Silicon Containing Patents (Class 546/14)
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Patent number: 6358976Abstract: This invention relates to novel fused heterocycles which are useful as antagonists of the &agr;v&bgr;3 and related integrin receptors, to pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of cell adhesion, the treatment of angiogenic disorders, inflammation, bone degradation, cancer metastasis, diabetic retinopathy, thrombosis, restenosis, macular degeneration, and other conditions mediated by cell adhesion and/or cell migration and/or angiogenesis.Type: GrantFiled: February 22, 2000Date of Patent: March 19, 2002Inventors: John Wityak, Aleksandra Ewa Tobin
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Publication number: 20020032174Abstract: The invention relates to polycyclic aryl and heteroaryl substituted 4 pyridone compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a variety of thrombotic conditions including coronary artery and cerebrovascular diseases.Type: ApplicationFiled: April 4, 2001Publication date: March 14, 2002Inventors: Michael S. South, Chun C. Ma, Kevin J. Koeller, Hayat K. Rahman, William L. Neumann
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Patent number: 6355636Abstract: This invention provides compounds of formula I having the structure useful as inhibitors of protein tyrosine kinase.Type: GrantFiled: April 18, 2000Date of Patent: March 12, 2002Assignee: American Cyanamid CompanyInventors: Allan Wissner, Philip R. Hamann, Ayako Yamashita
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Patent number: 6352997Abstract: The present invention provides for a method of treating polycystic ovary syndrome in a subject in need of such treatment comprising the administration of a therapeutically effective amount of a compound of structural formula I: to the subject. The present invention further provides for a method for improving fertility and the response to in vitro fertilization (I.V.F.), comprising administration of therapeutically effective amount of compound of structural formula I to the subject. Further, the present invention provides for compositions useful in the methods of the present invention, as well as a method of manufacture of a medicament useful for treating polycystic ovary syndrome or for improving fertility or the response to in vitro fertilization (I.V.F.).Type: GrantFiled: May 3, 1999Date of Patent: March 5, 2002Assignee: Merck & Co., Inc.Inventors: Joanne Waldstreicher, Georgianna S. Harris
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Patent number: 6350756Abstract: (20S) esters of camptothecin analogs are provided. The compounds are (20S) esters of an oxyalkanoic acid and camptothecin, which is optionally substituted at the 7, 9, 10, 11, and 12 positions of the camptothecin ring. The compounds are useful for treating cancer.Type: GrantFiled: March 1, 2001Date of Patent: February 26, 2002Assignee: California Pacific Medical CenterInventors: Li-Xi Yang, Xiandao Pan, Huijuan Wang
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Patent number: 6350827Abstract: Disclosed is a process for pressurizing ethylenically unsaturated monomers to 200-5000 bar in the absence of a polymerization initiator, which comprises effecting said pressurizing in the presence of nitroxyl compounds of the formula I where R1 and R2 are singly C1-C4-alkyl or combine with the joining carbon atom to form a 5- or 6-membered saturated hydrocarbon ring, R3 is C1-C4-alkyl, and R4 is hydrogen or C1-C12-alkyl. Also disclosed are a process for preparing copolymers by such pressurization and subsequent polymerization and copolymers obtainable thereby.Type: GrantFiled: December 2, 1999Date of Patent: February 26, 2002Assignee: BASF AktiengesellschaftInventors: Heinz Friedrich Sutoris, Andreas Deckers, Wilhelm Weber
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Publication number: 20020010155Abstract: A process for the preparation of a 4-aryl-3-oxymethyl-piperidine of structure (1) 1Type: ApplicationFiled: August 3, 2001Publication date: January 24, 2002Applicant: SmithKline Beecham p.l.c.Inventors: Mark Jason Hughes, John Kitteringham, Victor Witold Jacewicz, Gillian Elizabeth Smith, Martyn Voyle, Evgeny Shapiro
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Publication number: 20010051723Abstract: A (polycyclic secondary-amino)dialkoxysilane favorably employable as a catalyst for polymerization of &agr;-olefin can be prepared by reacting tetrachlorosilane or a mono (C1-C8) alkyltrichlorosilane with a polycyclic secondary-amine in a non-hydrous, non-alcoholic organic solvent in the presence of a hydrogen chloride-trapping reagent, to produce a (polycyclic secondary-amino) chlorosilane and reacting the (polycyclic secondary-amino) chlorosilane with an alkali metal alkoxide or an alkaline earth metal alkoxide in the presence of a lower alcohol.Type: ApplicationFiled: June 12, 2001Publication date: December 13, 2001Applicant: Ube Industries, Ltd.Inventors: Hiroyuki Ikeuchi, Yasuhisa Sakakibara, Masayoshi Oue
