Abstract: (2S,5Z)-2-amino-7-(ethanimidoylamino)-2-methylhept-5-enoic acid is crystallized as an anhydrous, stoichiometric 1.5 HCl salt and a scaleable crystallization method is disclosed. The salt form was characterized and the absolute configuration of the chiral center was confirmed as “S”. (2S,5Z)-2-amino-7-(ethanimidoylamino)-2-methylhept-5-enoic acid was high melting and appears acceptably non-hygroscopic for use in a pharmaceutical composition.
Abstract: The present invention provides a pharmaceutical composition comprising an aqueous solution of arginine and ibuprofen, wherein the molar ratio of arginine to ibuprofen is less than 1:1, as well as a method of making the same. The present invention also provides a pharmaceutical composition comprising an aqueous solution of arginine and ibuprofen, wherein the solution has a pH of less than about 7.8, as well as a method of making the same. The present invention also provides a method of treating a condition chosen from pain, inflammation, fever, and/or other conditions alleviated by ibuprofen comprising administering a pharmaceutical composition comprising an aqueous solution of arginine and ibuprofen, wherein the molar ratio of arginine to ibuprofen is less than 1:1, and wherein the molar ratio of arginine to ibuprofen is selected to achieve a pH of less than about 7.8.
Abstract: Therapeutic methods for the prevention and treatment of conditions and diseases of the gastrointestinal tract involving an overproduction of nitric oxide by inducible nitric oxide synthase are described, the methods including administering to a subject in need thereof a therapeutically effective amount of a selective inhibitor of inducible nitric oxide synthase (iNOS). The methods also include the use of selective inhibitors of iNOS in combination with other therapeutic agents, including antimicrobial agents and antisecretory agents.
Abstract: A nutritional supplement for sports nutrition and also as a general population dietary supplement for aging people is provided. The nutritional supplement is a combination of a high glycemic sugar or carbohydrate, vitamin B6, electrolytic minerals, and amino acids some of which have neuromodulating properties and some of which are muscle cell volumizers. The amino acids included in the nutritional supplement include the amino acids include glutamine, taurine, creatine, cysteine, glycine, leucine, and arginine. The amino acids having neuromodulating properties is chosen from the group consisting of glutamine, taurine, glycine, and cysteine, and combinations thereof. The amino acids having cell volumizing properties is chosen from the group consisting of creatine, taurine, and glycine, and combinations thereof. The combination of the ingredients has a synergistic effect of increasing muscle mass, increasing physical abilities (strength, stamina, and endurance), and decreasing body fat.
Abstract: The present invention relates to the technical field of stabilizing proteins, in particular to the therapeutic aspects of protein stabilization. L-carnitine is a useful agent for stabilizing proteins, and in a particularly favourable aspect in proteins used in the medical field. In a preferred aspect, L-carnitine is used for protecting chaperone activity, and in the medical field for preserving the activity of altered chaperone proteins. In connection with this invention L-carnitine is used for the preparation of a medicament for the treatment of diseases due to altered chaperone proteins, such as eye diseases, in particular cataract.
Abstract: The present invention relates to the use of creatine compounds for treating or preventing a metabolic disorder related to body weight control such as obesity, and it's associated diseases in a patient experiencing said disorder. The creatine compounds which can be used in the present method include (1) analogues of creatine which can act as substrates or substrate analogues for the enzyme creatine kinase; (2) compounds which can act as inhibitors of creatine kinase; (3) compounds which can modulate the creatine transporter (4) N-phosphocreatine analogues bearing transferable or non-transferable moieties which mimic the N-phosphoryl group. (5) compounds which modify the association of creatine kinase with other cellular components.
Abstract: The present invention provides for a method and composition for treatment and prevention of Type II Diabetes Mellitus and its complications comprising the step of administering to a patient a therapeutically-effective amount of Rhamnan Sulphate, its functional analogs, or its physiologically acceptable salts, in therapeutic proportions. The anticoagulation activity in the blood plasma of a patient is not appreciably increased.
