Nitrogen Bonded Directly To Ring Carbon Of The Hetero Ring Patents (Class 514/245)
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Patent number: 6794398Abstract: The invention provides an agent for the prophylaxis and treatment of liver disease and an activation inhibitor of hepatic stellate cells, which contains a compound having a Rho kinase inhibitory activity. The compound having a Rho kinase inhibitory activity, such as (+)-trans-4-(1-aminoethyl)-1-(4-pyridylcarbamoyl)cyclohexane, is useful for the prophylaxis and treatment of liver diseases, such as hepatitis, hepatic fibrosis, hepatic cirrhosis, hepatic cancer and the like, because it has various actions, such as a superior inhibitory action on the activation of hepatic stellate cell, suppressive action on hepatic fibrogenesis in liver tissues and the like.Type: GrantFiled: March 6, 2002Date of Patent: September 21, 2004Assignee: Mitsubishi Pharma CorporationInventors: Makoto Nakamuta, Hajime Nawata, Masayoshi Uehata
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Publication number: 20040162288Abstract: The invention relates to triazines and the use thereof to inhibit lysophosphatidic acid acyltransferase &bgr; (LPAAT-&bgr;) activity. The invention further relates to methods of treating cancer using said triazines. The invention also relates to methods for screening for LPAAT-&bgr; activity.Type: ApplicationFiled: November 13, 2003Publication date: August 19, 2004Applicant: Cell Therapeutics, Inc.Inventors: Baoqing Gong, John Tulinsky, Lynn Bonham, J. Peter Klein, Robert E. Finney, David M. Hollenback, Scott A. Shaffer, Norina M. Tang, Thayer H. White, David W. Leung
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Publication number: 20040157839Abstract: Compounds of Formula (I) that act as cannabinoid receptor ligands and their uses in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals are described herein.Type: ApplicationFiled: January 21, 2004Publication date: August 12, 2004Applicant: Pfizer IncInventor: David A. Griffith
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Patent number: 6767548Abstract: This invention relates to a biocidal composition resistant to the formation of a gel and to the method for stabilizing a concentrate containing, in addition to the biocide, a carbodiimide, a lipophilic/hydrophilic emulsifier mixture having a HLB of 6 to 20 and optionally an oil and/or an alkoxylated ester of a polyhydroxylated compound, by adding to the concentrate an effective anti-gelling amount of an anti-gelling agent selected from the group of an inorganic oxide, a epoxidized naturally occurring or synthetic vegetable oil and an epoxylated ester of a saturated or unsaturated C6 to C18 aliphatic acid optionally containing hydroxy substitution and mixtures of the foregoing anti-gelling agents.Type: GrantFiled: February 15, 2002Date of Patent: July 27, 2004Assignee: ISP Investments Inc.Inventors: Kolazi S. Narayanan, Domingo Jon, George B. Beestman
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Publication number: 20040122009Abstract: Trisubstituted triazines can be synthesized from cyanuric chloride. These compounds are useful anti-tubulin agents for treating cancer and proliferative diseases.Type: ApplicationFiled: June 20, 2003Publication date: June 24, 2004Applicant: New York UniversityInventors: Young-Tae Chang, Alexander Schier, Ho-Sang Moon, Eric Jacobson, Puja Parikh
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Patent number: 6747016Abstract: The present invention relates to compounds of formula (I), in which B, D, E, G, X, Y, Z, R1, R2 and s have the meanings indicated in the claims, their physiologically tolerable salts and their prodrugs. The compounds of formula (I) are valuable pharmacologically active compounds. They are vitronectin receptor antagonist and inhibitors of cell adhesion and are suitable for the therapy and prophylaxis of illnesses which are based on the interaction between vitronectin receptors and their ligands in cell-cell or cell-matrix interaction processes or which can be prevented, alleviated or cured by influencing such interactions. For example, they can be applied for inhibiting bone resorption by osteoclasts and thus for treating and preventing osteoporosis, or for inhibiting undesired angiogenesis or prolifertion of cells of the vascular smooth musculature.Type: GrantFiled: March 6, 2002Date of Patent: June 8, 2004Assignees: Aventis Pharma Deutschland GmbH, Genetech Inc.Inventors: Anuschirwan Peyman, Jochen Knolle, Thomas R Gadek, Jean-Francois Gourvest, Jean-Marie Ruxer
