Polycyclo Ring System Having The Asymmetrical Triazine Ring As One Of The Cyclos Patents (Class 544/183)
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Publication number: 20030144293Abstract: The present invention relates to novel to N-alkyl adamantyl triazinyl benzylamide derivatives of formmula I 1Type: ApplicationFiled: November 12, 2002Publication date: July 31, 2003Applicant: Pfizer Inc.Inventor: Allen J. Duplantier
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Publication number: 20030144507Abstract: The present invention provides a sulfonamide- or sulfonylurea-containing heterocyclic compounds. Specifically, it provides a heterocyclic compound represented by the formula (I), a pharmacologically acceptable salt thereof or a hydrate of them.Type: ApplicationFiled: June 10, 2002Publication date: July 31, 2003Inventors: Toru Haneda, Akihiko Tsuruoka, Junichi Kamata, Tadashi Okabe, Keiko Takahashi, Kazumasa Nara, Shinichi Hamaoka, Norihiro Ueda, Toshiaki Wakabayashi, Yasuhiro Funahashi, Taro Semba, Naoko Hata, Yuji Yamamoto, Yoichi Ozawa, Naoko Tsukahara, Takashi Owa
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Publication number: 20030114457Abstract: The present invention relates to novel inhibitors of Factors VIIa, IXa, Xa, XIa, in particular Factor VIIa, pharmaceutical compositions comprising these inhibitors, and methods for using these inhibitors for treating or preventing thromboembolic disorders. Processes for preparing these inhibitors are also disclosed.Type: ApplicationFiled: July 3, 2002Publication date: June 19, 2003Applicant: Axys Pharmaceuticals, Inc.Inventors: Huiyong Hu, John Hendrix, Aleksandr Kolesnikov, Roopa Rai, William Dvorak Shrader, David Sperandio, Wendy Young, Steve Torkelson
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Patent number: 6562944Abstract: Disclosed is an improved method for preparing an activated carboxylic acid in the form of a pentafluorophenyl ester, an improved method for making a carboxamide from a pentaflourophenyl ester, and a carboxamide and carboxamide library prepared using both of these methods.Type: GrantFiled: March 22, 2000Date of Patent: May 13, 2003Assignee: Lexicon PharmaceuticalsInventors: Hartmuth C. Kolb, Qun Sun
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Publication number: 20030087907Abstract: An object of the present invention is to provide compounds having potent antitumor activity.Type: ApplicationFiled: April 26, 2002Publication date: May 8, 2003Applicant: KIRIN BEER KABUSHIKI KAISHAInventors: Kazuo Kubo, Teruyuki Sakai, Rika Nagao, Yasunari Fujiwara, Toshiyuki Isoe, Kazumasa Hasegawa
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Patent number: 6545155Abstract: Glucokinase activating amides useful for increasing insulin secretion in the treatment of type II diabetes are disclosed.Type: GrantFiled: December 4, 2001Date of Patent: April 8, 2003Assignee: Hoffmann-La Roche Inc.Inventors: Wendy Lea Corbett, Joseph Samuel Grimsby, Nancy-Ellen Haynes, Robert Francis Kester, Paige Erin Mahaney, Ramakanth Sarabu
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Publication number: 20030064990Abstract: Compound of general formula I: 1Type: ApplicationFiled: March 12, 2002Publication date: April 3, 2003Inventors: Stephen Martin Denton, Mark Ian Kemp, Sandra Dora Newman, David James Rawson
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Publication number: 20030055059Abstract: The present invention describes novel imidazo-pyridines, -pyridazines, and -triazines of formula I: 1Type: ApplicationFiled: February 11, 2002Publication date: March 20, 2003Inventors: Paul Joseph Gilligan, Richard Eric Olson, William Eric Frietze
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Patent number: 6525056Abstract: Corticotropin releasing factor (CRF) antagonists of Formula (I): and their use in treating psychiatric disorders and neurological diseases, anxiety-related disorders, post-traumatic stress disorder, supranuclear palsy and feeding disorders as well as treatment of immunological, cardiovascular or heart-related diseases and colonic hypersensitivity associated with psychopathological disturbance and stress in mammals.Type: GrantFiled: February 21, 2001Date of Patent: February 25, 2003Assignee: Bristol-Myers Squibb CompanyInventors: Argyrios G. Arvanitis, Paul J. Gilligan, James P. Beck, Rajagopal Bakthavatchalam
