Additional Hetero Ring Patents (Class 514/402)
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Patent number: 7410999Abstract: The present invention relates to novel compounds and methods that are useful in treating members of the Flaviviridae family of viruses. Compounds of the present invention will have a structure according to Formulas (I)-(VI) as recited throughout the application.Type: GrantFiled: November 20, 2006Date of Patent: August 12, 2008Assignees: University of North Carolinia at Chapel Hill, Georgia State University Research Foundation, Inc., Auburn UniversityInventors: Christine C. Dykstra, Maurice Daniel Givens, David A. Stringfellow, Kenny Brock, David Boykin, Arvid Kumar, W. David Wilson, Richard R. Tidwell, Chad F. Stephens
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Publication number: 20080153872Abstract: Certain bis-(coumarin) compounds as well as the products of their intramolecular cyclization including pharmaceutically acceptable salts, hydrates, solvates, clathrates, prodrugs, tautomers and stereoisomers thereof are disclosed. Certain processes and intermediates for the preparation of certain bis-(coumarin) compounds, as well as for the use of these compounds as therapeutically active agents in the prophylaxis and treatment of asthma and other inflammatory diseases and conditions in mammals, especially humans are also disclosed.Type: ApplicationFiled: January 13, 2006Publication date: June 26, 2008Inventors: Mladen Mercep, Ivica Malnar, Boska Hrvacic, Stribor Markovic, Anita Filipovic Sucic, Berislav Bosnjak, Andreja Cempuh Klonkay, Renata Rupcic, Antun Hutinec, Ivaylo Jivkov Elenkov, Milan Mesic
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Publication number: 20080146445Abstract: The present invention concerns nematicidal compounds, their formulation as nematicidal composition and their use for controlling nematodes, preferably plant parasitic nematodes.Type: ApplicationFiled: December 16, 2005Publication date: June 19, 2008Applicant: Devgen NVInventors: Jan Octaaf De Kerpel, Dirk Leysen
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Publication number: 20080139619Abstract: A subject of the present application is novel derivatives of benzimidazole and imidazo-pyridine which have a good affinity for certain sub-types of melanocortin receptors, in particular the MC4 receptors. They are particularly useful for treating pathological conditions and diseases in which one or more melanocortin receptors are involved. The invention also relates to pharmaceutical compositions containing said products.Type: ApplicationFiled: January 31, 2008Publication date: June 12, 2008Inventors: Lydie Poitout, Valerie Brault, Carole Sackur, Pierre Roubert, Pascale Plas
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Publication number: 20080140450Abstract: The invention relates to methods of treating metabolic syndrome, or the specific disorders associated with metabolic syndrome, comprising the administration of norfluoxetine enriched for the (R) or (S) enantiomer conjointly with a statin, a calcium channel blocker, halofenate, captopril, or an imidazoline receptor agonist (e.g., an I1, I2, or I3 receptor agonist).Type: ApplicationFiled: November 28, 2007Publication date: June 12, 2008Applicant: AMPLA Pharmaceuticals Inc.Inventor: James R. Hauske
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Patent number: 7375125Abstract: Provided are MC4-R binding compounds of the formula XVII: wherein L2 is a linker group, and P1, P2, P3, P4, Z1, Z2, Z3, Z4, Z5, t, s, and R are as described in the specification. Methods of using the compounds to treat MC4-R associated disorders, such as disorders associated with weight loss, are also provided.Type: GrantFiled: June 16, 2003Date of Patent: May 20, 2008Assignee: Ore Pharmaceuticals, Inc.Inventors: Tricia J. Vos, Michael E. Solomon, Christopher F. Claiborne, Martin P. Maguire, Mingshi Dai, Michael Patane, Thomas H. Marsilje
