Nitrogen Attached Directly Or Indirectly To The Hetero Ring By Acyclic Nonionic Bonding Patents (Class 549/419)
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Patent number: 6723858Abstract: The application discloses methods of treating mammalian diseases characterized by abnormal cell mitosis by administering estradiol derivatives including those comprising colchicine or combretastatin A-4 structural motifs of the general formulae found below in a dosage sufficient to inhibit cell mitosis. The application discloses novel compounds used in the methods.Type: GrantFiled: February 21, 2002Date of Patent: April 20, 2004Assignee: The Children's Medical Center CorporationInventors: Robert John D'Amato, Moses Judah Folkman
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Publication number: 20040063974Abstract: The present invention relates compounds of the formula (I): 1Type: ApplicationFiled: July 15, 2003Publication date: April 1, 2004Inventors: Jose Luis Castro Pineiro, Piotr Antoni Raubo, Christopher John Swain
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Publication number: 20040058880Abstract: This invention relates to novel aminoglycoside compounds having antibacterial and anti-infective activity and to pharmaceutical compositions, methods of making and methods of treatment employing the same.Type: ApplicationFiled: June 26, 2003Publication date: March 25, 2004Inventors: Chang-Hsing Liang, Kenneth Marby, David Rabuka, Alex Romero, Paul W. M. Sgarbi, Steven J. Sucheck, Youe-Kong Shue, Sulan Yao
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Publication number: 20040059138Abstract: The present invention provides novel dihydropyrancarboxamide compounds of formula (I): 1Type: ApplicationFiled: August 27, 2003Publication date: March 25, 2004Inventors: Stuart L. Schreiber, Robert A. Stavenger, Timothy J. Mitchison, Zoltan Maliga
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Publication number: 20040048815Abstract: The invention relates to novel amidines and quanidines, the production and use thereof and the use thereof as trypsine-type serine protease competitive inhibitors, especially thrombine and compliment proteases CIs and C1r. The invention also relates to pharmaceutical compositions which contain said compounds as active ingredients, in addition to the use of the compounds as thrombine inhibitors, anticoagulants, compliment inhibitors and anti-inflammatory agents. The novel compositions are characterised by the linkage of a serine protease inhibitor having amidine or quanidine functions with an alkyl radical having two or more hydroxyl functions, whereby said alkyl radical is derived from sugar derivates.Several sugar structural components or components derived from sugar can therefore be linked to each other. Said principle of linking sugar derivates enables oral active compounds to be obtained.Type: ApplicationFiled: August 18, 2003Publication date: March 11, 2004Inventors: Dieter Herr, Helmut Mack, Werner Seitz, Wilfried Hornberger
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Publication number: 20040030160Abstract: Tetrahydropyranyloxyamines are extremely useful as intermediates in the production of pharmaceuticals and agricultural chemicals, and as raw materials, additives or precursors in the production of perfumes, resins and adhesives. The present invention provides a process for producing a tetrahydropyranyloxyamine from an aminoalcohol which is both simple and produces a high yield. According to the present invention, an aminoalcohol represented by a general formula (1) shown below is reacted with an acid, the obtained aminoalcohol salt is reacted with 3,4-dihydro-2H-pyran, and the obtained tetrahydropyranyloxyamine salt is subsequently reacted with an alkali to form a tetrahydropyranyloxyamine represented by the general formula (2) shown below.Type: ApplicationFiled: June 20, 2002Publication date: February 12, 2004Inventors: Kunihiko Sakano, Kimio Tamura, Toshitaka Uragaki, Kuniyoshi Ogura
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Publication number: 20040019217Abstract: This invention relates to dihydroxyhexanoic acid derivatives and their intermediates, as well as to methods of preparing such compounds. Additionally, present invention relates to removing a protecting group from a protected amine wherein the method comprises reacting the protected amine with phosphoric acid.Type: ApplicationFiled: May 7, 2003Publication date: January 29, 2004Applicant: Pfizer Inc.Inventors: John C. Kath, Zhengong B. Li, V. John Jasys, Frank J. Urban
