Tricyclo Ring System Having The Hetero Ring As One Of The Cyclos Patents (Class 514/437)
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Publication number: 20040167151Abstract: Compounds are described having a structure according to Formula I or Formula II: 1Type: ApplicationFiled: February 24, 2003Publication date: August 26, 2004Inventors: Kuo-Hsiung Lee, Yi Xia, Zheng-Yu Yang, Kenneth F. Bastow, Sheng-Chu Kuo
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Patent number: 6767919Abstract: A process for producing new anticancer drugs such that the drugs can be administered in a nontoxic, proto-drug form and, subsequent to a time delay which allows for differential concentration in the target cancer or invasive tissues or cells, the non-toxic drug is then modified by an activation drug to selectively provide toxic levels of a pharmacologically active agent to the target issue.Type: GrantFiled: December 17, 2002Date of Patent: July 27, 2004Assignee: Walker Cancer Research Institute, Inc.Inventors: Evan Harris Walker, Eduardo Palomino, Steven L. Blumenthal
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Patent number: 6750244Abstract: Method and compositions for treating a patient having a neurological disease or disorder, such as stroke, head trauma, spinal cord injury, spinal cord ischemia, ischemia- or hypoxia-induced nerve cell damage, epilepsy, anxiety, neuropsychiatric or cognitive deficits due to ischemia or hypoxia such as those that frequently occur as a consequence of cardiac surgery under cardiopulmonary bypass, or neurodegenerative diseases such as Alzheimer's Disease, Huntington's Disease, Parkinson's Disease, or amyotrophic lateral sclerosis (ALS).Type: GrantFiled: April 2, 2001Date of Patent: June 15, 2004Assignee: NPS Pharmaceuticals, Inc.Inventors: Alan L. Mueller, Scott T. Moe
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Publication number: 20040110784Abstract: The present invention provides a therapeutic agent for bladder irritative symptoms associated with benign prostatic hyperplasia comprising, as an active ingredient, a tricyclic compound represented by formula (I): 1Type: ApplicationFiled: September 22, 2003Publication date: June 10, 2004Inventors: Tsuyoshi Yamagata, Kaoru Atsuki, Tetsuji Ohno, Shiro Sirakura, Akira Karasawa
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Patent number: 6730697Abstract: Dihydrothiaphenanthrenecarbonylguanidine compound of formula I These compounds are potentially suitable as antiarrythmic medicaments with a cardioprotective component for prophylaxis of an infarction and treatment of infarction, and for treatment of angina pectoris. They may also inhibit in a preventive manner the pathophysiological processes involved in the development of ischemia-induced damage, especially in the initiation of ischemia-induced cardiac arrhythmias.Type: GrantFiled: January 23, 2003Date of Patent: May 4, 2004Assignee: Aventis Pharma Deutschland GmbHInventors: Heinz-Werner Kleemann, Peter Below
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Publication number: 20040082601Abstract: This invention relates to anti-inflammatory compounds, methods of making such compounds and methods of using such compounds having the following structure: 1Type: ApplicationFiled: October 21, 2003Publication date: April 29, 2004Inventors: Malcolm K. Scott, Pauline J. Sanfilippo, Louis J. Fitzpatrick, Richard Cordova, Kevin Pan, Joseph Meschino
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Patent number: 6693136Abstract: Compounds of formula (I) are novel P2X3 and P2X2/P2X3 containing receptor antagonists and are useful in treating pain, urinary incontinence, and bladder overactivity.Type: GrantFiled: July 26, 2002Date of Patent: February 17, 2004Assignee: Abbott LaboratoriesInventors: Chih-Hung Lee, Meiqun Jiang, Richard A. Perner, Arthur Gomtsyan, Erol K. Bayburt, Guo Zhu Zheng
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Publication number: 20030229233Abstract: Processes are described for the preparation of thioxanthones (Formula I). A reactant mixture of a 2-chlorothiobenzoyl chloride (Formula II) and an aromatic compound (Formula III) is added to a slurry of a Friedel-Crafts catalyst in an organic Friedel-Crafts solvent. Products of the processes may be used for the preparation of a pharmaceutical product for use in the field of psycho-therapeutics, or as activators or sensitizers in the photo-polymerization of ethylenically unsaturated monomers.Type: ApplicationFiled: April 7, 2003Publication date: December 11, 2003Inventor: Carsten Berg