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Patent number: 7371773Abstract: The invention provides a drug which inhibits BCRP. A breast cancer resistance protein inhibitor containing, as an active ingredient, a diphenylacrylonitrile derivative represented by the following formula (1): [wherein, each of 8 R's, which are the same or different from one another, represents a hydrogen atom, a hydroxyl group, a nitro group, an amino group, an acetylamino group (—NHCOCH3 group); a cyano group (—CN group); a formyl group (—CHO group), —COOR1 (R1 is hydrogen or C1-C4 alkyl), —O(CH2)nCOOR2 (n=1?7: R2 is hydrogen or C1-C4 alkyl), —OOCCH2CH2COOR3 (R3 is hydrogen, C1-C4 alkyl, (Z)-2-(3,4-dimethoxy-phenyl)-3-(4-hydroxy-phenyl)-acrylonitrile, or glycopyranosyl), a C1-C8 alkoxy group, a C1-C4 alkyl group, a halogen atom, a C1-C4 alkoxy C1-C4 alkoxy C1-C4 alkoxy group, a C2-C8 acyloxy group, a C2-C8 halogenoacyloxy group, a methylenedioxy group, a trifluoromethyl group, a phosphate group (i.e., —OP(O) (OH)2) or a salt thereof, a sulfate group (i.e.Type: GrantFiled: February 3, 2004Date of Patent: May 13, 2008Assignee: Kabushiki Kaisha Yakult HonshaInventors: Ryuta Yamazaki, Yukiko Nishiyama, Tomio Furuta, Takeshi Matsuzaki, Hiroshi Hatano, Oh Yoshida, Masato Nagaoka, Ritsuo Aiyama, Shusuke Hashimoto, Yoshikazu Sugimoto
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Patent number: 7345078Abstract: A new class of imidazolines as 4-position acids or esters with very potent anti-inflammatory as well as antimicrobial activity is described. The synthesis of these imidazolines includes a multicomponent reaction applicable to a combinatorial synthetic approach. The combination of these two key characteristics provides an effective therapeutic drug in the treatment of septic shock as well as many other inflammatory (arthritis and asthma) and infectious disorders. The use of this novel class of non-steroidal agents as anti-inflammatory agents (for the treatment of asthma, etc.), antibacterial agents, and antiseptic agents is described. The compounds are also useful in the treatment of tumors (such as cancers). The imidazolines are potent inhibitors of the transcription factor NF-?B as well as potent activity against the Gram (+) bacterium. The compositions are also useful for treating autoimmune diseases and for inhibiting rejection of organ and tissue transplants.Type: GrantFiled: May 30, 2003Date of Patent: March 18, 2008Assignee: The Board of Trustees of Michigan State UniversityInventors: Jetze J. Tepe, Satyamaheshwar Peddibhotla
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Patent number: 7338970Abstract: Pharmaceutical composition comprising 5 to 20% of an idazoxan salt or of idazoxan hydrate, 10 to 40% of microcrystalline cellulose, 1 to 5% of lubricant, 0.1 to 0.5% of colloidal silica and from 29.5% to 84.8% of lactose, with respect to the total mass.Type: GrantFiled: November 28, 2003Date of Patent: March 4, 2008Assignee: Pierre Fabre MedicamentInventors: Joël Bougaret, Jean-Louis Avan, Roland Segonds
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Publication number: 20080050336Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.Type: ApplicationFiled: August 8, 2007Publication date: February 28, 2008Inventors: Carol Bachand, Makonen Belema, Daniel H. Deon, Andrew C. Good, Jason Goodrich, Clint A. James, Rico Lavoie, Omar D. Lopez, Alain Martel, Nicholas A. Meanwell, Van N. Nguyen, Jeffrey Lee Romine, Edward H. Ruediger, Lawrence B. Snyder, Denis R. St. Laurent, Fukang Yang, David R. Langley, Gan Wang, Lawrence G. Hamann
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Publication number: 20070197621Abstract: The present invention relates a method for treating depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder, stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders which comprises administering to an individual a therapeutically effective amount of a compound of formula I wherein R, R1, R2, A and n are as defined in the specification and to their pharmaceutically active salts. The invention also relates to novel compounds of formula I, pharmaceutical compositions containing them, and methods for their preparation.Type: ApplicationFiled: January 19, 2007Publication date: August 23, 2007Inventors: Guido Galley, Katrin Groebke Zbinden, Marius Hoener, Sabine Kolczewski, Roger Norcross, Henri Stalder
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Publication number: 20070197569Abstract: The present invention relates to a method for treating depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders which comprises administering to an individual a therapeutically effective amount of a compound of formula I wherein R, X, A, and n are as defined in the specification and pharmaceutically active salts, racemic mixtures, enantiomers, optical isomers and tautomeric forms thereof.Type: ApplicationFiled: January 19, 2007Publication date: August 23, 2007Inventors: Marius Hoener, Sabine Kolczewski, Henri Stalder
