The Chalcogen, X, Is In A -c(=x)- Group Patents (Class 548/253)
  • Method of storing tetrazolium compound, stabilizer for use therein, and tetrazolium compound reagent solution stored by the method
    Publication number: 20040157285
    Abstract: A method for storing a tetrazolium compound stably is provided. The tetrazolium compound is stored in the presence of sodium azide. The tetrazolium compound (A) and the sodium azide (B) are present at a ratio (A:B) in the range from 1:0.02 to 1:6.2. Furthermore, when the tetrazolium compound is stored as a solution, the concentration of the sodium azide is in the range from 0.08 to 3.2 mmol/L and the concentration of the tetrazolium compound is in the range from 0.5 to 8 mmol/L. As the tetrazolium compound, it is preferable to use 2-(4-iodophenyl)-3-(2,4-dinitrophenyl)-5-(2,4-disulfophenyl)-2H-tetrazolium salt.
    Type: Application
    Filed: November 24, 2003
    Publication date: August 12, 2004
    Inventors: Kaori Ishimaru, Satoshi Yonehara
  • Delta1 pyrrolines
    Publication number: 20040152904
    Abstract: The invention relates to novel &Dgr;1-pyrrolines of the formula (I) 1
    Type: Application
    Filed: December 12, 2003
    Publication date: August 5, 2004
    Inventors: Andrew Plant, Fritz Maurer, Albrecht Marhold, Christoph Erdelen, Andreas Turberg, Olaf Hansen, Angelika Lubos-Erdelen
  • Colchinol derivatives as angiogenesis inhibitors
    Publication number: 20040142909
    Abstract: The invention related to colchinol derivatives of the formula (I): Wherein; R1; R2 and R3 are each independently hydroxy, phosphoryloxy (—OPO3H2), C1-4alkoxy or an in vivo hydrolysable ester of hydroxy, with the proviso that at least 2 of R1, R2 and R3 are C1-4alkoxy; A is —CO—, —C(O)O—, —CON(R8)— (wherein R8 is hydrogen, C1-4alkyl, C1-3alkoxyC1-3alkyl, aminoC1-3alkyl or hydroxyC1-3alkyl); a is an integer from 1 to 4 inclusive; Ra and Rb are independently selected from hydrogen, hydroxy and amino; B is —O—, —CO—, N(R9)CO—, —CON(R9)—, —N(R9)C(O)O—, —N(R9)CON(R10)—, —N(R9)SO2—, —SO2N(R9)— or a direct single blond (wherein R9 and R10 are independently selected from hydrogen, C1-4alkyl, C1-3alkoxyC1-3alkyl, aminoC1-3alkyl and hydroxyC1-3alkyl); b is O or an integer from 1 to 4 inclusive, (provided that when bis O, B is a single direct bond); D is carboxy, sulpho, tetrazolyl, imidazol
    Type: Application
    Filed: November 12, 2003
    Publication date: July 22, 2004
    Applicant: ANGIOGENE PHARMACEUTICALS LIMITED
    Inventor: Jean Claude Arnould
  • 5-Aryltetrazole compounds, compositions thereof, and uses therefor
    Publication number: 20040116423
    Abstract: The present invention relates to 5-Aryltetrazole Compounds, compositions comprising an effective amount of a a 5-Aryltetrazole Compound, and methods for treating an inflammation disease, a reperfusion disease, or hyperuricemia in an animal in need thereof comprising administering to the animal an effective amount of a 5-Aryltetrazole compound.
