Nitrogen Or A -c(=x)- Group, Wherein X Is Chalcogen, Attached Directly To The Bicyclo Ring System By Nonionic Bonding Patents (Class 549/57)
-
Patent number: 7105513Abstract: The present invention relates to acylated, heteroaryl-condensed cycloalkenylamines, to pharmaceutical compositions comprising such compounds, to methods for the stimulation of the expression of endothelial NO synthase, and methods of treatment comprising administering such compounds.Type: GrantFiled: July 31, 2003Date of Patent: September 12, 2006Assignee: Sanofi-Avertis Deutschland GmbHInventors: Hartmut Strobel, Paulus Wohlfart
-
Patent number: 7019024Abstract: The invention provides a pharmaceutical for treatment of neurological and neuropsychiatric disorders comprising a compound of the formula: or a pharmaceutically acceptable salt thereof.Type: GrantFiled: January 9, 2001Date of Patent: March 28, 2006Assignee: Allelix Neuroscience Inc.Inventors: Vassil Iliya Ognyanov, Laurence A. Borden, Stanley Charles Bell, Jing Zhang
-
Patent number: 7019027Abstract: The present invention relates to a compound of formula (I): wherein: R3 is selected from the group consisting of 1-napthyl, 2-napthyl and cycloalkylphenyl; and R4 and R5 taken together form a ring having from 5 to 10 carbon atoms. Additionally, the invention provides a therapeutic method for preventing or treating a pathological condition or symptom in a mammal subject, such as a human, wherein increased angiogenesis is desired, comprising administering to a mammal in need of such therapy an effective amount of the aforementioned thiophene selective adenosine A1 allosteric enhancer.Type: GrantFiled: March 23, 2004Date of Patent: March 28, 2006Inventors: Joel M. Linden, Ray A. Ollson, Peter J. Scammells
-
Patent number: 6998407Abstract: Chemical compounds which are antagonists of Monocyte Chemoattractant Protein-1 (MCP-1) function, pharmaceutical compositions comprising these compounds, methods of treatment employing these compounds and compositions, and processes for preparing these compounds. The compounds are useful in the prevention or treatment of chronic or acute inflammatory or autoimmune diseases, especially those associated with aberrant lymphocyte or monocyte accumulation such as arthritis, asthma, atherosclerosis, diabetic nephropathy, inflammatory bowel disease, Crohn's disease, multiple sclerosis, nephritis, pancreatitis, pulmonary fibrosis, psoriasis, restenosis, and transplant rejection.Type: GrantFiled: November 18, 2003Date of Patent: February 14, 2006Assignees: Telik, Inc., Sanwa Kagaku Kenkyusho Co. Ltd.Inventors: Edgardo Laborde, Louise Robinson, Fanying Meng, Brian T. Peterson, Hugo O. Villar, Steven E. Anuskiewicz, Yoshiro Ishiwata, Shoji Yokochi, Yukiharu Matsumoto, Takuji Kakigami, Hideaki Inagaki, Takahito Jomori, Kouji Matsushima
-
Patent number: 6982348Abstract: The present invention provides a pharmaceutical agent having cholesteryl ester transfer protein inhibitory action and useful as a blood lipid lowering agent and the like. The present invention relates to a compound represented by the formula wherein Ar1 is an aromatic ring group optionally having substituents, Ar2 is an aromatic ring group having substituents, OR? is an optionally protected hydroxyl group, R is an acyl group, R? is a hydrogen atom or a hydrocarbon group optionally having substituents, or a salt thereof, and a pharmaceutical composition containing a compound of the formula (I) or a salt thereof or a prodrug thereof.Type: GrantFiled: January 25, 2002Date of Patent: January 3, 2006Assignee: Takeda Pharmaceutical Company LimitedInventors: Masakuni Kori, Kazumasa Hamamura, Hiromitsu Fuse, Toshihiro Yamamoto
-
