Nitrogen In Q Patents (Class 514/603)
  • Acylsulfonamide derivatives
    Patent number: 6812252
    Abstract: The present invention provides new acylsulfonamide derivatives such as 4-(3-trifluoromethyl)phenylethynyl-N-(2-(5-ketohexanoylamino)sulfonylphenyl)benzamide, 4-(3-trifluoromethyl)phenylethynyl-N-(2-(2-propyloxyacetylamino)sulfonylphenyl)benzamide or analogues thereof. These acylsulfonamide derivatives have a hypoglycemic effect equal to or superior to the effects of the conventional hypoglycemic agents and they are free from the side effects unlike the glitazone compounds.
    Type: Grant
    Filed: January 3, 2003
    Date of Patent: November 2, 2004
    Assignee: Ajinomoto Co., Inc.
    Inventors: Hiroshi Ikawa, Masato Nishimura, Keiji Okada, Takashi Nakamura, Kazuhiro Kojima, Hideki Kosono
  • Branched chain amino acid-dependent aminotransferase inhibitors and their use in the treatment of neurodegenerative diseases
    Patent number: 6809119
    Abstract: The invention relates to BCAT inhibitors and the use thereof for treating or preventing neuronal loss associated with stroke, ischemia, CNS trauma, hypoglycemia and surgery, as well as treating neurodegenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease and Down's syndrome, treating or preventing the adverse consequences of the overstimulation of the excitatory amino acids, treating anxiety, psychosis, convulsions, aminoglycoside antibiotics-induced hearing loss, migraine headache, chronic pain, neuropathic pain, Parkinson's disease, diabetic retinopathy, glaucoma, CMV retinitis, urinary incontinence, opioid tolerance or withdrawal, and inducing anesthesia, as well as for enhancing cognition.
    Type: Grant
    Filed: November 26, 2002
    Date of Patent: October 26, 2004
    Assignee: Warner-Lambert Company LLC
    Inventors: Lain-Yen Hu, Suzanne Ross Kesten, Huangshu Lei, Todd Robert Ryder, David Juergen Wustrow
  • Compositions and method for treating microbial and parasitic infections in cattle and other animals
    Publication number: 20040198704
    Abstract: Novel formulations combining an antiparasitic compounds, such as an avermectin, with a fluorinated chloramphenicol or thiamphenicol derivative antibiotic such as Florfenicol are disclosed. Methods for using such formulations in the treatment and prevention of infectious diseases of bovines and swine, including bovine respiratory disease and parasitic infections are also disclosed.
    Type: Application
    Filed: April 2, 2004
    Publication date: October 7, 2004
    Applicant: Schering Corporation
    Inventors: Dale E. Shuster, David G. Sawutz, Kanwal J. Varma
  • Pharmaceutical combination for treating benign prostatic hyperplasia or for treating abacterial prostatitis
    Publication number: 20040198826
    Abstract: The present invention relates to a new pharmaceutical combination for treating benign prostatic hyperplasia (BPH) or for treating abacterial prostatitis.
    Type: Application
    Filed: April 1, 2004
    Publication date: October 7, 2004
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Wolfgang Baiker, Ludwig Mehlburger
  • Method and compositions for treating diseases mediated by transglutaminase activity
    Patent number: 6794414
    Abstract: Diseases Mediated by transglutaminase, such as Huntington's Disease, spinobulbar atrophy, spinocerebellar ataxia, and dentatorubralpallidoluysian atrophy, as well as inflammatory diseases of the central nervous system, including mautiple sclerosis, rheumatoid arthritis, and insulin dependent diabetes mellitus, can be treated by administering a transglutaminase inhibitor such as monadansyl cadaverine, monoamines and diamines such as cystamine, putrescine, GABA. (gamma-amino benzoic acid), N-benzyloxy carbonyl, 5-deazp-4-oxonorvaline p-nitrophenylester, glycine methyl ester, CuSO4, and the oral anti-hyperglycemic agent tolbutamide.
    Type: Grant
    Filed: September 6, 2001
    Date of Patent: September 21, 2004
    Assignee: Yeda Research and Development Co. Ltd.
    Inventor: Lawrence Steinman
  • Phenethanolamine derivatives for treatment of respiratory diseases
    Publication number: 20040180876
    Abstract: The present invention relates to novel compounds of Formula (I), to a process for their manufacture, to pharmaceutical compositions containing them, and to their use in therapy, in particular their use in the prophylaxis and treatment of respiratory diseases.
