Abstract: Substituted pyridoindoles for incorporation in pharmaceutical compositions employed in the treatment of various diseases correspond to formula (I) wherein R1 is H or optionally substituted alkyl; R2, R3, R4 are each independently selected from H, —O-alkyl, —S-alkyl, alkyl, halo, —CF3, and —CN; G is —CR12R13—NR5— or —NR5—CR12R13; R5; is H, optionally substituted alkyl, optionally substituted heterocycle, —C(?O)—R6, —C(?O)—O—R7, or —C(?O)—NR19R20; R6 and R7 are each optionally substituted alkyl or optionally substituted heterocycle; R8, R9, R10, R11, R12, R13, R19 and R20 are each independently selected from H or optionally substituted alkyl; R14 and R15 are each independently H or halogen; L is —CH2—O—, —CH2CH2—, —CH?CH— or a bond; and B is aryl or heteroaryl or cycloalkyl; with the proviso that, when L is a direct bond, B cannot be unsubstituted heteroaryl or heteroaryl monosubstituted with fluorine.

Abstract: Provided herein are compounds of the formula (I): wherein R1-R8 are as described herein, R4 being aryl or heteroaryl Such compounds are particularly useful in the treatment of a disorder which is created by or is dependent upon decreased availability of serotonin, norepinephrine or dopamine.

Abstract: Compounds of formulae I and II: are disclosed as 5-HT3 inhibitors. Those compounds are useful in treating CINV, IBS-D and other diseases and conditions.

Abstract: The present invention discloses processes for preparing piperidine derivative compounds of the formula: wherein n is 0 or 1; R1 is hydrogen or hydroxy; R2 is hydrogen; or, when n is 0, R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2, provided that when n is 1, R1 and R2 are each hydrogen; R3 is —COOH or —COOR4; R4 is an alkyl or aryl moiety; A, B, and D are the substituents of their rings, each of which may be different or the same, and are selected from the group consisting of hydrogen, halogens, alkyl, hydroxy, alkoxy, and other substituents.

Abstract: Compounds of formulae I and II: are disclosed as 5-HT3 inhibitors. Those compounds are useful in treating CINV, IBS-D and other diseases and conditions.

Abstract: Processes are disclosed for preparing piperidine derivative compounds of the formulae I, II or III:

Abstract: Processes are disclosed for preparing piperidine derivative compounds of the formulae I, II or III: The processes involve reacting a compound of formula Ia, IIa or IIIa with isobutyrate or an isobutyrate equivalent.

Abstract: Processes are disclosed for preparing piperidine derivative compounds of the formulae I, II or III: The processes involve reacting a compound of formula Ia, IIa or IIIa with isobutyrate or an isobutyrate equivalent.

Abstract: Processes are disclosed for preparing piperidine derivative compounds of the formulae I, II or III:

Abstract: The present invention relates to a group of aza-anthrapyrazole compounds having antitumor activity, and processes for their preparation. Compositions containing the aza-anthrapyrazole compounds and methods of treating tumors and cancer in mammals with the compounds of the present invention are also disclosed.

Abstract: The compounds of the present invention are 2,6,9-trisubstituted purine derivatives which are inhibitors of cyclin/cdk complexes. The compounds of the current invention also are potent inhibitors of human cellular proliferation. As such, the compounds of the present invention constitute pharmaceutical compositions with a pharmaceutically acceptable carrier. Such compounds are useful in treating a disorder mediated by elevated levels of cell proliferation in a mammal compared to a healthy mammal by administering to such mammal an effective amount of the compound. Examples of the compounds of the present invention are represented by the following chemical structures: with X, Y, D, Q, V, A, R1, R2, R3, R4, and n1 defined herein.

Abstract: The compounds of the present invention are 2,6,9-trisubstituted purine inhibitors of cyclin/cdk complexes. The compounds also are potent inhibitors of human cellular proliferation. As such, the compounds constitute pharmaceutical compositions with a pharmaceutically acceptable carrier. Such compounds are useful in inhibiting cellular proliferation in a mammal by administering to such mammal an effective amount of the compound. An example is represented by the following chemical structure: wherein: X=N; R2= phenyl; substituted phenyl; 1-naphthyl; 2-naphthyl; heterocycles; or substituted heterocycle; Y= H; OR1; NHR1; NHC(O)R3; NHSO2R3; NHC(O)NHR3; NHC(O)R5; or NHC(O)OR6; and R1, R3, and R4 are defined herein.