    Type: Application
    Filed: July 17, 2003
    Publication date: June 17, 2004
    Inventors: Alex Nivorozhkin, John Van Duzer, Andrew Salzman, Garry Southan, Siya Ram, Qi Zeng, Csaba Szabo
  • Processes for preparing 6-hydroxy-3,4-dihydroquinolinone, cilostazol and N-(4-methoxyphenyl)-3-chloropropionamide
    Patent number: 6740758
    Abstract: A process for preparing 6-hydroxy-3,4-dihydroquinolinone by intramolecular Friedel-Crafts alkylation of N-(4-methoxyphenyl)-3-chloropropionamide in which an equivalent of N-(4-methoxphenyl)-3-chloropropionamide is contacted with a Lewis acid in DMSO or a high boiling amide or amine at an elevated temperature of from about 150° C. to about 220° C. is provided. The process produces 6-HQ in high yield and a high state of purity such that it may be used in subsequent reactions toward the preparation of cilostazol without intermediate purification. A process for preparing cilostazol from 6-hydroxy-3,4-dihydroquinolinone prepared by the process and improved processes for preparing N-(4-methoxyphenyl)-3-chloropropionamide are also provided.
    Type: Grant
    Filed: June 20, 2003
    Date of Patent: May 25, 2004
    Assignee: Teva Pharmaceutical Industries
    Inventors: Marioara Mendelovici, Gideon Pilarsky, Tamar Nidam, Ben-Zion Dolitzky
  • Inhibitors of neuraminidases
    Publication number: 20040097471
    Abstract: Disclosed are compounds of the formula: 1
    Type: Application
    Filed: September 24, 2002
    Publication date: May 20, 2004
    Inventors: Clarence J. Maring, Yu Gui Gu, Hui-Ju Chen, Yuanwei Chen, David A. Degoey, William J. Flosi, Vincent L. Giranda, David J. Grampovnik, Warren M. Kati, Dale J. Kempf, April Kennedy, Larry L. Klein, Allan C. Krueger, Zhen Lin, Darold L. Madigan, Keith F. McDaniel, Steven W. Muchmore, Hing L. Sham, Kent D. Stewart, Vincent S. Stoll, Minghua Sun, Noah P. Tu, Frank L. Wagenaar, Gary T. Wang, Sheldon Wang, Paul E. Wiedeman, Yibo Xu, Ming C. Yeung, Chen Zhao, Stephen Hanessian, Malken Bayrakdarian, Xuehong Luo
  • Angiotensin II antagonists
    Publication number: 20040092563
    Abstract: The present invention relates to the use of an angiotensin II type 1 receptor antagonist of the general formula (I) in the manufacture of a medicament for the prophylactic and/or therapeutic treatment of a vascular headache condition such as migraine, in a subject suffering from, or susceptible to, such a vascular headache condition. A further aspect of the invention is a pharmaceutical formulation useful in any one of said vascular headache conditions, as well as a method of treatment thereof.
    Type: Application
    Filed: December 18, 2002
    Publication date: May 13, 2004
    Inventor: Harald Schrader
  • 8-Azaprostaglandin carbonate and thiocarbonate analogs as therapeutic agents
    Patent number: 6734201
    Abstract: The present invention provides a compound represented by the general formula I; wherein A, Ar, X, Z, n, x, y, R and R3 are as defined in the specification.
    Type: Grant
    Filed: June 2, 2003
    Date of Patent: May 11, 2004
    Assignee: Allergan, Inc.
    Inventors: David W. Old, Thang D. Dinh, Robert M. Burk
  • Substituted tryptophan derivatives
    Patent number: 6727266
    Abstract: A compound of the formula (I): wherein: R1 is represented by the formula: wherein R4, R5, R6, R7 and R8 are monovalent radicals such as: hydrogen, halogen, optionally substituted lower alkyl, lower alkyloxy, lower alkylthio, optionally substituted amino, nitro; non-aromatic heterocyclic group, and the like with certain provisos; Y is —OH or —NHOH; R2 is hydrogen, optionally substituted lower alkyl, or optionally substituted aralkyl; R3 is halogen, hydroxy, lower alkyloxy, or lower alkylthio; (b) n is an integer from 1 to 3; its optically active substance, its prodrug, its pharmaceutically acceptable salt, and its solvate.
    Type: Grant
    Filed: July 10, 2002
    Date of Patent: April 27, 2004
    Assignee: Shionogi & Co., Ltd.