    Type: Application
    Filed: February 9, 2004
    Publication date: September 16, 2004
    Inventors: Keith Biggadike, Diane Mary Coe, Dean David Edney, Stephen Barry Guntrip, Abigail Halton, Brian Edgar Looker, Michael John Monteith, Rajnikant Patel, Panayiotis Alexandrou Procopiou
  • Compositions and method for treating infection in cattle and swine
    Patent number: 6790867
    Abstract: Novel formulations combining a non-steroidal anti-inflammatory drug (NSAID) such as flunixin, with a fluorinated chloramphenicol or thiamphenicol derivative antibiotic such as florfenicol are disclosed. Methods for using such formulations in the treatment and prevention of infectious diseases of bovines and swine, including bovine respiratory disease and swine respiratory disease, are also disclosed.
    Type: Grant
    Filed: January 24, 2003
    Date of Patent: September 14, 2004
    Assignee: Schering-Plough Animal Health Corporation
    Inventors: Raul E. Kohan, Kanwal J. Varma, Robert D. Simmons, Abu Huq, Keith A. Freehauf
  • NPY Y5 antagonist
    Publication number: 20040176462
    Abstract: The present invention provides a pharmaceutical composition for use as an NPY Y5 receptor antagonist comprising a compound of the formula (I): 1
    Type: Application
    Filed: December 30, 2003
    Publication date: September 9, 2004
    Applicant: Shionogi & Co., Ltd.
    Inventors: Yasuyuki Kawanishi, Hideyuki Takenaka, Kohji Hanasaki, Tetsuo Okada
  • Aspartyl protease inhibitors
    Publication number: 20040132782
    Abstract: The present invention provides compounds having formula (I): 1
    Type: Application
    Filed: June 16, 2003
    Publication date: July 8, 2004
    Inventors: Wenjin Yang, Douglas R. Cary, Jeffrey W. Jacobs, Wanli Lu, Yafan Lu, Jian Sun, Min Zhong
  • Benzenesulfonamide derivatives and their use as MEK inhibitors
    Patent number: 6750217
    Abstract: Benzenesulfonamides of formula (I), in which W is OR1, NR2OR1, NRARB, NR2NRARB, or NR2(CH2)2-4NRARB and the other variables as defined in the claims, are inhibitors of MEK and are effective in the treatment of proliferative diseases, cancer, stroke, heart failure, xenograft rejection, arthritis, cystic fibrosis, hepatomegaly, cardiomegaly, Alzheimer's disease, complications of diabetes, septic shock, and viral infection.
    Type: Grant
    Filed: July 18, 2002
    Date of Patent: June 15, 2004
    Assignee: Warner-Lambert Company
    Inventors: Stephen Douglas Barrett, Haile Tecle, Richard John Booth
  • Aryl and heteroaryl compounds and methods to modulate coagulation
    Publication number: 20040110832
    Abstract: This invention provides certain compounds, methods of their preparation, pharmaceutical compositions comprising the compounds, and their use in treating human or animal disorders. The compounds of the invention are useful as antagonists, or more preferably, partial antagonist of factor IX and thus, may be used to inhibit the intrinsic pathway of blood coagulation. The compounds are useful in a variety of applications including the management, treatment and/or control of diseases caused in part by the intrinsic clotting pathway utilizing factor IX. Such diseases or disease states include stroke, myocardial infarction, aneurysm surgery, and deep vein thrombosis associated with surgical procedures, long periods of confinement, and acquired or inherited pro-coagulant states.
    Type: Application
    Filed: August 8, 2003
    Publication date: June 10, 2004
    Inventors: Adnan M.M. Mjalli, Robert C. Andrews, Xiao-Chuan Guo, Daniel Peter Christen, Devi Reddy Gohimmukkula, Guoxiang Huang, Robert Rothlein, Sameer Tyagi, Tripura Yaramasu, Christopher Behme
  • Thiol sulfonamide metalloprotease inhibitors
    Patent number: 6747027
    Abstract: This invention is directed to proteinase (protease) inhibitors, and more particularly to thiol sulfonamide inhibitors for matrix metalloproteinase 13(MMP-13), compositions of proteinase inhibitors, intermediates for the syntheses of proteinase inhibitors, processes for the preparation of proteinase inhibitors and processes for treating pathological conditions associated with pathological matrix metalloproteinase activity related to MMP-13.
