Thiocarbonyl Bonded Directly To The Six-membered Hetero Ring Patents (Class 546/313)
-
Patent number: 8835467Abstract: Compounds are disclosed which inhibit SIR2 base exchange more than deacetylation, thus enhancing SIR2 deacetylation activity. Methods of using the compounds for enhancing SIR2 deacetylation activity and increasing longevity of an organism are also disclosed. Methods for screening for compounds that enhance SIR2 deacetylation activity and increase longevity of an organism are additionally disclosed.Type: GrantFiled: January 23, 2013Date of Patent: September 16, 2014Assignee: Albert Einstein College of Medicine of Yeshiva UniversityInventors: Vern L. Schramm, Anthony A. Sauve
-
Patent number: 8796175Abstract: The invention relates to the use of at least one compound selected from the class of the sulphoximines for enhancing plants' intrinsic defenses and/or for improving plant growth and/or for enhancing the resistance of plants to plant diseases which are caused by fungi, bacteria, viruses, MLOs (mycoplasma-like organisms) and/or RLOs (rickettsia-like organisms), and/or for enhancing the resistance of plants to abiotic stress factors.Type: GrantFiled: August 17, 2009Date of Patent: August 5, 2014Assignee: Bayer CropScience AGInventors: Peter Jeschke, Wolfgang Thielert, Heike Hungenberg
-
Patent number: 8680100Abstract: The present invention is directed to compounds represented by structural formula (I), or a pharmaceutically acceptable salt or a transition metal chelate, coordinate or complex thereof or a transition metal chelate, coordinate or complex of a deprotonated form of the compound. Pharmaceutical composition and method of use for these compounds are also included.Type: GrantFiled: December 1, 2009Date of Patent: March 25, 2014Assignee: Synta Pharmaceuticals Corp.Inventors: Jun Jiang, Teresa Kowalczyk-Przewloka, Stefan M. Schweizer, Zhi-Qiang Xia, Shoujun Chen, Christopher Borella, Lijun Sun
-
Publication number: 20130324737Abstract: The invention disclosed in this document is related to the field of processes to produce certain 2-(pyridine-3-yl)thiazoles as intermediates for the synthesis of pesticidal thiazole amides.Type: ApplicationFiled: May 30, 2013Publication date: December 5, 2013Applicant: DOW AGROSCIENCES LLCInventors: Ronald Ross, JR., Carl DeAmicis, Yuanming Zhu, Noormohamed M. Niyaz, Kim E. Arndt, Scott P. West, Gary Roth
-
Publication number: 20130231351Abstract: Compounds are disclosed which inhibit SIR2 base exchange more than deacetylation, thus enhancing SIR2 deacetylation activity. Methods of using the compounds for enhancing SIR2 deacetylation activity and increasing longevity of an organism are also disclosed. Methods for screening for compounds that enhance SIR2 deacetylation activity and increase longevity of an organism are additionally disclosed.Type: ApplicationFiled: January 23, 2013Publication date: September 5, 2013Applicant: Albert Einstein College of Medicine of Yeshiva UniversityInventors: Vern L. Schramm, Anthony A. Sauve
-
Patent number: 8461346Abstract: The present invention relates to the compounds of formula I, processes for their production and their use as anti-inflammatory agents.Type: GrantFiled: May 7, 2012Date of Patent: June 11, 2013Assignee: Bayer Pharma AktiengesellschaftInventors: Markus Berger, Jan Dahmen, Hartmut Rehwinkel, Stefan Jaroch, Heike Schaecke
-
Publication number: 20130102774Abstract: A process for transforming a group >C?O (I) in a compound into a group >C?S (II) or into a tautomeric form of group (II) in a reaction giving a thionated reaction product, by use of crystalline P2S5.2 C5H5N as a thionating agent. A thionating agent which is crystalline P2S5.2 C5H5N.Type: ApplicationFiled: February 3, 2012Publication date: April 25, 2013Applicant: VIRONOVA ABInventors: Birgitta Pettersson, Vedran Hasimbegovic, Per H Svensson, Jan Bergman