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Publication number: 20070197620Abstract: The present invention relates to a method for treating a disorder selected from depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder, stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders which comprises administering to an individual a therapeutically effective amount of a compound of formula I wherein R1, R2, Q, W, X, Y, m, and n are as defined in the specification d or not; and their pharmaceutically active salts, racemic mixtures, enantiomers, optical isomers and tautomeric forms.Type: ApplicationFiled: January 19, 2007Publication date: August 23, 2007Inventors: Guido Galley, Katrin Groebke Zbinden, Roger Norcross, Henri Stalder
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Patent number: 7029706Abstract: The inventions relates to the use of silica in the formulation of antifungal composition for the treatment of cutaneous mycoses, and method to manufacture an antifungal powder with boric acid and silica.Type: GrantFiled: November 21, 2002Date of Patent: April 18, 2006Inventor: Carlos Alberto Marrodan
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Patent number: 6956051Abstract: The present invention relates to amphiphilic drug-oligomer conjugates capable of traversing the blood-brain barrier (“BBB”) and to methods of making and using such conjugates. An amphiphilic drug-oligomer conjugates comprise a therapeutic compound conjugated to an oligomer, wherein the oligomer comprises a lipophilic moiety coupled to a hydrophilic moiety. The conjugates of the invention further comprise therapeutic agents such as proteins, peptides, nucleosides, nucleotides, antiviral agents, antineoplastic agents, antibiotics, etc., and prodrugs, precursors, derivatives and intermediates thereof, chemically coupled to amphiphilic oligomers.Type: GrantFiled: October 29, 1999Date of Patent: October 18, 2005Assignee: Nobex CorporationInventors: Nnochiri N. Ekwuribe, Balasingam Rhadakrishnan, Christopher H. Price, Wes Anderson Jr., Aslam M. Ansari
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Patent number: 6878735Abstract: A new class of imidazolines as 4-position acids or esters with very potent anti-inflammatory as well as antimicrobial activity is described. The synthesis of these imidazolines includes a multicomponent reaction applicable to a combinatorial synthetic approach. The combination of these two key characteristics provides an effective therapeutic drug in the treatment of septic shock as well as many other inflammatory (arthritis and asthma) and infectious disorders. The use of this novel class of non-steroidal agents as anti-inflammatory agents (for the treatment of asthma etc.), antibacterial agents and antiseptic agents is described. The compounds are also useful in the treatment of tumors (such as cancers). The imidazolines are potent inhibitors of the transcription factor NF-?B as well as potent activity against the Gram (+) bacterium B. subtillus and B. cereus with MIC values in the range of 50 ?m/mL.Type: GrantFiled: January 17, 2003Date of Patent: April 12, 2005Assignee: Board of Trustees of Michigan State UniversityInventors: Jetze J. Tepe, Satyamaheshwar Peddibhotla
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Patent number: 6852726Abstract: This invention relates to compounds which are alpha-1 receptor agonists, preferably alpha-1A/L receptor agonists, and which are represented by Formula I: wherein X is —S(O)n— or —C(O)—, A is C1-6alkyl, aryl, heteroaryl, hydroxyalkyl, or —(CH2)p—NRaRb, and the other substituents are as defined in the specification; or individual isomers, racemic or non-racemic mixtures of isomers, or pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds, methods for their use as therapeutic agents, and methods of preparation thereof.Type: GrantFiled: January 31, 2003Date of Patent: February 8, 2005Assignee: Syntex LLCInventors: Robert Greenhouse, Saul Jaime-Figueroa, Lubica Raptova
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Patent number: 6835743Abstract: Process for the protection of a building that has already been built or is going to be built, whereby an effective amount of an insecticidally active compound is spread around or under the said building at discrete locations. The insecticide may be an arylpyrazole.Type: GrantFiled: May 13, 2002Date of Patent: December 28, 2004Assignee: Bayer CropScience S.A.Inventor: Yasuo Kimura
