Nitrogen Bonded Directly To Ring Carbon Of The Hetero Ring Patents (Class 514/245)
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Publication number: 20030055044Abstract: 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: ApplicationFiled: September 14, 2001Publication date: March 20, 2003Inventors: Robert Davies, Pan Li, Julian Golec
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Publication number: 20030022885Abstract: This invention describes novel pyrazole compounds of formula II: 1Type: ApplicationFiled: December 20, 2001Publication date: January 30, 2003Inventors: David Bebbington, Jean-Damien Charrier, Julian Golec, Francoise Pierard
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Publication number: 20030008868Abstract: Disclosed are compounds useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are processes of making such compounds.Type: ApplicationFiled: May 10, 2002Publication date: January 9, 2003Applicant: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Pier Francesco Cirillo, Daniel R. Goldberg, Abdelhakim Hammach, Neil Moss, John Robinson Regan
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Publication number: 20030004166Abstract: This invention is directed to sorbitol dehydrogenase inhibitory compounds of formula I 1Type: ApplicationFiled: March 26, 2002Publication date: January 2, 2003Inventor: Banavara L. Mylari
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Patent number: 6500825Abstract: This invention is related to substituted 2-aminoacetamides represented by Formula II: or a pharmaceutically acceptable salt or prodrug thereof, wherein: R1, R2, R3 and R4 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl; R5, R6 and R7 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl, or R5, is defined as above, and R6 and R7 together with the nitrogen atom to which they are attached form a heterocycle, including piperidine, piperazine, morpholine; A1 and A2 are independently aryl, heteroaryl, saturated or partially unsaturated carbocycle or saturated or partially unsaturated heterocycle, any of which is optionally substituted; X is one or O, S, NR8, CH2, C(O), NR8C(O), C(O)NR8, SO, SO2 or a covalent bond; where R8 is hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl orType: GrantFiled: August 21, 2001Date of Patent: December 31, 2002Assignee: Euro-Celtique S.A.Inventors: Nancy C. Lan, Yan Wang, Sui Xiong Cai
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Patent number: 6495684Abstract: This invention is directed to poly-hydroxylated monocyclic N-heterocyclic derivatives selected from the following formula: wherein Z1, Z2, R1, R2, R3, R4, R5, R6, and R7 are defined herein. These compounds are useful as anti-coagulants.Type: GrantFiled: May 4, 2001Date of Patent: December 17, 2002Assignee: Berlex Laboratories, Inc.Inventor: Gary B. Phillips
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Publication number: 20020183323Abstract: N-Heterocyclic derivatives of the formula (I): 1Type: ApplicationFiled: April 12, 2002Publication date: December 5, 2002Applicant: 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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Patent number: 6489333Abstract: This invention relates to novel heterocycles which are useful as antagonists of the &agr;v&bgr;3 integrin, the &agr;2b&bgr;3 integrin, and related cell surface adhesive protein receptors, to pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of cell adhesion, the treatment of angiogenic disorders, inflammation, bone degradation, cancer metastasis, diabetic retinopathy, thrombosis, restenosis, macular degeneration, and other conditions mediated by cell adhesion and/or cell migration and/or angiogenesis.Type: GrantFiled: April 9, 2001Date of Patent: December 3, 2002Assignee: Bristol - Meyers Squibb Pharma CompanyInventors: William J. Pitts, Prabhakar K. Jadhav
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Patent number: 6482829Abstract: The invention relates to compounds of the formula as described herein and pharmaceutically acceptable acid addition salts thereof. The described compounds have a good affinity to the NK1 receptor.Type: GrantFiled: May 21, 2001Date of Patent: November 19, 2002Assignee: Hoffmann-La Roche Inc.Inventors: Guido Galley, Thierry Godel, Annick Goergler, Torsten Hoffmann, Sabine Kolczewski, Stephan Roever
