Nitrogen Bonded Directly To The Bicyclo Ring System Patents (Class 549/404)
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Publication number: 20040186167Abstract: The present invention relates to synthetic green tea derived polyphenolic compounds, their modes of syntheses, and their use in inhibiting proteasomal activity and in treating cancers. The present invention is also directed to pharmaceutical compositions useful in methods of inhibiting proteasomes and of treating cancers.Type: ApplicationFiled: January 26, 2004Publication date: September 23, 2004Inventors: Q. Ping Dou, Tak-Hang Chan, David M. Smith
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Patent number: 6790965Abstract: Combinatorial libraries are disclosed which are represented by Formula I: (T′—L)q—Ŝ—C(O)—L′—II′ I wherein: Ŝ is a solid support; T′—L— is an identifier residue; and —L′—II′ is a ligand/linker residue. These libraries contain dihydrobenzopyrans of the formula: which interact (i.e., as agonists or antagonists) with &agr; adrenergic receptors, dopamine receptors, &dgr;-opiate receptors, and K+ channels and are inhibitors of carbonic anhydrase isozymes. They are useful in the treatement of ocular diseases such as glaucoma.Type: GrantFiled: September 8, 1999Date of Patent: September 14, 2004Assignee: Pharmacopeia Drug Discovery, Inc.Inventors: John J. Baldwin, John C. Reader, Lawrence W. Dillard, Ge Li, Wenguang Zeng
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Publication number: 20040152763Abstract: This invention relates to benzopyran derivatives of the formula (1) or the formula (2) wherein R1 and R2 represent independently of each other hydrogen atom or C1-6alkyl group, R3 represents hydroxyl group or C1-6 alkylcarbonyloxy group, R4 represents hydrogen atom or C1-6 alkyl group, R5 represents C1-6 alkyl group substituted with C6-14 aryl group or heteroaryl group, R6 represents C1-6 alkyl group, C1-6 alkoxy group, halogen atom, nitro group, C(O)NH2, C(O)NHR8 or C(O)NR8R9, or pharmaceutically acceptable salts thereof. These compounds are useful as an antiarrhythmic agent.Type: ApplicationFiled: November 28, 2003Publication date: August 5, 2004Inventors: Yoshio Ohara, Kazuhiko Ohrai, Kazufumi Yanagihara, Yukihiro Shigeta, Toru Tsukagoshi, Toru Yamashita
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Patent number: 6756403Abstract: Disclosed are process steps and novel processes for producing chromane compositions enriched in at least one (2R or 2S) enantiomer, preferably chroman-2-yl carboxylic acid compounds and chroman-2-yl carboxylic acid esters which are intermediates for producing platelet aggregation inhibitors and/or are themselves potent platelet aggregation inhibitors. Further disclosed are enzymatic processes for resolving chiral intermediates or final products to provide desired enantiomers.Type: GrantFiled: July 11, 2003Date of Patent: June 29, 2004Assignee: Eli Lilly and CompanyInventors: Barbara Briggs, James Kanter, John J. G. Mullins, Gerd Ruhter, Uko Udodong, Milton Zmijewski, Jr., Daniel Verral, II
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Patent number: 6750346Abstract: The disclosure is directed to so-called laser-compatible NIR marker dyes based on polymethines for use in optical, in particular, fluorescence optical determination and detection methods, for example, in the fields of medicine, pharmaceutics and in the areas of life science, materials science and environmental science. The disclosure further discusses the aim of the invention which was to create NIR marker dyes based on polymethine which have a high degree of photostability and stability in storage as well as a high fluorescent yield and which can be excited to fluorescence in the easiest possible manner by means of laser radiation in the visible or NIR spectral range, particularly with light of an argon, helium/neon, or diode laser. Dyes based on polymethine of general formula (I) are used.Type: GrantFiled: January 22, 2002Date of Patent: June 15, 2004Assignee: Carl Zeiss Jena GmbHInventors: Peter Czerney, Frank Lehmann, Bernd Schweder, Matthias Wenzel