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Publication number: 20040147575Abstract: Nitric acid salts with medicines having an antihypertensive activity.Type: ApplicationFiled: September 29, 2003Publication date: July 29, 2004Applicant: Nicox S.A.Inventor: Piero Del Soldato
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Patent number: 6762190Abstract: The present invention relates to compounds of formula (I), in which A, B, X, Y, R1, R2, R3 and n have the meanings indicated in the claims. The compounds of formula (I) are valuable pharmacologically active compounds. They are vitronectin receptor antagonists and inhibitors of cell adhesion and are suitable for the therapy and prophylaxis of illnesses which are based on the interaction between vitronectin receptors and their ligands in cell-cell or cell-matrix interaction processes or which can be prevented, alleviated or cured by influencing such interactions. For example, they can be applied for inhibiting bone resorption by osteoclasts and thus for treating and preventing osteoporosis, or for inhibiting undesired angiogenesis or proliferation of cells of the vascular smooth musculature. The invention furthermore relates to processes for the preparation of compounds of formula (I), their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.Type: GrantFiled: September 23, 2002Date of Patent: July 13, 2004Assignee: Aventis Pharma S.A. Deutschland GmbH Genentech, Inc.Inventors: Thomas Gadek, Jean-Francois Gourvest, Anuschirwan Peyman, Jean-Marie Ruxer, Karl-Heinz Scheunemann
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Patent number: 6756395Abstract: Compounds of the Formula: where R1-R6 are those defined herein and methods for producing the same. Also provided are pharmaceutical compositions comprising a Compound of Formula I and methods for their use as therapeutic agents.Type: GrantFiled: April 22, 2003Date of Patent: June 29, 2004Assignee: Roche Palo Alto LLCInventors: Michael Patrick Dillon, Clara Jeou Jen Lin, Counde O'Yang, Xiaoming Zhang
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Publication number: 20040122053Abstract: This invention relates to IP receptor antagonists selected from the group of compounds represented by Formula I: 1Type: ApplicationFiled: December 9, 2003Publication date: June 24, 2004Inventors: Keith Roger Bley, Robin Douglas Clark, Alam Jahangir, Bruce Andrew Kowalczyk, Francisco Javier Lopez-Tapia, Alexander Victor Muehldorf, Counde O'Yang, Thomas Weitao Sun
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Patent number: 6743817Abstract: Disclosed are compounds of the formula and the pharmaceutically acceptable salts thereof wherein R, Ar, A, n, R1 and R2 are defined herein. These compounds are highly selective agonists, antagonists or inverse agonists for GABAA brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAA brain receptors and are therefore useful in the diagnosis and treatment of anxiety, depression, Down Syndrome, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory. Pharmaceutical compositions, including packaged pharmaceutical compositions, are also disclosed.Type: GrantFiled: September 6, 2001Date of Patent: June 1, 2004Assignee: Neurogen CorporationInventors: George Maynard, LingHong Xie, Stanislaw Rachwal
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Publication number: 20040087638Abstract: Compounds of formula (I): 1Type: ApplicationFiled: October 20, 2003Publication date: May 6, 2004Inventors: Sylvain Rault, Marina Kopp, Jean-Charles Lancelot, Stephane Lemaitre, Daniel-Henri Caignard, Jean-Guy Bizot-Espiard, Pierre Renard
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Patent number: 6720317Abstract: Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.Type: GrantFiled: September 15, 2000Date of Patent: April 13, 2004Assignee: Millennium Pharmaceuticals, Inc.Inventors: Bing-Yan Zhu, Zhaozhong Jon Jia, Wenrong Huang, Yonghong Song, James Kanter, Robert M. Scarborough