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Patent number: 6323355Abstract: A high-efficiency organic luminous element by which blue luminescence with high luminance and high color purity becomes possible, which comprises at least one compound represented by general formula (A): wherein Ra, Rb, Rc and Rd each represents a hydrogen atom or a substituent group, with the proviso that at least one substituent group of Ra, Rb, Rc and Rd is a group represented by general formula (B): wherein Re and Rf each represents a hydrogen atom or a substituent group, and Ara represents an aryl group, a heteroaryl group or an alkenyl group; and when at least two substituent groups of Ra, Rb, Rc and Rd are groups represented by general formula (B), the groups represented by general formula (B) may be the same or different.Type: GrantFiled: February 20, 2001Date of Patent: November 27, 2001Assignee: Fuji Photo Film Co., Ltd.Inventor: Tatsuya Igarashi
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Publication number: 20010039358Abstract: Compounds of formulaType: ApplicationFiled: February 6, 2001Publication date: November 8, 2001Inventors: Zhimin Hao, John S. Zambounis, Abul Iqbal
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Publication number: 20010039345Abstract: Novel compounds comprising a C—C double bond substituted at one carbon with two oxygen or sulfur atom-containing groups are disclosed. The compounds are useful in methods and compositions for generating chemiluminescence by reaction with a peroxidase enzyme and a peroxide. The chemiluminescence thus produced can be used as a detectable signal in assays for peroxidase enzymes and in assays employing enzyme-labeled specific binding pairs.Type: ApplicationFiled: April 11, 2001Publication date: November 8, 2001Inventors: Hashem Akhavan-Tafti, Zahra Arghavani, Renuka DeSilva
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Patent number: 6310211Abstract: The present invention provides for 8-hydroxy-7-substituted quinoline compounds such as formula IA These compounds are useful as anti-viral agents. Specifically, these compounds have anti-viral activity against the herpes virus, cytomegalovirus (CMV). Many of these compounds are also active against other herpes viruses, such as the varicella zoster virus, the Epstein-Barr virus, the herpes simplex virus and the human herpes virus type 8 (HHV-8).Type: GrantFiled: September 5, 1997Date of Patent: October 30, 2001Assignee: Pharmacia & Upjohn CompanyInventors: Valerie Ann Vaillancourt, Karen Rene Romines, Arthur Glenn Romero, John Alan Tucker, Joseph Walter Strohbach, Olivier Bezencon, Suvit Thaisrivongs
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Patent number: 6307083Abstract: Silane compounds represented by formula (1), a synthesis method thereof, luminescent device materials comprising such silane compounds, and luminescent devices containing such materials: wherein each of R1 and R2 groups represents an aryl group containing no alkenyl substituent, or a heteroaryl group containing no alkenyl substituent; each of R3, R4, R5 and R6 groups represents a hydrogen atom or a substituent group; each of R7 and R8 groups represents an aryl group or a heteroaryl group; and each of Ar1 and Ar2 groups represents an arylene group or a heteroarylene group; provided that the compound represented by the formula (1) takes neither polymeric nor oligomeric form and the case is excluded therefrom wherein all or three of R1 R2, Ar1 and Ar2 groups have heteroaryl structures.Type: GrantFiled: April 4, 2000Date of Patent: October 23, 2001Assignee: Fuji Photo Film Co., Ltd.Inventor: Tatsuya Igarashi
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Patent number: 6306839Abstract: The present invention provides novel 2-methoxyimino-2-(pyridinyloxymethyl)phenyl acetamide compounds with (derivatised) hydroxyalkyl substituents on the pyridine ring, their use as fungicidal compounds, and their use in fungicidal compositions comprising at least one of the 2-methoxyimino-2-(pyridinyloxymethyl)phenyl acetamide compounds as the active ingredient.Type: GrantFiled: September 16, 1999Date of Patent: October 23, 2001Assignee: Dow AgroSciences LLCInventors: Emily J. Canada, Robert P. Gajewski, Christopher S. Galka, Neil V. Kirby, Irene M. Morrison, Jeannie R. Phillips, Mary E. Pieczko, Brent J. Rieder, Chrislyn M. Carson, Zhengyu Huang
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Patent number: 6281221Abstract: The invention relates to novel substituted 1,3-dioxan-5-ylamino-heterocyclic compounds of the formula in which A is CH or N; X is NH, O or S(O)q, where q=0-2; Y is O or S(O)m, where m=0-2, and R1, R2, R3, R4, R4′ and R5 have the meanings given in the description, processes for their preparation and their use as pest control compositions and fungicides.Type: GrantFiled: September 25, 1998Date of Patent: August 28, 2001Assignee: Hoechst Scering AgrEvo GmbHInventors: Wolfgang Schaper, Werner Knauf, Ulrich Sanft, Manfred Kern, Heinz Ehrhardt, Adolf Heinz Linkies, Dieter Bernd Reuschling, Werner Bonin