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Publication number: 20040110750Abstract: Compounds of formula (I′) wherein the two OH— substituents in the phenyl moiety are in a position ortho to one another and R1 in a position ortho to one of the hydroxy groups; and X, R1 to R6 are as defined in claims, exhibit COMT enzyme inhibiting activity so that they are useful as COMT inhibitors.Type: ApplicationFiled: March 31, 2003Publication date: June 10, 2004Inventors: Jarmo Pystynen, Martti Ovaska, Jukka Vidgren, Timo Lotta, Marjo Yliperttula-Ikonen
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Publication number: 20040102479Abstract: The present invention relates to a novel benzopyran or thiobenzopyran derivative represented by formula (1): pharmaceutically acceptable salt or stereoisomer thereof, in which X, R1, R2, R3, R4 and A are defined as described in the specification, and to a process for preparation thereof and a pharmaceutical composition having anti-estrogenic activity which contains the compound (1) as an active component.Type: ApplicationFiled: August 12, 2003Publication date: May 27, 2004Applicant: Chugai Seiyaku Kabushiki KaishaInventors: Jae Chon Jo, Hyun Suk Lim, Jong Min Kim, Ju Su Kim, Kazumi Morikawa, Yoshitake Kanbe, Myung Hwa Kim, Masahiro Nishimoto
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Publication number: 20040097580Abstract: The present invention provides (i) novel 6-amino-2,2-dimethyl-3,4,6-trisubstituted benzopyran derivatives; (ii) a process for synthesizing novel benzopyran derivatives with high efficiency by parallel synthesis on a solid-phase as one of combinatorial chemical synthesis technologies; and (iii) a use of the novel benzopyran derivatives for preventing and treating diseases or disorders induced by promotion of lipid peroxidation or accumulations of oxidized products.Type: ApplicationFiled: June 16, 2003Publication date: May 20, 2004Applicant: KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGYInventors: Young-Dae Gong, Jin-Soo Seo, Jong Yeon Hwang, Sung-Eun Yoo
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Publication number: 20040097581Abstract: Disclosed is a method for treating a disorder responsive to the positive modulation of AMPA receptors in animals suffering therefrom, comprising administering to an animal in need thereof a compound of Formula I: 1Type: ApplicationFiled: July 2, 2003Publication date: May 20, 2004Inventors: Christopher S. Konkoy, David B. Fick, Sui Xiong Cai, Nancy C. Lan, John F.W. Keana
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Publication number: 20040068002Abstract: This invention relates to benzopyran derivatives of the formula (I) wherein, R1 and R2 represent each independently a C1-6alkyl group, etc, R3 represents a hydroxyl group, etc, R4 represents a hydrogen atom, etc, R6 represents a hydrogen atom, R7 represents a hydrogen atom, etc, X is absent, or represents C═O, etc, R8 represents a hydrogen atom, a C1-6alkyl group, etc, R9 represents a hydrogen atom or a nitro group, when R9 represents a nitro group, Y represents a C4-8alkylene group, —(CH2)m—CR11R12—(CH2)n— or —(CH2)o—O—(CH2)p—, R5 represents a hydrogen atom, an amino group, a C1-6alkoxy group, a C1-6alkylthio group, a C1-6alkylamino group, a C1-6 alkoxycarbonylamino group, etc, or pharmaceutically acceptable salts thereof. These compounds are useful as an antiarrhythmic agent.Type: ApplicationFiled: July 14, 2003Publication date: April 8, 2004Inventors: Yoshi Ohara, Kazuhiko Ohrai, Kazufumi Yanagihara, Yukihiro Shigeta, Toru Tsukagoshi, Toru Yamashita
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Patent number: 6713651Abstract: Disclosed are multibinding compounds which are &bgr;2-adrenergic receptor agonists and are useful in the treatment and prevention of respiratory diseases such as asthma, and bronchitis. They are also useful in the treatment of nervous system injury and premature labor.Type: GrantFiled: November 1, 2000Date of Patent: March 30, 2004Assignee: Theravance, Inc.Inventors: Edmund J. Moran, Seok-Ki Choi
