Polycyclo Ring System Which Contains The Hetero Ring As One Of The Cyclos Patents (Class 540/455)
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Patent number: 6984734Abstract: The present invention provides an oxidative coupling procedure that allows efficient synthesis of novel cyclo[n]pyrrole macrocycles. Therefore, the present invention provides cyclo[n]pyrroles where n is 6, 7, 8, 9, 10, 11, or 12, and derivatives, multimers, isomers, and ion and neutral molecule complexes thereof as new compositions of matter. A protonated form of cyclo[n]pyrrole displays a gap of up to 700 nm between strong Soret and Q-like absorption bands in the electronic spectrum, demonstrating no significant ground state absorption in the visible portion of the electronic spectrum. Uses of cyclo[n]pyrroles as separation media, nonlinear optical materials, information storage media and infrared filters are provided.Type: GrantFiled: February 26, 2003Date of Patent: January 10, 2006Assignee: Board of Regents, The University of Texas SystemInventors: Jonathan L. Sessler, Daniel Seidel, Frederic R. Bolze, Thomas Koehler
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Patent number: 6984635Abstract: Materials and methods are disclosed for regulation of biological events such as target gene transcription and growth, proliferation or differentiation of engineered cells.Type: GrantFiled: February 12, 1999Date of Patent: January 10, 2006Assignees: Board of Trustees of The Leland Stanford Jr. University, President and Fellows of Harvard CollegeInventors: Stuart L. Schreiber, Gerald R. Crabtree, Stephen D. Liberles
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Patent number: 6962992Abstract: The invention describes crown ether chelators, including crown ethers having the formula and aza-substituted and thia-substituted analogs thereof. These crown ethers are substituted by a dye moiety, a chemically reactive group, a conjugated substance, or a combination thereof. Chelators that are substituted by fluorescent dyes are particularly useful as indicators for metal cations, particularly Na+ and K+ ions, and particularly where binding of the target ion results in a change in the fluorescence properties of the indicator that can be correlated with the ion concentration. Methods are provided for utilizing reactive groups on the chelators for conjugation to dyes, lipids and polymers and methods for enhancing entry of the indicators into living cells.Type: GrantFiled: December 19, 2001Date of Patent: November 8, 2005Assignee: Molecullar Probes, Inc.Inventors: Vladimir V. Martin, Kyle R. Gee, Richard P. Haugland, Zhenjun Diwu
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Patent number: 6924277Abstract: Compounds having the general formula wherein R1a, R1b, R1c, X1, X2, R2, R3, R4, R5, R6, n, Y and Z are as defined in the specification, methods of using such compounds for the treatment of diseases and pharmaceutical composition comprising such compounds.Type: GrantFiled: September 27, 2001Date of Patent: August 2, 2005Assignee: AstraZeneca ABInventor: Peter Bernstein
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Patent number: 6911428Abstract: The present invention is directed to certain diaryl amide compounds as NS3-Serine protease inhibitors of hepatitis C virus.Type: GrantFiled: December 10, 2001Date of Patent: June 28, 2005Assignee: Schering CorporationInventors: Zhaoning Zhu, Zhong-Yue Sun, Srikanth Venkatraman, F. George Njoroge, Ashok Arasappan, Bruce A. Malcolm, Viyyoor M. Girijavallabhan, Raymond G. Lovey, Kevin X. Chen
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Patent number: 6903129Abstract: The invention relates to compounds of formulas wherein R1 and R2 are independently from each other lower alkoxy, lower alkenyloxy, benzyloxy, hydroxy, —OCH(CH3)OC(O)-lower alkyl or —OCH2C(O)N(R3)(R4), with the proviso that only one of R1 or R2 may be hydroxy; R3 and R4 are independently from each other and signify hydrogen, lower alkyl, lower alkenyl or cycloalkyl; or R1 and R2 form together with the carbon atom, to which they are attached the linking group X, wherein X is —O(CH2)nCH?CH(CH2)nO— or —O(CH2)mO—; n is 1, 2 or 3; and m is 4-8, or a pharmaceutically acceptable salt of said compound. Compounds of the present invention can be used for the treatment of diseases where Serum Amyloid P Component depletion has a beneficial effect, in particular in the treatment or prevention of central and systemic amyloidosis.Type: GrantFiled: December 2, 2002Date of Patent: June 7, 2005Assignee: Hoffman-La Roche Inc.Inventors: Joerg Huwyler, Roland Jakob-Roetne, Sonia Maria Poli
