Bicyclo Ring System Having The Six-membered Hetero Ring As One Of The Cyclos Patents (Class 544/47)
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Publication number: 20090012054Abstract: The present invention provides a compound of the formula [I]: wherein R1 is lower alkyl, etc. and R2 is hydrogen, etc., or R1 and R2 are bonded together to form lower alkylene; R3 is a group represented by wherein R6 and R7 are independently optionally protected amino, etc.; m and n are independently an integer of 0 to 6; R8 and R9 are independently optionally protected amino, etc., and q and r are independently an integer of 0 to 6, or R8 and R9, together with the adjacent alkylene(s) and the nitrogen atom, form saturated nitrogen-containing heterocycle optionally having substituent(s); R4 is lower alkyl, etc.; and R5 is amino, etc., or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: March 16, 2007Publication date: January 8, 2009Applicants: ASTELLAS PHARMA INC., WAKUNAGA PHARMACEUTICAL CO. LTD.Inventors: Toshio Yamanaka, Ayako Toda, Hidenori Ohki, Shinya Okuda, Kohji Kawabata, Kenji Murano, Kazuo Hatano, Shinobu Takeda, Toru Nakai, Masaru Oogaki, Satoshi Inoue, Keiji Misumi, Kenji Itoh
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Patent number: 7354771Abstract: The absolute configuration of a chiral compound is determined by (i) coordinating the chiral compound to a metalloporphyrin having a carbon chain-crosslinked porphyrin dimer structure in which one of the two porphyrin rings has at least one ethyl or substituent bulkier than ethyl at at least one of the second peripheral carbon atoms from the carbon atom at the carbon chain crosslink site, and (ii) analyzing the resultant coordination compound by circular dichroism spectrophotometry to determine the absolute configuration of the asymmetric carbon based on the sign of the Cotton effect. The chiral compound has an asymmetric carbon bonded to a basic group capable of coordinating to the metal of the other porphyrin ring of the metalloporphyrin dimer or an asymmetric carbon atom adjacent to the carbon atom bonded to the basic group.Type: GrantFiled: December 4, 2000Date of Patent: April 8, 2008Assignee: Japan Science and Technology CorporationInventors: Yoshihisa Inoue, Victor Borovkov, Juha Lintuluoto
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Patent number: 7342009Abstract: Compounds of formula I: inhibit the processing of APP by gamma-secretase, and hence are useful in the treatment or prevention of Alzheimer's disease.Type: GrantFiled: May 14, 2004Date of Patent: March 11, 2008Assignee: Merck & Co., Inc.Inventors: Kevin Dinnell, Timothy Harrison, Alan John Nadin, Andrew Pate Owens, Duncan Edward Shaw, Brian John Williams
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Patent number: 7342010Abstract: A process for producing 2-thiaquiolizidines which are glycosidase and glycosyltransferase inhibitors is described. The compounds are of the formula: where x is 0 to 3.Type: GrantFiled: November 15, 2004Date of Patent: March 11, 2008Assignee: Board of Trustees of Michigan State UniversityInventors: Rawle I. Hollingsworth, Li Gao
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Patent number: 7030238Abstract: A C-nitroso compound having a molecular weight ranging from about 225 to about 1,000 (from about 225 to about 600 for oral administration) on a monomeric basis wherein a nitroso group is attached to a tertiary carbon, which is obtained by nitrosylation of a carbon acid having a pKa less than about 25, is useful as an NO donor. When the compound is obtained from a carbon acid with a pKa less than about 10, it provides vascular relaxing effect when used at micromolar concentrations and this activity is potentiated by glutathione to be obtained at nanomolar concentrations. When the compound is obtained from a carbon acid with a pKa ranging from about 15 to about 20, vascular relaxing effect is obtained at nanomolar concentrations without glutathione. The compound is preferably water-soluble and preferably contains a carbon alpha to the nitrosylated carbon which is part of a ketone group.Type: GrantFiled: February 9, 2005Date of Patent: April 18, 2006Assignee: Duke UniversityInventors: Jonathan S. Stamler, Eric J. Toone