    Inventor: Fumihiko Watanabe
  • Novel spiro[2.4]heptane amino carboxy compounds and derivatives thereof
    Publication number: 20040077599
    Abstract: The present invention relates to therapeutically active novel spiro[2,4]heptane amino carboxy compounds and derivatives thereof. Also provided is a method of preparing compounds of Formula (I), and pharmaceutical compositions comprising the compounds. The novel compounds act as modulators of metabotropic glutamate receptors and, as such, are useful in treating diseases of the central nervous system related to the metabotropic glutamate receptor system.
    Type: Application
    Filed: November 13, 2003
    Publication date: April 22, 2004
    Inventor: Kenneth Curry
  • Heterocyclic aromatic compounds useful as growth hormone secreagogues
    Publication number: 20040072881
    Abstract: Heterocyclic aromatic compounds are provided which are useful in stimulating endogenous production or release of growth hormone and in treating obesity, osteoporosis (improving bone density) and in improving muscle mass and muscle strength.
    Type: Application
    Filed: October 28, 2002
    Publication date: April 15, 2004
    Inventors: Jeffrey A. Robl, Joseph A. Tino, Andres S. Hernandez, Jun Li
  • Imaging agents and methods of imaging NAALADase or PSMA
    Publication number: 20040054190
    Abstract: The present invention relates to compounds particularly asymmetric urea compounds which are labeled with one or more radioisotopes and which are suitable for imaging or therapeutic treatment of tissues, organs, or tumors which express NAALADase and/or PSMA. In another embodiment, the invention relates to methods of imaging tissues, organs, or tumors using radiolabeled compounds of the invention, particularly tissues, organs, or tumors which express NAALADase and/or PSMA to which the compounds of the invention have an affinity.
    Type: Application
    Filed: January 10, 2003
    Publication date: March 18, 2004
    Applicant: Johns Hopkins University
    Inventors: Martin Gilbert Pomper, Jiazhong Zhang, Alan P. Kozikowski, John L. Musachio
  • Glucagon antagonists/inverse agonists
    Patent number: 6706744
    Abstract: Novel compounds, which act to antagonize the action of the glucagon hormone on the glucagon receptor. Owing to their antagonizing effect of the glucagon receptor the compounds may be suitable for the treatment and/or prevention of any diseases and disorders, wherein a glucagon antagonistic action is beneficial, such as hyperglycemia, Type 1 diabetes, Type 2 diabetes, disorders of the lipid metabolism and obesity.
    Type: Grant
    Filed: November 16, 2001
    Date of Patent: March 16, 2004
    Assignee: Novo Nordisk A/S
    Inventors: Peter Madsen, Jesper Lau, Anthony Ling
  • Substituted phenyl derivatives, their preparation and use
    Patent number: 6706749
    Abstract: The present invention discloses compounds having formula (I) wherein the substituents are defined in the application. The compounds are useful as chloride channel blockers.
    Type: Grant
    Filed: April 19, 2001
    Date of Patent: March 16, 2004
    Assignee: NeuroSearch A/S
    Inventors: Bjarne H. Dahl, Palle Christophersen
  • Biphenyl derivatives
    Publication number: 20040048909
    Abstract: Biphenyl derivatives represented by the following formula (1): 1
    Type: Application
    Filed: June 23, 2003
    Publication date: March 11, 2004
    Inventors: Takayuki Namiki, Kenichi Kishii, Masaki Mitani, Masashi Tamai, Naoki Hiyama, Makoto Kimura, Satoshi Ichinomiya
  • 1-phenyl imidazol-2-one biphenylmethyl compounds for treatment of circulatory disorders
    Publication number: 20040048911
    Abstract: A class of 1-phenyl imidazol-2-one biphenylmethyl compounds is described for use in treatment of circulatory disorders.
    Type: Application
    Filed: August 27, 2003
    Publication date: March 11, 2004
    Applicant: G. D. Searle & Co.