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Publication number: 20040106599Abstract: The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.Type: ApplicationFiled: September 12, 2002Publication date: June 3, 2004Inventors: Daniel Delorme, Soon Hyung Woo, Arkadii Vaisburg, Oscar Moradei, Silvana Leit, Stephane Raeppel, Sylvie Frechette, Giliane Bouchain
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Patent number: 6743817Abstract: Disclosed are compounds of the formula and the pharmaceutically acceptable salts thereof wherein R, Ar, A, n, R1 and R2 are defined herein. These compounds are highly selective agonists, antagonists or inverse agonists for GABAA brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAA brain receptors and are therefore useful in the diagnosis and treatment of anxiety, depression, Down Syndrome, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory. Pharmaceutical compositions, including packaged pharmaceutical compositions, are also disclosed.Type: GrantFiled: September 6, 2001Date of Patent: June 1, 2004Assignee: Neurogen CorporationInventors: George Maynard, LingHong Xie, Stanislaw Rachwal
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Patent number: 6730672Abstract: The invention concerns compounds of formula (I) wherein each of G1, G2 and G3 is CH or N; m is 1 or 2; R1 includes hydrogen, halogeno and (1-4C)alkyl; M1 is a group of the formula: NR2—L1—T1R3 in which R2 and R3 together form a (1-4C)alkylene group, L1 includes (1-4C)alkylene, and T1 is CH or N; A may be a direct link; M2 is a group of the formula: (T2R4)r—L2—T3R5 in which r is 0 or 1, each of T2 and T3 is CH or N, each of R4 and R5 is hydrogen or (1-4C)alkyl, or R4 and R5 together form a (1-4C)alkylene group, and L2 includes (1-4C)alkylene; M3 may be a direct link to X; X includes sulphonyl; and Q includes naphthyl and a heterocyclic moiety; or a pharmaceutically-acceptable salt thereof; processes for their preparation, pharmaceutical compositions containing them and their use as antithrombotic or anticoagulant agents.Type: GrantFiled: March 8, 2001Date of Patent: May 4, 2004Assignee: Zeneca LimitedInventors: Alan Wellington Faull, Andrew Stocker, Colette Marie Mayo, John Preston
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Patent number: 6720341Abstract: A compound having a Rho kinase inhibitory activity, such as (+)-trans-4-(1-aminoethyl)-1-(4-pyridylcarbamoyl)-cyclohexane, has a renal interstitial fibrosis inhibitory action in renal interstitial fibrosis model mice and various other actions, and therefore, is useful as an agent for the prophylaxis or treatment of renal diseases.Type: GrantFiled: October 17, 2002Date of Patent: April 13, 2004Assignee: Mitsubishi Pharma CorporationInventors: Toshiki Moriyama, Enyu Imai
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Patent number: 6716421Abstract: This invention relates to devices, kits, and methods for eliminating termite colonies. The kits, devices, and methods employ a termiticidal bait matrix containing a) a termiticide selected such that the termiticide causes death to about 50 to about 100% of termites within about 24 to about 84 days after the termites begin to ingest the termiticide or the bait matrix comprising the termiticide, b) a cellulose containing material, and c) water. The termiticidal bait matrix can be used in a bait station installed in the ground. The kits are suitable to be used by consumers in their homes.Type: GrantFiled: March 5, 2001Date of Patent: April 6, 2004Assignee: University of Florida Research Foundation, Inc.Inventors: Philip Frederick Brode, III, Garry Steven Garrett, Leo Timothy Laughlin, Randall Stryker Matthews, Dale Edwin Barker, Daniel James Kinne, Gary Eugene McKibben, Christopher Miles Miller, Timothy Robert Probst
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Publication number: 20040063705Abstract: The invention encompasses compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions, uses and methods for prophylaxis and treatment of cancer.Type: ApplicationFiled: August 21, 2002Publication date: April 1, 2004Inventors: Jean-Christophe Harmange, Shon Booker, John L. Buchanan, Stuart Chaffee, Perry M. Novak, Simon Van Der Plas, Xiaotian Zhu
