Plural Ring Chalcogens In The Polycyclo Ring Sytem (e.g., Methylenedioxyphenyl Containing, Etc.) Patents (Class 548/526)
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Patent number: 6380241Abstract: A compound of the formula (I): or a pharmaceutically acceptable salt thereof is disclosed, as well as processes for and intermediates in the preparation thereof, and a method of antagonizing endothelin.Type: GrantFiled: November 17, 2000Date of Patent: April 30, 2002Assignee: Abbott LaboratoriesInventors: Martin Winn, Steven A. Boyd, Charles W. Hutchins, Hwan-Soo Jae, Andrew S. Tasker, Thomas W. von Geldern, Jeffrey A. Kester, Bryan K. Sorensen, Bruce G. Szczepankiewicz, Kenneth J. Henry, Gang Liu, Steven J. Wittenberger, Steven A. King
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Patent number: 6376538Abstract: The present invention relates to novel compounds that are useful for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. This invention also relates to pharmaceutical formulations comprising these compounds and methods of using them for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. The compounds and pharmaceutical compositions of this invention can be used as therapeutic or prophylactic agents. They are particularly well-suited for treatment of many inflammatory and autoimmune diseases.Type: GrantFiled: September 19, 1997Date of Patent: April 23, 2002Assignee: Biogen, Inc.Inventors: Steven P. Adams, Ko-Chung Lin, Wen-Cherng Lee, Alfredo C. Castro, Craig N. Zimmerman, Charles E. Hammond, Yu-Sheng Liao, Julio Hernan Cuervo, Juswinder Singh
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Patent number: 6355672Abstract: The invention provides compounds of the formula: wherein the ring A is an optionally substituted benzene ring; R1 is an optionally substituted non-aromatic heterocyclic group; R2 and R3 are independently hydrogen atom or an optionally substituted hydrocarbon group; n is an integer of 0-3; or salts thereof, which are useful as medicines having an osteogenesis promoting effect and chondrogensis promoting effect. The present invention relates to an amine compound having an excellent effect of inhibiting production and/or secretion of amyloid-b protein, a production and use thereof. Especially, it is effective for preventing and/or treating, for example, neurodegenerative diseases, amyloid angiopathy, neurological disorders caused by cerebrovascular disorders, and so forth.Type: GrantFiled: January 30, 2001Date of Patent: March 12, 2002Assignee: Takeda Chemical Industries, Ltd.Inventors: Tsuneo Yasuma, Haruhiko Makino, Akira Mori
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Patent number: 6355441Abstract: Chemiluminescent 1,2-dioxetane compounds capable of producing light energy when decomposed, substantially stable at room temperature, represented by the formulas I or II:Type: GrantFiled: July 28, 1999Date of Patent: March 12, 2002
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Patent number: 6342517Abstract: Novel thienopyran compounds are disclosed, useful as anti-hypertensive agents and for asthma treatment. One group of the compounds has a heterocyclic ring spiro-connected at the 7-position of the thienopyran ring structure. Use of thienopyran compounds in hair growth modulation is described.Type: GrantFiled: December 3, 1999Date of Patent: January 29, 2002Assignee: Cambridge Bioclinical LimitedInventors: Peter Esch, Franz Rovenszky, Robertson Towart, Thomas Christoph, Michael Hartmann, George Terence Evelyn Kealey
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Patent number: 6340704Abstract: The present invention provides a compound represented by the formula: wherein R1 is an amino group which may be substituted; R2 is a hydrogen atom or a lower alkyl group which may be substituted; X is a methyne group which may be substituted or N(O)m (m is 0 or 1); a ring A is a homo- or hetero-cycle which is substituted by a halogen atom, lower alkyl, lower alkoxy or lower alkylenedioxy; and a ring B is a homo- or hetero-cycle which may be substituted; or a salt thereof, which exhibits excellent cell differentiation-inducing action and cell differentiation-inducing factor action-enhancing action, and is useful in the treatment and prevention of various nerve diseases or bone/joint diseases.Type: GrantFiled: July 19, 1999Date of Patent: January 22, 2002Assignee: Takeda Chemical Industries, Ltd.Inventors: Shogo Marui, Masatoshi Hazama, Kohei Notoya, Koki Kato