Abstract: This invention defines a novel method for treatment of several neurological diseases and pathophysiologically related symptomology, said diseases including peripheral neuropathies, secondary symptomology of diabetes, Alzheimer's disease, Parkinson's disease, alcoholic polyneuropathy and age-onset symptomology, as well as analogous veterinary disease states. An opportunity exists for pharmacological intervention in some neurological diseases by use of water soluble, small molecular weight primary amine agents and chemical derivatives thereof. Examples of such primary pharmacological agents include 4-aminobenzoic acid and derivatives thereof.
Abstract: The present invention provides methods and compositions for promoting healing of damaged tissue that result in an increased level of nitric oxide in the vicinity of the damaged tissue. Also provided are methods and compositions for inhibiting unwanted wound healing by inhibiting the activity of nitric oxide in the tissue.
Type:
Grant
Filed:
February 28, 2003
Date of Patent:
June 8, 2004
Assignee:
New York Society for the Ruptured and Crippled Maintaining
the Hospital for Special Surgery
Abstract: The present invention relates to the use of creatine compounds including creatine, creatine phosphate or analogs of creatine, such as cyclocreatine, for treating diseases of the nervous system. Creatine compounds can be used as therapeutically effective agents against a variety of diseases of the nervous system such as diabetic and toxic neuropathies, peripheral nervous system diseases, Alzheimer's disease, Parkinson's disease, stroke, Huntington's disease, amyotropic lateral sclerosis, motor neuron disease, traumatic nerve injury, multiple sclerosis, dysmyelination and demyelination disorders, and mitochondrial diseases.
Type:
Application
Filed:
November 21, 2003
Publication date:
June 3, 2004
Applicants:
AVICENA GROUP, INC., The General Hospital Corporation
Inventors:
Rima Kaddurah-Daouk, Ghaleb Daouk, M. Flint Beal
Abstract: Isolated polynucleotide molecules and peptides encoded by these molecules are used in the analysis of human carbamyl phosphate synthetase I phenotypes, as well as in diagnostic and therapeutic applications, relating to a human carbamyl phosphate synthetase I polymorphism. By analyzing genomic DNA or amplified genomic DNA, or amplified cDNA derived from mRNA, it is possible to type a human carbamyl phosphate synthetase I with regard to the human carbamyl phosphate synthetase I polymorphism, for example, in the context of diagnosing and treating hepatic veno-occlusive disease (HVOD) associated with bone marrow transplants.
Abstract: The present invention relates to the use of creatine compounds including creatine, creatine phosphate or analogs of creatine, such as cyclocreatine, for treating diseases of the nervous system. Creatine compounds can be used as therapeutically effective agents against a variety of diseases of the nervous system such as diabetic and toxic neuropathies, peripheral nervous system diseases, Alzheimer's disease, Parkinson's disease, stroke, Huntington's disease, amyotropic lateral sclerosis, motor neuron disease, traumatic nerve injury, multiple sclerosis, dysmyelination and demyelination disorders, and mitochondrial diseases.
Type:
Application
Filed:
November 21, 2003
Publication date:
May 27, 2004
Applicants:
AVICENA GROUP, INC., The General Hospital Corporation
Inventors:
Rima Kaddurah-Daouk, Ghaleb Daouk, M. Flint Beal
Abstract: The present invention provides for compositions and methods for the preservation of tissues and organs ex vivo and in situ. In addition, the present invention provides for kits that may be used in the preparation of the solutions of the present invention. The present invention also provides a device for perfusing tissues and organs with the solutions of the present invention.
Type:
Application
Filed:
July 14, 2003
Publication date:
May 27, 2004
Inventors:
Hemant Thatte, Kunda Biswas, Shukri Khuri, Thomas Michel
Abstract: Improved drug compositions and methods useful in the treatment of male erectile dysfunction. An optimized mixture of the drugs phentolamine mesylate, papaverine hydrochloride, and alprostadil in a buffer containing L-arginine and glycine is to be injected into the penile tissue to produce an erection in otherwise impotent men.
Abstract: Water soluble tin mesoporphyrin compounds are described. Methods of preparation of water soluble metal mesoporphyrin compounds and pharmaceutical preparations are also described.