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Patent number: 6677355Abstract: Compounds of the formula; are useful for inhibiting matrix metalloproteinase enzymes in animals, and as such, prevent and treat diseases resulting from the breakdown of connective tissues. Also disclosed are methods for the preparation of such compounds, pharmaceutical compositions including the same, and methods of treating diseases in which matrix metalloproteinases are involved including multiple sclerosis, atherosclerotic plaque rupture, restenosis, aortic aneurysm, heart failure, periodontal disease, corneal ulceration, burns, decubital ulcers, chronic ulcers or wounds, cancer metastasis, tumor angiogenesis, osteoporosis, rheumatoid or osteoarthritis, renal disease, left ventricular dilation, or other autoimmune or inflammatory diseases dependent upon tissue invasion by leukocytes.Type: GrantFiled: February 13, 2002Date of Patent: January 13, 2004Assignee: Warner-Lambert CompanyInventors: Christopher Alan Conrad, Patrick Michael O'Brien, Daniel Fred Ortwine, Joseph Armand Picard, Drago Robert Sliskovic
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Publication number: 20040002492Abstract: The application concerns a compound of formula I: 1Type: ApplicationFiled: February 24, 2003Publication date: January 1, 2004Applicant: Kudos Pharmaceuticals LtdInventors: Graeme Cameron Murray Smith, Niall Morrison Barr Martin, Stephen Philip Jackson, Mark James O'Connor, Alan Yin Kai Lau, Xiao-Ling Fan Cockcroft, Ian Timothy Williams Matthews, Keith Allan Menear, Laurent Jean Martin Rigoreau, Marc Geoffery Hummersone, Roger John Griffin
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Publication number: 20030228984Abstract: The invention relates to novel phenyl-substituted cyclic ketoenols of the formula (I) 1Type: ApplicationFiled: April 1, 2003Publication date: December 11, 2003Inventors: Hermann Hagemann, Reiner Fischer, Christoph Erdelen, Ulrike Wachendorff-Neumann, Udo Schneider, Wolfram Andersch
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Patent number: 6638947Abstract: This invention is related to carbocyclic and heterocyclic substituted semicarbazones and thiosemicarbazones represented by Formula I: or a pharmaceutically acceptable salt or prodrug thereof, wherein: Y is oxygen or sulfur; R1, R21, R22 and R23 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl; or R22 and R23, together with the N, form a heterocycle; A1 and A2 are independently aryl, heteroaryl, saturated or partially unsaturated carbocycle or saturated or partially unsaturated heterocycle, any of which is optionally substituted; X is one or O, S, NR24, CR25R26, C(O), NR24C(O), C(O)NR24, SO, SO2 or a covalent bond; where R24, R25 and R26 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl.Type: GrantFiled: December 6, 2001Date of Patent: October 28, 2003Assignee: Euro-Celtique S.A.Inventors: Yan Wang, Sui Xiong Cai, John F. W. Keana
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Patent number: 6617350Abstract: 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: August 9, 2001Date of Patent: September 9, 2003Assignee: Vertex Pharmaceuticals IncorporatedInventors: Michael R. Hale, Christopher T. Baker, Timothy A. Stammers, Ronald George Sherrill, Andrew Spaltenstein, Eric Steven Furfine, François Maltais, Clarence Webster Andrews, III, John Franklin Miller, Vicente Samano
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Patent number: 6608218Abstract: Substituted benzene acetamide compounds and pharmaceutically acceptable salts thereof are useful as glucokinase activators.Type: GrantFiled: June 25, 2002Date of Patent: August 19, 2003Assignee: Hoffmann-La Roche Inc.Inventors: Robert Francis Kester, Ramakanth Sarabu
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Patent number: 6583299Abstract: A family of molecules is disclosed that inhibit matrix metalloprotease (MMP) activity, and particularly inhibit the activity of one or more of MMP-2, MMP-9, or MMP-13, while generally exhibiting little activity against MMP-1. A contemplated compound also exhibits little inhibition of the production of TNF. A contemplated compound is an &agr;-amino-&bgr;-sulfonyl carbocyclo, heterocyclo, aryl, or heteroaryl hydroxamic acid. Also disclosed are processes for preparing a contemplated compound and for treating a mammal having a condition associated with pathological matrix metalloprotease activity.Type: GrantFiled: May 16, 2000Date of Patent: June 24, 2003Assignee: G.D. Searle & Co.Inventors: Susan L Hockerman, Daniel P. Becker, Louis J Bedell, Gary A DeCrescenzo, John N Freskos, Daniel P Getman, Robert M Heintz, Madeleine H Li, Brent V Mischke, Clara I Villamil, Thomas E Barta
