Abstract: The presence of diverse microorganisms in the gingiva of patients having periodontal disease is very well known to be deleterious to gingival health, and particularly to facilitate the appearance and development of dental cavities. Such microorganisms are always associated with periodontal disease, and if such microorganisms remain unchecked or uncontrolled, extraction of teeth are likely to occur. In the past, the presence of microorganisms in the gingiva of patients with periodontal disease has been periodically and erratically treated with anti-microbial agents, including antibiotics. For anti-microbial agents and antibiotics to be effective in the gingiva, such agents and antibiotics must come into direct contact with microorganisms, and such contact is known to be incomplete, partly because there may be barriers of fluid and tissue which prevent direct contact between the agents and antibiotics with the microorganisms.

Abstract: Antide is the decapeptide, N-Ac-D-2-Nal,D-pClPhe, D-3-Pal, Ser,NicLys, D-NicLys, Leu, ILys, Pro, D-Ala,NH.sub.2 which is an antagonist of luteinizing hormone releasing hormone (LHRH). This decapeptide, like others of the present invention, has high antiovulatory activity (AOA) and releases negligible histamine. Antide is scheduled for scale-up, safety testing and evaluation in the experimental primate and in clinical medicine. Numerous other peptides having structures related to Antide were prepared and tested. These peptides had variations primarily in positions 5, 6, 7, and 8. Of these, N-Ac-D-2-Nal, D-pClPhe,D-3-Pal,Ser,PicLys,cis-DPzACAla,Leu,ILys,Pro,D-Ala-NH.sub.2 was one of the most potent and had higher antiovulatory activity than Antide, i.e. 73%/0.25 ug and 100%/0.5 ug vs. 36%/0.5 ug and 100%/1.0 ug. Antide showed significant, (p<0.001) duration of action, when injected at a dose of 10 ug, 44 hours before 50 ng of the agonist, ?D-3-Qal.sup.6 !-LHRH.

Abstract: LHRH analogs and congeners with high water solubility have been synthesized. These new analogs had 0%-100% antiovulatory activity at a 0.5 .mu.g dosage and 0%-80% at 0.25 .mu.g. The ED.sub.50 for histamine release was 30.5 .mu.g/ml->300 .mu.g/ml.

Abstract: LHRH antagonists similar to antide and congeners with higher water solubility have been synthesized by substitutions in positions 1, 5 or 6 with hydrophilic residues. These peptides have antiovulatory activity with minimal histamine releasing effect.

Abstract: Antide is the decapeptide, N--Ac--D--2--Nal,D--pClPhe, D--3--Pal, Ser,NicLys, D--NicLys, Leu, ILys, Pro, D--Ala,NH.sub.2 which is an antagonist of luteinizing hormone releasing hormone (LHRH). This decapeptide, like others of the present invention, has high antiovulatory activity (AOA) and releases negligible histamine. Antide is scheduled for scale-up, safety testing and evaluation in the experimental primate and in clinical medicine. Numerous other peptides having structures related to Antide were prepared and tested. These peptides had variations primarily in positions 5, 6, 7, and 8. Of these, N--Ac--D--2--Nal, D--pClPhe,D--3--Pal,Ser,PicLys,cis--DpzACAla, Leu,ILys,pro,D--Ala--NH.sub.2 was one of the most potent and had higher antiovulatory activity than Antide, i.e. 73%/0.25 ug and 100%/0.5 ug vs. 36%/0.5 ug and 100%/1.0 ug. Antide showed significant, (p<0.001) duration of action, when injected at a dose of 10 ug, 44 hours before 50 ng of the agonist, [D--3--Qal.sup.6 ]--LHRH.

Abstract: Disclosed are methods for inhibiting the side effects attendant treatment with HMG-CoA reductase inhibitors. Treatment of a patient with and HMG-CoA reductase inhibitor in combination with coenzyme Q.sub.10 provides a reduction in patient cholesterol levels and guards against typical HMG-CoA reductase-inhibitor side effects, most notably liver dysfunction and cardiac dysfunction. The combination of lovastatin, an HMG-CoA reductase inhibitor, and coenzyme Q.sub.10 in ratios of between 1:2 to 1:29 provide significant enhancement of a patient's caridac condition. By way of example, other HMG-CoA reductase inhibitors which may be included in the claimed combinations include pravastatin, compactin, fluvastatin, dalvastatin, simvastatin, BMY 22089, GR-95030, HR-780, CI-981, SQ 33,600, and BMY 22566 and XU-62-320.