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Publication number: 20030027829Abstract: Compounds which are useful as potassium channel inhibitors and which because of their slow off-rates are especially useful for the treatment of cardiac arrhythmias are described.Type: ApplicationFiled: July 24, 2001Publication date: February 6, 2003Inventors: Aimee Dolores Reed, Michael Francis Gross, Serge Beaudoin
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Patent number: 6514972Abstract: A compound of the formula wherein, independently at each occurrence, v, w, and x are selected from C, N, O, and S, with H substitution as needed to fulfill open valence sites; y and z are selected from N and C, with H substitution as needed to fulfill open valence sites, with the proviso that each of w, v, x, y and z is not simultaneously C; the ring formed from v, w, x, y and z may be saturated or unsaturated; and R1, R2, R3 and R4 are selected from hydrogen, alkyl, aryl, alkaryl, aralkyl, heteroalkyl, and heteroaryl; wherein any adjacent two of R1, R2, R3 and R4 may join together to form a 5, 6 or 7-membered carbocyclic or heterocyclic ring, with the proviso that each of R1, R2, R3 and R4 is not simultaneously hydrogen. Pharmaceutical compositions of said compounds, and methods of use in the treatment of biological conditions including cellular hyperproliferation, are disclosed.Type: GrantFiled: July 6, 2001Date of Patent: February 4, 2003Assignee: Kinetek Pharmaceuticals, Inc.Inventors: Zaihui Zhang, Xinyao Du, Serguei Sviridov, Greg Chopiuk
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Publication number: 20030013714Abstract: This invention is directed to novel aryl sulfonamide and sulfamide compounds which bind selectively to and inhibit the activity of the human Y5 receptor. This invention is also related to uses of these compounds for the treatment of feeding disorders such as obesity, anorexia nervosa, bulimia nervosa, and abnormal conditions such as sexual/reproductive disorders, depression, epileptic seizure, hypertension, cerebral hemorrhage, congestive heart failure or sleep disturbances and for the treatment of any disease in which antagonism of a Y5 receptor may be useful.Type: ApplicationFiled: April 2, 2002Publication date: January 16, 2003Applicant: Synaptic Pharmaceutical CorporationInventors: Imadul Islam, Daljit S. Dhanoa, John M. Finn, Ping Du, Charles Gluchowski, Yoon T. Jeon
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Patent number: 6492364Abstract: Novel triazolo derivatives represented by the following formula and pharmaceutically acceptable salts thereof, as well as chemokine inhibitors containing the same as an effective component. These are useful as therapeutic agents for allergic diseases such as bronchial asthma and atopic dermatitis; therapeutic agents for inflammatory diseases such as chronic rheumatoid arthritis; therapeutic agents for autoimmune diseases such as ulcerative colitis and nephritis; and as anti-AIDS drugs.Type: GrantFiled: September 22, 2000Date of Patent: December 10, 2002Assignee: Toray Industries, Inc.Inventors: Toshiya Takahashi, Takayuki Imaoka, Noriko Mori, Masayuki Kaneko, Koh Tanida, Yuichi Torii
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Patent number: 6476028Abstract: A method of treating a CCR5-mediated disease state in mammals which comprises administering to a mammal in need of such treatment, an effective amount of a compound of formula (I) or a pharmaceutically acceptable salt thereof.Type: GrantFiled: August 8, 2000Date of Patent: November 5, 2002Assignees: SmithKline Beecham Corporation, SmithKline Beecham p.l.c.Inventors: William E. Bondinell, James Chan, Roderick A. Porter, Joseph W. Venslavsky, Steven Dabbs, David T. Davies
