Nitrogen Or -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To Ring Carbon Of The 1,4-diazine Ring Patents (Class 514/255.06)
-
Publication number: 20040033267Abstract: Nanoparticulate compositions comprising at least one poorly soluble angiogenesis inhibitor and at least one surface stabilizer are described. The nanoparticulate compositions have an average particle size of less than about 2000 nm. The invention also describes methods of making and using such compositions.Type: ApplicationFiled: March 20, 2003Publication date: February 19, 2004Applicant: Elan Pharma International Ltd.Inventors: Elaine Merisko-Liversidge, H. William Bosch, Greta A. Cary, John Pruitt, Tuula Ryde, Rajeev Jain, Amy Walters
-
Patent number: 6693094Abstract: 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.Type: GrantFiled: March 7, 2002Date of Patent: February 17, 2004Assignee: Chrono RX LLCInventors: Don C. Pearson, Kenneth T. Richardson
-
Publication number: 20040029871Abstract: Use of an MPO inhibitor for the treatment of COPD.Type: ApplicationFiled: December 7, 2002Publication date: February 12, 2004Inventors: Kam-Wah Thong, Anthony J Kettle
-
Publication number: 20040029873Abstract: Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.Type: ApplicationFiled: December 11, 2002Publication date: February 12, 2004Inventors: Francine S. Grant, Andrei W. Konradi, Michael A. Pleiss, Eugene D. Thorsett
-
Publication number: 20040029881Abstract: The invention relates to novel substituted iminoazines of the general formula (I) 1Type: ApplicationFiled: November 15, 2002Publication date: February 12, 2004Inventors: Klaus- Helmut Muller, Mark Wilhelm Drewes, Peter Dahmen, Dieter Feucht, Rolf Pontzen
-
Publication number: 20040029883Abstract: The present invention relates to compounds of general formula (I), wherein the residues R represent organic radicals, X represents a bond, oxygen or —NR12 and Y represents oxygen or sulfur, processes for their preparation, pharmaceutical compositions containing them as well as their use for the production of pharmaceutical compositions for the treatment of inflammatory, autoimmune and immune diseases.Type: ApplicationFiled: November 19, 2002Publication date: February 12, 2004Inventors: Markus Albers, Thomas Lehmann, Thomas Rlle, Gerhard Mller, Gerhard Hessler, Masaomi Tajimi, Karl Ziegelbauer, Hiromi Okigami, Haruki Hasegawa
-
Patent number: 6689780Abstract: This application relates to heteroaromatic amides (or a pharmaceutically acceptable salt thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.Type: GrantFiled: June 8, 2001Date of Patent: February 10, 2004Assignee: Eli Lilly and CompanyInventors: Douglas Wade Beight, Trelia Joyce Craft, Jeffry Bernard Franciskovich, Theodore Goodson, Jr., Steven Edward Hall, David Kent Herron, Sajan Joseph, Valentine Joseph Klimkowski, Jeffrey Alan Kyle, John Joseph Masters, David Mendel, Guy Milot, Marta Maria Piñeiro-Nuñez, Jason Scott Sawyer, Robert Theodore Shuman, Gerald Floyd Smith, Anne Louise Tebbe, Jennifer Marie Tinsley, Leonard Crayton Weir, James Howard Wikel, Michael Robert Wiley, Ying Kwong Yee
-
Patent number: 6686364Abstract: This invention is directed to benzamidine derivatives which are useful as anti-coagulants. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat disease-states characterized by thrombotic activity.Type: GrantFiled: August 7, 2001Date of Patent: February 3, 2004Assignee: Berlex Laboratories, Inc.Inventors: Brad O. Buckman, David D. Davey, William J. Guilford, Michael M. Morrissey, Howard P. Ng, Gary B. Phillips, Shung C. Wu, Wei Xu
-
Publication number: 20040019038Abstract: Disclosed are novel aromatic compounds which are useful for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are pharmaceutical compositions containing and processes of making such compounds.Type: ApplicationFiled: July 21, 2003Publication date: January 29, 2004Applicant: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Pier F. Cirillo, Steffen Breitfelder, Usha R. Patel, John Robert Proudfoot, Alan D. Swinamer, Hidenori Takahashi, Thomas A. Gilmore, Rajiv Sharma