Abstract: Present invention features methods for induction of angiogenesis by administration of lysine (l-&d-) or lysine oligomers (molecular weight approx between 500 and 2500), both homo and hetero-oligomers, consisting of either l-or d- or both enantiomers.
Abstract: Stable emulsions comprising as a base one or more diene conjugated fatty acids. Amino acids and other macromolecules can be used to stabilize the emulsion. The emulsion is also useful as a carrier and delivery vehicle of the macromolecules to humans or animals in need of the macromolecules. Plant oil extracts, such as conjugated linoleic acid and its acylated derivatives, are useful as the diene conjugated fatty acids that form the base of the stable emulsion. The emulsions formed are useful as nutritional or cosmetic adjuvant for oral based nutrition, skin diseases, cosmetic utility, enhancing oral nutrition, or pharmacological benefit. Methods of producing and using the emulsions are also provided.
Abstract: Compounds of the formula (I) in which R1 is CN, or C(═NH)—NH2, CON(R3)2 or [C(R4)2]nN(R3)2, each of which is unsubstituted or monosubstituted by C(═O)R3, COOR3, or3 or by a conventional amino-protecting group, or W is —NR3CO—, —NR3COC(R4)2, NR3C(R4)2) or —C(R4)2NR3C(4)2—, X is —C(R3)2—, —[C(R3)2]2—, —C(R—3)2O— or —C(R3)2NR3, Y is alkylene, cycloalkylene, Het-diyl or Ar-diyl, T is OR3, N(R3)2, N(R3)2CON(R3)2, a monocyclic or bicyclic, saturated, unsaturated or aromatic heterocyclic radical having from 1 to 4 N, O and/sor S atoms which is unsubstituted or monosubstituted, disubstituted or trisubstituted, or a phenyl radical which is unsubstituted or monosubstituted, disubstituted or trisubstituted are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic disorders and for the treatment of tumours.
Type:
Application
Filed:
September 3, 2003
Publication date:
May 13, 2004
Inventors:
Werner Mederski, Horst Juraszyk, Dieter Dorsch, Christos Tsaklakidis, Johannes Gleitz, Christopher Barnes, Bertram Cezanne
Abstract: Linking Magnesium ions to Nitric Oxide precursor L-Arginine, chemically 2-amino-5-guanidino valeric acid, with a platelet aggregation inhibitor compound such as, but not limited to acetylsalicylic acid or clopidogrel bisulfate, unexpectedly results in a pharmaceutically stabilized compositions with extended shelf life to be taken orally to provide gradual release vasodilatory and anti-platelet aggregation pharmacological activity with reduced potential for producing gastrointestinal lesions. L-Arginine releases ADNO (Arginine derived Nitric Oxide) in the coronary artery epithelium as EDRF (endothelium dependent relaxing factor) to dilate the arteries to promote blood flow to the myocardium, and the platelet aggregation inhibitor such acetylsalicylic acid or clopidogrel and others of this class of drugs inhibits or antagonizes the aggregation adhesion of platelets in the blood stream.
Abstract: The invention describes novel compositions containing at least one phosphodiesterase inhibitor, and at least one compound that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or one or more vasoactive agents.
Type:
Application
Filed:
October 28, 2003
Publication date:
May 6, 2004
Inventors:
David S. Garvey, Inigo Saenz de Tejada, Richard A. Earl, Subhash P. Khanapure
Abstract: Compositions for the promotion of muscle protein synthesis and control of tumor-induced weight loss in patients that are, for example, suffering from cancer cachexia, and methods of administering such compositions.
Abstract: The present invention is a stable topical creatine application suitable for absorption directly through the skin into the underlying muscle without traveling through the blood system for the purpose of increasing muscle energy. It is created by combining creatine with phosphoric acid in a cosmetically elegant vehicle suitable for topical use. Chondroitin sulfate and glucosamine can also be added. Topical creatine avoids the side effects of oral creatine supplements.
