Plural Chalcogens Bonded Directly To Ring Carbons Of The Six-membered Hetero Ring Patents (Class 546/296)
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Patent number: 6362193Abstract: Novel pyridyl or pyrimidinyl substituted cycloalkenyl compounds and compositions for use in therapy.Type: GrantFiled: April 7, 2000Date of Patent: March 26, 2002Assignee: SmithKline Beecham CorporationInventors: Jerry L. Adams, Ravi Garigipati
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Publication number: 20020035259Abstract: The present invention provides novel 2-methoxyimino-2-(pyridinyloxymethyl)phenyl acetamide compounds with (derivatised) hydroxyalkyl substituents on the pyridine ring, their use as fungicidal compounds, and their use in fungicidal compositions comprising at least one of the 2-methoxyimino-2-(pyridinyloxymethyl)phenyl acetamide compounds as the active ingredient.Type: ApplicationFiled: August 30, 2001Publication date: March 21, 2002Inventors: Emily J. Canada, Christopher S. Galka, Robert P. Gajewski, Neil V. Kirby, Irene M. Morrison, Mary E. Pieczko, Chrislyn M. Carson, Jeannie R. Phillips, Brent J. Rieder, Zhengyu Huang
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Publication number: 20020035109Abstract: This invention is directed to benzamidine derivatives which are useful as anti-coagulants. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat disease-,states characterized by thrombotic activity.Type: ApplicationFiled: August 7, 2001Publication date: March 21, 2002Applicant: Berlex Laboratories, Inc.Inventors: Brad O. Buckman, David D. Davey, William J. Guilford, Michael M. Morrissey, Howard P. Ng, Gary B. Phillips, Shung C. Wu, Wei Xu
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Publication number: 20020032223Abstract: This invention is directed to benzamidine derivatives which are useful as anti-coagulants. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat disease-states characterized by thrombotic activity.Type: ApplicationFiled: August 8, 2001Publication date: March 14, 2002Applicant: Berlex Laboratories, Inc.Inventors: Brad O. Buckman, David D. Davey, William J. Guilford, Michael M. Morrissey, Howard P. Ng, Gary B. Phillips, Shung C. Wu, Wei Xu
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Publication number: 20020028820Abstract: This invention is directed to benzamidine derivatives which are useful as anti-coagulants. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat disease-states characterized by thrombotic activity.Type: ApplicationFiled: August 7, 2001Publication date: March 7, 2002Applicant: Berlex Laboratories, Inc.Inventors: Brad O. Buckman, David D. Davey, William J. Guilford, Michael M. Morrissey, Howard P. Ng, Gary B. Phillips, Shung C. Wu, Wei Xu
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Patent number: 6350746Abstract: This invention is directed to benzamidine derivatives which are useful as anti-coagulants. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat disease-states characterized by thrombotic activity.Type: GrantFiled: December 8, 1999Date of Patent: February 26, 2002Assignee: Berlex Laboratories, Inc.Inventors: Brad O. Buckman, David D. Davey, William J. Guilford, Michael M. Morrissey, Howard P. Ng, Gary B. Phillips, Shung C. Wu, Wei Xu
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Patent number: 6346541Abstract: The present invention relates to hitherto unknown compounds of formula (I) or their tautomeric forms, the attachment to the pyridine ring being in the 3- or 4-position, in which formula R1 stands for one or more substituents which can be the same or different and are selected from the group consisting of: hydrogen, halogen, trifluoromethyl, carboxy, C1-C4 alkyl, alkoxy or alkoxycarbonyl, nitro, amino or cyano and Q stands for C4-C20 divalent hydrocarbon radical which can be straight, branched, cyclic, saturated or unsaturated and X stands for carbonyl, carbonylamino, aminocarbonyl, oxycarbonyloxy, oxycarbonyl, carbonyloxy, aminocarbonyloxy, aminothiocarbonyloxy, oxycarbonylamino or oxythiocarbonylamino and Y stands for benzylene or phenylene and R2 stands for one or more substituents which can be the same or different and are selected from the group consisting of: hydrogen, C1-C4 alkyl, hydroxyalkyl or alkoxy, hydroxy, halogen, trifluoromethyl, cyano, carboxamido, sulfamoyl, nitro, amino, caType: GrantFiled: November 26, 1999Date of Patent: February 12, 2002Assignee: Leo Pharmaceutical Products Ltd. A/SInventor: Charlotte Schou Hunneche