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Publication number: 20040053926Abstract: This invention relates to triazine compounds of formula (I): 1Type: ApplicationFiled: September 5, 2003Publication date: March 18, 2004Applicant: Synta Pharmaceuticals Corp., a Delaware CorporationInventors: M. Ono, Lijun Sun, Shijie Zhang, Teresa Przewloka, David A. James, Wenli Ding, Yumiko Wada
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Publication number: 20040043997Abstract: The present invention provides methods for the control of insect pests in the vicinity of feces or manure of a domestic animal. Such methods comprise orally administering cyromazine, wherein said administering results in the presence of an insecticidal amount of cyromazine in the feces of the animal being treated. The present invention further provides methods for inhibiting the development of fly larvae on feces or manure of a domestic animal. Such methods also comprise orally administering cyromazine, wherein said administering results in the presence of an insecticidal amount of cyromazine in the feces of the animal being treated.Type: ApplicationFiled: August 29, 2002Publication date: March 4, 2004Inventor: Kathleen G. Palma
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Patent number: 6696445Abstract: The present invention also provides a general method to whereby mono-, bi-, or tricyclic heterocycles may be modified to obtain potent antagonists at the NPY1 receptor. The present invention provides novel, potent, non-peptidic antagonists of NPY receptors, particularly, the NPY1 receptors, designed from a selection of mono-, bi-, or tri-cyclic heterocyclic cores. This invention relates to novel compounds, compositions, and methods for the treatment of physiological disorders associated with an excess of neuropeptide Y. The novel compounds encompassed by the present invention are those of the formula I-XV.Type: GrantFiled: November 8, 2002Date of Patent: February 24, 2004Assignees: Neurogen Corporation, Pfizer Inc.Inventors: Raymond F. Horvath, Jennifer N Tran, Stéphane De Lombaert, Kevin J. Hodgetts, Philip A. Carpino, David A. Griffith
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Publication number: 20040023966Abstract: A pyrimidinylbenzimidazole or triazinylbenzimidazole derivative represented by the general formula (I): 1Type: ApplicationFiled: March 10, 2003Publication date: February 5, 2004Applicant: KUMIAI CHEMICAL INDUSTRY CO., LTD.Inventors: Masaru Shibata, Kiyoshi Kawai, Takechi Makihara, Norihisa Yonekura, Takehiro Kawashima, Junetsu Sakai, Norimichi Muramatsu
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Publication number: 20040019050Abstract: This invention is directed to triazine derivatives which are selective antagonists for a NPY (Y5) receptor. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention provides a pharmaceutical composition made by combining a therapeutically effective amount of the compound of this invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier.Type: ApplicationFiled: April 22, 2003Publication date: January 29, 2004Applicant: Synaptic Pharmaceutical CorporationInventors: Mohammad R. Marzabadi, Stewart A. Nobel, Mahesh N. Desai
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Patent number: 6677353Abstract: 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-phenyl-N-heteroaralkyl aminoalcohols.Type: GrantFiled: May 23, 2002Date of Patent: January 13, 2004Assignee: 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
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Patent number: 6677341Abstract: The invention relates to substituted aryl and heteroaryl (R)-Chiral Halogenated 1-Substitutedamino-(n+1)-Alkanol compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Novel high yield, stereoselective processes for the preparation of the chiral substituted alkanol compounds from chiral and achiral intermediates are described. Preferred (R)-Chiral 1-Substitutedamino-(n+1)-Alkanol compounds are substituted (R)-Chiral heteroaryl aminoalcohols.Type: GrantFiled: December 12, 2001Date of Patent: January 13, 2004Assignee: Pharmacia CorporationInventors: James A. Sikorski, Richard C. Durley, Margaret L. Grapperhaus, Mark A. Massa, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Brian S. Hickory, Monica B. Norton, William F. Vernier, Deborah A. Mischke, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