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Publication number: 20030212061Abstract: The present invention relates to a group of aza-thioxanthenone compounds having antitumor activity, and processes for their preparation. Compositions containing the aza-thioxanthenone compounds and methods of treating tumors and cancer in mammals with the compounds of the present invention are also disclosed.Type: ApplicationFiled: March 12, 2002Publication date: November 13, 2003Inventor: Simon N. Haydar
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Publication number: 20030181511Abstract: Dihydrothiaphenanthrenecarbonylguanidine compound of formula I 1Type: ApplicationFiled: January 23, 2003Publication date: September 25, 2003Inventors: Heinz-Werner Kleemann, Peter Below
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Patent number: 6620834Abstract: Medicinal compositions for colorectal cancer to be administered to the large intestine by taking advantage of preparations disintegrating in the large intestine, characterized by containing a cyclooxygenase inhibitor and an HMG-CoA reductase inhibitor. These compositions are appropriate for inhibiting the postoperative liver metastasis and recurrence of colorectal cancer.Type: GrantFiled: April 15, 2002Date of Patent: September 16, 2003Assignee: Hisamitsu Pharmaceutical Co., Inc.Inventors: Norifumi Tanida, Takeshi Goto, Naoko Tomizawa
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Patent number: 6613797Abstract: Therapeutic compounds and compositions for the treatment of infectious diseases are disclosed. The compounds are xanthones and xanthone derivatives, such as 3,5-bis-&egr;-(N,N-diethylamino)amyloxyxanthone. The described compositions include such compounds and a pharmaceutical carrier. These compositions also can include additional materials conventionally used to form therapeutic compositions. 3,5-bis-&egr;-(N,N-diethylamino)amyloxyxanthone has an IC50 for Plasmodium falciparum of about 0.15 &mgr;M, and an IC50 for Leishmania mexicana of <<0.5 &mgr;M. These compositions are additionally useful for forming soluble complexes with heme and porphyrins.Type: GrantFiled: December 1, 2000Date of Patent: September 2, 2003Assignee: Interlab, Inc.Inventors: Rolf W. Winter, Michael K. Riscoe, David J. Hinrichs
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Publication number: 20030158191Abstract: The invention provides cannabinol derivatives and pharmaceutical preparations thereof.Type: ApplicationFiled: December 22, 2002Publication date: August 21, 2003Inventor: Craig R. Travis
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Patent number: 6602903Abstract: The invention relates to compounds of formula (I): and medicinal products containing the same are useful in treating or in preventing melatoninergic disorders.Type: GrantFiled: August 28, 2001Date of Patent: August 5, 2003Assignee: Les Laboratories ServierInventors: Gérald Guillaumet, Marie-Claude Viaud, Ahmed Mamai, Isabelle Charton, Pierre Renard, Caroline Bennejean, Béatrice Guardiola, Philippe Daubos
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Patent number: 6566389Abstract: A method for treating or preventing symptoms of tardive dyskensia comprises administering melatonin to patient exhibiting or liable to develop such symptoms. The melatonin is administered in an amount effective to ameliorate or prevent symptoms of tardive dyskensia developing in the patient.Type: GrantFiled: November 26, 2001Date of Patent: May 20, 2003Assignee: Neurim Pharmaceuticals (1991) Ltd.Inventors: Nava Zisapel, Moshe Laudon
