Abstract: The present invention comprises 6-9-Disubstituted 2-[trans-(4-aminocyclohexyl]aminopurines that are useful in inhibiting cyclin dependent kinases, particularly cdk-2. The present invention also provides a method of preventing apoptosis in neuronal cells and a method of inhibiting the development of neoplasms.

Abstract: The present invention comprises 6-9-Disubstituted 2-[trans-(4-aminocyclohexyl]aminopurines that are useful in inhibiting cyclin dependent kinases, particularly cdk-2. The present invention also provides a method of preventing apoptosis in neuronal cells and a method of inhibiting the development of neoplasms.

Abstract: The present invention relates to compounds of the formula wherein X is N3, NH2, NHR, N(R)2, CN, SH, SR, or OR1; R is C1-C4 alkyl or (CH2)n—&phgr;; n is an integer 0, 1, 2, 3 or 4; &phgr; is a phenyl group unsubstituted or substituted with from 1 to 3 substituents, each substituent is independently selected from the group consisting of C1-C4 alkyl, C1-C4 alkoxy, halogen, CF3, OCF3, OH, CN, NO2 or NH2; R1 is C1-C4 alkyl or (CH2)m—NR2R3; m is an integer 1, 2, 3 or 4; R2 and R3 are each independently C1-C4 fluorinated akyl or cycloalkyl; The X substituent on the cyclopentanyl ring is in the TRANS configuration relative to the bicyclic substituent; Y is nitrogen; Z1 and Z2 are each independently hydrogen, halogen or NH2; and ---- represents a singe or double bond; or pharmaceutically acceptable salts thereof, compositions comprising such compounds, and methods of treatment comprising administering of such compounds.

Abstract: The present invention provides novel compounds of the formula (I) wherein R is selected from the group consisting of R2, R2NH—, or R3R4N—R5- wherein R2 is selected from the group consisting of C9-C12 alkyl, Z is selected from the group consisting of phenyl, heterocycle, cycloalkyl, and naphthanlene; and M is selected from the group consisting of hydrogen, C1-C4 alkyl, and wherein each C9-C12 alkyl or Z is optionally substituted with 1 to 3 substituents, which may be the same or different, and which are selected from the group consisting of D, E, wherein each D is independently selected from the group consisting of trifluoromethyl, trifluoromethoxy, and C1-C4 alkoxy; each E is independently selected from the group consisting of Hal, OH, and C1-C8 alkyl; R3 and R4 are selected from the group consisting of hydrogen, C1-C4 alkyl and (CH2)y-phenyl, wherein y is an integer 0-8, with the proviso that R3 and R4 not both be hydrogen

Abstract: This invention relates to Trans cyclopentanyl purine analogs of the formula (1) wherein the substituent in the 3-position on the cyclopentanyl ring is in the Trans configuration relative to the bicyclic substituent, Y3, Y5 Y7, Y9 are each nitrogen and Y8 is a CH group, R is a hydrogen, a C1-C7 alkyl acyl or aryl acyl, Q is NH2, halogen or hydrogen, Z is hydrogen, halogen, or NH2; or a pharmaceutically-acceptable salt thereof, and to their use as immunosuppressants.

Abstract: The present invention relates to novel 9-N-bicyclic nucleoside agents which are useful as selective inhibitors of proinflammatory cytokines.

Abstract: The present invention provides novel compounds of the formula (I) wherein R is selected from the group consisting of R2, R2NH—, or H2N—R3— wherein R2 is selected from the group consisting of C1-C8 alkyl and  wherein Z is selected from the group consisting of phenyl, heterocycle and cycloalkyl, each R4 is independently hydrogen or C1-C4 alkyl, and n is an integer 1-8; wherein each C1-C8 alkyl and Z is optionally substituted with 1 to 3 substituents, which may be the same or different, selected from the group consisting of Ha1, OH, and C1-C4 alkyl; R3 is C1-C8 alkylene; and R1 is selected from the group consisting of cyclopentyl and isopropyl, and the pharmaceutically acceptable salts, optical isomers, and hydrates thereof. In addition, the present invention provides a method of inhibiting cell cycle progression. More specifically, the present invention provides a method of inhibiting cyclin dependent kinases, particularly cdk-2.