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Patent number: 6337343Abstract: There is provided amino acid derivatives of formula I, wherein p, q, R1, R2, R3, R4, Y, n and B have meanings given in the description which are useful as competitive inhibitors of trypsin-like proteases, such as thrombin, and in particular in the treatment of conditions where inhibition of thrombin is required (e.g. thrombosis) or as anticoagulants.Type: GrantFiled: March 29, 2000Date of Patent: January 8, 2002Assignee: AstraZeneca ABInventors: David Gustafsson, Jan-Erik Nyström
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Patent number: 6319946Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.Type: GrantFiled: February 9, 2000Date of Patent: November 20, 2001Assignee: Vertex Pharmaceuticals IncorporatedInventors: Michael R. Hale, Christopher T. Baker, Timothy A. Stammers, Ronald George Sherrill, Andrew Spaltenstein, Eric Steven Furfine, Francois Maltais, Clarence Webster Andrews, III, John Franklin Miller, Vicente Samano
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Publication number: 20010041796Abstract: The present invention relates to a novel taxol derivative having an antitumor-activity which is represented by formula (1).Type: ApplicationFiled: January 16, 2001Publication date: November 15, 2001Inventors: Hirofumi Terasawa, Tsunehiko Soga, Takashi Ishiyma
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Patent number: 6310080Abstract: Selected amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically inhibiting retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.Type: GrantFiled: December 1, 1999Date of Patent: October 30, 2001Assignee: G. D. Searle & Co.Inventors: Daniel P Getman, Gary A. DeCrescenzo, John N. Freskos, Michael L. Vazquez, James A. Sikorski, Balekudru Devadas, Srinivasan Nagarajan, David L. Brown, Joseph J. McDonald
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Patent number: 6281229Abstract: A disease treatment is provided by controlling the expression of a protein induced by a heat shock factor. The novel compound benzo-1,3-dioxole provides an inhibitor of HSF activity or an inhibitor of inducing the production of a protein regulated by HSF, which inhibits the activity of a heat shock factor, a transcriptional regulatory factor, thereby in turn inhibiting transcription of a structural gene having a heat shock element sequence in the gene region for transcriptional regulation into RNA, and thus inhibiting translation of the gene into a protein, and resulting in inhibition of inducing production of RNA or protein encoded by the gene. It also provides a drug for treating or preventing cancer through thermotherapy and a drug for treating or preventing stress diseases such as depression.Type: GrantFiled: March 27, 2000Date of Patent: August 28, 2001Assignee: Kaneka CorporationInventors: Shin-ichi Yokota, Kozo Yamamoto, Souichi Morikawa, Yoshihide Fuse, Mikio Kitahara
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Patent number: 6258954Abstract: The present invention relates to compounds of formula I provided that R1 and R2 not simultaneously stand for phenyl, the use thereof in, for example, electroluminescent devices and as void detection compounds.Type: GrantFiled: August 22, 2000Date of Patent: July 10, 2001Assignee: Ciba Specialty Chemicals Corp.Inventors: Kazuhiko Kunimoto, Junji Otani, Kunihiko Kodama, Hiroshi Yamamoto, Patrick Verhoustraeten, Sonia Megert, Adalbert Braig
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Patent number: 6255336Abstract: Novel amino ceramide-like compounds are provided which inhibit glucosyl ceramide (GlcCer) formation by inhibiting the enzyme GlcCer synthase, thereby lowering the level of glycosphingolipids. The compounds of the present invention have improved GlcCer synthase inhibition activity and are therefore highly useful in therapeutic methods for treating various conditions and diseases associated with altered glycosphingolipid levels.Type: GrantFiled: July 9, 1999Date of Patent: July 3, 2001Assignee: The Regents of the University of MichiganInventors: James A. Shayman, Norman S. Radin
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Patent number: 6214861Abstract: Selected heterocycle carbonyl amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.Type: GrantFiled: February 9, 2000Date of Patent: April 10, 2001Assignee: G.D. Searle & Co.Inventors: Daniel P Getman, Gary A DeCrescenzo, John N Freskos, Michael L Vazquez, James A Sikorski, Balekudru Devadas, Srinivasan Nagarajan, David L Brown, Joseph J McDonald
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Patent number: 6211225Abstract: There is provided a novel series of heterocyclic aminopyrrolidine compounds of Formula I wherein R1, R2, R3, R4, W, Z and the wavy bond are as defined herein which bind to the human melatonin receptor and therefore are useful as melatonergic agents.Type: GrantFiled: June 6, 2000Date of Patent: April 3, 2001Assignee: Bristol-Meyers SquibbInventors: Katherine S. Takaki, Guanglin Luo, Stephen R. Bertenshaw
