Plural Ring Hetero Atoms In The Additional Hetero Ring Patents (Class 514/217.05)
-
Publication number: 20040063689Abstract: Compositions useful for improving effectiveness of alpha-2-adrenergic agonist components include carrier components, alpha-2-adrenergic agonist components, solubility enhancing components which aid in solubilizing the alpha-2-adrenergic agonist components. In one embodiment, the alpha-2-adrenergic agonist components include alpha-2-adrenergic agonists. In another embodiment, the solubility enhancing components include carboxymethylcellulose.Type: ApplicationFiled: October 22, 2003Publication date: April 1, 2004Applicant: Allergan, Inc.Inventors: Orest Olejnik, Edward D.S. Kerslake
-
Patent number: 6713472Abstract: A compound which is a chymase inhibitor and which is represented by a formula [I] and salts thereof. In the formula [I], X is R6—(A2)n—N, R1 and R2 are H, alkyl, cycloalkyl or aryl, R3 and R4 are H, alkyl, cycloalkyl, aryl or aromatic heterocycle, R5 is H, alkyl, cycloalkyl, aryl or —A3—A4—R7, R6 is H, alkyl, cycloalkyl, OH, alkoxy, aryl, aryloxy or an aromatic heterocycle, R7 is H, alkyl, OH, alkoxy, aryl, aryloxy, amino, alkylamino, arylamino, an aromatic heterocycle or a nonaromatic heterocycle, A1 is alkylene, A2 is carbonyl or sulfonyl, A3 is alkylene, A4 is carbonyl or oxalyl and n is o or 1.Type: GrantFiled: January 18, 2002Date of Patent: March 30, 2004Assignee: Santen Pharmaceutical Co., Ltd.Inventors: Kazuo Nishimura, Masakazu Ban, Ken-ichi Fujimura, Naoyuki Kobayashi, Masanori Hori, Eiko Matsumoto
-
Patent number: 6713478Abstract: This invention provides compounds of Formula (I): wherein R1 and R2 are independent substituents or are fused to form spirocyclic rings; R3, RC, and R4 are as defined herein; and R5 is a substituted benzene ring or a substituted five or six membered heterocyclic ring having in its backbone 1, 2, or 3 heteroatoms including O, S, SO, SO2 or NR6; or pharmaceutically acceptable salt thereof, as well as pharmaceutical compositions and methods using the compounds as antagonists of the progesterone receptor.Type: GrantFiled: March 12, 2003Date of Patent: March 30, 2004Assignees: Wyeth, Ligand Pharmaceuticals, Inc.Inventors: Puwen Zhang, Eugene A. Terefenko, Andrew Fensome, Jay E. Wrobel, Horace Fletcher, III, Lin Zhi, Todd K. Jones, James P. Edwards, Christopher M. Tegley
-
Publication number: 20040048849Abstract: The invention concerns novel cyclin-dependent kinase (CDK) and glycolene synthase kinase-3 (GSK-3) inhibitors, corresponding to general formula (I), wherein: A represents a hydrogen atom, a halogen atom, a formyl, cyano, nitro, guanidinoaminomethylenyl, (1,3-dihydro-2-oxoindol)-3-ylidenemethyl, alkylcarbonyl, aralkylcarbonyl or heteroaralkylcarbonyl radical, or a -L-NR1R2 radical wherein L represents an alkylene radical and R1 and R2 are selected independently among a hydrogen atom and an alkyl radical or R1 and R2 together with the nitrogen bearing them form a heterocycle with 5 to 7 members optionally substituted; X represents a hydrogen atom, an alkylthio, aralkylthio, alkylthioxo or aralkylthioxo radical, or a NR4R5 radical wherein R4 represents an alkyl radical, a hydroxyalkyl radical, a cycloalkyl radical optionally substituted, an aralkyl radical whereof the aryl radical is optionally substituted, or R4 represents a heteroaryl or heteroarylalkyl radical, the heteroaryl radical of the heteroaryl or heteType: ApplicationFiled: June 6, 2003Publication date: March 11, 2004Inventors: Gregoire Prevost, Marie-Odile Lonchampt, Sun Kim, Barru Morgan, Gerard Ulibarri, Christophe Thurieau
-
Publication number: 20040048848Abstract: This invention discloses novel gamma secretase inhibitors of the formula: 1Type: ApplicationFiled: February 5, 2003Publication date: March 11, 2004Applicant: Schering-Plough Corporation and Pharmacopeia, Inc.Inventors: Dmitri A. Pissarnitski, Hubert B. Josien, Elizabeth M. Smith, John W. Clader, Theodros Asberom, Tao Guo, Douglas W. Hobbs
