SPIRO-COMPOUNDS AS SIP MODULATORS

The invention relates to heterocyclic compounds of formula (I) as SIP modulators, pharmaceutical compositions comprising such compounds, and uses thereof in the treatment or alleviation of diseases or disorders mediated by an SIP receptor. 2. A compound according to wherein m and n are both 0 or both 1.4. A compound according to wherein R1 is selected from the group consisting of -1 claim 3 ,3-cyclobutylene-R2 and —(C1-3)alkylene-R2 claim 3 , wherein the (C1)alkyl is unsubstituted claim 3 , and the (C2)alkyl and the (C3)alkyl are substituted with up to two CHgroups claim 3 , with (CH)to form a cyclopropyl moiety or with (CH)to form a cyclobutyl moiety.5. A compound according to wherein X is CH.6. A compound according to wherein R3 is selected from the group consisting of:(C3-6)cycloalkyl, preferably cyclohexyl, optionally substituted with (C1-4) alkyl; halogen,', 'cyano,', '(C1-4)alkyl optionally substituted with one or more fluoro atoms,', '(C1-4)alkoxy optionally substituted with one or more fluoro atoms or with (C3-6)cycloalkyl,', '(C3-5)cycloalkoxy optionally substituted with one or more fluoro atoms; and', '(C3-6)cycloalkyl optionally substituted with (C1-4)alkyl, (C1-4)alkoxy or a halogen atom,, 'monocyclic heterocycle, preferably oxanyl or pyridyl, optionally substituted with 1 or 2 substituents independently selected from the group consisting ofindanyl, optionally substituted with one or two halogen atoms8-10 membered fused bicyclic group, preferably preferably 2,3-dihydrobenzofuranyl, indanyl, indoly or 1,3-dioxaindanyl, optionally substituted with one or two halogen atoms; halogen,', 'cyano,', '(C1-4)alkyl optionally substituted with one or more fluoro atoms,', '(C1-4)alkoxy optionally substituted with one or more fluoro atoms or with (C3-6)cycloalkyl,', '(C3-5)cycloalkoxy optionally substituted with one or more fluoro atoms; and', '(C3-6)cycloalkyl optionally substituted with (C1-4)alkyl, (C1-4)alkoxy or a halogen atom., 'phenyl optionally substituted ...

MODULATORS OF 5-HT RECEPTORS AND METHODS OF USE THEREOF

The present application relates to aryl- and heteroaryl-fused decahydropyrroloazepine, octahydrooxepinopyrrole, octahydropyrrolothiazepine dioxide, decahydrocyclohepta[c]pyrrole, and octahydrocyclohepta[c]pyrrole derivatives of formula (I) 4. The compound of claim 1 , wherein Yis C(O) or S(O) claim 1 , Yis NR claim 1 , and Yis CRR; or wherein Yis C(O) claim 1 , Yand Yare each CRR.5. The compound of claim 1 , wherein Yis CRR claim 1 , Yis NR claim 1 , and Yis C(O) claim 1 , or wherein Yis CRR claim 1 , Yis C(O) claim 1 , and Yis NR.6. The compound of claim 1 , wherein Y is CRR claim 1 , Yis NR claim 1 , and Yis CRR.7. The compound of wherein Ris alkylcarbonyl claim 6 , —C(O)-G claim 6 , —C(O)NR-G claim 6 , or —S(O)-G.8. The compound of claim 1 , wherein Yis O claim 1 , and Yand Yare independently CRR.9. The compound of claim 1 , wherein Yis NR claim 1 , wherein Ris hydrogen claim 1 , alkyl claim 1 , alkylcarbonyl claim 1 , —C(O)-G claim 1 , —(CRR)-G claim 1 , —C(O)-G claim 1 , and —(CRR)-G claim 1 , and Yand Yare independently CRR.10. The compound of claim 1 , wherein Yis NR claim 1 , wherein Ris hydrogen claim 1 , alkyl claim 1 , alkylcarbonyl claim 1 , —C(O)-G claim 1 , —(CRR)-G claim 1 , —C(O)-G claim 1 , and —(CRR)-G claim 1 , Yis C(O) and Yis CRR.11. The compound of claim 1 , wherein Yand Ytogether are CR═CRand Yis CRR.12. The compound of claim 1 , wherein Ris selected from the group consisting of hydrogen claim 1 , alkyl claim 1 , haloalkyl claim 1 , —(CRR)-G claim 1 , or —S(O)R.14. The compound of claim 3 , wherein R claim 3 , R claim 3 , Rand Rare each independently hydrogen claim 3 , alkyl claim 3 , halogen claim 3 , cyano claim 3 , -G claim 3 , -G claim 3 , —NO claim 3 , —OR claim 3 , —S(O)R claim 3 , —S(O)N(R)(R) claim 3 , —C(O)R claim 3 , —C(O)OR claim 3 , —C(O)N(R)(R) claim 3 , —(CRR)-G claim 3 , —CR═CR-G claim 3 , —(CRR)-G claim 3 , —CR═CR-G claim 3 , or haloalkyl claim 3 , or Rand Rtaken together with the carbon atoms to which they are attached form a ...

5-SUBSTITUTED INDAZOLES AS KINASE INHIBITORS

The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, 1162-. (canceled)169. The compound of claim 163 , that isN-cyclohexyl-6-(1H-indazol-5-yl)imidazo[2,1-b][1,3]thiazol-5-amine;N-cyclohexyl-2-(1H-indazol-5-yl)imidazo[1,2-a]pyridin-3-amine;N-cyclohexyl-2-(1H-indazol-5-yl)imidazo[1,2-a]pyrazin-3-amine;N-cyclohexyl-2-(1H-indazol-5-yl)imidazo[1,2-a]pyrimidin-3-amine;2-(1H-indazol-5-yl)-N-isopropylimidazo[1,2-a]pyrimidin-3-amine;N-benzyl-2-(1H-indazol-5-yl)imidazo[1,2-a]pyrimidin-3-amine;N-butyl-2-(1H-indazol-5-yl)imidazo[1,2-a]pyrimidin-3-amine;N-(4-chlorophenyl)-2-(1H-indazol-5-yl)imidazo[1,2-a]pyrimidin-3-amine;2-(1H-indazol-5-yl)-N-(4-methoxyphenyl)imidazo[1,2-a]pyrimidin-3-amine;2-(1H-indazol-5-yl)imidazo[1,2-a]pyrimidine;methyl N-[2-(1H-indazol-5-yl)imidazo[1,2-a]pyridin-3-yl]glycinate;N-benzyl-2-(1H-indazol-5-yl)imidazo[1,2-a]pyridin-3-amine;N-(4-chlorophenyl)-2-(1H-indazol-5-yl)imidazo[1,2-a]pyridin-3-amine;2-(1H-indazol-5-yl)-N-(4-methoxyphenyl)imidazo[1,2-a]pyridin-3-amine;2-(1H-indazol-5-yl)-3-phenylimidazo[1,2-a]pyrimidine;ethyl N-[2-(1H-indazol-5-yl)imidazo[1,2-a]pyrimidin-3-yl]-beta-alaninate; or{'sup': '3', 'N-[2-(1H-indazol-5-yl)imidazo[1,2-a]pyrimidin-3-yl]-β-alaninamide;'}170. A pharmaceutical composition comprising a therapeutically effective amount of a compound of formula (I) according to claim 163 , in combination with a pharmaceutically suitable carrier. This application is a continuation-in-part of U.S. application Ser. No. 12/132,993 filed on Jun. 4, 2008 which claims priority to provisional application Ser. No. 60/933,960 filed on, Jun. 8, 2007, the contents of each of which are herein incorporated by reference.The present invention relates to 5-substituted indazole containing compounds, methods of making the compounds, compositions containing the compounds which are useful for inhibiting kinases such as Glycogen Synthase kinase 3 (GSK-3), Rho kinase (ROCK), Janus Kinases (JAK), Cdc7, AKT, PAK4, PLK, CK2, ...