    Type: Grant
    Filed: July 22, 1997
    Date of Patent: June 8, 2004
    Assignee: Pharmacia Corporation
    Inventors: Gary DeCrescenzo, Zaheer S. Abbas, John N. Freskos, Daniel P. Getman, Robert M. Heintz, Brent V. Mischke, Joseph J. McDonald
  • 2'-Substituted 1,1'-biphenyl-2-carboxamides, processes for their preparation, their use as medicaments, and pharmaceutical preparations comprising them
    Publication number: 20040102513
    Abstract: Compounds of the formula I, 1
    Type: Application
    Filed: October 24, 2003
    Publication date: May 27, 2004
    Applicant: Aventis Pharma Deutschland GmbH
    Inventors: Joachim Brendel, Wolfgang Schmidt, Peter Below
  • Aryl sulfonamides and sulfamide derivatives and uses thereof
    Patent number: 6734182
    Abstract: This invention is directed to novel aryl sulfonamide and sulfamide compounds which bind selectively to and inhibit the activity of the human Y5 receptor. This invention is also related to uses of these compounds for the treatment of feeding disorders such as obesity, anorexia nervosa, bulimia nervosa, and abnormal conditions such as sexual/reproductive disorders, depression, epileptic seizure, hypertension, cerebral hemorrhage, congestive heart failure or sleep disturbances and for the treatment of any disease in which antagonism of a Y5 receptor may be useful.
    Type: Grant
    Filed: April 2, 2002
    Date of Patent: May 11, 2004
    Assignee: Synaptic Pharmaceutical Corporation
    Inventors: Imadul Islam, Daljit S. Dhanoa, John M. Finn, Ping Du, Charles Gluchowski, Yoon T. Jeon
  • Methods for the identification of inhibitors of 3-isopropylmalate dehydratase as antibiotics
    Patent number: 6733963
    Abstract: The present inventors have discovered that 3-Isopropylmalate dehydratase is essential for fungal pathogenicity. Specifically, the inhibition of 3-Isopropylmalate dehydratase gene expression in fungi results in no signs of successful infection or lesions. Thus, 3-Isopropylmalate dehydratase can be used as a target for the identification of antibiotics, preferably antifungals. Accordingly, the present invention provides methods for the identification of compounds that inhibit 3-Isopropylmalate dehydratase expression or activity. The methods of the invention are useful for the identification of antibiotics, preferably antifungals.
    Type: Grant
    Filed: December 6, 2001
    Date of Patent: May 11, 2004
    Assignee: Paradigm Genetics, Inc.
    Inventors: Lisbeth Hamer, Kiichi Adachi, Todd DeZwaan, Sze-Chung Lo, Maria Victoria Montenegro-Chamorro, Sheryl Frank, Blaise Darveaux, Sanjoy Mahanty, Ryan Heiniger, Amy Skalchunes, Huaqin Pan, Rex Tarpey, Jeffrey Shuster, Matthew M. Tanzer
  • Treating muscle wasting with selective androgen receptor modulators
    Publication number: 20040087557
    Abstract: This invention provides: 1) a method of treating a subject suffering from a muscle wasting disorder; 2) a method of preventing a muscle wasting disorder in a subject; 3) a method of treating, preventing, suppressing, inhibiting or reducing muscle loss in a subject suffering from a muscle wasting disorder; 4) a method of treating, preventing, inhibiting, reducing or suppressing muscle wasting in a subject suffering from a muscle wasting disorder; and/or 5) a method of treating, preventing, inhibiting, reducing or suppressing muscle protein catabolism in a subject suffering from a muscle wasting disorder, by administering to the subject a selective androgen receptor modulator (SARM) and/or its analog, derivative, isomer, metabolite, pharmaceutically acceptable salt, pharmaceutical product, hydrate, N-oxide or any combination thereof, as described herein.
    Type: Application
    Filed: December 5, 2002
    Publication date: May 6, 2004
    Inventors: Mitchell S. Steiner, Karen A. Veverka, James T. Dalton, Duane D. Miller
  • 3,4,5,-trisubstituted aryl nitrone compounds and pharmaceutical compositions containing the same
    Patent number: 6730700
    Abstract: Disclosed are 3,4,5-trisubstituted aryl nitrone compounds and pharmaceutical compositions containing such compounds. The 3,4,5-trisubstituted aryl nitrone compounds have formula (I); where R1-R4 are as defined in the specification. The disclosed compositions are useful as therapeutics for inflammation-related conditions in mammals, such as arthritis, and as analytical reagents for detecting free radicals.