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Publication number: 20040002496Abstract: The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.Type: ApplicationFiled: March 14, 2003Publication date: January 1, 2004Inventors: David Bebbington, Hayley Binch, Jean-Damien Charrier, Simon Everitt, Julian M. C. Golec, David Kay, Ronald Knegtel, Andrew Miller, Francoise Pierard
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Publication number: 20030229092Abstract: Bradykinin B1-receptor antagonists of formula 1Type: ApplicationFiled: January 14, 2002Publication date: December 11, 2003Applicant: PHARMACOPEIA, INC.Inventors: Michael H.J. Ohlmeyer, John G. Baldwin, Roland E. Dolle, Vidyadhar Paradkar, Jorge Gabriel Quintero, Gonghua Pan
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Patent number: 6649631Abstract: Compounds containing two aromatic systems covalently linked through a linker containing one or more atoms, or “linker” defined as including a covalent bond per se so as to space the aromatic systems at a distance 1.5-15 Å, are effective in treating conditions associated with bone deficits. The compounds can be administered to vertebrate subjects alone or in combination with additional agents that promote bone growth or that inhibit bone resorption. They can be screened for activity prior to administration by assessing their ability to effect the transcription of a reporter gene coupled to a promoter associated with a bone morphogenetic protein and/or their ability to stimulate calvarial growth in model animal systems.Type: GrantFiled: November 19, 1999Date of Patent: November 18, 2003Assignees: The Board of Regents of the University of Texas System, ZymoGenetics Corporation, OsteoScreenInventors: Mark W. Orme, Nand Baindur, Kirk G. Robbins, Scott M. Harris, Maria Kontoyianni, Laurence H. Hurley, Sean M. Kerwin, Gregory Mundy, Charles Petrie
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Patent number: 6645964Abstract: The present invention relates to cancer therapy and to novel anticancer agent having a mechanism of action which is quite specific. It also relates to novel chemical compounds as well as their therapeutic application in humans.Type: GrantFiled: November 28, 2000Date of Patent: November 11, 2003Assignee: Aventis Pharma S.A.Inventors: Patrick Mailliet, Jean-François Riou, Jean-Louis Mergny, Abdelazize Laoui, François Lavelle, Odile Petitgenet
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Publication number: 20030203908Abstract: A compound of formula (I) or (II), wherein X is hydrogen, halogen, alkyl, aralkyl,aryloxy, arylalkoxy or alkoxy, Y is hydrogen, halogen, alkyl, aralkyl, aryloxy, arylalkoxy or alkoxy, or formula (a) wherein A and B are different and one of A and B is CH2 and the other is O, NH, or S or A and B are both CH2 or CH═, and Ra, Rb, and Rc are the same or different and are hydrogen, halogen, alkyl, alkoxy, aryloxy, aralkyl or arylalkoxy. R1 is hydrogen, and R2 is hydrogen, C1-C6 alkyl or aryl which is unsubstituted or substituted by halogen, cyano, hydroxy, C1-C6 alkyl, which is unsubstituted or substituted by halogen, cyano, hydroxy, C1-C6 alkoxy, aralkyl, aryloxy or aryl, C1-C6 alkoxy, aralkyl, arylalkoxy, aryloxy or aryl, which is unsubstituted or substituted by halogen, cyano, hydroxy, C1-C6 alkyl or C1-C6 alkoxy; and pharmaceutically acceptable salts thereof; with the proviso that when R2 is phenyl and Y is hydrogen, X is not chlorine.Type: ApplicationFiled: February 24, 2003Publication date: October 30, 2003Inventor: Gordon Lowe
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Patent number: 6638926Abstract: This invention provides novel pyrazole compounds that are useful as protein kinase inhibitors, especially as inhibitors of aurora-2 and GSK-3. The compounds may be used to treat abnormal physiological function leading to diseases such as cancer, diabetes and Alzheimer's disease.Type: GrantFiled: September 14, 2001Date of Patent: October 28, 2003Assignee: Vertex Pharmaceuticals IncorporatedInventors: Robert J. Davies, Pan Li, Jean-Damien Charrier, David Bebbington
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Publication number: 20030199473Abstract: This invention concerns the compounds of formula 1Type: ApplicationFiled: March 26, 2003Publication date: October 23, 2003Applicant: Janssen Pharmaceutica N.V.Inventors: Paul A.J. Janssen, Jan Heeres, Henri E.L. Moereels, Michael Joseph Kukla, Donald W. Ludovici