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Publication number: 20040058931Abstract: Indanes, benzopyrans and analogues thereof are potassium channel inhibitors and blockers of IKur and have the structure 1Type: ApplicationFiled: November 15, 2002Publication date: March 25, 2004Inventors: John Lloyd, Heather J. Finlay, Wayne Vaccaro, Karnail S. Atwal, Michael F. Gross, Kerry L. Spear
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Publication number: 20040053992Abstract: Disclosed are process steps and novel processes for producing chromane compositions enriched in at least one (2R or 2S) enantiomer, preferably chroman-2-yl carboxylic acid compounds and chroman-2-yl carboxylic acid esters which are intermediates for producing platelet aggregation inhibitors and/or are themselves potent platelet aggregation inhibitors. Further disclosed are enzymatic processes for resolving chiral intermediates or final products to provide desired enantiomers.Type: ApplicationFiled: July 11, 2003Publication date: March 18, 2004Inventors: Barbara Briggs, James Kanter, John J.G. Mullins, Gerd Ruhter, Uko Udodong, Milton Zmijewski Jr., Daniel Verral II
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Patent number: 6706757Abstract: The present invention provides a compound of formula I and the use thereof for the therapeutic treatment of disorders relating to or affected by the 5-HT6 receptor.Type: GrantFiled: October 2, 2002Date of Patent: March 16, 2004Assignee: WyethInventors: Lynne Padilla Greenblatt, Michael Gerard Kelly
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Publication number: 20040034017Abstract: This invention describes the new 4-fluoroalkyl-2H-benzopyrans of general formula I, 1Type: ApplicationFiled: January 7, 2003Publication date: February 19, 2004Inventors: Hermann Kuenzer, Rolf Jautelat, Ludwig Zorn, Christa Hegele-Hartung, Uwe Kollenkirchen, Karl-Heinrich Fritzemeier
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Publication number: 20040019227Abstract: The invention provides an aminoflavone having formula (I), wherein each of R1 and R2 is H, COCH2—R7, wherein R7 is amino alkylamino, dialkylamino, or alkyl- or dialkylaminoalkyl, or an &agr;-amino acid residue, provided that at least one of R1 or R2 is other than H, and R3 is H, branched or straight-chain alkyl, hydroxyalkyl, alkanoyloxyalkyl, alkanoyloxy, alkoxy, or alkoxyalkyl, or pharmaceutically acceptable salts thereof. The present invention also provides a pharmaceutical composition comprising an aminoflavone as described above, and a method of inhibiting the growth of a tumor in a host by administering a tumor growth-inhibiting amount of an aminoflavone compound having the formula as described above.Type: ApplicationFiled: June 12, 2003Publication date: January 29, 2004Inventors: Kenneth M. Snader, B. Rao Vishnuvajjala, Tsutomu Akama
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Publication number: 20040014994Abstract: Disclosed are processes for resolving chiral (2S) and (2R) benzopyrans, racemizing benzopyrans, and recycling racemized benzopyrans to increase yield of a desired enantiomer to provide purified or substantially purified bicyclic amino substituted benzopyran derivatives. Such benzopyran derivatives are preferably chromans which can be coupled with benzoyl derivatives via an amide bond to produce potent platelet aggregation inhibitors.Type: ApplicationFiled: July 17, 2003Publication date: January 22, 2004Inventors: Luc Antoine, Pascal Bouquel, Alfio Borghese, Hugo Gorissen, Vien V. Khau, Michael Martinelli, Alain Merschaert, Gerd Ruhter, Carine Rypens