MODULATORS OF 5-HT RECEPTORS AND METHODS OF USE THEREOF

The present application relates to aryl- and heteroaryl-fused decahydropyrroloazepine, octahydrooxepinopyrrole, octahydropyrrolothiazepine dioxide, decahydrocyclohepta[c]pyrrole, and octahydrocyclohepta[c]pyrrole derivatives of formula (I) 4. (canceled)5. The compound of claim 1 , wherein Yis CRR claim 1 , Yis NR claim 1 , and Yis C(O) claim 1 , or wherein Yis CRR claim 1 , Yis C(O) claim 1 , and Yis NR.611.-. (canceled)12. The compound of claim 1 , wherein Ris selected from the group consisting of hydrogen claim 1 , alkyl claim 1 , haloalkyl claim 1 , —(CRR)-G claim 1 , or —S(O)R.14. The compound of claim 3 , wherein R claim 3 , R claim 3 , Rand Rare each independently hydrogen claim 3 , alkyl claim 3 , halogen claim 3 , cyano claim 3 , -G claim 3 , -G claim 3 , —NO claim 3 , —OR claim 3 , —S(O)R claim 3 , —S(O)N(R)(R) claim 3 , —C(O)R claim 3 , —C(O)OR claim 3 , —C(O)N(R)(R) claim 3 , —(CRR)-G claim 3 , —CR═CR-G claim 3 , —(CRR)-G claim 3 , —CR═CR-G claim 3 , or haloalkyl claim 3 , or Rand Rtaken together with the carbon atoms to which they are attached form a substituted or unsubstituted phenyl or heteroaryl ring.15. The compound of claim 1 , wherein the compound is selected from the group consisting of:trans-2-benzyl-1,2,3,3a,4,5-hexahydrobenzo[c]pyrrolo[3,4-e]azepin-6(10bH)-one;trans-1,2,3,3a,4,5-hexahydrobenzo[c]pyrrolo[3,4-e]azepin-6(10bH)-one;cis-2-benzyl-1,2,3,3a,4,5-hexahydrobenzo[c]pyrrolo[3,4-e]azepin-6(10bH)-one;cis-1,2,3,3a,4,5-hexahydrobenzo[c]pyrrolo[3,4-e]azepin-6(10bH)-one;trans-2-benzyl-1,2,3,3a,5,6-hexahydrobenzo[c]pyrrolo[3,4-e]azepin-4(10bH)-one;trans-2-(2,5-dimethylbenzyl)-1,2,3,3a,4,5-hexahydrobenzo[c]pyrrolo[3,4-e]azepin-6(10bH)-one;trans-2-(2,4-dimethylbenzyl)-1,2,3,3a,4,5-hexahydrobenzo[c]pyrrolo[3,4-e]azepin-6(10bH)-one;trains-2-(3,4-dimethylbenzyl)-1,2,3,3a,4,5-hexahydrobenzo[c]pyrrolo[3,4-e]azepin-6(10bH)-one;trans-2-(3-methylbenzyl)-1,2,3,3a,4,5-hexahydrobenzo[c]pyrrolo[3,4-e]azepin-6(10bH)-one;trans-2-(2,3-dimethylbenzyl)-1,2,3,3a,4,5 ...

5-heteroaryl substituted indazoles as kinase inhibitors

The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein A, R1, R2, R3 and m, are defined in the description. The present invention relates also to methods of making said compounds, and compositions containing said compounds which are useful for inhibiting kinases such as Glycogen Synthase kinase 3 (GSK-3), Rho kinase (ROCK), Janus Kinases (JAK), AKT, PAK4, PLK, CK2, KDR, MK2, JNK1, aurora, pim 1 and nek 2.

Preparation of modulators of 5-HT receptors

Heterocyclic compounds and their use as glycogen synthase kinase 3 inhibitors

The present invention relates to a heterocyclic compound of the general formula (I) and their use and preparation, methods of making the compounds, compositions containing at least one of said compounds, and methods of treatment using at least one compound. In particular, compounds of the general formula (I) are useful for inhibiting glycogen synthase kinase 3 (GSK-3).

5-heteroaryl substituted indazoles as kinase inhibitors.

La presente invención se refiere a compuestos de la fórmula (I) o sales farmacéuticamente aceptables, en donde A, R1, R2, R3 y m, son como se definieron en la descripción. La presente invención se refiere también a métodos para elaborar los compuestos, y composiciones que contienen los compuestos los cuales son útiles para inhibir las cinasas tales como Glicógeno Cintaza cinasa 3 (GSK-3), Rho cinasa (ROCK), Janus Cinasas (JAK), AKT, PAK4, PLK, CK2, KDR, MK2, JNK1, aurora, pim 1 y nek 2.