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Patent number: 6846814Abstract: Compounds having the general formula wherein R1a, R1b, R1c, R2, R3, R4, R5, R6, R7, R8, X1, X2, Y, Z and n are as defined in the specification, methods of using such compounds for the treatment of diseases and pharmaceutical composition comprising such compounds.Type: GrantFiled: April 5, 2001Date of Patent: January 25, 2005Assignee: Astra Zeneca ABInventors: Jeffrey Scott Albert, Peter Bernstein, Cyrus Ohnmacht, Jr., Keith Russell, Ashokkumar Bhikkappa Shenvi
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Patent number: 6841530Abstract: Disclosed are semi-synthetic methods for the preparation of Didemnin Analogs. The compounds of this type are illustrated in Formula (I).Type: GrantFiled: September 10, 2001Date of Patent: January 11, 2005Assignee: The Board of Trustees of the University of IllinoisInventors: Kenneth L. Rinehart, Alexandra J. Katauskas
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Publication number: 20040242553Abstract: Peripherally administered Brefeldin A and its analogs and derivatives are used to enhance learning and reverse memory dysfunction through induced long term potentiation in hippocampal issues.Type: ApplicationFiled: March 22, 2004Publication date: December 2, 2004Applicant: The Regents of the University of California a Oakland, California corporationInventors: Katumi Sumikawa, Ken-Ichi Ito, James L. McGaugh
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Patent number: 6821963Abstract: Phenylamino benzhydroxamic acid derivatives of formula (I) where R1, R2, R3, R4, R5, and R6 are hydrogen or substituent groups such as alkyl, and where R7 is hydrogen or an organic radical, are potent inhibitors of MEK and, as such, are effective in treating cancer and other proliferative diseases such as psoriasis and restenosis.Type: GrantFiled: June 4, 2002Date of Patent: November 23, 2004Assignee: Warner-Lambert CompanyInventors: Stephen Douglas Barrett, Alexander James Bridges, Annette Marian Doherty, David Thomas Dudley, Alan Robert Saltiel, Haile Tecle
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Publication number: 20040038872Abstract: The present invention relates to macrocyclic compounds, methods for making these compounds, pharmaceutical compositions and the therapeutic or prophylactic use of these compounds by administering said compounds to mammals to prevent or treat hepatitis C virus (HCV) infection.Type: ApplicationFiled: December 12, 2002Publication date: February 26, 2004Inventors: Jeffrey Allen Campbell, Andrew Charles Good
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Publication number: 20040029850Abstract: Compounds having the general formula 1Type: ApplicationFiled: March 26, 2003Publication date: February 12, 2004Inventor: Peter Bernstein
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Patent number: 6680311Abstract: The present invention provides cryptophycin compounds of Formula I that are useful in the treatment of neoplasms.Type: GrantFiled: February 25, 1998Date of Patent: January 20, 2004Assignees: Eli Lilly and Company, Wayne State University, University of HawaiiInventors: Rima S Al-Awar, William J Ehlhardt, Subbaraju V Gottumukkala, Michael J Martinelli, Eric D Moher, Richard E Moore, John E Munroe, Bryan H Norman, Vinod F Patel, James E Ray, Chuan Shih, John E Toth, Venkatraghavan Vasudevan
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Publication number: 20030236240Abstract: The present invention is macrocycles of the formula (X): 1Type: ApplicationFiled: June 13, 2002Publication date: December 25, 2003Inventors: Shon R. Pulley, James P. Beck, Ruth E. TenBrink, Jon S. Jacobs
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Patent number: 6656930Abstract: Certain aralkyl diazabicycloalkyl compounds are disclosed for treatment of CNS disorders, such as cerebral ischemia, psychosis, and convulsions.Type: GrantFiled: September 4, 2001Date of Patent: December 2, 2003Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Wayne D Bowen, Brian R. de Costa, Celia Dominguez, Xiao-Shu He, Kenner C. Rice
