Abstract: The present invention relates to personal care and pharmaceutical compositions comprising an alcohol, a personal care polymer, and an alcohol-masking perfumery component. These compositions can be applied to the skin, hair, or mucosa. The alcohol-masking perfumery component substantially reduces both the alcohol odor or aroma and the stinging or burning sensation in the nose or throat due to the alcohol when the compositions are sprayed or atomized.
Abstract: This invention relates to a new use discovered for the compound known as Aplidine (dehydrodidemnin B) which has the following structure: Aplidine has been found to be a potent L-type calcium channel enhancer in the human heart. This effect makes Aplidine a very useful drug for the treatment of congestive heart failure, as well as useful for the treatment of atrial fibrillation.
Abstract: A mixed micellar pharmaceutical formulation includes a micellar proteinic pharmaceutical agent, an alkali metal lauryl sulphate, alkali metal salicylate, a pharmaceutically acceptable edetate and at least one absorption enhancing compounds. The absorption enhancing compounds are selected from the group consisting of lecithin, hyaluronic acid, pharmaceutically acceptable salts of hyaluronic acid, octylphenoxypolyethoxyethanol, glycolic acid, lactic acid, chamomile extract, cucumber extract, oleic acid, linolenic acid, borage oil, evening of primrose oil, trihydroxy oxo cholanylglycine, glycerin, polyglycerin, lysine, polylysine, triolein and mixtures thereof. The amount of each absorption enhancing compound is present in a concentration of from 1 to 10 wt./wt. % of the total formulation, and the total concentration of absorption enhancing compounds are less than 50 wt./wt. % of the formulation.
Abstract: The present invention is to provide a prophylactic/therapeutic composition for the secondary cataract comprising a polypeptide having an inhibitory activity of cell adhesion and a lactic acid-glycolic acid polymer.The composition of the present invention inhibits adhesion and extension of lens epithelial cells onto the posterior lens capsule after extraction of lens and is useful as a prophylactic/therapeutic composition for the secondary cataract in the clinical point of view.
Abstract: The present invention provides peptides having pure somatostatin antagonist activity. Also provided are methods for increasing the release of growth hormone, insulin, glucagon and gastric enzymes in mammals and a method for the enhancement of immune function and growth in mammals.
Type:
Grant
Filed:
March 3, 1998
Date of Patent:
July 20, 1999
Assignee:
American Cyanamid Company
Inventors:
William Robert Baumbach, Richard A. Houghten
Abstract: The present invention is directed to teicoplanin derivatives of the following general formula, wherein R.sup.1 and R.sup.2 are as defined in the specification. ##STR1## These derivatives are useful as antibiotics for the control of gram-positive bacteria.
Type:
Grant
Filed:
April 1, 1998
Date of Patent:
June 29, 1999
Assignee:
Eli Lilly and Company
Inventors:
Robin David Grey Cooper, Nancy June Snyder
Abstract: The combination of a metabolic rate modifying agent (e.g., a .beta..sub.3 adrenergic receptor agonist) and a feeding behavior modifying agent (e.g., a NPY5 antagonist) is useful in the treatment of obesity and diabetes, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients. Methods of treating obesity and diabetes are also described.
Type:
Grant
Filed:
October 30, 1997
Date of Patent:
June 1, 1999
Assignee:
Merck & Co., Inc.
Inventors:
Roy G. Smith, Margaret A. Cascieri, Euan MacIntyre, Douglas J. MacNeil, John G. Menke
Abstract: The present invention relates to an analog of Neuropeptide FF (e.g., daY8Ra) and to a pharmaceutical composition containing same. The invention further relates to methods of using the analog to attenuate the effects of drug addiction, drug tolerance, drug dependence or of abstinence syndrome.
Abstract: The present invention relates to methods of purifying proteins having surface active, electron-rich amino acids using an aqueous two phase system. The methods include the use of salts and inert hydrophobic molecules, such as polymers, to produce the aqueous two phase system and the use a polymer-chelator-metal complex to purify the target proteins.
Abstract: The invention concerns pharmaceutically useful trifluoromethyl ketone substituted di-, tri- and tetra-peptide derivatives of the formulae Ia, Ib, Ic set out hereinafter, and salts thereof which are inhibitors of human leukocyte elastase. Also described herein are pharmaceutical compositions containing a peptide derivative and processes and intermediates for use in the manufacture of the peptide derivatives.
Abstract: A method of reducing side-effects associated with administering oxygen-carrying proteins to mammals is disclosed. The method includes:a) reacting an oxygen-carrying protein with a substantially non-antigenic polymer to form a oxygen-carrying protein-substantially non-antigenic polymer conjugate; andb) administering the oxygen-carrying protein-substantially non-antigenic polymer conjugate to a mammal in need of the oxygen-carrying protein. Preferred oxygen-carrying proteins include recombinantly prepared hemoglobins and preferred non-antigenic polymers include polyethylene glycol.
