Nitrogen Attached Indirectly To The Ring Nitrogen Of The Five-membered Hetero Ring By Acyclic Nonionic Bonding Patents (Class 548/477)
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Patent number: 6660736Abstract: This invention relates to phthalimido derivatives of the formula wherein X is —N═ or —CH═, and R1 to R4 and m are as defined in the specification, as well as their pharmaceutically acceptable salts. The invention further relates to pharmaceutical compositions containing these compounds, a method of treating a disease by administering a therapeutically effective amount of at least one of these compounds, and a process for their preparation for the treatment or prevention of diseases in which MAO-B inhibitors might be beneficial.Type: GrantFiled: March 13, 2003Date of Patent: December 9, 2003Assignee: Hoffmann-La Roche Inc.Inventors: Andrea Cesura, Rosa Maria Rodriguez Sarmiento, Andrew William Thomas, Rene Wyler
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Publication number: 20030216392Abstract: The compounds of formula 1, 1Type: ApplicationFiled: June 13, 2003Publication date: November 20, 2003Applicant: Dompe S.p.A.Inventors: Riccardo Bertini, Cinzia Bizzarri, Vilma Sabbatini, Gianfranco Caselli, Marcello Allegretti, Maria Candida Cesta, Carmelo Gandolfi, Marco Mantovanini, Francesco Colotta, Stefano Porzio
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Publication number: 20030207889Abstract: Hydroxamic and carboxylic acid derivatives having MMP and TNF inhibitory activity.Type: ApplicationFiled: April 29, 2003Publication date: November 6, 2003Inventors: David Alan Owen, John Gary Montana, John Fraser Keily, Robert John Watson, Andrew Douglas Baxter
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Publication number: 20030176486Abstract: The present invention relates to a novel sulfonic acid derivative of hydroxamic acid or a pharmacologically acceptable salt thereof. More particularly, the present invention relates to a sulfonic acid derivative of hydroxamic acid or a pharmacologically acceptable salt thereof, which is useful as an inhibitor of lipopolysaccharides (LPS). In addition, the present invention relates to a novel intermediate compound useful for the synthesis of this sulfonic acid derivative of hydroxamic acid.Type: ApplicationFiled: February 14, 2003Publication date: September 18, 2003Inventors: Kazuhiro Maeda, Shuji Sonda, Tadahiro Takemoto, Tomokazu Goto, Fujio Kobayashi, Masahiko Kajii, Naruyasu Komorita, Fumihiro Hirayama
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Publication number: 20030158436Abstract: The present invention provides a commercially profitable process for producing a &bgr;-amino acid ester derivativeType: ApplicationFiled: March 5, 2003Publication date: August 21, 2003Applicant: Kaneka CorporationInventors: Akira Nishiyama, Kenji Inoue
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Publication number: 20030130509Abstract: The present invention includes a number of novel intermediates such as the (S)-secondary alcohol of formula (VIIIA)Type: ApplicationFiled: January 28, 2003Publication date: July 10, 2003Applicant: Pharmacia & Upjohn CompanyInventor: Bruce Allen Pearlman
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Patent number: 6498004Abstract: This invention provides a photographic element comprising at least one silver halide emulsion layer in which the silver halide is sensitized with a compound of the formula (a): &Dgr;−(t)m−XY′ (a) XY′−(t)m−&Dgr; (b) &Dgr;−(t)m−XY′−(t)m−&Dgr; (c) wherein &Dgr; is protective group that is eliminated during development of the photographic element, t is a timing group, m is an integer from 0 to 3, and XY′ is a fragmentable electron donor moiety in which X is an electron donor group and Y′ is a leaving proton H or a leaving group Y, with the proviso that if Y′ is a proton, a base, &bgr;−, is present in the emulsion or is covalently linked directly or indirectly to X, and wherein: 1) X—Y′ has an oxidation potential between 0 and about 1.Type: GrantFiled: December 28, 2000Date of Patent: December 24, 2002Assignee: Eastman Kodak CompanyInventors: Jerome R. Lenhard, Annabel A. Muenter, Stephen A. Godleski, Paul A. Zielinski, Deepak Shukla, Donald R. Diehl