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Publication number: 20040014804Abstract: Disclosed are processes for producing benzopyran compounds, reduced 2-(chroman-2-yl) acetic acid compounds and 2-(6-aminochroman-2-yl)acetic acid esters which are intermediates for producing platelet aggregation inhibitors and/or are themselves potent platelet aggregation inhibitors.Type: ApplicationFiled: July 15, 2003Publication date: January 22, 2004Inventors: Luc Antoine, Pascal Bouquel, Alfio Borghese, Hugo Gorissen, Michael Martinelli, Alain Merschaert, Gerd Ruhter, Carine Rypens, Robert Scarborough, Theo Schotten, Jean-Pierre Van Hoeck
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Patent number: 6680332Abstract: Disclosed is a method for treating a disorder responsive to the positive modulation of AMPA receptors in animals suffering therefrom, comprising administering to an animal in need thereof a compound of Formula I: or a pharmaceutically acceptable salt or prodrug thereof, wherein: Y is NH2, NHR, and NHCOR; Z is O and S; and R1, R2, R3, R4, and X are defined herein. These compounds can be used as cognitive enhancers, for the treatment of neurodegenerative diseases, including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease, Parkinson's disease, AIDS associated dementia and Down's syndrome as well as for the treatment of schizophrenia and myoclonus. Also disclosed are pharmaceutical compositions useful for treating disorders responsive to the positive modulation of AMPA receptors, and novel compounds of Formula I.Type: GrantFiled: May 20, 2002Date of Patent: January 20, 2004Assignee: Euro-Celtique S.A.Inventors: Christopher S. Konkoy, David B. Fick, Sui Xiong Cai, Nancy C. Lan, John F. W. Keana
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Publication number: 20030236410Abstract: A compound of formula (I) or pharmaceutically acceptable salt thereof wherein: 1Type: ApplicationFiled: June 2, 2003Publication date: December 25, 2003Applicant: SmithKline Beecham p.l.c.Inventors: Wai Ngor Chan, John Morris Evans, Geoffrey Stemp, Neil Upton, Robert Nicholas Willette
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Patent number: 6660871Abstract: Substituted 4H-chromene derivatives are a new class of compounds that bind to Bcl-2 protein and induce apoptosis in tumor cells. The present invention is directed to an efficient synthetic method for the preparation of these compounds from salicylaldehyde derivatives and alkyl cyanoacetates under solid phase.Type: GrantFiled: February 1, 2002Date of Patent: December 9, 2003Assignee: Thomas Jefferson UnversityInventor: Ziwei Huang
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Publication number: 20030225154Abstract: Aminotetralin derivatives and pharmacological analogs thereof which contain an N-propynyl group exhibit differential dopaminergenic receptor activity. The subject compounds are useful in affecting dopamine receptor activity, particularly in exhibiting differing activity among the various dopamine receptor subtypes. The compounds are useful in treating CNS disorders in mammals in general, and humans in particular.Type: ApplicationFiled: April 21, 2003Publication date: December 4, 2003Inventor: Aloke K Dutta
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Patent number: 6645997Abstract: A class of benzopyrancarboxylic acid derivatives comprises compounds that are potent agonists of PPAR alpha and/or gamma, and are therefore useful in the treatment, control or prevention of non-insulin dependent diabetes mellitus (NIDDM), hyperglycemia, dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, atherosclerosis, obesity, vascular restenosis, inflammation, and other PPAR alpha and/or gamma mediated diseases, disorders and conditions.Type: GrantFiled: September 24, 2001Date of Patent: November 11, 2003Assignee: Merck & Co., Inc.Inventors: Soumya P. Sahoo, Hiroo Koyama, Daniel J. Miller, Julia K. Boueres, Ranjit C. Desai
