Abstract: The present invention relates to new, efficient processes for the preparation of 5-(-2-oxyazolylalkylthio)-2-azacycloalkanoylaminothiazole compounds of formula I or a pharmaceutically acceptable salt thereof, wherein: R is alkyl, aryl or heteroaryl; R1, R2, R3, R4 and R5 are each independently hydrogen, alkyl, aryl or heteroaryl; R6 and R7 are each independently hydrogen, alkyl, aryl, heteroaryl, halogen, hydroxy or alkoxy; R8 is hydrogen, alkyl, aryl, heteroaryl, CONR9, R10, COR11 or COOR12; R9, R10, R11 and R12 are each independently hydrogen, alkyl or aryl; m equals 0 to 5; and n equals 0 to 5, which are novel, potent inhibitors of cyclin dependent kinases (cdks). The present invention further concerns new key intermediate compounds, a quaternary ammonium salt of formula III? and a 2-oxazolylalkyl derivative of formula IX.

Abstract: Novel processes for the preparation of imidazoquinoxalinones, heterocyclic-substituted imidazopyrazinones, imidazoquinoxalines and heterocyclic-substituted imidazopyrazines are described.

Abstract: The present invention relates to new, efficient processes for the preparation of 5-(-2-oxyazolylalkylthio)-2-azacycloalkanoylaminothiazole compounds of formula I 1

Abstract: The present invention relates to new, efficient processes for the preparation of 5-(2-oxazolylalkylthio)-2-arylacetylaminothiazole compounds of formula I: 1

Abstract: The present invention relates to new, efficient processes for the preparation of 5-(2-oxazolylalkylthio)-2-azacycloalkanoylaminothiazole compounds of formula I or a pharmaceutically acceptable salt thereof, wherein: R is alkyl, aryl or heteroaryl; R1, R2, R3, R4 and R5 are each independently hydrogen, alkyl, aryl or heteroaryl; R6 and R7 are each independently hydrogen, alkyl, aryl, heteroaryl, halogen, hydroxy or alkoxy; R8 is hydrogen, alkyl, aryl, heteroaryl, CONR9R10, COR11 or COOR12; R9, R10, R11 and R12 are each independently hydrogen, alkyl or aryl; m equals 0 to 5; and n equals 0 to 5, which are novel, potent inhibitors of cyclin dependent kinases (cdks). The present invention further concerns new key intermediate compounds, a quaternary ammonium salt of formula III′ and a 2-oxazolylalkyl derivative of formula IX.

Abstract: The present invention relates to new, efficient processes for the preparation of 5-(2-oxazolylalkylthio)-2-arylacetylaminothiazole compounds of formula I: or a pharmnaceutically acceptable salt thereof, wherein: R1, R2, R4, R5, R6, R8, R9, R12 and R13 are each independently hydrogen, alkyl, aryl or heteroaryl; R3, R7, R10 and R11 are each independently hydrogen, alkyl, aryl, heteroaryl, halogen, hydroxy or alkoxy; and X is CH or N, which are novel, potent inhibitors of cyclin dependent kinases (cdks). The present invention also concerns a new process for the preparation of formylarylacetates and formylarylacetic acids.

Abstract: The present invention provides an improved process for the preparation of N-(substituted phenyl)-3-alkyl-, aryl- and heteroarylsulfonyl-2-hydroxy-2-alkyl- and haloalkylpropanamide compounds of formula I that exhibit antiandrogenic activity and are useful in the treatment of malignant or benign prostatic disease or of androgen dependent disease conditions such as acne, hirsutism or seborrhea.

Abstract: The present invention relates to new, efficient processes for the preparation of 5-(2-oxazolylalkylthio)-2-azacycloalkanoylaminothiazole compounds of formula I 1

Abstract: The present invention provides an improved process for the preparation of N-(substituted phenyl)-3-alkyl-, aryl- and heteroarylsulfonyl-2-hydroxy-2-alkyl- and haloalkylpropanamide compounds of formula I 1

Abstract: The present invention relates to new, efficient processes for the preparation of 5-(2-oxazolylalkylthio)-2-azacycloalkanoylaminothiazole compounds of formula I or a pharmaceutically acceptable salt thereof, wherein: R is alkyl, aryl or heteroaryl; R1, R2, R3, R4 and R5 are each independently hydrogen, alkyl, aryl or heteroaryl; R6 and R7 are each independently hydrogen, alkyl, aryl, heteroaryl, halogen, hydroxy or alkoxy; R8 is hydrogen, alkyl, aryl, heteroaryl, CONR9R10, COR11 or COOR12; R9, R10, R11 and R12 are each independently hydrogen, alkyl or aryl; m equals 0 to 5; and n equals 0 to 5, which are novel, potent inhibitors of cyclin dependent kinases (cdks). The present invention further concerns new key intermediate compounds, a quaternary ammonium salt of formula III′ and a 2-oxazolylalkyl derivative of formula IX.