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Patent number: 6271377Abstract: Hindered amines substituted on the N-atom with an —O—E—OH moiety are particularly effective in stabilizing polyolefin and automotive coating compositions against the deleterious effects of oxidative, thermal and actinic radiation where the presence of the OH group on the compounds adds important properties not attainable by the use of normal —O—E moieties.Type: GrantFiled: February 25, 1999Date of Patent: August 7, 2001Assignee: Ciba Specialty Chemicals CorporationInventors: James P. Galbo, Gerald A. Capocci, Nancy N. Cliff, Robert E. Detlefsen, Michael P. DiFazio, Ramanathan Ravichandran, Peter Solera
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Patent number: 6268381Abstract: The present invention relates to taxane derivatives each represented by the following formula (1): [wherein, A1 represents a group (in which R1 represents H or a (substituted) alkyl group) or a group (in which R2 represents an amino group, a mono- or di-alkylamino group, a piperidino group, a pyrrolidino group or a morpholino group), X represents H, an alkoxycarbonyl group or a benzoyl group, Y represents H or a trialkylsilyl group, A2 represents a furyl group, an alkylfuryl group, an alkyl group or a fluorophenyl group, Ac represents an acetyl group, and Bz represents a benzoyl group] or salts thereof; and drugs containing the same as an active ingredient. These compounds have excellent water solubility and antitumor activity.Type: GrantFiled: June 19, 2000Date of Patent: July 31, 2001Assignee: Kabushiki Kaisha Yakult HonshaInventors: Hideaki Shimizu, Atsuhiro Abe, Takanori Ogawa, Hiroshi Nagata, Seigo Sawada
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Patent number: 6262065Abstract: Compound of the formula (I): wherein: R is defined in the specification; each R′, independently of the other, is H, acetyl, benzyl, methoxymethyl, tosyl, mesyl, trifluoromesyl, tri(C1-4 alkyl)silyl, di(C1-4 alkyl)phenylsilyl, diphenyl(C1-4 alkyl)silyl, or triphenylsilyl, or both R together from an alkylidene protecting group; R″ is H, acetyl, benzyl, methoxymethyl, tosyl, mesyl, trifluoromesyl, tri(C1-4 alkyl)silyl, di(C1-4 alkylsilyl)phenylsilyl, diphenyl(C1-4 alkyl)silyl, or triphenylsilyl; X is H, Cl, Br, or R4 (where R4 is C1-22-alkyl); Y is H, Cl, Br, or —CHR2OH, —CR2R3OH, —CH2CHR2OH, —CH2CR2R3OH, —SR2, —SeR2, —OH, —NH2, —R5 (where R2, R3, and R5 are independently of each other C1-22-alkyl); or X and Y together form a covalent bond; A and A′ are both H or together A and A′ form ═O, are useful as anticancer agents and as glycosidase inhibitors.Type: GrantFiled: August 6, 1998Date of Patent: July 17, 2001Assignee: The Regents of the University of MichiganInventors: William H. Pearson, Erik J. Hembre
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Patent number: 6262222Abstract: Copolymers containing N-vinyllactam derivatives protected at 3-position are provided and represented by the following formula. The copolymers are used as a photoresist material suitable for deep uv process so that high sensitivity and resolution can be obtained. In addition, ultrafine circuits can be formed and an exceptional improvement in PED stability can be accomplished by use of the photoresist.Type: GrantFiled: October 8, 1998Date of Patent: July 17, 2001Assignee: Hyundai Electronics Industries Co., Ltd.Inventors: Jin Baek Kim, Min Ho Jung, Jong Ho Cheong
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Patent number: 6255301Abstract: There is provided compounds of formula I, wherein R1, R2, R3, Rx, 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 as in thrombosis or as anticoagulants.Type: GrantFiled: July 14, 1997Date of Patent: July 3, 2001Assignee: AstraZeneca ABInventors: David Gustafsson, Jan-Erik Nyström
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Patent number: 6252078Abstract: A method of controlling Take-all disease of plants by applying, preferably to the seed prior to planting, a fungicide of the formula wherein Z1 and Z2 are C or N and are part of an aromatic ring selected from benzene, pyridine, thiophene, furan, pyrrole, pyrazole, thiazole, and isothiazole; A is selected from —C(X)-amine, —C(O)—SR3, —NH—C(X)R4, and —C(═NR3)—XR7; B is —Wm—Q(R2)3 or selected from o-tolyl, 1-naphthyl, 2-naphthyl, and 9-phenanthryl, each optionally substituted with halogen or R4; Q is C, Si, Ge, or Sn; W is —C(R3)pH(2−p)—; or when Q is C, W is selected from —C(R3)pH(2−p)—, —N(R3)mH(1−m)—, —S(O)p—, and —O—; X is O or S; n is 0, 1, 2, or 3; m is 0 or 1; p is 0, 1, or 2; each R is independently selected from a) halo, formyl, cyano, amino, nitro, thiocyanato, isothiocyanato, trimethylsilyl, and hydroxy; b) C1-C4 alkyl, alkenyl, alkynyl,Type: GrantFiled: September 28, 1998Date of Patent: June 26, 2001Assignee: Monsanto CompanyInventors: Dennis Paul Phillion, Diane Susan Braccolino, Matthew James Graneto, Wendell Gary Phillips, Karey Alan Van Sant, Daniel Mark Walker, Sai Chi Wong
