Plural Ring Oxygens In The Additional Hetero Ring Patents (Class 546/283.7)
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Publication number: 20080119488Abstract: Compounds of the invention, such as compounds of formula (I), where n, m, A, R1, R2, R3, R4 and R5 are defined herein, are useful as modulators of the activity of liver X receptors. Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed.Type: ApplicationFiled: July 24, 2005Publication date: May 22, 2008Applicant: EXELIXIS, INC.Inventors: Christopher D. Bayne, Alan T. Johnson, Shao-Po Lu, Raju Mohan, Michael C. Nyman, Edwin J. Schweiger, William C. Stevens, Haixia Wang, Yinong Xie, Lynne Canne Bannen, Diva Sze-Ming Chan, Ping Huang, Vasu Jammalamadaka, Richard G. Khoury, Morrison B. Mac, Jason Jevious Parks, Yong Wang, Wei Xu
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Publication number: 20080113985Abstract: Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.Type: ApplicationFiled: November 8, 2006Publication date: May 15, 2008Inventors: Sara S. Hadida Ruah, Matthew Hamilton, Mark Miller, Peter D.J. Grootenhuis, Brian Bear, Jason McCartney, Jinglan Zhou
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Patent number: 7297797Abstract: The invention relates to novel ?1-pyrrolines of the formula (I) in which R1, R2, R3, R4, A1, A2, R5, R6, R7, R8, R9 and Q are as defined in the disclosure, to a process for preparing these compounds and to their use for controlling pests.Type: GrantFiled: September 8, 2003Date of Patent: November 20, 2007Assignee: Bayer CropScience AGInventors: Johannes Rudolf Jansen, Udo Kraatz, Hubertus Stakemeier, Thomas Seitz, Fritz Maurer, Martin Füsslein, Bernd Alig, Christian Funke, Werner Hallenbach, Jörg Konze, Udo Beckmann, Ulrich Görgens
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Patent number: 7205305Abstract: The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.Type: GrantFiled: July 17, 2003Date of Patent: April 17, 2007Assignee: Vertex Pharmaceuticals IncorporatedInventors: Guy W Bemis, Francesco G Salituro, John P Duffy, John E Cochran, Edmund M Harrington, Mark A Murcko, Keith P Wilson, Michael Su, Vincent P Galullo
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Patent number: 7157454Abstract: The invention relates to compounds of formula: These compounds show affinity for the bradykinin receptors with selectivity towards the B1 receptors; they may be used for the preparation of medicinal products intended for treating or preventing inflammation pathologies and persistent or chronic inflammatory diseases.Type: GrantFiled: March 27, 2002Date of Patent: January 2, 2007Assignee: Sanofi-AventisInventors: Bernard Ferrari, Jean Gougat, Yvette Muneaux, Pierre Perreaut, Lionel Sarran
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Patent number: 7119208Abstract: Compounds for the treatment of sickle-cell disease, and methods for their use are provided. The compounds have a dual mode of action. First, binding of the compounds to hemoglobin increases the oxygen affinity of both normal and sickle hemoglobin. Secondly, binding of these compounds to the N-terminal amino acid of sickle hemoglobin results in destabilization of potential contacts between sickle hemoglobin molecules, preventing polymerization and the formation of fibrous precipitates of the sickle hemoglobin. The compounds are also useful for inducing hypoxia, e.g. to augment cancer treatments.Type: GrantFiled: March 14, 2005Date of Patent: October 10, 2006Assignee: Virginia Commonwealth UniversityInventors: Martin K. Safo, Richmond Danso-Danquah, Gajanan S. Joshi, Donald J. Abraham
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Patent number: 7026476Abstract: Disclosed are novel aromatic compounds which are useful for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are and pharmaceutical compositions containing, intermediate compounds and processes of making such compounds.Type: GrantFiled: April 28, 2003Date of Patent: April 11, 2006Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Pier F. Cirillo, Steffen Breitfelder, Usha R. Patel, John R. Proudfoot, Alan D. Swinamer
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Patent number: 6900231Abstract: Phenyl acetamide compounds are described, including compounds of or a solvate, hydrate or pharmaceutically acceptable salt thereof; wherein R3-R6, R11, B, Y and W are set forth in the specification. The compounds of the invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as thrombin and factor Xa. Compositions for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation are described. Other uses of compounds of the invention are as anticoagulants either embedded in or physically linked to materials used in the manufacture of devices used in blood collection, blood circulation, and blood storage, such as catheters, blood dialysis machines, blood collection syringes and tubes, blood lines and stents. Additionally, the compounds can be detectably labeled and employed for in vivo imaging of thrombi.Type: GrantFiled: October 3, 2002Date of Patent: May 31, 2005Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Wenxi Pan, Tianbao Lu, Thomas P. Markotan, Bruce E. Tomczuk