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Publication number: 20030186975Abstract: Compounds of formula (I′) wherein the two OH— substituents in the phenyl moiety are in a position ortho to one another and R1 in a position ortho to one of the hydroxy groups; and X, R1 to R6 are as defined in claims, exhibit COMT enzyme inhibiting activity so that they are useful as COMT inhibitors.Type: ApplicationFiled: March 31, 2003Publication date: October 2, 2003Inventors: Jarmo Pystynen, Martti Ovaska, Jukka Vidgren, Timo Lotta, Marjo Yliperttula-Ikonen
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Patent number: 6620947Abstract: Novel processes and intermediates useful in the preparation of 11-oxa prostaglandin analogs are disclosed.Type: GrantFiled: August 26, 2002Date of Patent: September 16, 2003Assignee: Alcon, Inc.Inventors: Pete Delgado, Raymond E. Conrow, William D. Dean, Michael S. Gaines
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Patent number: 6613917Abstract: Compounds of the formula where the symbols are as defined in the specification, have retinoid agonist, antagonist or negative hormone-like biological activity.Type: GrantFiled: March 23, 2000Date of Patent: September 2, 2003Assignee: Allergan, Inc.Inventors: Richard L. Beard, Thong Vu, Diana F. Colon, Vidyasagar Vuligonda, Roshantha A. Chandraratna
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Patent number: 6593497Abstract: The present invention is directed to multibinding compounds which are &bgr;2 adrenergic receptor agonists and are therefore useful in the treatment and prevention of respiratory diseases such asthma, bronchitis, and the like. They are also useful in the treatment of nervous system injury and premature labor.Type: GrantFiled: February 14, 2000Date of Patent: July 15, 2003Assignee: Theravance, Inc.Inventors: Seok-Ki Choi, Edmund J. Moran
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Patent number: 6589983Abstract: This invention relates a benzopyran denvative of formula (I) wherein, R1 and R2 represent each independently a hydrogen atom, a (substituted)C1-6 alkyl group or a (substituted)phenyl group,R3 represents a hydroxyl group or C1-6 alkylcarbonyloxy group, R4 represents a hydrogen atom, or R3 and R4 together form a bond, m represents an integer of 0-4, n represents an integer of 0-4, Y is absent, or represents CR11R12 in which R11 and R12 represent each independently a hydrogen atom or a C1-6 alkyl group, R5 represents an aryl group or a (substituted)heteroaryl group,R6 represents a hydrogen atom or a C1-6 alkyl group,R7 represents a hydrogen atom or a C1-6 alkyl group,X is absent, or represents C=O or SO2, R8 represents a hydrogen atom, a (substituted)C1-6 alkyl group or C3-6 cycloalkyl group, and R9 represents a nitro group, etc., or a pharmaceutically acceptable salt thereof.Type: GrantFiled: March 29, 2002Date of Patent: July 8, 2003Assignee: Nissan Chemical Industries, Ltd.Inventors: Keizo Tanikawa, Kazuhiko Ohrai, Kazufumi Yanagihara, Yukihiro Shigeta, Toru Tsukagoshi, Toru Yamashita
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Patent number: 6586460Abstract: Compounds, known as heteroarotinoids, having varying abilities to inhibit growth of certain cancerous cells, induce normal cell differentiation, and induce apoptosis or death of cancerous cells, of the general formula: in which: Ar and Ar′ denote aryl substituents, and wherein at least one of said aryl substituents comprises an aromatic ring having at least one heteroatom in a fused, partially saturated ring; W denotes O or S; and Q denotes H or i-C3H7.Type: GrantFiled: April 2, 2001Date of Patent: July 1, 2003Assignees: The Board of Regents for Oklahoma State University, The Board of Regents for University of OklahomaInventors: Kenneth Darrell Berlin, Doris M. Benbrook, Eldon C. Nelson