Abstract: The present invention relates to new, efficient processes for the preparation of 5-(2-oxazolylalkylthio)-2-arylacetylaminothiazole compounds of formula I: 1

Abstract: The present invention relates to new, efficient processes for the preparation of 5-(2-oxazolylalkylthio)-2-arylacetylaminothiazole compounds of formula I or a pharmaceutically acceptable salt thereof, wherein: R1, R2, R4, R5, R6, R8, R9, R12 and R13 are each independently hydrogen, alkyl, aryl or heteroaryl; R3, R7, R10 and R11 are each independently hydrogen, alkyl, aryl, heteroaryl, halogen, hydroxy or alkoxy; and X is CH or N, which are novel, potent inhibitors of cyclin dependent kinases (cdks). The present invention also concerns a new process for the preparation of formylarylacetates and formylarylacetic acids.

Abstract: The present invention relates to new, efficient processes for the preparation of 5-(2-oxazolylalkylthio)-2-azacycloalkanoylaminothiazole compounds of formula I 1

Abstract: The present invention relates to new, efficient processes for the preparation of 5-(2-oxazolylalkylthio)-2-arylacetylaminothiazole compounds of formula I 1

Abstract: A process is provided for preparing chiral cyclopropane carboxylic acids, preferably of the structure ##STR1## which are intermediates used in preparing acyl guanidine sodium/proton exchange (NHE) inhibitors.

Abstract: A novel process for the production of tertiary amines by reductive alkylation of second amine using hydrosilane and a Lewis acid is disclosed. The novel process has applications in the preparation of imidazole-containing benzodiazepines, inhibitors of farnesyl protein transferase.

Abstract: Antibacterial activity is exhibited by novel compounds having the formula ##STR1## where R.sub.1, R.sub.2, and M are as defined herein and X is --(CH.sub.2).sub.n -- wherein n is 0, 1, 2, 3 or 4 or CR.sub.3 R.sub.4 wherein R.sub.3 and R.sub.4 are the same or different and each is hydrogen, --CH.sub.3 or --C.sub.2 H.sub.5 or R.sub.3 and R.sub.4 taken together with the carbon atom to which they are attached form a 3, 4, 5, 6 or 7-membered cycloalkyl ring.

Abstract: Antibacterial activity is exhibited by novel compounds having the formula ##STR1## where R.sub.1, R.sub.2, and M are as defined herein and X is --(CH.sub.2).sub.n -- wherein n is 0, 1, 2, 3 or 4 or CR.sub.3 R.sub.4 wherein R.sub.3 and R.sub.4 are the same or different and each is hydrogen, --CH.sub.3 or --C.sub.2 H.sub.5 or R.sub.3 and R.sub.4 taken together with the carbon atom to which they are attached form a 3, 4, 5, 6 or 7-membered cycloalkyl ring. Also described are various intermediates for the preparation of compounds of formula 1.

Abstract: Antibacterial activity is exhibited by novel compounds having the formula ##STR1## where R.sub.1, R.sub.2, and M are as defined herein and X is --(CH.sub.2).sub.n -- wherein n is 0, 1, 2, 3 or 4 or CR.sub.3 R.sub.4 wherein R.sub.3 and R.sub.4 are the same or different and each is hydrogen, --CH.sub.3 or --C.sub.2 H.sub.5 or R.sub.3 and R.sub.4 taken together with the carbon atom to which they are attached form a 3, 4, 5, 6 or 7-membered cycloalkyl ring.

Abstract: The compound [3S(Z)]-3-[[(2-amino-4-thiazolyl)[[2-(hydroxyamino)-2-oxoethoxy]imino]acet yl]amino]-2,2-dimethyl-4-oxo-1-azetidinyl sulfate has gram-positive and gram-negative activity and good oral absorption.