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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
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Patent number: 6335353Abstract: A novel 3-hydroxypyridin-4-one compound of formula I is provided wherein R is hydrogen or a group that is removed by metabolism in vivo to provide the free hydroxy compound, R1 is an aliphatic hydrocarbon group or an aliphatic hydrocarbon group substituted by a hydroxy group or a carboxylic acid ester, sulpho acid ester or a C1-6 alkoxy, C6-aryloxy or C7-10aralkoxy ether thereof, R3 is selected from hydrogen and C1-6alkyl; and R4 is selected from hydrogen, C1-6alkyl and a group as described for R2; characterised in that R2 is selected from groups —CONH—R5 (i) —CH2NHCO—R5 (ii) —SO2NH—R5 (iii) —CH2NHSO2—R5 (iv) —CR6R6OR7 (v) —CONHCOR5 (viii) wherein R5 is selected from hydrogen and optionally hydroxy, alkoxy, or aralkoxy substituted C1-13 alkyl, aryl and C71-13 aralkyl, R6 is independently selected from hydrogen, C1-13 alkyl, aryl and C7-13 aralkyl,Type: GrantFiled: November 10, 1999Date of Patent: January 1, 2002Assignee: BTG International LimitedInventors: Robert Charles Hider, Gary Stuart Tilbrook, Zudong Liu
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Patent number: 6331507Abstract: There is disclosed substituted thiocarboxamides of the general formula (I) useful as herbicides.Type: GrantFiled: December 22, 1999Date of Patent: December 18, 2001Assignee: Bayer AktiengesellschaftInventors: Karl-Heinz Linker, Kurt Findeisen, Roland Andree, Mark-Wilhelm Drewes, Andreas Lender, Otto Schallner, Wilhelm Haas, Hans-Joachim Santel, Markus Dollinger
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Publication number: 20010051732Abstract: A process for preparing a pyridone derivative (4), which comprises reacting the compound (1) with a hypochlorite or a hypobromite or with lead tetraacetate to give the compound (2), and reacting the compound (2) with the compound (3). Said process is preferably especially from the standpoint of safety.Type: ApplicationFiled: May 14, 2001Publication date: December 13, 2001Applicant: SUMITOMO PHARMACEUTICALS COMPANY, LIMITEDInventors: Masami Muraoka, Koji Morishita, Nagisa Aida, Masashi Tanaka, Masatoshi Yuri, Naohito Ohashi
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Patent number: 6323038Abstract: In view of the situation of the prior art, the present invention specifies the structure of a late-stage product of Mailard reaction in vivo having a close relation with various tissue disorders, and provides a diagnostic reagent for complications associated with diabetes or renal failure, containing the above compound as a main component.Type: GrantFiled: January 14, 2000Date of Patent: November 27, 2001Assignee: Asai Germanium Research Institute Co., Ltd.Inventors: Tomoko Oya, Hiroyuki Kobayashi, Mitsuo Akiba, Norihiro Kakimoto, Yasujiro Morimitsu, Toshihiko Osawa
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Publication number: 20010034450Abstract: Compounds of general formula (1): 1Type: ApplicationFiled: March 5, 2001Publication date: October 25, 2001Inventors: Rikki Peter Alexander, Graham John Warrellow
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Patent number: 6306884Abstract: This invention is directed to benzamidine derivatives which are useful as anti-coagulants. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat disease-states characterized by thrombotic activity.Type: GrantFiled: November 8, 1999Date of Patent: October 23, 2001Assignee: Berlex Laboratories, Inc.Inventors: Brad O. Buckman, David D. Davey, William J. Guilford, Michael M. Morrissey, Howard P. Ng, Gary B. Phillips, Shung C. Wu, Wei Xu