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Patent number: 6573295Abstract: This invention concerns compounds for inhibiting intracellular signal transduction, especially intracellular signal transduction mediated by one or more molecular interactions involving a phosphotyrosine-containing protein. This invention also relates to pharmaceutical compositions containing the compounds and prophylactic and therapeutic methods involving pharmaceutical and veterinary administration of the compounds. The compounds are of the formula as defined herein.Type: GrantFiled: November 21, 2001Date of Patent: June 3, 2003Assignee: Ariad Pharmaceuticals, Inc.Inventors: William C. Shakespeare, Michael G. Yang, Rajeswari Sundaramoorthi, Regine Bohacek, Charles Joseph Eyermann, Tomi K. Sawyer
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Patent number: 6566397Abstract: A method of and compositions for suppressing the growth of tumor cells in a patient are disclosed. In one embodiment, the method comprises treating the patient with an effective amount of an isoprenoid ether-linked compound, wherein the isoprenoid ether-linked compound comprises a first acyclic isoprenoid molecule linked via an ether linkage to a second molecule, wherein the second molecule can suppress tumor formation.Type: GrantFiled: July 16, 2001Date of Patent: May 20, 2003Assignee: Wisconsin Alumni Research FoundationInventors: Charles E. Elson, Manfred Jung, Huanbiao Mo
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Publication number: 20030080323Abstract: Disclosed is a novel methine compound, for examples, which is represented by the following formula (I): 1Type: ApplicationFiled: July 26, 2002Publication date: May 1, 2003Applicant: FUJI PHOTO FILM CO., LTD.Inventors: Hisashi Okada, Terukazu Yanagi
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Publication number: 20030073839Abstract: This invention related to novel sulfonamide substituted chroman derivatives which are useful in the treatment of beta-3 receptor mediated conditions.Type: ApplicationFiled: March 7, 2000Publication date: April 17, 2003Inventors: Gaetan H. Ladouceur, Richard D. Connell, Jeremy Baryza, Anne-Marie Campbell, Timothy G. Lease, James H. Cook
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Publication number: 20030065197Abstract: A first process for producing a benzopyran carboxamide represented by the general formula [1] includes reacting 3-aminopropionitrile.½ sulfate, N≡CCH2CH2NH2.½(H2SO4), with a benzopyran carboxylic halide represented by the general formula [2], in the presence of a base. A second process for producing the benzopyran carboxamide includes the steps of (a) reacting 3-aminopropionitrile.½ sulfate with a base, thereby forming 3-aminopropionitrile; and (b) reacting the 3-aminopropionitrile with the benzopyran carboxylic halide [2], thereby producing the benzopyran carboxamide. A process for stabilizing 3-aminopropionitrile includes turning the 3-aminopropionitrile into a sulfate of the 3-aminopropionitrile.Type: ApplicationFiled: August 8, 2002Publication date: April 3, 2003Applicant: Central Glass Company, LimitedInventors: Takeo Komata, Matsue Kawamura, Nariaki li
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Patent number: 6506507Abstract: A novel methine compound which is represented by the following formula (I): wherein R1, R2, R3, R4 and R5 each represents a hydrogen atom or a substituent; X represents an oxygen atom, a sulfur atom, or N—R6; Z represents —NR7R8, or —OG; R6, R7 and R8 each represents a hydrogen atom or a substituent; G represents a hydrogen atom, a cation or a substituent; L1, L2 and L3 each represents a substituted or unsubstituted methine group; n represents 1 or 2; and W represents an electron attractive group. Also, a material for organic luminescence element and organic luminescence element using the same are disclosed.Type: GrantFiled: October 12, 2000Date of Patent: January 14, 2003Assignee: Fuji Photo Film Co., Ltd.Inventors: Hisashi Okada, Terukazu Yanagi
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Publication number: 20020156024Abstract: The present invention provides an antiproliferative compound having the structural formula 1Type: ApplicationFiled: April 12, 2002Publication date: October 24, 2002Applicant: Research Development FoundationInventors: Bob G. Sanders, Kimberly Kline, Laurence Hurley, Robb Gardner, Marla Menchaca, Weiping Yu, Puthucode N. Ramanan, Shenquan Liu, Karen Israel