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Patent number: 6235920Abstract: The present invention relates to a method for preparing a functional halosilanes by reacting A) a cyclic silyl ether having the formula wherein each R is independently selected from a hydrocarbyl group or a halogen-substituted hydrocarbyl group having 1 to 20 carbon atoms, each R′ is independently selected from a group consisting of hydrogen and R and b is 3, 4 or 5; and (B) a halogen-functional compound having a formula selected from wherein Q is a monovalent group having 2 to 20 carbon atoms selected from alkenyl groups, aralkenyl groups or a heterocyclic hydrocarbyl group having oxygen, nitrogen or sulfur hetero atoms in its ring, G is an m-valent organic group, m is at least 2, X is halogen, R″ is independently selected from hydrocarbyl groups or halogen-substituted hydrocarbyl groups having 1 to 20 carbon atoms, j is an integer having a value of 1 to 3 and k is an integer having a value of 1 to 3.Type: GrantFiled: July 19, 1999Date of Patent: May 22, 2001Assignee: Dow Corning CorporationInventors: Michael Kang-Jen Lee, Aroop Kumar Roy
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Patent number: 6225489Abstract: Phospholipid compositions that may be represented by the following general formula: wherein: A is selected from H, M, and R—Y—; A1 is selected from H, OH, OM and R—Y—O—; x is 0 or an integer from 1 to 5; M is a cation; Y is alkylene or substitued alkylene; and R is a mixture of quaternized amidoamine and/or amine moieties selected from the group consisting of: a) a quaternized organosilicone amidoamine moiety of the formula: b) a quaternized organosilicone tertiary amine moiety of the formula: or a mixture of the quaternized organosilicone amidoamine moiety “a” and/or quaternized tertiary amine moiety “b” above and the moieties: c) a quaternized organic amidoamine moiety of the formula: d) an organic quaternized tertiary amine moiety of the formula: with the proviso that wherein R is a mixture of organosilicone amine and organic amine moieties, at leastType: GrantFiled: December 16, 1994Date of Patent: May 1, 2001Assignee: Mona Industries, Inc.Inventors: Dennis L. Fost, Abe Berger
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Patent number: 6214996Abstract: Naphthalene derivatives of the formula [I]: wherein R1 and R2 are the same or different and are each H, protected or unprotected OH, one of R3 and R4 is protected or unprotected hydroxymethyl, and the other is H, lower alkyl, or protected or unprotected hydroxymethyl, R5 and R6 are, the same or different and are each H, substituted or unsubstituted lower alkyl, substituted or unsubstituted phenyl or protected or unprotected NH2, or both combine together with the adjacent N to form substituted or unsubstituted heterocyclic group, and pharmaceutically acceptable salts thereof, these compounds showing excellent bronchoconstriction inhibitory activity, and hence, being useful in the prophylaxis or treatment of asthma.Type: GrantFiled: December 1, 1998Date of Patent: April 10, 2001Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Tatsuzo Ukita, Katsuo Ikezawa, Shinsuke Yamagata
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Patent number: 6211371Abstract: A method of synthesizing compounds having the formula via a 4+1 radical annulation/cyclization wherein the precursor is reacted with an aryl isonitrile having the formula wherein X is selected from the group consisting of Br and I, ≡Y is ≡N or ≡C—R3, R1, R2, and R6 are independently hydrogen, a normal alkyl group, a branched alkyl group, an allyl group, a benzyl group, an alkynyl group, a propargyl group, an alkoxyl group, a halogen group, a trialkylsilyl group, an amino group, an alkyl amino group, a dialkylamino group, an aminoalkyl group, a cyano group, or R16CO—, wherein R16 is an alkyl group, an alkoxyl group, or an amino group, R3 is hydrogen, a normal alkyl group, a branched alkyl group, an allyl group, a benzyl group, an alkynyl group, a propargyl group, an alkoxyl group, a halogen group, a trialkylsilyl group, an amino group, an alkyl amino group, a dialkylamino group, an aminoalkyl group, a cyano group, or R16COType: GrantFiled: January 15, 1998Date of Patent: April 3, 2001Assignee: University of PittsburghInventors: Dennis P. Curran, Hubert Josien, Sung Bo Ko
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Patent number: 6211369Abstract: Spiro compounds of the formula (I), where X1, X2, X3, X4 are identical or different and are —S—, —O—, —NR5—, —CR5═N— or —CR5═CH—, with the proviso that at least one of the groups X1-4 is different from —CR5═CH—, are suitable as charge transport materials, in particular for photovoltaic cells, and as electroluminescence materials.Type: GrantFiled: January 3, 2000Date of Patent: April 3, 2001Assignee: Aventis Research & Technologies GmbH & Co. KGInventors: Josef Salbeck, Donald Lupo
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Patent number: 6211192Abstract: The present invention relates to alkynyl-substituted camptothecins of formula (I) wherein X, R1, R2 are as defined herein, and the pharmaceutically salts thereof. These compounds are useful in therapy as antitumor agents.Type: GrantFiled: August 12, 1999Date of Patent: April 3, 2001Assignee: Pharmacia & Upjohn S.p.A.Inventors: Ilaria Candiani, Angelo Bedeschi, Giuseppina Visentin, Maria Chiara Fagnola, Laura Capolongo