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Patent number: 6632929Abstract: A covalent conjugate of a 4′-hydroxyazobenzene-2-carboxylic acid derivative (HABA) and an avidin-type molecule, of the formula: wherein A is (CH2)n or —CH═CH—, wherein n is an integer from 0-10; B is (CH2)n wherein n is an integer from 2 to 10; m is zero or 1; and Av is the residue of an avidin-type molecule selected from the group comprising native egg-white avidin, recombinant avidin, deglycosylated avidins, bacterial streptavidin, recombinant streptavidin, truncated streptavidin and other derivatives of said avidin-type molecules. These HABAylated avidins are red colored in the quinone configuration and can be used in many applications in the avidin-biotin technology.Type: GrantFiled: August 7, 2001Date of Patent: October 14, 2003Assignee: Yeda Research and Development Co. LTDInventors: Meir Wilchek, Edward A Bayer, Heike Hofstetter, Margherita Morpurgo
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Publication number: 20030191089Abstract: The present invention relates to compounds useful in the treatment of cancer or other proliferative diseases represented by formula I: 1Type: ApplicationFiled: March 11, 2003Publication date: October 9, 2003Inventors: Alicia Regueiro-Ren, Soong-Hoon Kim
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Publication number: 20030158170Abstract: A compound having the general formula (I) and methods of using such compounds for the treatment of diseases and pharmaceutical composition comprising such compounds.Type: ApplicationFiled: October 2, 2002Publication date: August 21, 2003Inventors: Jeffrey Scott Albert, Peter Bernstein, Cyrus Ohnmacht Jr, Keith Russell, Ashokkumar Bhikkappa Shenvi
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Patent number: 6608027Abstract: The present invention covers macrocyclic compounds of formula I active in-vitro and in cellular assays against the NS3 protease of the hepatitis C virus. wherein W, R21, R22, R3, R4, D and A are as defined herein, or a pharmaceutically acceptable salts or ester thereof.Type: GrantFiled: January 16, 2001Date of Patent: August 19, 2003Assignee: Boehringer Ingelheim (Canada) LtdInventors: Youla S. Tsantrizos, Dale R. Cameron, Anne-Marie Faucher, Elise Ghiro, Nathalie Goudreau, Teddy Halmos, Montse Llinas-Brunet
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Patent number: 6593360Abstract: The invention relates to novel 15-membered 8a- and 9a-lactams from the class of 6-O-methyl-erythromycin A of general formula (I) their pharmaceutically acceptable addition salts with inorganic or organic acids and their hydrates, to intermediates for their preparation, to a process for their preparation, to their pharmaceutically acceptable addition salts with inorganic or organic acids, to their hydrates, to a process for the preparation of pharmaceutical compositions as well as to a use of pharmaceutical compositions for the treatment of bacterial infections.Type: GrantFiled: January 22, 2002Date of Patent: July 15, 2003Assignee: Pliva, farmaceutska industrija, dionicko drustvoInventors: Gorjana Lazarevski, Sulejman Alihod{haeck over (z)}ić, Gabrijela Kobrehel, Stjepan Mutak
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Publication number: 20030114420Abstract: Fused cyclic compounds, methods of using such compounds in the treatment of nuclear hormone receptor-associated conditions such as cancer and immune disorders, and pharmaceutical compositions containing such compounds.Type: ApplicationFiled: December 19, 2001Publication date: June 19, 2003Inventors: Mark E. Salvati, James Aaron Balog, Weifang Shan, Soren Giese
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Patent number: 6545038Abstract: The invention provides compounds of formula as described in the claims, or an optical isomer, diastereomer or enantiomer thereof, or a pharmaceutically-acceptable salt, or biohydrolyzable amide, ester, or imide thereof are useful as inhibitors of metalloproteases. Also disclosed are pharmaceutical compositions and methods of treating diseases, disorders and conditions characterized by metalloprotease activity using these compounds or the pharmaceutical compositions containing them.Type: GrantFiled: November 6, 2000Date of Patent: April 8, 2003Assignee: The Procter & Gamble CompanyInventors: Biswanath De, Stanislaw Pikul, Menyan Cheng, Neil Gregory Almstead, Randall Stryker Matthews, Michael George Natchus, Yetunde Olabisi Taiwo