Arylsulfonylmethyl or arylsulfonamide substituted aromatic compounds suitable for treating disorders that respond to madulation of the dopamine d3 receptor

The present invention relates to aromatic compounds of the formula (I), wherein Ar is phenyl or an aromatic 5- or 6-membered C-bound heteroaromatic radical, wherein Ar may carry 1 radical Ra and wherein Ar may also carry 1 or 2 radicals Rb; X is N or CH; Y is O, S, -CH=N-, -CH=CH- or -N=CH-; A is CH2i O or S; E is CR6R7 or NR 3; R1 is C1-C4-alkyl, C3-C4-cycloalkyl, C3-C4-cycloalkylmethyl, C3-C4-alkenyl, fluorinated C1-C4-­alkyl, fluorinated C3-C4-cycloalkyl, fluorinated C3-C4-cycloalkylmethyl, fluorinated C3-C4­-alkenyl, formyl or C,-C3-alkylcarbonyl; R1a is H, C2-C4-alkyl, C3-C4-cycloalkyl, C3-C4-alkenyl, fluorinated C1-C4-alkyl, fluorinated C3-C4 -cycloalkyl, or R1a and R2 together are (CH2)n with n being 2 or 3, or R1a and R2a together are (CH2)n with n being 2 or 3; R2 and R2a are independently of each other H, CH3, CH2F, CHF2 or CF3; R3 is H or C1-C4-alkyl; R6, R7 independently of each other are selected from H, C1-C2-alkyl and fluorinated C1-C2-alkyl; and the physiologically tolerated acid addition salts thereof. The invention also relates to the use of a compound of the formula I or a pharmaceutically acceptable salt thereof for preparing a pharmaceutical composition for the treatment of a medical disorder susceptible to treatment with a dopamine D3 receptor ligand.

Modulators of 5-ht receptors and methods of use thereof.

La presente solicitud se refiere a derivados de decahidropirroloazepina fusionada a arilo- y heteroarilo, octahidrooxepinopirrol, dióxido de octahidropirrolotiazepina, decahidrociclohepta[c]pirrol, y octahidrociclohepta[cjpirrol de fórmula (I) (ver fórmula (I)) en donde R1, R2, R3, R4, R5, A, Y1, Y2, e Y3 son como se define en la especificación. La presente solicitud también se refiere a composiciones que comprenden tales compuestos, procesos para hacer tales compuestos, y métodos para tratar condiciones de enfermedad utilizando tales compuestos y composiciones y métodos para identificar tales compuestos.

Arylsulfonylmethyl or arylsulfonamide substituted aromatic compounds suitable for treating disorders that respond to madulation of the dopamine D3 receptor

Arylsulfonylmethyl or arylsulfonamide substituted aromatic compounds suitable for treating disorders that respond to madulation of the dopamine d3 receptor

The present invention relates to aromatic compounds of the formula (I), wherein Ar is phenyl or an aromatic 5- or 6-membered C-bound heteroaromatic radical, wherein Ar may carry 1 radical Ra and wherein Ar may also carry 1 or 2 radicals Rb; X is N or CH; Y is O, S, -CH=N-, -CH=CH- or -N=CH-; A is CH2i O or S; E is CR6R7 or NR 3; R1 is C1-C4-alkyl, C3-C4-cycloalkyl, C3-C4-cycloalkylmethyl, C3-C4-alkenyl, fluorinated C1-C4-­alkyl, fluorinated C3-C4-cycloalkyl, fluorinated C3-C4-cycloalkylmethyl, fluorinated C3-C4­-alkenyl, formyl or C,-C3-alkylcarbonyl; R1a is H, C2-C4-alkyl, C3-C4-cycloalkyl, C3-C4-alkenyl, fluorinated C1-C4-alkyl, fluorinated C3-C4 -cycloalkyl, or R1a and R2 together are (CH2)n with n being 2 or 3, or R1a and R2a together are (CH2)n with n being 2 or 3; R2 and R2a are independently of each other H, CH3, CH2F, CHF2 or CF3; R3 is H or C1-C4-alkyl; R6, R7 independently of each other are selected from H, C1-C2-alkyl and fluorinated C1-C2-alkyl; and the physiologically tolerated acid addition salts thereof. The invention also relates to the use of a compound of the formula I or a pharmaceutically acceptable salt thereof for preparing a pharmaceutical composition for the treatment of a medical disorder susceptible to treatment with a dopamine D3 receptor ligand.

Triazole compounds suitable for treating disorders that respond to modulaiont of the dopamine d3 receptor

The invention relates to compounds of formula (I), wherein n is 1 or 2, Ar is a C-bound 1,2,4-triazol radical which carries a radical R1 on the remaining carbon atom and a radical R1a on one of the nitrogen atoms; R1 is hydrogen, C1-C6 alkyl, C3-C6 cycloalkyl, C1-C4 alkoxymethyl, fluorinated C1-C6 alkyl, fluorinated C3-C6 cycloalkyl, fluorinated C1-C4 alkoxymethyl, or optionally substituted phenyl or 5- or 6-membered heteroaryl; R1a is hydrogen or C1-C4 alkyl; and R2 is C1-C6 alkyl, C3-C6 cycloalkyl, fluorinated C1-C6 alkyl or fluorinated C3-C6 cycloalkyl; and to the physiologically tolerated acid addition salts of there compounds. The invention also relates to a pharmaceuticaly composition that comprises at least one triazole compound of the formula (I) and/or at least one physiologically tolerated acid addition salt thereof, and further to a method for treating disorders that respond beneficially to dopamine D3 receptor antagonists or dopamine D3 agonists, said method comprising administering an effective amount of at least one traizole compound or physiologically tolerated acid addition salt of the formula (I) to a subject in need thereof.

6-amino(aza)indane compounds suitable for treating disorders that respond to modulation of the dopamine D3 receptor

The present invention relates to 6-amino(aza)indane compound of the formula (I) Wherein Ar is phenyl or an aromatic 5- or 6-membered C-bound heteroaromatic radical, wherein Ar may carry 1 radical R and wherein Ar may also carry I or 2 radicals R; X is N or CH; E is CRR or NR ; R is C-C-alkyl, C-C4-cycloalkyl, C-C-cycloalkylmethyl, C-C-alkenyl, fluorinated C-C-alkyl, fluorinated C-C-cycloalkyl, fluorinated C-C-cycloalkylmethyl, fluorinated C-C-alkenyl, formyl or C-C-alkylcarbonyl; R is H or R and R or R and Rtogether are (CH) with n being 1, 2, 3 or 4; R and Reach independently are H, CH, CHF, CHF or CF; R is H or C,-C4-alkyl; and the physiologically tolerated acid addition salts of these compounds. The invention also relates to pharmaceutical compositions comprising at least one compound of the formula (I) or a pharmaceutically acceptable salt thereof and to a method for treating a medical disorder susceptible to treatment with a dopamine D3 receptor ligand, said method comprising administering an effective amount of at least one compound of the formula (I) or a pharmaceutically acceptable salt thereof.