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Patent number: 6207832Abstract: A compound has the formula in racemic form, enantiomerically enriched form or enantiomerically pure form. R6 is preferably —Si(R8R9R10) or —(R7)Si(R8R9R10), wherein R7 is an alkylene group, an alkenylene group, or an alkynylene group; and R8, R9 and R10 are independently a C1-10 alkyl group, a C2-10 alkenyl group, a C2-10 alkynyl group, an aryl group or a —(CH2)NR11 group, wherein N is an integer within the range of 1 through 10 and R11 is a hydroxy group, alkoxy group, an amino group, an alkylamino group, a dialkylamino group, a halogen atom, a cyano group, —SRc or a nitro group. R1-R can be broadly substituted. R5 is preferably a C1-10 alkyl group, an alkenyl group, an alkynyl group, or a benzyl group. R13 is preferably H, F or —CH3. R16 is R16 is —C(O)Rf or H. The E-ring (the lactone ring) may be opened. A method of synthesis of compound (1) and intermediates in the synthesis thereof are provided.Type: GrantFiled: April 9, 1999Date of Patent: March 27, 2001Assignee: University of PittsburghInventors: Dennis P. Curran, Bom David, Thomas G. Burke
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Patent number: 6207846Abstract: The present invention provides an improved process and intermediate compounds for the preparation of di-fluorovinylsilane insecticidal and acaricidal agents of the formula I wherein Ar is phenyl, 1- or 2-napthyl or a 5- or 6-membered heteroaromatic ring, each of which may be optionally substituted by any combination of from one to three halogen, C1-C4alkyl, C1-C4haloalkyl, C1-C4alkoxy, C1-C4haloalkoxy, C(O)R2 or S(O)nR3 groups, R and R1 are each independently C1-C4 alkyl or C3-C5 cycloalkyl; Ar1 is phenoxyphenyl, phenyl, biphenyl; phenoxypyridyl, benzylpyridyl, benzylphenyl, 1- or 2- napthyl or a 5- or 6-membered heteroaromatic ring, each of which may be optionally substituted by any combination of from one to five halogen, C1-C4alkyl, C1-C4haloalkyl, C1-C4alkoxy, C1-C4haloalkoxy or C(O)R4 groups, n is an integer of 0, 1 or 2; R2 and R4 are each independently C1-C4alkyl, benzyl or phenyl; R3 is C114 C4alkyl or C1 -C4haloalkyl; and the fluorine atoms attached to the double bond are traType: GrantFiled: July 2, 1999Date of Patent: March 27, 2001Assignee: American Cyanamid Co.Inventors: Keith D. Barnes, Yulin Hu
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Patent number: 6204273Abstract: Compounds of the Formula I are inhibitors of the 5&agr;-reductase 1 isozyme, and are useful alone, or in combination with a 5&agr;-reductase 2 inhibitor, for the treatment of androgenic sensitive disorders such as acne vulgaris, seborrhea, female hirsutism, male pattern baldness, and benign prostatic hyperplasia.Type: GrantFiled: January 29, 1999Date of Patent: March 20, 2001Assignee: Merck & Co., Inc.Inventors: Philippe L. Durette, William K. Hagmann, Thomas J. Lanza, Jr., Soumya P. Sahoo, Gary H. Rasmusson, Richard L. Tolman, Derek Von Langen
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Patent number: 6174940Abstract: The present invention relates to mixtures comprising the compound I in a proportion of 65-95% by weight, the compound II in a proportion of 5-35% by weight and the compound III in a proportion of 0-10% by weight wherein the substituents are as defined in the description, and to mixtures with other compounds. The mixtures are suitable for stabilizing organic material against the effect of light and heat.Type: GrantFiled: August 13, 1998Date of Patent: January 16, 2001Assignee: Clariant GmbHInventors: Thomas St{umlaut over (a)}hrfeldt, Mathias Mehrer, Matthias Z{umlaut over (a)}h, Gerhard Pfahler
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Patent number: 6169080Abstract: This invention relates to novel derivatives of camptothecin, and will, particularly to derivatives having a substitution at the C-7 position, or at one of the C-9, C-10, C-11 or C-12 positions, or to disubstituted derivatives having a first substitution at C-7 and a second at one of C-9, C-10, C-11 or C-12. The invention also includes methods of using the compounds as Topoisomerase I inhibitors to treat patients with cancer. The invention also includes pharmaceutical formulations which consist of the novel compounds in solution or suspension with one or more pharmaceutical excipients or dilutes.Type: GrantFiled: February 11, 1998Date of Patent: January 2, 2001Assignee: BioNumerik Pharmaceuticals, Inc.Inventors: Frederick H. Hausheer, Kochat Haridas, P. Seetharamulu, Dasharatha G. Reddy, Shijie Yao, Pavankumar N.V. Petluru, Dhanabalan Murali
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Patent number: 6150343Abstract: The present invention provides generally a compound having the following general formula (1): ##STR1## wherein R.sup.1 and R.sup.2 are independently the same or different and are hydrogen, an alkyl group, an alkenyl group, a benzyl group, an alkynyl group, an alkoxyl group, an aryloxy group, an acyloxy group, a OC(O)OR.sup.d group, a carbamoyloxy group, a halogen, a hydroxyl group, a nitro group, a cyano group, an azido group, a formyl group, a hydrazino group, an acyl group, an amino group, --SR.sup.c, wherein, R.sup.c is hydrogen, an acyl group, an alkyl group, or an aryl group, or R.sup.1 and R.sup.2 together form a group of the formula --O(CH.sub.2).sub.n O-- wherein n represents the integer 1 or 2; R.sup.3 is H, F, a halogen atom, a nitro group, an amino group, a hydroxyl group, or a cyano id group; or R.sup.2 and R.sup.3 together form a group of the formula --O(CH.sub.2).sub.n O-- wherein n represents the integer 1 or 2; R.sup.4 is H, F, a C.sub.1-3 alkyl group, a C.sub.2-3 alkenyl group, a C.sub.Type: GrantFiled: August 29, 1997Date of Patent: November 21, 2000Assignee: University of PittsburghInventors: Dennis P. Curran, Hubert Josien, Bom David