    Type: Grant
    Filed: July 15, 2002
    Date of Patent: May 4, 2004
    Assignee: Renovis, Inc.
    Inventors: L. David Waterbury, Allan L. Wilcox, John M. Carney, Farah Mavandadi, Albert Danielzadeh
  • Fatty acid synthase inhibitors
    Patent number: 6723749
    Abstract: This invention relates to the use of compounds as inhibitors of the fatty acid synthase FabH.
    Type: Grant
    Filed: January 31, 2003
    Date of Patent: April 20, 2004
    Assignee: SmithKline Beecham Corporation
    Inventors: Siegfried B. Christensen, Daniel J. Mercer, Jia-Ning Xiang
  • Quaternary amines and related inhibitors of factor xa
    Publication number: 20040067938
    Abstract: Novel quaternary amine containing compounds including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compounds and compositions are useful in vitro or in vivo for preventing or treating conditions in mammals characterized by undesired thrombosis.
    Type: Application
    Filed: November 3, 2003
    Publication date: April 8, 2004
    Inventors: Penglie Zhang, Robert M. Scarborough, Bing-Yan Zhu
  • Methods for anti-tumor therapy
    Patent number: 6716879
    Abstract: Disclosed and claimed is a method for treating tumors using sulfonylamino-substituted N-aryl- or heteroarylcarboxamide derivatives.
    Type: Grant
    Filed: August 29, 2001
    Date of Patent: April 6, 2004
    Assignee: Compass Pharmaceuticals, LLC
    Inventor: Irwin Braude
  • Compounds for the treatment of estrogen-dependent illnesses and methods for making and using the same
    Patent number: 6716880
    Abstract: Novel sulfatase inhibitor/estrogen receptor blocker compounds useful in the treatment of estrogen dependent illnesses are disclosed. The compounds generally comprise a sulfamate moiety and an aromatic, estrogen receptor blocker moiety. Methods for synthesizing these compounds and using them in the therapeutic and/or prophylactic treatment of an estrogen-dependent disease are also disclosed.
    Type: Grant
    Filed: June 18, 2002
    Date of Patent: April 6, 2004
    Assignee: Duquesne University of the Holy Ghost
    Inventors: Pui-Kai Li, Kyle W. Selcer
  • Cyclohexyl(alkyl)-propanolamines, preparation method and pharmaceutical compositions containing same
    Publication number: 20040053916
    Abstract: The present invention relates to the compounds of formula (I): 1
    Type: Application
    Filed: May 21, 2003
    Publication date: March 18, 2004
    Inventors: Philippe R. Bovy, Roberto Cecchi, Gilles Courtemanche, Tiziano Croci, Ambrogio Oliva, Nunzia Viviani
  • 1, 2, 4-tribsubstituted benzenes as inhibitors of 15-lipoxygenase
    Publication number: 20040053983
    Abstract: The present invention provides compounds of formula (I) wherein R, Z, Y, W, R5, V, and X are as defined in the description, and pharmaceutically acceptable salts thereof, which are useful for the treatment of diseases responsive to the inhibition of the enzyme 15-lipoxygenase. Thus, the compounds of formula (I) and their pharmaceutically acceptable salts are useful for treating diseases with an inflammatory component, including atherosclerosis, diseases involving chemotaxis of monocytes, inflammation, stroke, coronary artery disease, asthma, arthritis, colorectal cancer, and psoriasis.
    Type: Application
    Filed: February 21, 2003
    Publication date: March 18, 2004
    Inventors: Nicole Chantel Barvian, Patrick Michael O.Brien, William Chester Patt, Joseph Armand Picard, Drago Robert Sliskovic
  • Use of IL-12 antagonists in the treatment of conditions promoted by an increase in levels of IFN-y
    Patent number: 6706264
    Abstract: Method of treating autoimmune conditions are disclosed comprising administering to a mammalian subject IL-12 or an IL-12 antagonist. In certain preferred embodiments the autoimmune condition is one which is promoted by an increase in levels of IFN-&ggr; or TNF-&agr;. Suitable conditions for treatment include multiple sclerosis, systemic lupus erythematosus, rheumatoid arthritis, autoimmune pulmonary inflammation, Guillain-Barre syndrome, autoimmune thyroiditis, insulin dependent diabetes melitis and autoimmune inflammatory eye disease.