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Patent number: 6436949Abstract: Heterocyclically substituted benzamides of the formula I are described, where R1, R2, R3, R4, R5, X, m and n have the meanings given in the description. The novel compounds are useful for controlling diseases.Type: GrantFiled: September 21, 2000Date of Patent: August 20, 2002Assignee: Abbott LaboratoriesInventors: Wilfried Lubisch, Achim Möller, Hans-Jörg Treiber
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Patent number: 6429221Abstract: Novel imides are inhibitors of tumor necrosis factor &agr; and can be used to combat cachexia, endotoxic shock, and retrovirus replication. A typical embodiment is 2-Phthalimido-3-(3′,4′-dimethoxyphenyl)propane.Type: GrantFiled: December 30, 1994Date of Patent: August 6, 2002Assignee: Celgene CorporationInventors: George W. Muller, Mary Shire, David I. Stirling
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Publication number: 20020068831Abstract: An intermediate for the synthesis of amlodipine, a process for the preparation thereof and the corresponding use are disclosed.Type: ApplicationFiled: January 10, 2002Publication date: June 6, 2002Applicant: ESTEVE QUIMICA, S.A.Inventors: Laura Coppi, Yolanda Gasanz Guillen, Julio Campon Pardo
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Patent number: 6359061Abstract: Amide compounds of formula (I), combinatorial libraries of amide compounds and methods of preparing the same are provided. Libraries of the invention are useful for screening in biological assays in order to identify pharmaceutically useful compounds.Type: GrantFiled: March 19, 1999Date of Patent: March 19, 2002Assignee: ISIS Pharmaceuticals, Inc.Inventors: Eric Edward Swayze, Peter William Davis
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Patent number: 6352958Abstract: Novel herbicidal compounds, compositions containing them, and methods for their use in controlling weeds are disclosed. The novel herbicidal compounds are represented by formula I: where J is a 1-substituted-6-trifluoromethyl-2,4-pyrimidinedione-3-yl, a 1-substituted-6-trifluoromethyl-1,3,5-triazine-2,4-dion-1-yl, a 3,4,5,6-tetrahydrophthalimid-1-yl, a 4-difluoromethyl-4,5-dihydro-3-methyl-1,2,4-triazol-5(1H)-on-1-yl, a 5,6,7,8-tetrahydro-1H,3H-[1,3,4]thiadiazolo[3,5-a]pyridazineimin-1-yl, or a 1,6,8-triazabicyclo[4.3.0]-nonane-7,9-dion-8-yl ring attached at the 7 position of a benzofuran, benzoxazole, indole, 2,3-dihydrobenzimidazole or benzimidazole, and X is selected from hydrogen, halogen, cyano, nitro, and amino. Preferred R groups are optionally substituted alkyl groups.Type: GrantFiled: April 12, 2000Date of Patent: March 5, 2002Assignee: FMC CorporationInventors: Scott D. Crawford, Lester L. Maravetz, George Theodoridis, Benjamin Dugan
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Patent number: 6342508Abstract: 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: August 17, 2000Date of Patent: January 29, 2002Assignee: American Cyanamid CompanyInventors: Aranapakam Mudumbai Venkatesan, George Theodore Grosu, Jamie Marie Davis, Derek Cecil Cole
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Patent number: 6310057Abstract: This invention relates to &agr;-ketoamide inhibitors of multicatalytic protease (MCP), to compositions including such inhibitors, and to methods for the use of MCP inhibitors. The MCP inhibitors of the present invention are useful, for example, to retard loss of muscle mass incident to various physiological states.Type: GrantFiled: March 7, 2000Date of Patent: October 30, 2001Assignee: Cephalon, Inc.Inventors: Sankar Chatterjee, John P. Mallamo
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Patent number: 6306873Abstract: This invention relates to compounds of general formula (I): in which Ar is a group selected from: A1, A2, B, C, D, E, Q1-Q3, R1-R9, Z1 and Z2 are as defined in the disclosure, and Y represents carboxy or an acid bioisostere. These compounds inhibit the production or physiological effects of TNF and inhibit cyclic AMP phosphodiesterase. The invention is also directed to pharmaceutical compositions comprising compounds of formula (I), their pharmaceutical use and methods for their preparation.Type: GrantFiled: July 20, 1999Date of Patent: October 23, 2001Assignee: Aventis Pharmaceuticals Products Inc.Inventors: Christopher J. Burns, Richard Labaudiniere, Stephen Condon, Robert D. Groneberg, Rose M. Mathew, Joseph M. Salvino