Patent number: 6962929Abstract: The invention provides methods and compositions relating to novel pentafluorophenylsulfonamide derivatives and analogs and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly cancer, vascular restenosis, microbial infections, and psoriasis, or as lead compounds for the development of such agents.Type: GrantFiled: October 11, 2002Date of Patent: November 8, 2005Assignee: Tularik Inc.Inventors: John A. Flygare, Julio Cesar Medina, Bei Shan, David Louis Clark, Terry J. Rosen
-
Patent number: 6960669Abstract: A method is disclosed for the preparation of benzo[b]thiophenecarbodithioic esters of the formula: wherein R is alkyl, R1 is hydrogen, halogen, or alkyl, R2, R3, R4, and R5 are independently selected from the group consisting of hydrogen, halogen, alkyl, alkoxy, alkylthio, trifluoromethyl, cyano, and aryl, wherein said method comprises reacting an equivalent of an S-thiol ester of the formula: with one-third of an equivalent of P2S5, 2 equivalents of at least one alkali metal carbonate, about 2.5 mole percent of a phase transfer catalyst, and a catalytic amount of water in hot toluene.Type: GrantFiled: September 10, 2003Date of Patent: November 1, 2005Assignee: Crompton Co./CieInventors: Ewa M. Osika, Walter G. Brouwer
-
Patent number: 6933317Abstract: Compounds of the general formula (I) which are metabolically stable and have an antagonistic activity against PGD2 receptor: ? wherein Y is bicyclic ring; R1 is optionally substituted heteroaryl; R2 is hydrogen, etc.; R3 is —CH2—CH2—CH2—CH2—CH?CH—COOR4, —CH2—CH2—CH2—CH2—X1—CH2—COOR4, —CH2—CH?CH—CH2—X1—CH2—COOR4 or —CH2—CH2—CH2—COOR4; R4 is hydrogen, etc.; X1 is —O—, etc.Type: GrantFiled: October 26, 2001Date of Patent: August 23, 2005Assignee: Shionogi & Co. Ltd.Inventors: Norihiko Tanimoto, Yoshiharu Hiramatsu, Tsunetoshi Honma, Masanao Inagaki
-
Patent number: 6887869Abstract: The invention concerns novel mikanolide derivatives, their preparation method and their therapeutic uses, in particular as anti-cancer and anti-viral agents.Type: GrantFiled: January 11, 2002Date of Patent: May 3, 2005Assignee: Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S.)Inventors: Olivier Lavergne, Christophe Lanco, Grégoire Prevost, Beng Poon Teng
-
Patent number: 6878706Abstract: Compounds according to the following formula (I): wherein the variables Q and R1 to R6 are as described herein, which reversibly inhibit the cysteine proteases, such as cathepsins K, S, F, L and B; pharmaceutical compositions containing such compounds, and method of treating diseases and pathological conditions exacerbated by these cysteine proteases such as, but not limited to rheumatoid arthritis, multiple sclerosis and other autoimmune diseases, osteoporosis, asthma, Alzheimer's disease, atherosclerosis and endometriosis.Type: GrantFiled: March 27, 2003Date of Patent: April 12, 2005Assignee: Boehringer Ingelheim Pharmaceuticals Inc.Inventors: Thomas A. Gilmore, Eugene Richard Hickey, Weimin Liu, Peter Allen Nemoto, Denice M. Spero
-
Patent number: 6872730Abstract: The present invention relates to novel substituted benzofurans and benzothiophenes compounds that are antagonists of alpha V (?v) integrins, for example ?v?3 and ?v?5 integrins, their pharmaceutically acceptable salts, and pharmaceutical compositions thereof. The compounds may be used in the treatment of pathological conditions mediated by ?v?3 and ?v?5 integrins, including such conditions as tumor growth, metastasis, restenosis, osteoporosis, inflammation, macular degeneration, diabetic retinopathy, and rheumatoid arthritis. The compounds have the general formula I: where R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, m, n, i, j and k are defined herein.Type: GrantFiled: April 26, 2002Date of Patent: March 29, 2005Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Beth M. Anaclerio, Juan J. Marugan Sanchez, Victor J. Marder, David C. U'Prichard, Bruce E. Tomczuk
-