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Patent number: 6489314Abstract: The present invention relates to 16-membered macrocyclic compounds. In one aspect of the present invention, compounds of the formula are provided wherein: R1, R2, R3, and R5 are each independently hydrogen, C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, aryl or alkylaryl; R4 is hydrogen, halogen, C1-C10 alkyl, C1-C10 hydroxyalkyl, C1-C10 haloalkyl, aryl, —C(═O)R6, —C(═O)OR6, —NR6R7 where R6 and R7 are each independently hydrogen, C1-C10 aliphatic, aryl or alkylaryl; W is O, NR8 where R8 is hydrogen, C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, aryl or alkylaryl; X is O, CH2 or a carbon-carbon double bond; Y is absent or a C1-C10 alkyl, C2-C10 alkenyl, or C2-C10 alkynyl; and Ar is aryl; provided that 10,11-dehydroepothilone C is excluded.Type: GrantFiled: April 3, 2001Date of Patent: December 3, 2002Assignee: Kosan Biosciences, Inc.Inventors: Gary Ashley, Brian Metcalf
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Patent number: 6468996Abstract: The present invention relates to compounds of the general formula (I) The compounds are useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR).Type: GrantFiled: October 19, 1999Date of Patent: October 22, 2002Assignees: Novo Nordisk A/S, Dr. Reddy's Research FoundationInventors: Lone Jeppesen, Paul Stanley Bury, Per Sauerberg
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Publication number: 20020147139Abstract: The present invention is directed to certain diaryl amide compounds as NS3-Serine protease inhibitors of hepatitis C virus.Type: ApplicationFiled: December 10, 2001Publication date: October 10, 2002Applicant: SCHERING CORPORATIONInventors: Zhaoning Zhu, Zhong-Yue Sun, Srikanth Venkatraman, F. George Njoroge, Ashok Arasappan, Bruce A. Malcolm, Viyyoor M. Girijavallabhan, Raymond G. Lovey, Kevin X. Chen
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Patent number: 6384014Abstract: Purified form of streptogramines, characterised in that it contains at least one component from group B streptogramines of general formula (I), wherein R1 is Me or Et, R2 is H or OH, and R3 is substituted benzyl of general formula (III), such that 1) if R2 is H, R is NR4R5, wherein one of R4 and R5 is H or an Me radical and the other is Me, and R′ is Cl or Br, or R is (C3-5)alkenyl if R4 and R5 are Me, or 2) R is H and R′ is halogen, alkylamino or dialkylamino, an ether-oxide residue, alkylthio, (C1-3)alkyl or trihalogenomethyl, or R is halogen, (C2-4)alkylamino, (C2-4)dialkylamino or methyl ethyl amino, pyrrolidino alkenyl alkyl amino, dialkylamino, an alkyl cycloalkylmethyl amino radical or in ether-oxide residue, alkylthio, alkylthiomethyl, (C1-6)alkyl, aryl or trihalogenomethyl, and R′ is H, or R is halogen, amino, alkylamino or dialkylamino, an ether-oxide residue, an alkylthio radical, (C1-6)alkyl or trihalogenomethyl and R′ is halogen, alkylamino or dialkylamino, an ether-oxideType: GrantFiled: March 10, 2000Date of Patent: May 7, 2002Assignee: Aventis Pharma S.A.Inventors: Pascal Anger, Jean-Claude Barriere, Bertrand Bonnavaud, Patrick Lefevre, Jean-Marc Paris, Denis Thibaut
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Patent number: 6358985Abstract: The present invention is directed to peptidomimetic macrocyclic compounds which inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.Type: GrantFiled: June 29, 1999Date of Patent: March 19, 2002Assignee: Merck & Co., Inc.Inventors: Neville J. Anthony, Ian M. Bell, Douglas C. Beshore, Terrence M. Ciccarone, S. Jane de Solms, Christopher J. Dinsmore, Gerald E. Stokker
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Patent number: 6288073Abstract: A compound selected from those of formula (I): in which: X and Y represent hydrogen, halogen, hydroxy, mercapto, cyano, nitro, alkyl, alkoxy, trihaloalkyl, optionally substituted amino, methylenedioxy, or ethylenedioxy, R1 represents hydrogen, or alkyl, R2 represents hydrogen, hydroxy, alkyl, alkoxy, alkylcarbonyloxy, or optionally substituted ammo, R3 and R4 represent hydrogen, or alkyl, A represents —CH═CH—, or —CH(R5)—CH(R6)— wherein R5 and R6 are as defined in the description, their isomers, N-oxides, and pharmaceutically-acceptable acid or base addition salts thereof, and medicinal products containing the same which are useful in the treatment of cancer.Type: GrantFiled: June 19, 2000Date of Patent: September 11, 2001Assignee: Adir et CompagnieInventors: Michel Koch, François Tillequin, Sylvie Michel, Ghanem Atassi, Alain Pierre, Bruno Pfeiffer, Pierre Renard