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Patent number: 6867230Abstract: This invention relates to compounds of the formula and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein R1, R2, R3 and R10 are as defined herein. The compounds of formula 1 are antibacterial and antiprotozoal agents that may be used to treat various bacterial and protozoal infections and disorders related to such infections. The invention also relates to pharmaceutical compositions containing the compounds of formula 1, methods of treating bacterial and protozoal infections by administering the compounds of formula 1.Type: GrantFiled: June 1, 2001Date of Patent: March 15, 2005Assignee: Pfizer, Inc.Inventors: Matthew Merrill Hayward, Michael S. Visser, Robert G. Linde, II, Takushi Kaneko
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Patent number: 6689798Abstract: The present invention provides novel benzofuran derivatives represented by the following formula (I) or salts thereof: wherein Py is a 2-, 3-, or 4-pyridyl group and R is a substituted or unsubstituted phenyl group or a substituted or unsubstituted aromatic heterocyclic group. The present invention also relates to inhibitors of steroid 17&agr;-hydroxylase and/or steroid C17-20 lyase and pharmaceutical compositions containing a benzofuran derivative of the above formula (I), or the salt.Type: GrantFiled: November 18, 2002Date of Patent: February 10, 2004Assignee: Daiichi Pharmaceutical Co., Ltd.Inventors: Shin'ichi Shimada, Shin Nomoto, Masayuki Okue, Ken'ichi Kimura, Junji Nakamura, Yoshikazu Ikeda, Takeko Takada
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Patent number: 6677330Abstract: The present invention provides a novel compound having an excellent acetylcholinesterase inhibitory effect. That is, it provides a 4-substituted piperidine compound fluoride represented by the following formula, a pharmaceutically acceptable salt thereof or hydrates thereof (provided that 1-benzyl-4-[(5,6-dimethoxy-2-fluoro-1-indanon)-2-yl]methylpiperidine, a pharmaceutically acceptable salt thereof and hydrates thereof are excluded). wherein R1 and R2 represent substituents.Type: GrantFiled: August 30, 2001Date of Patent: January 13, 2004Assignee: Eisai Co., Ltd.Inventors: Yoichi Iimura, Takashi Kosasa, Yoshiharu Yamanishi, Hachiro Sugimoto, Yoshio Takeuchi, Tetsuo Shibata, Emiko Suzuki
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Publication number: 20030225091Abstract: Compounds that are dual aP2/k-FABP inhibitors are provided having the formula 1Type: ApplicationFiled: November 15, 2002Publication date: December 4, 2003Inventors: David R. Magnin, Richard B. Sulsky, Jeffrey A. Robl, Thomas J. Caulfield, Rex A. Parker
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Publication number: 20030220366Abstract: The invention relates to nicotinamide derivatives and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The nicotinamide derivatives according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic, respiratory diseases, disorders and conditions, as well as wounds.Type: ApplicationFiled: February 6, 2003Publication date: November 27, 2003Inventors: Simon Bailey, Elisabeth C. L. Gautier, Alan J. Henderson, Thomas V. Magee, Anthony Marfat, John P. Mathias, Dale G. McLeod, Sandra M. Monaghan, Blanda L. C. Stammen
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Patent number: 6649633Abstract: This application is directed to compounds useful as inhibitors at PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic bronchitis and chronic obstructuive pulmonary disease, of the formula: where j is 0 or 1 provided that when j is 0, n must be 2; k is 0 or 1; m is 0, 1, or 2; n is 1 or 2; W1 is —O—; or —S(═O)t—, where t is 0, 1, or 2; Y is —C(R1a); Q1 is phenyl or substituted phenyl; Q2 is biphenyl or substituted biphenyl; and the remaining variables are defined as set forth in the specification. This application is also directed to pharmaceutical compositions comprising those compounds and to methods of treating diseases regulated by the activation and degranulation of eosinophils, in particular asthma, chronic bronchitis and chronic obstructive pulmonary disease.Type: GrantFiled: January 31, 2002Date of Patent: November 18, 2003Assignee: Pfizer IncInventors: Robert J. Chambers, Anthony Marfat, Thomas V. Magee