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Patent number: 6294573Abstract: Compounds having the formula are matrix metalloproteinase inhibitors. Also disclosed are matrix metalloproteinase-inhibiting compositions and methods of inhibiting matrix metalloproteinase in a mammal.Type: GrantFiled: January 27, 2000Date of Patent: September 25, 2001Assignee: Abbott LaboratoriesInventors: Michael L. Curtin, Yujia Dai, Steven K. Davidsen, Joseph F. Dellaria, Jr., Alan S. Florjancic, Jianchun Gong, Yan Guo, Howard R. Heyman, James H. Holms, Michael R. Michaelides, Jamie R. Stacey, Douglas H. Steinman, Carol K. Wada, Lianhong Xu
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Patent number: 6288063Abstract: Inhibitors for matrix metalloproteases, pharmaceutical compositions containing them, and a process for using them to treat a variety of physiological conditions. The compounds of the invention have the generalized formula (T)xA—B—D—E—G wherein A is an aryl or heteroaryl rings; B is an aryl or heteroaryl ring or a bond; each T is a substituent group; x is 0, 1, or 2; the group D represents the group E represents a two or three carbon chain bearing one to three substituent groups which are independent or are involved in ring formation, possible structures being shown in the text and claims; and the group G represents and with the proviso that when G is each of the substituents on E is an independent substituent; and include pharmaceutically acceptable salts thereof.Type: GrantFiled: May 27, 1998Date of Patent: September 11, 2001Assignee: Bayer CorporationInventors: Harold Clinton Eugene Kluender, David Ross Brittelli, William Riley Schoen, Sookhee Nicole Ha
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Patent number: 6277987Abstract: Compounds of formula wherein W is —OH or —NHOH; X is a heterocycle with the proviso that when X is a nitrogen containing heterocycle, the heterocycle is attached to the (CH2)m moiety by a ring nitrogen, —CONR2R3, —NR1COR2, —NR1SO2R2, —NR1CONR2R3, —NR1COOR4, heteroarylthio, alkylthio, arylalkylthio, heteroarylalkylthio, heterocycloalkylalkylthio, heterocycloalkylthio or arylthio; Y is carbon, nitrogen, oxygen or sulfur, provided that when Y is carbon, n is 2; Z is alkyl, aryl, alkoxy, aryloxy, aralkoxyaryl, aralkoxyheteroaryl, heteroaryl, heterocycloalkyl, heteroaryloxy, —CONR2R3, —NR1COR2, —NR1CONR2R3, —OCONR2R3, —NR1COOR4, or —SO2R2; R1 is hydrogen, alkyl, heterocycloalkylalkyl, aralkyl or heteroarylalkyl; R2 and R3 are independently R1, aryl or heteroaryl; or R2 and R3 taken together with the nitrogen atom to which they are attached form a 5- to 7-membered ring, which may optionally contain another heteroatType: GrantFiled: February 3, 1999Date of Patent: August 21, 2001Assignee: Novartis AGInventors: Paivi Jaana Kukkola, Leslie Anne Robinson, Motowo Nakajima, Junichi Sakaki
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Patent number: 6265432Abstract: Fluorine-substituted biphenyl butyric acid compounds and derivatives are described as well as acid methods for the preparation and pharmaceutical compositions of same, which are useful as inhibitors of matrix metalloproteinases, particularly gelatinase A, stromelysin-1, and collagenase-3, and for the treatment of atherosclerotic plaque rupture, aortic aneurism, heart failure, restenosis, periodontal disease, corneal ulceration, treatment of bums, decubital ulcers, wound healing, cancer, inflammation, pain, arthritis, osteoporosis, multiple sclerosis, renal disease, and other autoimmune or inflammatory disorders dependent upon tissue invasion by leukocytes or other activated migrating cells, acute and chronic neurodegenerative disorders including stroke, head trauma, spinal cord injury, Alzheimer's disease, amyotrophic lateral sclerosis, cerebral amyloid angiopathy, AIDS, Parkinson's disease, Huntington's disease, prion diseases, myasthenia gravis, and Duchenne's muscular dystrophy.Type: GrantFiled: February 11, 2000Date of Patent: July 24, 2001Assignee: Warner-LambertInventors: Claude Forsey Purchase, Jr., Bruce David Roth, Gerald Paul Schielke, Lary Craswell Walker, Andrew David White