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Publication number: 20030191125Abstract: The present invention provides novel compounds, and pharmaceutical compositions thereof, and methods of using same in the treatment of affective disorders, anxiety, depression, post-traumatic stress disorders, eating disorders, supranuclear palsey, irritable bowl syndrome, immune supression, Alzheimer's disease, gastrointestinal diseases, anorexia nervosa, drug and alcohol withdrawal symptoms, drug addiction, inflammatory disorders, or fertility problems.Type: ApplicationFiled: March 17, 2003Publication date: October 9, 2003Inventors: Robert John Chorvat, Parthasarathi Rajagopalan
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Patent number: 6630469Abstract: Amino-pyrimidine and amino-triazine derivatives having 5-HT7 antagonist activity for the treatment of sleeping disorders, depression, schizophrenia, anxiety, obsessive compulsive disorders, circadian rhythm disorders, ocular disorders and/or centrally and peripherally mediated hypertension are provided.Type: GrantFiled: April 24, 2001Date of Patent: October 7, 2003Assignee: Bristol-Myers Squibb CompanyInventors: Michael A. Poss, Ashok V. Purandare, Ronald J. Mattson, Li-Qiang Sun
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Publication number: 20030162773Abstract: The present invention relates to water-containing formulations for the dermal control of parasitic insects on animals, having the following compositionType: ApplicationFiled: January 17, 2003Publication date: August 28, 2003Inventors: Kirkor Sirinyan, Hubert Dorn, Ulrich Heukamp
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Patent number: 6610677Abstract: This invention describes novel pyrazole compositions comprising a pharmaceutically acceptable carrier and a compound of formula VIII: wherein Z1 is N or C—R9, Z2 is N or CH, and Z3 is N or C—Rx, provided that one of Z1 and Z3 is nitrogen; G is Ring C or Ring D; Ring C is selected from a phenyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, or 1,2,4-triazinyl ring, wherein said Ring C has one or two ortho substituents independently selected from —R1; Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; and Rx, R1, R2, R2′, R3, and R9 are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.Type: GrantFiled: September 14, 2001Date of Patent: August 26, 2003Assignee: Vertex Pharmaceuticals IncorporatedInventors: Robert Davies, Pan Li, Julian M. C. Golec, Jean-Damien Charrier, Ronald Knegtel, David Bebbington
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Publication number: 20030157062Abstract: A method for exterminating termites comprising using an entomopathogenic nematode together with an inset-growth regulator or a slow-acting insecticide, wherein insecticidal effects are reinforced compared with the cases using singly the entomopathogenic nematode and the insect-growth regulator or the slow-acting insecticide, respectively, and a bait station for exterminating termites that contains an entomopathogenic nematode with an insect-growth regulator or a slow-acting insecticide. According to the invention, emission of harmful chemicals to environment can be suppressed. The invention is nonpoisonous for human being and livestock, and is useful for indoor or outdoor extermination of termites.Type: ApplicationFiled: December 3, 2002Publication date: August 21, 2003Inventors: Kenji Mikami, Satoshi Yamanaka
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Publication number: 20030153570Abstract: The invention relates to aryl triazines and uses thereof, including to inhibit lysophosphatidic acid acyltransferase &bgr; (LPAAT-&bgr;) activity and/or proliferation of cells such as tumor cells.Type: ApplicationFiled: October 30, 2002Publication date: August 14, 2003Applicant: Cell Therapeutics, Inc.Inventors: Rama Bhatt, Baoqing Gong, Feng Hong, Scott A. Jenkins, J. Peter Klein, Anil M. Kumar, John Tulinsky
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Publication number: 20030149041Abstract: Compounds that selectively inhibit inappropriate kinase activities and methods for their preparation are disclosed.Type: ApplicationFiled: June 28, 2002Publication date: August 7, 2003Applicant: Pharmacopeia, Inc.Inventors: Shawn David Erickson, James Inglese, Jeffrey John Letourneau, Christopher Mark Riviello