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Patent number: 6458830Abstract: The present invention relates to compounds of the formula (I): wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and n are defined herein. The compounds are of particular use in the treatment or prevention of depression, anxiety, pain, inflammation, migraine, emesis and postherpetic neuralgia.Type: GrantFiled: September 10, 2001Date of Patent: October 1, 2002Assignee: Merck Sharp & Dohme Ltd.Inventors: Simon Neil Owen, Eileen Mary Seward, Christopher John Swain, Brian John Williams
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Patent number: 6451766Abstract: Compounds of formula (I) or their salts or esters: [wherein R1 is alkyl or haloalkyl; R2 and R3 each represents hydrogen or aliphatic acyl; X is hydroxy, halogen, alkoxy, or a group of formula RaO—, where Ra is aliphatic acyl; Y is a group of formula RbRcN— or RbRcN—O—, where Rb and Rc each is hydrogen or alkyl; and Z is oxygen or sulfur] have excellent sialidase inhibitory activity and are therefore useful for the treatment and prevention of influenza and other viral diseases where the replication of the virus is susceptible to sialidase inhibitors.Type: GrantFiled: October 3, 2001Date of Patent: September 17, 2002Assignee: Sankyo Company, LimitedInventors: Takeshi Honda, Yoshiyuki Kobayashi, Makoto Yamashita
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Patent number: 6436930Abstract: The present invention relates to antifungal compounds having the structural formula: and pharmaceutically acceptable salts, solvates and prodrugs thereof. The present invention further relates to pharmaceutical compositions containing said compound, or a pharmaceutically acceptable salt, solvate or prodrug thereof, for use in the treatment of a fungal infection in an animal host.Type: GrantFiled: September 14, 2001Date of Patent: August 20, 2002Assignee: Bristol-Myers Squibb CompanyInventors: Michael Serrano-Wu, Xuhua Du, Neelakantan Balasubramanian, Denis R. St. Laurent
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Patent number: 6391918Abstract: Novel &agr;-amino acid amides of formula (I) as well as possible isomers and mixtures of isomers thereof, wherein the substituents are defined as follows: n is the number zero or one; R1 is optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl or arylalkyl; or a group NRaRb wherein Ra and Rb are each independently of the other hydrogen, alkyl or form together an alkylene bridge; R2 is hydrogen or alkyl; R3 is optionally substituted aryl or heteroaryl; A is alkylene; and B is optionally substituted aryl; with the exception of the following compounds 2-phenyl-N-(1-phenyl-ethyl)-2-(4-methylphenyl)-sulfonylamino-acetamide, 2-phenyl-N-(1-phenyl-ethyl)-2-(4-chlorophenyl)-sulfonylamino-acetamide, 2-phenyl-N-(1-phenyl-ethyl)-2-(4-nitrolphenyl)-sulfonylamino-acetamide, 2-phenyl-N-(1-phenyl-ethyl)-2-(4-methoxyphenyl)-sulfonylamino-acetamide, 2-phenyl-N-(1-phenyl-ethyl)-2-(4-fluorophenyl)-sulfonylamino-acetamide, 2-phenyl-N-(1-phenyl-ethyl)-2-phenyl-sulfonylamino-acetamide and 2-phenyl-N-(1-pType: GrantFiled: August 25, 2000Date of Patent: May 21, 2002Assignee: Syngenta Crop Protection, Inc.Inventors: André Jeanguenat, Martin Zeller
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Patent number: 6350761Abstract: This invention is directed to benzenamine derivatives of formula (I): wherein A, W, m, n, R1, R2, R3, R4, R5 and R6 are defined herein. These compounds are useful as anti-coagulants.Type: GrantFiled: July 24, 2000Date of Patent: February 26, 2002Assignee: Berlex Laboratories, Inc.Inventors: William J. Guilford, Steven T. Sakata, Kenneth J. Shaw, Shung Wu, Wei Xu, Zuchun Zhao
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Publication number: 20020019534Abstract: A compound of the formula 1Type: ApplicationFiled: March 27, 2001Publication date: February 14, 2002Inventor: Mark C. Noe
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Patent number: 6340702Abstract: Compounds of formula (I) or their salts or esters: have excellent sialidase inhibitory activity and are therefore useful for the treatment and prevention of influenza and other viral diseases where the replication of the virus is susceptible to sialidase inhibitors.Type: GrantFiled: April 28, 1999Date of Patent: January 22, 2002Assignee: Sankyo Company, LimitedInventors: Takeshi Honda, Yoshiyuki Kobayashi, Takeshi Masuda, Makoto Yamashita, Masami Arai