Abstract: One aspect of the invention relates to anti-viral composition containing at least one zinc compound and at least one phenolic antioxidant (and optionally other ingredients such as at least one analgesic) at least one hydrocarbyl containing compound, and water. Another aspect of the invention relates to a method of treating lesionous symptoms of a viral infection involving applying an effective amount of the zinc containing anti-viral composition to the lesions.
Abstract: Vascular function and structure is maintained or improved by long term administration of physiologically acceptable compounds which enhance the level of endogenous nitric oxide or other intermediates in the NO induced relaxation pathway in the host.
Type:
Application
Filed:
July 15, 2003
Publication date:
April 29, 2004
Applicant:
The Board of Trustees of the Leland Stanford Junior University
Inventors:
John P. Cooke, Victor J. Dzau, Gary H. Gibbons
Abstract: A method of blocking dicarbonyls and carbonyls in vitro and in vivo includes using an effective quanity of an L- or D-arginine, substituted arginine, modified arginine or arginine-containing blocking agent. The method can, for example, include blocking toxic dicarbonyls and carbonyls in a patient suffering from a condition associated with toxic carbonyls and/or dicarbonyls, by administering to the patient a therapeutically effective dose of an L- or D-arginine, substituted arginine, modified arginine or arginine-containing blocking agent.
Abstract: The present invention provides a pharmaceutical composition comprising an aqueous solution of arginine and ibuprofen, wherein the molar ratio of arginine to ibuprofen is less than 1:1, as well as a method of making the same. The present invention also provides a method of treating a condition chosen from pain, inflammation, fever, and/or other conditions alleviated by ibuprofen comprising administering a pharmaceutical composition comprising an aqueous solution of arginine and ibuprofen, wherein the molar ratio of arginine to ibuprofen is less than 1:1.
Abstract: Therapeutic methods for the prevention and treatment of respiratory diseases or conditions are described, the methods including administering to a subject in need thereof a respiratory disease or condition effective amount of a selective inhibitor of inducible nitric oxide synthase.
Abstract: A method for the treatment and/or prophylaxis of Type II diabetes, which method comprises the administration, to a human or non-human mammal, of an effective non-toxic pharmaceutically acceptable amount of an NO synthase inhibitor, such as aminoguanidine, or a pharmaceutically acceptable derivative thereof.
Type:
Application
Filed:
July 24, 2003
Publication date:
April 15, 2004
Applicant:
SmithKline Beecham p.l.c.
Inventors:
Nicholas Charles Turner, Valerie Piercy
Abstract: The development and growth of oviparous species such as birds is enhanced by in ovo administration of an enteric modulator such as HMB. The enteric modulator is administered into the amnion, where it is then orally ingested by the subject. The enteric modulator enhances the enteric development of the subject prior to hatch, and enhances the growth of the animal before and after hatch.
Type:
Application
Filed:
June 30, 2003
Publication date:
April 15, 2004
Applicants:
North Carolina State University, Yissum Research Development Company of the Hebrew University of Jerusalem
Abstract: A composition is disclosed which, depending on the user, may take the form of a health food or a medicine, comprising a combination of the following as its characterising components: (a) L-carnitine inner salt or one of its pharmacologically acceptable salts; (b) acetyl L-carnitine inner salt or one of its pharmacologically acceptable salts; and (c) huperzine A or huperzine B or mixtures thereof or extracts of Huperzia serrata containing them, suitable for the prevention/treatment of learning disorders in children suffering form Attention Deficit/Hyperactive Disorder (ADHD).
Abstract: The present invention provides methods and compositions for modulating an immune response by controlling the level of arginase available to a cell, tissue or system. An immune response can be enhanced or depressed by altering the amount of arginine available to a cell, tissue or system through the manipulation of localized or systemic arginine levels using substances which provide arginine to the body and enzymes which break down arginine, such as arginase and nitric oxide synthase. Increasing or decreasing an immune response according to the present invention provides therapeutic treatments for a variety of conditions and diseases. The present invention also provides clinical methods and kits which can measure the strength or resistance to an immune response in a cell, tissue or system based upon the amount of available arginine and enzymes which break down arginine.