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Patent number: 6277839Abstract: The present invention relates to biphenylene lactams of Formula II which are ligands at the prostaglandin receptors, as well as a method for treating prostaglandin mediated diseases comprising administration to a patient in need of such a treatment of a non-toxic therapeutically effective amount of compound of Formula II, and the like.Type: GrantFiled: October 1, 1999Date of Patent: August 21, 2001Assignee: Merck Frosst Canada & Co.Inventors: Joseph G. Atkinson, Marc Labelle, Patrick Lacombe, Rejean Ruel
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Patent number: 6180619Abstract: A family of compounds capable of inhibiting the activity of prenyl transferases. The compounds are covered by the four following formulas Each of the R groups is defined in the disclosure.Type: GrantFiled: June 16, 1998Date of Patent: January 30, 2001Assignee: Biomeasure, IncorporatedInventor: Sun H. Kim
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Patent number: 6177551Abstract: The present invention provides for substituted metal chelating compounds in which at least two of the chelating atoms are nitrogen which are directly attached to aromatic rings and one or more of those nitrogen atoms has attached thereto a substituent other than hydrogen, and methods for making and using these compounds.Type: GrantFiled: May 12, 1999Date of Patent: January 23, 2001Assignee: NeoRx CorporationInventor: Sudhakar Kasina
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Patent number: 6147071Abstract: Novel compounds of the following general formula or salts thereof. ##STR1## wherein Ring M is a heterocyclic ring having --N.dbd.CC<, --CO--N< or --CS--N< as the partial structure --X . . . . . Y<; R.sup.a and R.sup.b are bonded to each other to form Ring A, or they are the same or different and represent, independently, a hydrogen atom or a substituent on the Ring M; Ring A and Ring B represent, independently, an optionally substituted homocyclic or heterocyclic ring, and at least one of them is optionally substituted heterocyclic ring; Ring C is optionally substituted homocyclic or heterocyclic ring; Ring Z is an optionally substituted ring; and n represents an integer of from 1 to 6, or a salt thereof, which has an excellent tachykinin receptor antagonistic effect, and their production, and pharmaceutical compositions.Type: GrantFiled: June 1, 1998Date of Patent: November 14, 2000Assignee: Takeda Chemical Industries, Ltd.Inventors: Hideaki Natsugari, Takenori Ishimaru, Takayuki Doi, Yoshinori Ikeura, Chiharu Kimura
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Patent number: 6124453Abstract: A novel class of macrolides in whichi) positions 2 to 6 inclusive of the macrocyclic ring are provided by a piperidazinyl carboxylic acid residue; and/orii) positions 7 to 9 inclusive of the macrocyclic ring are provided by an aromatic .alpha.-amino acid residue; and/oriii) positions 10 to 12 inclusive of the macrocyclic ring are provided by an aliphatic .alpha.-amino acid residue, preferably comprising two, or especially all three of the characteristic structural features i), ii) and iii), more especially a compound of formula IX ##STR1## is provided having immunosuppressant and antinflammatory properties and protected and ring-open forms thereof.Type: GrantFiled: December 24, 1996Date of Patent: September 26, 2000Assignee: Novartis AGInventors: Theodor Fehr, Lukas Oberer, Valerie Quesniaux Ryffel, Jean-Jacques Sanglier, Walter Schuler
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Patent number: 6107482Abstract: Novel macrocyclic compounds are constructed to include large cyclic structures that are interrupted by at least one ring system. Each interrupting ring system includes two bridgehead atoms. Bridgehead atoms are bonded to one or more bridges that interconnect one or more ring systems thereby forming a large cyclic structure. Located in each bridge are two or more nitrogenous moieties that are derivatized with chemical functional groups. The ring systems can include further nitrogenous moieties, either as ring atoms or on pendant groups attached to the ring. These can also be derivatized with chemical functional groups. The totality of the chemical functional groups imparts certain conformational and other properties to the macrocyclic compounds. In accordance with certain embodiments of the invention, libraries of such macrocyclic compounds are prepared utilizing permutations and combinations of the chemical functional groups and the nitrogenous moieties to build complexity into the library.Type: GrantFiled: September 19, 1997Date of Patent: August 22, 2000Assignee: Isis Pharmaceuticals, Inc.Inventors: Phillip Dan Cook, Haoyun An, Charles J. Guinosso, Pei-Pei Kung, Allister S. Fraser