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Patent number: 6699862Abstract: Novel indolyl-2-phenyl bisamidines are described which are DNA methyltransferase inhibiting agents, and pharmaceutical compositions containing them are used as antiproliferative agents for treating a disease, especially a neoplastic disease, characterized by abnormally rapid proliferation of tissue involved in said disease; said indolyl-2-phenyl bisamidines comprising a and a pharmaceutically acceptable salt thereof, wherein: R1 is hydrogen or (C1-C3)alkyl; R3, R4, R5, R8, R9, and R10 are hydrogen or (C1-C3)alkyl, or R3 and R4 may be taken together, or R8 and R9 may be taken together with the nitrogen atoms to which they are attached, to form an imidazolinyl group; R14 is —H; —NHC(═O)(CH2)mR20; —(CH2)mR20; —CH(CH3)R20; —(CH2)m(C6H3)—R17; —(CH2)m(C6H3)—R20; —(CH2)m(heterocyclyl)—R17; —(CH2)m(heterocyclyl)—R20; —CH2CH═CHR20; —(CH2)mC(═O)NH—CHR20R21; or —(CH2)mC(═O)NH—CH2&mType: GrantFiled: March 24, 2000Date of Patent: March 2, 2004Assignee: Pfizer Inc.Inventors: Steven W. Goldstein, Banauara L. Mylari, Jose R. Perez, Edward A. Glazer
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Patent number: 6680312Abstract: The present invention is to provide a compound or a salt thereof represented by the formula: wherein R1 is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, the ring A is an optionally substituted divalent nitrogen-containing heterocyclic group, X′ is an optionally substituted alkylene chain, Y is an optionally substituted divalent cyclic group, X is a chemical bond or an optionally substituted alkylene chain, and Z is (1) an optionally substituted amino group, (2) an optionally substituted imidoyl group or (3) an optionally substituted nitrogen-containing heterocyclic group, or a pro-drug thereof, which has activated coagulation factor X inhibitory activity and which are useful as anti-coagulants.Type: GrantFiled: April 24, 2002Date of Patent: January 20, 2004Assignee: Takeda Chemical Industries, Ltd.Inventors: Hiroyuki Tawada, Fumio Itoh, Hiroshi Banno, Zen-ichi Terashita
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Patent number: 6677341Abstract: The invention relates to substituted aryl and heteroaryl (R)-Chiral Halogenated 1-Substitutedamino-(n+1)-Alkanol compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Novel high yield, stereoselective processes for the preparation of the chiral substituted alkanol compounds from chiral and achiral intermediates are described. Preferred (R)-Chiral 1-Substitutedamino-(n+1)-Alkanol compounds are substituted (R)-Chiral heteroaryl aminoalcohols.Type: GrantFiled: December 12, 2001Date of Patent: January 13, 2004Assignee: Pharmacia CorporationInventors: James A. Sikorski, Richard C. Durley, Margaret L. Grapperhaus, Mark A. Massa, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Brian S. Hickory, Monica B. Norton, William F. Vernier, Deborah A. Mischke, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
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Publication number: 20030229123Abstract: This invention relates to IP receptor antagonists selected from the group of compounds represented by Formula I: 1Type: ApplicationFiled: April 29, 2003Publication date: December 11, 2003Inventors: Keith Roger Bley, Robin Douglas Clark, Alam Jahangir, Bruce Andrew Kowalczyk, Francisco Javier Lopez-Tapia, Alexander Victor Muehldorf, Counde O'Yang, Thomas Weitao Sun
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Patent number: 6632815Abstract: Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.Type: GrantFiled: February 28, 2001Date of Patent: October 14, 2003Assignee: Millennium Pharmaceuticals, Inc.Inventors: Bing-Yan Zhu, Zhaozhong Jon Jia, Wenrong Huang, Yonghong Song, James Kanter, Robert M. Scarborough
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Patent number: 6610725Abstract: The present invention relates to novel fluorinated benzodioxane imidazoline derivatives, to their preparation and to their therapeutic applications. The invention is directed more particularly toward the compounds corresponding to the structure of general formula 1: in which: R represents a linear, branched or cyclized alkyl or alkenyl group containing 1 to 7 carbon atoms, or a benzyl group, and the fluorine atom can occupy position 5, 6, 7 or 8, in their racemic form and their dextrorotatory and levorotatory pure enantiomeric forms, and also the addition salts thereof.Type: GrantFiled: May 7, 2002Date of Patent: August 26, 2003Assignee: Pierre Fabre MedicamentInventors: Thierry Imbert, Patrice Mayer, Marc Marien, Peters Pauwels
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Patent number: 6596745Abstract: Provided is a method of treating or ameliorating hypertension in an animal comprising administering an effective amount of a compound of formula I:Type: GrantFiled: May 30, 2002Date of Patent: July 22, 2003Assignee: Alteon, Inc.Inventor: Martin Gall