-
Publication number: 20040014761Abstract: A topical pharmaceutical composition is provided for the treatment of female sexual dysfunction, wherein the composition is formulated so as to contain a therapeutically effective amount of a phosphodiesterase inhibitor and a pharmaceutically acceptable carrier for topical administration. The phosphodiesterase inhibitor is generally selected from Type III, Type IV, Type V, and nonspecific phosphodiesterase inhibitors.Type: ApplicationFiled: October 22, 2002Publication date: January 22, 2004Inventors: Virgil A. Place, Leland F. Wilson, Paul C. Doherty, Mark S. Hanamoto, Alfred P. Spivack, Neil Gesundheit, Sean R. Bennett, Jane Doherty
-
Publication number: 20040006230Abstract: The invention relates to substituted polycyclic aryl and heteroaryl pyrazinone compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a variety of thrombotic conditions including coronary artery and cerebrovascular diseases.Type: ApplicationFiled: July 15, 2002Publication date: January 8, 2004Applicant: Pharmacia CorporationInventors: Michael S. South, Brenda L. Case, Thomas A. Dice, Ricky L. Fenton, Gary W. Franklin, Michael J. Hayes, Horng-Chih Huang, Wei Huang, Darin E. Jones, Carrie L. Kusturin, Richard J. Lindmark, Scott A. Long, William L. Neumann, David B. Reitz, John I. Trujillo, Ching-Cheng Wang, Rhonda Wood, Qingping Zeng, Matthew W. Mahoney, John J. Parlow, Melvin L. Rueppel
-
Publication number: 20030232841Abstract: A compound of the formula 1Type: ApplicationFiled: June 20, 2003Publication date: December 18, 2003Applicant: Pfizer IncInventor: Harry R. Howard
-
Publication number: 20030225087Abstract: The present invention provides novel N-alkyl-N-phenylhydroxylamine derivatives containing metal chelating groups, a process for preparing the same, the use of the novel compounds as therapeutics for treating and/or preventing various medical dysfunctions and diseases arising from reactive oxygen species (ROS) and/or excess Zn ions, in particular stroke, Parkinson's disease and Alzheimer's disease. The compounds of the invention possess similar or superior LPO inhibition activity to the reference compounds of Trolox and Ebselen. While showing lower toxicity, they also effectively inhibit the cerebral neuronal cell death caused by ROS and/or zinc ion, and show neuroprotective effects against ischemic neuronal degeneration.Type: ApplicationFiled: June 5, 2003Publication date: December 4, 2003Inventors: Eu-Gene Oh, Sung-Bo Ko, Won-Yeob Kim, Kyung-Hwa Kim, Dennis W. Choi, Laura L. Dugan, Tae-Cheon Kang, Jae-Young Koh, Kyung-Mi Kim, In-Jae Shin
-
Publication number: 20030225076Abstract: Diarylanines, such as 5-amide substituted diarylamines of formula (I) or formula (II) wherein A is hydroxy, C1-6 alkoxy, or NR6OR7; X is OR12, NR13R12, or NR14; inhibitors of MEK and are useful in the treatment of a variety of proliferative disease states, such as conditions related to the hyperactivity of MEK, as well as diseases modulated by the MEK cascade.Type: ApplicationFiled: September 13, 2002Publication date: December 4, 2003Inventors: Cathlin Biwersi, Haile Tecle, Joseph Scott Warmus
-
Patent number: 6656931Abstract: This invention provides methods of increasing urine flow in humans while minimizing the loss of electrolytes or ions, the methods comprising administering to a human in need thereof a combination of N-[4-(5H-pyrrolo[2,1-c][1,4]benzodiazepin-10(11H)ylcarbonyl)-3-chlorophenyl]-5-fluoro-2-methylbenzamide (or a pharmaceutically acceptable salt thereof), also known as VPA-985, and one or more diuretic agents, as well as pharmaceutical compositions and kits or packages for such combinations.Type: GrantFiled: June 4, 2002Date of Patent: December 2, 2003Assignee: Wyeth Holdings CorporationInventors: Evelyn Ellis-Grosse, Gayle P. Orczyk