AROMATIC ARYLSULFONYLMETHYL OR SUBSTITUTED ARYLSULFONAMIDE COMPOUNDS FOR TREATING DISORDERS THAT MEET MODULATION OF THE DOPAMINE D3 RECEPTOR

APPROPRIATE BENCESULFONAMIDE COMPOUNDS TO TREAT DISORDERS THAT CORRESPOND TO DOPAMINE D3 RECEPTOR MODULATION

1.- Un compuesto N-(6-piperazin-1-ilpiridin-3-il) bencensulfonamida de la fórmula Idonde R1 se selecciona entre el grupo que consiste en hidrógeno, C1-C3 alquilo lineal y C1-C3 alquilo lineal fluorado; R2 es hidrógeno o metilo; R3 se selecciona entre el grupo que consiste en hidrógeno, halógeno, C1-C2-alquilo, C1-C2-alquilo fluorado, C1-C2-alcoxi y C1-C2-alcoxi fluorado, R4 es C1-C2-alquilo o C1-C2-alquilo fluorado; n es 0,1 o 2;y las sales fisiológicamente toleradas de este compuesto y los N-óxidos del mismo. 2.- El compuesto de acuerdo con la reivindicación 1, donde R1 es hidrógeno. 3.- El compuesto de acuerdo con las reivindicaciones 1 o 2, donde R2 es metilo.4.- El compuesto de acuerdo con la reivindicación 3, donde el átomo de carbono que lleva a R2 tiene configuración S.5.- El compuesto de acuerdo con la reivindicación 3, donde el átomo de carbono que lleva a R2 tiene configuración R.6.- El compuesto de acuerdo con las reivindicaciones 1 o 2, donde R2 es hidrógeno. 7.- El compuesto de acuerdo con cualquiera de las reivindicaciones precedentes, donde R3 es metilo. 8.- El compuesto de acuerdo con cualquiera de las reivindicaciones precedentes, donde R4 es metilo. 9.- El compuesto de acuerdo con la reivindicación 8, donde el átomo de carbono que lleva a R4 tiene configuración S.10.- El compuesto de acuerdo con la reivindicación 8, donde el átomo de carbono que lleva a R4 tiene configuración R.11.- El compuesto de acuerdo con cualquiera de las reivindicaciones precedentes, donde n es 1.12.- El compuesto de acuerdo con cualquiera de las reivindicaciones precedentes, donde n es 2. 1.- An N- (6-piperazin-1-ylpyridin-3-yl) benzenesulfonamide compound of the formula Where R1 is selected from the group consisting of hydrogen, C1-C3 linear alkyl and C1-C3 fluorinated linear alkyl; R2 is hydrogen or methyl; R3 is selected from the group consisting of hydrogen, halogen, C1-C2-alkyl, C1-C2-fluorinated alkyl, C1-C2-alkoxy and C1-C2-fluorinated alkoxy, R4 is C1-C2-alkyl or C1 ...

Arylsulfonylmethyl or Arylsulfonamide substituted aromatic compounds suitable for treating disorders that respond to madulation of the dopamine D3 receptor

Disclosed is an sulfonyl aromatic compound of the formula I wherein Ar is phenyl or an aromatic 5- or 6-membered C-bound heteroaromatic radical, X is N or CH; Y is O, S, -CH=N ,-CH=CH- or -N=CH-; A is CH2 , O or S; E is CR6R7 or NR3. R1 is alkyl, cycloalkyl, cycloalkylmethyl, alkenyl, fluorinated alkyl, fluorinated cycloalkyl, fluorinated cycloalkylmethyl, fluorinated alkenyl, formyl or alkylcarbonyl; R" is H, or R" and R2 together are (CH2)n with n being 2 or 3, or R1a and R2a together are (CH2)n with n being 2 or 3; R2 and R2a are independently of each other H, CH3, CH2F, CHF2 or CF3 and R3 - R7 are defined as in the specification and the physiologically tolerated acid addition salts thereof. Also disclosed is a composition comprising said compound and the use of said compound in the manufacture of a medicament for the treatment of a medical disorder susceptible with a dopamine D3 receptor ligand e.g. addiction.

Dihydropyridine compounds and methods of use

Compounds having formula (I) are useful in treating diseases prevented by or ameliorated with potassium channel openers. Also disclosed are potassium channel opening compositions and a method of opening potassium channels in a mammal.

Azabicycloheptyl compounds suitable for treating disorders that respond to modulation of the dopamine d3 receptor

The present invention relates to a compound of the formula (I) wherein R1 is H, C1-C6-alkyl which may be substituted by C3-C6-cycloalkyl, fluorinated C1-C6-alkyl, C3-C6-cycloalkyl, fluorinated C3-C6-cycloalkyl, C3-C6-alkenyl, fluorinated C3-C6-alkenyl, formyl, acetyl or propionyl; A is phenylene, pyridylene, pyrimidylene, pyrazinylene, pyridazinylene or thiophenylene, which can be substituted by one or more substituents selected from halogen, methyl, methoxy and CF3; E is NR5 or CH2, wherein R5 is H or C1-C3-alkyl; Ar is a cyclic radical selected from the group consisting of phenyl, a 5- or 6-membered heteroaromatic radical comprising as ring members 1, 2 or 3 heteroatoms selected from N, O and S and a phenyl ring fused to a saturated or unsaturated 5- or 6-membered carbocyclic or heterocyclic ring, where the heterocyclic ring comprises as ring members 1, 2 or 3 heteroatoms selected from N, O and S and/or 1, 2 or 3 heteroatom-containing groups each independently selected from NR8, where R8 is H, C1-C4-alkyl, fluorinated C1-C4-alkyl, C1-C4-alkylcarbonyl or fluorinated C1-C4-alkylcarbonyl, and where the cyclic radical Ar may carry 1, 2 or 3 substituents Ra; wherein the variable Ra has the meanings given in the claims and in the description; and physiologically tolerated acid addition salts thereof. The invention also relates to the use of a compound of the formula I or a pharmaceutically acceptable salt thereof for preparing a pharmaceutical composition for the treatment of a medical disorder susceptible to treatment with a dopamine D3 receptor ligand.

Modulators of 5-ht receptors and methods of use thereof

The present application relates to aryl- and heteroaryl-fused decahydropyrroloazepine, octahydroox-epinopyrrole, octahydropyrrolothiazepine dioxide, decahy-drocyclohepta[c]pyrrole, and octahydrocyclohepta[c]pyr-role derivatives of formula (I), wherein R1, R2, R3, R4, R5, A, Y1, Y2, and Y3 are as defined in the specification. The present application also relates to compositions comprising such compounds, processes for making such compounds, and methods of treating disease conditions using such compounds and compositions, and methods for identifying such compounds.