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Patent number: 6646123Abstract: The present invention relates to a novel taxol derivative having an antitumor activity which is represented by formula (1). [In the formula (I), R1: a phenyl group, R2: an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group or an alkoxyl group, R3: a hydrogen atom, a hydroxyl group, a halogen atom, an alkoxyl group, a group —O—R311 an acyloxy group or a group —O—CO—R31, (in which R31: an alkylamino group, an alkenyl group, an alkynyl group, a cycloalkyl group, an aryl group or a heterocyclic group), R4 and R5: a hydrogen atom, an alkyl group, an alkenyl group, an alkynyl group, an aryl group or a heterocyclic group, Z1: a hydrogen atom, a hydroxyl group, a halogen atom or an alkyl group, Z2: a hydrogen atom, a hydroxyl group, a halogen atom or an alkyl group, Z3: an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, an aryl group or a heterocyclic group].Type: GrantFiled: April 22, 2002Date of Patent: November 11, 2003Assignee: Daiichi Pharmaceutical Co., Ltd.Inventors: Hirofumi Terasawa, Tsunehiko Soga, Takashi Ishiyama
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Publication number: 20030195233Abstract: The invention relates to nicotinamide derivatives and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The nicotinamide derivatives according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions as well as for wounds healing.Type: ApplicationFiled: February 6, 2003Publication date: October 16, 2003Inventor: Thomas V. Magee
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Publication number: 20030191158Abstract: The invention relates to a combination of a nicotinamide derivative and tiotropium or a derivative thereof, compositions containing it and the uses of, such a combination. The combination according to the present invention is useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.Type: ApplicationFiled: February 6, 2003Publication date: October 9, 2003Inventor: Thomas V. Magee
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Patent number: 6608060Abstract: The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.Type: GrantFiled: June 14, 1999Date of Patent: August 19, 2003Assignee: Vertex Pharmaceuticals IncorporatedInventors: Guy W. Bemis, Francesco Gerald Salituro, John Patrick Duffy, John E. Cochran, Edmund Martin Harrington, Mark A. Murko, Keith P. Wilson, Michael Su, Vincent P. Galullo
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Publication number: 20030135046Abstract: Disclosed are novel 2-(5-halopyridyl) and 2-(5-halopyrimidinyl) magnesium halides, processes of making and their use in the efficient synthesis in their respective 5-halo-2-substituted pyridines and pyrimidines.Type: ApplicationFiled: December 6, 2002Publication date: July 17, 2003Applicant: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Jinhua J. Song, Nathan K. Yee
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Patent number: 6545151Abstract: The present invention relates to a novel taxol derivative having an antitumor-activity which is represented by formula (1). [In the formula (I), R1: a phenyl group, R2: an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group or an alkoxyl group, R3: a hydrogen atom, a hydroxyl group, a halogen atom, an alkoxyl group, a group —O—R31, an acyloxy group or a group —O—CO—R31 (in which R31: an alkylamino group, an alkenyl group, an alkynyl group, a cycloalkyl group, an aryl group or a heterocyclic group), R4 and R5: a hydrogen atom, an alkyl group, an alkenyl group, an alkynyl group, an aryl group or a heterocyclic group, Z1: a hydrogen atom, a hydroxyl group, a halogen atom or an alkyl group, Z2: a hydrogen atom, a hydroxyl group, a halogen atom or an alkyl group, Z3: an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, an aryl group or a heterocyclic group].Type: GrantFiled: January 16, 2001Date of Patent: April 8, 2003Assignee: Daiichi Pharmaceutical Co., Ltd.Inventors: Hirofumi Terasawa, Tsunehiko Soga, Takashi Ishiyama
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Patent number: 6511995Abstract: A pyridine derivative represented by formula (1) wherein all the variables have been defined in the specification. The compounds are used for inhibiting collagen production and are useful for preventing or treating fibrosis.Type: GrantFiled: September 25, 2000Date of Patent: January 28, 2003Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Kouji Edamatsu, Takao Nagahama, Satoshi Hayakawa, Yutaka Kojima, Makoto Sakamoto, Koichi Yasumura
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Patent number: 6498172Abstract: This invention relates to prostaglandin agonists, methods of using such prostaglandin agonists, pharmaceutical compositions containing such prostaglandin agonists and kits containing such prostaglandin agonists. The prostaglandin agonists are useful for the treatment of bone disorders including osteoporosis.Type: GrantFiled: August 20, 1999Date of Patent: December 24, 2002Assignee: Pfizer Inc.Inventors: Kimberly O. Cameron, Bruce A. Lefker, Robert L. Rosati
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Publication number: 20020161000Abstract: Selective MMP-13 inhibitors are pyridine derivatives of the formula 1Type: ApplicationFiled: February 8, 2002Publication date: October 31, 2002Inventors: Nicole Chantel Barvian, David Thomas Connor, Patrick Michael O'Brien, Daniel Fred Ortwine, William Chester Patt, Kevon Ray Shuler, Michael William Wilson
