Abstract: This invention provides a method of attenuating post-surgical catabolic changes and hormonal responses to stress. GLP-1, a GLP-1 analog, or a GLP-1 derivative, is administered at a dose effective to normalize blood glucose.

Abstract: The present invention provides the cDNA sequence encoding bovine dipeptidylaminopeptidase 1. The invention demonstrates that bovine DAP 1 coded by a single cDNA. The mature protein is derived from a single polypeptide consisting of a signal peptide, and a major polypeptide which is processed to generate the a subunit, b subunit and g subunit.

Abstract: A method of preventing headache in a human is disclosed which comprises the administration to a human in need thereof of an effective amount of a compound of formula I ##STR1## wherein R.sup.1 and R.sup.3 are, independently, --H, --CH.sub.3, --CO(C.sub.1 -C.sub.6 alkyl), or --COAr, where Ar is optionally substituted phenyl;R.sup.2 is selected from the group consisting of pyrrolidine, piperidine, and hexamethyleneimino; ora pharmaceutically acceptable salt or solvate thereof.

Abstract: The present invention is directed to chemical processes for preparing 2-aryl-6-hydroxy-3-[4-(2-aminoethoxyl)benzoyl]benzoyl]benzo[b]-thiophenes.

Abstract: This invention relates to a chemical intermediate ##STR1## wherein f is 0, 1, 2 or 3, which is useful for the synthesis of a compound of the Formula IX--C(O)--Y--G--R I(wherein X, Y, G and R have the values defined in the description), or a pharmaceutically acceptable salt thereof, which compound of Formula I or salt and pharmaceutical compositions comprising such a compound or salt are useful as thrombin inhibitors, coagulation inhibitors and agents for the treatment of thromboembolic disorders.

Abstract: A method of treatment for human patients with an acquired hypercoagulable state or acquired protein C deficiency associated with sepsis, purpura fulminans, meningococcal sepsis, bone marrow and other transplantations, severe burns, pregnancy, major surgery, severe trauma, or ARDS, which comprises administering activated protein C providing a highly selective therapeutic agent with a low potential for causing bleeding complications.

Abstract: The present invention relates to processes for resolving N-methyl-3(R,S)-hydroxy-3-phenylpropylamine and N,N-dimethyl-3 (R,S) -hydroxy-3-phenylpropylamine with the isomers of mandelic acid and the resulting salts.

Abstract: The present invention provides compounds of formula I and II: ##STR1## wherein X is --O--, --S--, or --NR.sup.5 --;Y is --O--, --S--, --CH.sub.2 --, --Ch.sub.2 CH.sub.2 --, --CH.dbd.CH--, or --NR.sup.5 --;B is --CH.sup.2 -- or --CO--;R.sup.1, R.sup.2, and R.sup.3 are each independently --H, --OH, --O(C.sub.1 -C.sub.4 alkyl), --OCOC.sub.6 H.sub.5, --OCO(C.sub.1 -C.sub.6 alkyl), --OSO.sub.2 (C.sub.4 -C.sub.6 alkyl), --OSO.sub.2 CF.sub.3, Cl, or F;n is 1 or 2;W is CH.sub.2 or C.dbd.O;R.sup.4 is 1-piperidinyl, 2-oxo-1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 2-oxo-1-pyrrolidinyl, 4-morpholino, dimechylamino, diethylamino, or 1-hexamethyieneimino;R.sup.5 is C.sub.1 -C.sub.3 alkyl, --COC.sub.6 H.sub.5, --CO(C.sub.1 -C.sub.6 alkyl), --C(O)OC.sub.6 H.sub.5, --C(O)O(C.sub.1 -C.sub.6 alkyl), --SO.sub.2 (C.sub.1 -C.sub.6 alkyl), --SO.sub.2 C.sub.6 H.sub.5,or --SO.sub.2 CF.sub.3 ; or a pharmaceutically acceptable salt or solvate thereof.

Abstract: The instant invention provides a novel process for preparing benzyl-substituted rhodanine derivatives. Also provided are novel benzyl-substituted thiolamides and benzyl-substituted hemithioacetals. Such compounds are useful as intermediates in preparing the compounds by the process of the instant invention.

Abstract: The invention provides complexes of the formula: ##STR1## wherein X is chloro, hydrogen, vinyl, or --CH.sub.3,Z is CH.sub.2 or S;n is 0-5;Y is phenyl or 1,4-cyclohexadien-1-yl;R.sub.1 and R.sub.2 are hydrogen or hydroxy, with the proviso that R.sub.1 and R.sub.2 are not both hydrogen andR.sub.3 is --COO.sup.-, --COO(C.sub.1 -C.sub.4 alkyl), --NO.sub.2 or ##STR2## wherein R.sub.4 is C.sub.1 -C.sub.4 alkyl.

Abstract: An improved process to make gemcitabine hydrocrhloride, the improvement consisting essentially of making the lactone intermediate, 2-deoxy-2,2-difluoro-D-erythro-pentafuranose-1 ulose-3,5-dibenzoate: ##STR1## from D-erythro-2-Deoxy-2,2-difluoro 4,5-O-(1-ethylpropyl)-idene) pentoic acid tert Butyl ester wherein, the D-erythro-2-deoxy-2,2 difluoro-4,5-O-(1-ethylproyl)-ideno) pentoic acid tert-Butyl ester is prepared by the process of reacting S-tert-butyl difluoroethane thioate with 2,3-O (1-ethylpropylidene)-D-glyceraldehyde, in a solvent and in the presence of a strong base; with the proviso that the process is conducted in the absence of a catalyst and in the absence of a silyl containing compound.