-
Publication number: 20040044007Abstract: The present invention relates to methods of treating psychiatric or neurologic disorders, in particular psychoses, by administration of a compound formula of (I) 1Type: ApplicationFiled: June 17, 2003Publication date: March 4, 2004Applicant: H. Lundbeck A/SInventors: Jan Kehler, Benny Bang-Andersen
-
Patent number: 6699856Abstract: Compounds represented by formula I: as well as pharmaceutically acceptable salts, esters, N-oxides and hydrates thereof are disclosed. Pharmaceutical compositions and methods of use are also included. The compounds are active against the caspase-3 enzyme, and thus are useful to treat caspase-3 mediated diseases and conditions.Type: GrantFiled: July 25, 2002Date of Patent: March 2, 2004Assignee: Merck & Co., Inc.Inventors: Yongxin Han, Andre Giroux, Robert Zamboni, Daniel J. McKay, Christopher I. Bayly, Erich L. Grimm, John Colucci
-
Patent number: 6699864Abstract: The present invention provides compounds of the formula: wherein R1-R8, X, Y, Z, n and m are defined in the application. The compounds of the invention have affinity for the 5-HT1A receptor.Type: GrantFiled: June 20, 2002Date of Patent: March 2, 2004Assignee: H. Lundbeck A/SInventors: Thomas Ruhland, Christian Krog-Jensen, Mario Rottländer, Gitte Mikkelsen, Ejner Knud Moltzen, Kim Andersen
-
Publication number: 20040038982Abstract: This invention relates to substituted heterocyclic compounds which are modulators, agonists or antagonists, of the CCR5 receptor. In addition, this invention relates to the treatment and prevention of disease states mediated by CCR5, including, but not limited to, asthma and atopic disorders (for example, atopic dermatitis and allergies), rheumatoid arthritis, sarcoidosis, or idiopathic pulmonary fibrosis and other fibrotic diseases, atherosclerosis, psoriasis, autoimmune diseases such as multiple sclerosis, treating and/or preventing rejection of transplanted organs, and inflammatory bowel disease, all in mammals, by the use of substituted heterocyclic compounds which are CCR5 receptor antagonists. Furthermore, since CD8+ T cells have been implicated in COPD, CCR5 may play a role in their recruitment and therefore antagonists to CCR5 could provide potential therapeutic in the treatment of COPD.Type: ApplicationFiled: February 5, 2003Publication date: February 26, 2004Inventors: William E. Bondinell, Michael J. Neeb
-
Publication number: 20040029864Abstract: A method for the treatment, prevention and amelioration of colds and/or cough in a subject in need of such treatment, prevention and amelioration, comprises administering to the subject a cyclooxygenase-2 selective inhibitor or prodrug thereof and one or more colds and cough active ingredient. Compositions, pharmaceutical compositions and kits for practicing the method are also disclosed.Type: ApplicationFiled: February 4, 2003Publication date: February 12, 2004Applicant: Pharmacia CorporationInventor: Stephen P. MacMillan
-
Patent number: 6680314Abstract: Compounds of formula (1) or (2), enantiomers thereof, mixtures thereof, and pharmaceutically acceptable salts thereof: wherein: n is 0, or 1; R is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl; and R1 is aryl optionally substituted with alkyl, cycloalkyl, cycloalkylalkyl alkenyl, alkynyl, alkoxy, cycloalkoxy, thioalkoxy, thiocycloalkoxy, methylenedioxy, aryloxy, halogen, CF3, OCF3, CN, amino, nitro, aryl, or a monocyclic 5 to 6-membered heteroaryl group, or R is a monocyclic 5 to 6-membered heteroaryl group optionally substituted with alkyl, cycloalkyl, cycloalkylalkyl alkenyl, alkynyl, alkoxy, cycloalkoxy, thioalkoxy, thiocycloalkoxy, methylenedioxy, aryloxy, halogen, CF3, OCF3, CN, amino, nitro, aryl, or a monocyclic 5 to 6-membered heteraryl group, or R is a bicyclic heteroaryl group composed of a monocyclic 5 to 6-membered heteroaryl group fused to a benzene ring, optionally substituted with alkyl, cycloalkyl, cycloalkylalkyl alkenyl, alkynyl, alkoxy, cyType: GrantFiled: April 30, 2002Date of Patent: January 20, 2004Assignee: Neurosearch A/SInventors: Dan Peters, Gunnar M. Olsen, Simon F. Nielsen, Elsebet O. Nielsen