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Patent number: 6307054Abstract: The present invention is directed to a process for preparing 2,4-dihydroxy-pyridine comprising heating a compound of the formula A wherein R is H, alkyl or aralkyl and phosphoric acid where the ratio of phosphoric acid to water is not less than about 27 to 1 weight %. The invention is also directed to a process for preparing 2,4-dihydroxy-3-nitropyridine comprising reacting 2,4-dihydroxypyridine with nitric acid. The processes of the present invention prepare intermediates which are useful in preparing compounds which are useful for treating cardiovascular disease marked by hypertension or myocardial ischemia, ameliorating ischenic injury or myocardial infarct size, or treating hyperlipidemia or hypercholesterolemia.Type: GrantFiled: July 1, 1998Date of Patent: October 23, 2001Assignee: Aventis Pharmaceuticals Products Inc.Inventors: Larry K. Truesdale, James P. Sherbine, Benoit J. Vanasse
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Patent number: 6297197Abstract: 4-Aminopicolinic acids, having halogen, alkoxy, alkylthio, aryloxy, heteroaryloxy or trifluoromethyl substituents in the 3-, 5- and 6-positions, and their amine and acid derivatives are potent herbicides demonstrating a broad spectrum of weed control.Type: GrantFiled: January 12, 2001Date of Patent: October 2, 2001Assignee: Dow AgroSciences LLCInventors: Stephen Craig Fields, Anita Lenora Alexander, Terry William Balko, Leslie Anne Bjelk, Ann Marie Buysse, Renee Joan Keese, Karl Leopold Krumel, William Chi-Leung Lo, Christian Thomas Lowe, John Sanders Richburg, III, James Melvin Ruiz
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Patent number: 6271379Abstract: Intermediates useful for the synthesis of huperzine A represented by the structures below, and methods for their synthesis, wherein: R1 is lower alkyl, benzyl, or substituted benzyl; X is a suitable leaving group; Y is an electron withdrawing group that can subsequently be converted into an amino group; one broken line is present as a carbon—carbon bond and the other broken line is absent, where the broken line forms an unconjugated carbon—carbon double bond, which double bond may be endocyclic whereby n is 3 or the double bond may be exocyclic whereby n is 2.Type: GrantFiled: March 8, 2000Date of Patent: August 7, 2001Assignee: Georgetown UniversityInventors: Werner Tückmantel, Alan P. Kozikowski
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Patent number: 6252082Abstract: The invention concerns compounds of formula (I) in which: R is —NO2 or —NHR3, R3 being hydrogen, —COR4 (R4 selected among (C1-C4) alkyl, aryl and aryl (C1-C4) alkyl, —COOR5 (R5 selected among (C1-C4) alkyl and aryl (C1-C4) alkyl), —CONHR6 or SO2R6 (R6 selected among (C1-C5) alkyl, aryl and aryl(C1-C4) alkyl), —SO2NR7R8 (R7 and R8 independently of each other represent hydrogen or (C1-C4) alkyl or form with the nitrogen atom a morpholine group), aryl (C1-C4) alkyl, R1 is a (C1-C4) alkyl group linear or branched, cyclo (C3-C8) alkyl, aryl optionally substituted, aryl (C1-C4) alkyl optionally substituted, heteroaryl, R2 is a hydrogen atom, a (C1-C4) alkyl or arylmethyl group, X is an oxygen or sulphur atom, a —CH2—, —SO2 or —NR1— group and Y is a hydrogen atom or (C1-C6) alkyl. The invention is applicable to synthesis intermediates.Type: GrantFiled: July 14, 1999Date of Patent: June 26, 2001Assignee: Sanofi-SynthelaboInventors: Gilbert Lassalle, Patrice Bellevergue, Jean-Claude Bourbier, Daniel Galtier, Valérie Martin
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Patent number: 6235761Abstract: Substantially pure 3,5-dichloro-2-nethoxy-4-hydroxy-6-(trichloromethyl)pyridine or 4-demethylpenclomedine (formula I), acid addition salts thereof, pharmaceutical compositions containing the aforesaid compound, and a method of using the compound in the treatment of cancer in a mammal are disclosed.Type: GrantFiled: February 22, 1999Date of Patent: May 22, 2001Inventors: Neil Hartman, Robert F. Struck, Seamus O'Reilly, John M. Strong, Eric K. Rowinsky, Jerry M. Collins