Patent number: 6869913Abstract: Novel pyridazin-3-one derivatives of formula [1] are provided, which are useful as active ingredients of herbicides, wherein R1 is haloalkyl; R2 and R3 are hydrogen, alkyl, haloalkyl, or alkoxyalkyl; and Q is [Q-1], [Q-2], [Q-3], [Q-4] or [Q-5]. Also provided are their use and intermediates for their production.Type: GrantFiled: February 9, 2004Date of Patent: March 22, 2005Assignee: Sumitomo Chemical Company, LimitedInventors: Tadashi Katayama, Shinichi Kawamura, Yuzuru Sanemitsu, Yoko Mine
-
Patent number: 6869972Abstract: The subject invention pertains to novel compounds (and salts thereof), and compositions comprising the compounds, for the treatment of cardiac arrhythmias. The subject invention further concerns methods of making the novel compounds. The novel compounds are rapidly metabolized analogs of amiodarone, having the distinct and advantageous characteristic of being metabolized to a less lipophilic compound. This results in an improved safety profile. The new compounds have particular utility for treating life-threatening ventricular tachyarrhythmias, especially in patients with congestive heart failure (CHF). The compounds also provide effective management for ventricular arrhythmias and supraventricular arrhythmias, including atrial fibrillation and re-entrant tachyarrhythmias involving accessory pathways.Type: GrantFiled: March 11, 2004Date of Patent: March 22, 2005Assignee: ARYx TherapeuticsInventor: Pascal Druzgala
-
Patent number: 6812243Abstract: The invention relates to tyrosine kinase inhibitors of the bis-indolyl compound type of the general formula I: pharmaceuticals containing them and their use for the treatment of malignant and other diseases based on pathological cell proliferation.Type: GrantFiled: May 3, 2002Date of Patent: November 2, 2004Assignee: Zentaris AGInventors: Siavosh Mahboobi, Sabine Kuhr, Herwig Pongratz, Alfred Popp, Harald Hufsky, Frank-D Bohmer, Steffen Teller, Andrea Uecker, Thomas Beckers
-
Publication number: 20040176437Abstract: The subject invention pertains to novel compounds (and salts thereof), and compositions comprising the compounds, for the treatment of cardiac arrhythmias. The subject invention further concerns methods of making the novel compounds. The novel compounds are rapidly metabolized analogs of amiodarone, having the distinct and advantageous characteristic of being metabolized to a less lipophilic compound. This results in an improved safety profile. The new compounds have particular utility for treating life-threatening ventricular tachyarrhythmias, especially in patients with congestive heart failure (CHF). The compounds also provide effective management for ventricular arrhythmias and supraventricular arrhythmias, including atrial fibrillation and re-entrant tachyarrhythmias involving accessory pathways.Type: ApplicationFiled: March 11, 2004Publication date: September 9, 2004Inventor: Pascal Druzgala
-
Publication number: 20040157841Abstract: Mono-acylated o-phenylendiamines derivatives of formula I 1Type: ApplicationFiled: February 3, 2004Publication date: August 12, 2004Inventors: Georg Fertig, Frank Herting, Manfred Kubbies, Anja Limberg, Ulrike Reiff, Michael Weidner
-
Publication number: 20040110692Abstract: This invention provides a class of therapeutic compounds and methods for the treatment of mammals with physiological disorders, such as for example a frequently occurring type of essential hypertension, which are critically associated with the decreased binding of magnesium to the plasma membranes of their cells. These methods consist of administering to a mammal in need of such treatment a compound selected from a series of disubstituted trans, trans 1,3-butadienes, 1,3-disubstituted perhydrobutadienes, 1,2-disubstituted trans ethylenes and 1,2 disubstituted ethanes and disubstituted propanes, each of which embodies, in common, the unique structural feature essential for the biological activity of these compounds. This invention also provides for pharmaceutical formulations that employ these novel compounds.Type: ApplicationFiled: October 28, 2003Publication date: June 10, 2004Applicant: Magnesium Diagnostics, Inc.Inventor: Ibert Clifton Wells
