Polycyclo Ring System Having The 1,3-oxazole Ring As One Of The Cyclos Patents (Class 546/271.7)
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Publication number: 20030073697Abstract: Compounds of the formula 1Type: ApplicationFiled: April 25, 2002Publication date: April 17, 2003Applicant: WyethInventors: Megan Tran, Gary P. Stack
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Patent number: 6548667Abstract: The present invention provides a novel sulfonamide derivative of general formula (I) useful as an inhibitor of matrix metalloproteinase (MMP), its isomers, pharmaceutically acceptable salts thereof and a process for preparing the same. Since the sulfonamide derivatives of the present invention selectively inhibit MMP activity in vitro, the MMP inhibitors comprising the sulfonamide derivatives as an effective ingredient can be practically applied for the prevention and treatment of all sorts of diseases caused by overexpression and overactivation of MMP.Type: GrantFiled: December 6, 2001Date of Patent: April 15, 2003Assignee: Samsung Electronics Co. Ltd.Inventors: Young-Jun Park, Hae-Young Bae, Ji-Uk Yoo, Myeong-Yun Chae, Sang-Hyun Paek, Hye-Kyung Min, Hyun-Gyu Park, Choon-Ho Ryu, Kyung-Chul Kim, Jeoung-Wook Lee
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Publication number: 20030050477Abstract: A process for preparing 7-(pyrazol-3-yl)benzoxazoles of the formula I 1Type: ApplicationFiled: September 10, 2002Publication date: March 13, 2003Inventors: Cyrill Zagar, Robert Reinhard, Michael Puhl, Thorsten Volk, Norbert Gotz, Gerhard Hamprecht, Olaf Menke, Ingo Sagasser
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Patent number: 6525075Abstract: Compounds of the formula: useful for the treatment of depression and other diseases such as obsessive compulsive disorder, panic attacks, generalized anxiety disorder, social anxiety disorder, sexual dysfunction, eating disorders, obesity, addictive disorders caused by ethanol or cocaine abuse and related illnesses.Type: GrantFiled: April 25, 2002Date of Patent: February 25, 2003Assignee: WyethInventors: Megan Tran, Gary P. Stack
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Patent number: 6525076Abstract: 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: February 8, 2000Date of Patent: February 25, 2003Assignee: Millennium Pharmaceuticals, Inc.Inventors: Bing-Yan Zhu, Robert M. Scarborough
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Patent number: 6514996Abstract: An oxygen-containing heterocyclic compound represented by following Formula (I): wherein R1 and R2 independently represent hydrogen, lower alkyl, cyano, —(CH2)n—E1—CO—G1 (wherein E1 represents a bond, O, or NH; and G1 represents hydrogen, substituted or unsubstituted lower alkyl, OR6, or NR7R8; and n represents an integer of 0 to 4), or the like; R1 and R2 are combined to represent a saturated carbon ring together with a carbon atom adjacent thereto; or R2, and R11 or R13 described below are combined to form a single bond; R3 represents hydrogen, phenyl, or halogen; R4 represents hydroxy, lower alkoxy, or the like; A represents —C(R9)(R10)— or O; B represents O, NR11, —C(R12)(R13)—, or —C(R14)(R15)—C(R16)(R17)—; D represents (i) —C(R18)(R19)—X— (wherein X represents —C(R21)(R22)—, S, or NR23), (ii) —C(R19a)═Y— [Y represents —C(R24)—Z— (wherein Z represents CType: GrantFiled: November 19, 1997Date of Patent: February 4, 2003Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Etsuo Ohshima, Takashi Kawakita, Koji Yanagawa, Kyoichiro Iida, Rie Koike, Yoshisuke Nakasato, Tohru Matsuzaki, Kenji Ohmori, Soichiro Sato, Hidee Ishii, Haruhiko Manabe, Michio Ichimura, Fumio Suzuki
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Patent number: 6500847Abstract: 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: wherein r is 0-2, T is selected from and R40 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, corneal ulceration, proteinuria, aneurysmal aortic disease, dystrophobic epidermolysis, bullosa, conditions leading to inflammatory responses, osteopenias mediated by MMP activity, tempero mandibular joint 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: April 30, 2001Date of Patent: December 31, 2002Assignee: Bayer CorporationInventors: Michael C. VanZandt, David R. Brittelli, Brian R. Dixon