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Patent number: 6235909Abstract: This invention is directed to methods for the preparation of [1S-[1a,2b,3b,4a(S*)]]-4-[7-[[-(3-chloro-2-thienyl)methyl]propyl]amino]-3 H-imidazo[4,5-b]pyridin-3-yl]]-N-ethyl-2,3-dihydroxycyclopentanecarboxamide, methods for the preparation of intermediates thereto, and to said intermediates themselves.Type: GrantFiled: July 28, 2000Date of Patent: May 22, 2001Assignee: Aventis Pharmaceuticals Products Inc.Inventors: Herve Garcia, Patrick Leon, Benoit J. Vanasse
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Patent number: 6228810Abstract: Pyridine derivatives of the formula I and their salts, their preparation, and their use for controlling animal pests and harmful fungi.Type: GrantFiled: March 17, 1999Date of Patent: May 8, 2001Inventors: Franz Röhl, Volker Harries, Eberhard Ammermann, Gisela Lorenz, Siegfried Strathmann, Arne Ptock, Hubert Sauter, Wassilios Grammenos, Thomas Grote, Herbert Bayer, Reinhard Kirstgen, Klaus Oberdorf, Bernd Müller, Ruth Müller
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Patent number: 6221886Abstract: This invention is directed to monocyclic N-heterocyclics which are substituted by acyclic or cyclic thio derivatives which are useful as anti-coagulants. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat disease-states characterized by thrombotic activity.Type: GrantFiled: January 11, 2000Date of Patent: April 24, 2001Assignee: Berlex Laboratories, Inc.Inventors: Monica J. Kochanny, Michael M. Morrissey, Howard P. Ng
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Patent number: 6200996Abstract: Compounds of the formula: are useful in treating disease conditions mediated by TNF-&agr; such as rheumatoid arthritis, osteoarthritis, sepsis, AIDS, ulcerative colitis, multiple sclerosis, Crohn's disease and degenerative cartilage loss.Type: GrantFiled: January 27, 2000Date of Patent: March 13, 2001Assignee: American Cyanamid CompanyInventors: Jeremy I. Levin, James M. Chen, Frances C. Nelson
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Patent number: 6197795Abstract: The present invention relates to the discovery of novel, low molecular weight, non-peptide inhibitors of matrix metalloproteinases (e.g.Type: GrantFiled: June 11, 1999Date of Patent: March 6, 2001Assignee: American Cyanamid CompanyInventors: Jeremy Ian Levin, Frances Christy Nelson
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Patent number: 6197962Abstract: 2-Sulfonylpyridine derivatives can be industrially produced efficiently by reacting a sulfonyl cyanide derivative with an &agr;, &bgr;-unsaturated carbonyl compound and a 2-{[(2-pyridyl)methyl]thio}-1H-benzimidazole skeleton can be formed in one step in a good yield by reacting this type of the 2-sulfonylpyridine derivative with a 2-methylthio-1H-benzimidazole derivative in the presence of an organolithium compound.Type: GrantFiled: January 25, 1999Date of Patent: March 6, 2001Assignee: Kuraray Co., Ltd.Inventors: Ken-ichi Koyakumaru, Takashi Sugioka, Tomoya Kuwayama, Goro Asanuma
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Patent number: 6166014Abstract: This invention is directed to monocyclic N-heterocyclics which are substituted by acyclic or cyclic thio derivatives which are useful as anti-coagulants. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat disease-states characterized by thrombotic activity.Type: GrantFiled: May 19, 1999Date of Patent: December 26, 2000Assignee: Berlex Laboratories, Inc.Inventors: Monica J. Kochanny, Michael M. Morrissey, Howard P. Ng
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Patent number: 6159901Abstract: A 6-phenoxy picolinic acid alkylidene hydrazide derivative, a process for producing the derivative and a herbicide containing the derivative as an effective ingredient. Such a compound is a novel compound and is useful as an effective ingredient of herbicides.Type: GrantFiled: February 23, 2000Date of Patent: December 12, 2000Assignee: Kureha Kagaku Kogyo Kabushiki KaishaInventors: Hisashi Kanno, Kazuo Yoshida, Tsutomu Sato, Koki Sato, Yoichi Kanda