-
Patent number: 6723848Abstract: Process for the preparation of benzo-fused heterocycles of general formula I: in which X, R1, R2, R3, R4, R5 and n are as defined in claim 1, by reacting tetrahydrobenzo-fused heterocycles of formula II: in which X, R1, R2, R3, R4, R5, n and Ac are as defined in claim 1, with a catalytic amount of a noble metal catalyst in the presence of a hydrogen acceptor and then deacylating the acylated amino group by the addition of an amine.Type: GrantFiled: October 9, 2002Date of Patent: April 20, 2004Assignee: Merck Patent Gesellschaft mit Beschränkter HaftungInventors: Frank-Hardi Wartenberg, Thomas Koppe, Walter Wetzel, Markus Wydra, Achim Benz
-
Patent number: 6720423Abstract: Compounds of the formula where the variables have the meaning defined in the specification, are specific or selective agonists of RXR retinoid receptors.Type: GrantFiled: April 30, 2002Date of Patent: April 13, 2004Assignee: Allergan, Inc.Inventors: Jayasree Vasudevan, Dehua Huang, Vidyasagar Vuligonda, Roshanta S. Chandraratna
-
Patent number: 6713638Abstract: The present invention relates to a compound of formula (I): wherein: R3 is selected from the group consisting of 1-napthyl, 2-napthyl and cycloalkylphenyl; and R4 and R5 taken together form a ring having from 5 to 10 carbon atoms. Additionally, the invention provides a therapeutic method for preventing or treating a pathological condition or symptom in a mammal subject, such as a human, wherein increased angiogenesis is desired, comprising administering to a mammal in need of such therapy an effective amount of the aforementioned thiophene selective adenosine A1 allosteric enhancer.Type: GrantFiled: May 20, 2002Date of Patent: March 30, 2004Inventors: Joel M. Linden, Ray A. Ollson, Peter J. Scammells
-
Patent number: 6710070Abstract: The subject invention pertains to novel compounds (and salts thereof), and compositions comprising the compounds, for the treatment of cardiac arrhythmias. The subject invention further concerns methods of making the novel compounds. The novel compounds are rapidly metabolized analogs of amiodarone, having the distinct and advantageous characteristic of being metabolized to a less lipophilic compound. This results in an improved safety profile. The new compounds have particular utility for treating life-threatening ventricular tachyarrhythmias, especially in patients with congestive heart failure (CHF). The compounds also provide effective management for ventricular arrhythmias and supraventricular arrhythmias, including atrial fibrillation and re-entrant tachyarrhythmias involving accessory pathways.Type: GrantFiled: December 10, 2002Date of Patent: March 23, 2004Assignee: ARYx TherapeuticsInventor: Pascal Druzgala
-
Patent number: 6677369Abstract: This application relates to a compound of formula I (or a prodrug thereof or a pharmaceutically acceptable salt of the compound or prodrug thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.Type: GrantFiled: April 25, 2002Date of Patent: January 13, 2004Assignee: Eli Lilly and CompanyInventors: Douglas Wade Beight, Trelia Joyce Craft, Jeffry Bernard Franciskovich, Theodore Goodson, Jr., Steven Edward Hall, David Kent Herron, Valentine Joseph Klimkowski, John Joseph Masters, David Mendel, Guy Milot, Jason Scott Sawyer, Robert Theodore Shuman, Gerald Floyd Smith, Anne Louise Tebbe, Jennifer Marie Tinsley, Leonard Crayton Weir, James Howard Wikel, Michael Robert Wiley, Ying Kwong Yee
-
Publication number: 20030232988Abstract: Methods for making bis-heterocyclic compounds, especially bis-heterocyclic compounds having five and six-membered heterocyclic linkers are described. Also described are methods for making an alpha amino ketone synthon that enables facile syntheses of bisindole compounds, including topsentins and dragmacidins.Type: ApplicationFiled: December 5, 2002Publication date: December 18, 2003Inventors: David A. Horne, Kenichi Yakushijin