Abstract: Provided herein are compounds of the formula (I): wherein R1-R8 are as described herein, R4 being aryl or heteroaryl Such compounds are particularly useful in the treatment of a disorder which is created by or is dependent upon decreased availability of serotonin, norepinephrine or dopamine.

Abstract: Highly specific biocatalytic reactions have been used to create a population of taxol derivatives.

Abstract: The present invention relates to a method for preparing piperidine derivative compounds by converting, with a piperidine compound, regioisomers having the formula: where Z is —CG1G2G3; G1, G2, and G3 are the same or different and are selected from the group consisting of OR8, SR8, and NR8R9; and R8, and R9 are the same or different and are selected from the group consisting of hydrogen, an alkyl moiety, and an aryl moiety.

Abstract: The present invention relates to a method for preparing piperidine derivative compounds by converting, with a piperidine compound, regioisomers having the formula: where Z is or and where m is 1 or 4-6; Q and Y are the same or different and are selected from the group consisting of O, S, and NR5; R6 and R7 are the same or different and are selected from the group consisting of hydrogen, an alkyl moiety, an aryl moiety, OR8, SR8, and NR8R9; X3 is halogen, OR15, SR15, NR15R16, OSO2R15, or NHSO2R15; R5, R8, R9, R15, and R16 are the same or different and are selected from the group consisting of hydrogen, an alkyl moiety, and an aryl moiety; and A is a substituent of its ring and is selected from the group consisting of hydrogen, halogens, alkyl, hydroxy, alkoxy, and other substituents.

Abstract: The present invention relates to a method for preparing piperidine derivative compounds by converting, with a piperidine compound, regioisomers having the formula: where Z is —CG1G2G3; G1, G2, and G3 are the same or different and are selected from the group consisting of OR8, SR8, and NR8R9; X3 is halogen, OR15, SR15, NR15R16, OSO2R15, or NHSO2R15; R8, R9, R15, and R16 are the same or different and are selected from the group consisting of hydrogen, an alkyl moiety, and an aryl moiety; and A is a substituent of its ring and is selected from the group consisting of hydrogen, halogens, alkyl, hydroxy, alkoxy, and other substituents.

Abstract: The present invention relates to a method for preparing piperidine derivative compounds by converting, with a piperidine compound, regioisomers having the formula: where Z is and where m is 1 or 3-6; Q and Y are the same or different and are selected from the group consisting of O, S, and NR5; R6 and R7 are the same or different and are selected from the group consisting of hydrogen, an alkyl moiety, an aryl moiety, OR8, SR8, and NR8R9; and R5, R8, and R9 are the same or different and are selected from the group consisting of hyrogen, an alkyl moiety, and an aryl moiety.

Abstract: An apparatus and method for simultaneously loading a plurality of small items such as small items into the wells of a multiple well microtiter plate which includes a small item loading unit and a small item insertion device. The small item loading device includes a top plate having a plurality of openings positioned to register with the microtiter plate wells and a closure unit to close the openings on one side of the top plate. The small item insertion device includes a base mounting a plurality of plunger pins which each register with a well in the microtiter plate. A movable deck unit is mounted in spaced relationship above the base and is provided with apertures, each of which receives a plunger pin. The small item loading device rests on the deck unit and the closure unit opens the openings therein to drop small items into the apertures over the pins. The deck unit is moved toward the base to cause the pins to enter the wells of a microtiter plate and seat the small items.

Abstract: A method for derivatizing a compound having a hydroxyl group by back to back acylation is provided. The compound is acylated with a bifunctional acyl donor in the presence of a hydrolase to form an activated acyl ester or carbonate. Preferably the bifunctional acylating donor is a di(vinyl) ester or carbonate. The activated acyl ester or carbonate is then used to acylate a nucleophile in the presence of a lipase. The method of the invention provides regioselective enzymatic acylation of the base compound.