    Inventors: David B. Reitz, Robert E. Manning
  • PPAR agonists
    Patent number: 6699904
    Abstract: PPAR alpha activators, pharmaceutical compositions containing such compounds and the use of such compounds to elevate certain plasma lipid levels, including high density lipoprotein-cholesterol and to lower certain other plasma lipid levels, such as LDL-cholesterol and triglycerides and accordingly to treat diseases which are exacerbated by low levels of HDL cholesterol and/or high levels of LDL-cholesterol and triglycerides, such as atherosclerosis and cardiovascular diseases, in mammals, including humans.
    Type: Grant
    Filed: February 14, 2002
    Date of Patent: March 2, 2004
    Assignee: Pfizer Inc.
    Inventors: Cheryl M. Hayward, David A. Perry
  • Ketone compounds and compositions for cholesterol management and related uses
    Patent number: 6699910
    Abstract: The present invention relates to novel ketone compounds, compositions comprising ketone compounds, and methods useful for treating and preventing cardiovascular diseases, dyslipidemias, dysproteinemias, and glucose metabolism disorders comprising administering a composition comprising a ketone compound. The compounds, compositions, and methods of the invention are also useful for treating and preventing Alzheimer's Disease, Syndrome X, peroxisome proliferator activated receptor-related disorders, septicemia, thrombotic disorders, obesity, pancreatitis, hypertension, renal disease, cancer, inflammation, and impotence. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.
    Type: Grant
    Filed: October 11, 2001
    Date of Patent: March 2, 2004
    Assignee: Esperion Therapeutics, Inc.
    Inventors: Jean-Louis Henri Dasseux, Carmen Daniela Oniciu
  • Urea derivative and adhesive-molecule inhibitor containing the same as active ingredient
    Publication number: 20040039040
    Abstract: Disclosed are novel urea derivatives and their medical uses, especially as adhesion molecule inhibitors useful for therapies of inflammatory diseases.
    Type: Application
    Filed: March 14, 2003
    Publication date: February 26, 2004
    Inventors: Toshiya Takahashi, Takeshi Ishigaki, Miyuki Funahashi, Koji Taniguchi, Masayuki Kaneko, Mie Kainoh, Hiroyuki Meguro
  • Substituted phenyl derivatives, their preparation and use
    Patent number: 6696475
    Abstract: The present invention discloses compounds having the formula wherein the substituents are defined in the application. The compounds are useful as chloride channel blockers.
    Type: Grant
    Filed: August 8, 2001
    Date of Patent: February 24, 2004
    Assignee: NeuroSearch A/S
    Inventors: Bjarne H. Dahl, Palle Christophersen
  • Heterocyclic aromatic compounds useful as growth hormone secretagogues
    Publication number: 20040029935
    Abstract: Heterocyclic aromatic compounds are provided which are useful in stimulating endogenous production or release of growth hormone and in treating obesity, osteoporosis (improving bone density) and in improving muscle mass and muscle strength.
    Type: Application
    Filed: October 28, 2002
    Publication date: February 12, 2004
    Inventors: Jeffrey A. Robl, Joseph A. Tino, Andres S. Hernandez, Jun Li
  • Aromatic sulfone hydroxamates and their use as protease inhibitors
    Patent number: 6689794
    Abstract: This invention is directed to aromatic sulfone hydroxamates (also known as “aromatic sulfone hydroxamic acids”) and salts thereof that, inter alia, inhibit matrix metalloproteinase (also known as “matrix metalloprotease” or “MMP”) activity and/or aggrecanase activity. This invention also is directed to a prevention or treatment method that comprises administering such a compound or salt in an MMP-inhibiting and/or aggrecanase-inhibiting effective amount to an animal, particularly a mammal having (or disposed to having) a pathological condition associated with MMP and/or aggrecanase activity.