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Patent number: 6472391Abstract: 1,2,3 Triazines according to formula (I): and pharmaceutically acceptable salts thereof inhibit phosphorylation of platelet-derived growth factor receptor and thereby hinder abnormal cell growth and cell wandering.Type: GrantFiled: December 13, 2000Date of Patent: October 29, 2002Assignee: Millennium Pharmaceuticals, Inc.Inventors: Kenji Matsuno, Michio Ichimura, Yuji Nomoto, Shigeki Fujiwara, Shinichi Ide, Eiji Tsukuda, Junko Irie, Shoji Oda
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Patent number: 6469167Abstract: An improved process for the preparation of 5-[4-[[3-Methyl-4-oxo-3,4-dihydroquinazolin-2-yl]methoxy]benzyl]thiazolidine-2,4-dione of formula (1) which comprises: reducing the compound of formula (2′) where R represents a (C1-C4)alkyl group using Raney Nickel or Magnesium in alcohol having 1 to 4 carbon atoms or mixtures thereof, if desired reesterifying using sufphuric acid at a temperature in the range of 0° C. to 60° C. to obtain a compound of formula (3′) wherein R is as defined above, hydrolyzing the compound of formula (3′) wherein R is as defined above, by conventional methods to obtain the acid of formula (4), condensing the acid of formula (4) with N-methyl anthranilamide directly without any preactivation of the acid to produce the compound of formula (1) and if desired, converting the compound of formula (1) to pharmaceutically acceptable salts thereof by conventional methods.Type: GrantFiled: May 2, 2001Date of Patent: October 22, 2002Assignee: Dr. Reddy's Research FoundationInventors: Prabhakar Chebiyyam, Rajender Kumar Potlapally, Chinna Bakki Reddy Gade, Balaram Mahanti Satish, Ramabhadra Sarma Mamillapalli, Om Reddy Gaddam
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Publication number: 20020128479Abstract: A method of preparing a pyrrolotriazin-4-one and a method of preparing the isothiocyanatoformic acid ester derivative which can be used as a reactant in that method of preparing a pyrrolotriazin-4-one. The method of preparing the pyrrolotriazin-4-one includes an addition step of an aminopyrrole derivative and the isothiocyanatoformic compound and a step of ring-closing reaction of a resulting adduct.Type: ApplicationFiled: February 14, 2002Publication date: September 12, 2002Applicant: FUJI PHOTO FILM CO., LTD.Inventor: Tetsunori Matsushita
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Patent number: 6448399Abstract: Glucokinase activating amides are useful for increasing insulin secretion in the treatment of type II diabetes.Type: GrantFiled: December 4, 2001Date of Patent: September 10, 2002Assignee: Hoffmann-La Roche Inc.Inventors: Wendy Lea Corbett, Joseph Samuel Grimsby, Nancy-Ellen Haynes, Robert Francis Kester, Paige Erin Mahaney, Ramakanth Sarabu
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Patent number: 6448248Abstract: The present invention relates to carboxylic acid derivatives of the formula I where the substituents have the meanings explained in the description, and to preparation and use as endothelin receptor antagonists.Type: GrantFiled: June 14, 1999Date of Patent: September 10, 2002Assignee: Abbott LaboratoriesInventors: Wilhelm Amberg, Rolf Jansen, Andreas Kling, Dagmar Klinge, Hartmut Riechers, Stefan Hergenröder, Manfred Raschack, Liliane Unger
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Patent number: 6444672Abstract: The present invention relates to heterocyclic antithrombotic compounds comprising a compound of the Formula I, wherein X′ is independently CH or N, and m is 0, 1, 2 or 3, or a pharmaceutically acceptable salt or prodrug thereof.Type: GrantFiled: April 17, 2000Date of Patent: September 3, 2002Assignee: Akzo Nobel N.V.Inventors: Constant Adriaan Anton van Boeckel, Philippus Johannes Marie van Galen, Johannes Bernardus Maria Rewinkel