HETEROCICLICAL COMPOUNDS AND ITS USE AS INHIBITORS OF GLUCOGENO SYNTHEASE QUINASE 3

1.- Un compuesto heterocíclico CARACTERIZADO PORQUE responde a la fórmula general (I)los estereoisómeros, prodrogas y/o sales de adición ácida fisiológicamente toleradas del mismo, donde A se selecciona entre el grupo que consiste en CH2, NH, N-C1-C4-alquilo, C1-C4-alquilo N-halogenado (preferiblemente fluorado) y CRA1RA2, donde RA1 y RA2 se seleccionan en forma independiente entre sí entre el grupo que consiste en H, C1-C2-alquilo, C1-C2-alquilo halogenado (preferiblemente fluorado), NH2 y OH, preferiblemente RA1 y RA2 se seleccionan en forma independiente entre sí entre el grupo que consiste en H, C1-C2-alquilo, C1-C2-alquilo halogenado (preferiblemente fluorado), NH2 y OH con la condición de que al menos uno de RA1 y RA2 es metilo o metilo halogenado (preferiblemente fluorado), más preferiblemente RA1 y RA2 se seleccionan en forma independiente entre sí entre el grupo que consiste en metilo y metilo halogenado (preferiblemente fluorado); X1, y X2 se seleccionan en forma independiente entre sí entre el grupo que consiste en CH, CR2 y N; X3 se selecciona entre el grupo que consiste en CH, CR2 y N; X4, X5, X6 y X7 se seleccionan en forma independiente entre sí entre el grupo que consiste en C, CH, CR1 y N, con la condición de que al menos uno de X1, X2, X3, X4, X5, X6, y X7 es N; Y3, Y4, Y5 y Y6 se seleccionan en forma independiente entre sí entre el grupo que consiste en C, CH, CR3 y N formando un anillo C de 6 miembros; o uno de Y3, Y4, Y5 y Y6 es parte del puente entre dos átomos vecinos formando un anillo C de 5 miembros; o con Y5 = Y6 = C entonces Y5 y Y6 pueden formar junto con el anillo C de 5 o 6 miembros un sistema cíclico fusionado con 5 o 6 miembros del anillo incluyendo Y5 y Y6 como miembros del anillo y que comprende átomos de C como miembros del anillo o en lugar de un átomo de C miembro del anillo ... 1.- A heterocyclic compound CHARACTERIZED BECAUSE it responds to the general formula (I) the stereoisomers, prodrugs and / or physiologically tolerated ...

Triazole compounds suitable for treating disorders that respond to modulaiont of the dopamine d3 receptor.

La invencion se refiere a compuestos de formula (I), en donde n es 1 o 2, Ar es un radical de 1,2,4-triazol unido a C que porta un radical R1 en el atomo de carbono remanente y un radical R1a en uno de los atomos de nitrogeno; R1 es hidrogeno, alquilo de C1-C6, cicloalquilo de C3-C6, alcoximetilo de C1-C4, alquilo de C1-C6 fluorado, cicloalquilo de C3-C6, fluorado, alcoximetilo de C1-C4 fluorado, o fenilo opcionalmente sustituido o heteroarilo de 5 o 6 miembros; R1a es hidrogeno o alquilo de C1-C4; y R2 es alquilo de C1-C6, cicloalquilo de C3-C6, alquilo de C1-C6 fluorado o cicloalquilo de C3-C6 fluorado; y las sales de adicion de acido fisiologicamente toleradas de estos compuestos. La invencion tambien se refiere a una composicion farmaceutica que comprende al menos un compuesto de triazol de la formula (I) y/o al menos una sal de adicion de acido fisiologicamente tolerada de la misma, y ademas a un metodo para tratar trastornos que responden beneficamente a los antagonistas del receptor de dopamina D3 o agonistas de dopamina D3, el metodo que comprende administrar una cantidad efectiva de al menos un compuesto de triazol o una sal de adicion de acido fisiologicamente tolerada de la formula (I) a un sujeto que necesita el mismo.

Heterocyclic compounds suitable for treating disorders that respond to modulation of the dopamine d3 receptor

The invention relates to compounds of the formula (I) wherein n is 0, 1 or 2; G is CH2 or CHR3; R1 is H, C,-C6-alkyl, C,-C6-alkyl substituted by C3-C6-cycloalkyl, Cl-C6-hydroxyalkyl, fluorinated C,-C6-alkyl, C3-C6-cycloalkyl, fluorinated C3-C6-cycloalkyl, C3-C6~ alkenyl, fluorinated C3-C6-alkenyl, formyl, acetyl or propionyl; R2, R3 and R4 are, independently of each other, H, methyl, fluoromethyl, difluoromethyl, or trifluoromethyl; A is phenylene, pyridylene, pyrimidylene, pyrazinylene, pyridazinylene or thiophenylene, which can be substituted by one ore more substituents selected from halogen, methyl, methoxy and CF3; E is NR5 or CH2, wherein R5 is H or C1 -C3-alkyl; Ar is a cyclic radical selected from the group consisting of phenyl, a 5- or 6-~membered heteroaromatic radical comprising as ring members 1, 2 or 3 heteroatoms selected from N, O and S and a phenyl ring fused to a saturated or unsaturated 5- or 6-membered carbocyclic or heterocyclic ring, where the heterocyclic ring comprises as ring members 1, 2 or 3 heteroatoms selected from N, O and S and/or 1, 2 or 3 heteroatom-containing groups each independently selected from NR8, where R8 is H, C1-C4-alkyl, fluorinated C1-C4-alkyl, C1-C4~alkylcarbonyl or fluorinated C1-C4-alkylcarbonyl, and where the cyclic radical Ar may carry 1, 2 or 3 substituents Ra, wherein the variable Ra has the meanings given in the claims and in the description; and physiologically tolerated acid addition salts thereof. The invention also relates to the use of a compound of the formula I or a pharmaceutically acceptable salt thereof for preparing a pharmaceutical composition for the treatment of a medical disorder susceptible to treatment with a dopamine D3 receptor ligand.