-
Publication number: 20030195226Abstract: The present invention relates to novel oxime carbamyl derivatives and pharmaceutical compositions comprising said derivatives which inhibit fatty acid amide hydrolase. These pharmaceutical compositions are useful for the treatment of conditions which can be effected by inhibiting fatty acid amide hydrolase including, but not limited to, neuropathic pain, emesis, anxiety, altering feeding behaviors, movement disorders, glaucoma, brain injury, and cardiovascular disease.Type: ApplicationFiled: February 4, 2003Publication date: October 16, 2003Inventors: Sing-Yuen Sit, Kai Xie, Hongfeng Deng
-
Publication number: 20030187053Abstract: The invention relates to triamide MTP/ApoB inhibitors of the formula 1 1Type: ApplicationFiled: June 20, 2002Publication date: October 2, 2003Applicant: Pfizer Inc.Inventors: Peter Bertinato, Alan E. Blize, Brian S. Bronk, Hengmiao Cheng, Jin Li, Hiep Huatan, Clive Mason
-
Publication number: 20030134880Abstract: Compounds of formula (I) wherein R is hydrogen, alkyl, alkenyl, alkynyl, aryl, heteroaryl or heterocyclyl; R1 is bicyclyl or heterobicyclyl; R2 is aryl, heteroaryl, heterocyclyl, alkoxy, alkyl, hydroxy or optionally substituted amino and n is from 0 to 3; with the provisos than when n is 0 R2 is alkyl or when n is from 1 to 3 R2 is not alkyl, are useful in the treatment and prophylaxis of conditions mediated by CD23 or TNF.Type: ApplicationFiled: October 25, 2002Publication date: July 17, 2003Inventors: Gordon Bruton, Barry Sidney Orlek, Kishore Kalidas Rana
-
Patent number: 6555697Abstract: The invention concerns a novel method for preparing a benzofuran or benzothiophene compound by cyclizing an aromatic compound bearing a side-chain comprising at least two carbon atoms, one of the carbon atoms being bound to the benzene cycle by an oxygen or sulphur atom, the other carbon atom is in carboxylic form and a formyl radical in ortho position relative to said chain. The inventive method is characterised in that it consists in cyclizing the latter in the presence of an efficient amount of a carbonate base in a medium comprising a carboxylic acid anhydride and optionally an organic solvent.Type: GrantFiled: April 11, 2002Date of Patent: April 29, 2003Assignee: Rhodia ChimieInventor: Thierry Schlama
-
Patent number: 6518291Abstract: The present invention relates to a novel class of compounds which are IMPDH inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting IMPDH enzyme activity and consequently, may be advantageously used as therapeutic agents for IMPDH mediated processes. This invention also relates to methods for inhibiting the activity of IMPDH using the compounds of this invention and related compounds.Type: GrantFiled: September 14, 1999Date of Patent: February 11, 2003Assignee: Vertex Pharmaceuticals, IncorporatedInventors: Jeffrey O. Saunders, David M. Armistead, Michael C. Badia, Randy S. Bethiel, Catherine A. Frank, Doug Naegele, Perry M. Novak, David A. Pearlman, Steven M. Ronkin
-
Patent number: 6509369Abstract: This invention relates to anti-inflammatory compounds, methods of making such compounds and methods of using such compounds having the following structure:Type: GrantFiled: January 8, 2002Date of Patent: January 21, 2003Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Malcolm K. Scott, Pauline J. Sanfilippo, Louis J. Fitzpatrick, III, Richard Cordova, Kevin Pan, Joseph Meschino
-
Patent number: 6506780Abstract: This invention relates to a series of substituted benzophenone and sulfone compounds of the formula I wherein ring A, Z, Y, R and X are defined as in the specification, that exhibit activity as glycine transport inhibitors, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, and their use for the enhancement of cognition and the treatment of the positive and negative symptoms of schizophrenia and other psychoses in mammals, including humans.Type: GrantFiled: July 2, 2001Date of Patent: January 14, 2003Assignee: Pfizer Inc.Inventor: John A. Lowe, III