-
Patent number: 6649613Abstract: Diacylhydrazine derivatives of general formula (I) wherein X, Y, Z, R1, 2 and R3 are as defined herein, and their physiologically acceptable salts or solvates thereof, are integrin inhibitors and can be used to combat thromboses, myocardial infarcts, coronary cardiac diseases, arteriosclerosis, inflammations, tumors, osteoporosis, infections, and restenosis following angioplasty or during pathological processes that are maintained or propagated by angiogenesis.Type: GrantFiled: January 14, 2002Date of Patent: November 18, 2003Assignee: Merck Patent GmbHInventors: Günter Hölzemann, Simon Goodman, Horst Kessler, Christoph Gibson, Gabór Sulyok
-
Publication number: 20030203903Abstract: A method for treatment of bacterial infections with rifalazil administered once-weekly, or twice-weekly. A method for treatment of tuberculosis caused by Mycobacterium tuberculosis, infections caused by Mycobacterium avium complex, infections caused by Chlamydia pneumoniae and infections caused by Helicobacter pylori by administering to a patient suffering from the bacterial infection 1-100 mg of rifalazil once or twice a week. In this dose regimen, the treatment is fast, efficacious and eliminates undesirable secondary symptoms observed with daily doses of 1-50 mg of rifalazil.Type: ApplicationFiled: September 14, 2002Publication date: October 30, 2003Inventors: Lynn M. Rose, David J. Porubek, Alan B. Montgomery
-
Publication number: 20030198617Abstract: The present invention provides compositions and methods for treatment of a variety of disease states. The methods generally comprise administering to a host a therapeutically effective amount of a dipeptide having the formula X-Tryptophan or a pharmaceutically acceptable salt thereof, wherein x is glutamine, glutamate, leucine, or isoleucine. The present invention is useful for treatment of infections hyperimmune states, immunodeficiencies, and the like.Type: ApplicationFiled: June 6, 2002Publication date: October 23, 2003Inventors: Lawrence Green, Nicolay V. Sinackevich
-
Publication number: 20030199456Abstract: The present invention relates to sodium channel blockers. The present invention also relates to a variety of methods of treatment using the sodium channel blockers.Type: ApplicationFiled: February 19, 2002Publication date: October 23, 2003Applicant: CYFI, INC.Inventor: Michael R. Johnson
-
Publication number: 20030195160Abstract: The present invention relates to sodium channel blockers. The present invention also relates to a variety of methods of treatment using these sodium channel blockers.Type: ApplicationFiled: February 19, 2002Publication date: October 16, 2003Applicant: CYFI, INC.Inventor: Michael R. Johnson
-
Publication number: 20030186984Abstract: The present invention relates to compounds of formula (I) 1Type: ApplicationFiled: December 5, 2002Publication date: October 2, 2003Inventors: Jean Ackermann, Johannes Aebi, Henrietta Dehmlow, Hans-Peter Maerki, Olivier Morand
-
Patent number: 6624180Abstract: The present invention relates to compounds, and prodrugs thereof, composition and methods useful for preventing and treating thrombotic conditions in mammals. The compounds of the present invention, and prodrugs thereof, selectively inhibit certain proteases of the coagulation cascade.Type: GrantFiled: November 20, 2001Date of Patent: September 23, 2003Assignee: Pharmacia CorporationInventors: Michael J. South, Brenda Case, Danny J. Garland, Michael J. Hayes, Horng-Chih Huang, Wei Huang, Darin E. Jones, William L. Neumann, John J. Parlow, David B. Reitz, Melvin L. Rueppel, Rondald K. Webber
-
