcionalmente substituído, hetarila, aril-c~ 1~-c~ 6~-aqluila, aril-c~ 2~-c~ 6~-alquenila ou heraril-c~ 1~-c~ 4~-alquila, r^ 3^ é c~ 1~-c~ 3~-alquila, c~ 1~-c~ 3~-alquila, r^ 4^ e r^ 5^, independemente um do outro, são halogênio, cf~ 3~, chf~ 2~,ch~ 2~f, c~ 1~-c~ 2~-alquila ou c~ 1~-c~ 2-alcóxi, e m e n, independentemente um do outro, são 0 ou 1. carboxamide compounds and their use as calpain inhibitors. The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. carboxamide compounds are calpain inhibitors (calcium dependent cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for the treatment of a disorder associated with high calpain activity. carboxamide compounds are compounds of the general formula i wherein r ^ 1 ^, r ^ 2 ^, r ^ 3 ^, r ^ 4 ^, r ^ 5 ^ and m have the meanings mentioned in the claims and the description, the tautomers thereof, the hydrates thereof and the pharmaceutically acceptable salts thereof. Of these compounds, those wherein R 1 is R 2 is phenyl-C 1 -C 2 -alkyl or optionally substituted ...

N-phenyl-(piperazinyl or homopiperazinyl)-benzenesulfonamide or benzenesulfonyl-phenyl-(piperazine or homopiperazine) compounds suitable for treating disorders that respond to modulation of the serotonin 5-ht6 receptor

Carbidopa and l-dopa prodrugs and methods of use

The present disclosure relates to (a) carbidopa prodrugs, (b) pharmaceutical combinations and compositions comprising a carbidopa prodrug and/or an L-dopa prodrug, and (c) methods of treating Parkinson's disease and associated conditions comprising administering a carbidopa prodrug and an L-dopa prodrug to a subject with Parkinson's disease.

Pyrrolidine derivatives, pharmaceutical compositions containing them, and their use in therapy

The present invention relates to pyrrolidine derivatives of formula (I), or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such pyrrolidine derivatives, and the use of such pyrrolidine derivatives for therapeutic purposes. The pyrrolidine derivatives are GlyT1 inhibitors.

Carbidopa and L-dopa prodrugs and methods of use

The present disclosure relates to (a) carbidopa prodrugs, (b) pharmaceutical combinations and compositions comprising a carbidopa prodrug and/or an L-dopa prodrug, and (c) methods of treating Parkinson's disease and associated conditions comprising administering a carbidopa prodrug and an L-dopa prodrug to a subject with Parkinson's disease.

Carboxamide compounds and their use as calpain inhibitors V

Carbidopa and l-dopa prodrugs and methods of use

The present disclosure relates to (a) carbidopa prodrugs, (b) pharmaceutical combinations and compositions comprising a carbidopa prodrug and/or an L-dopa prodrug, and (c) methods of treating Parkinson's disease and associated conditions comprising administering a carbidopa prodrug and an L-dopa prodrug to a subject with Parkinson's disease.

Aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives, pharmaceutical compositions containing them, and their use in therapy

The present invention relates to aminochromane, aminothiochromane and amino-1,2,3,4- tetrahydroquinoline derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminochromane, aminothio-chromane and amino-1,2,3,4-tetrahydroquinoline derivatives, and the use of such aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives for therapeutic purposes. The aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives are GlyT1 inhibitors.

Carboxamide compounds and their use as calpain inhibitors

Aminotetraline and aminoindane derivatives, pharmaceutical compositions containing them, and their use in therapy

Aminotetraline and aminoindane derivatives, pharmaceutical compositions containing them, and their use in therapy

The present invention relates toaminotetralineand aminoindane derivatives of the formula (I) (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminotetralineand ami- noindane derivatives, and the use of such aminotetralineand aminoindane derivatives for therapeutic purposes. The aminotetraline and aminoindane derivatives are GlyT1 inhibitors.

Carbidopa and L-dopa prodrugs and their use to treat Parkinson's disease

Composición farmacéutica que comprende un primer compuesto que corresponde en estructura a la Fórmula (I):**Fórmula** o una sal farmacéuticamente aceptable del mismo, en la que R1 y R2 se seleccionan cada uno independientemente del grupo que consiste en hidrógeno, -P(O)(OH)2 y -R5-O-P(O)(OH)2; R5 es un alquilo C1-C4; R6 es hidrógeno o un alquilo C1-C4; y siempre que al menos uno de R1 y R2 sea -P(O)(OH)2 o -R5-O-P(O)(OH)2; y el segundo compuesto que corresponde en estructura a la Fórmula (II):**Fórmula** o una sal farmacéuticamente aceptable del mismo, en la que R3 y R4 se seleccionan cada uno independientemente del grupo que consiste en hidrógeno, -P(O)(OH)2 y -R5-O-P(O)(OH)2; R5 es un alquilo C1-C4; R6 es hidrógeno o un alquilo C1-C4; y siempre que al menos uno de R3 y R4 sea -P(O)(OH)2 o -R5-O-P(O)(OH)2.