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Patent number: 6239288Abstract: Biphenyl butyric acid compounds and derivatives are described as well as acid methods for the preparation and pharmaceutical compositions of same, which are useful as inhibitors of matrix metalloproteinases, particularly gelatinase A (72 kD gelatinase) and stromelysin-1 and for the treatment of multiple sclerosis, atherosclerotic plaque rupture, aortic aneurism, heart failure, restenosis, periodontal disease, corneal ulceration, treatment of bums, decubital ulcers, wound healing, cancer, inflammation, pain, arthritis, or other autoimmune or inflammatory disorders dependent upon tissue invasion by leukocytes or other activated migrating cells, acute and chronic neurodegenerative disorders including stroke, head trauma, spinal cord injury, Alzheimer's disease, amyotrophic lateral sclerosis, cerebral amyloid angiopathy, AIDS, Parkinson's disease, Huntington's disease, prion diseases, myasthenia gravis, and Duchenne's muscular dystrophy.Type: GrantFiled: March 2, 1999Date of Patent: May 29, 2001Assignee: Warner-Lambert CompanyInventors: Claude Forsey Purchase, Jr., Bruce David Roth, Gerald Paul Schielke, Lary Craswell Walker, Andrew David White
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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: 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: 6172085Abstract: A compound of the formula: wherein R1 and R2 each represents hydrogen, lower alkyl which may be substituted or acyl; R3, R4 and R5 each represents lower alkyl which may be substituted or lower alkoxy which may be substituted or R4 and R5 taken together represent a 5- or 6-membered carbocyclic group; R6 represents lower alkyl; Ar represents an aromatic group which may be substituted; ring A represents a 5- to 8-membered nitrogen-containing heterocyclic ring which may be substituted; X represents lower alkylene which may be substituted; Y represents carbon or nitrogen; Za represents CH2, COCH2, OCH2, SCH2, NHCH2, etc.; Zb represents a bond or a divalent aliphatic hydrocarbon group which may be substituted and may contain O, N or S; and m represents an integer of 1 to 3, or a salt thereof is useful for a pharmaceutical composition for modulating sodium channel.Type: GrantFiled: February 8, 1999Date of Patent: January 9, 2001Assignee: Takeda Chemical Industries, Ltd.Inventors: Shigenori Ohkawa, Tadatoshi Hashimoto, Kohji Fukatsu
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Patent number: 6169103Abstract: Fluorine-substituted biphenyl butyric acid compounds and derivatives are described as well as acid methods for the preparation and pharmaceutical compositions of same, which are useful as inhibitors of matrix metalloproteinases, particularly gelatinase A, stromelysin-1, and collagenase-3, and for the treatment of atherosclerotic plaque rupture, aortic aneurism, heart failure, restenosis, periodontal disease, corneal ulceration, treatment of burns, decubital ulcers, wound healing, cancer, inflammation, pain, arthritis, osteoporosis, multiple sclerosis, renal disease, and other autoimmune or inflammatory disorders dependent upon tissue invasion by leukocytes or other activated migrating cells, acute and chronic neurodegenerative disorders including stroke, head trauma, spinal cord injury, Alzheimer's disease, amyotrophic lateral sclerosis, cerebral amyloid angiopathy, AIDS, Parkinson's disease, Huntington's disease, prion diseases, myasthenia gravis, and Duchenne's muscular dystrophy.Type: GrantFiled: February 24, 1999Date of Patent: January 2, 2001Assignee: Warner-LambertInventors: Claude Forsey Purchase, Jr., Bruce David Roth, Gerald Paul Schielke, Lary Craswell Walker, Andrew David White
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Patent number: 6160126Abstract: Novel Intermediates ##STR1## wherein R is a substituted or unsubstituted hydrocarbon residue or acyl group; X is an electron withdrawing group; Y.sup.1 and Y.sup.2, which are the same or different, are each independently oxygen or sulfur; and A is a substituted or unsubstituted, divalent hydrocarbon residue have potent reactivity, this being useful in preparing guanidine derivatives.Type: GrantFiled: April 9, 1991Date of Patent: December 12, 2000Assignee: Takeda Chemical Industries, Ltd.Inventors: Yasuyuki Kando, Hideki Uneme, Isao Minamida
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Patent number: 6150416Abstract: The present invention provides non-peptide cathepsin D binding compounds and methods for using such compounds in the detection, labelling and inhibition of cathepsin D.Type: GrantFiled: February 3, 1998Date of Patent: November 21, 2000Assignee: The Regents of the University of CaliforniaInventors: Ellen K. Kick, Jonathan A. Ellman, Irwin D. Kuntz, Christina E. Lee, Guangcheng Liu, Diana C. Roe, A. Geoffrey Skillman