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Publication number: 20030073745Abstract: The invention relates to the discovery that specific adamantyl or adamantyl group derivatives containing retinoid-related compounds induce apoptosis of cancer cells and therefore may be used for the treatment of cancer, including advanced cancer. Also, the present invention relates to novel adamantyl or adamantyl group derivatives containing retinoid compounds and their usage for treatment and/or prevention of cancer, keratinization disorders, dermatological conditions, and other therapies More specifically, it has been shown that such adamantyl compounds, e.g., 6-[3-(1-adamantyl)-4-methoxyphenyl]-2-naphthoicacid, 2-[3-(1-adamantyl)-4-methoxyphenyl]-5-benzimidazole carboxylic acid, and 6-[3-(1-adamantyl)-4,5-methylenedioxyphenyl]-2-naphthoic acid, can be used to treat or prevent cervical cancers and precancers such as cervical dysplasias, including high grade and low grade dysplasias.Type: ApplicationFiled: June 24, 2002Publication date: April 17, 2003Inventors: Magnus Pfahl, Xian-Ping Lu, Darryl Rideout, Hongyue Zhang
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Patent number: 6521641Abstract: Methods and compositions for inhibiting or preventing spermatogenesis in a male mammal. Also disclosed are compounds and formulations for use in such methods.Type: GrantFiled: June 9, 2000Date of Patent: February 18, 2003Assignee: Allergan, Inc.Inventors: Elliott S. Klein, Yang-Dar Yuan, Roshantha A. Chandraratna
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Patent number: 6514967Abstract: The invention relates to compounds of the following general formula (I): in which: R1 and R2 represent a hydrogen atom, or form a ring, especially a benzene ring, R3 represents a hydrogen atom or an alkyl group, especially a methyl group, X and Y, independently of one another, represent a carbon atom, or a heteroatom such as a sulphur atom S, or a group with the formula (a) in which R4 and R5 represent a hydrogen atom or a methyl group, or R4 and R5 form a heterocycle, and their use for the preparation of a drug intended for the treatment of pathologies associated with abnormally high concentrations of extracellular glutamate.Type: GrantFiled: December 16, 1999Date of Patent: February 4, 2003Assignee: Centre National de la Recherche ScientifiqueInventors: Jean-Marc Kamenka, Isoline Caubere, Gerard Barbanel
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Patent number: 6511968Abstract: The invention provides a method for treating, preventing, or reducing the risk of developing a condition selected from the group consisting of acute coronary ischemic syndrome, thrombosis, thromboembolism, thrombotic occlusion and reocclusion, restenosis, transient ischemic attack, and first or subsequent thrombotic stroke, in a patient, comprising administering to the patient a therapeutically effective amount of an antiplatelet agent in combination with a therapeutically effective amount of a COX-2 inhibitor. The invention also provides a pharmaceutical composition comprising a therapeutically effective amount of a COX-2 inhibitor, or a pharmaceutically acceptable salt thereof, and an antiplatelet agent, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: October 23, 2000Date of Patent: January 28, 2003Assignee: Merck & Co., Inc.Inventor: Steven A. Nichtberger
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Publication number: 20030008891Abstract: 3′,4′-di-O-camphanoyl-(+)-cis-khellactone analogs according to the present invention have been found to have anti-HIV activity.Type: ApplicationFiled: March 13, 2002Publication date: January 9, 2003Applicant: Panacos Pharmaceuticals, Inc.Inventors: Kuo-Hsiung Lee, Lan Xie, Graham P. Allaway, Carl T. Wild
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Patent number: 6504052Abstract: Compounds of the formula (I) in which R1 is C1-10 allyl; C2-10 alkenyl; C2-10 alkynyl; phenyl-C2-10 alkyl or phenyl-C2-10 alkenyl; and salts and esters thereof, modulate metabotropic glutamate receptor function and are useful in treating disorders of the central nervous systemType: GrantFiled: November 16, 2001Date of Patent: January 7, 2003Assignee: Eli Lilly and CompanyInventors: Ivan Collado Cano, Concepcion Pedregal Tercero, Alicia Marcos Llorente
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Publication number: 20020177592Abstract: This invention discloses that a combination of two drugs, from two different and previously unrelated categories, provides effective and long-lasting relief from neuropathic pain. Both drugs can be taken orally, in a convenient, painless, non-invasive manner that does not require injections. One drug in this combination is an &agr;2 adrenergic agonist, exemplified by clonidine. The other drug in the pain-relieving combination has a tri-cyclo-alkyl-amine (TCAA) structure. At least some TCAA drugs have antagonist (receptor-blocking) activity at two entirely different classes of neuronal receptors: the muscarinic subclass of acetylcholine (ACh) receptors, and the NMDA subclass of glutamate receptors. Such drugs include ethopropazine, normally used as an anti-cholinergic drug, and desipramine, normally used as an anti-depressant.Type: ApplicationFiled: March 28, 2001Publication date: November 28, 2002Inventors: John W. Olney, Nuri B. Farber, Vesna Jevtovic-Todorovic