Abstract: The present invention comprises the serious side effect of mevinolin to depress body levels of coenzyme Q.sub.10 and to correspondingly depress cardiac function and the circumvention of this side effect by the clinical administration of a formulation of coenzyme Q.sub.10 concommitantly with the administration of the mevinolin.

Abstract: Therapy with a pharmaceutical formulation of coenzyme Q.sub.10 (CoQ.sub.10) of patients with Acquired Immune Deficiency Syndrome, known by the acronym AIDS and of patients with other retroviral diseases including the AIDS-related complex known as ARC is useful to reduce or negate opportunistic infections, adenopathy and other undesirable clinical symptoms. CoQ.sub.10 therapy may be used in conjunction with antibiotic therapy to prevent or suppress secondary opportunistic infections.

Abstract: The objective of the research was the achievement of antagonists of the luteinizing hormone releasing hormone (LHRH) which would have adequate antagonistic activity to prevent ovulation, and yet would not have a pronounced structural feature to release a histamine, in vivo. Some existing antagonists of LHRH produced edema of the face and extremities in rats. This recent recognition of the edematogenic and anaphylactoid activities of an antagonist of LHRH necessitated new structural changes if such antagonists were to be considered for potential use as contraceptive agents in the human. Consequently, 57 peptides have been designed, synthesized and bioassayed toward achieving a potent antagonist which releases negligible histamine.

Abstract: The present invention relates to the use of Coenzyme Q in the treatment of slow muscle degeneration, commonly known to those of skill in the art so a dystrophy or atrophy, and the accompanying cardiac complications typically identified in such patients. Administration of Coenzyme Q, and particularly the analog Coenzyme Q.sub.10 (CoQ.sub.10) to humans increases the pumping of blood by the heart, and thereby increases tissue oxygeneration throughout the body. The net physiological effect halts the progression of muscle deterioration and improves cardiac function. An overall improvement in the quality of life for these human subjects is also observed, said patients reportedly experiencing less fatigue.A method for treating human patients with progressive muscular dystrophies or the neurogenic atrophies with Coenzyme Q.sub.10 (CoQ.sub.10) specifically disclosed. The method is similarly effective for the treatment of any form of muscle degeneration or cardiac muscular dysfunction independently.

Abstract: The present invention comprises a stable and non-toxic coenzyme Q.sub.10 formulation suitable for intravenous administration to an animal to produce clinically effective blood levels of coenzyme Q.sub.10. Clinically effective blood levels of coenzyme Q.sub.10 are generally agreed to be between about 2 ug/ml and about 4 ug/ml. The formulation consists essentially of a clinically accepted fatty emulsion having an oil phase and coenzyme Q.sub.10 dissolved in the oil phase. The formulation preferably contains coenzyme Q.sub.10 at a level between about 7.5 ug/ml and about 30 ug/ml. The clinically accepted fatty emulsion comprises at least one vegetable oil, preferably corn oil, peanut oil, safflower oil, olive oil or soybean oil.

Abstract: The chemical structure of the luteinizing hormone releasing hormone (LHRH) was elucidatd in 1971. Since then, a very large number of international investigators synthesized more than 100 monosubstituted and about 14 disubstituted analogs of LHRH. All of these analogs were synthesized from natural amino acids having the L-configuration. Not one of these approximately 114 analogs showed agonist activity equivalent to that of LHRH. Two of the 114 were about 60% as active, and neither one has had any utility. We have investigated the six individual L-amino acids which occur in positions 5, 7, and 8 of the four naturally occurring LHRH's which exist in porcine/ovine, salmon, and chicken tissue.

Abstract: Two sets of hormonal peptides are synthesized which are super agonists of the lutenizing hormone releasing hormone (LHRH). Chronic administration results in the inhibition of LHRH which is responsible for stimulating cell growth in the testes. One peptide has the D(dextro)-form of a mono-heterocyclic amino acid in position six (D-3-pyridyl-alanine) while the other peptide has a bi-heterocyclic amino acid in that same position (.beta.-(3-quinolyl)-D-.alpha.-alanine. Both peptides are less metabolically reactive than those in the prior art and yet both peptides are significantly more potent than LHRH itself.