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Patent number: 6482815Abstract: Novel organic arsenic compounds are described as cytotoxic agents with potent anti-tumor activity against cancer cells and particularly, with regard to human leukemic cells and breast cancer cells.Type: GrantFiled: November 27, 2000Date of Patent: November 19, 2002Assignee: Parker Hughes InstituteInventors: Fatih M. Uckun, Xing-Ping Liu
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Patent number: 6479492Abstract: Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.Type: GrantFiled: January 21, 2000Date of Patent: November 12, 2002Assignee: Elan Pharmaceuticals, Inc.Inventors: Andrei W. Konradi, Michael A. Pleiss, Eugene D. Thorsett, Susan Ashwell, Dimitrios Sarantakis, Gregory S. Welmaker, Anthony Kreft, Christopher Semko, Robert Warren Sullivan, Christopher Joseph Soares, Kiev Sui Ly, Christine M. Tarby
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Publication number: 20020165203Abstract: N-Heterocyclic derivatives of the formula (I): 1Type: ApplicationFiled: April 12, 2002Publication date: November 7, 2002Applicant: 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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Patent number: 6472392Abstract: Triazole compounds of the following formula: where Ar1, A, B and Ar2 have the meanings given in the description, possess a high affinity for the dopamine D3 receptor and can therefore be used for treating diseases which respond to dopamine D3 ligands.Type: GrantFiled: December 28, 1999Date of Patent: October 29, 2002Assignee: Abbott LaboratoriesInventors: Dorothea Starck, Stefan Blank, Hans-Jörg Treiber, Liliane Unger, Barbara Neumann-Schultz, Theophile-Marie Le Bris, Hans-Jürgen Teschendorf, Karsten Wicke
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Publication number: 20020151548Abstract: The present invention provides a new process and intermediates for the production of antiviral compound 4′,4-bis-{4,6-bis-[3-(bis-carbamoyl-methyl-1-sulfamoyl)-phenylamino]-[1,3,5]triazin-2-ylamino}-biphenyl-2,2′-disulfonic acid and its pharmaceutically acceptable salts.Type: ApplicationFiled: January 31, 2002Publication date: October 17, 2002Applicant: American Home Products CorporationInventors: Silvio Iera, Christopher A. Demerson, Jacqueline F. Lunetta, Maria Papamichelakis, Michael F. MacEwan, Wayne G. McMahon, John R. Potoski, Arthur G. Mohan
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Publication number: 20020147196Abstract: This invention relates to a composition and method for alleviating neuropathic pain and/or its symptoms. The composition comprises (1) a compound that inhibits the reuptake of both norepinephrine and dopamine or inhibits the reuptake of norepinephrine alone in combination with (2) a compound that acts as a sodium channel blocker. The method involves the administration of the composition in an effective amount to alleviate neuropathic pain and/or its symptoms.Type: ApplicationFiled: April 3, 2002Publication date: October 10, 2002Inventors: Steven Noel Quessy, George David Rudd, Michael Fredrik Winnem
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Publication number: 20020147181Abstract: This invention concerns the compounds of formula 1Type: ApplicationFiled: November 15, 2001Publication date: October 10, 2002Inventors: Paul A.J. Janssen, Jan Heeres, Henri E.L. Moereels, Michael Joseph Kukla, Donald W. Ludovici
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Patent number: 6458803Abstract: 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: November 23, 2001Date of Patent: October 1, 2002Assignee: G.D. Searle & Co.Inventors: 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: 20020137747Abstract: N-heterocyclic compounds that block cytokine production via inhibition of p38 kinase are disclosed.Type: ApplicationFiled: June 26, 2001Publication date: September 26, 2002Inventors: Kevin Joseph Moriarty, Yvonne Shimshock, Gulzar Ahmed, Junjun Wu, James Wen, Wei Li, Shawn David Erickson, Jeffrey John Letourneau, Edward McDonald, Katerina Leftheris, Stephen T. Wrobleski, Zahid Hussain, Ian Henderson, Axel Metzger, John J. Baldwin, Alaric J. Dyckman