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Patent number: 6331563Abstract: Matrix metalloproteinases (MMPs) are a group of enzymes that have been implicated in the pathological destruction of connective tissue and basement membranes. These zinc containing endopeptidases consist of several subsets of enzymes including collagenases, stromelysins and gelatinases. TNF-&agr; converting enzyme (TACE), a pro-inflammatory cytokine, catalyzes the formation of TNF-&agr; from membrane bound TNF-&agr; precursor protein. It is expected that small molecule inhibitors of MMPs and TACE therefore have the potential for treating a variety of disease states.Type: GrantFiled: June 5, 2000Date of Patent: December 18, 2001Inventors: Aranapakam Mudumbai Venkatesan, George Theodore Grosu, Jannie Lea Baker
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Publication number: 20010039287Abstract: A treatment process is disclosed that comprises administering an effective amount of an aromatic sulfone hydroxamic acid that exhibits excellent inhibitory activity of one or more matrix metalloprotease (MMP) enzymes, such as MMP-2, MMP-9 and MMP-13, while exhibiting substantially less inhibition at least of MMP-1 to a host having a condition associated with pathological matrix metalloprotease activity. Also disclosed are metalloprotease inhibitor compounds having those selective activities, processes for manufacture of such compounds and pharmaceutical compositions using an inhibitor.Type: ApplicationFiled: February 24, 1999Publication date: November 8, 2001Inventors: THOMAS E BARTA, DANIEL P BECKER, TERRI L BOEHM, GARY A DECRESCENZO, CLARA I WILLAMI1, JOSEPH J MCDONALD, JOHN N FRESKOS, DANIEL P GETMAN, GUNNAR J HANSON
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Patent number: 6265446Abstract: Hydrazine derivatives of the formula wherein R1 represents lower alkyl, lower alkenyl, lower cycloalkyl, lower cycloalkyl-lower alkyl, aryl or aryl-lower alkyl, R2 represents heterocyclyl or NR5R6, R3 represents hydrogen, lower alkyl, halo-lower alkyl, cyano-lower alkyl, hydroxy-lower alkyl, amino-lower alkyl, lower alkoxy-lower alkyl, lower alkoxycarbonyl-lower alkyl, lower cycloalkyl-lower alkyl, aryl-lower alkyl, heterocyclyl-lower alkyl, heterocyclylcarbonyl-lower alkyl, lower alkenyl, lower alkynyl, lower cycloalkyl, aryl, heteroaryl or aryl-lower alkyl, R4 represents lower alkyl, lower alkenyl, lower cycloalkyl, lower cycloalkyl-lower alkyl or a grouping of the formula -Z-aryl, -Z-heterocyclyl or —(CH2)n—, CH═CR7R8, R5 and R6 each independently represent hydrogen or lower alkyl, R7 and R8 each independently represent hydrogen or lower alkyl or R7 and R8 together represent lower alkylene in which one CH2 group is optionally replaced by a hetero atom, X and Z each represType: GrantFiled: November 22, 1999Date of Patent: July 24, 2001Assignee: Hoffmann-La Roche Inc..Inventors: Michael John Broadhurst, William Henry Johnson, Daryl Simon Walter
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Patent number: 6242616Abstract: Synthetic methods for lactone-containing compounds such as the discodermolides are provided, as are compounds which mimic the chemical and/or biological activity thereof, and methods and intermediates useful in their preparation.Type: GrantFiled: December 7, 1999Date of Patent: June 5, 2001Assignee: The Trustees of the University of PennsylvaniaInventors: Amos B. Smith, III, Thomas J. Beauchamp, Matthew J. LaMarche, Hirokazu Arimoto
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Patent number: 6235922Abstract: Compounds having the following formula I, and pharmaceutically acceptable salts thereof, including dual inhibitors of ACE and NEP and selective ACE inhibitors: wherein: Y1 and Y2 are each independently hydrogen, alkyl, aryl, halogen, or alkoxy; X is O or S(O)t; A is t is zero, one or two; m and n are independently zero or one; and wherein R, R5, R5a, R5b, R6, R7, R11, q and r are defined herein.Type: GrantFiled: December 4, 1998Date of Patent: May 22, 2001Assignee: Bristol-Myers Squibb Co.Inventors: Jeffrey A. Robl, Chong-Qing Sun
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Patent number: 6211370Abstract: The present invention relates to a process for stereoselective cycloaddition reactions which generally comprises a cycloaddition reaction between a pair of substrates, each either chiral or prochiral, that contain reactive &pgr;-systems, in the presence of a non-racemic chiral catalyst, to produce a stereoisomerically enriched product. The present invention also relates to novel asymmetric catalyst complexes comprising a metal and an asymmetric tridentate ligand.Type: GrantFiled: February 23, 1999Date of Patent: April 3, 2001Assignee: Harvard UniversityInventors: Eric N. Jacobsen, Scott E. Schaus, Alexander G. Dossetter, Timothy F. Jamison