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Publication number: 20020156077Abstract: Novel non-steroidal estrogen receptor ligands and methods of synthesis are disclosed. The novel molecules are intended for use in therapeutic preparations for the treatment of estrogen receptor related disease states. The compounds specified are tetra-cyclic derivatives and have been shown to be antiproliferative against human estrogen-dependent cancer cells and to have good binding affinity for the estrogen receptor.Type: ApplicationFiled: August 21, 2001Publication date: October 24, 2002Inventors: Jonathan Martin Schmidt, Julie Mercure, Jeffry Lawrence Lowell, Stefan Kwiatkowski, Krzysztof Pupek, Shuguang Zhu, John Whelan, Natalie Lazarowych
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Patent number: 6462064Abstract: The invention relates to the discovery that specific adamantyl or adamantyl group derivatives containing retinoid-related compounds induce apoptosis of cancer cells and therefore may be used for the treatment of cancer, including advanced cancer. Also, the present invention relates to novel adamantyl or adamantyl group derivatives containing retinoid compounds and their usage for treatment and/or prevention of cancer, keratinization disorders, dermatological conditions, and other therapies More specifically, it has been shown that such adamantyl compounds, e.g., 6-[3-(1-adamantyl)-4-methoxyphenyl]-2-naphthoic acid, 2-[3-(1-adamantyl)-4-methoxyphenyl]-5-benzimidazole carboxylic acid, and 6-[3-(1-adamantyl)-4,5-methylenedioxyphenyl]-2-naphthoic acid, can be used to treat or prevent cervical cancers and precancers such as cervical dysplasias, including high grade and low grade dysplasias.Type: GrantFiled: February 4, 2000Date of Patent: October 8, 2002Assignee: Galderma Research & Development S.N.C.Inventors: Magnus Pfahl, Xian-Ping Lu, Darryl Rideout, Hongyue Zhang
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Patent number: 6455546Abstract: The present invention generally relates to various methods for promoting ovulation, parturition and lactation in female mammals. These benefits are obtained by administering to the mammals a composition containing a D2 receptor antagonist that does not substantially cross the blood brain barrier. In one embodiment, the D2 receptor antagonist is domperidone. The domperidone can be administered to the mammal either orally or subcutaneously and can be used to treat, for instance, anestrous mammals, mammals that have problems bearing offspring and mammals suffering from agalactia. Unexpectedly, it has also been discovered that the D2 receptor antagonist may also stimulate feed intake, causing the mammal to eat more and gain weight faster.Type: GrantFiled: February 14, 2001Date of Patent: September 24, 2002Assignee: Clemson UniversityInventor: Dee L. Cross
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Publication number: 20020132796Abstract: Novel compounds having the Formulas 1 through 8, wherein the symbols have the meaning defined in the specification, and certain previously known compounds have been discovered to act as inhibitors of the cytochrome P450RAI (retinoic acid inducible) enzyme, and are used for treating diseases responsive to treatment by retinoids. The compound can also be used in co-treatment with retinoids.Type: ApplicationFiled: June 7, 2001Publication date: September 19, 2002Inventors: Jayasree Vasudevan, Alan T. Johnson, Liming Wang, Dehua Huang, Roshantha A. Chandraratna
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Publication number: 20020119992Abstract: Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: 1Type: ApplicationFiled: December 18, 2001Publication date: August 29, 2002Inventors: Harold G. Selnick, James C. Barrow, Philippe G. Nantermet, Peter D. Williams, Kenneth J. Stauffer, Philip E. Sanderson, Kenneth E. Rittle, Matthew M. Morrissette, Catherine M. Wiscount, Lekhanh O. Tran, Terry A. Lyle, Donnette D. Staas