    Type: Grant
    Filed: February 25, 2000
    Date of Patent: March 16, 2004
    Assignee: Genetics Institute, LLC
    Inventors: John Leonard, Samuel Goldman, Richard O'Hara, Jr.
  • &bgr;3 adrenergic receptor agonists and uses thereof
    Patent number: 6706743
    Abstract: The instant invention provides &bgr;3 adrenergic receptor agonists of structural Formula (I), the stereoisomers and prodrugs thereof, and the pharmaceutically acceptable salts of the compounds, stereoisomers and prodrugs, wherein Ar, R, R1, R2, R3, R4, R5, R6, R7, R8, X, and Y, are as defined herein.
    Type: Grant
    Filed: March 5, 2003
    Date of Patent: March 16, 2004
    Assignee: Pfizer Inc
    Inventors: Robert F. Day, Jennifer A. Lafontaine
  • Bis-aromatic alkanols
    Publication number: 20040048857
    Abstract: The present invention relates to biphenylyl derivatives, processes for their production, their uses and pharmaceutical compositions containing them.
    Type: Application
    Filed: May 27, 2003
    Publication date: March 11, 2004
    Applicants: IRM LLC, Novartis AG
    Inventors: Shifeng Pan, Nathanael S. Gray, Wenqi Gao, Klaus Hinterding, Sophie Lefebvre, Yuan Mi, Peter Nussbaumer, Wei Wang, Federic Zecri, Fan Yi, Lawrence Blas Perez, Kenneth Richard la Montagne, Peter Ettmayer
  • Il-8 receptor antagonists
    Publication number: 20040048897
    Abstract: This invention relates to the novel use of sulfonamide squaramides in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).
    Type: Application
    Filed: July 16, 2003
    Publication date: March 11, 2004
    Inventors: Brent McCleland, Michael R. Palovich, Katherine L. Widdowson
  • Benzene derivatives and pharmaceutical use thereof
    Patent number: 6703379
    Abstract: The present invention provides an AP-1 activation inhibitor, NF-kappa B activation inhibitor, inflammatory cytokine production inhibitor, matrix metalloprotease production inhibitor, inflammatory cell adhesion molecule expression inhibitor, anti-inflammatory agent, antirheumatic agent, immunosuppressant, cancer metastasis inhibitor, remedy for arteriosclerosis and antiviral agent which contain the benzene derivative of the following general formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient.
    Type: Grant
    Filed: March 12, 2001
    Date of Patent: March 9, 2004
    Assignee: Ajinomoto Co., Inc.
    Inventors: Yukio Iino, Kohichi Fujita, Takashi Tsuji, Ariko Kodaira, Kenji Takehana, Tsuyoshi Kobayashi, Takashi Yamamoto
  • Antipsychotic sulfonamide-heterocycles, and methods of use thereof
    Patent number: 6703383
    Abstract: One aspect of the present invention relates to heterocyclic compounds comprising a sulfonamide moiety. A second aspect of the present invention relates to the use of the heterocyclic compounds comprising a sulfonamide moiety to treat diseases, afflictions or maladies caused at least in part by abnormal activity of one or more GPCRs or ligand-gated ion channels. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the heterocyclic compounds comprising a sulfonamide moiety, and the screening of those libraries for biological activity, e.g., in animal models of psychosis.
    Type: Grant
    Filed: September 12, 2001
    Date of Patent: March 9, 2004
    Assignee: Sepracor, Inc.
    Inventors: Xinhe Wu, Brian M. Aquila, Liming Shao, Heike Radeke, Gregory D. Cuny, James R. Hauske, Roger L. Xie
  • Substituted 1 and 2 naphthol mannich bases
    Publication number: 20040044061
    Abstract: The invention relates to substituted 1 and 2 naphthol Mannich bases, a method for the production thereof, medicaments containing said compounds and the use of said compounds in the production of medicaments.