    Type: Grant
    Filed: May 10, 2002
    Date of Patent: February 10, 2004
    Assignee: Pharmacia Corporation
    Inventors: John N. Freskos, Yvette M. Fobian, Thomas E. Barta, Daniel P. Becker, Louis J. Bedell, Terri L. Boehm, Jeffery N. Carroll, Gary A. DeCrescenzo, Susan L. Hockerman, Darren J. Kassab, Steve A. Kolodziej, Joseph McDonald, Deborah A. Mischke, Monica B. Norton, Joseph G. Rico, John J. Talley, Clara I. Villamil, Lijuan Jane Wang
  • 5-Aryltetrazole Compounds, compositions thereof, and uses therefor
    Publication number: 20040019208
    Abstract: The present invention relates to 5-Aryltetrazole compounds, compositions comprising a 5-Aryltetrazole compound, and methods for treating an inflammation disease, a reperfusion disease, hyperuricemia, gout, or tumor-lysis syndrome in an animal in need thereof comprising administering to the animal an effective amount of a 5-Aryltetrazole compound.
    Type: Application
    Filed: July 18, 2002
    Publication date: January 29, 2004
    Inventors: Alex Nivorozhkin, John Van Duzer, Andrew Salzman, Garry Southan, Siya Ram, Qi Zeng, Csaba Szabo
  • Substituted acid derivatives useful as antidiabetic and antiobesity agents and method
    Patent number: 6673815
    Abstract: Compounds are provided which have the structure wherein Q is C or N, X1 is CH or N and, A, E, M, G, X2, X3, X4, R1, R2, R2a, R2b, R2c, R3, Y, x, m, and n are as defined herein, which compounds are useful as antidiabetic, hypolipidemic, and antiobesity agents.
    Type: Grant
    Filed: November 6, 2002
    Date of Patent: January 6, 2004
    Assignee: Bristol-Myers Squibb Company
    Inventors: Pratik Devasthale, Yoon T. Jeon
  • Novel glucagon antagonists
    Publication number: 20030236292
    Abstract: Novel compounds that act to antagonize the action of the glucagon peptide hormone on the glucagon receptor. More particularly, it relates to glucagon antagonists or inverse agonists.
    Type: Application
    Filed: December 3, 2002
    Publication date: December 25, 2003
    Inventors: Janos Tibor Kodra, Peter Madsen, Jesper Lau, Anker Steen Jorgensen, Inge Thoger Christensen
  • Inhibitors of caspases
    Publication number: 20030232986
    Abstract: The present invention relates to novel classes of compounds which are caspase inhibitors, in particular interleukin-1&bgr; converting enzyme (“ICE”) inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting caspase activity and consequently, may be advantageously used as agents against interleukin-1-(“IL-1”) , apoptosis-, interferon-&ggr; inducing factor-(IGIF), or interferon-&ggr;-(“IFN-&ggr;”) mediated diseases, including inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, and degenerative diseases.
    Type: Application
    Filed: December 6, 2002
    Publication date: December 18, 2003
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: Marion M. Wannamaker, Guy W. Bemis, Paul S. Charifson, David J. Lauffer, Michael D. Mullican, Mark A. Murcko, Keith P. Wilson, James W. Janetka, Robert J. Davies, Anne-Laure Grillot, Zhan Shi, Cornelia J. Forster
  • Compounds and methods for the treatment or prevention of flavivirus infections
    Publication number: 20030229053
    Abstract: the present invention provides novel compounds represented by formula I: 1
    Type: Application
    Filed: June 11, 2002
    Publication date: December 11, 2003
    Applicant: Shire BioChem Inc.