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Publication number: 20030114425Abstract: The present invention relates to the use of &agr;1L-agonists for treating urinary incontinence.Type: ApplicationFiled: November 15, 2002Publication date: June 19, 2003Applicant: Boehringer Ingelheim Pharma KGInventors: Franz Esser, Helmut Stahle, Sven Luttke, Ikonobu Muramatsu, Hisato Kitagawa, Shuji Uchida
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Publication number: 20030105147Abstract: This invention is directed to novel indole and benzothiazole compounds which are selective for cloned human alpha 2 receptors. This invention is also related to uses of these compounds for any indication where use of an alpha 2 agonist may be appropriate. specifically, this includes use as analgesic, sedative and anaesthetic agents. In addition, this invention includes using such compounds for lowering intraocular pressure, presbyopia, treating migraine, hypertension, alcohol withdrawal, drug addiction, rheumatoid arthritis, ischemic pain, spasticity, diarrhea, nasal decongestion, urinary incontinence as well as for use as cognition enhancers and ocular vasoconstriction agents. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.Type: ApplicationFiled: October 22, 2002Publication date: June 5, 2003Applicant: SYNAPTIC PHARMACEUTICAL CORPORATIONInventors: Yoon T. Jeon, Charles Gluchowski
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Publication number: 20030092741Abstract: Aspects of the present invention are directed towards compounds of Formula I for the treatment of human erectile disorders including erectile dysfunction in men.Type: ApplicationFiled: August 9, 2002Publication date: May 15, 2003Inventors: Duane D. Miller, Seoung-Soo Hong
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Patent number: 6528535Abstract: The present invention provide compounds of Formula I The present invention also provides a method of treating cancer and treating or preventing restenosis or atherosclerosis. Also provided by the present invention is a pharmaceutically acceptable composition containing a compound of Formula I.Type: GrantFiled: July 23, 2001Date of Patent: March 4, 2003Assignee: Warner-Lambert CompanyInventors: Jack Bikker, Ellen Myra Dobrusin, Annette Marian Doherty, Matthew Drowns, James Stanley Kaltenbronn, Juergen Kleinschroth, Dennis Joseph McNamara, John Quin, III, Joseph Thomas Repine, Marcin Stasiak
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Patent number: 6525086Abstract: The present invention relates to compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, A, X, T, Q, Z, U, Y, Ar, p and n are as defined in the specification. These 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: March 14, 2001Date of Patent: February 25, 2003Assignee: Novo Nordisk A/SInventors: Lone Jeppesen, Paul Stanley Bury, Per Sauerberg
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Publication number: 20020091147Abstract: This invention relates to compounds which are generally IP receptor modulators, particularly IP receptor antagonists, and which are represented by Formula I: 1Type: ApplicationFiled: November 13, 2001Publication date: July 11, 2002Inventor: Alam Jahangir
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Patent number: 6410539Abstract: The present invention relates to a compound of Formula (1) wherein Ar1 represent (A) or (B) or (C); R1 is hydrogen, C1-4alkyl or C1-4alkanoyl; R12 and R13 are independently hydrogen or C1-4alkyl; Ar2 is phenyl or heteroaryl; p is 0 or 1; Ar3 is of formula (I) wherein W, X, Y and Z are independently CH or N, provided that at least two of W, X, Y and Z are CH and R2 and —(CH2)nR3 are attached to ring carbon atoms; R2 is a group of Formula (II) or R2 represents a lactone of Formula (III) the group of Formula (II) or (III) having L or D configuration at the chiral alpha carbon in the corresponding free amino acid; n is 0, 1 or 2; R3 is phenyl or heteroaryl; provided that: when n is 0, Ar3 is substituted by R2 in the 4-position and —(CH2)nR3 in the 3- or 5-position; and when n is 1 or 2, Ar3 is substituted by R2 in the 3- or 5-position and —(CH2)nR3 in the 4-position; and R5-R9, m and n are as defined in the specification; or a pharmaceutically-acceptable salt, prodrug or solvate thereof.Type: GrantFiled: March 24, 2000Date of Patent: June 25, 2002Assignees: Astrazenca UK Limited, Zeneca Pharma SAInventor: Jean-Claude Arnould