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Patent number: 6211363Abstract: The present invention relates to a novel taxol derivative having an antitumor-activity which is represented by formula (1). [In the formula (I), R1: a phenyl group, R2: an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group or an alkoxyl group, R3: a hydrogen atom, a hydroxyl group, a halogen atom, an alkoxyl group, a group —O—R31, an acyloxy group or a group —O—CO—R31, (in which R31: an alkylamino group, an alkenyl group, an alkynyl group, a cycloalkyl group, an aryl group or a heterocyclic group), R4 and R5: a hydrogen atom, an alkyl group, an alkenyl group, an alkynyl group, an aryl group or a heterocyclic group, Z1: a hydrogen atom, a hydroxyl group, a halogen atom or an alkyl group, Z2: a hydrogen atom, a hydroxyl group, a halogen atom or an alkyl group, Z3: an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, an aryl group or a heterocyclic group].Type: GrantFiled: February 25, 2000Date of Patent: April 3, 2001Assignee: Daiichi Pharamaceutical Co., Ltd.Inventors: Hirofumi Terasawa, Tsunehiko Soga, Takashi Ishiyama
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Patent number: 6172101Abstract: Selected heterocyclecarbonyl amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.Type: GrantFiled: April 23, 1998Date of Patent: January 9, 2001Assignee: G. D. Searle & Co.Inventors: Daniel P. Getman, Gary A. De Crescenzo, John N. Freskos, Michael L. Vazquez, James A. Sikorski, Balekudru Deyadas, Srinivasan Nagarajan, David L. Brown, Joseph J. McDonald
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Patent number: 6166015Abstract: This invention relates to certain 3-aminomethylpyrrolidine derivatives of Formula (I): ##STR1## that are CCR-3 receptor antagonists, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.Type: GrantFiled: November 18, 1999Date of Patent: December 26, 2000Assignee: Syntex (U.S.A.) Inc.Inventors: Daniel Harry Rogers, John Saunders, John Patrick Williams
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Patent number: 6162927Abstract: A compound of the formula (I): ##STR1## or a pharmaceutically acceptable salt thereof is disclosed, as well as processes for and intermediates in the preparation thereof, and a method of antagonizing endothelin.Type: GrantFiled: August 4, 1997Date of Patent: December 19, 2000Assignee: Abbott LaboratoriesInventors: Martin Winn, Steven A. Boyd, Charles W. Hutchins, Hwan-Soo Jae, Andrew S. Tasker, Thomas W. von Geldern, Jeffrey A. Kester, Bryan K. Sorensen, Bruce G. Szczepankiewicz, Kenneth J. Henry, Gang Liu, Steven J. Wittenberger, Steven A. King
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Patent number: 6149841Abstract: Described are novel photochromic benzopyrano-fused naphthopyran compounds, examples of which are naphthopyran compounds having a substituted or unsubstituted benzopyran group fused to one side of the naphtho portion of the naphthopyran and having certain substituents at the position ortho to the oxygen atom of the naphthopyran ring. These compounds may be represented by the following: ##STR1## Also described are polymeric organic host materials that contain or that are coated with such compounds or combinations thereof with complementary photochromic compounds, e.g., certain other naphthopyrans, benzopyrans, and spiro(indoline)type compounds.Type: GrantFiled: December 17, 1999Date of Patent: November 21, 2000Assignee: PPG Industries Ohio, Inc.Inventor: Anil Kumar
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Patent number: 6146554Abstract: What is described here are photochromic naphthopyrane dyes with different substituents whose properties can be set by controlled selection of the substituents. In this manner it is possible to take an influence on the migration characteristics, the absorption characteristics and the brightening rate and kinetics. The inventive compounds display good darkening and brightening properties at a very good service life.The invention excels itself by the fact that a method is made available which is substantially improved over prior art, in addition to the surprising influence on specific properties of the inventive compounds. The described compounds are suitable for application in synthetic materials of any kind.A photochromic object is also the subject matter of the invention, which comprises one or several photochromic naphthopyrane dyes as well as at least one polymer material, with the photochromic object being producible by mass-dyeing or superficial dyeing.Type: GrantFiled: May 21, 1999Date of Patent: November 14, 2000Assignee: Optische Werke G. RodenstockInventors: Manfred Melzig, Claudia Mann, Udo Weigand