Abstract: This invention provides methods for the treatment or prevention of sleep apnea in a mammal which comprise administering to a mammal in need thereof an effective amount of a compound of formula (I) where R.sup.1 and R.sup.2 are independently selected from the group consisting of hydrogen, methyl, methoxy, chloro, and trifluoromethyl, with the proviso that no more than one of R.sup.1 and R.sup.2 can be hydrogen; and Y is (a), (b), (c), (d), (e), (f), N-R.sup.a, or CH-NR.sup.b R.sub.c, where R.sup.a, R.sup.b, and R.sup.c are independently selected from the group consisting of hydrogen and C.sub.1 -C.sub.6 alkyl; or a pharmaceutically acceptable salt or solvate thereof.

Abstract: The present invention provides antiretroviral methods using the compounds of formula (I)X-X1-P1-Val-Z-Leu-P2-Ywherein:Z is Statine or ACHPA;and when Z is Statine,X is H-Pro-paF, H-Pro-His, Ac-Tyr, Ac-NA, Ac-Trp, Ac-YOM, Ac-Phe, Ac-paF, H-His, Ac-His or Ac-Gly-Tyr-YOM,X1 is Pro Ser or Ac,P1 is Phe, paF or YOM,P2 is Phe or Leu, andY is NH.sub.2, paF--NH.sub.2, His--NH.sub.2, Phe--NH.sub.2 or Tyr-Lue--NH.sub.2,provided that when X1 is Ac then there is no X residue;and when Z is ACHPA,X is H-Pro-His, H-Pro-paF, Ac-paF or Ac-His,P1 is Phe,P2 is Phe, andY is paF--NH.sub.2 and His--NH.sub.2.The invention further provides methods for determining the retroviral protease inhibitory activity of compounds using viral polypeptides made using recombinant DNA techniques.

Abstract: Monoclonal antibodies which react with the human influx peptide transporter are provided. The human influx peptide transporter-reactive antibodies are useful in the purification of influx peptide transporter and in immunoassays to identify agents taken up into the cell by the human influx peptide transporter mechanism. The monoclonal antibodies are also useful for the detection and treatment of carcinomas derived from the gastrointestinal tract and pancreatic duct.

Abstract: A multi-use pen-shaped medication dispensing device made of a plastic material that is recyclable after the contents of the medication cartridge have been exhausted. The device is made of a minimal number of parts, which include a housing, a dial assembly, a generally cylindrical button assembly located within the proximal end of the dial assembly, an internally threaded nut, and an externally threaded leadscrew. The device is arranged so that the dial must be rotated to the zero dose position prior to setting a dose. The device includes a lockout mechanism that prevents the dial from being depressed during dosing. The device further includes a mechanism that limits the maximum dosage that can be dialed up and a mechanism that prevents the user from dialing up a dosage greater than that remaining in the cartridge.

Abstract: A class of substituted phenoxy naphthalene compounds of the structure: ##STR1## where n is 2 or 3; R.sup.1 is hydrogen, hydroxy, C.sub.1 -C.sub.4 alkoxy, phenoxycarbonyl, C.sub.1 -C.sub.6 alkoxycarbonyl, or C.sub.2 -C.sub.6 alkoxy-sulfonyl; R.sup.2 is is hydrogen, hydroxy, C.sub.1 -C.sub.4 alkoxy, phenoxycarbonyl, C.sub.1 -C.sub.6 alkoxycarbonyl, or C.sub.2 -C.sub.6 alkoxy-sulfonyl, or halo; and R.sup.3 is 1-piperidinyl, 1-pyrollidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino; are useful in the treatment of pathological conditions associated with post-menopause including osteoporosis, endometriosis, uterine fibroid disease, cardiovascular disease (particularly hyperlipidemia), and hormonally-dependent cancers (particularly breast and uterine cancer).

Abstract: This invention provides 5-HT.sub.1F agonists of Formula I; ##STR1## where A-B, X, and R are as defined in the specification. The invention also encompasses pharmaceutical formulations employing compounds of Formula I as well as methods of treating conditions associated with 5-HT.sub.1F activation employing these compounds or compositions. The invention also provides intermediates useful for the preparation of the compounds of Formula I.

Abstract: This invention is concerned with improved processes for reductive alkylation of glycopeptide antibiotics. The improvement residing in providing a source of copper which results in the initial production of a copper complex of the glycopeptide antibiotic. Reductive alkylation of this complex favors regioselective alkylation and increased yields. Copper complexes of the glycopeptide antibiotic starting materials and of the alkylated products are also part of the invention.

Abstract: The present invention provides a composition and method for treating pain using Selected Muscarinic Compounds and one or more compounds selected from the group consisting of Nonsteroidal Anti-inflammatory drugs, acetaminophen, opioids, and alpha-adrenergic compounds.

Abstract: The present invention relates to therapeutically active azacyclic or azabicyclic compounds of formula I ##STR1## and to pharmaceutical formulations comprising these compounds and methods of treatment comprising administering these compounds to a subject in need of treatment. The novel oxadiazole compounds, such as (.+-.)-3-butyloxy-4-(1-azabicyclo[2.2.2]octyl-3-oxy)-1,2,5-oxadiazole, are useful in treating central nervous system disorders caused by malfunctioning of the muscarinic cholinergic system.