-
Patent number: 6492390Abstract: A class of benzopyrans, benzothiopyrans, dihydroquinolines, dihydronaphthalenes, and analogs thereof, is described for use in treating cyclooxygenase-2 mediated disorders. Compounds of particular interest are defined by Formula I′ wherein X, A1, A2, A3, A4, R, R″, R1 and R2 are as described in the specification.Type: GrantFiled: May 24, 2001Date of Patent: December 10, 2002Assignee: G.D. Searle & Co.Inventors: Jeffery S Carter, Mark G Obukowicz, Balekudru Devadas, John J Talley, David L Brown, Matthew J Graneto, Stephen R Bertenshaw, Donald J Rogier, Jr., Srinivasan Raj Nagarajan, Cathleen E Hanau, Susan J Hartmann, Cindy L Ludwig, Suzanne Metz, Donald E Korte
-
Publication number: 20020173645Abstract: The present invention is directed to chemical processes for preparing 2-aryl-6-hydroxy-3-[4-(2-aminoethoxy)benzoyl]benzo[b]-thiophenes. The present invention is also directed to crystalline solvates and a non-solvated crystalline form of 6-hydroxy-2-(4-hydroxyphenyl)-3-[4-(2-piperidinoethoxy)benzoyl]-benzo[b]thiophene hydrochloride, as well as processes for their preparation.Type: ApplicationFiled: February 26, 2002Publication date: November 21, 2002Inventor: Wayne Douglas Luke
-
Patent number: 6479604Abstract: A diarylethene compound of the following formula (1) wherein R1 is a hydrogen or a substituted or unsubstituted C1-22 alkyl group, a fluoro group, a substituted or unsubstituted phenyl group, a substituted or unsubstituted phenylalkyl group, R2 is a C1-22 alkylene group which may be unsubstituted or substituted with fluorine, R3 is a chemical bond, O, S, NR1, N(R2R1), or a C1-3 alkylene group which may be unsubstituted or substituted with one or more oxygen atoms or fluorine atoms, X and Y independently of one another O, S, nitrogen, NR1, or N(R2R1), and Z is a carbonyl group or a methylene group which may be unsubstituted or substituted with fluorine.Type: GrantFiled: January 27, 2000Date of Patent: November 12, 2002Assignee: Korea Research Institute of Chemical TechnologyInventors: Eun-Kyoung Kim, Yun-Ki Choi
-
Publication number: 20020161242Abstract: A process for preparing a compound having PGD2 antagonism represented by the formula (I), or a pharmaceutically acceptable salt or hydrate thereof, which process comprises reacting an amino alcohol of the formula (II) or its salt with a compound of the formula (III) or its reactive derivative, oxidizing the product with halo oxoacid in the presence of 2,2,6,6-tetramethylpiperidine-1-oxyls, reacting the product with an ylide under the conditions for Wittig reaction, and optionally deprotecting the product.Type: ApplicationFiled: April 29, 2002Publication date: October 31, 2002Inventors: Tsunetoshi Honma, Yoshiharu Hiramatsu
-
Publication number: 20020156297Abstract: A process for preparing a compound having PGD2 antagonism represented by the formula (I), or a pharmaceutically acceptable salt or hydrate thereof, which process comprises reacting an amino alcohol of the formula (II) or its salt with a compound of the formula (III) or its reactive derivative, oxidizing the product with halo oxoacid in the presence of 2,2,6,6-tetramethylpiperidine-1-oxyls, reacting the product with an ylide under the conditions for Wittig reaction, and optionally deprotecting the product.Type: ApplicationFiled: April 29, 2002Publication date: October 24, 2002Inventors: Tetsuo Okada, Makoto Kakinuma
-