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Patent number: 6114372Abstract: Compounds of formula (I) having MMP and TNF inhibitory activity.Type: GrantFiled: October 2, 1998Date of Patent: September 5, 2000Assignee: Darwin Discovery LimitedInventors: Andrew Douglas Baxter, David Alan Owen, John Gary Montana, Robert John Watson, John Fraser Keily
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Patent number: 6090840Abstract: The subject invention concerns mercaptoalkylacyl compounds of formula (I): ##STR1## The compounds of the subject invention can be used to inhibit matrix metalloproteinases and/or TNF.alpha.- and L-selectin sheddase-mediated diseases including degenerative diseases and cancers. The subject invention also concerns methods of using the compounds of the invention to treat or prevent conditions associated with matrix metalloproteinases or that are mediated by TNF.alpha. or L-selectin sheddase.Type: GrantFiled: October 5, 1998Date of Patent: July 18, 2000Assignee: Darwin Discovery LimitedInventors: Andrew Douglas Baxter, David Alan Owen, John Gary Montana, Robert John Watson, John Fraser Keily
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Patent number: 6066743Abstract: A method for the solventless synthesis of a phthalimide or phthalimide mixture is provided comprising contacting at least one amine reactant and at least one anhydride reactant in a solventless environment at a first temperature sufficient to allow the reactants to at least partially condense; and increasing the temperature to a second temperature sufficient to melt the reaction mixture, thereby allowing the reaction to go essentially to completion and form the reaction product.Type: GrantFiled: May 7, 1999Date of Patent: May 23, 2000Assignee: General Electric CompanyInventors: Robert Joseph Nick, Mark Erik Nelson, Joseph John Caringi, Drew Elliot Williams
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Patent number: 6017889Abstract: Matrix metalloproteinase inhibiting compounds of formula (I), wherein X is a --CO.sub.2 H or --CONHOH group; and one of the groups proximate to the amide bonds is a steric bulky group, showing enhanced oral absorption.Type: GrantFiled: December 23, 1998Date of Patent: January 25, 2000Assignee: British Biotech Pharmaceuticals LimitedInventors: Raymond Paul Beckett, Mark Whittaker, Andrew Miller
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Patent number: 5994558Abstract: The invention provides methods for preparing a 2-isoxazoline compound represented by formula (1) and a 2,5-diamino-1,6-diphenyl-3-hydroxyhexane compound obtainable by reducing the 2-isoxazoline compound and represented by formula (6): ##STR1## wherein Ph is phenyl; and each of R.sup.1 and R.sup.2 independently represents hydrogen, acyl, alkyloxycarbonyl, arylalkyloxycarbonyl, aryloxycarbonyl, alkylaminocarbonyl, arylalkylaminocarbonyl, arylaminocarbonyl, alkyl, arylalkyl, aryl, alkylsulfonyl, acylalkylsulfonyl, or arylsulfonyl, or R.sup.1 and R.sup.2 are linked to each other to form divalent acyl. These compounds are useful as intermediates in the synthesis of medicines such as retrovirus protease inhibitors including human immunodeficiency virus (HIV) protease inhibitors.Type: GrantFiled: November 24, 1997Date of Patent: November 30, 1999Assignee: Daicel Chemical Industries, Ltd.Inventors: Yoshiyuki Murai, Masahiro Nishikawa, Yoichiro Ueda, Ichiro Takase
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Patent number: 5902791Abstract: Matrix metalloproteinase inhibiting compounds of formula (I), wherein X is a --CO.sub.2 H or --CONHOH group; and one of the groups proximate to the amide bonds is a steric bulky group, showing enhanced oral absorption.Type: GrantFiled: July 22, 1996Date of Patent: May 11, 1999Assignee: British Biotech Pharmaceuticals LimitedInventors: Raymond Paul Beckett, Mark Whittaker, Andrew Miller
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Patent number: 5872146Abstract: Described herein are compounds of formula (I): ##STR1## which have MMP and TNF inhibitory activity.Type: GrantFiled: April 4, 1997Date of Patent: February 16, 1999Assignee: Chiroscience LimitedInventors: Andrew Douglas Baxter, John Gary Montana, David Alan Owen