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Patent number: 6156902Abstract: The invention relates to novel bis-o-aminophenols, and bis-o-aminothiophenols of the following structure: ##STR1## where A.sup.1 to A.sup.3 are--independently of one another--H, CH.sub.3, OCH.sub.3, CH.sub.2 CH.sub.3, or OCH.sub.2 CH.sub.3T is O or S, andZ is a carbocyclic or heterocyclic aromatic radical.Type: GrantFiled: September 24, 1998Date of Patent: December 5, 2000Assignee: Infineon Technologies AGInventors: Recai Sezi, Michael Keitmann, Andreas Weber
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Patent number: 6150382Abstract: This invention is directed to monocyclic N-heterocyclics which are substituted by acyclic or cyclic thio derivatives which are useful as anti-coagulants. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat disease-states characterized by thrombotic activity.Type: GrantFiled: May 21, 1999Date of Patent: November 21, 2000Assignee: Berlex Laboratories, Inc.Inventors: Monica J. Kochanny, Michael M. Morrissey, Howard P. Ng
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Patent number: 6130188Abstract: The novel compounds of formula I: ##STR1## wherein R, A, X.sup.1, X.sup.2, X.sup.3, Z and m have the meaning given in claim 1, and the agronomically acceptable salts or N-oxides thereof, and herbicidal compositions containing such compounds as active ingredients.Type: GrantFiled: April 7, 1999Date of Patent: October 10, 2000Assignee: American Cyanamid CompanyInventors: Stefan Scheiblich, Thomas Maier, Helmut Siegfried Baltruschat, Thomas Hoellmueller
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Patent number: 6114363Abstract: Pyridyl phenyl and pyridyl benzyl ethers of the formula I ##STR1## and their salts and N-oxides where the substituent and indices have the following meanings:Q is C(CO.sub.2 CH.sub.3).dbd.CHCl.sub.3, C(CO.sub.2 CH.sub.3).dbd.CHOCH.sub.3, C(CONH.sub.2).dbd.NOCH.sub.3, C(CO.sub.2 CH.sub.3).dbd.NOCH.sub.3, C(CONHCH.sub.3).dbd.NOCH.sub.3 or N(OCH.sub.3)--CO.sub.2 CH.sub.3 ;n is 0 or 1;R.sup.1 is hydrogen or an organic radical linked via a carbon atom;R.sup.2 is hydrogen, cyano, halogen or an organic radical linked via a carbon, oxygen, sulfur or nitrogen atom;R.sup.3 is hydrogen, halogen, C.sub.1 -C.sub.4 -alkyl or C.sub.1 -C.sub.2 -haloalkyl;x is 0, 1 or 2;R.sup.4 is cyano, nitro, halogen or an organic radical linked via a carbon, oxygen, sulfur or nitrogen atom;y is 0, 1, 2 or 3;R.sup.5 is cyano, halogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -haloalkyl or C.sub.1 -C.sub.4 -alkoxy,processes and intermediates for their preparation and their use.Type: GrantFiled: August 4, 1998Date of Patent: September 5, 2000Assignee: BASF AktiengesellschaftInventors: Klaus Oberdorf, Wassilios Grammenos, Hubert Sauter, Thomas Grote, Bernd Muller, Reinhard Kirstgen, Ruth Muller, Herbert Bayer, Arne Ptock, Michael Rack, Albrecht Harreus, Franz Rohl, Gisela Lorenz, Eberhard Ammermann, Siegfried Strathmann, Volker Harries
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Patent number: 6103732Abstract: Carboxylic acid derivatives of the formula I ##STR1## where the radicals have the meanings stated in the description, and the preparation of these agreements [sic] and their use as drugs are described.Type: GrantFiled: October 8, 1998Date of Patent: August 15, 2000Assignee: BASF AktiengesellschaftInventors: Wilhelm Amberg, Andreas Kling, Dagmar Klinge, Hartmut Riechers, Ernst Baumann, Liliane Unger, Manfred Raschack, Stefan Hergenroder, Sabine Schult
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Patent number: 6090817Abstract: (4-oxy-3-(aryl)phenyl)pyridine compounds, in free or acid addition salt form, are useful as pharmaceuticals for treatment and prophylaxis of inflammation, particularly inflammatory or obstructive diseases of the airways, e.g. for asthma therapy. Preferred compounds are novel biphenyl pyridines, biphenyl benzamides and biphenyl phenylcarboxy compounds. The compounds are selective inhibitors of PDE 4 isoenzyme activity and also act to down regulate or inhibit TNF-.alpha. release.Type: GrantFiled: September 1, 1998Date of Patent: July 18, 2000Assignee: Novartis AGInventor: Paul W. Manley