-
Publication number: 20040009968Abstract: The present invention provides compounds of formula I: 1Type: ApplicationFiled: January 23, 2003Publication date: January 15, 2004Inventors: Hayley Binch, Guy Brenchley, Julian M. C. Golec, Ronald Knegtel, Michael Mortimore, Sanjay Patel, Alistair Rutherford
-
Publication number: 20030236247Abstract: Compounds having the formula 1Type: ApplicationFiled: March 21, 2003Publication date: December 25, 2003Inventors: Steven W. Elmore, Cheol-Min Park, Xilu Wang
-
Publication number: 20030236251Abstract: An isomer, enantiomer, diastereoisomer, or tautomer of a compound, represented by formula I: 1Type: ApplicationFiled: July 18, 2002Publication date: December 25, 2003Applicant: Boehringer Ingelheim (Canada) Ltd.Inventors: Pierre Louis Beaulieu, Gulrez Fazal, Sylvie Goulet, George Kukolj, Martin Poirier, Youla S. Tsantrizos
-
Publication number: 20030207842Abstract: Novel compounds having activity as non-covalent inhibitors of urokinase and having activity in reducing or inhibiting blood vessel formation are provided. These compounds have at a group having a guanidino moiety or derivative thereof. These compounds are useful in vitro for monitoring plasminogen activator levels and in vivo in treatment of conditions which are ameliorated by inhibition of or decreased activity of urokinase and in treating pathologic conditions wherein blood vessel formation is related to a pathologic condition.Type: ApplicationFiled: December 4, 2002Publication date: November 6, 2003Inventors: Amir P. Tamiz, L. Josue Alfaro-Lopez, Odile Esther Levy, Joseph Edward Semple
-
Publication number: 20030207867Abstract: Compounds of general structural formula (I) and use of the compounds and salts and solvates thereof, as therapeutic agents.Type: ApplicationFiled: January 15, 2003Publication date: November 6, 2003Inventors: Mark W. Orme, Jason Scott Sawyer, Lisa M Schultze
-
Patent number: 6642242Abstract: The invention provides compounds of formula (I), wherein R1 represents C1-4 alkoxy optionally substituted by one or more fluorine atoms; R2 represents H or C1-6 alkoxy optionally substituted by one or more fluorine atoms; R3 represents one or more groups independently selected from H, halogen, C1-4 alkoxy and CF3; in addition, R2 and one R3 group may together represent —OCH2—, the methylene group being attached to the ortho-position of the pendant phenyl ring; R4 represents a 4-, 5- or 6-membered heterocyclic ring containing 1 or 2 heteroatoms selected from N, O and S, the ring being optionally fused to a benzene ring or a 5- or 6-membered heterocyclic ring containing 1 or 2 heteroatoms selected from N, O and S, the ring system as a whole being optionally substituted; X represents CH or N; and L is absent or represents a cyclic group or an open chain group; and pharmaceutically acceptable salts thereof.Type: GrantFiled: March 19, 2001Date of Patent: November 4, 2003Assignee: Pfizer Inc.Inventors: Alan John Collis, David Nathan Abraham Fox, Julie Newman
-
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
-
Publication number: 20030191110Abstract: The present invention relates to methods for modulating the cholesterol biosynthetic pathway. The level of cholesterol in the body is linked to numerous pathological states. The methods of the present invention alter the transcription levels of genes involved in the cholesterol biosynthesis. The methods of the present invention can used for treating diseases mediated by the cholesterol biosynthetic pathway.Type: ApplicationFiled: November 1, 2002Publication date: October 9, 2003Inventors: Martyn Botfield, Fiona McDonald, Joern Kraetzschmar, Bernhard Lindenthal, Bertold Kreft