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Patent number: 6432975Abstract: Pharmaceutical compositions include aryl substituted amine compounds, and in particular, carbon-linked aromatic azabicyclo compounds, and in particular, aromatic alkylene azabicyclo compounds and aromatic alkyl azabicyclo compounds.Type: GrantFiled: December 11, 1998Date of Patent: August 13, 2002Assignee: Targacept, Inc.Inventors: Jeffrey Daniel Schmitt, Peter Anthony Crooks, Gary Maurice Dull
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Patent number: 6432955Abstract: The present invention relates to therapeutically active antithrombotic compounds.Type: GrantFiled: October 4, 2000Date of Patent: August 13, 2002Assignee: Akzo Nobel N.V.Inventors: Constant Adriaan Anton van Boeckel, Philippus Johannes Marie van Galen, Johannes Bernardus Maria Rewinkel
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Publication number: 20020107396Abstract: Glucokinase activating amides are useful for increasing insulin secretion in the treatment of type II diabetes.Type: ApplicationFiled: December 4, 2001Publication date: August 8, 2002Inventors: Wendy Lea Corbett, Joseph Samuel Grimsby, Nancy-Ellen Haynes, Robert Francis Kester, Paige Erin Mahaney, Ramakanth Sarabu
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Publication number: 20020103199Abstract: Glucokinase activating amides are useful for increasing insulin secretion in the treatment of type II diabetes.Type: ApplicationFiled: December 4, 2001Publication date: August 1, 2002Inventors: Wendy Lea Corbett, Joseph Samuel Grimsby, Nancy-Ellen Haynes, Robert Francis Kester, Paige Erin Mahaney, Ramakanth Sarabu
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Publication number: 20020103200Abstract: A method of using 1,2,4-benzotriazine oxides, some of which are novel compounds, as radiosensitizers and selective cytotoxic agents is disclosed. These compounds are shown to specifically radiosensitize hypoxic tumor cells. Some are additionally disclosed to be useful as specific cytotoxic agents for these cells. They also show an unexpected ability to radiosensitize aerobic cells following or preceding a hypoxic incubation of the cells with the drug. This provides a basis for selective radiosensitization of tumors compared to normal cells. A novel method for preparing the 1,2,4-benzotriazine oxides is also disclosed.Type: ApplicationFiled: December 17, 2001Publication date: August 1, 2002Inventors: William W. Lee, J. Martin Brown, Edward W. Grange, Abelardo P. Martinez, Michael Tracy, Daniel J. Pollart
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Patent number: 6426346Abstract: The present application describes 6-membered aromatics of formula I: or pharmaceutically acceptable salt forms thereof, wherein D may be CH2NH2 or C(═NH)NH2, which are useful as inhibitors of factor Xa.Type: GrantFiled: February 15, 2000Date of Patent: July 30, 2002Assignee: Bristol - Myers Squibb Pharma CompanyInventors: James Russell Pruitt, Donald Joseph Phillip Pinto, Mimi Lifen Ouan, Ruth Richmond Wexler
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Publication number: 20020040019Abstract: Substituted pyrazoles, methods of manufacturing them, compositions containing them, and methods of using them to treat, for example, autoimmune diseases mediated by cathepsin S are described.Type: ApplicationFiled: August 10, 2001Publication date: April 4, 2002Inventors: Hui Cai, James P. Edwards, Steven P. Meduna, Barbara A. Pio, Jianmei Wei
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Publication number: 20020025960Abstract: The present invention provides a compound of formula I 1Type: ApplicationFiled: June 22, 2001Publication date: February 28, 2002Inventors: Gordon L. Bundy, Fred L. Ciske, Michael J. Genin, Steven E. Heasley, Scott D. Larsen, Byung Hyun Lee, Paul D. May, John R. Palmer, Mark E. Schnute, Valerie A. Vaillancourt, Atli Thorarensen, Allison J. Wolf, Nancy Anne Wicnienski, David Wilhite
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Publication number: 20020013317Abstract: Disclosed are compounds of the formula: 1Type: ApplicationFiled: July 2, 2001Publication date: January 31, 2002Applicant: Neurogen CorporationInventors: William Greenlee, Ashit Gangly, Jan W.F. Wasley