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Publication number: 20020103217Abstract: This invention relates to anti-inflammatory compounds, methods of making such compounds and methods of using such compounds having the following structure: 1Type: ApplicationFiled: January 8, 2002Publication date: August 1, 2002Inventors: Malcolm K. Scott, Pauline J. Sanfilippo, Louis J. Fitzpatrick, Richard Cordova, Kevin Pan, Joseph Meschino
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Publication number: 20020091150Abstract: The present invention is a compound of formula 1Type: ApplicationFiled: December 10, 2001Publication date: July 11, 2002Inventors: Konrad Bleicher, Vincent Mutel, Eric Vieira, Jurgen Wichmann, Thomas Johannes Woltering
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Patent number: 6407137Abstract: The invention involves the formation of a prodrug from a fatty acid carrier and a neuroactive drug. The prodrug is stable in the environment of both the stomach and the bloodstream and may be delivered by ingestion. The prodrug passes readily through the blood brain barrier. Once in the central nervous system, the prodrug is hydrolyzed into the fatty acid carrier and the drug to release the drug. In a preferred embodiment, the carrier is 4, 7, 10, 13, 16, 19 docosahexa-enoic acid and the drug is dopamine. Both are normal components of the central nervous system. The covalent bond between the drug and the carrier preferably is an amide bond, which bond may survive the conditions in the stomach. Thus, the prodrug may be ingested and will not be hydrolyzed completely into the carrier molecule and drug molecule in the stomach.Type: GrantFiled: July 9, 2001Date of Patent: June 18, 2002Assignee: Protarga, Inc.Inventor: Victor E. Shashoua
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Patent number: 6391911Abstract: Disclosed is a method of treating a cancer of the central nervous system in a host including administering radiation to the host; and administering lucanthone to the host; wherein the radiation and lucanthone are administered in amounts effective to cause the arrest or regression of the cancer of the central nervous system in the host. Also disclosed is method of treating tumors of the central nervous system including inducing base damage to a tumor cell's DNA; and inhibiting excision repair of that damage by providing lucanthone to the cell.Type: GrantFiled: April 9, 1999Date of Patent: May 21, 2002Inventor: Robert E. Bases
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Patent number: 6387892Abstract: Novel compounds having the Formulas 1 through 8, wherein the symbols have the meaning defined in the specification, and certain previously known compounds have been discovered to act as inhibitors of the cytochrome P450RAI (retinoic acid inducible) enzyme, and are used for treating diseases responsive to treatment by retinoids. The compound can also be used in co-treatment with retinoids.Type: GrantFiled: June 7, 2001Date of Patent: May 14, 2002Assignee: Allergan Sales, Inc.Inventors: Jayasree Vasudevan, Alan T. Johnson, Liming Wang, Dehua Huang, Roshantha A. Chandraratna
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Publication number: 20020055530Abstract: The present invention relates to compositions and methods for promoting tissue regeneration, preferably neural tissue regeneration. Compositions of the invention include (i) certain diphenyl sulfides, diphenyl sulfoxides, diphenyl sulfones, and sulfide, sulfoxide and sulfones of dibenzothiophene and thioxanthene, as well as various analogues and derivatives of these compounds; (ii) one or more cells harvested from an animal or organism subsequent to the administration of a composition comprising a compound of (i); or (iii) any combination of (i) and (ii). The invention can be useful in treating decreases in neuronal function, for example from injury or disease.Type: ApplicationFiled: April 6, 2001Publication date: May 9, 2002Inventors: Timothy J. Neuberger, Uri Herzberg, Veronica Mallon