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Patent number: 6069114Abstract: Compounds of the formula (I) and their salts ##STR1## in which R.sup.1 to R.sup.6, Y.sup.1, to Y.sup.2, Y.sup.3, m and n are as defined in claim 1 are suitable as herbicides and plant growth regulators. They can be prepared analogously to known processes using intermediates of the formula (V) (cf. claim 6).Type: GrantFiled: February 25, 1997Date of Patent: May 30, 2000Assignee: Hoechst Schering AgrEvo GmbHInventors: Klaus Lorenz, Klemens Minn, Lothar Willms, Klaus Bauer, Hermann Bieringer, Christopher Rosinger
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Patent number: 6025350Abstract: This invention relates to compounds of the formula ##STR1## and to pharmaceutically acceptable salts thereof. The compounds of formula 1 are potent antibacterial and antiprotozoal agents that may be used to treat various bacterial and protozoal infections and disorders related to such infections. The invention also relates to pharmaceutical compositions containing the compounds of formula 1 and to methods of treating bacterial and protozoal infections by administering the compounds of formula 1.Type: GrantFiled: July 29, 1998Date of Patent: February 15, 2000Assignee: Pfizer Inc.Inventors: Hiroko Masamune, Wei-Guo Su, Bingwei V. Yang
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Patent number: 6008225Abstract: Mono- or di-substituted derivatives of GE2270 factors C.sub.2a, D.sub.2 and E of general formula (I), wherein W represents a moiety of formula (a), (b) or (c), R.sup.1 and R.sup.2 representing a variety of substituents, X.sup.1 is methyl, X.sup.2 is a --CH.sub.2 --W.sup.1 moiety and X.sup.3 is methylamino or amino, or X.sup.1 is a --CH.sub.2 --W.sup.1 moiety, X.sup.2 is methoxymethylene and X.sup.3 is methylamino, with the proviso that when X.sup.3 is amino, then W must be 2-(aminocarbonyl)-pyrrolidinyl; with the further proviso that when W is 2-(aminocarbonyl)-pyrrolidinyl, then W.sup.1 cannot be hydroxy; and the pharmaceutically acceptable salts thereof. The mono- or di-substituted derivatives of antibiotic GE 2270 of formula (I) are antimicrobial agents mainly active against gram positive bacteria.Type: GrantFiled: June 29, 1998Date of Patent: December 28, 1999Assignee: BioSearch Italia, S.p.A.Inventors: Sergio Lociuro, Paolo Tavecchia, Romeo Ciabatti, Ermenegildo Restelli
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Patent number: 5998613Abstract: The present invention relates to novel 4-aminotetrahydrobenzisoxazoles or 4-aminotetrahydrobenziothiazoles having gamma-aminobutanoic acid (GABA)-uptake inhibiting activity and thus useful in the treatment of analgesia, psychosis, convulsions, anxiety, epileptic disorders or muscular and movement disorders, such as spastic disorders or symptoms in Huntington's disease or Parkinson disease.Type: GrantFiled: August 5, 1997Date of Patent: December 7, 1999Assignee: H. Lundbeck A/SInventors: Erik Falch, Jens Kristian Perregaard, Arne Schousboe, Povl Krogsgaard-Larsen, Bente Frolund, Sibylle Moltzen Lenz
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Patent number: 5952320Abstract: Macrocyclic compounds of formula ##STR1## are potent inhibitors of matrix metalloproteinase and are useful in the treatment of diseases in which matrix metalloproteinase play a role. Also disclosed are matrix metalloproteinase inhibiting compositions and a method of inhibiting matrix metalloproteinase in a mammal.Type: GrantFiled: December 17, 1997Date of Patent: September 14, 1999Assignee: Abbott LaboratoriesInventors: Steven K. Davidsen, Douglas H. Steinman, George S. Sheppard, Lianhong Xu, James H. Holms, Yan Guo, James B. Summers, Alan S. Florjancic, Michael R. Michaelides