Type:
Application
Filed:
March 12, 2003
Publication date:
March 25, 2004
Applicant:
LSU Medical Center
Inventors:
Augusto C. Ochoa, Juan B. Ochoa, Mircea Popescu, Arnold H. Zea, Paulo C. Rodriguez
Abstract: The present invention relates to the use of creatine compounds including creatine, creatine phosphate or analogs of creatine, such as creatine-pyruvate, creatine ascorbate, cyclocreatine, 3 guanidinopropionic acid, guanidinoacetate, homocyclocreatine for preventing or treating TSE diseases of the nervous system. The Creatine compounds which can be used in the present method include (1) creatine, creatine phosphate and analogs of these compounds which can act as substrates or substrate analogs for creatine kinase; (2) molecules that mimic the biological activity of creatine (3) molecules that modulate the creatine kinase system.
Abstract: The present invention relates to the use of creatine compounds including creatine, creatine phosphate or analogs of creatine, such as cyclocreatine, for treating diseases of the nervous system. Creatine compounds can be used as therapeutically effective agents against a variety of diseases of the nervous system such as diabetic and toxic neuropathies, peripheral nervous system diseases, Alzheimer disease, Parkinson's disease, stroke, Huntington's disease, amyotropic lateral sclerosis, motor neuron disease, traumatic nerve injury, multiple sclerosis, dysmyelination and demyelination disorders, and mitochondrial diseases.
Type:
Grant
Filed:
May 7, 1997
Date of Patent:
March 16, 2004
Assignees:
Avicena Group, Inc., The General Hospital Corporation
Inventors:
Rima Kaddurah-Daouk, Ghaleb Daouk, M. Flint Beal
Abstract: The invention relates to a food composition intended to prevent or restore age-related functional deficits in mammals, which comprises a combination being able to mimic the effects of caloric restriction on gene expression. The combination contains at least one molecule that stimulates energy metabolism of the cell and at least one antioxidant. Also, methods of treating age-related functional deficits in mammals by administering the combination or a food composition containing the same.
Abstract: A combination of chemical agents reduces reductive stress by limiting the accumulation of high-energy electrons potentially available to the electron transport chain. A method of metabolic uncoupling therapy comprises: analyzing a specific physiologic process involving reductive stress; identifying a plurality of MUT agents that modulate metabolic pathways by influencing electron flux; and formulating a combination of MUT agents that limits the accumulation of high-energy electrons potentially available to the electron transport chain.
Abstract: The products of the acidification of nitrite are useful to control multiply drug resistant bacteria, such as methicillin resistant S. aureurs.
Abstract: A use for agents that disrupt actin cytoskeletal organization is provided. In the instant invention, agents that disrupt actin cytoskeletal organization are found to upregulate endothelial cell Nitric Oxide Synthase activity. As a result, agents that disrupt actin cytoskeletal organization are useful in treating or preventing conditions that result from the abnormally low expression and/or activity of endothelial cell Nitric Oxide Synthase. Such conditions include hypoxia-induced conditions. Subjects thought to benefit mostly from such treatments include nonhyperlipidemics and nonhypercholesterolemics, but not necessarily exclude hyperlipidemics and hypercholesterolemics.
Abstract: The compositions and dosage forms of the invention are clinically useful as methods for increasing the effectiveness, efficiency and safety of biguanides (metformin) and/or sulfonylureas in the prevention and treatment of insulin resistance and diabetes mellitus, alone or in combination, as a nutrient for humans. The carefully chosen active ingredients of the invention are designed in a modular fashion to prevent and rectify adverse events associated with insulin resistance syndrome and diabetes mellitus, and with the clinical use of biguanides (metformin) and/or the sulfonylureas. These modules are: (1) Mitochondrial Metabolic Group, (2) Plasma and Mitochondrial Membrane Integrity Group, (3) Nocturnal Group and, (4) Insulin Alternative Group. When used in concert with a biguanide, a sulfonylurea or with a combination of both, the invention will broaden the clinical usefulness of these drugs.