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Publication number: 20020132807Abstract: The present invention relates to novel heterocyclyl-containing diaryl sulfide compounds that are useful for treating inflammatory and immune diseases, to pharmaceutical compositions comprising these compounds, and to methods of inhibiting inflammation or suppressing immune response in a mammal.Type: ApplicationFiled: June 25, 2001Publication date: September 19, 2002Inventors: Gary T. Wang, Sheldon Wang, Robert Gentles
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Patent number: 6451825Abstract: A Rho kinase inhibitor is provided as a novel pharmaceutical agent, particularly as a therapeutic agent of hypertension, a therapeutic agent of angina pectoris, a suppressive agent of cerebrovascular contraction, a therapeutic agent of asthma, a therapeutic agent of peripheral circulation disorder, a prophylactic agent of immature birth, a therapeutic agent of arteriosclerosis, an anti-cancer drug, an anti-inflammatory agent, an immunosuppressant, a therapeutic agent of autoimmune disease, an anti-AIDS drug, a contraceptive, a prophylactic agent of digestive tract infection, a therapeutic agent of osteoporosis, a therapeutic agent of retinopathy and a brain function improving drug. In addition, the Rho kinase inhibitor is provided as a reagent and a diagnostic.Type: GrantFiled: February 26, 2001Date of Patent: September 17, 2002Assignee: Mitsubishi Pharma CorporationInventors: Masayoshi Uehata, Takashi Ono, Hiroyuki Satoh, Keiji Yamagami, Toshio Kawahara
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Publication number: 20020128266Abstract: The present invention provides compounds that elevate cellular expression of the ABCA-1 gene, promoting cholesterol efflux from cells and increasing HDL levels in the plasma of a mammal, in particular humans. The compounds are useful for treating coronary artery disease.Type: ApplicationFiled: December 4, 2001Publication date: September 12, 2002Inventors: Michael Campbell, Prabha N. Ibrahim, Jeff A. Zablocki, Richard Lawn
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Patent number: 6448244Abstract: The present invention concerns novel water-soluble azole compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and stereochemically isomeric forms thereof; as antifungals; their processes for preparation, composition containing them and their use as a medicine.Type: GrantFiled: November 9, 2000Date of Patent: September 10, 2002Assignee: Janssen Pharmaceutica N.V.Inventors: Lieven Meerpoel, Leo Jacobus Jozef Backx, Louis Jozef Elisabeth Van der Veken
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Patent number: 6444667Abstract: The invention relates to insecticidal mixtures of spinosyns and agonists or antagonists of nicotinic acetylcholine receptors for protecting plants against attack by pests.Type: GrantFiled: November 17, 2000Date of Patent: September 3, 2002Assignee: Bayer AktiengesellschaftInventors: Wolfram Andersch, Hans-Jürgen Schnorbach, Detlef Wollweber
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Patent number: 6444638Abstract: This invention provides methods for screening a modulating agent which when combined with antitumor therapeutic agent increases apoptosis in tumor cells. This invention also provides methods for screening antitumor therapeutic agents suitable for combination therapy with a protein kinase C inhibitors capable of potentiating apoptosis in tumor cells. This invention further provides different combination therapies comprising the specific protein kinase C inhibitors and the antitumor therapeutic agents.Type: GrantFiled: August 20, 1998Date of Patent: September 3, 2002Assignee: Sloan-Kettering Institute for Cancer ResearchInventors: Gary K. Schwartz, Anthony P. Albino
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Publication number: 20020115668Abstract: This invention concerns the use of the compounds of formula 1Type: ApplicationFiled: February 5, 2002Publication date: August 22, 2002Inventors: Frederik Frans Desire Daeyaert, Bart De Corte, Marc Rene De Jonge, Jan Heeres, Chih Yung Ho, Paul Adriaan Jan Janssen, Robert W. Kavash, Lucien Maria Henricus Koymans, Michael Joseph Kukla, Donald William Ludovici