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Publication number: 20030139416Abstract: The invention encompasses compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions, uses and methods for prophylaxis and treatment of cancer and polycystic kidney disease.Type: ApplicationFiled: April 10, 2002Publication date: July 24, 2003Inventors: John L. Buchanan, Joseph L. Kim, Perry M. Novak, Joseph J. Nunes, Vinod F. Patel
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Patent number: 6596064Abstract: A use of tetralin derivatives as biocidal and antifouling agents for preventing and slowing the growth of algae, molds and microorganisms. In particular, the vitamin derivatives are constituted by salts of menadione bisulfite with the heterocyclic bases triazine and piperazine.Type: GrantFiled: December 26, 2001Date of Patent: July 22, 2003Assignee: Luigi Stoppani S.p.A.Inventors: Stefano Bonati, Francesco Monteleone
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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
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Publication number: 20030109530Abstract: The invention concerns compounds of general formula (I) wherein: R1, R2, R3, R4, R5 and R6 are as defined in claim 1. Said compounds are useful in the treatment of pathologies related to the insulin-resistance syndrome.Type: ApplicationFiled: July 15, 2002Publication date: June 12, 2003Inventors: Gerard Moinet, Daniel Cravo, Liliane Doare, Micheline Kergoat, Didier Mesangeau
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Publication number: 20030109529Abstract: This invention relates to novel compositions and methods of treating humans and animals infected by Apicomplexan parasites. More specifically, the present invention relates to treating an Apicomplexan infection by administering s-triazines, such as atrazine, to an infected human or animal. The present invention also relates to pharmaceutical compositions containing therapeutically effective amounts of s-triazines, such as atrazine, useful in treating parasitic infections.Type: ApplicationFiled: October 2, 2002Publication date: June 12, 2003Applicant: Biomes, Inc.Inventors: Miles P. Hacker, Greg Manske, Lori L. Shatney-Leach
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Patent number: 6573284Abstract: Novel pro-drugs and assay reagents are provided which are useful as therapeutic agents especially for delivery and targetting therapeutically active agents to melanoma cells. The pro-drugs and assay reagents are substrates for tyrosinase and may be represented by the formula TyrX—B—ThrAg*. The compounds of formula TyrX—B—ThrAg* are capable of releasing a therapeutically active agent or assayable substance (ThrAg) at a desired location. TyrX— being a residue of an optionally substituted tyrosine analogue.Type: GrantFiled: June 14, 1999Date of Patent: June 3, 2003Inventors: Patrick Anthony Riley, Andrew Photiou, Tariq Hussain Khan, Helen Mary Osborn
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Publication number: 20030100557Abstract: The invention relates to triazines and the use thereof to inhibit lysophosphatidic acid acyltransferase &bgr; (LPAAT-&bgr;) activity. The invention further relates to methods of treating cancer using said triazines. The invention also relates to methods for screening for LPAAT-&bgr; activity.Type: ApplicationFiled: September 6, 2002Publication date: May 29, 2003Applicant: Cell Therapeutics, Inc.Inventors: Robert Finney, David Leung, J. Peter Klein, David M. Hollenback, Lynn Bonham, Scott A. Shaffer, Norina M. Tang, Thayer H. White, John Tulinsky, Baoqing Gong
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Patent number: 6569856Abstract: This invention is directed to triazine derivatives which are selective antagonists for a NPY (Y5) receptor. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention provides a pharmaceutical composition made by combining a therapeutically effective amount of the compound of this invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier.Type: GrantFiled: January 3, 2002Date of Patent: May 27, 2003Assignee: Synaptic Pharmaceutical CorporationInventors: Mohammad R. Marzabadi, Stewart A. Noble, Mahesh N. Desai