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Patent number: 6960579Abstract: Compounds with 5HT7 receptor affinity (some of which are novel) useful for lowering IOP, improving blood flow to the optic nerve head and the retina, providing neuroprotection, and treating retinal diseases are disclosed. The Compounds are also useful for treating sleep disorders, depression, and other psychiatric disorders, such as, schizophrenia, anxiety, obsessive compulsive disorder, circadian rhythm disorders, and centrally and peripherally mediated hypertension. Compositions and methods for their use are also disclosed.Type: GrantFiled: May 10, 1999Date of Patent: November 1, 2005Assignee: Alcon Manufacturing, Ltd.Inventors: Jesse A. May, Thomas R. Dean, Najam A. Sharif, Hwang-Hsing Chen
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Patent number: 6933304Abstract: The present invention relates to a class of compounds represented by the Formula I or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of the Formula I, and methods of selectively antagonizing the ?V?3 and/or the ?V?5 integrin without significantly antagonizing the IIb/IIIa or ?V?6 integrin.Type: GrantFiled: June 15, 2001Date of Patent: August 23, 2005Assignee: Pharmacia CorporationInventors: Srinivasan Raj Nagarajan, Ish Kumar Khanna, Michael B. Tollefson, Scott B. Mohler, Barbara Chen, Mark Russell, Balekudru Devadas, Thomas D. Penning, Lori A. Schretzman, Dale P. Spangler, Mark Laurence Boys, Nizal Samuel Chandrakumar, Hung-Fun Lu
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Patent number: 6841559Abstract: Novel pyridinones and their derivatives which are effective in treating or preventing Gram-negative bacterial infections are provided. The pyridinones are stable and easily derivatized; the methods by which these derivatizations occur is described. Two regioselective and functional group tolerant methods for the synthesis of the novel pyridinones are also provided. One such synthetic method involves reacting an imine and a Meldrum's acid derivative in solution. The other synthetic method is a solid phase synthesis of the pyridinones in which an imine is prepared bound to a solid support and a Meldrum's acid derivative is reacted with the imine. Novel imine intermediates useful in the solid phase and solution methods of synthesizing the pyridionones are also described.Type: GrantFiled: November 20, 2000Date of Patent: January 11, 2005Assignee: Washington University of St. LouisInventors: Frederic Almqvist, Hans Emtenas, Scott J. Hultgren, Jerome S. Pinkner
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Patent number: 6825184Abstract: Disclosed are compounds of the formulas (I) & (II) shown below which are active as anti-inflammatory agents. Also disclosed are methods of using and making such compounds. wherein G, X, A and Q are described herein.Type: GrantFiled: October 11, 2002Date of Patent: November 30, 2004Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Pier Francesco Cirillo, Abdelhakim Hammach, John R. Regan
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Patent number: 6756370Abstract: The invention relates to compounds of formula (I), wherein R1, R2 and A have the meanings given in claim 1, are potent 5-HT2A antagonists and are suitable for treating psychoses, schizophrenia, depression, neurological disorders, impaired memory, Parkinson's disease, amyotrophic lateral sclerosis, Alzheimer's disease, Huntington's disease, eating disorders such as bulimia and anorexia nervosa, Pre-Menstrual Syndrome and/or for positively influencing obsessive-compulsive disorders, (OCD).Type: GrantFiled: February 21, 2002Date of Patent: June 29, 2004Assignee: Merck Patent GmbHInventors: Helmut Prücher, Henning Böttcher, Karl-August Ackermann, Rudolf Gottschlich, Christoph van Amsterdam, Christoph Seyfried, Jürgen Harting, Gerd Bartoszyk, Hartmut Greiner
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Publication number: 20040102626Abstract: The invention relates to the compounds of formula (I), to a method for producing them and to their use as medicaments.Type: ApplicationFiled: January 7, 2004Publication date: May 27, 2004Inventors: Ulrich Rosentreter, Thomas Kramer, Andrea Vaupel, Walter Hubsch, Nicole Diedrichs, Thomas Krahn, Klaus Dembowsky, Johannes Peter Stasch, Mitsuyuki Shimada