    Type: Application
    Filed: June 27, 2002
    Publication date: March 4, 2004
    Inventors: Matthias Gerlach, Corina Maul
  • Upregulation of type III endothelial cell nitric oxide synthase by agents that disrupt actin cytoskeletal organization
    Patent number: 6696480
    Abstract: A use for agents that disrupt actin cytoskeletal organization is provided. In the instant invention, agents that disrupt actin cytoskeletal organization are found to upregulate endothelial cell Nitric Oxide Synthase activity. As a result, agents that disrupt actin cytoskeletal organization are useful in treating or preventing conditions that result from the abnormally low expression and/or activity of endothelial cell Nitric Oxide Synthase. Such conditions include hypoxia-induced conditions. Subjects thought to benefit mostly from such treatments include nonhyperlipidemics and nonhypercholesterolemics, but not necessarily exclude hyperlipidemics and hypercholesterolemics.
    Type: Grant
    Filed: May 13, 2002
    Date of Patent: February 24, 2004
    Assignee: Brigham and Women's Hospital, Inc.
    Inventor: James K. Liao
  • Fluorenes and anthracenes that inhibit P2X3 and P2X2/3 containing receptors
    Patent number: 6693136
    Abstract: Compounds of formula (I) are novel P2X3 and P2X2/P2X3 containing receptor antagonists and are useful in treating pain, urinary incontinence, and bladder overactivity.
    Type: Grant
    Filed: July 26, 2002
    Date of Patent: February 17, 2004
    Assignee: Abbott Laboratories
    Inventors: Chih-Hung Lee, Meiqun Jiang, Richard A. Perner, Arthur Gomtsyan, Erol K. Bayburt, Guo Zhu Zheng
  • Halogenated selective androgen receptor modulators and methods of use thereof
    Publication number: 20040029913
    Abstract: This invention provides a class of androgen receptor targeting agents (ARTA). The agents define a new subclass of compounds, which are selective androgen receptor modulators (SARM). Several of the SARM compounds have been found to have an unexpected androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. Other SARM compounds have been found to have an unexpected antiandrogenic activity of a nonsteroidal ligand for the androgen receptor.
    Type: Application
    Filed: February 24, 2003
    Publication date: February 12, 2004
    Inventors: James T. Dalton, Duane D. Miller, Mitchell S. Steiner, Karen A. Veverka
  • Substituted N-phenyl 2-hydroxy-2-methyl-3,3,3-trifluoropropanamide derivatives which elevate pyruvate dehydrogenase activity
    Patent number: 6689909
    Abstract: A compound of formula (I) wherein: n is 1 or 2; R1 is chloro, fluoro, bromo, methyl or methoxy; R2 is as defined within; R3 is as defined within; and R4 is hydrogen or fluoro; or a pharmaceutically acceptable salt or an in vivo hydrolysable ester thereof is described. The use of compounds of formula (I) in the production of an elevation of PDH activity in a warm-blooded animal such as a human being are also described. Pharmaceutical compositions, methods and processes for preparation of compounds of formula (I) are detailed.
    Type: Grant
    Filed: June 17, 2002
    Date of Patent: February 10, 2004
    Assignee: AstraZeneca AB
    Inventors: Roger John Butlin, Janet Elizabeth Pease, Michael Howard Block, Thorsten Nowak, Jeremy Nicholas Burrows
  • IL-8 receptor antagonists
    Patent number: 6680317
    Abstract: This invention relates to novel compounds of Formula (I), and compositions thereof, useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).
    Type: Grant
    Filed: September 17, 2002
    Date of Patent: January 20, 2004
    Assignee: SmithKline Beecham Corporation
    Inventors: Michael R. Palovich, Katherine L. Widdowson, Hong Nie
  • Novel potassium channels modulators
    Publication number: 20040009973
    Abstract: The invention relates to compounds having the Formula (I) 1
    Type: Application
    Filed: March 11, 2003
    Publication date: January 15, 2004
    Applicant: 4SC AG
    Inventors: Heiko Rauer, Gabriel Garcia, Bernd Kramer, Juergen Kraus, Claudia Klemenz, Wael Saeb
  • Non-peptidic cyclophilin binding compounds and their use
    Patent number: 6677376
    Abstract: The invention relates to non-peptidic compounds that possess bioactive properties, such as the ability to protect neuronal cells from otherwise lethal treatments or the ability to promote the growth or regeneration of neuronal cells. In part, the invention provides compounds that interact with or bind to a cyclophilin and compounds that have activity towards neuronal cells. Methods for using the compounds, such as administering them to cells or animals or using them to treat neurodegenerative conditions, are specifically included.