Patent number: 6465662Abstract: A process for preparing a compound having PGD2 antagonism represented by the formula (I), or a pharmaceutically acceptable salt or hydrate thereof, which process comprises reacting an amino alcohol of the formula (II) or its salt with a compound of the formula (III) or its reactive derivative, oxidizing the product with halo oxoacid in the presence of 2,2,6,6-tetramethylpiperidine-1-oxyls, reacting the product with an ylide under the conditions for Wittig reaction, and optionally deprotecting the product.Type: GrantFiled: April 29, 2002Date of Patent: October 15, 2002Assignee: Shionogi & Co., Ltd.Inventors: Tsunetoshi Honma, Yoshiharu Hiramatsu
-
Patent number: 6465508Abstract: Ortho-sulfonamido aryl hydroxamic acids are provided which are useful, inter alia, for the inhibition of matrix metalloproteinases and the treatment of conditions associated with overexpression of MMPs.Type: GrantFiled: February 23, 2001Date of Patent: October 15, 2002Assignee: WyethInventors: Frances Christy Nelson, Arie Zask, James Ming Chen, Dominick Mobilio, Ramaswamy Nilakantan
-
Patent number: 6455684Abstract: A method for analyzing an objective substance, comprising reacting a labeled probe with an objective substance on a biological sample, said probe comprising a label substance of the formula (I): wherein A1 is an aromatic group, R1 is a hydrogen or —COCH2COCnF2n+1 and n is an integer of 1-6, which is bonded to a probe selected from the group consisting of nucleic acid, nucleic acid binding protein, low molecular ligand and receptor for ligand (except antibody) to give a fluorescent complex, reacting the complex with an objective substance on a biological sample and assaying fluorescence of the resultant fluorescent complex, a labeled nucleic acid probe and a labeled nucleotide. According to the method of the present invention, defects such as hindrance of fluorescence due to contaminant substance, low sensitivity and the like can be resolved, thereby enabling analysis on a tissue.Type: GrantFiled: September 28, 2001Date of Patent: September 24, 2002Assignees: Toyo Boseki Kabushiki KaishaInventors: Kazuhiro Matsui, Katsunori Ikeda, Shinichi Teshima, Yoshihisa Kawamura, Kazuko Matsumoto
-
Patent number: 6441196Abstract: Novel processes and intermediates useful in the preparation of 11-oxa prostaglandin analogs are disclosed.Type: GrantFiled: May 18, 2001Date of Patent: August 27, 2002Assignee: Alcon, Inc.Inventors: Pete Delgado, Raymond E. Conrow, William D. Dean, Michael S. Gaines
-
Publication number: 20020115871Abstract: A process for preparing a compound having PGD2 antagonism represented by the formula (I), or a pharmaceutically acceptable salt or hydrate thereof, which process comprises reacting an amino alcohol of the formula (II) or its salt with a compound of the formula (III) or its reactive derivative, oxidizing the product with halo oxoacid in the presence of 2,2,6,6-tetramethylpiperidine-1-oxyls, reacting the product with an ylide under the conditions for Wittig reaction, and optionally deprotecting the product.Type: ApplicationFiled: April 29, 2002Publication date: August 22, 2002Inventors: Tetsuo Okada, Makoto Kakinuma
-
Publication number: 20020107280Abstract: This invention relates to compounds, which are generally anti-inflammatory and analgesic compounds, and which are represented by Formula I: 1Type: ApplicationFiled: December 3, 2001Publication date: August 8, 2002Inventors: Kevin L. McLaren, David Bernard Smith, Jahari Laurant Tracy
-
Patent number: 6429317Abstract: The present invention provides novel indane-like compounds which can be useful for treating psychosis and other conditions associated with the modulation of a muscarinic receptor. The invention provides formulations and methods for using the novel compounds.Type: GrantFiled: September 5, 2000Date of Patent: August 6, 2002Assignee: Eli Lilly and CompanyInventors: Sean P. Hollinshead, Michael A. Staszak, John S. Ward, Joseph W. Wilson, Bret E. Huff, Philip F. Hughes, Jose S. Mendoza, Charles H. Mitch
-