Preparation of 5-HT receptor modulators

Un proceso para preparar un compuesto de fórmula (1-5):**Fórmula** o una sal farmacéuticamente aceptable del mismo, donde A se selecciona entre el grupo que consiste en**Fórmula** X1 es N o CR9; X2 es N o CR10; X3 es N o CR11; X4 es N o CR12; con la condición de que solamente uno o dos de X1, X2, X3, o X4 pueden ser N; R9, R10, R11, R12, R13, R14, R15 y R16 cada uno es independientemente hidrógeno, alquilo, alquenilo, alquinilo, halógeno, ciano, -G1, -G2, -NO2, -OR1a, -OC(O)R1a, -OC(O)N(Rb)(R3a), -SR1a, -S(O)R2a, -S(O)2R2a, - S(O)2N(Rb)(R3a), -C(O)R1a, -C(O)G3, -C(O)OR1a, -C(O)N(Rb)(R3a), -N(Rb)(R3a), -N(RaC(O)R1a, -N(Ra)C(O)O(R1a), - N(Ra)C(O)N(Rb)(R3a), -N(Ra)S(O)2(R2a), -(CR4aR5a)m-NO2-(CR4aR5a)m-OR1a, -(CR4aR5a)m-OC(O)R1a, -(CR4aR5a)m- OC(O)N(Rb)(R3a), -(CR4aR5a)m-SR1a, -(CR4aR5a)m-S(O)R2a, -(CR4aR5a)m-S(O)2R2a, -(CR4R5a)S(O)2N(Rb)(R3a), -(CR4aR5a)m(O)R1a, -(CR4aR5a)m-C(O)OR1a, -(CR4aR5a)m-C(O)N(Rb)(R3a), -(CR4aR5a)m-N(Rb)(R3a), -(CR4aR5a)m- N(Ra) C(O)R1a, -(CR4aR5a)m-N(Ra)C(O)O(R1a), -(CR4aR5a)m-N(Ra)C(O)N(Rb)(R3a), -(CR4aR5a)m-G1, -CR4a>=CR5a-G1, -(CR4aR5a)m-G2, -CR4a>=CR5a-G2, -CR6a-C(R7a)2, cianoalquilo, haloalquilo, (v), (vi), (vii) o (viii); donde**Fórmula** R1a y R3a, en cada caso, cada uno es independientemente hidrógeno, alquilo, haloalquilo G1, -(CR4aR5a)m-G1, G2, o -(CR4aR5a)m-G2; R2a, en cada caso, es independientemente alquilo, haloalquilo, G1, o -(CR4aR5a)m-G1; R6a es alquilo o haloalquilo; R7a en cada caso, es independientemente hidrógeno, alquilo, o haloalquilo; R4a y R5a, en cada caso, cada uno es independientemente hidrógeno, halógeno, alquilo, o haloalquilo; G1, en cada caso, es independientemente arilo o heteroarilo, donde cada G1 está independientemente sin sustituir o sustituido con 1, 2, 3, 4 o 5 sustituyentes seleccionados entre el grupo que consiste en alquilo, alquenilo, alquinilo, halógeno, ciano, -NO2, -OR1b, -OC(O)R1b, -OC(O)N(Rb)(R3b), -SR1b, -S(O)R2b, -S(O)2R2b, - S(O)2N(Rb)(R3b), -C(O)R1b, -C(O)OR1b, -C(O)N(Rb)(R3b), -N(Rb)( ...

Aminoethylaromatic compounds suitable for treating disorders that respond to modulation of the dopamine d3 receptor

The present invention relates to aromatic compounds of the formula I wherein the variables have the definitions given in the claims and description. The invention also relates to the use of a compound of the formula I or a pharmaceutically acceptable salt thereof for preparing a pharmaceutical composition for the treatment of a medical disorder susceptible to treatment with a dopamine D3 receptor ligand.

Modulators of 5-ht receptors and methods of use thereof

596827 Disclosed is a compound of formula (I), such as (3aS,10bS)-8-chloro-2-methyl-1,2,3,3a,4,5-hexahydrobenzo[e]pyrrolo [3,4-c]azepin-6(10bH)-one and (3aS,10bS)-8-chloro-2-methyl-1,2,3,3a,4,5-hexahydrobenzo[e]pyrrolo [3,4-c]azepin-6(10bH)-one, which is useful for treating disorders associated with 5HT receptors. Also disclosed is a process for making such compounds.

Aminoethylaromatic compounds suitable for treating disorders that respond to modulation of the dopamine d3 receptor

The present invention relates to aromatic compounds of the formula (I) wherein Ar is phenyl or an aromatic 5- or 6-membered C-bound heteroaromatic radical, wherein Ar may carry 1 radical Ra and wherein Ar may also carry 1 or 2 radicals Rb; X is N or CH; E is CR6R7 or NR3;R1 is C1-C4-alkyl, C3-C4-cycloalkyl, C3-C4-cycloalkylmethyl, C3-C4-alkenyl, fluorinated Cl-C4~-alkyl, fluorinated C3-C4-cycloalkyl, fluorinated C3-C4-cycloalkylmethyl, fluorinated C3-C4~-alkenyl, formyl or C1-C3-alkylcarbonyl; R1a is H, C1-C4-alkyl, C3-C4-cycloalkyl, C3-C4-cycloalkylmethyl, C3-C4-alkenyl, fluorinated C1-~C4-alkyl, fluorinated C3-C4-cycloalkyl, fluorinated C3-C4-cycloalkylmethyl, fluorinated C3~-C4-alkenyl, or R1a and R2 together are (CH2)n with n being 2, 3 or 4, or R1a and R2a together are (CH2)n with n being 2, 3 or 4; R2 and R2a are independently of each other H, C1-C4-alkyl or fluorinated C1-C4-alkyl or R2a and R2 together are (CH2)m with m being 1, 2, 3, 4 or 5; R3 is H or C1-C4-alkyl; R6, R7 independently of each other are selected from H, fluorine, C1-C4-alkyl and fluorinated C1-C4-alkyl or together form a moiety (CH2)p with p being 2, 3, 4 or 5; and the physiologically tolerated acid addition salts thereof. The invention also relates to the use of a compound of the formula (I) or a pharmaceutically acceptable salt thereof for preparing a pharmaceutical composition for the treatment of a medical disorder susceptible to treatment with a dopamine D3 receptor ligand.

5-heteroaryl substituted indazoles as kinase inhibitors

Fused azabicyclic compounds that inhibit vanilloid receptor subtype 1 (VR1) receptor

Compounds of formula (I) are novel VR1 antagonists that are useful in treating pain, inflammatory thermal hyperalgesia, urinary incontinence and bladder overactivity, wherein X<SUB>1</SUB>, X<SUB>2</SUB>, X<SUB>3</SUB>, X<SUB>4</SUB>, X<SUB>5</SUB>, R<SUB>5</SUB>, R<SUB>6</SUB>, R<SUB>7</SUB>, R<SUB>8a</SUB>, R<SUB>8b</SUB>, R<SUB>9</SUB>, Z<SUB>1</SUB>, Z<SUB>2 </SUB>and L are as defined in the description.

Spiro-compounds as s1p modulators

The invention relates to heterocyclic compounds of formula (I) as SIP modulators, pharmaceutical compositions comprising such compounds, and uses thereof in the treatment or alleviation of diseases or disorders mediated by an SIP receptor.

Fused azabicyclic compounds that inhibit vanilloid receptor subtype 1 (vr1) receptor

Compounds of formula (I), are novel VR1 antagonists that are useful in treating pain, inflammatory thermal hyperalgesia, urinary incontinence and bladder overactivity.