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Patent number: 6455708Abstract: Starting, for example, from 1-fluoro-2-fluoromethyl-3-butyn-2-yl 4-trifluoromethylphenyl; ether, N-(2-cyanoethyl)-5-fluoro-4-fluoromethyl-4-(4-trifluoromethylphenoxy)-2-pentynamide is produced and then cyclized to synthesize 2,2-bis(fluoromethyl)-N-(2-cyanoethyl)-6-trifluoromethyl-2H-1-benzopyran-4-carboxamide. The invention processes for producing 4-substituted benzopyran derivatives involve fewer steps, feature greater safety and allow for easier purification than the prior art processes.Type: GrantFiled: March 21, 2001Date of Patent: September 24, 2002Assignee: Chugai Seiyaku Kabushiki KaishaInventors: Yukio Suzuki, Takenori Ishizawa, Vladimir A. Khlebnikov, Masashi Watanabe
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Publication number: 20020123630Abstract: A compound of formula (I) or pharmaceutically acceptable salt thereof: 1Type: ApplicationFiled: December 17, 2001Publication date: September 5, 2002Applicant: SmithKline Beecham p.l.c.Inventors: Wai Ngor Chan, John Morris Evans, Geoffrey Stemp, Neil Upton, Robert Nicholas Willette
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Publication number: 20020106338Abstract: The invention relates to compounds of the formula I 1Type: ApplicationFiled: November 14, 2001Publication date: August 8, 2002Inventors: Frank Pfluecker, Joachim Buenger, Hans-Juergen Driller, Herwig Buchholz, Ralf Rosskopf
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Patent number: 6399542Abstract: Alkoxyimino-substituted bicyclic derivatives or salts thereof having an excellent effect of controlling diseases and insect pests are disclosed.Type: GrantFiled: June 29, 2001Date of Patent: June 4, 2002Assignee: Agro-Kanesho Co., Ltd.Inventors: Shinya Henmi, Seiji Kakinuma, Satomi Katoh, Yuriko Shiihashi
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Patent number: 6395909Abstract: This invention relates to 6-(hydroxyalkylcarbonyl) benzopyrans and their use as anticonvulsants.Type: GrantFiled: December 19, 2000Date of Patent: May 28, 2002Inventors: David Bell, Peter J. Cox, Mervyn Thompson, Gillian Turner
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Patent number: 6323238Abstract: The present invention relates to novel benzopyranyl guanidine derivatives of the formula 1, process for preparation therof and pharmaceutical use of the benzopyranyl guanidine derivatives. The benzopyranyl guanidine derivatives of the present invention can be used for protecting heart, neuronal cell or brain damage, preserving organs, and also the benzopyranyl guanidine derivatives are pharmacologically useful for inhibiting NO generation, and for suppressing lipid peroxidation, angiogenesis or restenosis. Wherein R1, R2, R3, R4, R5, R6, n and * are each defined in specification.Type: GrantFiled: October 20, 2000Date of Patent: November 27, 2001Assignee: Dongbu Hannong Chemical Co., Ltd.Inventors: Sung-Eun Yoo, Kyu Yang Yi, Sun Kyung Lee, Nak-Jeong Kim, Jee Hee Suh, Young Sook Park, Sun Kyung Hwang, Hwa Sup Shin, Byung Ho Lee, Ho Won Seo, Hong Lim, Sun-Ok Kim, In Sun Cho, Miae Namgoong, Dongsoo Jang
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Patent number: 6291399Abstract: Alkoxyimino-substituted bicyclic derivatives or salts thereof having an excellent effect of controlling diseases and insect pests are disclosed.Type: GrantFiled: January 14, 2000Date of Patent: September 18, 2001Assignee: Agro-Kanesho Co., Ltd.Inventors: Shinya Henmi, Seiji Kakinuma, Satomi Katoh, Yuriko Shiihashi
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Publication number: 20010021780Abstract: A compound of formula (I) or pharmaceutically acceptable salt thereof: 1Type: ApplicationFiled: May 1, 2001Publication date: September 13, 2001Applicant: SmithKline Beecham p.l.c.Inventors: Wai Ngor Chan, John Morris Evans, Geoffrey Stemp, Neil Upton, Robert Nicholas Willette