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Patent number: 6348464Abstract: The present invention relates to pharmaceutical compositions and methods of using pyrrolecarbonylimino derivatives to inhibit N-Acetylated &agr;-Linked Acidic Dipeptidase (NAALADase) enzyme activity, thereby effecting neuronal activities, inhibiting angiogenesis, and treating glutamate abnormalities, compulsive disorders, prostate diseases and cancers.Type: GrantFiled: November 12, 1999Date of Patent: February 19, 2002Assignee: Guilford Pharmaceuticals, Inc.Inventors: Paul F. Jackson, Barbara S. Slusher
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Patent number: 6331552Abstract: Substituted imidazolidine derivatives of the formula I, in which B, E, W, Y, R, R2, R3, R30, e and h have the meanings indicated in the claims. The compounds of the formula I are valuable pharmaceutical active compounds, which are suitable, for example, for the therapy of inflammatory disorders, for example of rheumatoid arthritis, or of allergic disorders. The compounds of the formula I are inhibitors of the adhesion and migration of leucocytes and/or antagonists of the adhesion receptor VLA-4 belonging to the integrins group. They are generally suitable for the therapy or prophylaxis of illnesses which are caused by an undesired extent of leucocyte adhesion and/or leucocyte migration or are associated therewith, or in which cell-cell or cell-matrix interactions which are based on interactions of VLA-4 receptors with their ligands play a part.Type: GrantFiled: March 1, 2000Date of Patent: December 18, 2001Assignee: Aventis Pharma Deutschland GmbHInventors: Volkmar Wehner, Hans Ulrich Stilz, Wolfgang Schmidt, Dirk Seiffge
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Patent number: 6319935Abstract: A compound of formula I in which: ring A is one of the five alternative multi-cyclic rings as shown wherein a dotted line adjacent to a bond indicates that a single bond or a double bond may be present at that position; X is nitrogen, oxygen or sulfur; R is hydrogen, lower straight or branched chain alkyl of 1 to 6 carbon atoms, or lower straight or branched chain alkenyl of 2 to 6 carbon atoms, a cycloaliphatic ring of 3 to 6 carbon atoms, phenyl optionally mono- or di-substituted with hydroxy, halogen, alkyl of 1 to 3 carbon atoms or alkoxy of 1 to 2 carbon atoms, or methylenedioxyphenyl; or a stereoisomer, or a pharmaceutically acceptable salt thereof. These compounds have &agr;2 receptor blocking activity and hence find use in the treatment or palliation of elevated intraocular pressure, non insulin-dependent diabetes, male impotence and obesity.Type: GrantFiled: April 4, 2000Date of Patent: November 20, 2001Assignee: Allergan Sales, Inc.Inventors: Stephen A. Munk, Michael E. Garst, James A. Burke
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Patent number: 6232336Abstract: The present invention relates to nitric oxide-releasing amidine- and enamide-derived diazeniumdiolates, compositions comprising such compounds, methods of using such compounds and compositions, a method for the preparation of nitric oxide-releasing amidine- and enamide-derived diazeniumdiolates via the direct reaction of nitric oxide with amidines and enamides, and a method of converting amines into such compounds.Type: GrantFiled: March 30, 2000Date of Patent: May 15, 2001Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Joseph A. Hrabie, Larry K. Keefer
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Patent number: 6191159Abstract: The present application describes disubstituted pyrazolines and triazolines of formulae I and II: or pharmaceutically acceptable salt forms thereof, wherein one of M1 and M2 maybe N and D may be a variety of N-containing groups, which are useful as inhibitors of factor Xa.Type: GrantFiled: March 26, 1999Date of Patent: February 20, 2001Assignee: Dupont Pharmaceuticals CompanyInventor: Donald J. P. Pinto
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Patent number: 6175013Abstract: This invention provides a series of substituted 2-imidazolines which are useful in the treatment or prevention of a physiological disorder associated with an excess of tachykinins. This invention also provides methods for the treatment of such physiological disorders as well as pharmaceutical formulations which employ these compounds.Type: GrantFiled: June 10, 1994Date of Patent: January 16, 2001Assignee: Eli Lilly and CompanyInventors: Philip A. Hipskind, J. Jeffry Howbert, Brian S. Muehl
