Abstract: The invention features targeted cytotoxic compounds and methods relating to their therapeutic use for the treatment of neoplasia and other conditions.

Abstract: Disclosed is a series of somatostatin-dopamine chimeric analogs which retain both somatostatin and dopamine activity in vivo. An example is: 6-n-propyl-8?-ergolinglmethylthioacetyl-D-Phe-c(Cys-Tyr-D-Trp-Lys-Abu-Cys)-Thr-NH2.

Abstract: Disclosed is a series of somatostatin-dopamine chimeric analogs which retain both somatostatin and dopamine activity in vivo. An example is: 6-n-propyl-8?-ergolinglmethylthioacetyl-D-Phe-c(Cys-Tyr-D-Trp-Lys-Abu-Cys)-Thr-NH2.

Abstract: The present invention is directed to peptide analogs of chemokine, the pharmaceutically acceptable salts thereof, to methods of using such analogs to treat mammals and to pharmaceutical compositions useful therefor comprising said analogs.

Abstract: The present invention relates to methods and intermediates for chemical synthesis of polypeptides and proteins, and more particularly to methods and intermediates for chemically ligating a peptide fragment containing N-terminal ?-methyl-cysteine (SEQ ID NO: 1) with another peptide fragment having C-terminal thioester to generate a ?-amino-thioester intermediate that spontaneously rearranges to form an amide bond. The invention also relates to methods of synthesizing ?-methyl-cysteine (SEQ ID NO: 1) and its protected forms. Furthermore, the invention relates to converting a ?-methyl-thiazolidine residue to a ?-methyl-cysteine (SEQ ID NO: 1) residue of polypeptides and proteins.

Abstract: Disclosed is a series of somatostatin-dopamine chimeric analogs which retain both somatostatin and dopamine activity in vivo.

Abstract: Disclosed is a series of somatostatin-dopamine chimeric analogs which retain both somatostatin and dopamine activity in vivo.

Abstract: Disclosed is a series of somatostatin-dopamine chimeric analogs which retain both somatostatin and dopamine activity in vivo. An example is: 6-n-propyl-8?-ergolinglmethylthioacetyl-D-Phe-c-(Cys-Tyr-D-Trp-Lys-Abu-Cys)-Thr-NH2.

Abstract: Disclosed is a series of somatostatin-dopamine chimeric analogs which retain both somatostatin and dopamine activity in vivo.

Abstract: Disclosed is a series of somatostatin-dopamine chimeric analogs which retain both somatostatin and dopamine activity in vivo.

Abstract: A family of compounds capable of inhibiting the activity of prenyl transferases. The compounds are covered by the four following formulas Each of the R groups is defined in the disclosure.

Abstract: A family of compounds capable of inhibiting the activity of prenyl transferases.

Abstract: A family of compounds capable of inhibiting the activity of prenyl transferases. The compounds are covered by the four following formulas Each of the R groups is defined in the disclosure.

Abstract: A family of compounds capable of inhibiting the activity of prenyl transferases. The compounds are covered by one of the two following formulas: ##STR1## Each of the R groups is defined in the disclosure.

Abstract: A family of compounds capable of inhibiting the activity of prenyl transferases. The compounds are covered by either of the two following formulas ##STR1## Each of the R groups is defined in the disclosure.

Abstract: Peptide derivatives containing one or more substituents separately linked by an amide, amino or sulfonamide bond to an amino group on either the N-terminal end or side chain of a biologically active peptide moiety. The peptide derivatives have relatively enhanced biological activity when compared to the corresponding peptide alone.

Abstract: A bradykinin analog which contains nine or ten amino acid residues and at least one [CH.sub.2 NH] pseudopeptide bond, the analog being useful as an antagonist or agonist of the naturally occuring bradykinin.

Abstract: Peripheral benzodiazepines (BZDs) are useful in treating disorders caused by abnormal level of peripheral benzodiazepene receptor activity and having, in one aspect, the formula: ##STR1## wherein each X, X.sub.1, X.sub.2, X.sub.3, X.sub.4, X.sub.5, X.sub.6, and X.sub.8, independently, is hydrogen, halogen (F, Cl, Br, I), C.sub.1 -C.sub.4 straight or branched alkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylthio, hydroxy, nitro, cyano, amino, or trifluoromethyl; R.sub.1 =H, C.sub.1 -C.sub.4 alkyl, cyclo C.sub.3 -C.sub.5 alkyl, C.sub.1 -C.sub.4 alkenyl, CH.sub.2 --CO.sub.2 H, or CH.sub.3 --C.dbd.O; R.sub.2 =a member of the group of the formula (Ia) ##STR2## wherein each R.sub.3, R.sub.4, R.sub.8, R.sub.9, R.sub.10 and R.sub.11, independently, can be any of the groups listed as possibilities for X.sub.1 -X.sub.8, and can be attached at any available ring carbon atom, said R.sub.2 group being bonded to (CH.sub.

Abstract: A linear (i.e., non-cyclic) analog of biologically active amphibian bombesin, mammalian gastrin-releasing peptide (GRP), or mammalian growth hormone releasing factor (GRF), having an active site and a binding site responsible for the binding of the peptide to a receptor on a target cell. Cleavage of a peptide bond in the active site of naturally occurring bombesin, GRP, or GRF is unnecessary for in vivo biological activity. The analog has one of the following modifications: (a) a deletion of an amino acid residue within the active site and a modification of an amino acid residue outside of the active site, (b) a replacement of two amino acid residues within the active site with a synthetic amino acid, a .beta.-amino acid, or a .gamma.-amino acid residue, or (c) a non-peptide bond instead of a peptide bond between an amino acid residue of the active site and an adjacent amino acid residue.

Abstract: In general, the invention features compounds having the formula: ##STR1## or a pharmaceutically acceptable salt thereof, wherein AR is an indolyl, quinolyl, naphthyl or a mono- or di- R.sup.1 substituted naphthyl in which R.sup.1 is, independently, an alkyl group having 1-5, inclusive, carbon atoms, an alkoxy group having 1-5, inclusive, carbon atoms, a halogen, amino, hydroxy, nitro, cyano, carboxyl, trifluoromethyl, ethyl carboxylate, or a hydrogen; m is an integer between 0 and 2, inclusive; and A is either ##STR2## where n is an integer between 1 and 5, inclusive, and R.sup.