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Publication number: 20020103195Abstract: 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: October 31, 2001Publication date: August 1, 2002Applicant: CELL THERAPEUTICS,INC.Inventors: 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: 20020103201Abstract: 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: January 3, 2002Publication date: August 1, 2002Applicant: Synaptic Pharmaceutical CorporationInventors: Mohammad R. Marzabadi, Stewart A. Noble, Mahesh N. Desai
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Publication number: 20020094985Abstract: This invention relates to devices and methods for the local, differential delivery of nitric oxide within the body. The devices include devices having at least two differing nitric oxide donor compounds, such as nitric oxide donor compounds having differing half-lives and nitric oxide donor compounds having different release mechanisms. The devices also include devices having at least two chemically distinct compositions to which nitric oxide donor compounds are adsorbed or attached or within which the donor compounds are disposed. The devices are typically used to increase local nitric oxide concentration in the body upon placement of the medical article at a delivery position on or within a patient.Type: ApplicationFiled: January 18, 2001Publication date: July 18, 2002Inventors: Robert A. Herrmann, David Knapp
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Patent number: 6420438Abstract: The invention relates to serine protease inhibitor compounds of formula (I) where R1 is hydrogen, halo, cyano, nitro or hydroxyl, amino, alkoxy, alkyl, aminoalkyl, hydroxyalkyl, thiol, alkylthio, aminosulphonyl, alkoxyalkyl, alkoxycarbonyl, acyloxymethoxycarbonyl or alkylamino optionally substituted by hydroxy, alkylamino, alkoxy, oxo, aryl, cycloalkyl, amino, halo, cyano, nitro, thiol, alkylthio, alkylsulphonyl, alkylsulphenyl, alkylsulphonamido, alkylaminosulphonyl, haloalkoxy and haloalkyl; R2 is hydrogen, halo, methyl, amino, hydroxy, or oxo; and R is X—X—Y(R7)—L—Lp(D)n; wherein each X independently is C, N, O or S atom or a CO, CR1, C(R1)2 or NR1 group, at least one X being C, CO, CR1 or a C(R1)2 group; Y (the &agr;-atom) is a nitrogen atom or a CR1 group or Y and L taken together form a cyclic group; R7 is a lipophilic group selected from alkyl, alkenyl, mono- or bi-cycloalkyl, aryl, heteroaryl, mono- or bicycloalkylalkyl, mono- or bicycloalkylalkenyl, aralkyl,Type: GrantFiled: May 29, 2001Date of Patent: July 16, 2002Assignee: Tularik LimitedInventors: John Walter Liebeschuetz, William Alexander Wylie, Bohdan Waszkowycz, Christopher William Murray, Andrew David Rimmer, Pauline Mary Welsh, Stuart Donald Jones, Jonathan Michael Ernest Roscoe, Stephen Clinton Young, Phillip John Morgan, Nicholas Paul Camp, Andrew Philip Austin Crew
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Patent number: 6413962Abstract: The compositions are aromatic, gaunidino group containing compounds used for inducing anesthesia and reducing core temperatures in mammals.Type: GrantFiled: August 19, 1999Date of Patent: July 2, 2002Inventor: N. Eric Naftchi
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Publication number: 20020082259Abstract: This invention relates to triazine compounds of formula (I): 1Type: ApplicationFiled: November 30, 2001Publication date: June 27, 2002Inventors: M Ono, Lijun Sun, Shijie Zhang, Teresa Przewloka, David A. James, Wenli Ding, Yumiko Wada
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Patent number: 6403593Abstract: The present invention relates to triazole compounds of the following formula: where R1, R2, A, B and Ar have the meanings stated in the description. The compounds according to the invention have a high affinity for the dopamine D3 receptor and can therefore be used to treat disorders which respond to dopamine D3 ligands.Type: GrantFiled: January 13, 2000Date of Patent: June 11, 2002Assignee: Abbott LaboratoriesInventors: Beate Hellendahl, Annegret Lansky, Rainer Munschauer, Siegfried Bialojan, Liliane Unger, Hans-Jürgen Teschendorf, Karsten Wicke, Karla Drescher