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Patent number: 6303542Abstract: This invention relates to 3-substituted-phenyl-1,2,3-benzotriazin-4-ones which have activity as herbicides, to compositions which contain these compounds and to methods of use of these compounds.Type: GrantFiled: August 18, 2000Date of Patent: October 16, 2001Assignee: Rohm and Haas CompanyInventors: Bin Li, Adam Chi-Tung Hsu
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Patent number: 6245769Abstract: Corticotropin releasing factor (CRF) antagonists of Formula (I): and their use in treating psychiatric disorders and neurological diseases, anxiety-related disorders, post-traumatic stress disorder, supranuclear palsy and feeding disorders as well as treatment of immunological, cardiovascular or heart-related diseases and colonic hypersensitivity associated with psychopathological disturbance and stress in mammals.Type: GrantFiled: September 1, 1998Date of Patent: June 12, 2001Assignee: DuPont Pharmaceuticals CompanyInventors: Argyrios G. Arvanitis, Paul J. Gilligan, James P. Beck, Rajagopal Bakthavatchalam
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Patent number: 6197766Abstract: Insecticidal dihydrooxadiazine compounds having the formula: wherein X is O, N or S; R is a substituted or unsubstituted phenyl or C4-C5 heterocyclic group; R2, R3, R4, and R5 are one of the following: a) R2, R3, and R4 are, independently, hydrogen, alkyl, alkoxy, or furanyl; and R5 is nitro, cyano, alkyl, dialkylamino, alkylthio, alkoxy, haloalkoxy, phenoxy, phenylthio, or alkoxycarbonyl, wherein R3 and R5 together can form a ring; or b) R3, R4, and R5 are hydrogen; and R2 is alkylthio, alkylsulfinyl, alkylsulfonyl, nitroalkoxy, hydroxy, dialkoxyphosphinyl, cyano, acyloxy, alkoxy, haloalkoxy, cycloalkyl, or alkenyl; or R2 is a substituted or unsubstituted phenyl, phenylthio, phenylsulfinyl, phenylsulfonyl, pyrazolyl, furanyl, thienyl, phenylalkoxy, or benzoyloxy; and R6 is hydrogen, alkyl, alkylthio, alkoxyalkyl, acyl, benzyl, or alkoxycarbonyl.Type: GrantFiled: January 11, 1999Date of Patent: March 6, 2001Assignees: Uniroyal Chemical Company, Inc. and Uniroyal Chemical Co., Uniroyal Chemical Cie.Inventors: Sheldon Bernard Park, Anupama Mishra, Mark Achiel Dekeyser, Paul Thomas McDonald
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Patent number: 6194409Abstract: The present invention relates to antithrombotic compounds comprising the group Q, Q having formula (I), wherein the substructure (i) is a structure selected from (a, b and c), wherein X is O or S; X′ being independently CH or N; and m is 0, 1, 2 or 3; wherein the group Q is bound through an oxygen atom or an optionally substituted nitrogen or carbon atom, or a pharmaceutically acceptable salt thereof or a prodrug thereof. The compounds of the invention are therapeutically active and in particular are antithrombotic agents.Type: GrantFiled: October 19, 1999Date of Patent: February 27, 2001Assignee: Akzo Nobel N.V.Inventors: Constant Adriaan Anton van Boeckel, Philippus Johannes Marie van Galen, Johannes Bernardus Maria Rewinkel
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Patent number: 6166205Abstract: Disclosed are compounds of the formula: ##STR1## or the pharmaceutically acceptable acid addition salts thereof wherein: R.sub.a represents ##STR2## where X, Y and Z are the same or different and represent CH or nitrogen;R.sub.1 R.sub.2, R.sub.3 and R.sub.4 independently represent organic or inorganic groups; andR.sub.5 is hydrogen, C.sub.1 -C.sub.6 alkyl or halogen,which compounds are useful for the treatment and/or prevention of neuropsychological disorders including, but not limited to, schizophrenia, mania, dementia, depression, anxiety, compulsive behavior, substance abuse, Parkinson-like motor disorders and motion disorders related to the use of neuroleptic agents.Type: GrantFiled: September 2, 1999Date of Patent: December 26, 2000Assignee: Neurogen CorporationInventors: Xi Chen, Andrew Thurkauf