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Patent number: 6730681Abstract: A class of substituted or 6,7-ring fused [1, 2, 3]triazolo[1,5-&agr;]-pyrimidine derivatives, possessing an optionally substituted cycloalkyl, phenyl or heteroaryl substituent at the 3-position and an amino moiety at the 5-position, are selective ligands for GABAA receptors, in particular having high affinity for the &agr;2 and/or &agr;3 subunit thereof, and are accordingly of benefit in the treatment and/or prevention of disorders of the central nervous system, including anxiety and convulsions.Type: GrantFiled: June 14, 2002Date of Patent: May 4, 2004Assignee: Merck Sharp & Dohme Ltd.Inventors: Mark Stuart Chambers, Ian James Collins, Simon Charles Goodacre, David James Hallett, Philip Jones, Linda Elizabeth Keown, Robert James Maxey, Leslie Joseph Street
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Patent number: 6727258Abstract: The present invention relates to compounds of formula (IA): the preparation thereof, pharmaceutical formulations thereof, and their use in medicine as allosteric adenosine receptor modulators for uses including protection against hypoxia and ischemia induced injury and treatment of adenosine-sensitive cardiac arrhythmias.Type: GrantFiled: March 19, 2001Date of Patent: April 27, 2004Assignee: King Pharmaceutical Research & Development, Inc.Inventor: Pier Giovanni Baraldi
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Patent number: 6713477Abstract: A hydroxamic acid derivative represented by formula (1) or a prodrug thereof, or a pharmaceutically acceptable salt thereof, which has a matrix metalo-proteinase inhibitor.Type: GrantFiled: November 9, 2001Date of Patent: March 30, 2004Assignee: Sumitomo Pharmaceuticals Company, LimitedInventors: Gerard Robert Scarlato, Sara Sabina Hadida Ruah, Tamiki Nishimura, Masashi Nakatsuka, Fumio Samizo, Yumiko Kamikawa, Hitoshi Houtigai
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Publication number: 20040002490Abstract: The invention concerns compounds of formula (I): R-A-R′ wherein: A is as defined in the description; R represent a group (V), (VI), (VII), or (VIII), where E, Q, R1, R2, R3, v and R4 are as defined in the description; R′ represents a —(CH2)t—R5 group wherein t and R5 are as defined in the description, and medicaments containing the same.Type: ApplicationFiled: June 16, 2003Publication date: January 1, 2004Inventors: Daniel Lesieur, Frederique Klupsch, Gerald Guillaumet, Marie-Claude Viaud, Michel Langlois, Caroline Bennejean, Pierre Renard, Philippe Delagrange
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Publication number: 20030236245Abstract: Compounds which mimic the secondary structure of helical regions of biologically active peptides and proteins having the following structure: 1Type: ApplicationFiled: August 29, 2002Publication date: December 25, 2003Applicant: Molecumetics, Ltd.Inventors: Vincent Huber, Jan Urban, Hiroshi Nakanishi, Masakatsu Eguchi, Jessymol Mathew, Min Sang Lee
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Publication number: 20030229079Abstract: Certain 1-(aromatic- or heteroaromatic-substituted-3-(heteroaromatic substituted)-1,3-propanediones are described as inhibitors of HIV integrase and inhibitors of HIV replication. These compounds are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.Type: ApplicationFiled: June 6, 2003Publication date: December 11, 2003Inventors: Linda S. Payne, Lekhanh O. Tran, Linghang H. Zhuang, Steven D. Young, Melissa S. Egbertson, John S. Wai, Mark W. Embrey, Thorsten E. Fisher, James P. Guare, H. Marie Langford, Jeffrey Y. Melamed, David L. Clark
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Patent number: 6649758Abstract: A process for preparing symmetrical or asymmetrical trans-thiazineindigo pigments of the formula (1) which comprises a) condensing, in an aqueous medium, a compound of the formula (2) with a compound of the formula (3a) or (3b) or a compound of the formula (4) with a compound of the formula (3a) and/or (3b) by maintaining the reaction mixture at a temperature between 30 and 65° C. for at least 1 hour and then b) maintaining the reaction mixture at a temperature between 100 and 180° C. and a pressure between 2 and 50 bar for at least 1 hour in the presence of an amide.Type: GrantFiled: June 21, 2001Date of Patent: November 18, 2003Assignee: Clariant Finance (BVI) LimitedInventors: Petra Maria Rothe, Leonhard Unverdorben, Bruno Piastra
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Publication number: 20030208066Abstract: Compounds of the formula 1Type: ApplicationFiled: March 17, 2003Publication date: November 6, 2003Applicant: American Cyanamid CompanyInventors: Jeremy I.. Levin, James Ming Chen, Xue-Mei Du, Jay D. Albright, Arie Zask