Abstract: The present invention relates to novel carbocyclic nucleoside agents which are useful as selective inhibitors of proinflammatory cytokines.

Abstract: This invention relates to Trans cyclopentanyl purine analogs of the formula (1) ##STR1## wherein the substituent in the 3-position on the cyclopentanyl ring is in the Trans configuration relative to the bicyclic substituent,Y.sub.3, Y.sub.5, Y.sub.7, Y.sub.8 and Y.sub.9 are each nitrogen,R is a hydrogen, a C.sub.1 -C.sub.7 alkyl acyl or aryl acyl,Q is NH.sub.2, halogen or hydrogen,Z is hydrogen, halogen, or NH.sub.2 ;or a pharmaceutically-acceptable salt thereof, and to their use as immunosuppressants.

Abstract: This invention relates to Trans cyclopentanyl purine analogs of the formula (1) ##STR1## wherein the substituent in the 3-position on the cyclopentanyl ring is in the Trans configuration relative to the bicyclic substituent,Y.sub.3, Y.sub.5 and Y.sub.9 are each nitrogen and Y.sub.7 and Y.sub.8 are a CH group,R is a hydrogen, a C.sub.1 -C.sub.7 alkyl acyl or aryl acyl,Q is NH.sub.2, halogen or hydrogen,Z is hydrogen, halogen, or NH.sub.2 ;or a pharmaceutically-acceptable salt thereof, and to their use as immunosuppressants.

Abstract: This invention relates to novel Trans cyclopentanyl purine analogs of the formula (1) ##STR1## wherein the substituent in the 3-position on the cyclopentanyl ring is in the Trans configuration relative to the bicyclic substituent,Y.sub.3 and Y.sub.8 are CH, Y.sub.5, Y.sub.7 and Y.sub.9 are each independently nitrogen,R is a hydrogen, a C.sub.1 -C.sub.7 alkyl acyl or aryl acyl,Q is NH.sub.2, halogen or hydrogen,Z is hydrogen, halogen, or NH.sub.2 ;or a pharmaceutically-acceptable salt thereof, and to their use as immunosuppressants.

Abstract: This invention relates to Trans cyclopentanyl purine analogs of the formula (1) ##STR1## wherein the substituent in the 3-position on the cyclopentanyl ring is in the Trans configuration relative to the bicyclic substituent,Y.sub.3, Y.sub.5 Y.sub.7, Y.sub.9 are each nitrogen and Y.sub.8 is a CH group,R is a hydrogen, a C.sub.1 -C.sub.7 alkyl acyl or aryl acyl,Q is NH.sub.2, halogen or hydrogen,Z is hydrogen, halogen, or NH.sub.2 ;or a pharmaceutically-acceptable salt thereof, and to their use as immunosuppressants.

Abstract: This invention relates to novel Trans cyclopentanyl purine analogs of the formula (1) ##STR1## wherein the substituent in the 3-position on the cyclopentanyl ring is in the Trans configuration relative to the bicyclic substituent, Y.sub.3 and Y.sub.8 are CH, Y.sub.5, Y.sub.7 and Y.sub.9 are each independently nitrogen,R is a hydrogen, a C.sub.1 -C.sub.7 alkyl acyl or aryl acyl,Q is NH.sub.2, halogen or hydrogen,Z is hydrogen, halogen, or NH.sub.2 ;or a pharmaceutically-acceptable salt thereof, and to their use as immunosuppressants.