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Publication number: 20020193365Abstract: Compounds of the formula 1Type: ApplicationFiled: April 25, 2002Publication date: December 19, 2002Applicant: WyethInventors: Gary P. Stack, Megan Tran
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Publication number: 20020188131Abstract: Sulphonylbenzazolones of the formula 1Type: ApplicationFiled: April 1, 2002Publication date: December 12, 2002Inventors: Lutz Assmann, Hans-Ludwig Elbe, Robert Markert, Ralf Tiemann, Klaus Stenzel
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Patent number: 6492397Abstract: A class of N-arylheteroarylalkyl imidazol-2-one compounds is described for use in treatment of arteriosclerosis.Type: GrantFiled: July 26, 2000Date of Patent: December 10, 2002Assignee: Pharmacia CorporationInventors: David B. Reitz, Robert E. Manning
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Patent number: 6437141Abstract: A cyanine dye having the formula wherein R1-R8 are each independently selected from a group consisting of hydrogen, C1-C6 alkyl group, and C0-C4 alkyl group having a hydrophilic substituent thereon. R11 and R12 are chosen to include a free or protected thiol, amine or hydroxyl substituent capable of reacting with a target molecule through a nucleophilic displacement mechanism. The dye is useful in labeling a variety of target molecules. Processes are described for synthesizing suitable heterocyclic and indole derivatives as precursors for the aforementioned cyanine dyes.Type: GrantFiled: April 2, 2001Date of Patent: August 20, 2002Assignee: NEN Life Science Products, Inc.Inventors: Malcolm Harry Randall, Philip Richard Buzby, Thomas Joseph Erickson, Joseph David Trometer, Joseph John Miller, Jr., David George Ahern, Mark Norman Bobrow
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Patent number: 6437149Abstract: Cationic aminoanthraquinones in which at least one cationic charge is delocalized on a 5-membered unsaturated polynitrogen-containing heterocycle, their use as a direct dye in dyeing compositions for keratinous materials, in particular for human keratinous fibers such as hair, dyeing compositions containing them, and dyeing methods using these compositions.Type: GrantFiled: November 29, 1999Date of Patent: August 20, 2002Assignee: L'Oreal S.A.Inventors: Alain Genet, Alain Lagrange
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Patent number: 6383666Abstract: Disclosed are new organometallic complex molecules having light-emitting and electron-transporting characteristics. Also disclosed is organic EL (electroluminescent) devices using these organometallic complex molecules as electron-transporting materials. The organometallic complex molecules are used to form a light-emitting layer with or without doping of another light-emitting material. The organometallic complex molecules can also be used in an electron-transporting layer of the organic EL device. The organic EL devices incorporating the organometallic complex molecules have high thermal stability.Type: GrantFiled: March 31, 2000Date of Patent: May 7, 2002Assignee: LG Chem, Ltd.Inventors: Kongkyeom Kim, Sehwan Son, Okhee Kim, Seok-Hee Yoon, Hyo-Seok Kim, Jaesoon Bae, Youn-Gu Lee
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Patent number: 6383986Abstract: 2-(Benzaryl)pyridines I and salts thereof where n=zero, 1; R1=H, CN, NO2, NH2, OH, SH, SO2—OH, SO2—Cl, SO2—NH2, halogen, optionally halogenated alkyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylaminosulfonyl, dialkylaminosulfonyl; R2, R3=H, halogen; R4=CN, OH, halogen, alkoxy or optionally substituted benzyloxy; X=—Y—C(ZR5)═N— where the nitrogen is attached to &agr; or &bgr; and Y=—O—, —S—, —N(R6)—; Z=a chemical bond, —O—, —S—, —S(O)—, —SO2—, —N(R7)—; R5, R6, R7=H, optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, phenyl or 3- to 7-membered heterocyclyl; or R5=H, CN, SH, NH2, halogen, —CH2—CH(halogen)-R8, —CH═CH—R8 or —CH═C(halogen)-R8 (R8=COOH, alkoxycarbonyl, alkylthiocarbonyl, CONH2, alkylaminocarbonyl or dialkylaminoType: GrantFiled: January 11, 2000Date of Patent: May 7, 2002Assignee: BASF AktiengesellschaftInventors: Markus Menges, Gerhard Hamprecht, Olaf Menke, Robert Reinhard, Peter Schäfer, Cyrill Zagar, Karl-Otto Westphalen, Martina Otten, Helmut Walter