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Patent number: 6136978Abstract: A compound and a method of synthesizing a compound having the following general formula (1): ##STR1## wherein R.sup.1 and R.sup.2 are independently the same or different and are hydrogen, an alkyl group, an alkenyl group, a benzyl group, an alkynyl group, an alkoxy group, an aryloxy group, an acyloxy group, --OC(O)OR.sup.d, wherein R.sup.d is an alkyl group, a carbamoyloxy group, a halogen, a hydroxy group, a nitro group, a cyano group, an azido group, a formyl group, a hydrazino group, an acyl group, an amino group, --SR.sup.c, wherein, R.sup.c is hydrogen, an acyl group, an alkyl group, or an aryl group, or R.sup.1 and R.sup.2 together form a group of the formula --O(CH.sub.2).sub.n O-- wherein n represents the integer 1 or 2; R.sup.3 is H, F, a halogen atom, a nitro group, an amino group, a hydroxy group, or a cyano group; or R.sup.2 and R.sup.3 together form a group of the formula --O(CH.sub.2).sub.n O-- wherein n represents the integer 1 or 2; R.sup.4 is H, a trialkylsilyl group, F, a C.sub.Type: GrantFiled: December 15, 1998Date of Patent: October 24, 2000Assignee: University of PittsburghInventors: Dennis P. Curran, Hubert Josien, David Bom, Thomas G. Burke
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Patent number: 6133446Abstract: Novel aromatic bicyclic amines of formula (I) ##STR1## are useful in treating central nervous system disorders and cardiac arrhythmias and cardiac fibrillation.Type: GrantFiled: January 28, 1999Date of Patent: October 17, 2000Assignee: Pharmacia & Upjohn CompanyInventors: Ruth E. TenBrink, Michael D. Ennis, Chiu-Hong Lin, Robert A. Lahti, Arthur G. Romero, John C. Sih
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Patent number: 6130180Abstract: An aminosilane of the formula: ##STR1## where R.sub.1 is a linear or branched C.sub.1-22 alkyl or C.sub.3-22 cycloalkyl, which may be substituted with at least one halogen atom; R.sub.2 is a bis(linear or branched C.sub.1-22 alkyl or C.sub.3-22 cycloalkyl)amino, a substituted piperidinyl, a substituted pyrrolidinyl, decahydroquinolinyl, 1,2,3,4-tetrahydroquinolinyl or 1,2,3,4-tetrahydroisoquinolinyl, with the substituent selected from the group consisting of C.sub.1-8 alkyl, pheny. C.sub.1-8 linear or branched alkylsubstituted phenyl and trimethylsilyl, with the proviso that when the substituent is C.sub.1-8 alkyl, there must be at least two such substituent groups present and R.sub.1 must contain halogen; and R.sub.3 is a linear or branched C.sub.1-8 alkyl or C.sub.3-8 cycloalkyl.Type: GrantFiled: December 23, 1997Date of Patent: October 10, 2000Assignee: Montell North America Inc.Inventors: Constantine A. Stewart, Eric J. Evain
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Patent number: 6130231Abstract: This invention relates to novel fused heterocycles which are useful as antagonists of the .alpha..sub.v .beta..sub.3 and related integrin receptors, to pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of cell adhesion, the treatment of angiogenic disorders, inflammation, bone degradation, cancer metastasis, diabetic retinopathy, thrombosis, restenosis, macular degeneration, and other conditions mediated by cell adhesion and/or cell migration and/or angiogenesis.Type: GrantFiled: November 26, 1997Date of Patent: October 10, 2000Assignee: DuPont PharmaceuticalsInventors: John Wityak, Aleksandra Ewa Tobin
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Patent number: 6124457Abstract: The instant invention relates to intermediates of Formula II, ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are as defined in the specification, and to processes for preparing such intermediates. This invention also relates to processes for preparing compounds of Formula III, ##STR2## and enantiomers thereof, wherein R.sup.2, R.sup.3 and R.sup.4 are as defined in the specification. Compounds of Formula II and Formula III are intermediates in the preparation of a potent .beta..sub.3 adrenergic receptor agonist. The instant invention also relates to processes for preparing the .beta..sub.3 adrenergic receptor agonist using the compounds of Formula II and Formula III.Type: GrantFiled: January 20, 2000Date of Patent: September 26, 2000Assignee: Pfizer Inc.Inventors: Keith M. DeVries, Jeffrey W. Raggon, Ravi M. Shanker, Frank J. Urban, Brian C. Vanderplas