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Patent number: 6054583Abstract: This invention relates to a process for preparing 2-substituted pyridines via metal halogen exchange with sec-butyllithium on optionally substituted 2-bromo or 2-iodopyridines. The resulting lithopyridine intermediate is reacted with an electrophile to provide the desired 2-substituted pyridine. The substitution of sec-butyllithium for n-butyllithium in such a process results in an enhanced yield and purity of the desired 2-substituted pyridine.Type: GrantFiled: May 5, 1999Date of Patent: April 25, 2000Assignee: Rohm and Haas CompanyInventors: Martha Jean Kelly, Damian Gerard Weaver
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Patent number: 6046218Abstract: Described is a pyridine derivative represented by the following formula (1): ##STR1## wherein R.sup.1 and R.sup.2 individually represent H, an alkyl group, a cycloalkyl group, a hydroxyalkyl group, an alkoxyalkyl group which may have a substituent, a carboxyalkyl group, an alkoxycarbonylalkyl group, an aralkyl group which may have a substituent, a phenacyl group or an acyl group, R.sup.3 represents an alkyl group, a phenyl group which may have a substituent, a heteroaryl group or a cyclic amino group, X represents O or combination of OH and H, or a salt thereof; and a medicament, such as cytokine production suppressant, comprising the derivative or salt thereof as an effective ingredient. The invention compound has potential, highly specific and highly safe immunoregulating capacity so that it can suppress the excessive production of a specific cytokine in various diseases related to the immune system.Type: GrantFiled: November 17, 1997Date of Patent: April 4, 2000Assignee: SS Pharmaceutical Co., Ltd.Inventors: Hiroshi Hasegawa, Tadashi Mikami, Koichi Tachibana, Kazuo Yamazaki, Noriyuki Kawamoto, Noriaki Shioiri, Koji Kusano, Susumu Sato, Hideaki Matsuda, Toshio Yokoyama
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Patent number: 6046217Abstract: The invention encompasses the novel compound of Formula I as well as a method of treating cyclooxygenase-2 mediated diseases comprising administration to a patient in need of such treatment of a non-toxic therapeutically effective amount of a compound of Formula I. ##STR1## The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.Type: GrantFiled: September 11, 1998Date of Patent: April 4, 2000Assignee: Merck Frosst Canada & Co.Inventors: Richard Friesen, Rejean Fortin, Daniel Dube, Denis Deschenes
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Patent number: 6046221Abstract: Novel aryl amides are inhibitors of tumor necrosis factor .alpha. and can be used to combat cachexia, endotoxic shock, and retrovirus replication. A typical embodiment is N-benzoyl-3-amino-3-(3',4'-dimethoxyphenyl)propanamide.Type: GrantFiled: August 25, 1998Date of Patent: April 4, 2000Assignee: Celgene CorporationInventors: George W. Muller, Mary Shire, David I. Stirling
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Patent number: 6046219Abstract: The present invention relates to a method of treating conditions mediated by collagen formation together with cell proliferation by administering to a patient or living system an effective amount of a compound of Formulae (I) or (II) and derivatives thereof: ##STR1## R.sub.1, R.sub.2, R.sub.3, and R.sub.4 each individually represent a hydrogen, an alkyl, alkenyl, or alkoxy group containing 1 to about 8 carbon atoms, an aryl, aralkyl, or cycloalkyl group containing about 5 to 12 carbon atoms, or a carboalkoxy or carbamyl group containing up to 8 carbon atoms, or a peptide or peptidomimetic moiety containing 10 to about 30 carbon atoms.Type: GrantFiled: December 16, 1997Date of Patent: April 4, 2000Assignee: Cornell Research Foundation, Inc.Inventors: Hartmut M. Hanauske-Abel, Timothy A. McCaffrey, Robert W. Grady
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Patent number: 6020350Abstract: There are described 3-hydrixypyridine-2-carboxamidoesters of the formula ##STR1## their preparation, their use for the inhibition of collagen biosynthesis and their use as pharmaceuticals for the treatment of fibrotic disorders.Type: GrantFiled: December 4, 1997Date of Patent: February 1, 2000Assignee: Hoechst AktiengesellschaftInventors: Klaus Weidmann, Karl-Heinz Baringhaus, Georg Tschank, Martin Bickel