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Patent number: 6384045Abstract: This invention provides cancer-active tricyclic and tetracyclic oxypyrones and a method of synthesizing these compounds. Preferred compounds have aryl groups at the 3-position of the oxypyrone ring. The tricyclic oxypyrone synthetic method is a simple condensation reaction of pyrones with cyclohexenecarboxaldehydes, providing high yields and using few steps. The tetracyclic oxypyrone synthetic method is a simple condensation reaction of carvones with pyrones.Type: GrantFiled: June 24, 1999Date of Patent: May 7, 2002Assignee: Kansas State University Research FoundationInventors: Duy H. Hua, Jean-Pierre Perchellet
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Patent number: 6353018Abstract: The present invention relates to compounds of the general formula (I) The compounds are useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR).Type: GrantFiled: October 19, 1999Date of Patent: March 5, 2002Assignees: Novo Nordisk A/S, Dr. Reddy's Research FoundationInventors: Lone Jeppesen, Paul Stanley Bury, Per Sauerberg
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Publication number: 20010056116Abstract: The invention involves the formation of a prodrug from a fatty acid carrier and a neuroactive drug. The prodrug is stable in the environment of both the stomach and the bloodstream and may be delivered by ingestion. The prodrug passes readily through the blood brain barrier. Once in the central nervous system, the prodrug is hydrolyzed into the fatty acid carrier and the drug to release the drug.Type: ApplicationFiled: July 9, 2001Publication date: December 27, 2001Inventor: Victor Shashoua
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Patent number: 6313107Abstract: Novel compounds having the Formulas 1 through 8, wherein the symbols have the meaning defined in the specification, and certain previously known compounds have been discovered to act as inhibitors of the cytochrome P450RAI (retinoic acid inducible) enzyme, and are used for treating diseases responsive to treatment by retinoids. The compound can also be used in co-treatment with retinoids.Type: GrantFiled: September 28, 2000Date of Patent: November 6, 2001Assignee: Allergan Sales, Inc.Inventors: Jayasree Vasudevan, Alan T. Johnson, Liming Wang, Dehua Huang, Roshantha A. Chandraratna
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Patent number: 6258836Abstract: The invention involves the formation of a prodrug from a fatty acid carrier and a neuroactive drug. The prodrug is stable in the environment of both the stomach and the bloodstream and may be delivered by ingestion. The prodrug passes readily through the blood brain barrier. Once in the central nervous system, the prodrug is hydrolyzed into the fatty acid carrier and the drug to release the drug. In a preferred embodiment, the carrier is 4, 7, 10, 13, 16, 19 docosahexa-enoic acid and the drug is dopamine. Both are normal components of the central nervous system. The covalent bond between the drug and the carrier preferably is an amide bond, which bond may survive the conditions in the stomach. Thus, the prodrug may be ingested and will not be hydrolyzed completely into the carrier molecule and drug molecule in the stomach.Type: GrantFiled: November 29, 1999Date of Patent: July 10, 2001Assignee: Protarga, Inc.Inventor: Victor E. Shashoua
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Patent number: 6252090Abstract: Compounds having Formula 1 wherein the symbols have the meaning defined in the specification are inhibitors of the cytochrome P450RAI (retinoic acid inducible) enzyme, and are used for treating diseases responsive to treatment by retinoids.Type: GrantFiled: August 29, 2000Date of Patent: June 26, 2001Assignee: Allergan Sales, Inc.Inventors: Jayasree Vasudevan, Alan T. Johnson, Dehua Huang, Roshantha A. Chandraratna
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Patent number: 6245797Abstract: The instant invention provides a drug combination comprised of an HMG-CoA reductase inhibitor in combination with a COX-2 inhibitor, which is useful for treating, preventing, and/or reducing the risk of developing atherosclerosis and atherosclerotic disease events.Type: GrantFiled: October 20, 1998Date of Patent: June 12, 2001Assignee: Merck & Co., Inc.Inventor: Melvin Winokur