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Patent number: 6110914Abstract: A compound of formula ##STR1## wherein n is 0 or 1; m is 0 or 1; p is 0 or 1; X is oxygen or sulfur; Y is CH, N or NO; W is oxygen, H.sub.2 or F.sub.2 ;A is N or C(R.sup.2); G is N or C(R.sup.3); D is N or C(R.sup.4);with the proviso that no more than one of A, G, and D is nitrogen, but at least one of Y, A, G, and D is nitrogen or NO;R.sup.1 is hydrogen or C.sub.1 to C.sub.4 alkyl;R.sup.2, R.sup.3, and R.sup.4 are independently hydrogen, halogen, C.sub.1 -C.sub.4 alkyl, C.sub.2 -C.sub.4 alkenyl, C.sub.2 -C.sub.4 alkynyl, aryl, heteroaryl, OH, OC.sub.1 -C.sub.4 alkyl, CO.sub.2 R.sup.1, --CN, --NO.sub.2, --NR.sup.5 R.sup.6, --CF.sub.3, --OSO.sub.2 CF.sub.3 or R.sup.2 and R.sup.3, or R.sup.3 and R.sup.4, respectively, may together form another six membered aromatic or heteroaromatic ring sharing A and G, or G and D, respectively, containing between zero and two nitrogen atoms, and substituted with one to two of the following substituents: independently hydrogen, halogen, C.sub.1 -C.sub.4 alkyl, C.sub.2 -C.sub.Type: GrantFiled: October 29, 1998Date of Patent: August 29, 2000Assignee: Astra AktiebolagInventors: Eifion Phillips, Robert Mack, John Macor, Simon Semus
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Patent number: 6096771Abstract: An isoxazole compound having the following formula: ##STR1## wherein R.sup.1 represents hydrogen, halogen, alkyl, alkoxy, hydroxyl, alkylthio, amino, alkanoyl, alkanoylamino, alkanoyloxy, alkoxycarbonyl, carboxy, (alkylthio)thiocarbonyl, carbamoyl, nitro or cyano; R.sup.2 represents an amino; m is 2 or 3; n is 1 to 6; ring A represents a phenyl ring, a naphthyl ring or an aromatic heterocycle; and X represents oxygen or sulfur. The isoxazole compound has an excellent monoamine oxidase inhibitory activity, and is useful for treating Parkinson's disease, depression and Alzheimer's disease.Type: GrantFiled: February 3, 1999Date of Patent: August 1, 2000Assignee: Sankyo Company, LimitedInventors: Koichi Kojima, Junichi Sakai, Yuichi Aizawa, Naozumi Samata, Masao Kozuka, Kenji Yoshimi, Isao Kaneko, Kazuo Koyama
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Patent number: 6096895Abstract: Compounds of Formula I, and their N-oxides and agriculturally suitable salts, are disclosed which are useful as fungicides ##STR1## In said formula, E is a ring system selected from certain 5- to 12-membered monocyclic and fused bicyclic aromatic heterocyclic ring systems, or an optionally substituted naphthalene ring as defined in the disclosure;A is O; S; N; NR.sup.5 ; or CR.sup.14 ;G is C or N; provided that when G is C, then A is O, S or NR.sup.5 and the floating double bond is attached to G; and when G is N, then A is N or CR.sup.14 and the floating double bond is attached to A;W is O; S; NH; N(C.sub.1 -C.sub.6 alkyl); or NO(C.sub.1 -C.sub.6 alkyl);X is OR.sup.1 ; S(O).sub.m R.sup.1 ; or halogen;R.sup.1 is C.sub.1 -C.sub.6 alkyl; C.sub.1 -C.sub.6 haloalkyl; C.sub.2 -C.sub.6 alkenyl; C.sub.2 -C.sub.6 haloalkenyl; C.sub.2 -C.sub.6 alkynyl; C.sub.2 -C.sub.6 haloalkynyl; C.sub.3 -C.sub.6 cycloalkyl; C.sub.2 -C.sub.4 alkylcarbonyl; or C.sub.2 -C.sub.4 alkoxycarbonyl;R.sup.2 is H; C.sub.1 -C.sub.6 alkyl; C.Type: GrantFiled: November 13, 1997Date of Patent: August 1, 2000Assignee: E. I. du Pont de Nemours and CompanyInventors: Richard James Brown, Dilon Jancey Daniel, Deborah Ann Frasier, Michael Henry Howard, Jr., Gerard Michael Koether, Morris Padgett Rorer
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Patent number: 6090942Abstract: The instant invention relates to intermediates of Formula II, ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are as defined in the specification, and to processes for preparing such intermediates. This invention also relates to processes for preparing compounds of Formula III, ##STR2## and enantiomers thereof, wherein R.sup.2, R.sup.3 and R.sup.4 are as defined in the specification. Compounds of Formula II and Formula III are intermediates in the preparation of a potent .beta..sub.3 adrenergic receptor agonist. The instant invention also relates to processes for preparing the .beta..sub.3 adrenergic receptor agonist using the compounds of Formula II and Formula III.Type: GrantFiled: September 29, 1999Date of Patent: July 18, 2000Assignee: Pfizer Inc.Inventors: Keith M. DeVries, Jeffrey W. Raggon, Ravi M. Shanker, Frank J. Urban, Brian C. Vanderplas
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Patent number: 6083961Abstract: This invention relates to a heterocyclic compound of the formula: ##STR1## wherein a group of the formula: ##STR2## is a group of the formula: ##STR3## etc., X is O, S or N--R.sup.5,R.sup.1 is lower alkyl, etc.,R.sup.5 is hydrogen, lower alkyl, etc.,R.sup.2 is hydrogen, halogen, lower alkyl, etc.,R.sup.3 is halogen, lower alkyl, etc.,R.sup.4 is amino optionally having suitable substituent(s), andA is lower alkylene,and a salt thereof, to processes for preparation thereof, and to a pharmaceutical composition comprising the same for the prevention and/or the treatment of bradykinin or its analogues mediated diseases in human being or animals.Type: GrantFiled: February 3, 1997Date of Patent: July 4, 2000Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Teruo Oku, Hiroshi Kayakiri, Shigeki Satoh, Yoshito Abe, Yuki Sawada, Takayuki Inoue, Hirokazu Tanaka