-
Patent number: 8383653Abstract: Compounds are disclosed which inhibit SIR2 base exchange more than deacetylation, thus enhancing SIR2 deacetylation activity. Methods of using the compounds for enhancing SIR2 deacetylation activity and increasing longevity of an organism are also disclosed. Methods for screening for compounds that enhance SIR2 deacetylation activity and increase longevity of an organism are additionally disclosed.Type: GrantFiled: June 30, 2004Date of Patent: February 26, 2013Assignee: Albert Einstein College of Medicine of Yeshiva UniversityInventors: Vern L. Schramm, Anthony A. Sauve
-
Publication number: 20120065206Abstract: The present invention is directed to compounds represented by structural formula (I), or a pharmaceutically acceptable salt or a transition metal chelate, coordinate or complex thereof or a transition metal chelate, coordinate or complex of a deprotonated form of the compound. Pharmaceutical composition and method of use for these compounds are also included.Type: ApplicationFiled: December 1, 2009Publication date: March 15, 2012Applicant: SYNTA PHARMACEUTICALS CORP.Inventors: Jun Jiang, Teresa Kowalczyk-Przewloka, Stefan M. Schweizer, Zhi-Qiang Xia, Shoujun Chen, Christopher Borella, Lijun Sun
-
Publication number: 20110218220Abstract: The present invention relates to the use of isotopically labeled derivatives of isoniazid, ethionamide and related compounds as effective therapy for the treatment of mycobacterial diseases, including Mycobacterium tuberculosis.Type: ApplicationFiled: August 20, 2008Publication date: September 8, 2011Applicants: STC.UNM, THE JOHN HOPKINS UNIVERSITYInventors: Graham Timmins, Sharon Master, Vojo P. Deretic, William Bishai
-
Publication number: 20110178102Abstract: Compounds are disclosed which inhibit SIR2 base exchange more than deacetylation, thus enhancing SIR2 deacetylation activity. Methods of using the compounds for enhancing SIR2 deacetylation activity and increasing longevity of an organism are also disclosed. Methods for screening for compounds that enhance SIR2 deacetylation activity and increase longevity of an organism are additionally disclosed.Type: ApplicationFiled: June 30, 2004Publication date: July 21, 2011Applicant: ALBERT EINSTEIN COLLEGE OF MEDICINE OF YESHIVA UNIVERSITYInventors: Vern L Schramm, Anthony A. Suave
-
Patent number: 7915253Abstract: Compounds as modulators of peroxisome proliferator activated receptors, pharmaceutical compositions comprising the same, and methods of treating disease using the same are disclosed.Type: GrantFiled: September 4, 2008Date of Patent: March 29, 2011Assignee: Kalypsys, IncInventors: Stewart A. Noble, Guy Oshiro, James W. Malecha, Cunxiang Zhao, Carmen K. Robinson, Sergio G. Duron, Michael Sertic, Andrew K. Lindstrom, Andrew K. Shiau, Christopher D. Bayne, Mehmet Kahraman, Boliang Lou, Steve P. Govek
-
Patent number: 7678920Abstract: N-Substituted sulfoximines are effective at controlling insects.Type: GrantFiled: April 8, 2005Date of Patent: March 16, 2010Assignee: Dow AgroSciences LLCInventors: Yuanming Zhu, Richard Brewer Rogers, Jim Xinpei Huang
-
Patent number: 7528274Abstract: Certain thiol and acylthiol compounds inhibit retrovirus growth by attacking the highly conserved zinc finger regions of essential viral proteins. These compounds, compositions containing them, and methods of using them to treat retroviral infections such as HIV are described. These compounds are also useful for preparation of vaccines comprised of inactivated retroviruses such as HIV, prevention of the transmission of such retroviruses, and detection of retroviral proteins.Type: GrantFiled: July 25, 2002Date of Patent: May 5, 2009Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: John K. Inman, Atul Goel, Ettore Appella, Jim Turpin, Marco Schito