N-phenyl-(piperazinyl or homopiperazinyl)-benzenesulfonamide or benzenesulfonyl-phenyl-(piperazine or homopiperazine) compounds suitable for treating disorders that respond to modulation of the serotonin 5-ht6 receptor 5-ht6 n--()- --()

Carboxamide compounds and their use as calpain inhibitors

The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. The carboxamide compounds are compounds of the general formula I in which R 1 , R 2 , R 3 R 4 , R 5 , m and n have the meanings mentioned in the claims and the description, the tautomers thereof, the hydrates thereof and the pharmaceutically suitable salts thereof. Of these compounds those are preferred wherein R 1 is optionally substituted phenyl-C 1 -C 2 -alkyl or hetaryl-C 1 -C 2 -alkyl, R 2 is optionally substituted aryl, hetaryl, aryl-C 1 -C 6 -alkyl, aryl-C 2 -C 6 -alkenyl or hetaryl-C 1 -C 4 -alkyl, R 3 is C 1 -C 3 -alkyl, C 1 -C 3 -haloalkyl, C 2 -C 4 -alkenyl, C 3 -C 6 -cycloalkyl, C 3 -C 6 -cycloalkyl-C 1 -C 2 -alkyl, or phenyl-C 1 -C 3 -alkyl, R 4 and R 5 independently of one another are halogen, CF 3 , CHF 2 , CH 2 F, C 1 -C 2 -alkyl or C 1 -C 2 -alkoxy, and m and n independently of one another are 0 or 1.

Aminotetraline and aminoindane derivatives, pharmaceutical compositions containing them, and their use in therapy

The present invention relates toaminotetralineand aminoindane derivatives of the formula (I) (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminotetralineand ami- noindane derivatives, and the use of such aminotetralineand aminoindane derivatives for therapeutic purposes. The aminotetraline and aminoindane derivatives are GlyT1 inhibitors.

Carboxamide compounds and their use as calpain inhibitors v

The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. The carboxamide compounds are compounds of the general formula (I) in which R1, R2 and n have the meanings mentioned in the claims and the description, Y is a radical of the formulae (Y1) or (Y2) where # indicates the point of attachment of Y to the pyridine ring, R3, R4, R5, Ry and m have the meanings mentioned in the claims and the description, A is is (CH2)p with p being 1, 2, 3 or 4, where one or two hydrogen atoms may be replaced by a radical R6, where A is attached to the 3-or 4-positon of the pyrazole radical and R6 has the meaning mentioned in the claims and the description; A1 is (CH2)q with q being 0, 1, 2 or 3, where one or two hydrogen atoms may be replaced by halogen or C1-C4-alkyl; and A2 is (CH2)r with r being 0, 1, 2 or 3, where one or two hydrogen atoms may be replaced by halogen or C1-C4-alkyl, provided that that r + q is 2, 3, 4, 5 or 6; their tautomers, the hydrates thereof, the pharmaceutically suitable salts of the carbox-amide compounds (I), the prodrugs of (I) and the pharmaceutically suitable salts of the prodrugs, tautomers or hydrates of (I).

Προφαρμακα καρβιντοπας και l-ντοπας και η χρηση τους στην αγωγη της νοσου parkinson

Η παρούσα αποκάλυψη αναφέρεται σε (a) προφάρμακα καρβιντόπας, (b) φαρμακευτικούς συνδυασμούς και συνθέσεις που περιλαμβάνουν ένα προφάρμακο καρβιντόπας και/ή ένα προφάρμακο L-ντόπας και (c) μεθόδους αγωγής της νόσου Parkinson και σχετικών παθήσεων που περιλαμβάνουν τη χορήγηση ενός προφαρμάκου καρβιντόπας και ενός προφαρμάκου L-ντόπας σε ένα άτομο με νόσο Parkinson.

Carbidopa and l-dopa prodrugs and methods of use

The present disclosure relates to (a) carbidopa prodrugs, (b) pharmaceutical combinations and compositions comprising a carbidopa prodrug and/or an L-dopa prodrug, and (c) methods of treating Parkinson's disease and associated conditions comprising administering a carbidopa prodrug and an L-dopa prodrug to a subject with Parkinson's disease.

カルビドパおよびｌ－ドーパプロドラッグならびにそれらの使用方法

【課題】パーキンソン病および関連状態の治療するための組成物の提供。【解決手段】式（I-a)等のカルビドパプロドラッグと式（II-a)等のＬ－ドーパプロドラッグを含む医薬組み合わせ及び組成物。TIFF2023174770000165.tif75164【選択図】なし

4,5-dihydropyrazole derivatives, pharmaceutical compositions containing them, and their use in therapy

The present invention relates to 4,5-dihydropyrazole derivatives of the formula (I) and physiologically tolerated salts thereof which are GlyTl inhibitors. The invention further relates to pharmaceutical compositions comprising such 4,5-dihydropyrazole derivatives, and the use of such 4,5-dihydropyrazole derivatives for therapeutic purposes.