Publication number: 20030171300Abstract: The present invention concerns the use of compounds of the Formula (I) for treating different types and symptoms of acute and chronic pain, especially non neuropathic inflammatory pain in mammals. The pain to be treated may be e.g. chronic inflammatory pain, rheumatoid arthritis pain and/or secondary inflammatory osteoarthritic pain. The compounds show an antinociceptive profile and differ from classical analgesics like opioids and non-steroidal anti-inflammatory drugs (NSAIDS) and are useful as specific analgesics.Type: ApplicationFiled: February 11, 2003Publication date: September 11, 2003Inventor: Norma Selve
-
Publication number: 20030166509Abstract: The present invention features pharmaceutical compositions comprising nanoparticles containing a sustained release bioactive agent, method of making such compositions, and method of therapy using such compositions.Type: ApplicationFiled: November 20, 2002Publication date: September 4, 2003Applicant: Advanced Inhalation Research, Inc.Inventors: David A. Edwards, Richard P. Batycky, Jennifer L. Schmitke, Nicolas Tsapis, David A. Weitz, Jeffrey S. Hrkach
-
Patent number: 6608067Abstract: The present invention relates to compounds, methods and pharmaceutical compositions for inhibiting proteases, particularly serine proteases, and more particularly HCV NS3 proteases. The compounds, and the compositions and methods that utilize them, can be used, either alone or in combination to inhibit viruses, particularly HCV virus.Type: GrantFiled: September 29, 2000Date of Patent: August 19, 2003Assignee: Vertex Pharmaceuticals IncorporatedInventors: Roger D. Tung, Govinda Rao Bhisetti, Luc J. Farmer
-
Publication number: 20030149053Abstract: The present invention relates to a process for the preparation of both the phenyl pyrazine derivative 2,6-diamino-3-(2,3,5-trichlorophenyl)pyrazine and an intermediate in the synthesis of 2,6-diamino-3(2,3,5-trichlorophenyl)pyrazine, 2-{[Cyano-(2,3,5-trichlorophenyl)-methyl]-amino}-acetamidine or a salt thereof.Type: ApplicationFiled: November 5, 2002Publication date: August 7, 2003Inventors: Dean David Edney, Andrew Kennedy
-
Publication number: 20030144297Abstract: Substituted aryl 1,4-pyrazine derivatives and their use in treating anxiety disorders, depression and stress related disorders are disclosed.Type: ApplicationFiled: November 15, 2002Publication date: July 31, 2003Inventors: Patrick R. Verhoest, Robert Louis Hoffman, Jeffrey W. Corbett, Michael Dalton Ennis, Kristine E. Frank, Jian-Min Fu
-
Publication number: 20030144276Abstract: Described is a heterocycle-containing carboxylic acid derivative represented by the following formula (I): 1Type: ApplicationFiled: January 6, 2003Publication date: July 31, 2003Applicant: Eisai Co. Ltd.Inventors: Kouichi Kikuchi, Katsuya Tagami, Hiroyuki Yoshimura, Shigeki Hibi, Mitsuo Nagai, Shinya Abe, Makoto Okita, Takayuki Hida, Seiko Higashi, Naoki Tokuhara, Seiichi Kobayashi
-
Patent number: 6599905Abstract: Compounds of formula (I) where R1 is phenyl substituted by one or more halogen atoms, naphthyl and naphthyl substituted by one or more halogen atoms; R2 is —NH2 and —NHC(═O)Ra; R3 is —NRbRc, —NHC(═O)Ra or hydrogen; R4 is hydrogen, —C1-4 alkyl, —CN, —CH2OH, —CH2ORd, —CH2S(O)xRd and —C1-4 alkyl substituted by one or more halogen atoms in which Ra represents C1-4 alkyl or C3-7cycloalkyl, and Rb and Rc, which may be the same or different, are hydrogen or C1-4 alkyl, or together with the nitrogen atom to which they are attached, form a 6-membered nitrogen containing heterocycle, which heterocycle can be further substituted with one or more C1-4 alkyl; Rd is C1-4 alkyl or C1-4 alkyl substituted by one or more halogen atoms; x is an integer zero, one or two; and salts, solvates and prodrugs thereof, provided that R1 does not represent: when R2 is —NH2, and both R3 and R4 are hydrogen.Type: GrantFiled: May 16, 2001Date of Patent: July 29, 2003Assignee: SmithKline Beecham CorporationInventors: Brian Cox, Dean David Edney, Michael Simon Loft, Malcolm Stuart Nobbs, Gita Punjabhai Shah