-
Patent number: 7507828Abstract: One aspect of the invention relates to HDAC inhibitors. Methods of sensitizing a cancer cell to the cytotoxic effects of radiotherapy are also provided. The invention also provides methods for treating cancer and methods for treating neurological diseases. Additionally, the invention further provides pharmaceutical compositions comprising an HDAC inhibitor of the invention, and kits comprising a container containing an HDAC inhibitor of the invention.Type: GrantFiled: May 11, 2004Date of Patent: March 24, 2009Assignee: Georgetown UniversityInventors: Alan P. Kozikowski, Bin Chen
-
Publication number: 20090029971Abstract: Compounds as modulators of peroxisome proliferator activated receptors, pharmaceutical compositions comprising the same, and methods of treating disease using the same are disclosed.Type: ApplicationFiled: September 4, 2008Publication date: January 29, 2009Applicant: KALYPSYS, INC.Inventors: Stewart A. Noble, Guy Oshiro, James W. Malecha, Cunxiang Zhao, Carmen Robinson, Sergio G. Duron, Michael Sertic, Andrew K. Lindstrom, Andrew K. Shiau, Christopher D. Bayne, Mehmet Kahraman, Boliang Lou, Steve P. Govek
-
Patent number: 7241782Abstract: The invention relates to a novel polymorph V of torasemide, to a process for its preparation, to its use as a raw material for the preparation of crystalline modifications I and III of torasemide, to amorphous torasemide modifications and to pharmaceutically acceptable salts of torasemide, to pharmaceutical forms containing the said novel polymorph V of torasemide as the active ingredient as well as to its use.Type: GrantFiled: September 25, 2000Date of Patent: July 10, 2007Assignee: PLIVA, farmaceutska industrija, dionicko drustvoInventors: Darko Filić, Miljenko Dumić, Bo{hacek over (z)}ena Klepić, Aleksandar Danilovski, Marijan Tudja
-
Patent number: 7105549Abstract: This invention relates aryl substituted pyridines of Formula I: or a pharmaceutically acceptable salt, prodrug or solvate thereof, wherein Ar and R1–R4 are set in the specification. The invention is also directed to the use of compounds of Formula I for the treatment of neuronal damage following global and focal ischemia, for the treatment or prevention of neurodegenerative conditions such as amyotrophic lateral sclerosis (ALS), and for the treatment, prevention or amelioration of both acute or chronic pain, as antitinnitus agents, as anticonvulsants, and as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy.Type: GrantFiled: September 6, 2002Date of Patent: September 12, 2006Assignee: Euro-Celtique S.A.Inventors: Bin Shao, R. Richard Goehring, Samuel F Victory, Qun Sun
-
Patent number: 6936597Abstract: Polymeric prodrugs of the formula: wherein B is selected from the group consisting of OH, leaving groups, residues of amine-containing moieties and a residues of hydroxyl-containing moieties; Y1 is selected from the group consisting of O, S, and NR5; M is NR3, O or S; Ar is a moiety which when included in Formula I forms a multi-substituted aromatic or heteroaromatic hydrocarbon or a multi-substituted heterocyclic group; (m) is zero or a positive integer; R1-3 and R5 are independently selected from the group consisting of hydrogen, C1-6 alkyls, C3-12 branched alkyls, C3-8 cycloalkyls, C1-6 substituted alkyls, C3-8 substituted cycloalkyls, aryls, substituted aryls, aralkyls, C1-6 heteroalkyls, substituted C1-6 heteroalkyls, C1-6 alkoxy, phenoxy and C1-6 heteroalkoxy; and R4 is a polymeric residue; as well as methods of making and using the same are disclosed.Type: GrantFiled: March 21, 2002Date of Patent: August 30, 2005Assignee: Enzon, Inc.Inventors: Richard B. Greenwald, Yun H. Choe
-
Patent number: 6930130Abstract: The present invention relates to novel active compounds named Citrullimycines, which are obtainable by cultivation of Streptomyces sp. ST 101396 (DSM 13309), and to their pharmaceutically acceptable salts and derivatives. The present invention further relates to a process for the production of the Citrullimycines, to the microorganism Streptomycetes sp. ST 101396 (DSM 13309), to the use of the Citrullimycines and their pharmaceutically acceptable salts and derivatives as pharmaceuticals, for example as inhibitors of the neurotensin receptor, and to pharmaceutical compositions comprising Citrullimycines or a pharmaceutically acceptable salt or derivative thereof.Type: GrantFiled: October 1, 2001Date of Patent: August 16, 2005Assignee: Aventis Pharma Deutschland GmbHInventors: Cordula Hopmann, Michael Kurz, Mark Brönstrup, Joachim Wink
-
Patent number: 6852863Abstract: The present invention relates to metabolites of (3-{[4-tert-butyl-benzyl)-(pyridine-3-sulfonyl)-amino]-methyl}-phenoxy)-acetic acid.Type: GrantFiled: January 29, 2003Date of Patent: February 8, 2005Assignee: Pfizer Inc.Inventors: Kimberly O. Cameron, Kim A. Johnson, Bruce A. Lefker, Chandra A. Prakash
-
Patent number: 6825221Abstract: According to the invention there is provided a compound the formula I; wherein A, X, B, R1, R2, R3 and R4 are as defined in the specification.Type: GrantFiled: August 29, 2002Date of Patent: November 30, 2004Assignee: Allergan, Inc.Inventors: Robert M. Burk, Sophie Beauchemin
-
Publication number: 20040110802Abstract: The invention provides antimicrobial agents and methods of using the agents for sterilization, sanitation, antisepsis, disinfection, and treatment of infections in mammals.Type: ApplicationFiled: August 20, 2003Publication date: June 10, 2004Inventors: Atli Thorarensen, J. Craig Ruble, Jed F. Fisher, Donna Lee Romero, Thomas J. Beauchamp, Jill M. Northuis
-
Patent number: 6747041Abstract: Heterocyclic dicarboxylic acid diamide derivative represented by the general formula (I): wherein R1, R2 and R3 represent each H, optionally halogenated C3-6 cycloalkyl, etc.; Het represents a 5- or 6-membered heterocycle; X and Y represent each halocyano, nitro, optionally halogenated C3-6, cycloalkyl, optionally substituted phenyl, an optionally substituted heterocycle, etc; n is from 0 to 3; m is from 1 to 5; Z1 and Z2 represent each O or S; and B1 to B4 represent each C or N. Agricultural/horticultural insecticides having an excellent controlling effect on pest insects such as diamond-back moth (Pluntella xylostella) and tobacco cutworm (Spodoptera litura).Type: GrantFiled: April 10, 2002Date of Patent: June 8, 2004Assignee: Nihon Nohyaku Co., Ltd.Inventors: Takeshi Katsuhira, Takashi Furuya, Makoto Gotoh, Masanori Tohnishi, Hideo Takaishi, Kazuyuki Sakata, Masayuki Morimoto, Akira Seo
-
Publication number: 20040034069Abstract: A method for the inhibition of high affinity glycine transporters, compounds that inhibit these transporters; pharmaceutically active compositions comprising such compounds; and the use of such compounds either as above, or in formulations for the control or prevention of disease states in which glycine is involved are disclosed.Type: ApplicationFiled: August 8, 2003Publication date: February 19, 2004Inventors: Syed M. Ali, Kurt R. Brunden, Jack B. Jiang
-
Publication number: 20040018942Abstract: The compound of the formula 1Type: ApplicationFiled: July 17, 2002Publication date: January 29, 2004Applicant: ISHIHARA SANGYO KAISHA, LTD.Inventors: Masamitsu Tsukamoto, Mark Read
-
Publication number: 20030195230Abstract: Selected amines are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: ApplicationFiled: January 10, 2002Publication date: October 16, 2003Inventors: Guoqing Chen, Jeffrey Adams, Jean Bemis, Lucian Di Pietro, Celia Dominguez, Daniel Elbaum, Julie Germain, Qi Huang, Joseph L. Kim, Xiaohu Ouyang, Vinod F. Patel, Leon M. Smith, Andrew Tasker, Ning Xi, Shimin Xu, Chester Chenguang Yuan, Michael Croghan, Tae-Seong Kim
-
Publication number: 20030191113Abstract: The invention concerns compounds of general formula (1) wherein: n, G, Q1, Q2, X1, X2, Y and Z are as defied in the description, the method for preparing said compounds, fungicide compositions comprising said compounds and methods for treating plants using said compounds or compositions.Type: ApplicationFiled: July 8, 2002Publication date: October 9, 2003Inventors: Francisco Nieto-Roman, Jean-Pierre Vors, Alain Villier, Helene Lachaise, Adeline Mousques, Benoit Hartmann, Pierre Hutin, Jose Lorenzo Molina, Benoit Muller
-
Publication number: 20030119883Abstract: The present invention relates to amlodipine free base in a crystalline form, to pharmaceutical formulations comprising such material, processes of manufacture and its use in therapy.Type: ApplicationFiled: August 20, 2002Publication date: June 26, 2003Applicant: Pfizer Inc.Inventors: Alan Craig Bentham, Alan John Pettman, Keith Stephen Ruddock
-
Publication number: 20030119852Abstract: What is described are compounds of the formulae (I) and (II) 1Type: ApplicationFiled: September 18, 2002Publication date: June 26, 2003Inventors: Marion Beckmann, Oswald Ort, Uwe Doller, Gerhard Krautstrunk, Wolfgang Schaper, Peter Lummen, Daniela Jans, Waltraud Hempel, Jutta Maria Waibel, Barbara Lorkens
-
Publication number: 20030083523Abstract: A compound represented by the following general formula (I): 1Type: ApplicationFiled: June 18, 2002Publication date: May 1, 2003Applicant: Mitsubishi Chemical CorporationInventors: Ryoichi Ando, Makoto Kawamura, Noriko Chiba, Kazutoshi Watanabe
-
Patent number: 6521626Abstract: Compounds of formula (1): wherein R1 is a hydrogen atom or an optionally substituted cycloaliphatic, polycycloaliphatic, heterocycloaliphatic, polyheterocycloaliphatic, aromatic or heteroaromatic group; Alk1 is an optionally substituted aliphatic or heteroaliphatic chain; L1 is a linker atom or group; r and s is each zero or an integer 1; R2 and R3, which may be the same or different, is each a hydrogen or halogen atom or a straight or branched alkyl, haloalkyl, alkoxy, haloalkoxy, hydroxyl or nitro group; Alk2 is a straight or branched alkylene chain; m is zero or an integer 1; R4 is a hydrogen atom or a methyl group; R5 is a hydrogen atom or a straight or branched alkyl group; R6 is a group —(CH2)tR7 in which t is zero or the integer 1 and R7 is an optionally substituted polycycloaliphatic, heterocycloaliphatic, polyheterocycloaliphatic, aromatic or heteroaromatic group; R is a carboxylic acid (—CO2H) or a derivative thereof; and the salts, solvates and hydrates theType: GrantFiled: March 23, 1999Date of Patent: February 18, 2003Assignee: Celltech R&D LimitedInventors: Sarah Catherine Archibald, John Clifford Head, Graham John Warrellow, John Robert Porter
-
Patent number: 6511993Abstract: Compounds of formula (I) and pharmaceutically-acceptable derivatives thereof, are matrix metalloprotease inhibitors, useful in treatment of conditions mediated by matrix metalloproteases, such as chronic dermal ulcers.Type: GrantFiled: June 2, 2000Date of Patent: January 28, 2003Inventors: Kevin Neil Dack, Michael Jonathan Fray, Gavin Alistair Whitlock, Mark Llewellyn Lewis, Nicholas Murray Thomson
-
Publication number: 20020173631Abstract: Compounds of the formula 1Type: ApplicationFiled: May 8, 2002Publication date: November 21, 2002Inventors: Alan T. Johnson, Min Teng, Vidyasagar Vuligonda, Richard L. Beard, Samuel J. Gillett, Tien T. Duong, Roshantha A. Chandraratna
-
Patent number: 6465471Abstract: Compounds of formula (1) are described: in which Het is a heteroaromatic group, Alk1 is an optionally substituted aliphatic or heteroaliphatic chain and R is a carboxylic acid or a derivative thereof. The compounds are able to inhibit the binding of &agr;4 integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders.Type: GrantFiled: July 1, 1999Date of Patent: October 15, 2002Assignee: Celltech Therapeutics LimitedInventors: Graham John Warrellow, John Clifford Head, John Robert Porter, Sarah Catherine Archibald
-
Publication number: 20020143206Abstract: Process for the oxidation of aldehydes to the corresponding acids in which an aldehyde as substrate is oxidized to the corresponding acid in the presence of an equimolar amount, or a molar excess, of periodate, catalytic amounts of dichromate or CrO3, and in the presence of an acid in water, a water/solvent mixture or in a solvent at a temperature of −20° C. to +50° C.Type: ApplicationFiled: March 28, 2002Publication date: October 3, 2002Inventors: Paul Alsters, Elisabeth Schmieder Van De Vondervoort
-
Patent number: 6339045Abstract: N-(substituted or unsubstituted)-4-substituted-6-(substituted or unsubstituted) phenoxy-2-pyridine carboxamide or thiocarboxamide represented by the general formula (I) and a process for producing the compound. A herbicide containing as an effective ingredient N-(substituted or unsubstituted)-4-substituted-6-(substituted or unsubstituted) phenoxy-2-pyridine carboxamide or thiocarboxamide represented by the general formula (I).Type: GrantFiled: August 12, 1998Date of Patent: January 15, 2002Assignee: Kureha Kagaku Kogyo Kabushiki KaishaInventors: Hisashi Kanno, Yoshikazu Kubota, Tsutomu Sato, Koki Sato
-
Patent number: 6214835Abstract: The present invention provides dihalopropene compounds of the general formula: wherein R1 is C1-C10 alkyl or the like; L is C(═O)NH or the like; R2, R3 and R4 are independently halogen or the like; R5, R6 and R7 are independently hydrogen or the like; m is an integer of 0 to 4; n is an integer of 0 to 2; X is chlorine or the like; Y is oxygen or the like; and Z is oxygen or the like, which have excellent insecticidal activity so that they are satisfactorily effective for the control of noxious insects.Type: GrantFiled: June 2, 1999Date of Patent: April 10, 2001Assignee: Sumitomo Chemical Company, LimitedInventors: Sanshiro Matsuo, Taro Hirose, Keiichi Izumi, Masaya Suzuki, Noriyasu Sakamoto, Kazunori Tsushima, Shigeru Saito, Hirotaka Takano
-
Patent number: 6191280Abstract: A process for preparing thiopyridines of the formula I where the substituents are as defined in the description.Type: GrantFiled: November 17, 1999Date of Patent: February 20, 2001Assignee: BASF AktiengesellschaftInventors: Gerhard Hamprecht, Markus Menges, Olaf Menke, Robert Reinhard, Peter Schäfer, Cyrill Zagar
-
Patent number: 6121273Abstract: This invention relates to neurotrophic low molecular weight, small molecule N-linked sulfonamides of heterocyclic thioesters having an affinity for FKBP-type immunophilins, and their use as inhibitors of the enzyme activity associated with immunophilin proteins, particularly peptidyl-prolyl isomerase, or rotamase, enzyme activity.Type: GrantFiled: December 22, 1997Date of Patent: September 19, 2000Assignee: GPI NIL Holdings, IncInventors: Gregory S. Hamilton, Jai-He Li, Wei Huang
-
Patent number: 6110945Abstract: Aromatic amines of formula (1) are described: ##STR1## wherein Az is an optionally substituted monocyclic six-membered nitrogen-containing aromatic group;L.sup.1 is a linker atom or group;R is a carboxylic acid or a derivative thereof;and R.sup.5 is a group --L.sup.2 (CH.sub.2).sub.t R.sup.6 in which L.sup.2 is a --N(R.sup.7)CO-- or --N(R.sup.7)CS-- group.The compounds are able to inhibit the binding of .alpha..sub.4 integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders.Type: GrantFiled: June 2, 1999Date of Patent: August 29, 2000Assignee: Celltech Therapeutics LimitedInventors: John Clifford Head, Graham John Warrellow, John Robert Porter, Sarah Catherine Archibald
-
Patent number: 6005112Abstract: A process for producing N-substituted pyridine carboxamide or thiocarboxamide, comprising reacting a substituted or unsubstituted pyridine metal compound with substituted isocyanate or isothiocyanate to obtain an addition reaction product thereof, and then substituting the metal of said addition reaction product with a proton. The process according to the present invention can be applied even to compounds having an oxidation-susceptible substituent group and, therefore, industrially useful.Type: GrantFiled: August 12, 1998Date of Patent: December 21, 1999Assignee: Kureha Kagaku Kogyo Kabushiki KaishaInventors: Hisashi Kanno, Yoshikazu Kubota
-
Patent number: 5919792Abstract: This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as vitronectin receptor antagonists. The vitronectin receptor antagonist compounds of the present invention are .alpha.v.beta.3 antagonists, .alpha.v.beta.5 antagonists or dual .alpha.v.beta.3/.alpha.v.beta.5 antagonists useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation and tumor growth.Type: GrantFiled: October 28, 1997Date of Patent: July 6, 1999Assignee: Merck & Co., Inc.Inventors: Mark E. Duggan, George D. Hartman, William F. Hoffman, Nathan C. Ihle
-
Patent number: 5834467Abstract: HIV protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and optionally other anti-viral agents as active ingredients, are suitable for treating patients or hosts infected with the HIV virus, which is known to cause AIDS.Type: GrantFiled: June 7, 1995Date of Patent: November 10, 1998Assignee: Agouron Pharmaceuticals, Inc.Inventors: Vincent J. Kalish, Bruce A. Dressman, James E. Fritz, Marlys Hammond, William J. Hornback, Stephen W. Kaldor, John E. Munroe, Siegfried Heinz Reich, John H. Tatlock, Timothy A. Shepherd, Michael J. Rodriquez
-
Patent number: 5705513Abstract: A compound, composition, and method for controlling Take-all disease of plants by applying to the seed prior to planting, a fungicide of the formula: ##STR1## wherein Z.sub.1 and Z.sub.2 are C and are part of an aromatic ring which is pyridine; R and n are defined herein; A is selected from the group consisting of --C(O)--SR.sub.3, --NH--C(X)R.sub.4, --C(.dbd.NR.sub.3)--XR.sub.7, and --C(X)-amine wherein the amine is substituted with with an alkylaminocarbonyl and a hydrogen or wherein the amine has a first and a second amine substituent defined herein; B is --W.sub.m --Q(R.sub.2).sub.3 or selected from 0-tolyl, 1-naphthyl, 2-naphthyl, and 9-phenanthryl, each optionally substituted with halogen or R.sub.4 ; Q is C, Si, Ge, or Sn; W is --C(R.sub.3).sub.p H.sub.(2-p) --; or when Q is C, W may also be selected from --N(R.sub.3).sub.m H(.sub.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.sub.Type: GrantFiled: December 28, 1994Date of Patent: January 6, 1998Assignee: Monsanto CompanyInventors: Dennis Paul Phillion, Diane Susan Braccolino, Matthew James Graneto, Wendell Gary Phillips, Karey Alan Van Sant, Daniel Mark Walker, Sai Chi Wong
-
