Abstract: This invention is directed to a compound of formula (I): wherein R1, R2 and R3 are as defined herein, a pharmaceutical composition comprising the compound, intermediates and processes for making said compounds, and the use of the compound to treat allergic and/or inflammatory disorders, particularly disorders such as allergic rhinitis, asthma, chronic obstructive pulmonary disease (COPD) and age-related macular degeneration (AMD).

Abstract: This invention is directed to a compound of formula (1): wherein R1, R2 and R3 are as defined herein, a pharmaceutical composition comprising the compound, intermediates and processes for making said compounds, and the use of the compound to treat allergic and/or inflammatory disorders, particularly disorders such as allergic rhinitis, asthma, chronic obstructive pulmonary disease (COPD) and age-related macular degeneration (AMD).

Abstract: This invention is directed to a compound of formula (I): wherein R1, R2 and R3 are as defined herein, a pharmaceutical composition comprising the compound, intermediates and processes for making said compounds, and the use of the compound to treat allergic and/or inflammatory disorders, particularly disorders such as allergic rhinitis, asthma, chronic obstructive pulmonary disease (COPD) and age-related macular degeneration (AMD).

Abstract: This invention is directed to a compound of formula (I): wherein R1, R2 and R3 are as defined herein, a pharmaceutical composition comprising the compound, intermediates and processes for making said compounds, and the use of the compound to treat allergic and/or inflammatory disorders, particularly disorders such as allergic rhinitis, asthma, chronic obstructive pulmonary disease (COPD) and age-related to macular degeneration (AMD).

Abstract: This invention is directed to a compound of formula (I): wherein R1, R2 and R3 are as defined herein, a pharmaceutical composition comprising the compound, intermediates and processes for making said compounds, and the use of the compound to treat allergic and/or inflammatory disorders, particularly disorders such as allergic rhinitis, asthma, chronic obstructive pulmonary disease (COPD) and age-related macular degeneration (AMD).

Abstract: This invention is directed to a compound of formula (I): wherein R1, R2 and R3 are as defined herein, a pharmaceutical composition comprising the compound, intermediates and processes for making said compounds, and the use of the compound to treat allergic and/or inflammatory disorders, particularly disorders such as allergic rhinitis, asthma, chronic obstructive pulmonary disease (COPD) and age-related macular degeneration (AMD).

Abstract: This invention is directed to a compound of formula (I): wherein R1, R2 and R3 are as defined herein, a pharmaceutical composition comprising the compound, intermediates and processes for making said compounds, and the use of the compound to treat allergic and/or inflammatory disorders, particularly disorders such as allergic rhinitis, asthma, chronic obstructive pulmonary disease (COPD) and age-related macular degeneration (AMD).

Abstract: This invention is directed to a compound of formula (I): wherein R1, R2 and R3 are as defined herein, a pharmaceutical composition comprising the compound, intermediates and processes for making said compounds, and the use of the compound to treat allergic and/or inflammatory disorders, particularly disorders such as allergic rhinitis, asthma, chronic obstructive pulmonary disease (COPD) and age-related macular degeneration (AMD).

Abstract: An improved synthesis method for making diazaindoles using a Chichibabin cyclization is disclosed. In particular, this method is useful for making the compound of Formula I.

Abstract: An improved chemical synthesis for intermediates of compounds having useful biological activity is disclosed, where the use of PBr3 is employed as a reagent for a selective ring opening of cyclopropylcarbinols to give bromopropylidene products which are highly selectively the E isomer.

Abstract: The invention relates to heterocyclic substituted amide derivatives that display selective binding to dopamine D3 receptors. In another aspect, the invention relates to a method for treating central nervous system disorders associated with the dopamine D3 receptor activity in a patient in need of such treatment comprising administering to the subject a therapeutically effective amount of said compounds for alleviation of such disorder. The central nervous system disorders that may be treated with these compounds include Psychotic Disorders, Substance Dependence, Substance Abuse, Dyskinetic Disorders (e.g. Parkinson's Disease, Parkinsonism, Neuroleptic-Induced Tardive Dyskinesia, Gilles de la Tourette Syndrome and Huntington's Disease), Dementia, Anxiety Disorders, Sleep Disorders, Circadian Rhythm Disorders and Mood Disorders.

Abstract: The invention relates to heterocyclic substituted amide derivatives that display selective binding to dopamine D3 receptors. In another aspect, the invention relates to a method for treating central nervous system disorders associated with the dopamine D3 receptor activity in a patient in need of such treatment comprising administering to the subject a therapeutically effective amount of said compounds for alleviation of such disorder. The central nervous system disorders that may be treated with these compounds include Psychotic Disorders, Substance Dependence, Substance Abuse, Dyskinetic Disorders (e.g. Parkinson's Disease, Parkinsonism, Neuroleptic-Induced Tardive Dyskinesia, Gilles de la Tourette Syndrome and Huntington's Disease), Dementia, Anxiety Disorders, Sleep Disorders, Circadian Rhythm Disorders and Mood Disorders.

Abstract: This invention relates to a process for the preparation of a product of the formula ##STR1## wherein R, R.sup.1, R.sup.2, X and m are defined within which process comprises(a) contacting a compound of Formula II ##STR2## wherein R.sup.3 is loweralkyl, with a reagent selective from the group consisting of aluminum chloride, hydrobromic acid and boron tribromide followed by tartaric acid to afford a compound of Formula III ##STR3## wherein R, X and m are as defined above; (b) contacting the reaction mixture containing compound of Formula IV ##STR4## wherein R.sup.4 is hydrogen or loweralkyl in the presence of a carboxylic acid of the formulaR.sup.5 COOHwherein R.sup.5 is loweralkyl to afford a compound of formula V ##STR5## wherein R, R.sup.4, X and m are as above; contacting the reaction mixture containing the compound of Formula V obtained in step(b) with a compound of the formulaR.sup.1 R.sup.2 NHwherein R.sup.1 and R.sup.2 are as above; and isolating the product of Formula I.

Abstract: This application relates to a new process for the preparation of a product of the formula ##STR1## wherein R is loweralkyl;R.sup.1 is hydrogen, loweralkyl, lowercycloalkyl, lowercycloalkylloweralkyl, lowerbicycloalkyl, aryl or arylloweralkyl;R.sup.2 is loweralkyl, lowercycloalkyl, lowercycloalkylloweralkyl, lowerbicycloalkyl, aryl or arylloweralkyl; orR.sup.1 and R.sup.2 taken together with the nitrogen atom to which they are attached from a 3,4-dihydro-2H(1H)-isoquinoline group;X is loweralkyl, loweralkoxy, halogen or trifluoromethyl; andm is 0, 1 or 2;which process comprises(a) contacting a compound of formula II ##STR2## wherein R, X and m are as defined above and R.sup.3 is loweralkyl, with aluminum chloride followed by tartaric acidto afford a compound of formula III ##STR3## wherein R, X and m are as defined above; (b) contacting the reaction mixture containing the compound of Formula III either(1) with an isocyanate of the formula R.sup.1 NCO and obtaining a product of the formula I wherein R.sup.