    Inventors: Laval Chan Chun Kong, Jean Bedard, Sanjoy Kumar Das, Nghe Nguyen Ba, Oswy Z. Pereira, Stephen Joseph Shuttleworth, Mohammad Arshad Siddiqui, Wuyi Wang
  • Substituted imidazoles as selective modulators of bradykinin B2 receptors
    Publication number: 20030229076
    Abstract: Disclosed are compounds of the formula: 1
    Type: Application
    Filed: September 16, 2002
    Publication date: December 11, 2003
    Inventors: Stanislaw Rachwal, Alan Hutchison, Kenneth Shaw, George D. Maynard, Xiao-Shu He, Robert DeSimone, Kevin Hodgetts
  • 5-Amide substituted diarylamines as mex inhibitors
    Publication number: 20030225076
    Abstract: 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: Application
    Filed: September 13, 2002
    Publication date: December 4, 2003
    Inventors: Cathlin Biwersi, Haile Tecle, Joseph Scott Warmus
  • 8-Azaprostaglandin analogs as agents for lowering intraocular pressure
    Publication number: 20030220506
    Abstract: The present invention provides a method of treating ocular hypertension or glaucoma which comprises administering to an animal having ocular hypertension or glaucoma therapeutically effective amount of a compound represented by the general formula I; 1
    Type: Application
    Filed: April 9, 2003
    Publication date: November 27, 2003
    Inventors: David W. Old, Danny Thang Dinh, Robert M. Burk
  • 3-(4-amidopyrrol-2-ylmethylidene)-2-indolinone derivatives as protein kinase inhibitors
    Patent number: 6653308
    Abstract: The present invention relates to pyrrole substituted 2-indolinone compounds and their pharmaceutically acceptable salts which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related cellular disorders such as cancer.
    Type: Grant
    Filed: February 15, 2002
    Date of Patent: November 25, 2003
    Assignees: Sugen, Inc., Pharmacia & Upjohn Company
    Inventors: Huiping Guan, Congxin Liang, Li Sun, Peng Cho Tang, Chung Chen Wei, Tomas Vojkovsky, Qingwu Jin, Paul M. Herrinton, Michael A. Mauragis
  • Glucagon antagonists/inverse agonists
    Patent number: 6649641
    Abstract: A novel class of compounds, which act to antagonize the action of the glucagon hormone on the glucagon receptor. Owing to their antagonizing effect of the glucagon receptor the compounds may be suitable for the treatment and/or prevention of any diseases and disorders, wherein a glucagon antagonistic action is beneficial, such as hyperglycemia, Type 1 diabetes, Type 2 diabetes, disorders of the lipid metabolism and obesity.
    Type: Grant
    Filed: November 16, 2001
    Date of Patent: November 18, 2003
    Assignee: Novo Nordisk A/S
    Inventors: Carsten Behrens, Jesper Lau, Peter Madsen
  • Valsartan salts
    Publication number: 20030207930
    Abstract: The invention relates to new salts of valsartan or crystalline, also partly crystalline and amorphous salts of valsartan, the respective production and usage, and pharmaceutical preparations containing such a salt.
    Type: Application
    Filed: February 24, 2003
    Publication date: November 6, 2003
    Inventors: Erwin Marti, Hans Rudolf Oswald, Peter Buhlmayer, Wolfgang Marterer
  • Carbamic acid esters as inhibitors of factor xa
    Publication number: 20030199698
    Abstract: Novel compounds of the formula I 1
    Type: Application
    Filed: May 16, 2003
    Publication date: October 23, 2003
    Inventors: Horst Juraszyk, Dieter Dorsch, Werner Mederski, Christos Tsaklakidis, Christopher Barnes, Johannes Gleitz
  • Colchinol derivatives as angiogenesis inhibitors
    Publication number: 20030195173
    Abstract: The invention related to colchinol derivatives of the formula (I): Wherein: R1, R2 and R3 are each independently hydroxy, phosphoryloxy (—OPO3H2), C1-4alkoxy or an in vivo hydrolysable ester of hydroxy, with the proviso that at least 2 of R1, R2 and R3 are C1-4alkoxy; A is —CO—, —C(O)O—, —CON(R8)— (wherein R8 is hydrogen, C1-4alkyl, C1-3alkoxyC1-3alkyl, aminoC1-3alkyl or hydroxyC1-3alkyl); a is an integer from 1 to 4 inclusive; Ra and Rb are independently selected from hydrogen, hydroxy and amino; B is —O—, —CO—, N(R9)CO—, —CON(R9)—, —N(R9)C(O)O—, —N(R9)CON(R10)—, —N(R9)SO2—, —SO2N(R9)— or a direct single blond (wherein R9 and R10 are independently selected from hydrogen, C1-4alkyl, C1-3alkoxyC1-3alkyl,aminoC1-3alkyl and hydroxyC1-3alkyl); b is O or an integer from 1 to 4 inclusive, (provided that when bis O, B is a single direct bond); D is carboxy, sulpho, tetrazolyl, imidazoly
    Type: Application
    Filed: January 7, 2003
    Publication date: October 16, 2003
    Inventor: Jean Claude Arnould
  • Amide compounds and use thereof
    Publication number: 20030195354
    Abstract: An amide compound given by formula [I]: 1
    Type: Application
    Filed: December 12, 2002
    Publication date: October 16, 2003
    Inventor: Hiroshi Sakaguchi
  • N-substituted arylsulfonylamino hydroxamic acids useful as inhibitors of C-proteinase and for treating or preventing disorders related to unregulated collagen production
    Publication number: 20030191309
    Abstract: The present invention relates to a novel class of organic molecules capable of inhibiting C-proteinase, and to their use to regulate, modulate and/or inhibit abnormal collagen formation as a therapeutic approach towards the treatment of fibrotic disorders.