    Type: Grant
    Filed: September 7, 2000
    Date of Patent: January 13, 2004
    Assignee: Guilford Pharmaceuticals, Inc.
    Inventors: Gregory S. Hamilton, Joseph P. Steiner, Mark J. Vaal, Chi Choi, Ling Wei
  • Substituted phenylsulfonamide inhibitors of beta amyloid production
    Publication number: 20040006050
    Abstract: Compounds of Formula I, 1
    Type: Application
    Filed: June 9, 2003
    Publication date: January 8, 2004
    Applicants: Wyeth, ArQule Inc.
    Inventors: Anthony Frank Kreft, Derek Cecil Cole, Kevin Roger Woller, Joseph Raymond Stock, Kristina Martha Kutterer, Dennis Martin Kubrak, Charles William Mann, William Jay Moore, David Scott Casebier
  • Benzenesulfonamide-derivatives and their use as medicaments
    Patent number: 6667342
    Abstract: Compounds of formula (I), pharmaceutically acceptable salts or in vivo hydrolysable esters thereof, wherein: Ring X is phenyl or a six membered heteroaryl ring containing one or two ring nitrogens where said nitrogens are optionally oxidised to form the N-oxide; R1 and R2 are substituents as defined within; R3 and R4 are defined within and are alkyl or halo alkyl or together form a halocycloalkyl ring; R5 is a substituent as defined within; Y—Z is a linking group as defined within; are useful in the production of a elevation of PDH activity in a warm-blooded animal such as a human being. Pharmaceutical compositions, methods and processes for preparation of compounds of formula (I) are described.
    Type: Grant
    Filed: August 22, 2000
    Date of Patent: December 23, 2003
    Assignee: Astrazeneca AB
    Inventors: David S Clarke, Jeremy N Burrows, Paul Ro Whittamore, Roger J Butlin, Thorsten Nowak
  • Selective androgen receptor modulators and methods of use thereof
    Publication number: 20030232792
    Abstract: This invention provides a class of androgen receptor targeting agents (ARTA). The agents define a new subclass of compounds, which are selective androgen receptor modulators (SARM). Several of the SARM compounds have been found to have an unexpected androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. Other SARM compounds have been found to have an unexpected antiandrogenic activity of a nonsteroidal ligand for the androgen receptor.
    Type: Application
    Filed: October 15, 2002
    Publication date: December 18, 2003
    Inventors: James T. Dalton, Duane D. Miller, Donghua Yin, Yali He
  • Pharmaceutical combination for the treatment of benign prostatic hyperplasia or for the long-term prevention of acute urinary retention
    Publication number: 20030225118
    Abstract: The present invention relates to a new pharmaceutical combination for treating benign prostatic hyperplasia (BPH) or for the long-term prevention of acute urinary retention (AUR).
    Type: Application
    Filed: April 24, 2003
    Publication date: December 4, 2003
    Applicant: Boehringer Ingelheim Pharma GmbH & Co. KG
    Inventors: Wolfgang Baiker, Ludwig Mehlburger
  • Compositions and method for treating infection in cattle and swine
    Publication number: 20030220302
    Abstract: Novel formulations combining a non-steroidal anti-inflammatory drug (NSAID) such as flunixin, with a fluorinated chloramphenicol or thiamphenicol derivative antibiotic such as florfenicol are disclosed. Methods for using such formulations in the treatment and prevention of infectious diseases of bovines and swine, including bovine respiratory disease and swine respiratory disease, are also disclosed.
    Type: Application
    Filed: January 24, 2003
    Publication date: November 27, 2003
    Applicant: Schering-Plough Animal Health Corporation
    Inventors: Raul E. Kohan, Kanwal J. Varma, Robert D. Simmons, Abu Huq, Keith A. Freehauf
  • Use of inhibitors of the sodium-dependent chloride/bicarbonate exchanger for the treatment of thrombotic and inflammatory disorders
    Publication number: 20030220383
    Abstract: Inhibitors of the cellular sodium-dependent chloride/bicarbonate exchangers show an inhibiting effect on the secretion of von-Willebrand factor. These inhibitors can therefore be employed for the treatment of thrombotic and inflammatory disorders.