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Patent number: 6197810Abstract: A compound of the formula wherein R1, R2, R3, R4 and Q are as defined above, are useful in the treatment of arthritis (including osteoarthritis and rheumatoid arthritis), cancer and other diseases. In addition, the compounds of the present invention may be used in combination therapy with standard non-steroidal anti-inflammatory drugs (NSAID's), COX-2 inhibitors and analgesics, and in combination with cytotoxic drugs such as adriamycin, daunomycin, cis-platinum, etoposide, taxol, taxotere and other alkaloids, such as vincristine, in the treatment of cancer.Type: GrantFiled: May 26, 2000Date of Patent: March 6, 2001Assignee: Pfizer IncInventor: Lawrence A. Reiter
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Patent number: 6194451Abstract: A compound of formula (I), wherein W is —NHOH or —OH, R1 is either free or protected hydroxymethyl or mercaptomethyl or derivatives thereof, R2 is free or protected hydroxy, R3 and R4 is an organic group, R5 is hydrogen or methyl, or R4 and R5, together with the nitrogen atom to which they are attached, constitute an azaheterocyclyl group, and the solvates, hydrates and pharmaceutically acceptable salts thereof, can inhibit matrix metalloproteinases and the release of tumour necrosis factor (TNF). Processes for producing the compound, intermediates involved in the processes, and pharmaceutical compositions containing the compound are also described.Type: GrantFiled: July 30, 1999Date of Patent: February 27, 2001Assignee: Pharmacia & Upjohn S.p.A.Inventors: Marco Alpegiani, Massimiliano Palladino, Riccardo Corigli, Daniela Jabes, Ettore Perrone, Maria Francesca Abrate, Pierluigi Bissolino, Marina Lombroso
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Patent number: 6172057Abstract: Matrix metalloproteinases (MMPs) are a group of enzymes that have been implicated in the pathological destruction of connective tissue and basement membranes. These zinc containing endopeptidases consist of several subsets of enzymes including collagenases, stromelysins and gelatinases. TNF-&agr; converting enzyme (TACE), a pro-inflammatory cytokine, catalyzes the formation of TNF-&agr; from membrane bound TNF-&agr; precursor protein. It is expected that small molecule inhibitors of MMPs and TACE therefore have the potential for treating a variety of disease states. The present invention provides low molecular weight, non-peptide inhibitors of matrix metalloproteinases (MMPs) and TNF-&agr; converting enzyme (TACE) for the treatment of arthritis, tumor metastasis, tissue ulceration, abnormal wound healing, periodontal disease, bone disease, diabetes (insulin resistance) and HIV infection.Type: GrantFiled: February 19, 1998Date of Patent: January 9, 2001Assignee: American Cyanamid CompanyInventors: Aranapakam Mudumbai Venkatesan, George Theodore Grosu, Jamie Marie Davis, Baihua Hu, Derek Cecil Cole, Jannie Lea Baker, Marcy Pamela Jacobson, Matthew Robin O'Dell
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Patent number: 6159973Abstract: The subject of the invention is the compounds of formula (I):Q(CH.sub.2).sub.a --(X.sub.1).sub.b --Q.sub.1 --Q.sub.2 --C(X.sub.2)--N(R.sub.1)(R.sub.2) (I)in which:Q represents an aryl radical,X.sub.1 represents oxy, thio, sulphinyl or sulphonyl,X.sub.2 represents oxygen or sulphur,Q.sub.1 represents a cyclopropanediyl radical,Q.sub.2 represents an arylene radical,R.sub.1 and R.sub.2 represent:either a hydrogen atom or a hydrocarbon radicalor one of the groupsR.sub.3 --C.dbd.X.sub.3, (R.sub.3).sub.2 --P.dbd.X.sub.3, T.sub.2 --R.sub.5 or S(O).sub.j --N(R.sub.6)(R.sub.7)in which X.sub.3 represents an oxygen atom or a sulphur atom, T.sub.2 represents a bivalent oxy, carbonyl or oxycarbonyl group and j is equal to 0, 1 or 2,their preparation process and their use as pesticides.Type: GrantFiled: July 21, 1999Date of Patent: December 12, 2000Assignee: Hoechst Schering Agrevo S.A.Inventors: Jacques Demassey, Michel Gohar, Christian Wehrey