Abstract: This invention relates to Trans cyclopentanyl purine analogs of the formula (1) ##STR1## wherein the substituent in the 3-position on the cyclopentanyl ring is in the Trans configuration relative to the bicyclic substituent,Y.sub.3, Y.sub.5, Y.sub.7, Y.sub.8 and Y.sub.9 are each nitrogen,R is a hydrogen, a C.sub.1 -C.sub.7 alkyl acyl or aryl acyl,Q is NH.sub.2, halogen or hydrogen,Z is hydrogen, halogen, or NH.sub.2 ;or a pharmaceutically-acceptable salt thereof, and to their use as immunosuppressants.

Abstract: This invention relates to Trans cyclopentanyl purine analogs of the formula (1) ##STR1## wherein the substituent in the 3-position on the cyclopentanyl ring is in the Trans configuration relative to the bicyclic substituent,Y.sub.3, Y.sub.5 and Y.sub.9 are each nitrogen and Y.sub.7 and Y.sub.8 are a CH group,R is a C.sub.1 -C.sub.7 alkyl acyl or aryl acyl,Q is NH.sub.2, halogen or hydrogen,Z is hydrogen, halogen, or NH.sub.2 ;or a pharmaceutically-acceptable salt thereof, and to their use as immunosuppressants.

Abstract: This invention relates to methods of effecting immunosuppression and inhibiting tumor necrosis factor .alpha. in a patient in need thereof comprising administering to said patient an effective immunosuppressive amount of a compound of the formula ##STR1## wherein the hydroxy substituent on the cyclopentanyl ring is in the CIS configuration relative to the bicyclic substituent,Y.sub.3 is N, Y.sub.7, Y.sub.8 and Y.sub.9 are each independently nitrogen or a CH group,Q is NH.sub.2, halogen or hydrogen, andZ is hydrogen, halogen, or NH.sub.2 ;or a pharmaceutically-acceptable salt thereof. Also presented are pharmaceutical compositions comprising compounds of the same formula.

Abstract: This invention relates to a method of effecting immunosuppression in a patient in need thereof comprising administering an effective amount of a compound of the formula (1) ##STR1## wherein the hydroxy substituent on the cyclopentenyl ring is in the CIS configuration relative to the bicyclic substituent,Y.sub.3, Y.sub.7, Y.sub.8 and Y.sub.9 are each independently nitrogen or a CH group,Q is NH.sub.2, halogen or hydrogen, andZ is hydrogen, halogen, or NH.sub.2 ;or a pharmaceutically-acceptable salt thereof.

Abstract: This invention relates to a method of effecting immunosuppression in a patient in need thereof comprising administering an effective amount of a compound of the formula (1) ##STR1## wherein the hydroxy substituent on the cyclopentenyl ring is inthe CIS configuration relative to the bicyclic substituent,Y.sub.3, Y.sub.7, Y.sub.8 and Y.sub.9 are each independently nitrogen or a CH group,Q is NH.sub.2, halogen or hydrogen, andZ is hydrogen, halogen, or NH.sub.2 ;or a pharmaceutically-acceptable salt thereof.

Abstract: This invention relates to carbocyclic adenosine compounds of the formula (1) ##STR1## wherein the hydroxy substituent on the cyclopentanyl ring is in the CIS configuration relative to the bicyclic substituent,Y.sub.3, Y.sub.7, Y.sub.8 and Y.sub.9 are each independently nitrogen or a CH group,Q is NH.sub.2, halogen or hydrogen, andZ is hydrogen, halogen, or NH.sub.2 ;or a pharmaceutically-acceptable salt thereof, and to their use as immunosuppressants.

Abstract: This invention relates to a method of effecting immunosuppression in a patient in need thereof comprising administering an effective amount of a compound of the formula (1) ##STR1## wherein the hydroxy substituent on the cyclopentenyl ring is in the CIS configuration relative to the bicyclic substituent,Y.sub.3, Y.sub.7, Y.sub.8 and Y.sub.9 are each independently nitrogen or a CH group,Q is NH.sub.2, halogen or hydrogen, andZ is hydrogen, halogen, or NH.sub.2 ;or a pharmaceutically-acceptable salt thereof.