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Patent number: 6143747Abstract: Bis-sulfonamido hydroxyethylamino compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to retroviral protease inhibiting compounds of the formula: ##STR1## or a pharmaceutically acceptable salt, prodrug or ester thereof, wherein the variables are as defined herein.Type: GrantFiled: February 26, 1998Date of Patent: November 7, 2000Assignee: G. D. Searle & Co.Inventors: John N. Freskos, Daniel P. Getman, John J. Talley, James A. Sikorski
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Patent number: 6140321Abstract: Donepezil hydrochloride, 1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride, is provided here in the form of four polymorphs which are stable against heat and humidity in the pharmaceutical use. They can be industrially produced. They are specified by peaks in X-ray powder diffraction pattern and absorption peaks in infrared absorption spectra in potassium bromide.Type: GrantFiled: December 30, 1996Date of Patent: October 31, 2000Assignee: Eisai Co., Ltd.Inventors: Akio Imai, Hideaki Watanabe, Takashi Kajima, Yasushi Ishihama, Akiyo Ohtsuka, Tomohide Tanaka
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Patent number: 6136847Abstract: Biologically-active, water soluble, 3-substituted trioxanes of the formula ##STR1## wherein R represents a COOH-- substituted aryl group, a substituted or unsubstituted heteroaryl group or an alkyl group, and C.sub.12 -(p-carboxy)benzyloxy trioxanes of formula ##STR2## wherein R represents a substituted or unsubstituted alkyl, alkenyl, aryl or heteroaryl group and methods for their use as antiparasitic agents, particularly for the treatment of malaria.Type: GrantFiled: April 7, 1999Date of Patent: October 24, 2000Assignee: Johns Hopkins UniversityInventors: Gary H. Posner, Michael H. Parker, Mikhail Krasavin, Theresa A. Shapiro
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Patent number: 6133455Abstract: There is provided a process for the preparation of 2-aryl-5-(perfluoroalkyl)pyrrole compounds from N-(arylmethylene)-1-chloro-1-(perfluoroalkyl)methylamine compounds. The 2-aryl-5-(perfluoroalkyl)pyrrole compounds are useful for the control of insect and acarid pests, and may also be used to prepare other pesticidal arylpyrrole compounds.In addition, the present invention provides N-(arylmethylene)-1-chloro-1-(perfluoroalkyl)methylamine compounds which are useful as intermediates in the preparation of arylpyrrole compounds.Type: GrantFiled: February 9, 1999Date of Patent: October 17, 2000Assignee: American Cyanamid CompanyInventor: Venkataraman Kameswaran
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Patent number: 6133263Abstract: Novel nonpeptide endothelin antagonists with ether-linked groups are described, as well as methods for the preparation and pharmaceutical compositions of the same, which are useful in treating atherosclerosis, restenosis, Raynaud's phenomenon, mild or severe congestive heart failure, cerebral ischemia, cerebral infarction, embolic stroke, cerebral vasospasm, subarachnoid hemorrhage, hemorrhagic stroke, diabetes, gastric ulceration and mucosal damage, ischemnic bowel disease, Chrohn's disease, essential or malignant hypertension, pulmonary hypertension, pulmonary hypertension after bypass, acute respiratory distress syndrome, chronic obstructive pulmonary diseases, male penile erectile dysfunction, cancer, especially malignant hemangicendothelioma or prostate cancer, myocardial infarction or ischemia, acute or chronic renal failure, renal ischemia, radiocontrast-induced nepbrotoxicity, endotoxic, septic, hemorrhagic shock, angina, preeclampsia, asthma, arhythmias, benign prostatic hyperplasia, and elevated levType: GrantFiled: August 3, 1998Date of Patent: October 17, 2000Assignee: Warner-Lambert CompanyInventors: Xue-Min Cheng, Annette Marian Doherty, William Chester Patt, Joseph Thomas Repine
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Patent number: 6124341Abstract: A compound of the formula (I): ##STR1## or a pharmaceutically acceptable salt thereof is disclosed, as well as processes for and intermediates in the preparation thereof, and a method of antagonizing endothelin.Type: GrantFiled: May 29, 1998Date of Patent: September 26, 2000Assignee: Abbott LaboratoriesInventors: Andrew S. Tasker, Martin Winn, Steven A. Boyd, Hwan-Soo Jae, Thomas W. von Geldern, Bryan K. Sorensen, Kenneth J. Henry