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Patent number: 6136986Abstract: The invention relates to a process for preparing substituted chroman derivatives of the general formula VII, ##STR1## where X is the group --CN, --COOR.sup.3, --CHO, --CH.sub.2 OR.sup.7 or --CH(OR.sup.8).sub.2,R.sup.2 is a C.sub.1 -C.sub.23 -alkyl, C.sub.2 -C.sub.23 -alkenyl, C.sub.6 -C.sub.18 -aryl or C.sub.7 -C.sub.18 -aralkyl radical,R.sup.3 is hydrogen or an optionally substituted C.sub.1 -C.sub.4 -alkyl radical,R.sup.4, R.sup.5, R.sup.6 are, independently of one another, hydrogen or a C.sub.1 -C.sub.4 -alkyl radical,R.sup.7 is hydrogen or a C.sub.1 -C.sub.4 -alkyl radical,R.sup.8 is a C.sub.1 -C.sub.4 -alkyl radical, or the two radicals are a C.sub.2 -C.sub.6 -alkylene radical which links the two oxygen atoms to form a cyclic acetal and is optionally branched or may carry one or two carboxyl groups, cyclohexyl or phenyl radicals,and to the novel intermediates of the process.Type: GrantFiled: December 13, 1999Date of Patent: October 24, 2000Assignee: BASF AktiengesellschaftInventors: Rainer Sturmer, Kai-Uwe Baldenius
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Patent number: 6100266Abstract: For the treatment of cancer, inflammation, and other conditions associated with matrix metalloproteinases or that are mediated by TNF.alpha. or enzymes involved in the shedding of L-selectin, CD23, the TNF receptors, IL-1 receptors, or IL-6 receptors, disclosed are compounds of the general formulaB--X--(CH.sub.2).sub.m --(CR.sup.1 R.sup.2).sub.n --W--COY.Type: GrantFiled: January 29, 1999Date of Patent: August 8, 2000Assignee: Darwin Discovery LimitedInventors: John Gary Montana, Andrew Douglas Baxter, David Alan Owen
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Patent number: 6063816Abstract: A compound selected from those of formula (I): ##STR1## wherein: R.sub.1 represents optionally substituted alkyl, acyl, cycloalkyl, aryl, aminocarbonylalkyl, or heterocycle,R.sub.2 represents alkylene,R.sub.3 represents X or Y as defined in the description,R.sub.4 represents--either alkyl, cycloalkyl, aryl, arylalkyl, cycloalkylalkyl, heterocycloalkylene, or heterocycle when R.sub.3 represents Y,or biaryl, arylheteroaryl or heteroarylaryl, when R.sub.3 represents X or Y,their isomers and also pharmaceutically-acceptable acid or base addition salts thereof, and medicinal products containing the same which are useful as metalloprotease inhibitors in the treatment of cancers.Type: GrantFiled: August 9, 1999Date of Patent: May 16, 2000Assignee: Adir et CompagnieInventors: Stephen Hanessian, Ghanem Atassi, Gordon Tucker, Daniel-Henri Caignard, Pierre Renard
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Patent number: 6057342Abstract: The present application describes amidinophenyl-pyrrolidines, -pyrrolines, and -isoxazolidines and derivatives thereof of formula I: ##STR1## or pharmaceutically acceptable salt forms thereof, wherein one of D and D' may be C(.dbd.NH)NH.sub.2 and the other H, and J.sup.1 and J.sup.2 may be O or CH.sub.2, which are useful as inhibitors of factor Xa.Type: GrantFiled: July 7, 1997Date of Patent: May 2, 2000Assignee: Dupont Pharmaceutical Co.Inventors: John Matthew Fevig, Donald Joseph Phillip Pinto, Mimi Lifen Quan, Petrus Fredericus Wilhelmus Stouten
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Patent number: 6040463Abstract: Sordarin derivatives are antifungal agents useful in the treatment and/or prevention of human and animal fungal infections, as well as in the control of phytopathogenic fungi in crops.Type: GrantFiled: September 24, 1997Date of Patent: March 21, 2000Assignee: Merck & Co., Inc.Inventors: James M. Balkovec, Bruno Tse
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Patent number: 6030997Abstract: The invention relates to a pharmaceutically acceptable prodrug which is a covalent conjugate of a pharmacologically active compound and a blocking group, characterized by the presence of a covalent bond which is cleaved at pH values below 7.0. The prodrug may be used in a technique for treating a condition or disease in a mammal related to elevated hydrogen ion concentrations, whereby on administering it to a mammal having such a condition or disease, the pharmacologically active compound is activated selectively within tissues having such elevated hydrogen ion concentrations.Type: GrantFiled: January 21, 1998Date of Patent: February 29, 2000Inventors: Eran Eilat, Rina Arad-Yellin