    Type: Application
    Filed: November 12, 2002
    Publication date: October 9, 2003
    Inventor: Wen-Bin Ho
  • Disubstituted pyrazolines and triazolines as factor Xa inhibitors
    Patent number: 6630468
    Abstract: 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: Grant
    Filed: June 26, 2002
    Date of Patent: October 7, 2003
    Inventor: Donald J. P. Pinto
  • SUBSTITUTED N-BENZOYL-N'(TETRAZOLYLPHENYL)-UREAS AND THEIR USE AS PEST CONTROL AGENTS
    Publication number: 20030187043
    Abstract: The present invention relates to new substituted N-benzoyl-N′-(tetrazolylphenyl)-ureas of the formula (I) 1
    Type: Application
    Filed: November 8, 2002
    Publication date: October 2, 2003
    Inventors: Fritz Maurer, Christoph Erdelen
  • Novel aromatic compounds
    Publication number: 20030186944
    Abstract: Disclosed are compounds of formula I 1
    Type: Application
    Filed: March 21, 2003
    Publication date: October 2, 2003
    Inventors: Marit Kristiansen, Palle Jakobsen, Jane Marie Lundbeck
  • R-isomers of nonnucleoside inhibitors
    Publication number: 20030181717
    Abstract: Novel chiral derivitaves of non-nucleoside inhibitors (NNI), particularly R-isomers of halopyridyl and thiazoyl thiourea compounds are provided as potent inhibitors of reverse transcriptase (RT), and particularly of retroviral RT, most particularly HIV RT. The stereospecific compounds and compositions of the invention inhibit replication of retrovirus, particularly human immunodeficiency virus-1 (HIV-1) and drug resistant strains.
    Type: Application
    Filed: January 21, 2003
    Publication date: September 25, 2003
    Applicant: Parker Hughes Institute located at Roseville, Minnesota
    Inventors: Fatih M. Uckun, Taracad K. Venkatachalam
  • Benzoic acid derivatives and related compounds as antiarrhythmic agents
    Patent number: 6624309
    Abstract: Benzoic acid derivatives of the formula where X is oxygen, sulfur, —NH, —NR1, —N—CN, —N—OR1 or —N—NO2; Y is a single bond, —C═C—, or —NH; R1 is alkyl, alkenyl, alkynyl, aryl, cycloalkyl, heterocyclo, or (heterocyclo)alkyl; and R2 is aryl or heterocyclo. The compounds of formula I are useful in the treatment of arrhythmia.
    Type: Grant
    Filed: September 25, 2002
    Date of Patent: September 23, 2003
    Assignee: Bristol-Myers Squibb Company
    Inventors: John Lloyd, George C. Rovnyak, Philip D. Stein, Saleem Ahmad, Karnail S. Atwal, Thomas J. Caulfield, Michael A. Poss
  • New salt hydrates
    Publication number: 20030171414
    Abstract: The invention relates to new forms of salts of valsartan or crystalline, also partly crystalline and amorphous salts of valsartan, the respective production and usage, and pharmaceutical preparations containing such a salt.