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Patent number: 6172058Abstract: A pharmaceutical compound of the formula in which R1 is C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, C3-10 cycloalkyl, C3-10 cycloalkyl-C1-10 alkyl, C3-10 cycloalkyl-C2-10 alkenyl, C3-10 cycloalky-C2-10 alkynyl, optionally substituted phenyl-C1-10 alkyl, optionally substituted phenyl-C2-10 alkenyl, optionally substituted phenyl-C2-10 alkynyl, optionally substituted naphthyl, optionally substituted naphthyl-C1-10 alkyl, C1-10 alkoxy-C1-10 alkyl, C3-10 cycloalkoxy-C1-10 alkyl, optionally substituted heterocyclyl, optionally substituted heterocyclyl-C1-10 alkyl, optionally substituted phenyl fused to C5-10 cycloalkyl, optionally substituted tricyclic, optionally substituted tricyclic-C1-10 alkyl, or [optionally substituted phenyl(CH2)n]2-C1-10 alkyl, where n is 0 or 1 to 4, and R2 is hydrogen or one of the values for R1; or a salt or ester thereof.Type: GrantFiled: April 3, 1998Date of Patent: January 9, 2001Assignee: Lilly, SAInventors: Concepci{acute over (o)}n Pedregal Tercero, Ivan Collado Cano, Angel Maz{acute over (o)}n Ruiz
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Patent number: 6127415Abstract: The present invention relates to specific adamantyl or adamantyl group derivative containing retinoid compounds induce apoptosis of cancer cells. These adamantyl retinoid derivatives are useful for the treatment of many cancers and solid tumors, especially androgen-independent prostate cancer, skin cancer, pancreatic carcinomas, colon cancer, melanoma, ovarian cancer, liver cancer, small cell lung carcinoma, non-small cell lung carcinoma, cervical carcinoma, brain cancer, bladder cancer, breast cancer, neuroblastoma/glioblastoma, and leukemia. Also, the invention relates to novel adamantyl or adamantyl group derivative compounds which are useful as active agents for the treatment or prevention of keratinization disorders and other dermatological conditions, and other diseases.Type: GrantFiled: April 14, 1999Date of Patent: October 3, 2000Assignee: Galderma Research & Development, S.N.C.Inventors: Magnus Pfahl, Xian-Ping Lu, Darryl Rideout, Hongyue Zhang
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Patent number: 6117869Abstract: The present invention relates to compounds of Formula I that inhibit matrix metalloproteinases and to a method of inhibiting matrix metalloproteinases using the compounds ##STR1## More particularly, the present invention relates to a method of treating diseases in which matrix metalloproteinases are involved such as multiple sclerosis, atherosclerotic plaque rupture, restenosis, aortic aneurysm, heart failure, periodontal disease, corneal ulceration, burns, decubital ulcers, chronic ulcers or wounds, cancer metastasis, tumor angiogenesis, osteoporosis, rheumatoid or osteoarthritis, renal disease, left ventricular dilatation, or other autoimmune or inflammatory diseases dependent upon tissue invasion by leukocytes.Type: GrantFiled: July 26, 1999Date of Patent: September 12, 2000Assignee: Warner-Lambert CompanyInventors: Joseph Armand Picard, Bruce David Roth, Drago Robert Sliskovic
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Patent number: 6100253Abstract: The present invention relates to novel N-substituted azaheterocyclic compounds of the general formula ##STR1## wherein X, Y, Z, R.sup.1, R.sup.2 and r are as defined in the detailed part of the present description, or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation as well as their use for treatment of indications caused by or related to the secretion and circulation of insulin antagonising peptides, e.g. non-insulin-dependent diabetes mellitus (NIDDM) and ageing-associated obesity.Type: GrantFiled: August 17, 1999Date of Patent: August 8, 2000Assignee: Novo Nordisk A/SInventors: Knud Erik Andersen, Tine Krogh J.o slashed.rgensen, Rolf Hohlweg, Erik Fischer, Uffe Bang Olsen, Zdenek Polivka, Karel Sindelar, Vladimir Valenta
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Patent number: 6054448Abstract: Compounds of the formula ##STR1## in which R.sup.1 is Y or Y--C.sub.1-6 alkyl, where Y is carboxy, tetrazolyl, --SO.sub.2 H, --SO.sub.3 H, --OSO.sub.3 H, --CONHOH, or --P(OH)OR', --PO(OH)OR', --OP(OH)OR' or --OPO(OH)OR' where R' is hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl or optionally substituted phenyl-C.sub.1-6 alkyl,and R.sup.2, R.sup.3, R.sup.4, X and Z are as defined in the specification, possess affinity for metabotropic glutamate receptors and are useful in the treatment of disorders of the central nervous system.Type: GrantFiled: October 17, 1997Date of Patent: April 25, 2000Assignee: Eli Lilly and Company LimitedInventors: Barry Peter Clark, John Richard Harris