    Type: Application
    Filed: February 14, 2003
    Publication date: November 27, 2003
    Applicant: AVENTIS PHARMA DEUTSCHLAND GMBH
    Inventors: Hans-Jochen Lang, Heinz-Werner Kleemann, Stefan Werner Schneider, Hans Oberleithner, Andre Niemeyer
  • Targeted drug delivery using sulfonamide derivatives
    Patent number: 6653331
    Abstract: The present invention relates to Glutathione S-transferase (GST)/Reduced Glutathione (GSH) as a means for the in-vivo release of a drug that has been conjugated to specific electrophilic moieties via a sulfonamide bond. The drug may be an anticancer agent (or one with other therapeutic properties) carrying a free —NH— which has been derivatized by the attachment of an electrophile containing a moiety, such as p-CN— or p-NO2-pyridinylsulfonyl groups, or p-NO2- or 2,4 dinitrophenylsulfonyl groups, or suitable derivatives thereof, to make a prodrug. Optionally, the sulfonamide moiety may have attached to it a targeting molecule. The present invention also provides Glutathione S-transferase (GST)/Reduced Glutathione (GSH) as a means for the release of a protected amino derivative that has been conjugated to specific electrophilic moieties via a sulfonamide bond.
    Type: Grant
    Filed: March 17, 1999
    Date of Patent: November 25, 2003
    Assignee: Pharmacia & Upjohn Company
    Inventors: Zhiyang Zhao, Alfredo G. Tomasselli, Kenneth A. Koeplinger, Tillie Peterson
  • Labelled factor XIIIa substrates
    Patent number: 6653299
    Abstract: A complex of a radiometal or paramagnetic metal ion with a metal chelating agent such as a diaminedioxime has attached thereto a substituent of formula —(Y)m—A—NHR, can function as a substrate for the fibrin-stabilizing Factor XIIIa. The complex is useful for the diagnosis or therapy of thrombosis, embolism, atherosclerosis, inflammation or cancer.
    Type: Grant
    Filed: October 4, 1999
    Date of Patent: November 25, 2003
    Assignee: Nycomed Amersham PLC
    Inventors: Alan Michael Forster, Peter Knox, Marivi Mendizabal, Timothy Charles Richardson, Anthony Eamon Storey, Ian Andrew Wilson, Susan Champion, Alex Gibson, Benedicte Guilbert
  • Il-8 receptor anatagonists
    Publication number: 20030216375
    Abstract: This invention relates to novel compounds of Formula (I), and compositions thereof, useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).
    Type: Application
    Filed: September 17, 2002
    Publication date: November 20, 2003
    Inventors: Michael R. Palovich, Katherine L. Widdowson, Hong Nie
  • Stable emulsion compositions
    Publication number: 20030212114
    Abstract: An emulsion composition containing a compound represented by the formula: 1
    Type: Application
    Filed: July 30, 2002
    Publication date: November 13, 2003
    Inventor: Jun Sato
  • Matrix metalloprotease inhibitors
    Publication number: 20030212067
    Abstract: Compounds of the formula (I) 1
    Type: Application
    Filed: April 16, 2003
    Publication date: November 13, 2003
    Inventors: Arlindo Lucas Castelhano, Steven Lee Bender, Judith Gail Deal, Stephen Horne, Teng J. Liak, Zhengyu Yuan
  • Nitromethylthiobenzene derivatives as aldose reductase inhihibitors
    Publication number: 20030203966
    Abstract: The invention concerns novel compounds of general formula (1), their tautomeric forms, and their additive salts with pharmaceutically acceptable bases. The invention also concerns methods for preparing these compounds and their applications as medicines. These compounds inhibit the aldose reductase enzyme and can be used in the treatment or prevention of peripheral and autonomous neurological diabetic complications, renal and ocular disorders such as cataract and retinopathy.
    Type: Application
    Filed: November 12, 2002
    Publication date: October 30, 2003
    Inventors: Francois Collonges, Herve Dumas, Claude Lardy, Philippe Durbin
  • Use of bissulfonamides for producing medicines for the treatment of hyperlipidemia
    Patent number: 6632838
    Abstract: The use of bissulfonamides for producing medicines for the treatment of hyperlipidemia. The invention relates to the use of bissulfonamides and their salts for producing medicines for the treatment of hyperlipidemia. The use of compounds of formula I in which the radicals have the stated meanings, and of their salts for producing a medicine for the treatment of hyperlipidemia is described.
    Type: Grant
    Filed: August 31, 2000
    Date of Patent: October 14, 2003
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Reinhard Kirsch, Hans-Ludwig Schaefer, Eugen Falk, Norbert Krass