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Patent number: 6110956Abstract: Compounds effective in treating disorders of the serotonin-affected neurological systems are provided, such compounds having the following formula: ##STR1## wherein: R.sub.1 and R.sub.2 are each, independently, hydrogen, halogen, CF.sub.3, lower alkyl, lower alkoxy, MeSO.sub.2, or together can form a 5-7 membered carbocyclic or heterocyclic ring;R.sub.3 is alkoxy, halogen, hydrogen or carbamoyl;R.sub.4 is hydrogen, hydroxy, lower alkyl, or lower alkoxy;R.sub.5 is hydrogen, lower alkyl, or halogen;R.sub.6 is hydrogen, lower alkyl, or phenyl;R.sub.7 is hydrogen, lower alkyl, lower alkoxy, halogen, CN, CF.sub.3, or hydroxy; andX is (CH.sub.2).sub.n,wherein n is 0 to 3; or pharmaceutically acceptable salts thereof.Type: GrantFiled: April 7, 1999Date of Patent: August 29, 2000Assignee: American Home Products Corp.Inventors: Richard E. Mewshaw, Dahui Zhou, Ping Zhou
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Patent number: 6075140Abstract: The present invention relates to a novel taxol derivative having an antitumor activity which is represented by formula (1). ##STR1## [In the formula (I), R.sup.1 : a phenyl group, R.sup.2 : an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group or an alkoxyl group, R.sup.3 : a hydrogen atom, a hydroxyl group, a halogen atom, an alkoxyl group, a group --O--R.sup.31, an acyloxy group or a group --O--CO--R.sup.31, (in which R.sup.31 : an alkylamino group, an alkenyl group, an alkynyl group, a cycloalkyl group, an aryl group or a heterocyclic group), R.sup.4 and R.sup.5 : a hydrogen atom, an alkyl group, an alkenyl group, an alkynyl group, an aryl group or a heterocyclic group, Z.sup.1 : a hydrogen atom, a hydroxyl group, a halogen atom or an alkyl group, Z.sup.2 : a hydrogen atom, a hydroxyl group, a halogen atom or an alkyl group, Z.sup.3 : an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, an aryl group or a heterocyclic group].Type: GrantFiled: February 5, 1998Date of Patent: June 13, 2000Assignee: Daiichi Pharmaceutical Co., Ltd.Inventors: Hirofumi Terasawa, Tsunehiko Soga, Takashi Ishiyama
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Patent number: 6063795Abstract: Selected heterocyclecarbonyl amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.Type: GrantFiled: May 10, 1999Date of Patent: May 16, 2000Assignee: G.D. Searle & CompanyInventors: Daniel P Getman, Gary A DeCrescenzo, John N Freskos, Michael L Vazquez, James A Sikorski, Balekudru Devadas, Srinivasan Nagarajan, David L Brown, Joseph J McDonald
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Patent number: 6057441Abstract: This invention concerns the compounds of formula (I), ##STR1## the N-oxide forms, the pharmaceutically acceptable addition salts and the stereoisomeric forms thereof, wherein n is zero to 6; p and q are zero to 4; r is zero to 5; R.sup.1 and R.sup.2 each independently are hydrogen; optionally substituted C.sub.1-6 alkyl; C.sub.1-6 alkylcarbonyl; halomethylcarbonyl; or R.sup.1 and R.sup.2 taken together with the nitrogen atom to which they are attached may form a morpholinyl ring or an optionally substituted heterocycle; each R.sup.3 and R.sup.4 independently are halo, cyano, hydroxy, halomethyl, halomethoxy, carboxyl, nitro, amino, mono- or di(C.sub.1-6 alkyl)amino, C.sub.1-6 alkylcarbonylamino, aminosulfonyl, mono- or di(C.sub.1-6 alkyl)aminosulfonyl, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, C.sub.1-6 alkylcarbonyl, C.sub.1-6 alkyloxycarbonyl; each R.sup.5 independently is C.sub.1-6 alkyl, cyano or halomethyl; X is CR.sup.6 R.sup.7, NR.sup.8, O, S, S(.dbd.O) or S(.dbd.O).sub.Type: GrantFiled: October 6, 1998Date of Patent: May 2, 2000Assignee: Janssen Pharmaceutica, N.V.Inventors: Pilar Gil-Lopetegui, Francisco Javier Fernandez-Gadea, Theo Frans Meert
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Patent number: 6022495Abstract: Described are novel photochromic benzopyrano-fused naphthopyran compounds, examples of which are naphthopyran compounds having a substituted or unsubstituted benzopyran group fused to one side of the naphtho portion of the naphthopyran and having certain substituents at the position ortho to the oxygen atom of the naphthopyran ring. These compounds may be represented by the following graphic formulae: ##STR1## Also described are polymeric organic host materials that contain or that are coated with such compounds or combinations thereof with complementary photochromic compounds, e.g., certain other naphthopyrans, nenzopyrans, and spiro(indoline)type compounds.Type: GrantFiled: July 10, 1998Date of Patent: February 8, 2000Assignee: Transitions Optical, Inc.Inventor: Anil Kumar
