Abstract: The present invention relates to compounds of the Formula (I), or a pharmaceutically acceptable salt, pharmaceutical preparation, or pharmaceutical composition thereof, and their use for the treatment of pain, inflammatory disease, neuropathy, dermatological disorders, pulmonary conditions, and cough, as well as inhibiting the Transient Receptor Potential A1 ion channel (TRPA1).

Abstract: The present invention relates to compounds of the Formula (I), or a pharmaceutically acceptable salt, pharmaceutical preparation, or pharmaceutical composition thereof, and their use for the treatment of pain, inflammatory disease, neuropathy, dermatological disorders, pulmonary conditions, and cough, as well as inhibiting the Transient Receptor Potential A1 ion channel (TRPA1).

Abstract: The present invention relates to compounds of the Formula (I), or a pharmaceutically acceptable salt, pharmaceutical preparation, or pharmaceutical composition thereof, and their use for the treatment of pain, inflammatory disease, neuropathy, dermatological disorders, pulmonary conditions, and cough, as well as inhibiting the Transient Receptor Potential A1 ion channel (TRPA1).

Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.

Abstract: The present invention provides 2,4-disubstituted pyrimidine compounds useful as kinase inhibitors, pharmaceutically acceptable compositions thereof, and methods of using the same.

Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.

Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.

Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.

Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.

Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.

Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.

Abstract: Disclosed are new methods of making camptothecin and camptothecin analogs defined by Formula I: ##STR1## wherein R is loweralkyl; R.sub.1 is H, loweralkyl, loweralkoxy, or halo; and R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are each independently H, amino, hydroxy, loweralkyl, loweralkoxy, loweralkylthiol, di(loweralkyl)amino, cyano, methylenedioxy, formyl, nitro, halo, trifluoromethyl, aminomethyl, azido, amido, hydrazino, or any of the twenty standard amino acids bonded to the A ring via the amino-nitrogen atom. The methods comprise cyclizing a compound of Formula IV: ##STR2## wherein X is Br or I, and Y is H, by an Aryl-to-Aryl free radical coupling reaction to yield a compound of Formula I. Compounds of Formula IV are made by alkylating a compound of Formula III: ##STR3## wherein R is loweralkyl and Y is H with a compound of Formula II-x: ##STR4## wherein X is a Br or I and V is hydroxy, by a Mitsunobu reaction to yield the compound of Formula IV.

Abstract: Disclosed are new methods of making camptothecin and camptothecin analogs defined by Formula I: ##STR1## wherein R is loweralkyl; R.sub.1 is H, loweralkyl, loweralkoxy, or halo; and R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are each independently H, amino, hydroxy, loweralkyl, loweralkoxy, loweralkylthiol, di(loweralkyl)amino, cyano, methylenedioxy, formyl, nitro, halo, trifluoromethyl, aminomethyl, azido, amido, hydrazino, or any of the twenty standard amino acids bonded to the A ring via the amino-nitrogen atom. The methods comprise cyclizing a compound of Formula IV: ##STR2## wherein X is Br or I, and Y is H, by an Aryl-to-Aryl free radical coupling reaction to yield a compound of Formula I. Compounds of Formula IV are made by alkylating a compound of Formula III: ##STR3## wherein R is loweralkyl and Y is H with a compound of Formula II-x: ##STR4## wherein X is a Br or I and V is hydroxy, by a Mitsunobu reaction to yield the compound of Formula IV.

Abstract: Compounds of Formula I ##STR1## are made in accordance with the following scheme: ##STR2## wherein R may be loweralkyl; R.sub.1 may be H, loweralkyl, loweralkoxy, or halo; R.sub.2, R.sub.3, R.sub.4, and R.sub.5 may each independently be H, amino, hydroxy, loweralkyl, loweralkoxy, loweralkylthio, di(loweralkyl)amino, cyano, methylenedioxy, formyl, nitro, halo, trifluoromethyl, aminomethyl, azido, amido, hydrazino, or any of the twenty standard amino acids bonded to the A ring via the amino-nitrogen atom; Y is H and W and X are halogen. Also disclosed are novel processes for making starting materials for the scheme given above, and novel intermediates employed in these processes.

Abstract: Processes for making compounds of Formulae XIV, XV, and XVII ##STR1## wherein R.sub.6 is lower alkyl, R.sub.7 is lower alkyl, R is lower alkyl, Y is H, F or Cl, R.sub.8 is a compound of Formula XVIII ##STR2## wherein n is 1, 2, or 3, R.sub.11 is C.sub.1 -C.sub.4 alkyl and R.sub.12 is the same as R.sub.11, or R.sub.11 and R.sub.12 together form cyclopentane or cyclohexane, and R.sub.13 is:(a) phenyl substituted 1 to 5 times with C.sub.3 -C.sub.7 secondary alkyl or C.sub.4 -C.sub.7 tertiary alkyl, or(b) selected from the group consisting of naphthyl, anthryl, and phenanthryl optionally substituted 1 to 5 times with C.sub.3 -C.sub.7 secondary alkyl or C.sub.4 -C.sub.7 tertiary alkyl groups,R.sub.10 is C.sub.6 -C.sub.10 alkyl, aryl or alkyl aryl,and Y is H, F or Cl,are disclosed. These processes can be used to make optically enhanced and optically pure forms of the compounds, which are useful in the making of camptothecin and analogs thereof.