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Patent number: 6001823Abstract: Novel methods for the treatment and/or prophylaxis of diseases caused by tissue-adhering bacteria are disclosed. By interacting with periplasmic molecular chaperones it is achieved that the assembly of pili is prevented or inhibited and thereby the infectivity of the bacteria is diminished. Also disclosed are methods for screening for drugs as well as methods for the de novo design of such drugs, methods which rely on novel computer drug modelling methods involving an approximative calculation of binding free energy between macromolecules. Finally, novel pyranosides which are believed to be capable of interacting with periplasmic molecular chaperones are also disclosed.Type: GrantFiled: June 5, 1995Date of Patent: December 14, 1999Inventors: Scott Hultgren, Meta Kuehn, Zheng Xu, Derek Ogg, Mark Harris, Matti Lepisto, Jan Kihlberg, Charles Hal Jones
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Patent number: 5972996Abstract: 4-Cyano-4-deformylsordarin derivatives are antifungal agents useful in the treatment and/or prevention of human and animal fungal infections, as well as in the control of phytopathogenic fungi in crops.Type: GrantFiled: July 28, 1998Date of Patent: October 26, 1999Assignee: Merck & Co., Inc.Inventors: Jennifer Nielsen-Kahn, Bruce Tse
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Patent number: 5965612Abstract: 4-Cyano-4-deformylsordaricin derivatives are antifungal agents useful in the treatment and/or prevention of human and animal fungal infections, as well as in the control of phytopathogenic fungi in crops.Type: GrantFiled: July 28, 1998Date of Patent: October 12, 1999Assignee: Merck & Co., Inc.Inventor: Bruno Tse
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Patent number: 5908863Abstract: Compounds of formula I: ##STR1## wherein R.sub.a, R.sub.b, .PHI., B and R are as defined in the disclosure, have antagonistic activity on osteoclast hyper-reactivity.Type: GrantFiled: February 26, 1997Date of Patent: June 1, 1999Assignee: Dompe' S.p.A.Inventors: Marcello Allegretti, Marco Mantovanini, Gianfranco Caselli, Simonetta Fiorentino, Gaetano Clavenna, Carmelo A. Gandolfi
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Patent number: 5869523Abstract: Process for the preparation of 6-(substitutedaminopropionyl)-derivatives of forskolinProcess for the manufacture of 6.beta.Type: GrantFiled: July 22, 1991Date of Patent: February 9, 1999Assignee: Hoechst AktiengesellschaftInventors: Noel John de Souza, Adolf D'Sa, Samba Laxminarayan Kattige, Gulab Bajirao Padwal, Jurgen Blumbach
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Patent number: 5856573Abstract: A process for producing a compound of the formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and are hydrogen or alkyl, and R is hydrogen or alkyl, which comprises removing the protective group (P) of hydroxyl of a compound of the formula (II): ##STR2## wherein P is a protective group of hydroxyl, .about. indicates an E-isomer, Z-isomer or a mixture thereof, and the other symbols are as defined above; and an intermediate for the production of the compound of the formula (I).Type: GrantFiled: June 10, 1997Date of Patent: January 5, 1999Assignee: Shionogi & Co., LtdInventors: Akira Takase, Hiroyuki Kai, Takami Murashi
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Patent number: 5814608Abstract: 8-fluoro-anthracyclines of formula (I) have anti-tumor activity. ##STR1## wherein: R is chosen in the group consisting of H, OH, OR.sub.4 wherein R.sub.4 is chosen in the group consisting of CHO, COCH.sub.3, acyl derivative of a carboxylic acid containing up to 6 carbon atoms;R.sub.1 is chosen in the group consisting of: H, OH, OCH.sub.3 ;R.sub.2 is chosen in the group consisting of: H, OH, NH.sub.2R.sub.3 is chosen in the group consisting of: H, OH, NH.sub.2, residue of formula (A) ##STR2## The compounds are characterized by having cis-stereochemistry between the groups 8--F and 9--OH. Their preparation and pharmaceutical compositions containing them are also described.Type: GrantFiled: April 21, 1997Date of Patent: September 29, 1998Assignees: Bristol-Myers Squibb, S.p.A., A. Menarini Industrie Farmaceutiche Riunite S.R.L.Inventors: Fabio Animati, Federico Arcamone, Giuseppe Giannini, Paolo Lombardi, Edith Monteagudo
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Patent number: 5808111Abstract: Novel acitretinamide compounds which are soluble and stable in water and useful in aqueous delivery systems, particularly to treat cancer, are provided. The novel acitretinamide compounds, 1-(D-glucopyranosyl)acitretinamide, 1-(D-glucopyranuronosyl)acitretinamide and the metal salts thereof, are hereinafter collectively referred to as the "acitretinamide compounds". The invention also relates to novel methods of making the acitretinamide compounds.Type: GrantFiled: May 6, 1997Date of Patent: September 15, 1998Assignee: The Ohio State Research FoundationInventor: Robert W. Curley, Jr.