-
Publication number: 20030139402Abstract: Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.Type: ApplicationFiled: September 20, 2002Publication date: July 24, 2003Inventors: Andrei W. Konradi, Michael A. Pleiss, Eugene D. Thorsett, Susan Ashwell, Gregory S. Welmaker, Anthony Kreft, Dimitrios Sarantakis, Darren B. Dressen, Francine S. Grant, Christopher Semko, Ying-Zi Xu
-
Patent number: 6596750Abstract: The use is described of 3,5-diphenyl-1,2,4-triazoles of the formula I in which R1-R5 are as defined in the description. The compounds have useful pharmaceutical properties and are particularly active as iron chelators. They can be used for the treatment of iron overload in warm-blooded animals.Type: GrantFiled: September 23, 2002Date of Patent: July 22, 2003Assignee: Novartis AGInventors: René Lattmann, Pierre Acklin
-
Publication number: 20030134859Abstract: A compound of the following formula or a pharmacologically acceptable salt thereof: 1Type: ApplicationFiled: October 23, 2002Publication date: July 17, 2003Applicant: SANKYO COMPANY, LIMITEDInventors: Yoshiya Amemiya, Kenji Wakabayashi, Sachiko Takaishi, Chie Fukuda
-
Publication number: 20030130169Abstract: Methods for treatment of antibiotic-resistant and multi-drug resistant bacterial infections are provided. The methods comprise administration of compositions which mimic plasmid incompatibility in bacteria, resulting in their sensitization to previously resistant drugs. Also provided herein are methods for screening compositions for the ability to mimic plasmid incompatibility by inhibiting Rep protein or by destabilizing RNA/RNA stem loop “kissing” structures. The invention also encompasses compositions identified by the screening methods disclosed herein.Type: ApplicationFiled: October 1, 2002Publication date: July 10, 2003Applicant: The Board of Trustees of the University of IllinoisInventors: Paul J. Hergenrother, Dinty J. Musk, Johna C.B. DeNap
-
Publication number: 20030130213Abstract: Pyrazine derivatives represented by general formula [1]: 1Type: ApplicationFiled: August 16, 2002Publication date: July 10, 2003Applicant: Toyama Chemical Co., Ltd.Inventors: Hiroyuki Egawa, Yousuke Furuta, Jun Sugita, Sayuri Uehara, Shoichi Hamamoto, Kenji Yonezawa
-
Publication number: 20030125331Abstract: Novel CycloHexenyl-Ethyl-Thiourea (CHET) compounds as inhibitors of reverse transcriptase and effective agents for the treatment of HIV infection, including mutant, drug-sensitive, drug-resistant, and multi-drug resistant strains of HIV.Type: ApplicationFiled: October 22, 2002Publication date: July 3, 2003Applicant: Parker Hughes InstituteInventors: Fatih M. Uckun, Taracad K. Ventatachalam
-
Publication number: 20030125338Abstract: Methods and compositions useful in the treatment of amyloidosis and conditions and diseases associated therewith, such as Alzheimer's disease, are provided. The methods involve administering to a subject in need thereof a pharmaceutical composition including one or more agents that modulate PPAR&agr; and/or PPAR&dgr; activity, resulting in an inhibition of &bgr;-amyloid production and/or release from cells of the subject, particularly brain cells.Type: ApplicationFiled: June 12, 2002Publication date: July 3, 2003Applicant: Active Pass Pharmaceuticals, Inc.Inventors: Bruce P. Connop, Amelia Grant, Parimal S. Nathwani
-
Patent number: 6586416Abstract: Co-administration of a channel blocking epithelial sodium channel (ENaC) blocker in conjunction with a mineralocorticoid receptor inhibitor makes it possible to achieve desired lowering of blood pressure with use in the range of 20% to 75% or less of the presently used dosage of the mineralocorticoid receptor inhibitor (MRI), thus avoiding many of the deleterious side effects usually associated with administration of an MRI. As little as 10% of the usual dosage of MRI may, in some cases, be efficacious. The most commonly used ENaC blocker now in use is amiloride. The most commonly used inhibitors of the mineralocorticoid receptor are precursors of canrenone.Type: GrantFiled: April 19, 2002Date of Patent: July 1, 2003Inventor: James K. Bubien