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Patent number: 6399609Abstract: Corticotropin releasing factor (CRF) antagonists of formula I: and their use in treating anxiety, depression, and other psychiatric and neurological disorders.Type: GrantFiled: May 11, 2000Date of Patent: June 4, 2002Assignee: Bristol-Myers Squibb Pharma CompanyInventor: Richard Gerald Wilde
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Patent number: 6399620Abstract: There are described cycloalkyl derivatives of the formula (I) R1—Y—A—B—D—E—F—G (I) in which R1, Y, A, B, D, E, F and G have the meaning indicated herein, their preparation and their use as medicaments. The compounds according to the invention can be used as vitronectin receptor antagonists and as inhibitors of bone resorption.Type: GrantFiled: June 29, 2000Date of Patent: June 4, 2002Assignee: Aventis Pharma S.A.Inventors: Volkmar Wehner, Jochen Knolle, Hans Ulrich Stilz, Jean-Francois Gourvest, Denis Carniato, Thomas Richard Gadek, Robert McDowell, Robert Maurice Pitti, Sarah Catherine Bodary
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Publication number: 20020065270Abstract: N-heterocyclic compounds that block cytokine production via inhibition of p38 kinase are disclosed.Type: ApplicationFiled: December 22, 2000Publication date: May 30, 2002Inventors: Kevin Joseph Moriarty, Yvonne Shimshock, Gulzar Ahmed, Junjun Wu, James Wen, Wei Li, Shawn David Erickson, Jeffrey John Letourneau, Edward McDonald, Katerina Leftheris, Stephen T. Wrobleski
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Patent number: 6380194Abstract: This invention concerns the compounds of formula the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein R1 and R2 are each independently selected from hydrogen; hydroxy; amino; optionally substituted C1-6alkyl; C1-6alkyloxy; C1-6alkylcarbonyl; C1-6alkyloxycarbonyl; Ar1; mono- or di(C1-6alkyl)amino; mono- or di(C1-6alkyl)-aminocarbonyl; dihydro-2(3H)-furanone; or R1and R2 taken together may form pyrrolidinyl, piperidinyl, morpholinyl, azido or mono- or di(C1-6alkyl)amino-C1-4alkylidene; R3 is hydrogen, Ar1, C1-6alkylcarbonyl, C1-6alkyl, C1-6alkyloxycarbonyl, C1-6alkyl substituted with C1-6alkyloxycarbonyl; and R4, R5, R6, R7 and R8 are each independently selected from hydrogen, halo, C1-6alkyl, C1-6alkyloxy, cyano, aminocarbonyl, nitro, amino, trihalomethyl or trihalomethyloxy; L is optionally substituted C1-10alkyl; C3-10alkenyl; C3-10alkynyl; C3-7cycloalkyl; Ar1is optionally substituted phenyl; for the manufacture of a medicine for the tType: GrantFiled: September 26, 1997Date of Patent: April 30, 2002Assignee: 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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Patent number: 6372743Abstract: Disclosed are compounds of the formula: where R1, R2, R3, R4, R5, R6, and X are defined herein. These compounds are selective modulators of NPY1 receptors. These compounds are useful in the treatment of a number of CNS disorders, metabolic disorders, and peripheral disorders, particularly eating disorders and hypertension. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also provided. Compounds of the invention are also useful as probes for the localization of NPY1 receptors and as standards in assays for NPY1 receptor binding. Methods of using the compounds in receptor localization studies are given.Type: GrantFiled: September 29, 2000Date of Patent: April 16, 2002Assignees: Neurogen Corporation, Pfizer Inc.Inventors: James W. Darrow, Stephane De Lombaert, Charles Blum, Jennifer Tran, Mark Giangiordano, David Andrew Griffith, Philip Albert Carpino
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Patent number: 6372729Abstract: This invention concerns the use of the compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein A is CH, CR4 or N; n is 0, 1, 2, 3 or 4; R1 and R2 are each independently selected from hydrogen, hydroxy, C1-12alkyl, C1-12alkyloxy, C1-12alkylcarbonyl, C1-12alkyloxycarbonyl, aryl, amino, mono- or di(C1-12alkyl)amino, mono- or di(C1-12alkyl)aminocarbonyl wherein each of the aforementioned C1-12alkyl groups may optionally and each individually be substituted; or R1 and R2 taken together may form pyrrolidinyl, piperidinyl, morpholinyl, azido or mono- or di(C1-12alkyl)aminoC1-4alkylidene; R3 is hydrogen, aryl, C1-6alkylcarbonyl, optionally substituted C1-6alkyl; and each R4 independently is hydroxy, halo, C1-6alkyl, C1-6alkyloxy, cyano, aminocarbonyl, nitro, amino, trihalomethyl or trihalomethyloxy; L is —X—R5 or —X-Alk-R6; wherein R5 and R6 each independently are indanyl, indolyl or phenyl; each ofType: GrantFiled: August 8, 2000Date of Patent: April 16, 2002Assignee: Janssen Pharmaceutica N.V.Inventors: Frederik Frans Desiré Daeyaert, Bart De Corte, Marc René De Jonge, Jan Heeres, Chih Yung Ho, Paul Adriaan Jan Janssen, Robert W. Kavash, Lucien Maria Henricus Koymans, Michael Joseph Kukla, Donald William Ludovici