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Publication number: 20030191307Abstract: Novel compounds according to the formula 1Type: ApplicationFiled: November 22, 2002Publication date: October 9, 2003Inventors: Todd A. Blumenkopf, Eileen Elliott Mueller, Eric Jan Roskamp
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Publication number: 20030191115Abstract: The present application describes lactam-containing compounds and derivatives thereof of Formula I: 1Type: ApplicationFiled: September 17, 2002Publication date: October 9, 2003Inventors: Donald J.P. Pinto, Mimi L. Quan, Michael J. Orwat, Yun-Long Li, Wei Han, Jennifer X. Qiao, Patrick Y.S. Lam, Stephanie L. Koch
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Publication number: 20030139398Abstract: The invention is directed to novel quinazoline and quinazoline-like derivatives of Formula (I): 1Type: ApplicationFiled: April 5, 2002Publication date: July 24, 2003Inventors: William J. Hoekstra, Edward C. Lawson, Michael J. Costanzo
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Publication number: 20030135045Abstract: This invention relates to certain bicyclic compounds having a nucleus formed of two fused six membered rings, for example, isoquinoline, isoquinolone, tetrahydronaphthalene, dihydronaphthalene, or tetralone, substituted with both basic and acidic functionality, which are useful in inhibition of platelet aggregation.Type: ApplicationFiled: October 28, 2002Publication date: July 17, 2003Inventors: Matthew J. Fisher, Anne Marie Happ, Joseph A. Jakubowski, Michael Dean Kinnick, Allen D. Kline, John Michael Morin, Daniel J. Sall, Marshall A. Skelton, Robert Theodore Vasileff
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Publication number: 20030078258Abstract: This invention is related to novel di-substituted aminomethyl chroman derivatives which are useful in the treatment of beta-3 receptor-mediated conditions.Type: ApplicationFiled: December 7, 2001Publication date: April 24, 2003Inventors: Gaetan H. Ladouceur, William H. Bullock, Steven R. Magnuson, Stephen J. O'Connor, Roger A. Smith, Quanrong Shen, Qingjie Liu, Ning Su, Emil J. Velthuisen, Ann-Marie Campbell, Paul P. Ehrlich
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Publication number: 20030060431Abstract: Nucleoside analogues or base analogues having structure (1), where X=O or NH or S, Y=N or CHR6 or CR6, W=N or NR6 or CHR6 or CR6 or S, n=1 or 2; each R6 is independently H or O or alkyl or alkenyl or alkoxy or aryl or a reporter moiety; where necessary (i.e. when Y and/or W is N or CR6 where R6 is not O) a double bond is present between Y and W or W and W, and Q is H or a sugar or a sugar analogue or a nucleic acid backbone or backbone analogue.Type: ApplicationFiled: September 3, 2002Publication date: March 27, 2003Applicant: NYCOMED AMERSHAM PLCInventors: Adrian Christopher Simmonds, Alan Hamilton, Clifford Smith, David Loakes, Daniel Brown, Fergal Hill, Shiv Kumar, Satyam Nampalli, Mark McDougall
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Patent number: 6531484Abstract: Pyrrolidine compounds of Formula I: (wherein R1, R2, R3, R4, R5, R6, R7, R8a, R8b, j, k, 1, m, and n are defined herein) are described. The compounds are modulators of CCR5 chemokine receptor activity. The compounds are useful, for example, in the prevention or treatment of infection by HIV and the treatment of AIDS, as compounds or pharmaceutically acceptable salts, or as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.Type: GrantFiled: October 10, 2001Date of Patent: March 11, 2003Assignee: Merck & co., Inc.Inventors: Christopher A. Willoughby, Keith Rosauer, Kevin T. Chapman, Sander G. Mills, Dong-Ming Shen, Min Shu
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Publication number: 20030040513Abstract: The invention provides piperidine compounds of general formula (I) in which A, B, X, Y, Z, R, R1 and R2 are as defined in the specification, their use as medicaments, compositions containing them and processes for their for their preparation.Type: ApplicationFiled: June 13, 2002Publication date: February 27, 2003Inventors: Andrew Baxter, Nicholas Kindon, Garry Pairaudeau, Bryan Roberts, Stephen Thom
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Publication number: 20030018023Abstract: The present application describes 5-6 or 5-7 heterobicyclics of Formula I: 1Type: ApplicationFiled: March 25, 2002Publication date: January 23, 2003Inventors: Donald Joseph Philip Pinto, Renhua Li