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Patent number: 6566365Abstract: In accordance with the present invention there is provided a method for treating or preventing a Flaviviridea viral infection in a host comprising administering a therapeutically effective amount of at least one compound of formula (I) or (II) or a pharmaceutically acceptable salts thereof, wherein Ra, R, Z and Y are defined in the application.Type: GrantFiled: November 3, 2000Date of Patent: May 20, 2003Assignee: BioChem Pharma Inc.Inventor: Richard Storer
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Publication number: 20030087908Abstract: The invention encompasses compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions, uses and methods for prophylaxis and treatment of cancer and angiogenesis-related disease.Type: ApplicationFiled: April 10, 2002Publication date: May 8, 2003Inventors: Stephanie D. Geuns-Meyer, Lucian V. DiPietro, Joseph L. Kim, Vinod F. Patel
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Patent number: 6559148Abstract: Use of compounds modulating P2 purinoceptors, in particular antagonists such as Basilen Blue E-3G (Reactive Blue 2), for the prevention of the damages due to global cerebral ischemia and ischemia-reperfusion. Said compounds reduce the mortality in case of global cerebral ischemia as well as the neuronal damage of the hippocampus.Type: GrantFiled: September 19, 2001Date of Patent: May 6, 2003Assignees: Consiglio Nazionale delle Ricerche, Fondazione Santa LuciaInventors: Cinzia Volonte′, Giuseppe Sancesario, Giorgio Bernardi
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Publication number: 20030083332Abstract: N-Heterocyclic derivatives of the formula (I): 1Type: ApplicationFiled: April 12, 2002Publication date: May 1, 2003Applicant: Berlex Laboratories, Inc.Inventors: Damian O. Arnaiz, John J. Baldwin, David D. Davey, James J. Devlin, Roland Ellwood Dolle, Shawn David Erickson, Kirk McMillan, Michael M. Morrissey, Michael H. J. Ohlmeyer, Gonghua Pan, Vidyadhar Madhav Paradkar, John Parkinson, Gary B. Phillips, Bin Ye, Zuchun Zhao
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Publication number: 20030078265Abstract: N-Heterocyclic derivatives of the formula (I): 1Type: ApplicationFiled: April 12, 2002Publication date: April 24, 2003Applicant: Berlex Laboratories, Inc.Inventors: Damian O. Arnaiz, John J. Baldwin, David D. Davey, James J. Devlin, Roland Ellwood Dolle, Shawn David Erickson, Kirk McMillan, Michael M. Morrissey, Michael H. J. Ohlmeyer, Gonghua Pan, Vidyadhar Madhav Paradkar, John Parkinson, Gary B. Phillips, Bin Ye, Zuchun Zhao
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Publication number: 20030069239Abstract: The present invention is directed to substituted 2-aryl-4-arylaminopyrimidine and analogs thereof, represented by the general Formula I: 1Type: ApplicationFiled: December 12, 2001Publication date: April 10, 2003Applicant: Cytovia, Inc.Inventors: Sui Xiong Cai, John A. Drewe, P. Sanjeeva Reddy, Bao Nguyen, Azra Pervin
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Publication number: 20030069246Abstract: Disclosed are compounds of the formula: 1Type: ApplicationFiled: February 25, 2002Publication date: April 10, 2003Applicant: Neurogen CorporationInventors: James W. Darrow, Stephane J. De Lombaert, Charles A. Blum, Jennifer N. Tran, Mark A. Giangiordano, David Andrew Griffith, Philip Albert Carpino
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Publication number: 20030069210Abstract: N-Heterocyclic derivatives of the formula (I): 1Type: ApplicationFiled: April 12, 2002Publication date: April 10, 2003Applicant: Berlex Laboratories, Inc.Inventors: Damian O. Arnaiz, John J. Baldwin, David D. Davey, James J. Devlin, Roland Ellwood Dolle, Shawn David Erickson, Kirk McMillan, Michael M. Morrissey, Michael H. J. Ohlmeyer, Gonghua Pan, Vidyadhar Madhav Paradkar, John Parkinson, Gary B. Phillips, Bin Ye, Zuchun Zhao
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Publication number: 20030069245Abstract: This invention provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with indoleoxoacetyl piperazine derivatives. These compounds possess unique antiviral activity, whether used alone or in combination with other antivirals, antiinfectives, immunomodulators or HIV entry inhibitors. More particularly, the present invention relates to the treatment of HIV and AIDS.Type: ApplicationFiled: December 19, 2001Publication date: April 10, 2003Inventors: Owen B. Wallace, Tao Wang, Kap-Sun Yeung, Bradley C. Pearce, Nicholas A. Meanwell, Zhilei Qiu, Haiquan Fang, Qiufen May Xue, Zhiwei Yin