-
Publication number: 20030186966Abstract: This invention concerns amide derivatives of Formula (I) wherein X is CH or N; Y is CH or N; m is 0-3; R1 is a group such as hydroxy, halogeno, trifluoromethyl, cyano, mercapto, nitro, amino, carboxy and carbamoyl; n is 0-3; R2 is a group such as hydroxy, halogeno, trifluoromethyl, cyano, mercapto, nitro, amino, carboxy and (1-6C)alkoxycarbonyl; R3 is hydrogen, halogeno, (1-6C)alkyl or (1-6C)alkoxy; q is 0-4; and Q is a group such as aryl, aryloxy, aryl-(1-6C)alkoxy, arylamino, N-(1-6C)alkyl-arylamino and aryl-(1-6C)alkylamino; or pharmaceutically-acceptable salts or in-vivo-cleavable esters thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by cytokines.Type: ApplicationFiled: January 29, 2003Publication date: October 2, 2003Applicant: ASTRAZENECA ABInventor: Dearg S. Brown
-
Publication number: 20030176431Abstract: Triazinoindole derivatives are useful in the prophylaxis and treatment of pestivirus infections and diseases associated with pestivirus infections.Type: ApplicationFiled: February 5, 2003Publication date: September 18, 2003Inventors: Daniel C. Pevear, Theodore J. Nitz, Martin Seipel
-
Publication number: 20030176418Abstract: The present invention relates to tetrahydroquinoline compounds as muscarinic receptor agonists; compositions comprising the same; methods of inhibiting an activity of a muscarinic receptor with said compounds; methods of treating a disease condition associated with a muscarinic receptor using said compounds; and methods for identifying a subject suitable for treatment using said compounds.Type: ApplicationFiled: December 23, 2002Publication date: September 18, 2003Inventors: Niels Skjaerbaek, Kristian Norup Koch, Bo Lennart Mikael Friberg, Bo-Ragnar Tolf
-
Patent number: 6613776Abstract: This invention describes novel pyrazole compositions comprising a pharmaceutically acceptable carrier and a compound of formula V: wherein Z1 is N, CRa, or CH, and Z2 is N or CH, provided one of Z1 and Z2 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; Rx and Ry are independently selected from T—R3, or Rx and Ry are taken together with their intervening atoms to form a fused ring; and R1, R2, R2′, R3, and T 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: September 2, 2003Assignee: Vertex Pharmaceuticals IncorporatedInventors: Ronald Knegtel, David Bebbington, Hayley Binch, Julian Golec, Sanjay Patel, Jean-Damien Charrier, David Kay, Robert Davies, Pan Li, Marion Wannamaker, Cornelia Forster, Albert Pierce
-
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
-
Patent number: 6596715Abstract: This invention relates to the compound of Formula (I): or a pharmaceutically acceptable salt, hydrate or solvate thereof, which is an inhibitor of cysteine proteases, particularly cathepsin K, and is useful in the treatment of diseases in which inhibition of bone loss or of cartilage degradation is a factor.Type: GrantFiled: May 6, 2002Date of Patent: July 22, 2003Assignee: SmithKline Beecham CorporationInventors: Robert W. Marquis, Jr., Daniel Frank Veber
-
Publication number: 20030134839Abstract: The present invention relates to 5-(alkylidene-cycloalkyl)-pyrazoles and 5-(alkylidene-heterocyclyl)-pyrazoles of the formula I: 1Type: ApplicationFiled: November 1, 2002Publication date: July 17, 2003Inventor: Subas M. Sakya
-
Publication number: 20030130263Abstract: Compositions comprising both a sedative and a non-sedative antihistamine are disclosed as well as methods of inhibiting the release of histamines by administration of the compositions to a mammalian subject.Type: ApplicationFiled: December 5, 2001Publication date: July 10, 2003Applicant: PEIRCE MANAGEMENT,LLCInventor: Mark Hirsh
-