-
Patent number: 6586433Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine 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. Preferred tertiary-heteroalkylamine compounds are substituted N-heteroaryl-N-phenyl aminoalcohols.Type: GrantFiled: November 14, 2001Date of Patent: July 1, 2003Assignee: Pharmacia CorporationInventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
-
Patent number: 6586459Abstract: This application relates to a compound of formula I (or a prodrug thereof or a pharmaceutically acceptable salt of the compound or prodrug thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.Type: GrantFiled: September 28, 2001Date of Patent: July 1, 2003Inventors: Douglas Wade Beight, Trelia Joyce Craft, Jeffry Bernard Franciskovich, Theodore Goodson, Junior, Steven Edward Hall, David Kent Herron, Valentine Joseph Klimkowski, Jeffrey Alan Kyle, John Joseph Masters, David Mendel, Guy Milot, Jason Scott Sawyer, Robert Theodore Shuman, Gerald Floyd Smith, Anne Louise Tebbe, Jennifer Marie Tinsley, Leonard Crayton Weir, James Howard Wikel, Michael Robert Wiley, Ying Kwong Yee
-
Publication number: 20030119827Abstract: Disclosed are novel nitrile compounds of formula (I) further defined herein, which compounds are useful as reversible inhibitors of cysteine proteases such as cathepsin K, S, F, L and B. These compounds are useful for treating diseases and pathological conditions exacerbated by these proteases such as, but not limited to, osteoporosis, rheumatoid arthritis, multiple sclerosis, asthma and other autoimmune diseases, Alzheimer's disease, atherosclerosis. Also disclosed are processes for making such novel compounds.Type: ApplicationFiled: June 4, 2002Publication date: June 26, 2003Applicant: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Eugene R. Hickey, Younes Bekkali, Usha R. Patel, Denice Mary Spero, David S. Thomson, Erick Richard Roush Young
-
Patent number: 6583173Abstract: This application relates to a compound of formula I (or a prodrug thereof or a pharmaceutically acceptable salt of the compound or prodrug thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.Type: GrantFiled: September 28, 2001Date of Patent: June 24, 2003Assignee: Eli Lilly and CompanyInventors: Douglas Wade Beight, Trelia Joyce Craft, Jeffrey Bernard Franciskovich, Theodore Goodson, Junior, Steven Edward Hall, David Kent Herron, Valentine Joseph Klimkowski, Jeffrey Alan Kyle, John Joseph Masters, David Mendel, Guy Milot, Jason Scott Sawyer, Robert Theodore Shuman, Gerald Floyd Smith, Anne Louise Tebbe, Jennifer Marie Tinsley, Leonard Crayton Weir, James Howard Wikel, Michael Robert Wiley, Ying Kwong Yee
-
Publication number: 20030113352Abstract: Hyperkeratotic skin lesions are treated by the topical administration of inhibitors of hydrogen ion pumps, transporters, and antiporters, or buffers with a pH of 7.0 or greater, and inhibitors of physiological processes that generate free fatty acids from complex lipids.Type: ApplicationFiled: December 14, 2001Publication date: June 19, 2003Applicant: The Regents of the University of CaliforniaInventors: Peter M. Elias, Kenneth R. Feingold, Joachim W. Fluhr, Theodora M. Mauro, Martin J. Behne
-
Publication number: 20030100569Abstract: This invention provides compositions of matter, pharmaceutical compounds, methods of synthesizing such compounds and methods for using such compounds to treat animals infected with a pathogenic mycobacterium. The invention specifically provides compositions and pharmaceutical compositions thereof for the treatment of tuberculosis and other Mycobacterium-caused diseases.Type: ApplicationFiled: November 5, 2001Publication date: May 29, 2003Inventors: Milton B. Yatvin, Richard L. Pederson