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Patent number: 6015905Abstract: A process for preparing 2-(6-substituted pyrid-2-yloxymethyl)phenyacetates especially useful as intermediates for producing agricultural fungicides. The invention provides a compound having the formula (I): wherein A and D are independently selected from the group comprising halo, hydroxy, halo(C.sub.1-4)alkyl, C.sub.1-4 alkoxy, thio(C.sub.1-4)alkoxy, halo(C.sub.1-4)alkoxy, phenyl, phenoxy, nitro, amino, aclyamino, cyano, carboxy, C.sub.1-4 alkoxycarbonyl and C.sub.1-4 alkylcarbonyloxy, or D is C.sub.1-4 alkyl, and m is 0 or an integer of from 1 to 3. The process comprises treating a compound of formula (II): ##STR1## wherein A, D and m are defined as above and M is a metal atom, with a compound of formula (III): ##STR2## wherein L is a leaving group.Type: GrantFiled: December 2, 1997Date of Patent: January 18, 2000Assignee: Zeneca LimitedInventors: David John Ritchie, Gordon Richard Munns, Julie Forrester, Michael Charles Henry Standen, Paul Anthony Worthington, Raymond Vincent Heavon Jones
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Patent number: 6008234Abstract: This invention is directed to benzamidine derivatives substituted by cyclic amino acid and cyclic hydroxy acid derivatives which are useful as anti-coagulants. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat disease-states characterized by thrombotic activity.Type: GrantFiled: August 27, 1997Date of Patent: December 28, 1999Assignee: Berlex Laboratories, Inc.Inventors: Monica Kochanny, Michael M. Morrissey, Howard P. Ng
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Patent number: 6008161Abstract: Herbicidal 2-(hetero)aryloxy-6-arylpyridines and 2-Aryl-4-(hetero)aryloxypyrimidinesNew herbicidal pyridine and pyrimidine derivatives of general formula (1), ##STR1## wherein Z represents a nitrogen atom or a C--H group; A represents an optionally substituted aryl group or an optionally substituted 5- or 6-membered nitrogen-containing heteroaromatic group; n represents an integer from 0 to 2 and R.sup.1 or each R.sup.1 independently represents a hydrogen atom or an optionally substituted alkyl, alkoxy, alkylthio or dialkylamino group; m represents an integer from 0 to 5 and R.sup.1 or each R.sup.1 independently represents a hydrogen or a halogen atom or an optionally substituted alkyl, haloalkyl, haloalkoxy, alkoxy, alkylthio group or a nitro, cyano or a halosulphonyl group; and X represents an oxygen or sulphur atom.Type: GrantFiled: July 14, 1998Date of Patent: December 28, 1999Assignee: American Cyanamid CompanyInventors: Axel Kleemann, Helmut Siegfried Baltruschat, Thekla Haselwander, Thomas Maier, Stefan Scheiblich
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Patent number: 5994375Abstract: This invention is directed to benzamidine derivatives substituted by amino acid and hydroxy acid derivatives which are useful as anti-coagulants. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat disease-states characterized by thrombotic activity.Type: GrantFiled: February 12, 1996Date of Patent: November 30, 1999Assignee: Berlex Laboratories, Inc.Inventors: Monica Kochanny, Raju Mohan, Michael M. Morrissey, Howard P. Ng
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Patent number: 5981437Abstract: The novel compounds of formula I: ##STR1## wherein A represents an optionally substituted 5- or 6-membered heteroaromatic group or an optionally substituted aryl group or a difluorobenzodioxolyl group;B represents an optionally substituted cyclic hydrocarbon or thienyl, an alkyl, alkenyl or alkynyl group or independently has one of the meanings of A;n represents an integer from 0 to 2;R represents a hydrogen atom, a halogen atom, an optionally substituted alkyl, alkenyl, alkynyl, alkoxy, alkoxyalkyl, dialkoxyalkyl, alkoxyalkoxy, alkylthio, amino, alkylamino, dialkylamino or alkoxyamino group or a formamidino or cyano group;X.sub.1 and X.sub.2 independently represent an oxygen or sulphur atom, and the herbicidal use of these compounds.Type: GrantFiled: July 8, 1997Date of Patent: November 9, 1999Assignee: American Cyanamid CompanyInventors: Thomas Maier, Stefan Scheiblich, Helmut Siegfried Baltruschat, Joseph Luke Pont