5-ht receptor modulators and methods of using them

moduladores de receptores 5-ht e métodos de uso dos mesmos. o presente pedido refere-se à derivados de arila e heteroarila fundidos decahidropirrolazepina, octahidrooxepinopirrol, dióxido de octahidropirrolotiazepina, decahidrociclohepta[c]pirrol e octahidrociclohepta[c]pirrol, de fórmula (l) em que r1, r2, r3, r4, r5, a, y1, y2, y3 e são como definidos na especifficação. o presente pedido refere-se também a composições compreendendo esses compostos, processos para a preparação de tais compostos, e métodos de tratamento de condições de doença, utilizando tais compostos e composições, e métodos para identificação de tais compostos. 5-ht receptor modulators and methods of use thereof. The present application relates to fused aryl and heteroaryl derivatives of decahydropyrrolazepine, octahydrooxyepinopyrrol, octahydropyrrolothiazepine dioxide, decahidrocyclohepta [c] pyrrol and octahidrocyclohepta [c] pyrrol of formula (l) wherein r1, r2, r5, r3, a, y1, y2, y3 and are as defined in the specification. The present application also relates to compositions comprising such compounds, processes for the preparation of such compounds, and methods of treating disease conditions using such compounds and compositions, and methods for identifying such compounds.

Modulators of 5-ht receptors and methods of use thereof

Disclosed herein are aryl- and heteroaryl-fused decahydropyrroloazepine, octahydro-oxepinopyrrole, octahydropyrrolothiazepine dioxide, decahydrocyclohepta[c]pyrrole, and octahydrocyclohepta[c]pyrrole derivatives of formula (I) wherein R1, R2, R3, R4, R5, A, Y1, Y2, and Y3 are as defined in the specification. The present application also relates to compositions comprising such compounds, processes for making such compounds, and methods of treating disease conditions using such compounds and compositions, and methods for identifying such compounds. Specific embodiments of the derivatives of formula (I) include the following: trans-2-benzyl-1,2,3,3a,4,5-hexahydrobenzo[c]pyrrolo[3,4-e]azepin-6(10bH)-one; trans-2-benzyl-5-(naphthalen-1-ylsulfonyl)-1,2,3,3a,4,5,6,10b-octahydrobenzo[c]pyrrolo[3,4-e]azepine; and cis-8-amino-2-benzyl-1,2,3,3a,4,5-hexahydrobenzo[e]pyrrolo[3,4-c]azepin-6(10bH)-one.

6-amino(aza)indane compounds suitable for treating disorders that respond to modulation of the dopamine d3 receptor

The present invention relates to 6-amino(aza)indane compound of the formula I and the physiologically tolerated acid addition salts of these compounds. The invention also relates to pharmaceutical compositions comprising at least one compound of the formula I or a pharmaceutically acceptable salt thereof and to a method for treating a medical disorder susceptible to treatment with a dopamine D3 receptor ligand, said method comprising administering an effective amount of at least one compound of the formula I or a pharmaceutically acceptable salt thereof.

Dihydropyridine compounds and methods of use

Compounds having the formula (I) are useful in treating diseases prevented by or ameliorated with potassium channel openers. Also disclosed are potassium channel opening compositions and a method of opening potassium channels in a mammal.

Kondensierte azabicyclischeverbindungen als inhibitoren des vanilloid-rezeptors 1 (vr1)

Fused azabicyclic compounds that inhibit vanilloid receptor subtype 1 (vr1) receptor

Compounds of formula (I), are novel VR1 antagonists that are useful in treating pain, inflammatory thermal hyperalgesia, urinary incontinence and bladder overactivity.

Fused azabicyclic compounds that inhibit vanilloid receptor subtype 1 (VR1) receptor

Fused azabicyclic compounds that inhibit vanilloid receptor subtype 1 (vr1) receptor

Compounds of formula (I) are novel VR1 antagonists that are useful in treating pain, inflammatory thermal hyperalgesia, urinary incontinence and bladder overactivity, wherein X<SUB>1</SUB>, X<SUB>2</SUB>, X<SUB>3</SUB>, X<SUB>4</SUB>, X<SUB>5</SUB>, R<SUB>5</SUB>, R<SUB>6</SUB>, R<SUB>7</SUB>, R<SUB>8a</SUB>, R<SUB>8b</SUB>, R<SUB>9</SUB>, Z<SUB>1</SUB>, Z<SUB>2 </SUB>and L are as defined in the description.

Fused azabicyclic compounds that inhibit vanilloid receptor subtype 1 (vr1) receptor

Compounds of formula (I) are novel VR1 antagonists that are useful in treating pain, inflammatory thermal hyperalgesia, urinary incontinence and bladder overactivity, wherein X<SUB>1</SUB>, X<SUB>2</SUB>, X<SUB>3</SUB>, X<SUB>4</SUB>, X<SUB>5</SUB>, R<SUB>5</SUB>, R<SUB>6</SUB>, R<SUB>7</SUB>, R<SUB>8a</SUB>, R<SUB>8b</SUB>, R<SUB>9</SUB>, Z<SUB>1</SUB>, Z<SUB>2 </SUB>and L are as defined in the description.

Dihydropyridine compounds and methods of use

Compounds having the formula (I) are useful in treating diseases prevented by or ameliorated with potassium channel openers. Also disclosed are potassium channel opening compositions and a method of opening potassium channels in a mammal.

Aminomethyl substituted bicyclic aromatic compounds suitable for treating disorders that respond to modulation of the dopamine d3 receptor

The present invention relates to an aminomethyl substituted bicyclic aromatic compound of the formula I The invention also relates to the use of a compound of the formula I or a pharmaceutically acceptable salt thereof for preparing a pharmaceutical composition for the treatment of a medical disorder susceptible to treatment with a dopamine D3 receptor ligand.

Aminomethyl substituted bicyclic aromatic compounds suitable for treating disorders that respond to modulation of the dopamine d3 receptor