-
Patent number: 6569860Abstract: This invention relates to compounds which are IP receptor antagonists and which are represented by Formula (I): wherein G2 is a heteroaryl group containing one or two nitrogen atoms substituted with a carboxylic acid group, said heteroaryl ring containing one or two nitrogen atoms, and G1 is 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: March 1, 2002Date of Patent: May 27, 2003Assignee: Roćhe Palo Alto LLCInventors: Francisco Javier Lopez-Tapia, Dov Nitzan, Counde O'Yang
-
Publication number: 20030092702Abstract: Disclosed are novel aromatic compounds of the formula(I) described herein, wherein G, E, W, Ar, X, Y and Z are disclosed herein. The compounds are useful for treating cytokine mediated diseases or conditions such as chronic inflammatory diseases. Also disclosed are pharmaceutical compositions containing and processes of making such compounds.Type: ApplicationFiled: May 17, 2002Publication date: May 15, 2003Applicant: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Pier Francesco Cirillo, Victor Kamhi, John Robinson Regan, Michele Tsang
-
Publication number: 20030092679Abstract: The present invention provides compounds which have a pyrazinone or pyridinone ring at P3 and an optionally substituted heteroaryl group at P1. These compounds have biological activity as active and potent inhibitors of thrombin. Their pharmaceutically acceptable salts, pharmaceutical compositions thereof and methods of using these compounds and pharmaceutical compositions comprising these compounds as therapeutic agents for treatment of disease states in mammals which are characterized by abnormal thrombosis are also described.Type: ApplicationFiled: July 13, 2001Publication date: May 15, 2003Inventors: Daniel Vanna Siev, Joseph Edward Semple, Mallareddy Komandla, John Eugene Reiner, Scott Jeffrey Kemp
-
Publication number: 20030078235Abstract: Carbamate compounds of 2-heteroaryl-1,2-ethanediol are described. The compounds are effective in the treatment of disorders of the central nervous system, especially as anti-convulsive or anti-epileptic agents.Type: ApplicationFiled: June 21, 2002Publication date: April 24, 2003Inventors: Yong-Moon Choi, Ki-Ho Lee
-
Publication number: 20030073702Abstract: Cyclic oxyguanidine pyrazinone compounds are described, including compounds of the Formula I: 1Type: ApplicationFiled: October 4, 2002Publication date: April 17, 2003Applicant: 3-Dimensional Pharmaceuticals, Inc.Inventors: Aihua Wang, Bruce Edward Tomczuk, Tianbao Lu, Richard M. Soll, John Curtis Spurlino, Roger Francis Bone
-
Patent number: 6548507Abstract: The present invention relates to the use of sodium channel antagonists in the treatment of diseases mediated by, or exacerbated by, neuronal apoptosis, in particular sensory neuronal apoptosis.Type: GrantFiled: October 9, 2001Date of Patent: April 15, 2003Assignee: SmithKline Beecham CorporationInventors: Charanjit Bountra, Malcolm Stuart Nobbs
-
Publication number: 20030060629Abstract: The present invention provides pyrazine derivatives that inhibit tyrosine kinase activity. Certain pyrazine derivatives are selective inhibitors of vascular endothelial growth factor (VEGF) receptor tyrosine kinase. The present invention also provides pharmaceutical formulations containing the pyrazine derivatives and methods of use of these formulations as anti-tumor agents and to treat solid-tumor cancers, angiogenesis, diabetic retinopathy, rheumatoid arthritis, endometriosis and psoriasis.Type: ApplicationFiled: September 19, 2001Publication date: March 27, 2003Inventors: Gee-Hong Kuo, Peter J. Connolly, Catherine Prouty, Alan DeAngelis, Aihua Wang, Linda Jolliffe, Steve Middleton, Stuart Emanuel