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Patent number: 5837807Abstract: This invention is directed to tetrahydronaphthalene compounds of the formula ##STR1## wherein R.sup.1 is hydrogen, bromine, cyano, formyl, hydroxy, lower alkyl, lower alkenyl, lower alkynyl, lower alkoxy, aryloxy, lower aralkoxy or aryl; R.sup.2 is an amino acid residue or a chain of 2 to 20 amino acid residues wherein reactive moieties in the side chains of the amino acid residue(s) is/are protected or unprotected, and wherein the amino group of the N-terminal amino acid is a free or protected amino group; A.sup.1, A.sup.2, A.sup.3 and A.sup.4 each are .alpha.-amino acid residues wherein A.sup.1 and A.sup.2 are in the L configuration and A.sup.3 and A.sup.4 are in the D configuration when the .alpha.-C atom of said .alpha.-amino acid residue is asymmetric; X is oxygen or sulphur; Y is a residue of the formula ##STR2## n is 0 or 1; R.sup.3 is hydrogen or lower alkyl; R.sup.Type: GrantFiled: February 27, 1996Date of Patent: November 17, 1998Assignee: Hoffmann-La Roche Inc.Inventors: Christine Abrecht, Alfred Grieder, Klaus Muller, Daniel Obrecht
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Patent number: 5817602Abstract: Thiadiazabicyclodecanes of formula (I) wherein, Z is oxygen or sulfur; R is an optional substituent and W is an optionally condensed or substituted phenyl radical and the salts, complexes and stereisomers thereof, have good selective pre- and post-emergence herbicidal properties.Type: GrantFiled: December 21, 1995Date of Patent: October 6, 1998Assignee: Novartis CorporationInventors: Georg Pissiotas, Hans Moser, Hans-Georg Brunner
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Patent number: 5789587Abstract: There are disclosed certain novel compounds identified as heterocyclic-fused lactams which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to increase the stature of those afflicted with a lack of a normal secretion of natural growth hormone. Growth promoting compositions containing such heterocyclic-fused lactams as the active ingredient thereof are also disclosed.Type: GrantFiled: November 6, 1996Date of Patent: August 4, 1998Assignee: Merck & Co., Inc.Inventors: Michael H. Fisher, Helmut Mrozik, William R. Schoen, Thomas L. Shih, Matthew J. Wyvratt
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Patent number: 5747481Abstract: The present invention relates to novel N-substituted azaheterocyclic carboxylic acids and esters thereof in which a substituted alkyl chain forms part of the N-substituent or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation.Type: GrantFiled: May 27, 1997Date of Patent: May 5, 1998Assignee: Novo Nordisk A/JInventors: Tine Krough J.o slashed.rgensen, Knud Erik Andersen, Henrik Sune Andersen, Rolf Hohlweg, Peter Madsen, Uffe Bang Olsen
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Patent number: 5714603Abstract: A process for the pare-directed nuclear chlorination of an alkylbenzene, such as toluene, comprises reacting the alkylbenzene with chlorine in the presence of a Lewis acid catalyst and a novel co-catalyst of the formula: ##STR1## where Z is ##STR2## and R is Cl, Br, F, C.sub.1 to C.sub.8 alkyl to C.sub.1 to C.sub.8 alkoxy; x and y are each hydrogen, or taken together form a fused cyclopentyl or cyclohexyl ring; n is 0, 1 or 2, with the proviso that when Z is ?3!, n is 0 or 1.Type: GrantFiled: December 2, 1996Date of Patent: February 3, 1998Assignee: Occidental Chemical CorporationInventors: Ramesh Krishnamurti, Sandor Nagy, Thomas F. Smolka
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Patent number: 5694950Abstract: A method and system for use in treating a patient with an immunosuppressant to prevent an adverse immune response, either a rejection of a transplanted organ or an attack on the patient's body by its own immune system caused by an autoimmune disease, without unduly suppressing the ability of the patient's immune system to combat infection. The method employs an expert system to provide non-numerical information concerning the course of action to be taken with respect to a patient's immunosuppressant treatment, at a given time, including, in particular, an instruction on whether the immunosuppressant dosage being administered to the patient should be changed, and if so how. That instruction is determined by the expert system through analysis of standardized characterizations assigned to standardized patient examination criteria including levels of the immunosuppressant in blood plasma and whole blood.Type: GrantFiled: August 16, 1994Date of Patent: December 9, 1997Assignee: J & W McMichael Software, Inc.Inventor: John Patrick McMichael