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Publication number: 20020198178Abstract: Pyrrolidine compounds of Formula I: 1Type: ApplicationFiled: October 10, 2001Publication date: December 26, 2002Inventors: Christopher A. Willoughby, Keith Rosauer, Kevin T. Chapman, Sander G. Mills, Dong-Ming Shen, Min Shu
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Patent number: 6455522Abstract: The present application describes novel lactams and derivatives thereof of formula I: or pharmaceutically acceptable salt forms thereof, wherein rings ring B is a 4-8 membered cyclic sulfonamide containing from 0-3 additional heteroatoms selected from N, O, and S, which are useful as metalloprotease inhibitors.Type: GrantFiled: February 10, 1999Date of Patent: September 24, 2002Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Jingwu Duan, Lihua Chen, Robert J. Cherney, Carl P. Decicco, Matthew E. Voss
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Publication number: 20020111341Abstract: 1Type: ApplicationFiled: December 14, 2001Publication date: August 15, 2002Inventors: Guillaume DE Nanteuil, Philippe Gloanec, Tony Verbeuren, Alain Rupin, Marie-Odile Vallez
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Patent number: 6432945Abstract: This invention is directed to compounds of the formula and the pharmaceutically-acceptable salts thereof, where the substituents are as defined in the Specification, which are growth hormone secretogogues and which increase the level of endogenous growth hormone. The compounds of this invention are useful for the treatment and prevention of osteoporosis and/or frailty, congestive heart failure, frailty associated with aging, obesity; accelerating bone fracture repair, attenuating protein catabolic response after a major operation, reducing cachexia and protein loss due to chronic illness, accelerating wound healing, or accelerating the recovery of burn patients or patients having undergone major surgery; improving muscle strength, mobility, maintenance of skin thickness, metabolic homeostasis or renal homeostasis.Type: GrantFiled: March 30, 2001Date of Patent: August 13, 2002Assignee: Pfizer Inc.Inventors: Philip Albert Carpino, David Andrew Griffith, Bruce Allen Lefker
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Publication number: 20020107391Abstract: The present invention relates to a practical and efficient way to synthesize the compound for the endothelin receptor antagonist involving a Grignard addition and a cyclization reaction to give a desired compound of the general formula shown below: 1Type: ApplicationFiled: October 18, 2001Publication date: August 8, 2002Inventors: Lisa F. Frey, Cheng Y. Chen, Jing Li, Zhiguo J. Song, Lushi Tan, Richard D. Tillyer, David M. Tschaen, Matthew M. Zhao
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Publication number: 20020052503Abstract: This invention provides a compound of general formula (I) 1Type: ApplicationFiled: June 12, 2001Publication date: May 2, 2002Inventors: Hiroaki Wakabayashi, Masaya Ikunaka
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Patent number: 6369223Abstract: The present invention relates to a process for stereoselective cycloaddition reactions which generally comprises a cycloaddition reaction between a pair of substrates, each either chiral or prochiral, that contain reactive &pgr;-systems, in the presence of a non-racemic chiral catalyst, to produce a stereoisomerically enriched product. The present invention also relates to novel asymmetric catalyst complexes comprising a metal and an asymmetric tridentate ligand.Type: GrantFiled: January 4, 2001Date of Patent: April 9, 2002Assignee: President and Fellows of Harvard CollegeInventors: Eric N. Jacobsen, Scott E. Schaus, Alexander G. Dossetter, Timothy F. Jamison
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Publication number: 20020028933Abstract: It has been discovered that compounds of the formula: 1Type: ApplicationFiled: March 20, 2001Publication date: March 7, 2002Inventors: Kenneth Gregory Hull, Achytharao Sidduri, Jefferson W. Tilley
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Patent number: 6340752Abstract: Acylmercaptoalkanoylamino lactam esters or acids are converted to the corresponding mercaptoalkanoylamino lactam ester or acid under basic conditions by including an agent which minimizes the amount of disulfides. Suitable agents are bismercaptans, phosphine or phosphite reducing agents, zinc metal powder, and sodium hydrosulfite. Such agents are also employed in the recrystallization and reprocessing of the mercaptoalkanoylamino lactam acids.Type: GrantFiled: December 9, 1998Date of Patent: January 22, 2002Assignee: Bristol-Myers Squibb Co.Inventors: David R. Kronenthal, Theodor Denzel, Bang-Chi Chen, James H. Simpson, Rajendra P. Deshpande