Abstract: Two sets of hormonal peptides are synthesized which are super agonists of the luteinizing hormone releasing hormone (LHRH). Chronic administration results in the inhibition of LHRH which is responsible for stimulating cell growth in the testes. One peptide has the D(dextro)-form of a monoheterocyclic amino acid in position six (D-3-pyridyl-alanine) while the other peptide has a bi-heterocyclic amino acid in that same position (.beta.-(3-quinolyl)-D-.alpha.-alanine. Both peptides are less metabolically reactive than those in the prior art and yet both peptides are significantly more potent than LHRH itself.

Abstract: The present invention provides lipoidal biopterin and tetrahydrobiopterin compounds of the general structure: ##STR1## wherein --R is absent when ring B has two double bonds,--R is hydrogen when the two double bonds in ring B are absent, and--R' and R" are selected from saturated or unsaturated, cyclic or non-cyclic hydrocarbons of 1 to 31 carbon units.The compounds provided by this invention are oil soluble and can readily be formulated as an oil based pharmaceutical useful for the treatment of phenylketonuria, Parkinsonism, depression, senile dementia, Alzheimer's disease and related biopterin deficiency diseases.

Abstract: Pyridyl-alanyl decapeptides have been effectively synthesized and found to have antiovulatory activity. The exemplary [N-Ac-D-2-Nal.sup.1,pCl-D-Phe.sup.2, D-3-Pal.sup.3,D-Arg.sup.6,D-Ala.sup.10 ]-LHRH has very high potency to inhibit ovulation, both parenterally and orally. Also, this exemplary pyridyl-alanyl-decapeptide showed an unexpected prolonged duration of antiovulatory activity. Such pyridyl-alanyl-decapeptides are useful to control reproduction.

Abstract: Undecapeptides retaining the amino acids in positions 2, 3, 4, 5, 6, 8 and 10 of substance P (Arg.sup.1 -Pro.sup.2 -Lys.sup.3 -Pro.sup.4 -Gln.sup.5 -Gln.sup.6 -Phe.sup.7 -Phe.sup.8 -Gly.sup.9 -Leu.sup.10 -Met.sup.11 -NH.sub.2), but having substitutions in positions 1, 7, 9 and 11 of substance P have been discovered to have high antagonistic activity to block substance P in biological systems. Exemplifying these potent antagonists is D-Arg.sup.1,D-Trp.sup.7,D-Trp.sup.9 -Leu.sup.11 -Substance P, which is an effective inhibitor and has high potency. These antagonists of substance P are useful to elucidate some biological mechanisms of substance P, and to treat inflammatory responses in the eye for medical practice in ophthalmology, and to be novel analgesic agents for medical applications.

Abstract: A class of three substances has been isolated in highly purified form and in substantially pure form by utilizing thymus tissue as a source material. These three substances are designated thymone A, thymone B and thymone C. Thymones A and B are new peptides which yield approximately 13 and 14 individual amino acid moieties, respectively, on acid hydrolysis. Thymones A and B are chemically characterized by electrophoretic and chromatographic values which are appropriate for substances which are substantially pure. Thymone C was highly purified and its biological activity was reproducibly detected and measured. Thymones A, B and C stimulate the proliferation of lymphocytes. Thymone A stimulates the formation of cyclic adenosine monophosphate. Thymone B stimulates the formation of cyclic guanosine monophosphate.

Abstract: A tridecapeptide, [Gln.sup.4 ]-neurotensin, has been effectively synthesized and which has the sequence (pyro)glutamyl-leucyl-tyrosyl-glutaminyl-asparaginyl-lysyl-prolyl-arginyl- arginyl-prolyl-tyrosinyl-isoleucyl-leucyl-acid. [Gln.sup.4 ]-neurotensin has the unique hormonal activities and chemical structure of the native hormone in bovine hypothalamic tissue.

Abstract: Synthetic 2,3-dimethoxy-5-methyl-1,4-benzoquinone is converted into a series of new 6-alkyl derivatives. These 6-alkyl derivatives have straight carbon chains which are both saturated and unsaturated. The unsaturated derivatives contain one, two, three and four double bonds. These new synthetic quinones are analogs of the naturally occurring forms of coenzyme Q and have the same fundamental electron-transfer capacity of the natural forms of coenzyme Q. Although the degree of the activity of these new synthetic analogs differ, some of these new synthetic analogs are effective substitutes for the natural forms of coenzyme Q.