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Patent number: 6162818Abstract: This invention involves compounds having the following structure: ##STR1## wherein: a) R.sub.1 is hydrogen; or alkyl; bond (a) is a single or a double bond;b) R.sub.2 and R.sub.3 are each independently selected from hydrogen; unsubstituted C.sub.1 -C.sub.3 alkanyl, alkenyl or alkynyl; cycloalkanyl, cycloalkenyl; unsubstituted C.sub.1 -C.sub.3 alkylthio or alkoxy; hydroxy; thio; nitro; cyano; amino; C.sub.1 -C.sub.3 alkylamino or C.sub.1 -C.sub.3 dialkylamino and halo;c) R.sub.4, R.sub.5 and R.sub.6 are each independently selected from hydrogen; unsubstituted C.sub.1 -C.sub.3 alkanyl, alkenyl or alkynyl; cycloalkanyl, cycloalkenyl; unsubstituted C.sub.1 -C.sub.3 alkylthio or alkoxy; hydroxy; thio; nitro; cyano; amino; C.sub.1 -C.sub.3 alkylamino or C.sub.1 -C.sub.3 dialkylamino; halo; and 2-imidazolinylamino; and wherein one and only one of R.sub.4, R.sub.5 and R.sub.6 is 2-imidazolinylamino;d) R.sub.7 is selected from hydrogen; unsubstituted C.sub.1 -C.sub.Type: GrantFiled: April 13, 1999Date of Patent: December 19, 2000Assignee: The Procter & Gamble CompanyInventors: Raymond Todd Henry, Russell James Sheldon, William Lee Seibel
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Patent number: 6159998Abstract: This invention is directed to novel indole and benzothiazole compounds which are selective for cloned human alpha 2 receptors. This invention is also related to uses of these compounds for any indication where use of an alpha 2 agonist may be appropriate. Specifically, this includes use as analgesic, sedative and anaesthetic agents. In addition, this invention includes using such compounds for lowering intraocular pressure, presbyopia, treating migraine, hypertension, alcohol withdrawal, drug addiction, rheumatoid arthritis, ischemic pain, spasticity, diarrhea, nasal decongestion, urinary incontinence as well as for use as cognition enhancers and ocular vasoconstriction agents. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.Type: GrantFiled: January 27, 2000Date of Patent: December 12, 2000Assignee: Synaptic Pharmaceutical CorporationInventors: Yoon T. Jeon, Charles Gluchowski
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Patent number: 6153638Abstract: The invention concerns the use of efaroxan or therapeutically-acceptable salts, in its racemic form or in the form of an optically-active isomer, for treating Huntington's disease.Type: GrantFiled: February 12, 1999Date of Patent: November 28, 2000Assignee: Pierre Fabre MedicamentInventors: Marc Marien, Jean-Claude Martel, Francis Colpaert, Thierry Imbert
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Patent number: 6103744Abstract: Disclosed are compounds of the formula ##STR1## wherein: R.sup.1 is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sup.2 is selected from hydrogen, straight-chain and branched C.sub.1 -C.sub.10 alkyl, cyclohexylmethyl or --(CH.sub.2).sub.m Ar where Ar is phenyl, naphthyl, thienyl, furanyl or pyridinyl, each optionally substituted by one or two substituents selected independently from C.sub.1 -C.sub.6 alkyl, halogen, C.sub.1 -C.sub.6 alkoxide and trifluoromethyl;or NR.sup.1 R.sup.2 is 1, 2, 3, 4-tetrahydroquinolin-1-yl or 1, 2, 3, 4-tetrahydroisoquinolin-2-yl;m is 1-5;n is 1 or 2;R.sup.3 is hydrogen or C.sub.1 -C.sub.6 alkyl;Y is halogen, C.sub.1 -C.sub.6 alkyl, and C.sub.1 -C.sub.6 alkoxy;or a pharmaceutically acceptable salt thereof, which are dopamine autoreceptor agonists and as such are useful in the treatment of schizophrenia, Parkinson's disease, Tourette's syndrome, alcohol addiction and drug addiction.Type: GrantFiled: September 10, 1999Date of Patent: August 15, 2000Assignee: American Home Products CorporationInventors: Richard Eric Mewshaw, James Albert Nelson, Uresh Shantilal Shah
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Patent number: 6093727Abstract: This invention is directed to novel imidazole and imidazoline derivatives which are selective agonists for cloned human a, adrenergic receptors. This invention is also related to the use of these compounds for the treatment of any disease where modulation of the .alpha..sub.2 receptors may be useful. The invention further provides for a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.Type: GrantFiled: October 20, 1998Date of Patent: July 25, 2000Assignee: Synaptic Pharmaceutical CorporationInventors: Wai C. Wong, Yoon T. Jeon, Charles Gluchowski