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Patent number: 6200378Abstract: A compound according to the formula (I) wherein R1 and R2 are independently the atoms necessary to complete the formation of a substituted or unsubstituted aromatic or aliphatic carbocyclic or heterocyclic ring system and R3 and R4 have the meaning indicated in claim 1, a new process for the preparation of such a compound, solid solutions and mixtures comprising such a compound and the use of a compound of formula (I) as a pigment.Type: GrantFiled: July 23, 1999Date of Patent: March 13, 2001Assignee: Clariant Finance (BVIØ) LimitedInventors: Bruno Piastra, Bansi Lal Kaul
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Patent number: 6194426Abstract: A novel therapeutic use of pyrrole derivatives of the folloeing formula: in which the variables are as defined in the specification and their salts thereof for treating conditions in which TNF is involved.Type: GrantFiled: December 12, 1997Date of Patent: February 27, 2001Assignee: Rhona-Poulenc Rorer S.A.Inventors: Eric Bacque, Conception Nemecek, Georges Bashiardes, Norbert Dereu
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Patent number: 6057314Abstract: This invention relates to the discovery of heterocyclic competitive inhibitors of the enzyme thrombin, their preparation, and pharmaceutical compositions thereof. As well, this invention relates to the use of such compounds and compositions in vitro as anticoagulants and in vivo as agents for the treatment and prophylaxis of thrombotic disorders such as venous thrombosis, pulmonary embolism and arterial thrombosis resulting in acute ischemic events such as myocardial infarction or cerebral infarction. Moreover, these compounds and compositions have therapeutic utility for the prevention and treatment of coagulopathies associated with coronary bypass operations as well as restenotic events following transluminal angioplasty.Type: GrantFiled: June 23, 1997Date of Patent: May 2, 2000Assignee: Biochem Pharma Inc.Inventors: John Dimaio, M. Arshad Siddiqui, John W. Gillard, Yves St-Denis, Micheline Tarazi, Patrice Preville, Sophie Levesque, Benoit Bachand, Annette Marian Doherty, Jeremy John Edmunds
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Patent number: 6046211Abstract: The current invention discloses useful pharmaceutical compositions containing amidino derivative useful as nitric oxide synthase inhibitors.Type: GrantFiled: May 6, 1998Date of Patent: April 4, 2000Assignee: G.D. Searle & Co.Inventors: Donald W. Hansen, Jr., Mark G. Currie, E. Ann Hallinan, Kam F. Fok, Timothy J. Hagen, Arija A. Bergmanis, Steven W. Kramer, Len F. Lee, Suzanne Metz, William M. Moore, Karen B. Peterson, Barnett S. Pitzele, Dale P. Spangler, R. Keith Webber, Mihaly V. Toth, Mahima Trivedi, Foe S. Tjoeng
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Patent number: 5994274Abstract: The present invention relates to new compounds of the formula (I) ##STR1## in which X represents alkyl,Y represents halogen or alkyl andZ represents halogen or alkyl,with the proviso that one of the radicals Y and Z always represents halogen and the other alkyl,Het represents one of the groups ##STR2## in which A, B, D and G have the meanings given in the description,a plurality of processes for their preparation and their use as pesticides and herbicides.Type: GrantFiled: December 23, 1997Date of Patent: November 30, 1999Assignee: Bayer AktiengesellschaftInventors: Reiner Fischer, Thomas Bretschneider, Hermann Hagemann, Folker Lieb, Michael Ruther, Arno Widdig, Peter Dahmen, Markus Dollinger, Christoph Erdelen, Hans-Joachim Santel, Ulrike Wachendorff-Neumann, Alan Graff, Wolfram Andersch
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Patent number: 5990145Abstract: The present invention relates to compounds of the formula I,A--B--D--E--F--G (I)in which A, B, D, E, F and G have the meanings given in the patent claims, to their preparation and to their use as medicaments. The compounds of the invention are used as vitronectin receptor antagonists and as inhibitors of bone resorption.Type: GrantFiled: December 22, 1997Date of Patent: November 23, 1999Assignees: Hoechst Aktiengesellschaft, Genentech, Inc.Inventors: Volkmar Wehner, Hans Ulrich Stilz, Anuschirwan Peyman, Karlheinz Scheunemann, Jean-Marie Ruxer, Denis Carniato, Jean-Michel Lefrancois, Thomas Richard Gadek, Robert McDowell