Abstract: The present invention provides compositions and methods for lowering plasma Lp(a) levels in humans. The present invention provides compositions and methods for lowering the risk factors for cardiovascular diseases. Moreover, this invention provides therapeutic alternatives to current pharmaceutical interventions for the lowering of cholesterol, LDL-cholesterol, triglycerides and other metabolic risk factors.
Abstract: The invention describes formulations that include either metformin, sulfonylurea or a biguanide-sulfonylurea combination as one active ingredient in addition to specific, other active ingredients. The compositions and dosage forms of the invention are clinically useful as methods for increasing the effectiveness, efficiency and safety of the included biguanide (metformin) and/or sulfonylurea in the prevention and treatment of insulin resistance and diabetes mellitus. The carefully chosen additional active ingredients of the invention are designed in a modular fashion to prevent and rectify adverse events associated with insulin resistance syndrome and diabetes mellitus, and those adverse incidences associated with the concurrent use of metformin and/or the sulfonylureas. When clinically administered, the invention will provide therapeutic levels of metformin and of a sulfonylurea, alone or in combination, and broaden their usefulness.
Abstract: The present invention is a cosmetic or dermatological preparation or method of applying a cosmetic or dermatological preparation for the treatment or prophylaxis of skin damage or a skin condition, wherein the preparation includes creatine or a creatine derivative. The use of creatine or creatine derivatives in the cosmetic or dermatological preparations of the invention not only provides effective protection of the skin but also protects the preparations or the constituents of the preparations against harmful oxidation processes.
Type:
Application
Filed:
January 6, 2003
Publication date:
February 12, 2004
Applicant:
Beiersdorf AG
Inventors:
Thomas Blatt, Melanie Schmidt, Volker Schreiner, Franz Stab
Abstract: A process for producing solid creatine-containing dosage forms, wherein
a) a mixture which comprises at least one thermoplastic, physiologically tolerated, water-soluble or water-swellable polymeric binder and creatine, and contains 1 to 20 mol of water per mol of creatine is prepared,
b) the mixture is plasticated at or above the softening point of the polymeric binder, preferably with at least partial evaporation of the water,
c) the plasticated mixture is shaped to dosage forms and cooled.
Abstract: The invention relates to the use of peptide amides of formula (I)
and phenylamino-oxoacetic acid derivatives of formula (II)
as well as the salts of the above compounds as active substances for the preparation of pharmaceutical compositions possessing neurogenic and non-neurogenic antiinflammatory as well as analgetic effects.
Abstract: The key function of TNAP in bone is degradation of PPi to remove this mineralization inhibitor and provide free phosphate for apatite deposition. PC-1 is a direct antagonist of TNAP function. ANK also antagonizes TNAP-dependent matrix calcification. Specifically, the activity of PC-1 inhibits initial MV apatite deposition, but ANK inhibits propagation of apatite outside the MVs. Furthermore, loss of function of the two distinct skeletal TNAP antagonists, PC-1 and ANK, ameliorates TNAP deficiency-associated osteomalacia in vivo. Conversely, the hyperossification associated with both PC-1 null mice and ANK-deficient (ank/ank) mice is ameliorated by deficiency of TNAP in vivo.
Type:
Application
Filed:
April 28, 2003
Publication date:
February 5, 2004
Applicants:
The Regents of the University of California, The Burnham Institute
Abstract: The invention relates to a method of administering to a human subject a composition comprising a vitamin, an amino acid and a trace element for the prevention and treatment of health conditions caused by constriction of smooth muscle cells in organs of the human body like high blood pressure, asthma, glaucoma and tinnitus. The composition comprises a vitamin such as ascorbic acid, an amino acid such as arginine, and a trace element such as magnesium.
Abstract: The present invention relates to the use of arginine and, more in particular, to the injectable formulations for intravenous use comprising it, in the prevention and treatment of the side effects associated with the extravasation of drugs administered by intravenous route.
Type:
Application
Filed:
July 14, 2003
Publication date:
January 22, 2004
Inventors:
Lorena Muggetti, Alessandro Martini, Giovanni Buzzi, Paolo Colombo