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Patent number: 6372770Abstract: Novel compounds which are effective PDE IV inhibitors are disclosed. The compounds possess improved PDE IV inhibition as compared to theophylline or rolipram, with improved selectivity with regard to, e.g., PDE III inhibition.Type: GrantFiled: September 11, 1998Date of Patent: April 16, 2002Assignee: Euro-Celtique, S.A.Inventors: Mark Chasin, David Cavalla, Peter Hofer, Lloyd Dolby
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Publication number: 20020016460Abstract: Disclosed are novel compounds of formula (I): 1Type: ApplicationFiled: August 2, 2001Publication date: February 7, 2002Inventors: Roger John Snow, Mario Cardozo, Daniel Goldberg, Abdelhakim Hammach, Tina Morwick, Neil Moss, Usha R. Patel, Anthony S. Prokopowicz, Hidenori Takahashi, Matt Aaron Tschantz, Xiao-Jun Wang
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Publication number: 20010053785Abstract: This invention provides substituted compounds of the general formulae: 1Type: ApplicationFiled: March 2, 2001Publication date: December 20, 2001Inventors: Michael S. Malamas, Richard E. McDevitt, Folake O. Adebayo
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Patent number: 6274600Abstract: Compounds are useful for enhancing synaptic responses mediated by AMPA receptors are disclosed, as are methods for the preparation thereof and methods for their use for treatment of subjects suffering from impaired nervous or intellectual functioning due to deficiencies in the number of excitatory synapses or in the number of AMPA receptors. The invention compounds can also be used for the treatment of non-impaired subjects for enhancing performance in sensory-motor and cognitive tasks which depend on brain networks utilizing AMPA receptors and for improving memory encoding.Type: GrantFiled: April 5, 1999Date of Patent: August 14, 2001Assignee: The Regents of the University of CaliforniaInventors: Gary S. Lynch, Gary A. Rogers
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Patent number: 6265349Abstract: The present invention relates to pyridone derivatives and herbicidal compositions containing the pyridone derivatives as active ingredients.Type: GrantFiled: October 27, 1999Date of Patent: July 24, 2001Assignees: Kumiai Chemical Industry Co., Ltd, Ihara Chemical Industry Co., Ltd.Inventors: Mikio Yamaguchi, Yoshihiro Ito, Atsushi Shibayama, Yoshihiro Yamaji, Ryo Hanai, Sota Uotsu, Hideo Sadohara
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Patent number: 6245774Abstract: Compounds of general formula (1) are described: wherein ═W— is (1) ═C(Y)— where Y is a halogen atom, or an alkyl or —XRa group where X is —O—, —S(O)m— [where m is zero or an integer of value 1 or 2], or —N(Rb)— [where Rb is a hydrogen atom or an optionally substituted alkyl group] and Ra is a hydrogen atom or an optionally substituted alkyl group or, (2) ═N—; L is (1) a —C(R)═C(R1)(R2) or [—CH(R)]nCH(R1)(R2) group; is (2) a —(Xa)nAlk′Ar′, or Alk′XaAr′ group; or is (3) XaR1; Z is a group (A), (B), (C) or (D): wherein Ar is a monocyclic or bicyclic aryl group optionally containing one or more heteroatoms selected from oxygen, sulphur or nitrogen atoms; Z1is a group —NR12C(O)— [where R12 is a hydrogen atom or an optionally substituted alkyl or (Alk)tAr group], —C(O)NR12—, —NR12Type: GrantFiled: June 20, 1995Date of Patent: June 12, 2001Assignee: Celltech Therapeutics LimitedInventors: Graham John Warrellow, Ewan Campbell Boyd, Rikki Peter Alexander