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Patent number: 6121278Abstract: A compound of formula I: ##STR1## or a pharmaceutically acceptable salt, hydrate, ester, solvate, prodrug, metabolite, stereoisomer, or mixtures thereof, wherein:Y represents the atoms necessary to form a fused 5- to 6-membered, aromatic or non-aromatic, heterocyclic ring containing at least one nitrogen heteroatom in a 1,3-relationship with the nitrogen atom depicted in formula I, wherein Y may be unsubstituted or substituted with at least one alkyl, alkenyl, cycloalkyl, cycloalkenyl, aralkyl, aryl, double bonded oxygen, or --COOR.sup.5 group, or a moiety selected from the group consisting of: ##STR2## wherein R.sup.5 and R.sup.7 are independently hydrogen or alkyl, alkenyl, cycloalkyl, cycloalkenyl, aralkyl, or aryl.Type: GrantFiled: September 1, 1998Date of Patent: September 19, 2000Assignee: Guilford Pharmaceuticals, Inc.Inventors: Paul F. Jackson, Keith M. Maclin, Jie Zhang
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Patent number: 6114524Abstract: The present invention relates to a process for producing a compound represented by the formula (II): ##STR1## wherein X is a halogen atom, each of A.sup.1, A.sup.2 and A.sup.3 are the same or different and are selected from a carbon atom or a nitrogen atom, provided that at least A.sup.1, A.sup.2, or A.sup.3 is a nitrogen atom. Each of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are the same or different and are selected from a hydrogen atom, a lower alkyl group, a cyano group, a carboxyl group, a lower alkoxycarbonyl group, a halogen atom, and a nitro group. It is also provided that where R.sup.1 and R.sup.2 are adjacent to each other, R.sup.1 and R.sup.2 may be combined with each other to form a 5- or 6-membered ring which may carry on the ring thereof one substituent selected from the group consisting of a lower alkyl group, a nitrile group, a carboxyl group, a lower alkoxycarbonyl group, a carbamoyl group, a halogen atom, a nitro group, and an amino-(lower alkyl) group.Type: GrantFiled: June 8, 1999Date of Patent: September 5, 2000Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Shigemitsu Okada, Ryosuke Ushijima, Kiyofumi Ishikawa
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Patent number: 6093821Abstract: Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.Type: GrantFiled: October 8, 1997Date of Patent: July 25, 2000Assignee: Ligand Pharmaceuticals IncorporatedInventors: Todd K. Jones, Mark E. Goldman, Charlotte L. F. Pooley, David T. Winn, James P. Edwards, Sarah J. West, Christopher M. Tegley, Lin Zhi
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Patent number: 6084120Abstract: The present invention relates to compounds having the formulae ##STR1## wherein R, R.sup.1, R.sup.6, R.sup.7, Rn.sup.8, X, and Z are defined herein, which are useful in the treatment or prophylaxis of malaria. The compounds of the present invention are especially useful in the treatment or prophylaxis of chloroquine-sensitive and chloroquine-resistant malaria.Type: GrantFiled: June 22, 1998Date of Patent: July 4, 2000Assignee: Hoffmann-La Roche Inc.Inventors: Jawad Alzeer, Jacques Chollet, Christian Hubschwerlen, Hugues Matile, Robert George Ridley
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Patent number: 6075141Abstract: This invention provides Ddz-amino acid pentafluorophenyl esters and Ddz-amino acid 3,4-dihydro-3-hydroxy-4-oxo-1,2,3-benzotriazine (ODhbt) esters and their side-chain protected derivatives. Preferred esters and derivatives are crystalline solids. The invention also provides (.alpha.,.alpha.-Dimethyl-3,5-dimethoxybenzyl)-p-methoxycarbonylphenylcarb onate, an improved reagent for the introduction of the Ddz group. Pfp and ODhbt esters of this invention have favorable coupling to racemization ratios and are particularly suited for automated solid-phase peptide synthesis. The invention relates in addition to methods of making the esters of this invention and to methods of using these esters in peptide synthesis.Type: GrantFiled: July 10, 1997Date of Patent: June 13, 2000Assignee: University of Georgia Research Foundation, Inc.Inventor: Robert I. Carey
