Patent NZ-334271-A (NZ)
Title: Benzopyran derivatives to treat neurological disorders
Inventor: PARSONS ANDREW A
IPC: A61P25/14
Filed: 1997-09-15
Abstract: Benzopyran derivatives of Formula (A) useful for the treatment and/or prophylaxis of degenerative diseases such as Huntingdon's chorea, schizophrenia, neurological deficits associated with AIDS, sleep disorders (including circadian rhythm disorders, insomnia and narcolepsy), tics (e.g. Gilles de la Tourette's syndrome), traumatic brain injury, tinnitus, neuralgia, especially trigeminal neuralgia, neuropathic pain, dental pain, cancer pain, inappropriate neuronal activity resulting in neurodysthesias in diseases such as diabetes, MS and motor neurone disease, ataxias, muscular rigidity (spasticity), temporomandibular joint dysfunction. Wherein;  P is a ring system selected from Formula (I), (II), (III), (IV) or (V); wherein either and b together represent a bond or CH2 or a and b together represent a carbonyl group, a group C=NORF, CHORF or C-O-C(O)-RF, wherein RF is hydrogen or C1-6alkyl; Wherein either J is nitrogen and Ja is a lone pair of electrons, M is carbon and Ma is R5; or J is carbon and M is nitrogen and Ja and Ma are hydrogen; Wherein Z is oxygen or CH2; Wherein, either Y is N and R2 is hydrogen, or Y is C-R1; where: either one of R1 and R2 is hydrogen and the other is selected from the class of hydrogen, C3-8cycloalkyl, C1-6alkyl optionally interrupted by oxygen or substituted by hydroxy, C1-6alkoxy or substituted aminocarbonyl, C1-6alkylcarbonyl, C1-6alkoxycarbonyl, C1-6alkylcarbonyloxy, C1-6alkoxy, nitro, cyano, halo, trifluoromethyl, CF3S, or a group CF3-A-, where A is -CF2-, -CO-, -CH2-, CH(OH), SO2, SO, CH2-O, or CONH, or a group CF2H-A'- where A' is oxygen, sulfur, SO, SO2, CF2 or CFH; trifluoromethoxy, C1-6alkylsulfinyl, perfluoro-C2-6alkylsulfonyl, C1-6alkylsulfonyl, C1-6alkoxysulfinyl, C1-6alkoxysulfonyl, aryl, heteroaryl, arylcarbonyl, heteroarylcarbonyl, phosphono, arylcarbonyloxy, heteroarylcarbonyloxy, arylsulfinyl, heteroarylsulfinyl, arylsulfonyl, heteroarylsulfonyl in which any aromatic moiety is optionally substituted, C1-6alkylcarbonylamino, C1-6alkoxycarbonylamino, C1-6alkyl-thiocarbonyl, C1-6alkoxy-thiocarbonyl, C1-6 alkyl-thiocarbonyloxy, 1-mercapto-C2-7alkyl, formyl, or aminosulfinyl, aminosulfonyl or aminocarbonyl, any amino moiety being optionally substituted by one or two C1-6alkyl groups, or C1-6alkylsulfinylamino, C1-6alkylsulfonylamino,C1-6alkoxysulfinylamino or C1-6alkoxysulfonylamino, or ethylenyl terminally substituted by C1-6alkylcarbonyl, nitro or cyano, or -C(C1-6alkyl)NOH or -C(C1-6 alkyl)NNH2, Z is N only when Y is C-R1 or Z is C-Ra when Y is N or C-R1; wherein R is hydrogen, halogen, nitro; C1-4alkylcarbonyl, C1-4alkyl; aryl-C1-4alkyl, aryl-C1-4alkenyl, heteroaryl-C1-4alkyl or heteroaryl-C1-4alkenyl, Rb is hydrogen, halogen, nitro; C1-4alkylcarbonyl or C1-4alkyl; and in which any aryl or heteroaryl or alkyl moiety associated with Ra or Rb are optionally substituted; R5 is C1-6alkylcarbonyloxy, benzoyloxy, ONO2, benzyloxy, phenyloxy or C1-6alkoxy and R6 and R9 are hydrogen or R5 is hydroxy and R6 and Rg are independently hydrogen or C1-2alkyl; RX is shown as Formula (VI) in which, R11 and R12 are independently selected from hydrogen, alkyl, haloalkyl, cycloalkyl, aralkyl, cyano, nitro, COR13, CONHR13, CONR13R14 or halo where R13 and R14 are independently selected from hydrogen, alkyl, haloalkyl, aryl, aralkyl, cycloalkyl or (cycloalkyl)alkyl.