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Patent number: 5795981Abstract: Squarylium compounds of the formula: ##STR1## (in which Q.sup.1 and Q.sup.2 are each a chromophoric group having an aromatic unsaturated system conjugated with the squarylium ring and such that in the compounds of formulae Q.sup.1 CH.sub.2 R.sup.1 and Q.sup.2 CH.sub.2 R.sup.2 the methylene hydrogens are active hydrogens, R.sup.1 and R.sup.2 are each independently a hydrogen atom or an aliphatic or cycloaliphatic group, and R.sup.3 and R.sup.4 are each independently a hydrogen atom, or an acyl, aliphatic, cycloaliphatic, aromatic or heterocyclic group, subject to the proviso that one of R.sup.3 and R.sup.4 may be an amino or substituted amino group, or one of R.sup.3 and R.sup.4 is a hydrogen atom and the other is an organosulfonyl group, or R.sup.3 and R.sup.4 together with the intervening nitrogen atom form a nitrogenous heterocyclic ring) are useful as near infra-red absorbers.Type: GrantFiled: December 16, 1996Date of Patent: August 18, 1998Assignee: Polaroid CorporationInventors: John W. Lee, Donald A. McGowan, Mark R. Mischke, Socorro M. Ramos, Stephen J. Telfer
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Patent number: 5691372Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease 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 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.Type: GrantFiled: April 19, 1995Date of Patent: November 25, 1997Assignee: Vertex Pharmaceuticals IncorporatedInventors: Roger D. Tung, Govinda Rao Bhisetti
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Patent number: 5656750Abstract: Squarylium compounds of the formula: ##STR1## (in which Q.sup.1 and Q.sup.2 are each a chromophoric group having an aromatic unsaturated system conjugated with the squarylium ring and such that in the compounds of formulae Q.sup.1 CH.sub.2 R.sup.1 and Q.sup.2 CH.sub.2 R.sup.2 the methylene hydrogens are active hydrogens, R.sup.1 and R.sup.2 are each independently a hydrogen atom or an aliphatic or cycloaliphatic group, and R.sup.3 and R.sup.4 are each independently a hydrogen atom, or an acyl, aliphatic, cycloaliphatic, aromatic or heterocyclic group, subject to the proviso that one of R.sup.3 and R.sup.4 may be an amino or substituted amino group, or one of R.sup.3 and R.sup.4 is a hydrogen atom and the other is an organosulfonyl group, or R.sup.3 and R.sup.4 together with the intervening nitrogen atom form a nitrogenous heterocyclic ring) are useful as near infra-red absorbers.Type: GrantFiled: June 6, 1995Date of Patent: August 12, 1997Assignee: Polaroid CorporationInventors: Richard M. Allen, Peter K. Chu
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Patent number: 5656656Abstract: Tartronic acid acetalic ethers and esters of the general formula: ##STR1## are provided and are useful in treatment of bone dysmetabolism. As examples, Ra and Rb may be hydrogen, B is a C.sub.2 -C.sub.12 acyl group, R is phenyl and n is 0-12.Type: GrantFiled: May 23, 1995Date of Patent: August 12, 1997Assignee: Dompe Farmaceutici S.p.A.Inventors: Carmelo A. Gandolfi, Lorella Cotini, Marco Mantovanini, Gianfranco Caselli, Gaetano Clavenna, Claudio Omini
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Patent number: 5650428Abstract: An arylsulfonamide derivative of the formula (I): ##STR1## wherein R.sup.1 is unsubstituted phenyl or naphthyl, or phenyl substituted by 1 to 3 same or different substituents selected from the group consisting of halogen, alkyl, nitro and alkoxy, R.sup.2 is straight, branched, or branched cyclic alkyl with 1 to 15 carbon atoms, phenyl, phenyloxyl, phenyloxy substituted by one or more halogen atoms, cycloalkyl with 5 to 7 carbon atoms, indolyl, alkylthiol with 1 to 4 carbon atoms, hydroxyl, protected hydroxyl, imidazolyl, pyridyloxyl, or --OSO.sub.2 R.sup.4, R.sup.4 is straight or branched alkyl with 1 to 15 carbon atoms, or unsubstituted phenyl or thienyl, or phenyl or thienyl substituted by 1 to 3 same or different substituents of halogen, alkyl, nitro and alkoxy, R.sup.3 is hydrogen or straight or branched alkyl with 1 to 20 carbon atoms, n is an integer of 0 to 10, p is an integer of 0 to 10, X is a group of the formula--(CH.sub.2)m-A-(CH.sub.Type: GrantFiled: February 28, 1995Date of Patent: July 22, 1997Assignee: NKK CorporationInventors: Masayuki Ohmori, Shin-Ichi Sawamura, Takehiro Yamamoto, Yoshiko Kawada, Shihoko Maeda, Takeshi Yago, Akihiro Nakajima, Masatsugu Mizuguchi, Yasuo Miyoshi