Abstract: The invention relates to amino-heteroaryl derivatives having the general Formula I or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same, as well as to the use of these derivatives for the treatment of pain, such as neuropathic pain or inflammatory pain.

Abstract: The present invention relates to derivatives of known active pharmaceutical compounds. These derivatives are differentiated from the parent active compound by virtue of being redox derivatives of the active compound. This means that one or more of the functional groups in the active compound has been converted to another group in one or more reactions which may be considered to represent a change of oxidation state. We refer to these compounds generally as redox derivatives. The derivatives of the invention may be related to the original parent active pharmaceutical compound by only a single step transformation, or may be related via several synthetic steps including one or more changes of oxidation state.

Abstract: The present invention relates to derivatives of known active pharmaceutical compounds. These derivatives are differentiated from the parent active compound by virtue of being redox derivatives of the active compound. This means that one or more of the functional groups in the active compound has been converted to another group in one or more reactions which may be considered to represent a change of oxidation state. We refer to these compounds generally as redox derivatives. The derivatives of the invention may be related to the original parent active pharmaceutical compound by only a single step transformation, or may be related via several synthetic steps including one or more changes of oxidation state. In certain cases, the functional group obtained after two or more transformations may be in the same oxidation state as the parent active compound (and we include these compounds in our definition of redox derivatives).

Abstract: The invention relates to amino-heteroaryl derivatives having the general Formula I or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same, as well as to the use of these derivatives for the treatment of pain, such as neuropathic pain or inflammatory pain.

Abstract: The present invention relates to isoxazole-3-carboxamide derivative having the general Formula (I), or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same, as well as to the use of said isoxazole-3-carboxamide derivatives for the treatment of TRPV1 mediated disorders, such as acute and chronic pain disorders, acute and chronic neuropathic pain, acute and chronic inflammatory pain, respiratory diseases, and lower urinary tract disorders.

Abstract: The invention relates to (pyrrolidin-2-yl)phenyl derivatives having the general Formula I wherein R1 is (C1-4)alkyl, halo(C1-4)alkyl, (C1-4)alkyloxy, or halo(C1-4)alkyloxy; R2 is H, (C1-4)alkyl, halo(C1-4)alkyl, (C1-4)alkyloxy, halo(C1-4)alkyloxy or halogen; R3 is H, (C1-4)alkyl or halo(C1-4)alkyl; R4 is H, (C1-4)alkyl or halo(C1-4)alkyl; R5 is H, (C1-4)alkyl or halo-(C1-4)-alkyl; or R4 and R5, when bonded to the same carbon atom, can together with the carbon atom form a spiro(C3-6)cycloalkyl group, optionally substituted with halogen; R6 is H, (C1-4)alkyl, halo(C1-4)alkyl, (C1-4)alkyloxy, halo(C1-4)alkyloxy or halogen; or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same, as well as to the use of these (pyrrolidin-2-yl)phenyl derivatives for the treatment of pain, such as neuropathic pain or inflammatory pain.

Abstract: The present invention relates to isoxazole-5-carboxamide derivative having the general Formula (I), or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same, as well as to the use of said isoxazole-5-carboxamide derivatives for the treatment of TRPV1 mediated disorders, such as acute and chronic pain disorders, acute and chronic neuropathic pain, acute and chronic inflammatory pain, respiratory diseases, and lower urinary tract disorders.

Abstract: The present invention relates to isoxazole-3-carboxamide derivative having the general Formula I or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same, as well as to the use of said isoxazole-3-carboxamide derivatives for the treatment of TRPV1 mediated disorders, such as acute and chronic pain disorders, acute and chronic neuropathic pain, acute and chronic inflammatory pain, respiratory diseases, and lower urinary tract disorders.

Abstract: The present invention relates to isoxazole-3-carboxamide derivative having the general Formula (I), or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same, as well as to the use of said isoxazole-3-carboxamide derivatives for the treatment of TRPV1 mediated disorders, such as acute and chronic pain disorders, acute and chronic neuropathic pain, acute and chronic inflammatory pain, respiratory diseases, and lower urinary tract disorders.

Abstract: The invention relates to (pyrrolidin-2-yl)phenyl derivatives having the general Formula I wherein R1 is (C1-4)alkyl, halo(C1-4)alkyl, (C1-4)alkyloxy, or halo(C1-4)alkyloxy; R2 is H, (C1-4)alkyl, halo(C1-4)alkyl, (C1-4)alkyloxy, halo(C1-4)alkyloxy or halogen; R3 is H, (C1-4)alkyl or halo(C1-4)alkyl; R4 is H, (C1-4)alkyl or halo(C1-4)alkyl; R5 is H, (C1-4)alkyl or halo-(C1-4)-alkyl; or R4 and R5, when bonded to the same carbon atom, can together with the carbon atom form a spiro(C3-6)cycloalkyl group, optionally substituted with halogen; R6 is H, (C1-4)alkyl, halo(C1-4)alkyl, (C1-4)alkyloxy, halo(C1-4)alkyloxy or halogen; or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same, as well as to the use of these (pyrrolidin-2-yl)phenyl derivatives for the treatment of pain, such as neuropathic pain or inflammatory pain.

Abstract: The invention relates 2-(benzimidazol-1-yl)-N-(4-phenylthiazol-2-yl) acetamide derivatives having the general Formula I wherein R1 is H, (C1-4)alkyl, (C1-4)alkyloxy or halogen; R2 represents 1-3 substituents selected from H, (C1-4)alkyl (optionally substituted with 1 or more halogens), (C1-4)alkyl-oxy (optionally substituted with 1 or more halogens), halogen, CF3 or cyano; or a pharmaceutically acceptable salt thereof; to pharmaceutical compositions comprising the same and to the use of said 2-(benzimidazol-1-yl)-N-(4-phenylthiazol-2-yl)acetamide derivatives in the treatment of TRPV1 mediated disorders.