Publication number: 20030119817Abstract: The present invention relates to certain substituted phenyl oxazolidinones and to processes for the synthesis of the same. This invention also relates to pharmaceutical compositions containing the compounds of the present invention as antimicrobials. The compounds are useful antimicrobial agents, effective against a number of human and veterinary pathogens, including gram-positive aerobic bacteria such as multiply-resistant staphylococci, streptococci and enterococci as well as anaerobic organisms such as Bacterioides spp. and Clostridia spp. species, and acid fast organisms such as Mycobacterium tuberculosis, Mycobacterium avium and Mycobacterium spp.Type: ApplicationFiled: January 17, 2002Publication date: June 26, 2003Inventors: Anita Mehta, Sudershan K. Arora, Biswajit Das, Abhijit Ray, Sonali Rudra, Ashok Rattan
-
Publication number: 20030119811Abstract: Compounds represented by Formula (I): 1Type: ApplicationFiled: April 2, 2002Publication date: June 26, 2003Inventors: Nigel J. Liverton, John W. Butcher, Charles McIntyre, Christopher F. Claiborne, David A. Claremon, John A. McCauley, Joseph J. Romano, Wayne Thompson, Peter M. Munson
-
Patent number: 6583137Abstract: This invention relates to the compound of Formula (I) or a pharmaceutically acceptable salt, hydrate or solvent thereof, which is an inhibitor of cysteine proteases, particularly cathespin K, and is useful in the treatment of diseases in which inhibition of bone loss or of cartilage degradation is a factorType: GrantFiled: May 6, 2002Date of Patent: June 24, 2003Assignee: SmithKline Beecham CorporationInventors: Robert Wells Marquis, Jr., Daniel Frank Veber
-
Patent number: 6583136Abstract: The present invention concerns compounds of formula the N-oxide forms, the salts, the quaternary amines and stereochemically isomeric forms thereof, wherein D represents a tetrahydrofuran or dioxolane ring substituted with aryl and azolmethyl; —A—B— represents an optionally substituted bivalent radical of formula —N═CH—, —CH═N—, —CH═CH—, —CH2—CH2; Alk represents C1-6alkanediyl; Y represents optionally substituted C1-6alkanediyl; R1 and R2 represent hydrogen, C1-6alkyl or arylC1-6alkyl; or R1 and R2 may be taken together to form an optionally substituted heterocyclic radical selected from morpholinyl, pyrrolidinyl, piperidinyl, homopiperidinyl, piperazinyl or phthalimid-1-yl; aryl represents phenyl, naphthalenyl, 1,2,3,4-tetrahydro-naphthalenyl, indenyl or indanyl; each of said aryl groups may optionally be substituted; having broad-spectrum antifungal activity; their preparation, compositions containing them anType: GrantFiled: February 4, 2002Date of Patent: June 24, 2003Assignee: Janssen Pharmacuetica N.V.Inventors: Lieven Meerpoel, Leo Jacobus Jozef Backx
-
Publication number: 20030105074Abstract: The present invention provides a phthalazine compound as a therapeutic agent for erectile dysfunction represented by the following formula, a pharmacologically acceptable salt thereof or a hydrate thereof: 1Type: ApplicationFiled: October 28, 2002Publication date: June 5, 2003Applicant: Eisai Co., Ltd.Inventors: Nobuhisa Watanabe, Norio Karibe, Kazuki Miyazaki, Fumihiro Ozaki, Atsushi Kamada, Shuhei Miyazawa, Yoshimitsu Naoe, Toshihiko Kaneko, Itaru Tsukada, Tadashi Nagakura, Hiroki Ishihara, Kohtarou Kodama, Hideyuki Adachi
-
Publication number: 20030100548Abstract: 1 Compounds of formula (I) wherein Z is —CH2SR and R represents hydrogen or —COCH3, are useful as metalloproteinase inhibitors, especially as inhibitors of MMP 13.Type: ApplicationFiled: September 20, 2002Publication date: May 29, 2003Inventors: Bernard Christophe Barlaam, Nicholas John Newcombe, Howard Tucker, David Waterson
-
Publication number: 20030096824Abstract: The present invention relates to phenylamidines of general formula 1Type: ApplicationFiled: October 21, 2002Publication date: May 22, 2003Inventors: Frank Himmelsbach, Brian Guth
-