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Patent number: 5861427Abstract: Inhibitors for matrix metalloproteases, pharmaceutical compositions containing them, and a process for using them treat a variety of physiological conditions. The compounds of the invention have the generalized formula ##STR1## wherein each T is a substituent group; x is 0, 1, or 2; the group D represents ##STR2## the group R6 represents a variety of possible substituent groups on the carbon chain between D and G, and the group G represents M, ##STR3## in which M represents --CO.sub.2 H, --CON(R.sup.11).sub.2, or --CO.sub.2 R.sup.12 ; and R.sup.13 represents any of the side chains of the 19 noncyclic naturally occurring amino acids.Type: GrantFiled: May 30, 1997Date of Patent: January 19, 1999Inventors: Harold Clinton Eugene Kluender, Guenter Hans Herbert Heinz Benz, David Ross Brittelli, Brian Richard Dixon, Michael Christopher VanZandt, Scott McClelland Wilhelm, Donald John Wolanin
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Patent number: 5854277Abstract: Inhibitors for matrix metalloproteases, pharmaceutical compositions containing them, and a process for using them to treat a variety of physiological conditions. The compounds of the invention have the generalized formula ##STR1## wherein each T is a substituent group; x is 0, 1, or 2; the group D represents ##STR2## the group R6 represents a variety of possible substituent groups on the carbon chain between D and G, and the group G represents M, ##STR3## in which M represents --CO.sub.2 H, --CON(R.sup.11).sub.2, or --CO.sub.2 R.sup.12 ; and R.sup.13 represents any of the side chains of the 19 noncyclic naturally occurring amino acids.Type: GrantFiled: May 30, 1997Date of Patent: December 29, 1998Assignee: Bayer CorporationInventors: Harold Clinton Eugene Kluender, Guenter Hans Herbert Heinz Benz, William Harrison Bullock, Brian Richard Dixon, Michael Christopher VanZandt, Scott McClelland Wilhelm, Donald John Wolanin, Jill Elizabeth Wood, David Ross Brittelli
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Patent number: 5777117Abstract: Disclosed is a process for preparing compounds having a straight or branched aliphatic hydrocarbon structure of formula I: ##STR1## In formula I, n is an integer from one to four and m is an integer from four to twenty. Independently, R.sub.1 and R.sub.2 are hydrogen, a straight or branched chain alkyl, alkenyl or alkynyl of up to twenty carbon atoms in length or --(CH.sub.2).sub.w R.sub.5. If R.sub.1 or R.sub.2 is --(CH.sub.2).sub.w R.sub.5, w may be an integer from one to twenty and R.sub.5 may be an hydroxyl, halo, C.sub.1-8 alkoxyl group or a substituted or unsubstituted carbocycle or heterocycle. Alternatively, R.sub.1 and R.sub.2 may jointly form a substituted or unsubstituted, saturated or unsaturated heterocycle having from four to eight carbon atoms, N being a hetero atom of the resulting heterocyle. R.sub.3 may be either hydrogen or C.sub.1-3. In the compounds, a total sum of carbon atoms comprising R.sub.1 or R.sub.2, (CH.sub.2).sub.n and (CH.sub.2).sub.m does not exceed forty. R.sub.Type: GrantFiled: June 7, 1995Date of Patent: July 7, 1998Assignee: Cell Therapeutics, Inc.Inventors: J. Peter Klein, Gail E. Underiner, Anil M. Kumar
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Patent number: 5728845Abstract: Novel nitriles are inhibitors of tumor necrosis factor .alpha. and phosphodiesterase and can be used to combat cachexia, endotoxic shock, retrovirus replication, asthma, and inflammatory conditions. A typical embodiment is 3-Phthalimido-3-(3,4-dimethoxyphenyl)propionitrile.Type: GrantFiled: August 29, 1995Date of Patent: March 17, 1998Assignee: Celgene CorporationInventors: George W. Muller, Mary Shire
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Patent number: 5728844Abstract: Novel amides are inhibitors of TNF.alpha. and phosphodiesterase and can be used to combat cachexia, endotoxic shock, retrovirus replication, asthma, and inflammatory conditions. A typical embodiment is 3-phthalimido-3-(3-cyclopentyloxy-4-methoxyphenyl)propionamide.Type: GrantFiled: December 26, 1995Date of Patent: March 17, 1998Assignee: Celgene CorporationInventors: George W. Muller, Mary Shire