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Patent number: 5962479Abstract: Corticotropin-releasing factor (CRF) antagonists having formulae (I), (II) or (III) wherein the dashed lines, A, B, Y, Z, G, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.16 and R.sub.17 are as defined in the description, and processes for preparing them. These compounds and their pharmaceutically acceptable salts are useful in the treatment of CNS and stress-related disorders.Type: GrantFiled: December 6, 1996Date of Patent: October 5, 1999Assignee: Pfizer Inc.Inventor: Yuhpyng Liang Chen
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Patent number: 5962481Abstract: The present invention relates to the discovery of novel, low molecular weight, non-peptide inhibitors of matrix metalloproteinases (e.g. gelatinases, stromelysins and collagenases) and TNF-.alpha. converting enzyme (TACE, tumor necrosis factor-.alpha.Type: GrantFiled: October 6, 1997Date of Patent: October 5, 1999Assignee: American Cyanamid CompanyInventors: Jeremy Ian Levin, Frances Christy Nelson
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Patent number: 5959116Abstract: A pyridine-2,3-dicarboxylic acid diester of the formula Va ##STR1## where the radicals R.sup.2 and R.sup.4 have the meanings set out in the specification and where R.sup.8 is a C.sub.1 -C.sub.4 -alkyl, C.sub.3 -C.sub.5 -alkenyl or C.sub.3 -C.sub.5 -alkynyl radical, which may be substituted by halogen, phenyl or C.sub.1 -C.sub.4 -alkoxy.Type: GrantFiled: July 12, 1996Date of Patent: September 28, 1999Assignee: BASF AktiengesellschaftInventors: Gerhard Hamprecht, Peter Munster, Matthias Gerber, Helmut Walter, Karl-Otto Westphalen
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Patent number: 5952326Abstract: Compounds of the formula ##STR1## wherein R is an optionally substituted heteroaryl group such as 2-chromanyl, 2-pyridyl or 5-fluoro-2-benzothiazoyl;X is O, S or (CH.sub.2).sub.m ;R.sup.1 is phenyl or pyridyl, optionally substituted by one or more (C.sub.1 -C.sub.3)alkyl, (C.sub.1 -C.sub.3)alkoxy, carboxy or ?(C.sub.1 -C.sub.3)alkoxy!carbonyl groups;n is 0, 1 or 2;m is 1 or 2;Y and Y.sup.1 are taken together and are oxygen, or Y and Y.sup.1 are taken separately, Y is hydrogen and Y.sup.1 is hydroxy or an in vivo hydrolyzable acyloxy group;Z is CH.sub.2, NR.sup.2, O or S; andR.sup.2 is hydrogen or (C.sub.1 -C.sub.3)alkyl;are useful in the treatment of asthma, arthritis and related diseases mediated by leukotrienes.Type: GrantFiled: December 10, 1997Date of Patent: September 14, 1999Assignee: Pfizer Inc.Inventors: James F. Eggler, Anthony Marfat, Lawrence S. Melvin, Jr.
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Patent number: 5942623Abstract: The invention relates to a process for the preparation of 2-(pyrid-2-yloxymethyl)phenylacetates of formula (I) useful as intermediates for agricultural pesticides, which comprises reacting a 2-pyridine of formula (II), wherein L is a leaving group and A, D and m are as defined in the description with a compound MO--CH.sub.2 R where M is a metal atom and R is the residue of a metal salt of phenylacetic acid. It also includes the compounds MO--CH.sub.2 R, a process for their preparation and a "one-pot" process for the preparation of 2-(pyrid-2-yloxymethyl) phenylacetates from 3-isochromanone.Type: GrantFiled: February 19, 1998Date of Patent: August 24, 1999Assignee: ZENECA LimitedInventors: Alfred Glyn Williams, Gordon Richard Munns, Paul Anthony Worthington
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Patent number: RE37087Abstract: There are provided new alkane and alkoxyalkane derivatives of the general formula I in which R1, R2, R3, R4 and A have the meanings given in the description, processes for their preparation and insecticidal and acaricidal compositions containing these compounds.Type: GrantFiled: June 20, 1991Date of Patent: March 6, 2001Assignee: Schering AktiengesellschaftInventors: Helga Franke, Heinrich Franke, Hans-Rudolf Kruger, Hartmut Joppien, Dietrich Baumert, David Giles