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Patent number: 6071860Abstract: Compounds of the formula (I) and salts thereof ##STR1## where R.sup.1 to R.sup.5, A, Z, X, X', n and m are as defined in claim 1 are suitable as herbicides and plant growth regulators.Type: GrantFiled: February 6, 1997Date of Patent: June 6, 2000Assignee: Hoechst Schering AgrEvo GmbHInventors: Wolfgang Giencke, Lothar Willms, Klaus Bauer, Hermann Bieringer, Christopher Rosinger
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Patent number: 6069114Abstract: Compounds of the formula (I) and their salts ##STR1## in which R.sup.1 to R.sup.6, Y.sup.1, to Y.sup.2, Y.sup.3, m and n are as defined in claim 1 are suitable as herbicides and plant growth regulators. They can be prepared analogously to known processes using intermediates of the formula (V) (cf. claim 6).Type: GrantFiled: February 25, 1997Date of Patent: May 30, 2000Assignee: Hoechst Schering AgrEvo GmbHInventors: Klaus Lorenz, Klemens Minn, Lothar Willms, Klaus Bauer, Hermann Bieringer, Christopher Rosinger
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Patent number: 6057319Abstract: The invention encompasses the novel compound of formula (I) useful in the treatment of cyclooxygenase-2 mediated diseases. The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of formula (I).Type: GrantFiled: October 2, 1998Date of Patent: May 2, 2000Assignee: Merck Frosst Canada & Co.Inventors: Cameron Black, Serge Leger, Petpiboon Prasit, Zhaoyin Wang, Pierre Hamel, Yongxin Han, Gregory Hughes
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Patent number: 6011034Abstract: Insecticidal dihydrooxadiazine compounds having the formula: ##STR1## wherein X is O or S; R is a substituted or unsubstituted phenyl or heterocyclic group; R.sup.1 is halogen, haloalkyl or haloalkoxy; R.sup.2, R.sup.3 , and R.sup.4 are, independently, hydrogen, alkyl or alkoxy; R.sup.5 is nitro, cyano, alkoxy, alkyl, haloalkoxy, dialkylamino, alkylthio, phenoxy, phenylthio, or alkoxycarbonyl; R.sup.6 is hydrogen, alkyl, alkylthio, alkoxyalkyl, alkoxycarbonyl, acyl, or benzyl, wherein R.sup.3 and R.sup.5 together can form a ring.Type: GrantFiled: February 12, 1998Date of Patent: January 4, 2000Assignees: Uniroyal Chemical Company, Inc., Uniroyal Chemical Co./CIE.Inventors: Anupama Mishra, Mark Achiel Dekeyser, Paul Thomas McDonald
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Patent number: 5994544Abstract: Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors and the method of preparing these compounds are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.Type: GrantFiled: October 8, 1997Date of Patent: November 30, 1999Assignee: Ligand Pharmaceuticals IncorporatedInventors: Todd K. Jones, Christopher M. Tegley, Lin Zhi, James P. Edwards
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Patent number: 5955470Abstract: This invention relates to novel amide derivatives of certain 2,6-methano-2H-quinolizine-type compounds, to the intermediates and processes for their preparation, to their ability to antagonize the effects of serotonin at the 5HT.sub.3 receptors, and to their end-use application in the treatment of chemotherapeutically-induced nausea and vomiting, as anti-anxiety agents, in the symptomatic treatment of pain associated with migraine, as anti-arrhythmic agents, in the treatment of cognitive disorders, in treating hallucinatory endogenous psychoses of the type manifested in patients suffering from schizophrenia, and mania, in the treatment of glaucoma, for stimulating gastric motility, to combat drug abuse, to treat sleep apnea and to treat irritable bowel syndrome.Type: GrantFiled: October 29, 1998Date of Patent: September 21, 1999Assignee: Merrell Pharmaceuticals, Inc.Inventor: Maurice W. Gittos