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Patent number: 5691366Abstract: A new nitro compound of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are each lower alkyl or lower alkoxy(lower)-alkyl, or ##STR2## is cyclized to form ##STR3## X is --O--, --S-- or --NH--, m is an integer 0 or 1, andR.sup.3 is carbamoyl, lower alkylcarbamoyl, lower alkanoyl, di-lower alkylaminosulfonyl, lower alkylsulfonyl, oxamoyl or a group of the formula: --(Y).sub.n --R.sup.4 wherein Y is --CO--, --SO.sub.2 --, --COCH.sub.2 -- or ##STR4## n is an integer of 0 or 1, and R.sup.4 is heterocyclic group which is optionally substituted with one or more substituents selected from lower alkyl, lower alkoxy, phenyl, carbamoyl, halogen, amino, lower alkylthio, hydroxy, lower alkylsulfonylamino and carbamoylmethyl, and pharmaceutically acceptable salt thereof, which are useful as vasodilators.Type: GrantFiled: October 31, 1995Date of Patent: November 25, 1997Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Masayuki Kato, Shigetaka Nishino, Mitsuko Hamano, Hisashi Takasugi
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Patent number: 5663337Abstract: The present invention relates to benzoquinazoline thymidylate synthase inhibitors, processes for preparing them and pharmaceutical formulations containing them.Type: GrantFiled: May 25, 1995Date of Patent: September 2, 1997Assignee: Glaxo Wellcome Inc.Inventors: William Pendergast, Scott Howard Dickerson
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Patent number: 5646147Abstract: Acaricidal, insecticidal and nematicidal substituted (hetero)arylalkyl ketone oxime O-ethers, processes for their preparation, agents containing them, and their use as pesticides.The invention relates to compounds of the formula ##STR1## in which Ar.sup.1 and Ar.sup.2 are aryl or heteroaryl, each of which is optionally substituted, and R is an optionally substituted aliphatic or alicyclic radical, to processes for their preparation, and to agents containing these compounds, and to their use for controlling animal pests.Type: GrantFiled: April 20, 1994Date of Patent: July 8, 1997Assignee: Hoechst AktiengesellschaftInventors: Birgit Kuhn, Gerhard Salbeck, deceased, Uwe Doller, Stefan Schnatterer, Hans-Herbert Schubert, Werner Knauf, Anna Waltersdorfer, Manfred Kern
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Patent number: 5610318Abstract: This invention is directed to a process for preparing a compound containing a persalt activators and salts thereof which are derived from imidocarboxylic acids and sulfimidocarboxylic acids of the formula I: ##STR1## in which A is a group of the formula ##STR2## n is the number 0, 1 or 2, R.sup.1 is hydrogen, chlorine, bromine, C.sub.1 -C.sub.20 -alkyl, C.sub.2 -C.sub.20 -alkenyl, aryl, or alkylaryl,R.sup.2 is hydrogen, chlorine, bromine, --SO.sub.3 M, --CO.sub.2 M or --OSO.sub.3 M, X is C.sub.1 -C.sub.19 -alkylene or arylene,B is a group of the formula C.dbd.O or SO.sub.2,L is a leaving group.Type: GrantFiled: May 31, 1995Date of Patent: March 11, 1997Assignee: Hoechst AktiengesellschaftInventors: Frank Jaekel, Gerd Reinhardt, Wolf-Dieter M uller
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Patent number: 5576445Abstract: Compounds of the formula ##STR1## in which the variables are as defined in the claims and which are suitable diazo components for the synthesis of fibre-reactive dyes are described.Type: GrantFiled: May 26, 1995Date of Patent: November 19, 1996Assignee: Ciba-Geigy CorporationInventors: Paul Herzig, Anton Andreoli
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Patent number: 5554633Abstract: Compounds of formula (I), and salts and prodrugs thereof, wherein Q is optionally substituted phenyl or benzhydryl; X and Y are each H or together form a group=O; Z is O, S or NR.sup.9, where R.sup.9 is H or C.sub.1-6 alkyl; R.sup.1 represents H or C.sub.1-6 alkyl; R.sup.2 represents C.sub.1-6 alkyl substituted by CONR.sup.7 (CH.sub.2).sub.p R.sup.8 (where R.sup.7 is H or C.sub.1-6 alkyl, R.sup.8 is optionally substituted heteroaryl and p is 0, 1, 2, 3, 4, 5 or 6); R.sup.3 represents H, C.sub.1-6 alkyl or C.sub.2-6 alkynyl; R.sup.4 represents H, C.sub.1-6 alkyl or optionally substitute phenyl; R.sup.5 represents optionally substituted phenyl; R.sup.6 is H or C.sub.1-6 alkyl; and q is 0, 1, 2 or 3; are tachykinin antagonists useful in therapy.Type: GrantFiled: January 27, 1995Date of Patent: September 10, 1996Assignee: Merck, Sharp & Dohme, Ltd.Inventor: Martin R. Teall