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Publication number: 20020035109Abstract: This invention is directed to benzamidine derivatives which are useful as anti-coagulants. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat disease-,states characterized by thrombotic activity.Type: ApplicationFiled: August 7, 2001Publication date: March 21, 2002Applicant: Berlex Laboratories, Inc.Inventors: Brad O. Buckman, David D. Davey, William J. Guilford, Michael M. Morrissey, Howard P. Ng, Gary B. Phillips, Shung C. Wu, Wei Xu
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Patent number: 6358496Abstract: There is described the use of indoline derivatives of formula wherein R1 is hydrogen; C1-C5alkyl; C1-C18alkoxy; or halogen; R2 is C1-C8alkyl; C5-C7cycloalkyl; C6-C10aryl; R3 is C1-C18alkyl or a radical of formula R4 is hydrogen; or a radical of formula R5 is C1-C18alkoxy; or a radical of formula R6 and R7 are each independently of the other hydrogen; or C1-C5alkyl; R8 is hydrogen; C1-C5alkyl; C5-C7cycloalkyl; phenyl; phenyl-C1-C3alkyl; R9 is C1-C18alkyl; X is halogen; a radical of formula n is 0; or 1, as light-protective agents.Type: GrantFiled: March 29, 2001Date of Patent: March 19, 2002Assignee: Ciba Specialty Chemicals CorporationInventors: Rudolf Zink, Helmut Luther
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Publication number: 20020032199Abstract: 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: ApplicationFiled: April 24, 2001Publication date: March 14, 2002Inventors: Michael A. Poss, Ashok V. Purandare, Ronald J. Mattson, Li-Qiang Sun
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Patent number: 6352977Abstract: The invention is directed to physiologically active compounds of general formula (I): wherein R1 is hydrogen, halogen, lower alkyl or lower alkoxy; X1, X2 and X6 independently represent N or CR2; and one of X3, X4 and X5 represents CR3 and the others independently represents N or CR2 where R2 is hydrogen, halogen, lower alkyl or lower alkoxy; and R3 represents a group —L1—(CH2)n—C(═O)—N(R4)—CH2—CH2—Y; and their prodrugs, and pharmaceutically acceptable salts and solvates of such compounds and their prodrugs. Such compounds have valuable pharmaceutical properties, in particular the ability to regulate the interaction of VCAM-1 and fibronectin with the integrin VLA-4 (&agr;4&bgr;1).Type: GrantFiled: June 8, 2000Date of Patent: March 5, 2002Assignee: Aventis Pharma LimitedInventors: Peter Charles Astles, Neil Victor Harris, Andrew David Morley
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Patent number: 6346531Abstract: Invented are G-CSF mimetics. Also invented are selected octacyclic compounds, pharmaceutical compositions containing these compounds, and methods of using these compounds as G-CSF mimetics. Also invented are novel processes used in preparing these compounds.Type: GrantFiled: November 21, 2000Date of Patent: February 12, 2002Assignee: SmithKline Beecham CorporationInventors: Juan I Luengo, Kevin J Duffy
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Patent number: 6344453Abstract: Insecticidal heterocyclic compounds of the formula wherein A represents a five-membered or six-membered heteroaryl group containing one to three hetero atoms selected from the group consisting of S, O and N, said heteroaryl group being unsubstituted or substituted by a halogen atom or C1-4 alkyl group, Z represents a three-membered straight chain, each member being selected from the group consisting of CH2—, O, S and N—R2 with at least one of said three members being O, S or N—R2, E represents CH2, O, S or N—R2, wherein R2 represents a hydrogen atom, a C1-4 alkyl group, a C1-4 alkoxy group or the group wherein R3 represents a hydrogen atom or halogen atom, X represents CH or N, Y represents a nitro group or cyano group, and R1 represents a hydrogen atom or methyl group.Type: GrantFiled: April 19, 1999Date of Patent: February 5, 2002Inventors: Kozo Shiokawa, Shinichi Tsuboi, Koichi Moriya, Katsuhiko Shibuya