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Patent number: 5952497Abstract: This invention relates to N.sup..alpha. -Bpoc amino acid pentafluorophenyl (Pfp) esters and 3,4-dihydro-4-oxo-1,2,3-benzotriazin-3-yl (ODhbt) esters and side-chain protected derivatives thereof which are useful in peptide, polypeptide, and protein synthesis. The invention relates to the esters, their preparation and their use in peptide synthesis.Type: GrantFiled: July 10, 1997Date of Patent: September 14, 1999Assignee: University of Georgia Research FoundationInventor: Robert I. Carey
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Patent number: 5925637Abstract: Matrix metalloprotease inhibiting compounds, pharmaceutical compositions thereof and a method of disease treatment using such compounds are presented. The compounds of the invention have the generalized formulas: ##STR1## wherein r is 0-2, T is selected from ##STR2## and R.sup.40 is a mono- or bi-heterocyclic structure. These compounds are useful for inhibiting matrix metalloproteases and, therefore, combating conditions to which MMP's contribute, such as osteoarthritis, rheumatoid arthritis, septic arthritis, periodontal disease, comeal ulceration, proteinuria, aneurysmal aortic disease, dystrophobic epidermolysis, bullosa, conditions leading to inflammatory responses, osteopenias mediated by MMP activity, tempero mandibularjoint disease, demyelating diseases of the nervous system, tumor metastasis or degenerative cartilage loss following traumatic joint injury, and coronary thrombosis from athrosclerotic plaque rupture.Type: GrantFiled: May 15, 1997Date of Patent: July 20, 1999Assignee: Bayer CorporationInventors: Michael C. VanZandt, David R. Brittelli, Brian R. Dixon
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Patent number: 5889012Abstract: Substituted cycloalkylamino and cycloalkoxy heterocycles, processes for preparing them and their use as pesticides The invention relates to (I) ##STR1## in which R.sup.1 to R.sup.5, A, X, E, U, p and n are as defined in claim 1, to processes for their preparation and their use as pesticides, such as insecticides, acaricides and fungicides.Type: GrantFiled: October 16, 1995Date of Patent: March 30, 1999Assignee: Hoechst-Schering AgrEvo GmbHInventors: Martin Markl, Wolfgang Schaper, Werner Knauf, Ulrich Sanft, Manfred Kern, Werner Bonin, Adolf Linkies, Dieter Bernd Reuschling
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Patent number: 5885991Abstract: Disclosed are thiocyanomethyloxy(or thiocyanomethylthio)-1,2,3-benzatriazin-4(3H)-one compounds corresponding to one of the formulae: ##STR1## wherein Z represents oxygen or sulfur; X represents --C1, --F, --I, C.sub.1 -C.sub.7 straight or branched chain alkyl, C.sub.1 -C.sub.7 straight or branched chain alkoxy, --CF.sub.3, --OCF.sub.3, --CN, --COOR wherein R is C.sub.1 -C.sub.7 straight or branched chain alkyl and n is an integer of from 0-4.These compounds have been found to exhibit antimicrobial and marine antifouling activity in industrial and commercial applications and compositions containing these compounds are so employed.Type: GrantFiled: June 26, 1997Date of Patent: March 23, 1999Assignee: The Dow Chemical CompanyInventors: Ravi B. Shankar, R. Garth Pews, Duane R. Romer
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Patent number: 5886008Abstract: Compounds of formula (I), wherein R.sub.1 is (a), (b), (c) or (d); n is 0, 1 or 2; A, B, C and D are each independently nitrogen or carbon; R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are each independently hydrogen, C.sub.1 to C.sub.6 alkyl, aryl, C.sub.1 to C.sub.3 alkyl-aryl, halogen (e.g. fluorine, chlorine, bromine or iodine), cyano, nitro, --(CH.sub.2).sub.m NR.sub.14 R.sub.15, --(CH.sub.2).sub.m OR.sub.9, --SR.sub.9, --SO.sub.2 NR.sub.14 R.sub.15, --(CH.sub.2).sub.m NR.sub.14 SO.sub.2 R.sub.15 --(CH.sub.2).sub.m NR.sub.14 CO.sub.2 R.sub.9, --(CH.sub.2).sub.m NR.sub.14 COR.sub.9, --(CH.sub.2).sub.m NR.sub.14 CONHR.sub.9, --CONR.sub.14 R.sub.15, or --CO.sub.2 R.sub.9 ; R.sub.2 and R.sub.3, R.sub.3 and R.sub.4, or R.sub.4 and R.sub.Type: GrantFiled: April 27, 1995Date of Patent: March 23, 1999Assignee: Pfizer Inc.Inventor: John Eugene Macor