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Patent number: 6288071Abstract: Pesticidally active cyclohexadienyl derivative compounds of the formula I that are esters, oximes or amides are claimed. These compounds may be used as fungicides, acaricides and insecticides in plant protection.Type: GrantFiled: December 10, 1998Date of Patent: September 11, 2001Assignee: Bayer AktiengesellschaftInventors: Henry Szczepanski, Martin Zeller, Ottmar Franz Hüter
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Patent number: 6239171Abstract: The present invention relates to novel tocotrienols and tocotrienol-like compounds displaying biological activity. The tocotrienols and tocotrienol-like compounds of this invention may be conveniently obtained from biological sources or by chemical synthesis and may be used in pharmaceutical compositions, foodstuffs and dietary supplements. This invention also relates to the use of tocotrienols, tocotrienol-like compounds, and mixtures thereof, as hypocholesterolemic, antithrombotic, antioxidizing, antiathermogenic, antiinflammatory and immunoregulatory agents, or as agents useful to decrease lipoprotein (a) concentration in the blood or to increase feed conversion efficiency.Type: GrantFiled: October 28, 1998Date of Patent: May 29, 2001Assignee: Lipogenics, Inc.Inventors: Ronald H. Lane, Asaf A. Qureshi, Winston A. Salser
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Patent number: 6221900Abstract: The invention provides BTK inhibitors, methods for their identification and use, and pharmaceutical compositions comprising BTK inhibitors.Type: GrantFiled: October 4, 1999Date of Patent: April 24, 2001Assignee: Hughes InstituteInventors: Fatih M. Uckun, Yaguo Zheng, Sutapa Ghosh
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Patent number: 6222072Abstract: A novel process for producing an optically active amine is provided. The optically active amine is adapted for use as an intermediate in synthesizing physiologically active compounds such as pharmaceuticals and agricultural chemicals, as a functional material such as a liquid crystal, and as a starting material in synthesizing fine chemicals. The process comprises the step of reacting an imine with a hydride reagent in the presence of an optically active metal compound and an alcohol compound and/or carboxylic acid compound.Type: GrantFiled: November 6, 1998Date of Patent: April 24, 2001Assignee: Mitsui Chemicals Inc.Inventors: Teruaki Mukaiyama, Kiyoaki Sugi, Takushi Nagata, Toru Yamada
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Patent number: 6204290Abstract: The present invention relates to novel tocotrienols and tocotrienol-like compounds displaying biological activity. The tocotrienols and tocotrienol-like compounds of this invention may be conveniently obtained from biological sources or by chemical synthesis and may be used in pharmaceutical compositions, foodstuffs and dietary supplements. This invention also relates to the use of tocotrienols, tocotrienol-like compounds, and mixtures thereof, as hypocholesterolemic, antithrombotic, antioxidizing, antiatherogenic, antiinflammatory and immunoregulatory agents, or as agents useful to decrease lipoprotein (a) concentration in the blood or to increase feed conversion efficiency.Type: GrantFiled: October 28, 1998Date of Patent: March 20, 2001Assignee: Lipogenics, Inc.Inventors: Ronald H. Lane, Asaf A. Qureshi, Winston A. Salser
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Patent number: 6197978Abstract: A process for the manufacture of the racemic compound of the formula (I), its R-enantiomer (formula R-(I)) and its S-enantiomer (formula S-(I)), and pharmaceutically acceptable salts and/or solvates thereof, as well as new intermediates obtained and used in the process.Type: GrantFiled: May 6, 1998Date of Patent: March 6, 2001Assignee: Astra AktiebolagInventors: Sverker Hanson, Lars Johansson, Daniel D. Sohn