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Patent number: 5520844Abstract: Bleaching agents constituted by at least one imidearomatic (poly)peroxyacid, having the formula (I): ##STR1## wherein A represents a residue of a substituted or unsubstituted benzene or naphthalene ring, R is a hydrogen atom, a lower alkyl group, an OH group, a COOH group, a COOOH group or a COOR' group wherein R' represents a C.sub.1 -C.sub.5 alkyl group, and n is an integer from 1 to 5.Type: GrantFiled: January 4, 1991Date of Patent: May 28, 1996Assignee: Ausimont S.p.A.Inventors: Carlo Venturello, Claudio Cavallotti, Fulvio Burzio
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Patent number: 5514654Abstract: N-acyldipeptides of formula I ##STR1## wherein R represents a rest of formula ##STR2## and R.sub.4, Y, m, n and Z have the meaning as defined in the description, R.sub.1 represents hydrogen, a 1-10 C. alkyl, an optionally substituted methyl or benzyl,R.sub.2 represents a --CO--A group,wherein A has the meanings as defined in the description,R.sub.3 represents a --(CH.sub.2).sub.p --CO--W group,wherein p and W have the meaning as defined in the description.Type: GrantFiled: May 18, 1994Date of Patent: May 7, 1996Inventors: Slavko Pecar, Marija Sollner, Uros Urleb, Danijel Kikelj, Gasper Marc, Ales Krbavcic, Vlado Kotnik, Branka Wraber-Herzog, Sasa Simcic, Alojz Ihan, Lidija Klamfer, Lucka Povsic, Zdravko Kopitar, Anton Stalc
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Patent number: 5512682Abstract: Nitriles of formula ##STR1## wherein R3 is acetoxy or benzyloxycarbonyl, useful as intermediates in the production of beta-aminoalcohols.Type: GrantFiled: March 9, 1995Date of Patent: April 30, 1996Assignee: Hoffmann-La Roche Inc.Inventor: Hans Hilpert
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Patent number: 5510531Abstract: A Novel N-substituted peptidyl compound represented by the general formula (1): ##STR1## where R.sub.1 is a straight-chained or branched acyl group having 2-10 carbon atoms, a branched, cyclic or bridged cyclic alkyloxycarbonyl group having 4-15 carbon atoms; a benzyloxycarbonyl group which is unsubstituted or substituted with a halogen atom, nitro group or methoxy group; a 2,2,2-trichloroethyloxycarbonyl group, a 2-(trimethylsilyl)ethyloxycarbonyl group, a p-toluensulfonyl group, an o-nitrophenylsulfenyl group, a diphenylphosphonothioyl group, a triphenylmethyl group, a 2-benzoyl-1-methylvinyl group;R.sub.2 is a hydrogen atom or when taken together with R.sub.1, may form a phthaloyl group;R.sub.3 is an isobutyl group, a n-butyl group or an isopropyl group;R.sub.4 is a butyl group, andR.sub.5 is a hydrogen atom;provided that R.sub.1 can be an unsubstituted benzyloxycarbonyl group only when R.sub.3 is a n-butyl group.Type: GrantFiled: October 5, 1994Date of Patent: April 23, 1996Assignee: Suntory LimitedInventors: Naoki Higuchi, Masayuki Saitoh, Hiroshi Shibata
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Patent number: 5495023Abstract: A new nitro compound of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are each lower alkyl or lower alkoxy(lower)alkyl, or ##STR2## is cyclized to form ##STR3## X is --O--, --S-- or --NH--, m is an integer 0 or 1, andR.sup.3 is carbamoyl, lower alkylcarbamoyl, lower alkanoyl, di-lower alkylaminosulfonyl, lower alkylsulfonyl, oxamoyl or a group of the formula: --(Y).sub.n --R.sup.4whereinY is --CO--, --SO.sub.2 --, --COCH.sub.2 -- or ##STR4## n is an integer of 0 or 1, and R.sup.4 is heterocyclic group which is optionally substituted with one or more substituents selected from lower alkyl, lower alkoxy, phenyl, carbamoyl, halogen, amino, lower alkylthio, hydroxy, lower alkylsulfonylamino and carbamoylmethyl, and pharmaceutically acceptable salt thereof, which are useful as vasodilators.Type: GrantFiled: May 3, 1994Date of Patent: February 27, 1996Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Masayuki Kato, Shigetaka Nishino, Mitsuko Hamano, Hisashi Takasugi
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Patent number: 5495025Abstract: The compound of the formula, ##STR1## wherein R.sup.4 is hydrogen, lower-alkanoyl or benzyloxycarbonyl and R.sup.2 is lower-alkyl or acid-addition salts thereof, useful as intermediates in the production of beta-aminoalcohols.Type: GrantFiled: March 9, 1995Date of Patent: February 27, 1996Assignee: Hoffmann-La Roche Inc.Inventor: Hans Hilpert