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Patent number: 6015569Abstract: Novel pharmaceutically/cosmetically-active polycyclic aromatic compounds have the structural formula (I): ##STR1## wherein Ar is a radical having one of the formulae (a)-(e): ##STR2## and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.Type: GrantFiled: November 17, 1997Date of Patent: January 18, 2000Assignee: Centre International de Recherches Dermatologiques GaldermaInventor: Jean-Michel Bernardon
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Patent number: 5998459Abstract: The invention relates to a pharmaceutical composition comprising a pyrrole derivative of the following formula [1] or a pharmaceutically acceptable salt thereof, or a solvate of either of them, as an active ingredient. ##STR1## (wherein R.sup.1 represents hydrogen or alkoxycar91 bonylamino, R.sup.2 represents alkyl, aryl which may be substituted, aromatic heterocyclyl which may be substituted, unsubstituted amino, monoalkylamino, dialkylamino, or cyclic amino which may be substituted; R.sup.3 represents cyano or carbamoyl; R.sup.4 represents hydrogen or alkyl; E represents alkylene; q is equal to 0 or 1, A represents methyl, aryl which may be substituted, or aromatic heterocyclyl which may be substituted). The pharmaceutical composition of the invention is effective for the treatment of pollakiuria or urinary incontinence.Type: GrantFiled: December 8, 1997Date of Patent: December 7, 1999Inventors: Masami Tsuda, Mitsushi Tanaka, Ayatsugu Nakamura
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Patent number: 5994389Abstract: The invention relates to novel substituted N-aryl- and N-alkylsulfonylaminals of the formula (I) in whichA represents specific N-heterocycles specified in the description and R.sup.1, R.sup.2 and R.sup.3 have the meaning given in the description, to a process for their preparation and to their use as agents for combating pests.Type: GrantFiled: August 21, 1997Date of Patent: November 30, 1999Assignee: Bayer AktiengesellschaftInventors: Bernd Baasner, Hermann Hagemann, Markus Heil, Folker Lieb, Hermann Uhr, Christoph Erdelen
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Patent number: 5985864Abstract: Donepezil hydrochloride, 1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride, is provided here in the form of four polymorphs which are stable against heat and humidity in the pharmaceutical use. They can be industrially produced. They are specified by peaks in X-ray powder diffraction pattern and absorption peaks in infrared absorption spectra in potassium bromide.Type: GrantFiled: June 6, 1997Date of Patent: November 16, 1999Assignee: Eisai Co., Ltd.Inventors: Akio Imai, Hideaki Watanabe, Takashi Kajima, Yasushi Ishihama, Akiyo Ohtsuka, Tomohide Tanaka, Yukio Narabu
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Patent number: 5977111Abstract: A thiopyran derivative represented by the following formula (I) or (I'), or the salt thereof. ##STR1## wherein A is S or --CH.dbd.CH--; the dotted line indicates that the bond may be either present or absent; Z and Z' are typically ##STR2## L is an ethylene or trimethylene group; Y is CH or N; n is 2; B is a carbonyl group; m is 0 or 1; D is a phenyl group; and E.sub.1 and E.sub.2 are hydrogen atoms. These compounds exhibit a strong serotonin-2 blocking action and highly safe. Some compounds also exhibit an .alpha..sub.1 -blocking action and therefore are useful as an antihypertensive agent with less side effects. Thus, the thiopyran derivatives are useful as drugs for the treatment of circulatory diseases in general such as hypertension, ischemic heart disease, cerebrovascular disturbance, and peripheral circulatory disturbance.Type: GrantFiled: June 21, 1996Date of Patent: November 2, 1999Assignee: Suntory LimitedInventors: Akira Mizuno, Makoto Shibata, Tomoe Iwamori, Norio Inomata
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Patent number: 5972989Abstract: Selected heterocyclecarbonyl amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.Type: GrantFiled: February 24, 1998Date of Patent: October 26, 1999Assignee: G.D. Searle & Co.Inventors: Daniel P Getman, Gary A DeCrescenzo, John N Freskos, Michael L Vazquez, James A Sikorski, Balekudru Devadas, Srinivasan Nagarajan, David L Brown, Joseph J McDonald
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Patent number: 5968970Abstract: Described herein is a retroviral protease inhibiting compound of the formula: ##STR1## or a pharmaceutically acceptable salt, prodrug or ester thereof.Type: GrantFiled: January 2, 1998Date of Patent: October 19, 1999Assignee: G. D. Searle & CompanyInventors: Daniel P. Getman, Gary A. DeCrescenzo, John N. Freskos, Michael L. Vazquez, James A. Sikorski, Balekudru Devadas, Srinivasan R. Nagarajan, David L. Brown, Joseph J. McDonald
