Abstract: The present invention relates to phosphate derivatives of estrogen receptor beta agonists, compositions thereof, preparations thereof, and uses thereof. Formula (I).

Abstract: The present invention provides cycloalkylfused indole, benzothiophene, benzofuran, and indene derivatives, and methods for using them to, for example, treat, prevent and/or ameliorate central nervous system diseases by antagonizing 5-HT1A receptors and modulating serotonin levels.

Abstract: Compounds of formula (I) or pharmaceutically acceptable salts thereof are provided: wherein: A is alkylenyl of 1 to 4 carbon atoms, or alkenylenyl of 2 to 4 carbon atoms; R1 and R2 are, independently, hydrogen or a C5 to C7 aryl optionally substituted with 1 to 2 substituents, independently, selected from the group consisting of —C(O)R3, halogen, cyano, nitro, hydroxyl, C1-C6 alkyl, and C1-C6 alkoxy, with the proviso that at least one of R1 and R2 is not hydrogen; R3 is, independently, hydrogen, —OR4, alkyl, aryl, or heteroaryl; R4 is hydrogen, alkyl, aryl, or heteroaryl; R5 and R6 are, independently, hydrogen, alkyl, hydroxyl, alkoxy, or C5 to C7 aryl; wherein any R3 to R6 group having an aryl or heteroaryl moiety can optionally be substituted on the aryl or heteroaryl moiety with 1 to about 5 substituents, independently, selected from the group consisting of halogen, cyano, nitro, hydroxyl, C1-C6 alkyl, and C1-C6 alkoxy.

Abstract: Compounds of formula (I) or pharmaceutically acceptable salts thereof are provided where at least one of R2 or R3 is not hydrogen. The compounds of the present invention are N-methyl-D-aspartate (NMDA) receptor antagonists and are useful in treating a variety of conditions present in a mammal that benefit from inhibiting the NMDA receptor.

Abstract: The present invention provides cycloalkylfused indole, benzothiophene, benzofuran, and indene derivatives, and methods for using them to, for example, treat, prevent and/or ameliorate central nervous system diseases by antagonizing 5-HT1A receptors and modulating serotonin levels.

Abstract: Compounds of formula (I) or pharmaceutically acceptable salts thereof are provided: wherein: A is alkylenyl of 1 to 4 carbon atoms, or alkenylenyl of 2 to 4 carbon atoms; R1 and R2 are, independently, hydrogen or a C5 to C7 aryl optionally substituted with 1 to 2 substituents, independently, selected from the group consisting of —C(O)R3, halogen, cyano, nitro, hydroxyl, C1-C6 alkyl, and C1-C6 alkoxy, with the proviso that at least one of R1 and R2 is not hydrogen; R3 is, independently, hydrogen, —OR4, alkyl, aryl, or heteroaryl; R4 is hydrogen, alkyl, aryl, or heteroaryl; R5 and R6 are, independently, hydrogen, alkyl, hydroxyl, alkoxy, or C5 to C7 aryl; wherein any R3 to R6 group having an aryl or heteroaryl moiety can optionally be substituted on the aryl or heteroaryl moiety with 1 to about 5 substituents, independently, selected from the group consisting of halogen, cyano, nitro, hydroxyl, C1-C6 alkyl, and C1-C6 alkoxy.

Abstract: Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.

Abstract: 3-Amino chroman and 2-amino tetralin derivatives and compositions containing such compounds are disclosed. Methods of using the 3-amino chroman and 2-amino tetralin compounds and compositions containing such compounds in the treatment of serotonin disorders, such as depression and anxiety, are also disclosed.

Abstract: Compounds of formula (I) or pharmaceutically acceptable salts thereof are provided where at least one of R2 or R3 is not hydrogen. The compounds of the present invention are N-methyl-D-aspartate (NMDA) receptor antagonists and are useful in treating a variety of conditions present in a mammal that benefit from inhibiting the NMDA receptor.

Abstract: Pharmaceutical compositions for intranasal administration are provided that contain at least one compound of formula (I) or a pharmaceutically acceptable salt thereof: and one or more pharmaceutically acceptable additives for forming a composition for intranasal administration. Also provided are methods of treating one or more conditions in a mammal associated with a glutamate abnormality that includes administering intranasally to a mammal a therapeutically effective amount of a compound of formula (I) or a pharmaceutically acceptable salt thereof.

Abstract: Herein is disclosed 6,7,8,9-tetrahydro-10-methylpyrido[1,2-a]indol-9-amines and derivatives, therapeutically acceptable acid addition salts thereof, processes for their preparation, methods of using the derivatives and pharmaceutical compositions. The derivatives are chemically novel agents with cerebroactive and cognition activating properties.

Abstract: Herein is disclosed 6,7,8,9-tetrahydro-10-methylpyrido[1,2-a]indol-9-amines and derivatives, therapeutically acceptable acid addition salts thereof, processes for their preparation, methods of using the derivatives and pharmaceutical compositions. The derivatives are chemically novel agents with cerebroactive and cognition activating properties.