    Type: Application
    Filed: January 29, 2003
    Publication date: September 11, 2003
    Inventor: Erwin Ernst Marti
  • Urethane derivatives
    Publication number: 20030171579
    Abstract: The invention relates to novel compounds of formula (I), wherein R, R1 and R2 have the meaning as cited claim 1. According to the invention, the compounds are inhibitors of the coagulation factors Xa and VIIa and can be used for treating thrombosis, myocardial infarct, arteriosclerosis, inflammation, apoplexy, angina pectoris, restenosis post-angioplasty, intermittent claudication, tumours, tumour related illnesses and/or tumour metastases.
    Type: Application
    Filed: January 27, 2003
    Publication date: September 11, 2003
    Inventors: Werner Mederski, Horst Juraszyk, Dieter Dorsch, Christos Tsaklakidis, Johannes Gleitz, Christopher Barnes
  • Glycinamides
    Publication number: 20030166694
    Abstract: Novel compounds of the formula I 1
    Type: Application
    Filed: November 27, 2002
    Publication date: September 4, 2003
    Inventors: Dieter Dorsch, Werner Mederski, Christos Tsaklakidis, Johannes Gleitz, Christopher Barnes
  • Bicyclic metabotropic glutamate receptor ligands
    Patent number: 6610743
    Abstract: The present invention provides bicyclic metabotropic glutamate receptor ligands, as well as compositions comprising such ligands, and and methods for their use.
    Type: Grant
    Filed: March 6, 2002
    Date of Patent: August 26, 2003
    Assignee: Georgetown University
    Inventors: Alan P. Kozikowski, Darryl Hugh Steensma, Werner Tueckmantel, Gian Luca Araldi
  • Fatty acid synthase inhibitors
    Patent number: 6608059
    Abstract: This invention relates to the use of compounds as inhibitors of the fatty acid synthase FabH.
    Type: Grant
    Filed: December 13, 2002
    Date of Patent: August 19, 2003
    Assignee: SmithKline Beecham Corporation
    Inventors: Robert A. Daines, Israil Pendrak
  • EP4 receptor selective agonists in the treatment of osteoporosis
    Publication number: 20030149086
    Abstract: This invention is directed to EP4 receptor selective prostaglandin agonists of the Formula I, 1
    Type: Application
    Filed: December 20, 2002
    Publication date: August 7, 2003
    Inventors: Kimberly O. Cameron, Bruce A. Lefker
  • Inhibitors of factor Xa with a neutral P1 specificity group
    Patent number: 6602895
    Abstract: The present application describes inhibitors of factor Xa with a neutral P1 specificity group of formula I: or pharmaceutically acceptable salt forms thereof, wherein R and E may be groups such as methoxy and halo.
    Type: Grant
    Filed: May 16, 2002
    Date of Patent: August 5, 2003
    Assignee: Bristol-Myers Squibb Company
    Inventors: Robert A. Galemmo, Jr., Celia Dominguez, John M. Fevig, Qi Han, Patrick Y. Lam, Donald J. P. Pinto, James R. Pruitt, Mimi L. Quan
  • 5-aralkysufonyl-3-(pyrrol-2-ylmethylidene)-2-indolinone derivatives as kinase inhibitors
    Patent number: 6599902
    Abstract: The present invention relates to certain 5-aralkylsulfonyl-3-(pyrrol-2-yl-methylidene)-2-indolinone derivatives that inhibit kinases, in particular met kinase. Pharmaceutical compositions comprising these compounds, methods of treating diseases mediated by kinases utilizing pharmaceutical compositions comprising these compounds, and methods of preparing them are also disclosed.
    Type: Grant
    Filed: May 30, 2002
    Date of Patent: July 29, 2003
    Assignee: Sugen, Inc.
    Inventors: Jingrong Cui, John Ramphal, Congxin Liang, Connie Li Sun, Chung Chen Wei, Peng Cho Tang