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Patent number: 6080871Abstract: Compounds of formula (I) or (II) wherein R.sup.1 is C.sub.4 to C.sub.20 hydrocarbyl (in which one or more hydrogen atoms may be replaced by halogen, and up to three carbon atoms may be replaced by oxygen, nitrogen or sulphur atoms, provided that R.sup.1 does not contain an --O--O-- group), R.sup.2 is H or C.sub.1 to C.sub.3 alkyl, m is from 1 to 15, n is from 2 to 6, each X group is independently (a), or one X group is --N(R.sup.4)--, --O-- or --S-- and the remaining X groups are independently (a), wherein R.sup.3 is H, C.sub.1 to C.sub.6 alkyl, --CO.sub.2 R.sup.5, --CONR.sup.5.sub.2, --CR.sup.5.sub.2 OR.sup.6 or --OR.sup.5 (in which R.sup.5 and R.sup.6 are H or C.sub.1 to C.sub.3 alkyl), and R.sup.4 is H or C.sub.1 to C.sub.6 alkyl, each Y group is independently --C(R.sup.3)R.sup.4 --, or up to two Y groups are --N(R.sup.4)--, --O-- or --S-- and the remaining Y groups are independently --C(R.sup.3)R.sup.4 --, wherein R.sup.3 is as defined above, one R.sup.Type: GrantFiled: October 6, 1998Date of Patent: June 27, 2000Assignee: James Black Foundation LimitedInventors: Sarkis Barret Kalindjian, Nigel Paul Shankley, Matthew John Tozer, Iain Mair McDonald, Michael John Pether, Elaine Anne Harper, Gillian Fairfull Watt, Tracey Cooke, Caroline Minli Rachel Low
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Patent number: 6057303Abstract: Derivatives of Camptothecin are disclosed, particularly derivatives having multiple substitutions at the `A`, `B` and `E` rings thereof. The novel compounds are useful in treating a wide variety of susceptible tumors and are potent inhibitors of Topoisomerase I.Type: GrantFiled: October 20, 1998Date of Patent: May 2, 2000Assignee: BioNumerik Pharmaceuticals, Inc.Inventors: Kochat Haridas, Frederick H. Hausheer
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Patent number: 6054583Abstract: This invention relates to a process for preparing 2-substituted pyridines via metal halogen exchange with sec-butyllithium on optionally substituted 2-bromo or 2-iodopyridines. The resulting lithopyridine intermediate is reacted with an electrophile to provide the desired 2-substituted pyridine. The substitution of sec-butyllithium for n-butyllithium in such a process results in an enhanced yield and purity of the desired 2-substituted pyridine.Type: GrantFiled: May 5, 1999Date of Patent: April 25, 2000Assignee: Rohm and Haas CompanyInventors: Martha Jean Kelly, Damian Gerard Weaver
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Patent number: 6051678Abstract: Copolymers containing N-vinyllactam derivatives protected at 3-position are provided and represented by the following formula. The copolymers are used as a photoresist material suitable for deep uv process so that high sensitivity and resolution can be obtained. In addition, ultrafine circuits can be formed and an exceptional improvement in PED stability can be accomplished by use of the photoresist.Type: GrantFiled: March 13, 1997Date of Patent: April 18, 2000Assignee: Hyundai Electronics Industries Co., Ltd.Inventors: Jin Baek Kim, Min Ho Jung, Jong Ho Cheong
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Patent number: 6051713Abstract: Compounds of the formula ##STR1## wherein the symbols have the meaning described in the specification, have retinoid-like biological activity.Type: GrantFiled: December 17, 1998Date of Patent: April 18, 2000Assignee: Allergan Sales, Inc.Inventors: Min Teng, Tien T. Duong, Roshantha A. Chandraratna
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Patent number: 6037341Abstract: Compounds having potent antimicrobial effects over Gram-positive bacteria and Gram-negative bacteria, a high stability to .beta.-lactamases and DHP-I and a high safety for the human body and a process for producing the same. Carbapenem compounds represented by the following general formula (I) or salts thereof: ##STR1## wherein the ring A represents a 3- to 7-membered non-aromatic ring containing at least one nitrogen atom and optionally having a substituent other than R.sup.6 ; R.sup.1 represents hydrogen or methyl; R.sup.2 and R.sup.5 are the same or different and each represents hydrogen or a protecting group of the hydroxyl group; R.sup.3 represents hydrogen or a protecting group of the carboxyl group; R.sup.4 represents hydrogen, lower alkyl or a protecting group of the amino group; R.sup.6 represents: (1) hydrogen, (2) lower alkyl, optionally substituted by an optionally protected hydroxy, carbamoyl, formimidoyl, acetimidoyl or ##STR2## wherein R.sup.7 and R.sup.Type: GrantFiled: December 18, 1996Date of Patent: March 14, 2000Assignee: Eisai Co., Ltd.Inventors: Nobuaki Sato, Manabu Sasho, Atsushi Kamata, Takaaki Suzuki, Isao Sugiyama, Kanemasa Katsu, Takeshi Suzuki
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Patent number: RE37029Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: November 5, 1998Date of Patent: January 23, 2001Assignee: Aventis Pharmaceuticals Inc.Inventors: Joseph T. Strupczewski, Edward J. Glamkowski, Yulin Chiang, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegler