Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Thiazole Ring Patents (Class 548/200)
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Patent number: 6331634Abstract: A compound represented by the formula (1) which is useful as an agricultural fungicide or an intermediate thereof can be obtained by reacting a compound of the general formula (2) with a compound of the general formula (3) in the presence of an acid and reducing the resulted reaction mixture. wherein, each of R1 to R4 and R1a to R4a independently represents a hydrogen atom or an alkyl group, and R represents an alkyl group, alkoxy group, phenyl group or 5-membered or 6-membered heterocyclic group.Type: GrantFiled: October 24, 2000Date of Patent: December 18, 2001Assignee: Mitsui Chemicals, Inc.Inventors: Hiroyuki Katsuta, Seiichi Ishii, Kanji Tomiya, Kenji Kodaka
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Publication number: 20010047096Abstract: Novel sulfidoamidocarboxylic acids (salts), a method for the production thereof, and uses therefor are provided. Sulfidoamidocarboxylic acids (salt) with a thiazolidine residue such as dimethylthiazolidine or methylthiazolidine or thiazolidine residue (residues), or a polycarboxylic acid (salt) residue such as dicarboboxylic acid (salt) or tricarboxylic acid (salt) or tetracarboxylic acid (salt) residue, a method for the production thereof, and uses therefor are also provided.Type: ApplicationFiled: April 23, 2001Publication date: November 29, 2001Inventor: Yoshihisa Oda
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Patent number: 6320054Abstract: Compounds of the formula: as well as pharmaceutically usable salts and esters thereof, wherein R1, R2 and R3 have the significance ascribed herein, inhibit binding of adhesive proteins to the surface of different types of cell and accordingly influence cell-cell and cell-matrix interactions. These compounds can be used in the form of pharmaceutical preparations for the control or prevention of neoplasms, tumor metastasing, tumor growth, osteoporosis, Paget's disease, diabetic retinopathy, macular degeneration, restenosis following vascular intervention, psoriasis, arthritis, fibrosis, kidney failure, as well as infection caused by viruses, bacteria or fungi.Type: GrantFiled: March 15, 2000Date of Patent: November 20, 2001Assignee: Hoffman-La Roche Inc.Inventors: Leo Alig, Albrecht Edenhofer, Kurt Hilpert, Thomas Weller
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Publication number: 20010041789Abstract: The invention provides a compound of formula I: 1Type: ApplicationFiled: December 22, 2000Publication date: November 15, 2001Inventor: Herbert T. Nagasawa
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Patent number: 6316503Abstract: The invention provides compounds, compositions and methods for modulating the effects of LXR in a cell. The compounds and compositions are useful both as diagnostic indicators of LXR function and as pharmacologically active agents. The compounds and compositions find particular use in the treatment of disease states associated with cholesterol metabolism, particularly atherosclerosis and hypercholesterolemia.Type: GrantFiled: March 14, 2000Date of Patent: November 13, 2001Assignee: Tularik Inc.Inventors: Leping Li, Julio C. Medina, Kevin Lustig, Bei Shan, Hirohiko Hasegawa, Serena T. Cutler, Jiwen Liu, Liusheng Zhu
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Patent number: 6313164Abstract: Compounds of the formula (I): wherein one of m and n is 0, and the other is 0, 1 or 2; k is 0 or 1 to 12; R1 is hydrogen, a substituent which is an aryl or a heterocyclic, or an optionally substituted alkyl group; A is a single bond, an oxygen atom, a carbonyl group or a group of the formula —N(R2)CO—, —N(R2)CS—, —N(R2)SO2—, —CON(R2)N(R3)CO—, —CON(R2)CO—, —CON(R2)CS—, —CON(R2)SO2—, —O—CO—, —ON(R2)CO—, —ON(R2)SO2—, —O—CON(R2)N(R3)CO—, —O—CON(R2)CO—, —O—CON(R2)SO2—, —CO—O—, —CO—CO—, —CO—CON(R2)N(R3)CO—, —CO—CON(R2)CO—, —CO—CON(R2)SO2—, —N(R2)O—, —N(R2)COCO—, —N(R2)N(R3)CO—, —N(R2)N(R3)SO2—, —N(R2)CON(R3)N(R4)CO—, —N(R2)CON(R3)CO—, —N(R2)CON(R3)SO2&mdasType: GrantFiled: July 15, 1999Date of Patent: November 6, 2001Assignee: Sankyo Company, LimitedInventors: Takashi Fujita, Tomihisa Yokoyama
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Patent number: 6291678Abstract: A process for the preparation of novel keto heterocycle derivatives of basic natural and unnatural amino acids which affords products of high enantiomeric excess where a metalated heterocycle is reacted with N,O-dialkyl amide of an amino acid containing arylsulphonamide protected side chain amine in high chemical and optical yield as well as the novel compounds obtained by the process.Type: GrantFiled: December 11, 1998Date of Patent: September 18, 2001Assignee: Warner-Lambert CompanyInventors: Kent A. Berryman, Annette M. Doherty, Jeremy J. Edmunds, Janet S. Plummer
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Publication number: 20010020006Abstract: The present invention relates to compounds of unstable inhibitors of dipeptidyl peptidase IV (DP IV), which compounds have the general formula A—B—C, whereinType: ApplicationFiled: December 21, 2000Publication date: September 6, 2001Inventors: Hans-Ulrich Demuth, J?ouml;rn Schimdt, Torsten Hoffmann, Konrad Glund
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Patent number: 6274607Abstract: This invention relates to neurotrophic low molecular weight, small molecule N-linked ureas and carbamates 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: September 10, 1999Date of Patent: August 14, 2001Assignee: GPI NIL Holdings, Inc.Inventors: Gregory S. Hamilton, Jia-He Li, Wei Huang
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Patent number: 6268313Abstract: The dihalopropene compounds of the general formula [I] have excellent insecticidal/acaricidal activity, so that they are satisfactorily effective for the control of noxious insects, mites and ticks.Type: GrantFiled: March 7, 2000Date of Patent: July 31, 2001Assignee: Sumitomo Chemical Company, LimitedInventors: Noriyasu Sakamoto, Sanshiro Matsuo, Masaya Suzuki, Taro Hirose, Kazunori Tsushima, Kimitoshi Umeda
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Patent number: 6268363Abstract: The present invention relates to a novel imidazole derivative represented by formula (1) which shows an inhibitory activity against farnesyl transferase or pharmaceutically acceptable salts or isomers thereof, in which A, n1 and Y are defined in the specification; to a process for preparation of the compound of formula (1); to intermediates which are used in the preparation of the compound of formula (1); and to a pharmaceutical composition comprising the compound of formula (1) as an active ingredient.Type: GrantFiled: May 17, 2000Date of Patent: July 31, 2001Assignee: LG Chemical Ltd.Inventors: Hyun Il Lee, Jong Sung Koh, Jin Ho Lee, Won Hee Jung, You Seung Shin, Hyun Ho Chung, Jong Hyun Kim, Seong Gu Ro, Tae Saeng Choi, Shin Wu Jeong, Tae Hwan Kwak, In Ae Ahn, Hyun Sung Kim, Sun Hwa Lee, Kwi Hwa Kim, Jung Kwon Yoo
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Patent number: 6262047Abstract: Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.Type: GrantFiled: October 10, 1997Date of Patent: July 17, 2001Assignee: COR Therapeutics, Inc.Inventors: Bing-Yan Zhu, Robert M. Scarborough
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Patent number: 6262055Abstract: Sulfur-containing heteroaryl dioxo-butyric acid derivatives 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: GrantFiled: June 1, 1999Date of Patent: July 17, 2001Assignee: Merck & Co., Inc.Inventors: Steven D. Young, John S. Wai, Mark W. Embrey, Thorsten E. Fisher
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Patent number: 6239282Abstract: A compound represented by the formula (1) which is useful as an agricultural fungicide or an intermediate thereof can be obtained by reacting a compound of the general formula (2) with a compound of the general formula (3) in the presence of an acid and reducing the resulting reaction mixture. wherein, each of R1 to R4 and R1a to R4a independently represents a hydrogen atom or an alkyl group, and R represents an alkyl group, alkoxy group, phenyl group or 5-membered or 6-membered heterocyclic group.Type: GrantFiled: March 13, 2000Date of Patent: May 29, 2001Assignee: Mitsui Chemicals, Inc.Inventors: Hiroyuki Katsuta, Seiichi Ishii, Kanji Tomiya, Kenji Kodaka
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Patent number: 6229011Abstract: Compounds of the formula: are disclosed which have activity as inhibitors of binding between VCAM-1 and cells expressing VLA-4. Such compounds are useful for treating diseases whose symptoms and/or damage are related to the binding of VCAM-1 to cells expressing VLA-4.Type: GrantFiled: August 21, 1998Date of Patent: May 8, 2001Assignee: Hoffman-La Roche Inc.Inventors: Li Chen, Robert William Guthrie, Tai-Nang Huang, Achyutharao Sidduri, Jefferson Wright Tilley, Kenneth Gregory Hull
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Patent number: 6222043Abstract: The present invention provides synthetic methodology to produce novel dipeptide compounds and pharmaceutically acceptable salts thereof which exhibit excellent HIV protease inhibitory activity and excellent bioavailability from digestive tracts. Methods of using the dipeptide compounds and pharmaceutically acceptable salts thereof also are provided.Type: GrantFiled: January 8, 1999Date of Patent: April 24, 2001Assignee: Japan Energy CorporationInventors: Ryohei Kato, Tsutomu Mimoto, Tominaga Fukazawa, Naoko Morohashi, Yoshiaki Kiso
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Patent number: 6197803Abstract: Compounds having the formula: are provided which are useful in the treatment of diseases associated with herpes viruses.Type: GrantFiled: November 22, 1999Date of Patent: March 6, 2001Assignee: American Home Products CorporationInventors: Jonathan Bloom, Kevin Curran, Martin DiGrandi, Russell Dushin, Thomas Jones, Stanley Lang, Adma Ross, Eugene A. Terefenko, Bryan O'Hara
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Patent number: 6197802Abstract: Compounds of formula (I), wherein R1 represents a hydrogen atom or an optionally substituted alkyl, alkenyl, alkyloxiranyl, alkanoyl, alkoxycarbonyl, formyl, hydroxyalkyl, alkoxyalkyl, alkanoyloxyalkyl, hydroximinoalkyl, alkoxyiminoalkyl, hydrazonoalkyl or alkylhydrazonoalkyl group; R2 represents an alkoxy group; R3 and R4 each independently represent a hydrogen atom or an alkyl group; R5 represents an alkyl group, and R6 represents a group of formula —COOR7 or —CONR7R8, in which R7 and R8 show excellent fungicifal activity and systemicity and are thus useful in various agricultural applications.Type: GrantFiled: January 19, 2000Date of Patent: March 6, 2001Assignee: American Cyanamid Co.Inventors: Gerhard Hoefle, Udo Soeker, Annerose Rehnig, Gerhard Ewald Sieverding
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Patent number: 6197794Abstract: Phenylalanine derivatives of formula (1) are described: in which L1 is a linker atom or group; A is a chain —[C(R7)(R8)]pY[C(R9)(R10)]q— in which Y is a sulphur atom or a —S(O)— or —S(O)2— group, R7, R8, R9 and R10, which may be the same or different, is each a hydrogen atom or a straight or branched alkyl or optionally substituted aromatic group, or R7 and R8 together with the carbon atom to which they are attached, or R9 and R10 together with the carbon atom to which they are attached, each forms a C3-7cycloalkyl group, and p and q, which may be the same or different, is each zero or an integer 1 or 2, provided that when one of p or q is zero the other is an integer 1 or 2; L2 is a linker group selected from —C(O)—, —C(O)O—, —C(S)—, —S(O)2—, —CON(R11)—, [where R11 is a hydrogen atom or a straight or branched alkyl group], —CSN(R11)—, —SON(R11)&mType: GrantFiled: January 7, 1999Date of Patent: March 6, 2001Assignee: Celltech Therapeutics LimitedInventors: John Clifford Head, Sarah Catherine Archibald, Graham John Warrellow, John Robert Porter
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Patent number: 6159983Abstract: A composition in unit dosage form for the inhibition, prevention or treatment of inflammatory bowel disease comprising an effective amount of a compound having the formula: ##STR1## and a pharmaceutically acceptable carrier therefor.Type: GrantFiled: September 18, 1998Date of Patent: December 12, 2000Assignee: University of FloridaInventor: Raymond J. Bergeron, Jr.
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Patent number: 6153591Abstract: The present invention is directed to novel dipeptides represented by the general Formula I: ##STR1## where R.sub.1 -R.sub.2 and AA are defined herein. The present invention relates to the discovery that compounds having Formula I are potent inhibitors of caspases and apoptotic cell death. Therefore, the inhibitors of this invention can retard or block cell death in a variety of clinical conditions in which the loss of cells, tissues or entire organs occurs.Type: GrantFiled: March 16, 1999Date of Patent: November 28, 2000Assignee: Cytovia, Inc.Inventors: Sui Xiong Cai, John Drewe, Yan Wang, Eckard Weber
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Patent number: 6124455Abstract: Compounds of the formula ##STR1## wherein the symbols have the meaning defined in the specification have retinoid-like biological activity.Type: GrantFiled: January 25, 2000Date of Patent: September 26, 2000Assignee: Allergan Sales, Inc.Inventors: Min Teng, Tien T. Duong, Roshantha A. Chandraratna
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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
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Patent number: 6110949Abstract: The invention discloses certain N-(substituted glycyl)-4-cyanothiazolidines, pharmaceutical compositions containing said compounds as an active ingredient thereof, and the use of said compounds in inhibiting dipeptidyl peptidase-IV.Type: GrantFiled: June 24, 1999Date of Patent: August 29, 2000Assignee: Novartis AGInventor: Edwin Bernard Villhauer
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Patent number: 6107316Abstract: A method for treating protozoal infections is described. The method employs N-acetonylbenzamide compounds provided in an effective amount to inhibit the growth of protozoans. The compounds are useful in controlling such protozoan parasites as Giardia lamblia, Leishmania major, Entamoeba histolytica, Cryptosporidium parvum, Toxoplasma gondii and microsporidia.Type: GrantFiled: April 29, 1998Date of Patent: August 22, 2000Assignee: Rohm and Haas CompanyInventors: David Hamilton Young, Enrique Luis Michelotti, Thomas David Edlind, Santosh Kumar Katiyar
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Patent number: 6107311Abstract: A compound having the structure: ##STR1## wherein (a) n is from 1 to about 3;(b) X is selected from the group consisting of O, S, SO, or SO.sub.2 ;(c) Y is independently hydrogen or straight, branched or cyclic alkyl having from 1 to about 4 carbon atoms, or the Y's are bonded together to form an alkanyl ring having from about 3 to about 7 atoms;(d) Z is hydrogen or straight, branched or cyclic alkyl having from 3 to about 10 atoms other than hydrogen;(e) W is O or S; and(f) Het is a heteroaryl group comprising one or more rings each ring containing from about 5 to about 6 atoms other than hydrogen and wherein the group contains at least one heteroatom selected from O, N, or S.pharmaceutical compositions comprising such compounds, and methods of treating inflammation or pain using such compounds.Type: GrantFiled: April 9, 1998Date of Patent: August 22, 2000Assignee: The Procter & Gamble CompanyInventors: Laurence Ichih Wu, John Michael Janusz
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Patent number: 6103910Abstract: New compounds have the formula: ##STR1## wherein R, R.sup.1, X and Y have the meanings described herein. Methods are set forth for synthesizing these compounds and using these compounds to treat diseases associated with amyloidosis, such as Alzheimer's disease, maturity onset diabetes mellitus, familial amyloid polyneuropathy, scrapie, and Kreuzfeld-Jacob disease.Type: GrantFiled: October 27, 1998Date of Patent: August 15, 2000Assignee: Hoffmann-La Roche Inc.Inventors: Cornelia Hertel, Torsten Hoffmann, Roland Jakob-Roetne, Roger David Norcross
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Patent number: 6100282Abstract: Compounds of the formula: as well as pharmaceutically usable salts and esters thereof, wherein R.sup.1, R.sup.2 and R.sup.3 have the significance ascribed herein, inhibit binding of adhesive proteins to the surface of different types of cell and accordingly influence cell--cell and cell-matrix interactions. These compounds can be used in the form of pharmaceutical preparations for the control or prevention of neoplasms, tumor metastasing, tumor growth, osteoporosis, Paget's disease, diabetic retinopathy, macular degeneration, restenosis following vascular intervention, psoriasis, arthritis, fibrosis, kidney failure, as well as infection caused by viruses, bacteria or fungi.Type: GrantFiled: December 22, 1998Date of Patent: August 8, 2000Assignee: Hoffman-La Roche Inc.Inventors: Leo Alig, Albrecht Edenhofer, Kurt Hilpert, Thomas Weller
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Patent number: 6096898Abstract: One pot synthesis of 1,2,4-triazoles uses thioimidate intermediate and 1,2-dichloroethane solvent.Type: GrantFiled: October 22, 1999Date of Patent: August 1, 2000Assignee: Dow AgroSciences LLCInventors: David E. Podhorez, John W. Hull, Jr., Christine H. Brady
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Patent number: 6096747Type: GrantFiled: May 28, 1996Date of Patent: August 1, 2000Assignee: Celltech Therapeutics LimitedInventors: Nigel Robert Arnold Beeley, Thomas Andrew Millican
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Patent number: 6093696Abstract: Tyrosine derivatives of formula (1) are described: ##STR1## in which R is (1) a group R.sup.1 X.sup.1 -- where R.sup.1 is an optionally substituted alkyl or aromatic group, and X.sup.1 is a covalent bond or a --(CH.sub.2).sub.n -- [where n is an integer 1 or 2], --C(O)--, --CH.sub.2 C(O)--, --NHC(O)--, --CH.sub.2 NHC(O)--, or --SO.sub.2 -- group, or (2) a group (Hal.sup.1).sub.3 CSO.sub.2 --, where Hal.sup.1 is a fluorine or chlorine atom;R.sup.2 and R.sup.3, which may be the same or different, is each a hydrogen or halogen atom or an alkyl, alkoxy, hydroxyl or nitro group;Alk is an alkylene chain;m is zero or an integer 1;R.sup.4 is a hydrogen atom or a methyl group;R.sup.5 is a group --(CH.sub.2).sub.p CO.sub.2 R.sup.8 where p is zero or an integer 1 and R.sup.8 is a hydrogen atom or an alkyl group;R.sup.6 is a hydrogen atom or an alkyl group;Y is a sulphur atom or a --S(O).sub.q -- group where q is an integer 1 or 2;X.sup.2 is a --C(O)--, --C(O)O--, --CONH-- or --S(O).sub.2 -- group;R.sup.Type: GrantFiled: May 29, 1998Date of Patent: July 25, 2000Assignee: Celltech Therapeutics, LimitedInventors: John Clifford Head, Sarah Catherine Archibald, Graham John Warrellow
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Patent number: 6046190Abstract: The invention relates to sulfonamide-containing hydroxyethylamine protease inhibitor compounds, their process of making, composition and method of use for inhibiting retroviral proteases such as human immunodeficiency virus.Type: GrantFiled: January 24, 1996Date of Patent: April 4, 2000Assignee: G.D. Searle & Co.Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, John N. Freskos, Deborah E. Bertenshaw, Robert M. Heintz
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Patent number: 6043262Abstract: The present invention provides thifluzamide which has changed its crystalline form, its preparation method, and a pesticide composition containing thifluzamide as its effective ingredient. The rate of dissolution of the thifluzamide obtained is high and the pesticide compounds containing it has improved efficacy.Type: GrantFiled: November 24, 1998Date of Patent: March 28, 2000Assignee: Rohm and Haas CompanyInventors: Norihito Hayakawa, Masatoshi Baba, Norihiro Suwa, Kazuhiro Yamagishi
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Patent number: 6022885Abstract: This invention relates to a method of treating bacterial infections in humans or animals comprising administering, in combination with a .beta.-lactam antibiotic, a therapeutically effective amount of a compound of formula (I).Type: GrantFiled: June 10, 1998Date of Patent: February 8, 2000Assignee: SmithKline Beecham p.l.c.Inventors: Martin Leonard Gilpin, David John Payne, John Hargreaves Bateson
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Patent number: 6020357Abstract: The present application describes nitrogen containing heteroaromatics and derivatives thereof of formula I: ##STR1## or pharmaceutically acceptable salt or prodrug forms thereof, wherein J is N or NH and D may be C(.dbd.NH)NH.sub.2, which are useful as inhibitors of factor Xa.Type: GrantFiled: December 22, 1997Date of Patent: February 1, 2000Assignee: DuPont Pharmaceuticals CompanyInventors: Donald Joseph Phillip Pinto, James Russell Pruitt, Joseph Cacciola, John Matthew Fevig, Qi Han, Michael James Orwat, Mimi Lifen Quan, Karen Anita Rossi
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Patent number: 6013663Abstract: A compound of formula (I): ##STR1## wherein one of m and n represents 0, and the other represents 0, 1 or 2; k represents 0 or 1 to 12; R.sup.1 is hydrogen, an aryl, a heterocyclic, an alkyl, a hydroxy or --OR.sup.7, wherein R.sup.7 is an alkyl, an alkenyl or an aralkyl; A is --CON(R.sup.2)SO.sub.2--, wherein R.sup.2 is hydrogen, an alkyl or an aralkyl; B is a single bond; and pharmaceutically acceptable salts thereof. The compounds have the ability to enhance the activity of glutathione reductase and can therefore be used for the treatment and prevention of a variety of diseases including cataracts.Type: GrantFiled: March 31, 1998Date of Patent: January 11, 2000Assignee: Sankyo Company, LimitedInventors: Takashi Fujita, Tomihisa Yokoyama
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Patent number: 5998424Abstract: The present application describes inhibitors of factor Xa with a neutral P1 specificity group of formula I: ##STR1## or pharmaceutically acceptable salt forms thereof, wherein R and E may be groups such as methoxy and halo.Type: GrantFiled: June 18, 1998Date of Patent: December 7, 1999Assignee: DuPont Pharmaceuticals CompanyInventors: Robert A. Galemmo, Jr., Celia Dominguez, John M. Fevig, Qi Han, Patrick Y. Lam, Donald J. P. Pinto, James R. Pruitt, Mimi L. Quan
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Patent number: 5998450Abstract: Biphenylamides of the general formula I ##STR1## and their salts (A= ##STR2## R.sup.1 =F; R.sup.2 =H, halogen, alkyl, CF.sub.3, alkoxy, alkylthio; R.sup.3 =Cl, CF.sub.3 ; R.sup.4 =H, CH.sub.3 ; R.sup.5 =Cl, CH.sub.3, CHF.sub.2, CF.sub.3 ;R.sup.6 =CH.sub.3, CHF.sub.2, CF.sub.3), and compositions comprising I, the preparation of I and of the compositions, and of the use of both of them for controlling harmful fungi.Type: GrantFiled: February 17, 1998Date of Patent: December 7, 1999Assignee: BASF AktiengesellschaftInventors: Karl Eicken, Harald Rang, Albrecht Harreus, Norbert Gotz, Eberhard Ammermann, Gisela Lorenz, Siegfried Strathmann
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Patent number: 5985911Abstract: C-terminal 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: November 16, 1999Assignee: Abbott LaboratoriesInventors: Steven K. Davidsen, Alan S. Florjancic, George S. Sheppard, Jamie R. Giesler, Lianhong Xu, Yan Guo, Michael L. Curtin, Michael R. Michaelides, Carol K. Wada, James H. Holms
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Patent number: 5935973Abstract: Compounds of formula I ##STR1## and pharmaceutically acceptable salts thereof in which A is methylene or O; B is methylene or O; g is 0,1,2,3 or 4; R.sub.1 is an optional substituent; U is an alkylene chain optionally substituted by one or more alkyl; Q represents a divalent group containing nitrogen atoms; and T represents CO.HET, have utility in the treatment of central nervous system disorders, for example depression, anxiety, psychoses (for example schizophrenia), tardive dyskinesia, Parkinson's disease, obesity, hypertension, Tourette's syndrome, sexual dysfunction, drug addiction, drug abuse, cognitive disorders, Alzheimer's disease, senile dementia, obsessive-compulsive behavior, panic attacks, social phobias, eating disorders and anorexia, cardiovascular and cerebrovascular disorders, non-insulin dependent diabetes mellitus, hyperglycaemia, constipation, arrhythmia, disorders of the neuroendocrine system, stress, prostatic hypertrophy, and spasticity.Type: GrantFiled: January 5, 1998Date of Patent: August 10, 1999Assignee: Knoll AktiengesellschaftInventors: Alan Martin Birch, David John Heal, Frank Kerrigan, Keith Frank Martin, Patricia Lesley Needham, Bruce Jeremy Sargent
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Patent number: 5925659Abstract: A compound represented by formula I: ##STR1## is disclosed. The compounds are active primarily against gram negative organisms. Pharmaceutical compositions and methods of treatment are also disclosed.Type: GrantFiled: April 25, 1997Date of Patent: July 20, 1999Assignee: Merck & Co., Inc.Inventors: Arthur A. Patchett, Ravi Nargund, Meng-Hsin Chen, H. Russell Onishi
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Patent number: 5922740Abstract: Heterocyclyclcarbonyl substituted benzofuranyl-ureas are prepared by reacting heterocyclylcarbonyl substituted 3-amino-benzofuranes with appropriate isocyanates or isothiocyanates. The unsubstituted ureas are transferred into substituted ureas by usual methods of substitution. The heterocyclylcarbonyl substituted benzofuranyl-ureas are useful as active ingredients in medicaments particularly for the treatment of acute and chronical inflammatory processes.Type: GrantFiled: December 4, 1996Date of Patent: July 13, 1999Assignee: Bayer AktiengesellschaftInventors: Gabriele Braunlich, Mazen Es-Sayed, Rudiger Fischer, Burkhardt Fugmann, Rolf Henning, Michael Sperzel, Ulrich Nielsch, Graham Sturton
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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
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Patent number: 5917048Abstract: Compounds of the formula ##STR1## wherein the symbols have the meaning described in the specification, have retinoid-like biological activity.Type: GrantFiled: March 19, 1997Date of Patent: June 29, 1999Assignee: Allergan Sales Inc.Inventors: Min Teng, Tien T. Duong, Roshantha A. Chandraratna
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Patent number: 5914344Abstract: A substituted carboxanilide derivative represented by the formula (1): ##STR1## wherein A is a hydrogen atom or methyl, B is a methyl or ethyl, and Het is 1-methyl-3-substituted-4-pyrazolyl or 2-methyl-4-substituted-5-triazoyl group, exhibits a disease control effect against Botrytis cinerea, Powdery mildew, Pyricularia oryzae of rice plant and other various plant diseases, is excellent in residual effect, has also activity against resistant strain for conventional chemicals, particularly exerts control effects against Botrytis cinerea at a lower dosage as compared with a prior art, is also safe for crops, and thus is useful as a plant control agent.Type: GrantFiled: August 7, 1997Date of Patent: June 22, 1999Assignee: Mitsui Chemicals, Inc.Inventors: Yukihiro Yoshikawa, Kanji Tomiya, Naofumi Tomura, Hiroyuki Katsuta, Osamu Takahashi, Shunichi Inami, Yuji Yanase, Junro Kishi, Hideo Kawashima
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Patent number: 5891897Abstract: Oxopropionitrile derivatives represented by general formula (1), and insect pest control agents containing the same as the active ingredient and having reduced toxicity and persistence. In said formula R.sup.1 represents C.sub.2 -C.sub.8 alkyl, etc., R.sup.2 represents hydrogen, etc.; R.sup.3 represents a heterocyclic group; and R.sup.4 represents hydrogen, etc.Type: GrantFiled: October 27, 1997Date of Patent: April 6, 1999Assignee: Nissan Chemical Industries, Ltd.Inventors: Tomoyuki Ogura, Hiroshi Murakami, Rika Miyachi, Takeshi Nagaoka, Toshiro Miyake, Norihiko Mimori, Shinji Takii, Youichi Inoue
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Patent number: 5886188Abstract: The present invention relates to a method for converting 5-carboxanilido-haloalkylthiazoles having mixed structural forms into a single structural form. The invention also provides single-structural form 5-carboxanilido-haloalkylthiazoles, compositions of the single-structural form 5-carboxanilido-haloalkylthiazoles, and methods to formulate such compounds.Type: GrantFiled: June 10, 1997Date of Patent: March 23, 1999Assignee: Rohm and Haas CompanyInventors: Lois Merle Bryman, Enrique Luis Michelotti, Luong Tu Nguyen
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Patent number: 5872121Abstract: A compound of the formula ##STR1## wherein R is a) phenyl; phenyl(C.sub.1 -C.sub.4 alkoxy); phenoxy; or benzyl; the phenyl ring of each substituent being optionally substituted with one or more of halogen, nitro, C.sub.1 -C.sub.8 alkyl, C.sub.1 -C.sub.8 alkoxy, C.sub.1 -C.sub.8 haloalkyl, C.sub.1 -C.sub.8 haloalkoxy, di(C.sub.1 -C.sub.8 alkyl)amino, phenyl or phenoxy; or b) a 5- or 6-membered heterocyclic group comprising 1-3 heteroatoms selected from the group consisting of N, O or S, optionally substituted with one or more of halogen, nitro, C.sub.1 -C.sub.8 alkyl, C.sub.1 -C.sub.8 alkoxy, C.sub.1 -C.sub.8 haloalkyl, C.sub.1 -C.sub.8 haloalkoxy, or di-(C.sub.1 -C.sub.8 alkyl)amino. These compounds and pesticidal compositions prepared therefrom, are useful as plant protecting agents for the control of insects, nematodes, and mites.Type: GrantFiled: August 21, 1997Date of Patent: February 16, 1999Assignee: Uniroyal Chemical Company, Inc.Inventors: Mark Achiel Dekeyser, Paul Thomas McDonald
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Patent number: 5869508Abstract: Novel 1,2,3-benzothiadiazole derivatives of the formula ##STR1## in which Het has the meanings set forth in the specification,and addition products thereof with an acid or metal salt are very effective for the control of undesired microorganisms.Novel intermediates of the formulae ##STR2## in which Het.sup.1 and R.sup.5 have the meanings given in the specification.Type: GrantFiled: July 1, 1997Date of Patent: February 9, 1999Assignee: Nihon Bayer Agrochem K.K.Inventors: Yoshio Kurahashi, Haruko Sawada, Taro Kinbara, Yasuo Araki, Koichi Moriya, Koichi Ishikawa, Asami Motonaga
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Patent number: 5852043Abstract: 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: December 22, 1998Assignee: Agouron Pharmaceuticals, Inc.Inventors: Vincent J. Kalish, Siegfried Heinz Reich, John H. Tatlock, Michael J. Rodriguez