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Patent number: 5994392Abstract: The invention involves the formation of a prodrug from a fatty acid carrier and a neuroactive drug. The prodrug is stable in the environment of both the stomach and the bloodstream and may be delivered by ingestion. The prodrug passes readily through the blood brain barrier. Once in the central nervous system, the prodrug is hydrolyzed into the fatty acid carrier and the drug to release the drug. In a preferred embodiment, the carrier is 4, 7, 10, 13, 16, 19 docosahexa-enoic acid and the drug is dopamine. Both are normal components of the central nervous system. The covalent bond between the drug and the carrier preferably is an amide bond, which bond may survive the conditions in the stomach. Thus, the prodrug may be ingested and will not be hydrolyzed completely into the carrier molecule and drug molecule in the stomach.Type: GrantFiled: June 5, 1995Date of Patent: November 30, 1999Assignee: Neuromedica, Inc.Inventor: Victor E. Shashoua
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Patent number: 5990104Abstract: Polycyclic alkaloids of formula (I), wherein R.sub.1 is H, C.sub.1-6 alkyl, or C.sub.6-12 aryl optionally substituted with polar groups; R.sub.2 and R.sub.3 are independently H, OH, C.sub.1-6 alkyl, --C(NH)--NH.sub.2, a positively charged group, or C.sub.7-13 aralkyl optionally substituted with NH.sub.2, OH, C.sub.1-6 alkyl, or halogen; or R.sub.2 and R.sub.3 together form a 5 to 6 member ring optionally incorporating a heteroatom; R.sub.4 is H, C.sub.1-6 alkyl, OR.sub.6, SR.sub.6, or N(R.sub.6).sub.2, wherein each R.sub.6 is independently H, C.sub.1-3 alkyl; X ix O, S, SO, SO.sub.2, or N--R.sub.5, wherein each R.sub.5 is independently H, C.sub.1-6 alkyl, or C.sub.7-13 aralkyl optionally interrupted with one or more heteroatom; n is an integer from 0 to 2; and m is an integer from 0 to 3. These compounds act as antagonists at the ionotropic NMDA (N-methyl-(D)-aspartic acid) receptor.Type: GrantFiled: March 25, 1998Date of Patent: November 23, 1999Assignee: Biochem Pharma, Inc.Inventors: John Dimaio, Dilip M. Dixit
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Patent number: 5977077Abstract: Therapeutic compositions for the treatment of infectious diseases are disclosed. These compositions comprise xanthones and xanthone derivatives, such as 2,3,4,5,6-pentahydroxyxanthone. Also disclosed are methods for the treatment of infectious diseases using such compounds.Type: GrantFiled: March 20, 1996Date of Patent: November 2, 1999Assignee: Interlab CorporationInventors: Rolf Walter Winter, Michael Kevin Riscoe, David J. Hinrichs
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Patent number: 5958970Abstract: This invention provides cancer-active tricyclic and tetracyclic oxypyrones and a method of synthesizing these compounds. Preferred compounds have aryl groups at the 3-position of the oxypyrone ring. The tricyclic oxyprone synthetic method is a simple condensation reaction of pyrones with cyclohexenecarboxaldehydes, providing high yields and using few steps. The tetracyclic oxypyrone synthetic method is a simple condensation reaction of carvones with pyrones.Type: GrantFiled: July 29, 1997Date of Patent: September 28, 1999Assignee: Kansas State University Research FoundationInventors: Duy H. Hua, Jean-Pierre Perchellet
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Patent number: 5891899Abstract: A pharmaceutical compound of the formula: ##STR1## in which A is carboxy, tetrazolyl, --SO.sub.2 H, --SO.sub.3 H, --OSO.sub.3 H, --CONHOH, or --P(OH)OR', --PO(OH)OR', --OPO(OH)OR'B is a bond, C.sub.1-6 alkylene or C.sub.2-6 alkenylene,R.sup.1 is hydrogen, hydroxyl, halo or group of the formula A--B--,X is C.sub.1-6 alkylene, C.sub.2-6 alkenylene, C.sub.2-6 alkynylene or C.sub.1-6 alkylene linked through --O--, --S-- or --NR"-- to Y, where R" is hydrogen or C.sub.1-6 alkyl,andY is (1) ##STR2## where p is and Z is ##STR3## or (2) ##STR4## and salts and esters thereof.Type: GrantFiled: December 15, 1997Date of Patent: April 6, 1999Assignee: Eli Lilly and Company LimitedInventors: Barry Peter Clark, John Richard Harris