Patent number: 5597839Abstract: Di(aromatic) compounds corresponding to the following formula: ##STR1## in which: Ar represents either ##STR2## X represents a divalent radical, Z represents O, S or a divalent radical,and R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 represent a hydrogen atom or various organic radicals, and the salts of the compounds of formula (I) when R.sub.1 is a carboxylic acid function.Use in human and veterinary medicine and in cosmetics.Type: GrantFiled: April 28, 1995Date of Patent: January 28, 1997Assignee: Centre International de Recherches Dermatologiques Galderma (Cird Galderma)Inventors: Jean-Michel Bernardon, William R. Pilgrim
-
Patent number: 5571897Abstract: Lanthanide chelates which contain three heterocyclic rings covalently coupled to each other (either one 2,6-pyridylene and two five-membered unsaturated heterocyclic ring moieties or two 2,6-pyridylene and one five-membered unsaturated heterocyclic ring moiety) and two chelating groups so seated that they together chelate the same lanthanide ion even in aqueous solutions. These lanthanide chelates can optionally contain a reactive group for coupling to biologically active molecules. The new chelates are suitable for classical lanthanide chelate applications and are also useful as probes in time-resolved fluorescence microscopy, cytometry, multilabelling techniques and in process controls in industry.Type: GrantFiled: July 26, 1994Date of Patent: November 5, 1996Assignee: Wallac OyInventors: Harri Takalo, Veli-Matti Mukkala
-
Patent number: 5439925Abstract: Di(aromatic) compounds corresponding to the following formula: ##STR1## in which: Ar represents either ##STR2## n=1 or 2 or: ##STR3## X represents a divalent radical, Z represents O, S or a divalent radical, and R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 represent a hydrogen atom or various organic radicals, and the salts of the compounds of formula (I) when R.sub.1 is a carboxylic acid function. Use is in human and veterinary medicine and in cosmetics.Type: GrantFiled: December 16, 1993Date of Patent: August 8, 1995Assignee: Centre International de Recherches Dermatologiques Galderma (Cird Galderma)Inventors: Jean-Michel Bernardon, Willliam R. Pilgrim
-
Patent number: 5389653Abstract: Catechol derivatives of the formula ##STR1## wherein Ra, Rb and Rc have the significance given herein, the ester and ether derivatives thereof which are hydrolyzable under physiological conditions and the pharmaceutically acceptable salts thereof are described and possess valuable pharmacological properties. In particular, they inhibit the enzyme catechol-O-methyltransferase (COMT), a soluble, magnesium-dependent enzyme which catalyses the transference of the methyl group of S-adenosylmethionine to a catechol substrate, whereby the corresponding methyl ethers are formed. Suitable substrates which can be O-methylated by COMT and which can thus be deactivated are, for example, extraneuronal catecholamines and exogeneously-administered therapeutically active substances having a catechol structure.Formula Ia above embraces not only compounds which form part of the invention, but also known compounds; the compounds which form part of the invention can be prepared according to known methods.Type: GrantFiled: April 16, 1993Date of Patent: February 14, 1995Assignee: Hoffman-La Roche Inc.Inventors: Karl Bernauer, Janos Borgulya, Hans Bruderer, Mose Da Prada, Gerhard Zurcher
-
Patent number: 5225545Abstract: The compounds of the formula (1) indicated in claim 1 are suitable for use as direct dyes for dyeing and printing a wide range of materials, in particular cellulose-containing fibre materials, producing dyeings and prints having good fastness properties.Type: GrantFiled: May 12, 1992Date of Patent: July 6, 1993Assignee: Ciba-Geigy CorporationInventor: Urs Lauk