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Patent number: 6342604Abstract: The present invention relates to the use of pyrimidine compounds of the following formula: wherein R1, R2, R3, A, B and Ar have the meanings indicated in the description. The compounds according to the invention have a high affinity for the dopamine D3 receptor and can therefore be used to treat disorders which respond to dopamine D3 ligands.Type: GrantFiled: January 14, 1997Date of Patent: January 29, 2002Assignee: BASF AktiengesellschaftInventors: Beate Hellendahl, Annegret Lansky, Rainer Munschauer, Siegfried Bialojan, Liliane Unger, Hans-Jürgen Teschendorf, Karsten Wicke, Karla Drescher
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Publication number: 20020010179Abstract: The present invention relates to novel insoluble s-triazine derivatives bearing benzotriazole and/or benzothiazole groups, to a process for their preparation and to their uses in particulate form as UV screening agents, in particular in the cosmetic field.Type: ApplicationFiled: April 16, 2001Publication date: January 24, 2002Inventors: Herve Richard, Madeleine Leduc, Alain Lagrange
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Patent number: 6340683Abstract: 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: April 22, 1999Date of Patent: January 22, 2002Assignee: Synaptic Pharmaceutical CorporationInventors: Mohammad R. Marzabadi, Stewart A. Noble, Mahesh N. Desai
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Patent number: 6337078Abstract: Controlled release compositions of matter are disclosed comprising complexes for treating a population of one or more aquatic organisms in a column of water. The complexes comprise at least one system wherein the system comprises at least one bioactive agent as a component selected for treating a population of aquatic organisms, at least one carrier component, and at least one coating component for regulating the controlled release rate and release profile of the bioactive agent in water or at least one bioactive agent and one joint-function component that can serve as both a carrier and coating to regulate the controlled release rate and release profile of the bioactive agent in water, with or without optional binder components and/or additional formulation materials. The components are selected to sink or float so that the complexes will permeate and/or remain in any planar or volumetric segment of a water column for a period of time that is sufficient to effectively treat a population of aquatic organisms.Type: GrantFiled: December 10, 1999Date of Patent: January 8, 2002Assignee: Lee County Mosquito Control DistrictInventor: Richard Levy
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Patent number: 6335339Abstract: The present invention provides pharmaceutical formulations comprising 1,3,5-triazine derivatives. The compounds and formulations of the present invention exhibit a range of activities, including antiviral and antibiotic activities, and the formulations may be used, alone or in combination, as a method of treating a patient in need of antiviral and/or antibiotic therapy. The triazine derivatives of the present invention bind to and inhibit functional nucleic acids, and hence, have broad applicability in the treatment of conditions associated with DNA and RNA viruses.Type: GrantFiled: January 13, 1999Date of Patent: January 1, 2002Assignee: Scriptgen Pharmaceuticals, Inc.Inventors: Jaime E. Arenas, Sharon T. Cload, Elizabeth S. Fleming, Yi Bin Xiang
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Patent number: 6329374Abstract: Use of agonists and antagonists of the nicotinergic acetylcholine receptors of insects for the non-systemic control of parasitic insects, such as fleas, lice and flies, on humans and on animals.Type: GrantFiled: February 9, 2001Date of Patent: December 11, 2001Assignee: Bayer AktiengesellschaftInventors: Hubert Dorn, Terence Hopkins