Selective serotonin receptor antagonists and therapeutic applications thereof

A pharmaceutical composition comprising,

• a compound of formula
• wherein
• R1 and R2 are selected from the group consisting of —H, —OH, —OCH3, halogen, aryl, alkylaryl, and substituted or unsubstituted branched or unbranched C1-C10 alkyl or alkylaryl, and may be the same or different, and
• X is selected from the group consisting of a) carbon with two —H substituents, b) carbon with one or two lower alkyl substituents, and c) —SO2—,
• and
• a pharmaceutically acceptable carrier.

A method of treating a condition caused by abnormal serotonin activity in a patient in need thereof, comprising the step of

• administering a compound of formula
• wherein
• R1 and R2 are selected from the group consisting of —H, —OH, —OCH3, halogen, aryl, alkylaryl, and substituted or unsubstituted branched or unbranched C1-C10 alkyl or alkylaryl, and may be the same or different, and
• X is selected from the group consisting of a) carbon with two —H substituents, b) carbon with one or two lower alkyl substituents, and c) —SO2—,
• in a quantity to ameliorate symptoms of said condition in said patient;
• and wherein said condition is selected from the group consisting of depression, anxiety, schizophrenia, schizoaffective disorder, an eating disorder, and a sleep disorder.

A method of blocking a 5HT2 receptor in a patient in need thereof, comprising the step of

• identifying a patient that would benefit from blocking of the 5HT2 receptor, and
• administering to said patient a compound of formula
• wherein
• R1 and R2 are selected from the group consisting of —H, —OH, —OCH3, halogen, aryl, alkylaryl, and substituted or unsubstituted branched or unbranched C1-C10 alkyl or alkylaryl, and may be the same or different, and
• X is selected from the group consisting of a) carbon with two —H substituents, b) carbon with one or two lower alkyl substituents, and c) a heteroatom or heteroatomic group selected from the group consisting of —O—;
• —S—;
• and —SO2—,
• in a quantity to sufficient to block said 5HT2 receptor, wherein said method is carried out to treat a condition selected from the group consisting of depression, anxiety, schizophrenia, schizoaffective disorder, an eating disorder, and a sleep disorder.

A method of blocking an H1 receptor in a patient in need thereof, comprising the step of

• identifying a patient that would benefit from blocking of the H1 receptor, and
• administering to said patient a compound of formula
• wherein
• R1 and R2 are selected from the group consisting of —H, —OH, —OCH3, halogen, aryl, alkylaryl, and substituted or unsubstituted branched or unbranched C1-C10 alkyl or alkylaryl, and may be the same or different, and
• X is selected from the group consisting of a) carbon with two —H substituents, b) carbon with one or two lower alkyl substituents, and c) a heteroatom or heteroatomic group selected from the group consisting of —O—;
• —S—;
• and —SO2—,
• in a quantity to sufficient to block said 5HT2 receptor, wherein said method is carried out to treat a condition selected from the group consisting of depression, anxiety, schizophrenia, schizoaffective disorder, an eating disorder, and a sleep disorder.

A method of blocking both a 5HT2 receptor and an H1 receptor in a patient in need thereof, comprising the step of

• identifying a patient that would benefit from blocking of the 5HT2 receptor and the H1 receptor, and
• administering to said patient a compound of formula
• wherein
• R1 and R2 are selected from the group consisting of —H, —OH, —OCH3, halogen, aryl, alkylaryl, and substituted or unsubstituted branched or unbranched C1-C10alkyl or alkylaryl, and may be the same or different, and
• X is selected from the group consisting of a) carbon with two —H substituents, b) carbon with one or two lower alkyl substituents, and c) a heteroatom or heteroatomic group selected from the group consisting of —O—;
• —S—;
• and —SO2—, in a quantity to sufficient to block said 5HT2 receptor wherein method is carried out to treat a condition selected from the group consisting of depression, anxiety, schizophrenia, schizoaffective disorder, an eating disorder, and a sleep disorder.

A compound having the formula

• wherein
• R1 is selected from the group consisting of —OH, —OCH3, halogen, aryl, alkylaryl, and substituted or unsubstituted branched or unbranched C1-C10 alkyl or alkylaryl, and
• R2 is selected from the group consisting of —H, —OH, —OCH3, halogen, aryl, alkylaryl, substituted or unsubstituted branched or unbranched C1-C10 alkyl, substituted or unsubstituted branched or unbranched C1-C10 alkylaryl and may be the same or different, and
• X is selected from the group consisting of a) carbon with two —H substituents, b) carbon with one or two lower alkyl substituents, and c) a heteroatom or heteroatomic group selected from the group consisting of —O—;
• —S—;
• and —SO2—.

A pharmaceutical composition comprising,

• a compound of formula
• wherein
• R1 is selected from the group consisting of —OH, —OCH3, halogen, aryl, alkylaryl, and substituted or unsubstituted branched or unbranched C1-C10 alkyl or alkylaryl, and
• R2 is selected from the group consisting of —H, —OH, —OCH3, halogen, aryl, alkylaryl, substituted or unsubstituted branched or unbranched C5-C10 alkyl, substituted or unsubstituted branched or unbranched C1-C10 alkylaryl and may be the same or different, and
• X is selected from the group consisting of a) carbon with two —H substituents, b) carbon with one or two lower alkyl substituents, and c) a heteroatom or heteroatomic group selected from the group consisting of —O—;
• —S—;
• and —SO2—;
• and
• a pharmaceutically acceptable carrier.

A compound having the formula

• wherein
• R1 is selected from the group consisting of —H, —OH, —OCH3, halogen, aryl, alkylaryl, and substituted or unsubstituted branched or unbranched C1-C10 alkyl or alkylaryl, and
• R2 is selected from the group consisting of —OH, —OCH3, halogen, aryl, alkylaryl, substituted or unsubstituted branched or unbranched C5-C10 alkyl, substituted or unsubstituted branched or unbranched C1-C10 alkylaryl and may be the same or different, and
• X is selected from the group consisting of a) carbon with two —H substituents, b) carbon with one or two lower alkyl substituents, and c) a heteroatom or heteroatomic group selected from the group consisting of —O—;
• —S—;
• and —SO2—.

A pharmaceutical composition comprising,

• a compound of formula
• wherein
• R1 is selected from the group consisting of —H, —OH, —OCH3, halogen, aryl, alkylaryl, and substituted or unsubstituted branched or unbranched C1-C10 alkyl or alkylaryl, and
• R2 is selected from the group consisting of —H, —OH, —OCH3, halogen, aryl, alkylaryl, substituted or unsubstituted branched or unbranched C5-C10 alkyl, substituted or unsubstituted branched or unbranched C1-C10 alkylaryl and may be the same or different, and
• X is selected from the group consisting of a) carbon with two —H substituents, b) carbon with one or two lower alkyl substituents, and c) a heteroatom or heteroatomic group selected from the group consisting of —O—;
• —S—;
• and —SO2—,
• and
• a pharmaceutically acceptable carrier.