Abstract: Processes for making compounds of Formulae XIV, XV, and XVII ##STR1## wherein R.sub.6 is lower alkyl, R.sub.7 is lower alkyl, R is lower alkyl, Y is H, F or Cl, R.sub.8 is a compound of Formula ##STR2## wherein n is 1, 2, or 3, R.sub.11 is C.sub.1 -C.sub.4 alkyl and R.sub.12 is the same as R.sub.11, or R.sub.11 and R.sub.12 together form cyclopentane or cyclohexane, and R.sub.13 is:(a) phenyl substituted 1 to 5 times with C.sub.3 -C.sub.7 secondary alkyl or C.sub.4 -C.sub.7 tertiary alkyl, or(b) selected from the group consisting of naphthyl, anthryl, and phenanthryl optionally substituted 1 to 5 times with C.sub.3 -C.sub.7 secondary alkyl or C.sub.4 -C.sub.7 tertiary alkyl groups,R.sub.10 is C.sub.6 -C.sub.10 alkyl, aryl or alkyl aryl, and Y is H, F or Cl, are disclosed. These processes can be used to make optically enhanced and optically pure forms of the compounds, which are useful in the making of camptothecin and analogs thereof.

Abstract: Processes for making compounds of Formulae XIV, XV, and XVII ##STR1## wherein R.sub.6 is lower alkyl, R.sub.7 is lower alkyl, R is lower alkyl, Y is H, F or Cl, R.sub.8 is a compound of Formula XVIII ##STR2## wherein n is 1, 2, or 3, R.sub.11 is C.sub.1 -C.sub.4 alkyl and R.sub.12 is the same as R.sub.11, or R.sub.11 and R.sub.12 together form cyclopentane or cyclohexane, and R.sub.13 is:(a) phenyl substituted 1 to 5 times with C.sub.3 -C.sub.7 secondary alkyl or C.sub.4 -C.sub.7 ; tertiary alkyl, or(b) selected from the group consisting of naphthyl, anthryl, and phenanthryl optionally substituted 1 to 5 times with C.sub.3 -C.sub.7 secondary alkyl or C.sub.4 -C.sub.7 tertiary alkyl groups,R.sub.10 is C.sub.6 -C.sub.10 alkyl, aryl or alkyl aryl,and Y is H, F or Cl,are disclosed. These processes can be used to make optically enhanced and optically pure forms of the compounds, which are useful in the making of camptothecin and analogs thereof.

Abstract: Compounds of Formula I ##STR1## are made in accordance with the following scheme: ##STR2## wherein R may be loweralkyl; R.sub.1 may be H, loweralkyl, loweralkoxy, or halo; R.sub.2, R.sub.3, R.sub.4, and R.sub.5 may each independently be H, amino, hydroxy, loweralkyl, loweralkoxy, loweralkylthio, di(loweralkyl)amino, cyano, methylenedioxy, formyl, nitro, halo, trifluoromethyl, aminomethyl, azido, amido, hydrazino, or any of the twenty standard amino acids bonded to the A ring via the amino-nitrogen atom; Y is H and W and X are halogen. Also disclosed are novel processes for making starting materials for the scheme given above, and novel intermediates employed in these processes.

Abstract: Compounds of Formula I ##STR1## are made in accordance with the following scheme: ##STR2## wherein R may be loweralkyl; R.sub.t may be H, loweralkyl, loweralkoxy, or halo: R.sub.2, R.sub.3, R.sub.4, and R.sub.5 may each independently be H, amino, hydroxy, loweralkyl, loweralkoxy, loweralkylthio, di(loweralkyl)amino, cyano, methylenedioxy, formyl, nitro, halo, trifluoromethyl, aminomethyl, azido, amido, hydrazino, or any of the twenty standard amino acids bonded to the A ring via the amino-nitrogen atom; Y is H and W and X are halogen. Also disclosed are novel processes for making starting materials for the scheme given above, and novel intermediates employed in these processes.

Abstract: Compounds of Formula I ##STR1## are made in accordance with the following scheme: ##STR2## wherein R may be loweralkyl; R.sub.1 may be H, loweralkyl, loweralkoxy, or halo; R.sub.2, R.sub.3, R.sub.4, and R.sub.5 may each independently be H, amino, hydroxy, loweralkyl, loweralkoxy, loweralkylthio, di(loweralkyl)amino, cyano, methylenedioxy, formyl, nitro, halo, trifluoromethyl, aminomethyl, azido, amido, hydrazino, or any of the twenty standard amino acids bonded to the A ring via the amino-nitrogen atom; Y is H and W and X are halogen. Also disclosed are novel processes for making starting materials for the scheme given above, and novel intermediates employed in these processes.