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Patent number: 5663274Abstract: The present invention relates to heat-curable, cyclic isocyanate addition productsi) which are the reaction products ofa) a polyisocyanate component having an average isocyanate functionality of two or more and a uretdione group content (calculated as N.sub.2 C.sub.2 O.sub.2, MW 84) of 1 to 30%, based on the weight of the polyisocyanate component, withb) a compound containing two or more isocyanate-reactive groups andii) in which at least 10% by weight of the reaction products are in the form of cyclic groups containing urea and/or urethane groups. The present invention also relates to a process for the preparation of these cyclic isocyanate addition products and to the products obtained by curing these compositions, optionally in the presence of other isocyanate-reactive compounds, at elevated temperatures, e.g., coatings, adhesives, molded articles, elastomers and foams.Type: GrantFiled: June 5, 1996Date of Patent: September 2, 1997Assignee: Bayer CorporationInventors: Sze-Ming Lee, Philip E. Yeske, Duane B. Priddy, Jr., Robert J. Kumpf, Douglas A. Wicks
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Patent number: 5644024Abstract: The present invention is concerned with tetrahydronaphthalene derivatives which are mimics of domains of peptides or proteins which can interact with other proteins or with DNA or RNA through .alpha.-helical conformation, said tetrahydronaphthalene derivatives having the formulae: ##STR1## are valuable aids in the determination of biologically active peptide sequences and are accordingly so-called "research tools". They are, however, also potentially suitable as medicaments.Type: GrantFiled: August 17, 1994Date of Patent: July 1, 1997Assignee: Hoffmann-La Roche Inc.Inventors: Christine Abrecht, Klaus Muller, Daniel Obrecht, Arnold Trzeciak
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Patent number: 5622821Abstract: The invention provides lanthanide chelates capable of intense luminescence. The celates comprise a lanthanide chelator covalently joined to a coumarin-like or quinolone-like sensitizer. Exemplary sensitzers include 2- or 4-quinolones, 2- or 4-coumarins, or derivatives thereof e.g. carbostyril 124 (7-amino-4-methyl-2-quinolone), coumarin 120 (7-amino-4-methyl-2-coumarin), coumarin 124 (7-amino-4-(trifluoromethyl)-2-coumarin), aminomethyltrimethylpsoralen, etc.The chelates form high affinity complexes with lanthanides, such as terbium or europium, through chelator groups, such as DTPA. The chelates may be coupled to a wide variety of compounds to create specific labels, probes, diagnostic and/or therapeutic reagents, etc. The chelates find particular use in resonance energy transfer between chelate-lanthanide complexes and another luminescent agent, often a fluorescent non-metal based resonance energy acceptor.Type: GrantFiled: June 29, 1994Date of Patent: April 22, 1997Assignee: The Regents of the University of CaliforniaInventors: Paul R. Selvin, John Hearst
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Patent number: 5606054Abstract: There are disclosed certain novel compounds identified as heterocyclic-fused lactams which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to increase the stature of those afflicted with a lack of a normal secretion of natural growth hormone. Growth promoting compositions containing such heterocyclic-fused lactams as the active ingredient thereof are also disclosed.Type: GrantFiled: December 14, 1993Date of Patent: February 25, 1997Assignee: Merck & Co., Inc.Inventors: Michael H. Fisher, Helmut Mrozik, William R. Schoen, Thomas L. Shih, Matthew J. Wyvratt
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Patent number: 5597715Abstract: A compound of formula (I) is obtainable by the cultivation of a microorganism from the genus Streptomyces, such as Streptomyces NCIMB 40515. In the presence of rapamycin, and recovery thereof from the culture medium. The compound, and pharmaceutical compositions containing it, is useful as an immunomodulatory agent, as an anticancer agent, or in the treatment of microbial infections in animals including humans.Type: GrantFiled: August 10, 1995Date of Patent: January 28, 1997Assignee: SmithKline Beecham p.l.c.Inventor: Brian D. Ford