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Patent number: 6224644Abstract: A cyanine dye having the formula wherein R1-R8 are each independently selected from a group consisting of hydrogen, C1-C6 alkyl group, and C0-C4 alkyl group having a hydrophilic substituent thereon. R11 and R12 are chosen to include a free or protected thiol, amine or hydroxyl substituent capable of reacting with a target molecule through a nucleophilic displacement mechanism. The dye is useful in labeling a variety of target molecules. Processes are described for synthesizing suitable heterocyclic and indole derivatives as precursors for the aforementioned cyanine dyes.Type: GrantFiled: November 24, 1999Date of Patent: May 1, 2001Assignee: NEN Life Science Products, Inc.Inventors: Malcolm Harry Randall, Philip Richard Buzby, Thomas Joseph Erickson, Joseph David Trometer, Joseph John Miller, Jr., David George Ahern, Mark Norman Bobrow
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Patent number: 6207671Abstract: The cycloalkano-pyridines are prepared by reacting corresponding cycloalkano-pyridine-aldehydes with suitable organometallic compounds or Wittig or Grignard reagents or reacting compounds of the cycloalkano-pyridine alcohols type with suitable bromine compounds, and optionally varying the functional groups accordingly. The cycloalkanopyridines are suitable as active compounds in medicaments, in particular in medicaments for the treatment of hypertipoproteinaemia and arteriosclerosis.Type: GrantFiled: March 8, 2000Date of Patent: March 27, 2001Assignee: Bayer AktiengesellschaftInventors: Gunter Schmidt, Arndt Brandes, Rolf Angerbauer, Michael Lögers, Matthias Müller-Gliemann, Carsten Schmeck, Klaus-Dieter Bremm, Hilmar Bischoff, Delf Schmidt, Joachim Schuhmacher, Henry Giera, Holger Paulsen, Paul Naab, Michael Conrad, Jürgen Stoltefuss
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Patent number: 6204389Abstract: A cyanine dye having the formula wherein R1--R8 are each independently selected from a group consisting of hydrogen, C1-C6 alkyl group, and C0-C4 alkyl group having a hydrophilic substituent thereon. R11 and R12 are chosen to include a free or protected thiol, amine or hydroxyl substituent capable of reacting with a target molecule through a nucleophilic displacement mechanism. The dye is useful in labeling a variety of target molecules. Processes are described for synthesizing suitable heterocyclic and indole derivatives as precursors for the aforementioned cyanine dyes.Type: GrantFiled: November 24, 1999Date of Patent: March 20, 2001Assignee: NEN Life Science Products, Inc.Inventors: Malcolm Harry Randall, Philip Richard Buzby, Thomas Joseph Erickson, Joseph David Trometer, Joseph John Miller, Jr., David George Ahern, Mark Norman Bobrow
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Patent number: 6201126Abstract: Compounds of the formula (I) in which A represents N or a cyanomethylene radical, B represents S, O or NH and R1, R2, R3 and x have the meaning given in the description, are highly suitable for dyeing and printing high-molecular-weight materials, in particular automotive cover fabrics.Type: GrantFiled: June 2, 1997Date of Patent: March 13, 2001Assignee: Bayer AktiengesellschaftInventor: Manfred Lorenz
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Patent number: 6197956Abstract: A cyanine dye having the formula wherein R1-R8 are each independently selected from a group consisting of hydrogen, C1-C6 alkyl group, and C0-C4 alkyl group having a hydrophilic substituent thereon. R11 and R12 are chosen to include a free or protected thiol, amine or hydroxyl substituent capable of reacting with a target molecule through a nucleophilic displacement mechanism. The dye is useful in labeling a variety of target molecules. Processes are described for synthesizing suitable heterocyclic and indole derivatives as precursors for the aforementioned cyanine dyes.Type: GrantFiled: November 24, 1999Date of Patent: March 6, 2001Assignee: NEN Life Science Products, Inc.Inventors: Malcolm Harry Randall, Philip Richard Buzby, Thomas Joseph Erickson, Joseph David Trometer, Joseph John Miller, Jr., David George Ahern, Mark Norman Bobrow