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Patent number: 5968954Abstract: New 2-aminoindan compounds of formula: ##STR1## wherein: n, Ar, R, E, X.sub.1, X.sub.2, X.sub.3, and X.sub.4 are as defined in the description, in the form of a racemic mixture and in the form of optical isomers, and physiologically-tolerable acid addition salts thereof. The products of the invention are useful as medicaments and exhibit selective binding affinity for the 5HT.sub.1B receptors.Type: GrantFiled: February 26, 1998Date of Patent: October 19, 1999Assignee: Adir et CompagnieInventors: Jean-Louis Peglion, Bertrand Goument, Mark Millan, Alain Gobert
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Patent number: 5965601Abstract: Selected amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.Type: GrantFiled: March 3, 1998Date of Patent: October 12, 1999Assignee: G. D. Searle & Co.Inventors: Daniel P Getman, Gary A DeCrescenzo, John N Freskos, Michael L Vazquez, James A Sikorski, Balekudru Devadas, Srinivasan Nagarajan, David L Brown, Joseph J McDonald
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Patent number: 5965575Abstract: New N-arylpiperidine compounds of formula: ##STR1## wherein: A, m, R, E, n and Ar are as defined in the description, the isomers thereof and the addition salts thereof with a pharmaceutically acceptable acid, and medicinal products containing the same are useful in the treatment of disorders involving the serotininergic system.Type: GrantFiled: March 27, 1998Date of Patent: October 12, 1999Assignee: Adir Et CompagnieInventors: Jean-Louis Peglion, Bertrand Goument, Mark Millan, Alain Gobert, Valerie Audinot
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Patent number: 5955520Abstract: Described are novel photochromic indeno-fused naphthopyran compounds, examples of which are naphthopyran compounds having a substituted or unsubstituted indeno group, the 2,1 positions of which are fused to the f side of the naphtho portion of the naphthopyran, and having certain substituents at the 3-position of the pyran ring. Certain substituents may also be present at the number 5, 6, 7, 8, 9, 10, 11, 12 or 13 carbon atoms of the compounds. These compounds may be represented by the following graphic formula: ##STR1## Also described are polymeric organic host materials that contain or that are coated with such compounds. Optically clear articles such as ophthalmic lenses or other plastic transparencies that incorporate the novel naphthopyran compounds or combinations thereof with complementary photochromic compounds, e.g., certain other naphthopyrans, benzopyrans and spiro(indoline)type compounds, are also described.Type: GrantFiled: June 17, 1996Date of Patent: September 21, 1999Assignee: PPG Industries, Inc.Inventors: Harry G. Heller, Julian R. Levell
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Patent number: 5935973Abstract: Compounds of formula I ##STR1## and pharmaceutically acceptable salts thereof in which A is methylene or O; B is methylene or O; g is 0,1,2,3 or 4; R.sub.1 is an optional substituent; U is an alkylene chain optionally substituted by one or more alkyl; Q represents a divalent group containing nitrogen atoms; and T represents CO.HET, have utility in the treatment of central nervous system disorders, for example depression, anxiety, psychoses (for example schizophrenia), tardive dyskinesia, Parkinson's disease, obesity, hypertension, Tourette's syndrome, sexual dysfunction, drug addiction, drug abuse, cognitive disorders, Alzheimer's disease, senile dementia, obsessive-compulsive behavior, panic attacks, social phobias, eating disorders and anorexia, cardiovascular and cerebrovascular disorders, non-insulin dependent diabetes mellitus, hyperglycaemia, constipation, arrhythmia, disorders of the neuroendocrine system, stress, prostatic hypertrophy, and spasticity.Type: GrantFiled: January 5, 1998Date of Patent: August 10, 1999Assignee: Knoll AktiengesellschaftInventors: Alan Martin Birch, David John Heal, Frank Kerrigan, Keith Frank Martin, Patricia Lesley Needham, Bruce Jeremy Sargent