Abstract: The present invention provides a protein or polypeptide substance having at least one amino group bonded to a polyethyleneglycolosy group represented by the following general formula;R.sub.1 --(OCH.sub.2 CH.sub.2).sub.n --O--(wherein R.sub.1 represents an optionally substituted cholesteryl group; and n represents a positive integer which is arbitrarily variable), and a method for producing said the protein or polypeptide.The present invention also provides a reactive polyethyleneglycol derivative as an intermediated for above the method.The chemically modified protein or polypeptide of the present invention never impairs bonding with a receptor and has a high plysiological activity. Then, a behaviors in vivo of these substance is improved. Now medical substances or drugs having a high pharmacological activity can be developed by using these substance.
Abstract: This invention is a novel synthesis of BCA-peptides (BCA: bifunctional chelating agents). In this method, the starting material--Fmoc-Thr(ol)-Terephthal-Acetal-Amide Resin is coupled with the various amino acids. The straight peptide-resin of D-Phe-Cys(Trt)-Phe-D-Trp(Boc)-Lys(Boc)-Thr(tBu)-Cys(Trt)-Thr(ol)-Terephtha l-Acetal-Amide Resin was obtained. This compound reacted with iodine to give disulfide-containing peptide resin of ##STR1## Cleavage of the peptide from the resin was achieved by TFA. The cleavaged peptide was protected by the reaction of octreotide with di-t-butyldicarbonate. BCA was coupled to the selectively protected octreotide. This product was obtained by reaction of protected BCA-peptides with TFA. The final product was labeled by radioisotope .sup.111 InCl.sub.3 for tumor imaging radiopharmaceuticals.
Abstract: The present invention describes novel radiopharmaceuticals of formula (I): ##STR1## wherein J, K, L, and M, are amino acids or derivatives thereof and R', R.sup.1, R.sup.2 and n are as defined herein, that are radiolabeled cyclic compounds containing chelators which act as antagonists of the platelet glycoprotein IIb/IIIa complex, methods of using the same as imaging agents for the diagnosis of arterial and venous thrombi, and novel reagents for the preparation of the same and kits comprising the reagents.
Abstract: This invention provides processes for producing novel cyclic peptide compounds, which comprise cultivating Ctenomyces serratus FERM BP-5731 and then isolating the cyclic peptide compounds from the fermentation broth. The compounds produced by these processes include a cyclic peptide compound of the following formula (I): ##STR1## The present invention also relates to a pharmaceutical composition comprising the same, which is useful in the treatment of severe pain, detoxication of narcotics dependency or acute narcotics intoxication or the like.
Abstract: Novel backbone cyclized peptide analogs are formed by means of bridging groups attached via the alpha nitrogens of amino acid derivatives to provide novel non-peptidic linkages. Novel building units disclosed are N.sup..alpha. (.omega.-functionalized) amino acids constructed to include a spacer and a terminal functional group. One or more of these N.sup..alpha. (.omega.-functionalized) amino acids are incorporated into a peptide sequence, preferably during solid phase peptide synthesis. The reactive terminal functional groups are protected by specific protecting groups that can be selectively removed to effect either backbone-to-backbone or backbone-to-side chain cyclizations. The invention is exemplified by backbone cyclized bradykinin antagonists having biological activity. Further embodiments of the invention are somatostatin analogs having one or two ring structures involving backbone cyclization.
Type:
Grant
Filed:
December 5, 1996
Date of Patent:
March 16, 1999
Assignees:
Peptor Ltd., Yissum Research Development Co. of the Hebrew University
Inventors:
Chaim Gilon, Doron Eren, Irina Zeltser, Alon Seri-Levy, Gal Bitan, Dan Muller
Abstract: The present invention relates to a process for the aromatic sulfonylation, sulfenylation, thiocyanation and phosphorylation of cyclic depsipeptides having 6 to 24 ring atoms which are synthesized from .alpha.-hydroxycarboxylic acids and .alpha.-amino acids and contain at least one phenyl radical, characterized in that these cyclic depsipeptides are reacted with sulfonylating, sulfenylating, thiocyanating or phosphorylating agents, optionally in the presence of catalysts, auxiliaries and/or diluents, to novel thus-obtained compounds, and to their use as endoparasiticides.
Type:
Grant
Filed:
April 10, 1997
Date of Patent:
February 23, 1999
Assignee:
Bayer Aktiengesellschaft
Inventors:
Jurgen Scherkenbeck, Andrew Plant, Peter Jeschke, Achim Harder, Norbert Mencke
Abstract: Oligopeptides which comprise amino acid sequences that are recognized and proteolytically cleaved by free prostate specific antigen (PSA) are described. Also described are assays which comprise such oligopeptides useful for determining free PSA protease activity in vitro and in vivo. Therapeutic agents which comprise conjugates of such oligopeptides and known cytotoxic agents are also described.
Type:
Grant
Filed:
October 6, 1995
Date of Patent:
February 2, 1999
Assignee:
Merck & Co., Inc.
Inventors:
Deborah DeFeo-Jones, Victor M. Garsky, Dong-Mei Feng, Raymond E. Jones, Allen I. Oliff
Abstract: The present invention relates to peptides and polypeptides derived from the submaxillary gland of the rat. In particular, the present invention discloses a purified peptide of formula:X--His--Asn--Pro--Yin which X represents a Gln or Pro--Glu residue and Y represents an OH group or a residue of a basic amino acid. The present invention also relates to corresponding polyclonal and monoclonal antibodies as well as corresponding hybridomas. The products of the present invention are useful for therapeutic, diagnosis and detection purposes.