Publication number: 20030091505Abstract: The present invention provides compounds of Formula (I): 1Type: ApplicationFiled: October 15, 2002Publication date: May 15, 2003Inventor: Jian-Min Fu
-
Publication number: 20030073672Abstract: A method for treating an allergic condition, including an atopic allergic condition, using substituted pyrazoles.Type: ApplicationFiled: September 5, 2001Publication date: April 17, 2003Inventors: J. Guy Breitenbucher, Hui Cai, James P. Edwards, Cheryl A. Grice, Yin Gu, Darin J. Gustin, Lars Karlsson, Haripada Khatuya, Steven P. Meduna, Barbara A. Pio, Siquan Sun, Kevin L. Tays, Robin L. Thumond, Jianmei Wei
-
Patent number: 6541472Abstract: Triazinoindole derivatives are useful in the prophylaxis and treatment of pestivirus infections and diseases associated with pestivirus infections.Type: GrantFiled: April 12, 2000Date of Patent: April 1, 2003Assignee: ViroPharma IncorporatedInventors: Daniel C. Pevear, Theodore J. Nitz, Martin Seipel
-
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
-
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
-
Patent number: 6509329Abstract: A cyclic diamine compound of formula (1): wherein A is a single bond or C≡C; X and Y are individually CH or a nitrogen atom; m is 1 or 2; and n is a number of 1 to 5; an acid-addition salt thereof, or a hydrate thereof. The compound has excellent inhibitory effects on both cell adhesion and cell infiltration and is useful as a medicine for prevention or treatment of diseases such as allergy, asthma, rheumatism, arteriosclerosis and inflammation.Type: GrantFiled: June 29, 2001Date of Patent: January 21, 2003Assignee: Kowa Co., Ltd.Inventors: Tatsuhiko Kodama, Masahiro Tamura, Toshiaki Oda, Yukiyoshi Yamazaki, Masahiro Nishikawa, Takeshi Doi, Yoshinori Kyotani
-
Patent number: 6509334Abstract: This invention provides compounds of Formula (I): wherein R1 and R2 may be single substituents or fused to form spirocyclic or hetero-spirocyclic rings; R3 is H, OH, NH2, C1 to C6 alkyl, substituted C1 to C6 alkyl, C3 to C6 alkenyl, substituted C1 to C6 alkenyl, alkynyl, or substituted alkynyl, CORC; RC is H, C1 to C3 alkyl, substituted C1 to C3 alkyl, aryl, substituted aryl, C1 to C3 alkoxy, substituted C1 to C3 alkoxy, C1 to C3 aminoalkyl, or substituted C1 to C3 aminoalkyl; R4 is H, halogen, CN, NO2, C1 to C6 alkyl, substituted C1 to C6 alkyl, alkynyl, or substituted alkynyl, C1 to C6 alkoxy, substituted C1 to C6 alkoxy, amino, C1 to C6 aminoalkyl, or substituted C1 to C6 aminoalkyl; and R5 is selected from a trisubstituted benzene ring of a five or six membered ring with 1, 2, or 3 heteroatoms from the group including O, S, SO, SO2 or NR6 and containing one or two independent substituents from the group including H, halogen, CN, N02, amino, and C1 to C3 alkyl, C1 to C3 alkoxy, C1 to C3 aType: GrantFiled: April 19, 2000Date of Patent: January 21, 2003Assignees: American Home Products Corporation, Ligand Pharmaceuticals, Inc.Inventors: Puwen Zhang, Eugene A. Terefenko, Andrew Fensome, Jay E. Wrobel, Horace Fletcher, III, Lin Zhi, Todd K. Jones, James P. Edwards, Christopher M. Tegley
-
Patent number: 6498158Abstract: The present invention is concerned with the compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein p is 0 to 3; q is 0 to 4; —A—B— represents —(CH2)r—, —(CH2)t—O—, —(CH2)t—S(═O)u— or —(CH2)t—NR3—; r is 2 to 4; t is 1 to 3; u is 0 to 2; X1 is O, S, NR3 or a direct bond; R1 and R4 are C1-6alkyl, halo, polyhaloC1-6alkyl, hydroxy, mercapto, C1-6alkyloxy, C1-6alkylthio, C1-6alkylcarbonyloxy, aryl, cyano, nitro, Het3, R6, NR7R8 or substituted C1-4alkyl; R2 is aryl, Het1, C3-7cycloalkyl, cyano, optionally substituted C1-6alkyl, —C(═Q)—X2—R15; R3 is hydrogen or C1-4alkyl; R15 is hydrogen, optionally substituted C1-6alkyl, C3-7cycloalkyl, aryl; where X2 is a direct bond, R15 may also be halo or Het1; where X2 is NR5, R15 may also be hydroxy; where X2 is C(═O)—NH—NH or NH—NH—C(&boType: GrantFiled: May 22, 2001Date of Patent: December 24, 2002Assignee: Janssen Pharmaceutica N.V.Inventors: Jean Fernand Armand Lacrampe, Yannick Ligny, Eddy Jean Edgard Freyne, Frederik Dirk Deroose