The present invention relates to an aminomethyl substituted bicyclic aromatic compound of the formula (I) wherein Ar is a cyclic radical selected from the group consisting of phenyl, a 5- or 6-membered C-bound heteroaromatic radical comprising as ring member 1, 2 or 3 heteroatoms which are, independently of each other, selected from O, S and N, and a phenyl ring fused to a saturated or unsaturated 5- or 6-membered carbocyclic or heterocyclic ring, where the heterocyclic ring comprises as ring members 1, 2 or 3 heteroatoms selected from N, O and S and/or 1, 2 or 3 heteroatom-containing groups each independently selected from NR8, where R8 is H, C1-C4-alkyl, fluorinated C1-C4-alkyl, C1-C4-alkylcarbonyl or fluorinated C1-C4-alkylcarbonyl, and where the cyclic radical Ar may carry 1, 2 or 3 substituents Ra, wherein the variable Ra has the meanings given in the claims and in the description; X is a covalent bond or N-R2, CHR2, CHR2CH2, N or C-R2; Y is N-R2a, CHR2a, CHR2aCH2 or CHR2aCH2CH2; is a single bond or a double bond; E is CH2 or NR3; R1 is H, C1-C4-alkyl, C3-C4-cycloalkyl, C3-C4-cycloalkylmethyl, C3-C4-alkenyl, fluorinated C1~-C4-alkyl, fluorinated C3-C4-cycloalkyl, fluorinated C3-C4-cycloalkylmethyl, fluorinated C3~-C4-alkenyl, formyl or C1-C3-alkylcarbonyl; R1a is H, C1-C4-alkyl, C3-C4-cycloalkyl, C3-C4-alkenyl, fluorinated C1-C4-alkyl, fluorinated C3~-C4-cycloalkyl, fluorinated C3-C4-alkenyl, R2 and R2a each independently are H, CH3, CH2F, CHF2 or CF3 or R1a and R2 or R1a and R2a together are (CH2)n with n being 1, 2 or 3; R3 is H or C1-C4-alkyl; R4 and R5 independently of each other are H, C1-C4-alkyl, fluorinated C1-C4-alkyl or C1-C4~-alkoxy or may form, together with N, a 4-, 5- or 6-membered saturated or unsaturated ring; R6 and R7 independently of each other are H or halogen; and the physiologically tolerated acid addition salts thereof. The invention also relates to the use of a compound of the formula (I) or a pharmaceutically acceptable salt thereof for ...

Aminomethyl Substituted Bicyclic Aromatic Compounds Suitable for Treating Disorders That Respond to Modulation of the Dopamine D3 Receptor

The present invention relates to an aminomethyl substituted bicyclic aromatic compound of the formula I wherein Ar is a cyclic radical selected from the group consisting of phenyl, a 5- or 6-membered C-bound heteroaromatic radical comprising as ring member 1, 2 or 3 heteroatoms which are, independently of each other, selected from O, S and N, and a phenyl ring fused to a saturated or unsaturated 5- or 6-membered carbocyclic or heterocyclic ring, where the heterocyclic ring comprises as ring members 1, 2 or 3 heteroatoms selected from N, 0 and S and/or 1, 2 or 3 heteroatom-containing groups each independently selected from NR 8 , where R 8 is H, C 1 -C 4 -alkyl, fluorinated C 1 -C 4 -alkyl, C 1 -C 4 -alkylcarbonyl or fluorinated C 1 -C 4 -alkylcarbonyl, and where the cyclic radical Ar may carry 1, 2 or 3 substituents R a , wherein the variable R a has the meanings given in the claims and in the description; X is a covalent bond or N—R 2 , CHR 2 , CHR 2 CH 2 , N or C—R 2 ; Y is N—R 2a , CHR 2a , CHR 2a CH 2 or CHR 2a CH 2 CH 2 ; is a single bond or a double bond; E is CH 2 or NR 3 ; R 1 is H, C 3 -C 4 -cycloalkyl, C 3 -C 4 -cycloalkylmethyl, C 3 -C 4 -alkenyl, fluorinated C 1 -C 4 -alkyl, fluorinated C 3 -C 4 -cycloalkyl, fluorinated C 3 -C 4 -cycloalkylmethyl, fluorinated C 3 -C 4 -alkenyl, formyl or C 1 -C 3 -alkylcarbonyl; R 1a is H, C 1 C 4 -alkyl, C 3 -C 4 -cycloalkyl, C 3 -C 4 -alkenyl, fluorinated C 1 -C 4 -alkyl, fluorinated C 3 -C 4 -cycloalkyl, fluorinated C 3 -C 4 -alkenyl, R 2 and R 2a each independently are H, CH 3 , CH 2 F, CHF 2 or CF 3 or R 1a and R 2 or R 1a and R 2a together are (CH 2 ) n with n being 1, 2 or 3; R 3 is H or C 1 C 4 -alkyl; R 4 and R 5 independently of each other are H, C 1 -C 4 -alkyl, fluorinated C 1 -C 4 -alkyl or C 1 -C 4 -alkoxy or may form, together with N, a 4-, 5- or 6-membered saturated or unsaturated ring; R 6 and R 7 independently of each other are H or halogen; and the physiologically tolerated acid addition salts thereof. ...

Thienopyridyl compounds that inhibit vanilloid receptor subtype 1 (vr1) and uses thereof

The present invention discloses fused thienopyridyl compounds of general formula (I), wherein X1-X6, R5-R7, Z1 and L are as defined in the description. The resent invention also discloses a method for inhibiting the VR1 receptor in mammals using these compounds, a method for controlling pain, urinary incontinence, bladder overactivity, and inflammatory thermal hyperalgesia in mammals, and pharmaceutical compositions including those compounds.

Thienopyridyl compounds that inhibit vanilloid receptor subtype 1 (vr1) and uses thereof

The present invention discloses fused thienopyridyl compounds of general formula (I) wherein X 1 -X 6 , R 5 -R 7 , Z 1 and L are as defined in the description. The resent invention also discloses a method for inhibiting the VR1 receptor in mammals using these compounds, a method for controlling pain, urinary incontinence, bladder overactivity, and inflammatory thermal hyperalgesia in mammals, and pharmaceutical compositions including those compounds.

Compuestos de tienopiridilo que inhibien el receptor vanilloide subtipo 1 (vr1) y usos de los mismos.

La presente invencion describe compuestos de tienopiridilo de formula general (I), en donde X1-X6, R5-R7, Z1 y L son como se definen en la descripcion. La presente invencion tambien describe un metodo para inhibir el receptor VR1 en mamiferos usando estos compuestos, un metodo para controlar dolor, incontinencia urinaria, sobreactividad de vejiga, e hiperalgesia termica inflamatoria en mamiferos, y composiciones farmaceuticas que incluyen estos compuestos (ver formula).

Thienopyridyl compounds that inhibit vanilloid receptor subtype 1 (vr1) and uses thereof

The present invention discloses fused thienopyridyl compounds of general formula (I), wherein X1-X6, R5-R7, Z1 and L are as defined in the description. The resent invention also discloses a method for inhibiting the VR1 receptor in mammals using these compounds, a method for controlling pain, urinary incontinence, bladder overactivity, and inflammatory thermal hyperalgesia in mammals, and pharmaceutical compositions including those compounds.

Modulators of 5-HT receptors and methods of use thereof

The present application relates to aryl- and heteroaryl-fused decahydropyrroloazepine, octahydrooxepinopyrrole, octahydropyrrolothiazepine dioxide, decahydrocyclohepta[c]pyrrole, and octahydrocyclohepta[c]pyrrole derivatives of formula (I) wherein R 1 , R 2 , R 3 , R 4 , R 5 , A, Y 1 , Y 2 , and Y 3 are as defined in the specification. The present application also relates to compositions comprising such compounds, processes for making such compounds, and methods of treating disease conditions using such compounds and compositions, and methods for identifying such compounds.