Abstract: The invention relates to 2-(benzimidazol-1-yl)-acetamide bisaryl derivative having the general Formula I wherein n is 0 or 1; Ar1 represents a diradical derived from a 5- or-6-membered aromatic ring, optionally comprising 1-3 heteroatoms selected from N, O and S, said ring being optionally substituted with (C1-4)alkyl, (C1-4)alkyloxy, halogen, CF3 or cyano; Ar2 represents a 6-membered aryl ring, optionally comprising 1-3 nitrogen atoms, said ring being optionally substituted with 1-3 substituents selected from (C1-4)alkyl (optionally substituted with 1 or more halogens), (C1-4)alkyloxy (optionally substituted with 1 or more halogens), di(C1-4)alkylamino, halogen, CF3 or cyano; or a pharmaceutically acceptable salt thereof; to pharmaceutical compositions comprising the same and to the use of said 2-(benzimidazol-1-yl)-acetamide bisaryl derivatives in the treatment of TRPV1 mediated disorders.

Abstract: The invention relates to 2-(benzimidazol-1-yl)-acetamide bisaryl derivative having the general Formula I wherein n is 0 or 1; Ar1 represents a diradical derived from a 5- or-6-membered aromatic ring, optionally comprising 1-3 heteroatoms selected from N, O and S, said ring being optionally substituted with (C1-4)alkyl, (C1-4)alkyloxy, halogen, CF3 or cyano; Ar2 represents a 6-membered aryl ring, optionally comprising 1-3 nitrogen atoms, said ring being optionally substituted with 1-3 substituents selected from (C1-4)alkyl (optionally substituted with 1 or more halogens), (C1-4)alkyloxy (optionally substituted with 1 or more halogens), di(C1-4)alkylamino, halogen, CF3 or cyano; or a pharmaceutically acceptable salt thereof; to pharmaceutical compositions comprising the same and to the use of said 2-(benzimidazol-1-yl)-acetamide bisaryl derivatives in the treatment of TRPV1 mediated disorders.

Abstract: The invention relates 2-(benzimidazol-1-yl)-N-(4-phenylthiazol-2-yl)acetamide derivatives having the general Formula I wherein R1 is H, (C1-4)alkyl, (C1-4)alkyloxy or halogen; R2 represents 1-3 substituents selected from H, (C1-4)alkyl (optionally substituted with 1 or more halogens), (C1-4)alkyloxy (optionally substituted with 1 or more halogens), halogen, CF3 or cyano; or a pharmaceutically acceptable salt thereof; to pharmaceutical compositions comprising the same and to the use of said 2-(benzimidazol-1-yl)-N-(4-phenylthiazol-2-yl)acetamide derivatives in the treatment of TRPV1 mediated disorders.

Abstract: Disclosed is a 6-mercapto-cyclodextrin derivative having a general formula (I, ) wherein m is 0-7 and n is 1-8 and m+n=7 or 8; R is (C1-6) alkylene, optionally substituted with 1-3 OH groups, or (CH2)o-phenylene-CH2)p—; o and p are independently 0-4; X is COOH, CONHR3, NHCOR2, SO2OH, PO(OH)2, O(CH2—CH2—O)q—H, OH or tetrazol-5-yl: R2 is H or (C1-3)alkyl; R2 is carboxyphenyl; q is 1-3; or pharmaceutically acceptable salts thereof. The 6-mercaptocyclodextrin derivative is highly suitable for use in the reversal of drug-induced neuromuscular block.

Abstract: Disclosed is a 6-mercapto-cyclodextrin derivative having a general formula (I) wherein m is 0-7 and n is 1-8 and m+n=7 or 8; R is (C1-6) alkylene, optionally substituted with 1-3 OH groups, or (CH2)0-phenylene-CH2)p—; o and p are independently 0-4; X is COOH, CONHR3, NHCOR2, SO2OH, PO(OH)2, O(CH2—CH2—O)q—H, OH or tetrazol-5-yl: R1 is H or (C1-3)alkyl; R2 is carboxyphenyl; q is 1-3; or pharmaceutically acceptable salts thereof. The 6-mercaptocyclodextrin derivative is highly suitable for use in the reversal of drug-induced neuromuscular block.

Abstract: Disclosed is a 6-mercapto-cyclodextrin derivative having general formula (I) wherein m is 0-7 and n is 1-8 and m+n=7 or 8; R is (C1-6)alkylene, optionally substituated with 1-3 OH groups, or (CH2)o-phenylene-(CH2)p—; o and p are independently 0-4; X is COOH, CONHR1, NHCOR2, SO2OH, PO(OH)2, O(CH2—CH2—O)q—H, OH or tetrazol-5-yl; R1 is H or (C1-3)alkyl; R2 is carboxyphenyl; q is 1-3; or pharmaceutically acceptable salts thereof. The 6-mercaptocyclodextrin derivative is highly suitable for use in the reversal of drug-induced neuromuscular block.

Abstract: Disclosed is a 6-mercapto-cyclodextrin derivative having general formula (I) wherein m is 0-7 and n is 1-8 and m+n=7 or 8; R is (C1-6)alkylene, optionally substituated with 1-3 OH groups, or (CH2)o-phenylene-(CH2)p—; o and p are independently 0-4; X is COOH, CONHR1, NHCOR2, SO2OH, PO(OH)2, O(CH2—CH2—O)q—H, OH or tetrazol-5-yl; R1 is H or (C1-3)alkyl; R2 is carboxyphenyl; q is 1-3; or pharmaceutically acceptable salts thereof. The 6-mercaptocyclodextrin derivative is highly suitable for use in the reversal of drug-induced neuromuscular block.