-
Publication number: 20020193322Abstract: A physiologically acceptable aqueous solution, and water-soluble compositions suitable for obtaining it, comprising a first physiologically acceptable compound of an acidic nature and a second physiologically acceptable compound of a basic nature that are able to give rise to a precipitate in water, characterized in that it also contains a trisubstituted salt of glycyrrhizic acid in a sufficient quantity to form a clear solution in water.Type: ApplicationFiled: January 29, 2002Publication date: December 19, 2002Inventors: Leandro Baiocchi, Mauro De Gregorio
-
Publication number: 20020193366Abstract: Compounds of the formula 1Type: ApplicationFiled: April 25, 2002Publication date: December 19, 2002Applicant: WyethInventors: Gary P. Stack, Megan Tran, Jonathan L. Gross, George E. M. Husbands
-
Patent number: 6495688Abstract: Disclosed are compounds of formula wherein Ar represents an aryl or heteroaryl group; and R1, R2, R3, R4 and R5 represent organic or inorganic substituents, which compounds are highly selective partial agonists or antagonists at human CRF1 receptors and, thus, are useful in the diagnosis and treatment of treating stress related disorders such as post trumatic stress disorder (PTSD) as well as depression, headache and anxiety.Type: GrantFiled: June 21, 2001Date of Patent: December 17, 2002Assignee: Neurogen CorporationInventors: Jun Yuan, Alan Hutchison
-
Publication number: 20020165218Abstract: Compounds that inhibit DNA-dependent protein kinase, compositions comprising the compounds, methods to inhibit the DNA-PK biological activity, methods to sensitize cells the agents that cause DNA lesions, and methods to potentiate cancer treatment are disclosed.Type: ApplicationFiled: August 28, 2001Publication date: November 7, 2002Inventors: James Halbrook, Edward A. Kesicki, Laurence E. Burgess, Stephen T. Schlachter, Charles T. Eary, Justin G Schiro, Hongmei Huang, Michael Evans, Yongxin Han
-
Patent number: 6476016Abstract: Cyclic oxyguanidine pyrazinone compounds are described, including compounds of the Formula I: wherein R3, R4, R5, W, and A are as set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof. The compounds of the invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin. Compositions for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation are described.Type: GrantFiled: July 17, 2001Date of Patent: November 5, 2002Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Aihua Wang, Bruce Edward Tomczuk, Tianbao Lu, Richard M. Soll, John Curtis Spurlino, Roger Francis Bone
-
Publication number: 20020151541Abstract: A pharmaceutical composition comprising a tiotropium salt; and an antihistamine, optionally together with a pharmaceutically acceptable excipient, the tiotropium salt and the antihistamine optionally in the form of their enantiomers, mixtures of their enantiomers, their racemates, their solvates, or their hydrates, processes for preparing them, and their use in the treatment of respiratory tract diseases.Type: ApplicationFiled: October 19, 2001Publication date: October 17, 2002Inventors: Michel Pairet, Michael P. Pieper, Christopher John Montague Meade, Christel Schmelzer
-
Publication number: 20020132805Abstract: An antihistaminic syrup is stabilized against degradation of the active ingredient, by the addition of and about 0.05 to about 5 mg/mL of an aminopolycarboxylic acid such as a salt of ethylenediaminetetraacetic acid.Type: ApplicationFiled: July 5, 2001Publication date: September 19, 2002Inventors: Farah J. Munayyer, Frank Guazzo, Elliot I. Stupak, Imtiaz A. Chaudry, Joel A. Sequeira
-
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