Patent number: 6407102Abstract: The invention relates to tyrosine kinase inhibitors of the bis-indolyl compound type of the general formula I: pharmaceuticals containing them and their use for the treatment of malignant and other diseases based on pathological cell proliferation.Type: GrantFiled: May 4, 1999Date of Patent: June 18, 2002Assignee: Zentaris AGInventors: Siavosh Mahboobi, Sabine Kuhr, Herwig Pongratz, Alfred Popp, Harald Hufsky, Frank-D Bohmer, Steffen Teller, Andrea Uecker, Thomas Beckers
-
Patent number: 6399778Abstract: The present invention is directed to chemical processes for preparing 2-aryl-6-hydroxy-3-[4-(2-aminoethoxy)benzoyl]benzo[b]-thiophenes. The present invention is also directed to crystalline solvates and a non-solvated crystalline form of 6-hydroxy-2-(4-hydroxyphenyl)-3-[4-(2-piperidinoethoxy)benzoyl]-benzo[b]thiophene hydrochloride, as well as processes for their preparation.Type: GrantFiled: June 6, 1995Date of Patent: June 4, 2002Assignee: Eli Lilly and CompanyInventors: Elizabeth Smith LaBell, John McNeill McGill, Randal Scot Miller
-
Patent number: 6380221Abstract: This invention is directed to compounds of formula (III): wherein B, C, D, E, R1, R2 and R3 are disclosed herein. These components are disclosed as being useful as anti-coagulants.Type: GrantFiled: August 3, 2000Date of Patent: April 30, 2002Assignee: Berlex Laboratories, Inc.Inventors: Damian O. Arnaiz, Yuo-Ling Chou, Brian D. Griedel, Rushad E. Karanjawala, Monica J. Kochanny, Wheeseong Lee, Amy Mei Liang, Michael M. Morrissey, Gary B. Phillips, Karna Lyn Sacchi, Steven T. Sakata, Kenneth J. Shaw, R. Michael Snider, Shung C. Wu, Bin Ye, Zuchun Zhao
-
Patent number: 6372779Abstract: This invention relates to anti-inflammatory compounds, methods of making such compounds and methods of using such compounds having the following structure:Type: GrantFiled: December 28, 1998Date of Patent: April 16, 2002Assignee: Ortho Pharmaceutical CorporationInventors: Malcolm K. Scott, Pauline J. Sanfilippo, Louis J. Fitzpatrick, III, Richard Cordova, Kevin Pan, Joseph Meschino
-
Patent number: 6362216Abstract: The present invention is directed to compounds which are capable of inhibiting the activity of tryptase. Such compounds are useful in the treatment or prevention of inflammatory disease, particularly those disease states which are mediated by mast cell activation. Also encompassed by the invention are formulations comprising the noted compounds, processes for preparing such compounds and methods for treating or preventing an inflammatory disease.Type: GrantFiled: May 3, 2000Date of Patent: March 26, 2002Assignee: Array Biopharma Inc.Inventors: Laurence E. Burgess, James P. Rizzi
-
Patent number: 6353014Abstract: A method of treating glaucoma or ocular hypertension in a patient, which comprises administering to the patient a pharmaceutically effective amount of a compound of formula I:Type: GrantFiled: June 2, 1999Date of Patent: March 5, 2002Assignee: Alcon Laboratories, Inc.Inventors: Verney L. Sallee, Mark R. Hellberg, Peter G. Klimko
-
Publication number: 20020026061Abstract: Benzothiophenecarboxylic acid derivatives of the formula (I) which are useful as starting materials for producing drugs, and a process for preparing 5-hydroxybenzo[b]-thiophene-3-carboxylic acid derivatives of the formula (VI) which are specific PGD2 antagonists.Type: ApplicationFiled: September 26, 2001Publication date: February 28, 2002Inventors: Tsunetoshi Honma, Yoshiharu Hiramatsu
-
Patent number: 6350884Abstract: This invention is directed to a class of acrylic and propionic acid compounds and their use in the treatment of post-menopausal symptoms and restenosis. In other embodiments, the invention is directed to intermediates and to processes for the preparation of the acrylic and propionic acid compounds.Type: GrantFiled: September 30, 1997Date of Patent: February 26, 2002Assignee: Eli Lilly and CompanyInventors: Charles David Jones, Alan David Palkowitz, Kenneth Jeff Thrasher