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Patent number: 5939415Abstract: The present invention relates to heterocyclic compounds with the formula ##STR1## in which R.sup.1 to R.sup.7, B, a, and X have the meanings indicated in the specification. These compounds can be used for the treatment of diseases of the rheumatic variety and for the prevention of allergically-induced diseases.Type: GrantFiled: March 28, 1997Date of Patent: August 17, 1999Assignee: Merckle GmbHInventors: Stefan Laufer, Hans Gunther Striegel, Gerd Dannhardt
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Patent number: 5780465Abstract: 4-Substituted 5-polycyclylpyrimidine compounds in which the 5-substituent is polycyclic and is attached to the pyrimidine moiety through an aliphatic carbon atom, such as 5-(2,2-dimethylindan-1-yl)-4-methylthiopyrimidine, were prepared and found to possess excellent herbicidal activity. The compounds are especially useful for the control of undesirable vegetation in paddy rice.Type: GrantFiled: April 3, 1997Date of Patent: July 14, 1998Assignee: Dow AgroSciences LLCInventors: Lowell D. Markley, Kim E. Arndt, Patricia G. Ray, Terry W. Balko, Erik N. K. Cressman, David G. Ouse, Johnny L. Jackson, Jacob Secor
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Patent number: 5726126Abstract: There is provided a 1-(3-heterocyclylphenyl)-s-triazine-2, 4,6-oxo or thiotrione compound having the structural formula I ##STR1## Further provided are a composition and a method comprising that compound for the control of undesirable plant species.Type: GrantFiled: November 26, 1996Date of Patent: March 10, 1998Assignee: American Cyanamid CompanyInventors: Alvin Donald Crews, Jr., Philip Mark Harrington, Gary Mitchell Karp, Mark Christopher Manfredi, Michael Anthony Guaciaro
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Patent number: 5708169Abstract: The present invention provides for new 5-amidomethyl, .alpha.,.beta.-saturated and--unsaturated butyrolactone antibacterial agents of formula I ##STR1## characterized by 3-aryl substituents that include, for example, indolinyl and phenyl substituted with zero (0) to two(2) halogen atoms and substituted in the para position with, e.g., piperazinyl, thiomorpholinyl (and corresponding sulfoxide and sulfone), thiazolidinyl (and sulfoxide and sulfone), morpholinyl, azetidinyl, pyrrolidinyl, piperidinyl, pyrrolyl, azepinyl, troponyl, 3,7-diazabicyclo?3.3.0!octan-3-yl, bridged thiazinyl or bridged oxazinyl moieties. In those cases where a ring nitrogen is present, then this is substituted to form an amide, formamide, sulfonamide, urethane, or alkylated with a wide variety of moieties.Type: GrantFiled: September 5, 1996Date of Patent: January 13, 1998Assignee: Pharmacia & Upjohn CompanyInventors: Jackson B. Hester, Jr., Steven Joseph Brickner, Michael Robert Barbachyn, Douglas K. Hutchinson, Dana Scott Toops
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Patent number: 5705639Abstract: This invention includes compounds of Formula II and IV and a process for preparing Formula I compounds by first preparing the compounds of Formula IV and then further reacting to form the compounds of Formula II and further reacting to prepare the compounds of Formula I wherein Q, Z, R.sup.2 are as defined within.Type: GrantFiled: September 21, 1995Date of Patent: January 6, 1998Assignee: E. I. du Pont de Nemours and CompanyInventor: Rafael Shapiro
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Patent number: 5654294Abstract: Compounds of the formula ##STR1## are disclosed as possessing inhibotory activity against angiotensin converting enzyme (ACE) and neutral endopeptidase (NEP) and thus being useful as cardiovascular agents. Processes for preparing these compounds are also disclosed.Type: GrantFiled: June 19, 1996Date of Patent: August 5, 1997Assignee: Bristol-Myers SquibbInventor: Jeffrey A. Robl
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Patent number: 5646276Abstract: Compounds of the formula ##STR1## wherein X.sub.1 is ##STR2## are disclosed as possessing inhibotory activity against angiotensin converting enzyme (ACE) and neutral endopeptidase (NEP) and thus being useful as cardiovascular agents.Type: GrantFiled: June 19, 1996Date of Patent: July 8, 1997Assignee: Bristol-Myers Squibb Co.Inventor: Jeffrey A. Robl