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Patent number: 5919935Abstract: The present invention relates to novel, halogenated psoralen compounds that are useful for inactivating vital contaminants in blood-derived products, particularly blood-derived products that contain platelets or red blood cells. The psoralen compounds of the present invention have the following formula: The side chain S which is a attached to the carbon at position 8 of the psoralen moiety contains a quartemary ammonium group which comprises a central nitrogen atom, a linking group L, and an aromatic ring structure. The linking group L joins the central nitrogen atom of the quartenary ammonium group to the psoralen moiety. The linking group L comprises a carbon chain having 2 to 12 carbon atoms and an oxygen atom which links the carbon chain to the psoralen moiety. The psoralen compounds of the present invention also comprise one or more halogens attached to the psoralen moiety. Preferably the halogens are attached to the carbon atom at position 3 or 5 of the psoralen moiety.Type: GrantFiled: November 21, 1997Date of Patent: July 6, 1999Assignee: The Ohio State Research FoundationInventors: Matthew S. Platz, Tongqian Chen, Shashi S. Kagan, Helena M. Pereira
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Patent number: 5912262Abstract: The present invention relates to novel N-substituted amino alcohols, amino acids and acid derivatives thereof in which a substituted alkyl chain forms part of the N-substituent or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation.Type: GrantFiled: October 24, 1997Date of Patent: June 15, 1999Assignee: Novo Nordish A/SInventors: Rolf Hohlweg, Tine Krogh J.o slashed.rgensen, Knud Erik Andersen, Uffe Bang Olsen, Peter Madsen, Zdenek Polivka, Otylie Konigova, Frantisek Miksik, Martina Kovandova, Alexandra Silhankova, Karel Sindelar
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Patent number: 5908858Abstract: Compounds of formula (I) and (II): ##STR1## ?wherein R is hydrogen, halogen or alkyl; R.sup.1 is alkyl, amino or substituted amino; R.sup.2 is optionally substituted phenyl; R.sup.3 is hydrogen, halogen or optionally substituted alkyl; R.sup.4 is hydrogen, optionally substituted alkyl, cycloalkyl, aryl, or aralkyl! have valuable analgesic, anti-inflammatory, anti-pyretic and anti-allergic activities and have the ability to inhibit the production of leukotrienes and to inhibit bone resorption. They are relatively free from the side effects which generally result from the administration of compounds having these kinds of activities.Type: GrantFiled: March 26, 1997Date of Patent: June 1, 1999Assignee: Sankyo Company, LimitedInventors: Tomio Kimura, Yasuo Noguchi, Akira Nakao, Keisuke Suzuki, Shigeru Ushiyama, Akihiro Kawara, Masaaki Miyamoto
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Patent number: 5871938Abstract: 1,2-dioxetane compounds bearing a proteolytic enzyme specific amino acid or peptide are provided, which amino acid or peptide can be removed by action of the corresponding protease. When the amino acid or peptide is removed, the 1,2-dioxetane decomposes with chemiluminescence, the generation of light providing a rapid, ultra-sensitive and convenient means for detecting the presence of the protease in the sample being inspected. The amount of light generated, or degree of chemiluminescence, can be correlated with the amount of protease present. Immunoassays, as well as DNA hybridization and DNA probe assays are provided.Type: GrantFiled: September 22, 1997Date of Patent: February 16, 1999
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Patent number: 5869520Abstract: Novel carbamoyloxylabdanes, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure and treating cardiac failure utilizing compounds and compositions thereof are disclosed.Type: GrantFiled: January 8, 1997Date of Patent: February 9, 1999Assignee: Hoechst Marion Roussel, Inc.Inventors: Raymond W. Kosley, Jr., Robert Joseph Cherill, Gerard O'Malley
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Patent number: 5861429Abstract: Compounds of formula (I): ##STR1## wherein: R.sup.1 is methyl, ethyl, isopropyl or sec-butyl; X is carbonyl or methylene; Z is .dbd.C.dbd.(R.sup.2).sub.2 or .dbd.C.dbd.(CH.sub.2).sub.m, in which R.sup.2 is alkyl, and m is integer of from 2 to 5); n is 0 or 1; R.sup.3 is nitro, amino, alkylamino, dialkylamino, alkoxy, alkoxyalkoxy, or a group (iii), (iv), (v), (vi), (vii), (viii) or (ix): ##STR2## , wherein: R.sup.4 represents: alkyl; substituted alkyl; cycloalkyl having from 3 to 6 carbon atoms; substituted cycloalkyl; alkenyl; alkynyl; carbocyclic aryl; or heterocyclic; R.sup.5 is hydrogen atom or alkyl; R.sup.6 represents: hydrogen; alkyl; or cycloalkyl; R.sup.7 represents: alkyl; cycloalkyl; carbocyclic aryl; or aralkyl; or R.sup.6 and R.sup.7, together with the nitrogen atom to which they are attached, are fuised to form heterocyclic ring; Y is oxygen or sulfur; r is 1, 2 or 3; Q is methylene or carbonyl; R.sup.8 is: alkyl or carbocyclic aryl; R.sup.Type: GrantFiled: September 30, 1996Date of Patent: January 19, 1999Assignee: Sankyo Company, LimitedInventors: Kazuo Sato, Akio Saito, Toshimitsu Toyama