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Publication number: 20020156281Abstract: The present invention provides compounds having the Formula I 1Type: ApplicationFiled: December 12, 2001Publication date: October 24, 2002Inventors: Richard John Booth, Helen Tsenwhei Lee, Jason Keith Pontrello, Randy Ranjee Ramharack, Bruce David Roth
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Publication number: 20020133009Abstract: The present invention relates to a method for opening potassium channels in mammalian cells by administering to a mammal effective amounts of potassium channel-opening keto compounds as described herein.Type: ApplicationFiled: March 4, 2002Publication date: September 19, 2002Inventors: George N. Lambrou, Anna Ottlecz, Christine Percicot, Michael Wiederholt
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Patent number: 6441173Abstract: This invention relates to an improved process for preparing (+) (1S,2R,3S)-3-[2-(2-hydroxyeth-1-yloxy)-4-methoxyphenyl]-1-(3,4-methylenedioxyphenyl)-5-(prop-1-yloxy)indane-2-carboxylic acid and pharmaceutically acceptable salts thereof, preferably the ethylene diamine 2:1 salt. This invention relates to novel intermediates useful in preparing (+) (1S,2R,3S)-3-[2-(2-hydroxyeth-1-yloxy)-4-methoxyphenyl]-1-(3,4-methylenedioxyphenyl)-5-(prop-1-yloxy)indane-2-carboxylic acid. This invention relates to an improved process for preparing (+) (1S,2R,3S)-3-(2-carboxymethoxy-4-methoxyphenyl)-1-(3,4-methylenedioxyphenyl)-5-(prop-1-yloxy)indane-2-carboxylic acid and pharmaceutically acceptable salts thereof, preferably the disodium salt. This invention relates to novel intermediates useful in preparing (+) (1S,2R,3S)-3-(2-carboxymethoxy-4-methoxyphenyl)-1-(3,4-methylenedioxyphenyl)-5-(prop-1-yloxy)indane-2-carboxylic acid.Type: GrantFiled: July 27, 2000Date of Patent: August 27, 2002Assignee: SmithKline Beecham CorporationInventors: Jeffery L. Wood, Michael Anthony McGuire, Robert John Mills, Lendon Norwood Pridgen, Marvin Sungwhan Yu, Qiaogong Su
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Patent number: 6417161Abstract: The present invention is directed to aminoguanidine and alkoxyguanidine compounds, including compounds of Formula I: wherein X is O or NR19 and A1, A2, R7-R10, R18, Ra, Rb, Rc, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin. Also described are methods for preparing the compounds of Formula I. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity. The invention includes a composition for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation in a mammal.Type: GrantFiled: April 22, 1999Date of Patent: July 9, 2002Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Tianbao Lu, Bruce E. Tomczuk, Thomas P. Markotan, Richard M. Soll
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Patent number: 6413979Abstract: The present invention relates to a cyclopentenopyridine derivative represented by general formula (I) or a pharmaceutically acceptable salt thereof, wherein Ar is a phenyl group or the like. R1 is a mono- or di-C1-C6 alkylamino group or the like, and R2 is a hydroxyl group or the like, a process for its production and its use.Type: GrantFiled: July 21, 2000Date of Patent: July 2, 2002Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Takashi Hayama, Norikazu Otake, Masaru Nishikibe
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Patent number: 6376538Abstract: The present invention relates to novel compounds that are useful for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. This invention also relates to pharmaceutical formulations comprising these compounds and methods of using them for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. The compounds and pharmaceutical compositions of this invention can be used as therapeutic or prophylactic agents. They are particularly well-suited for treatment of many inflammatory and autoimmune diseases.Type: GrantFiled: September 19, 1997Date of Patent: April 23, 2002Assignee: Biogen, Inc.Inventors: Steven P. Adams, Ko-Chung Lin, Wen-Cherng Lee, Alfredo C. Castro, Craig N. Zimmerman, Charles E. Hammond, Yu-Sheng Liao, Julio Hernan Cuervo, Juswinder Singh
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Patent number: 6369083Abstract: The present invention provides novel 2-methoxyimino-2-(pyridinyloxymethyl) phenyl acetamide compounds with polyether 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: GrantFiled: September 16, 1999Date of Patent: April 9, 2002Assignee: Dow AgroSciences LLCInventors: Emily J. Canada, Carl P. Denny, Christopher S. Galka, Neil V. Kirby, Marc McKennon, Mary E. Pieczko, Rebecca L. Rezac, Brent J. Rieder, John K. Swayze, Chrislyn M. Carson, David D. Johnson, Gregory M. Kemmitt
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Patent number: 6353110Abstract: This invention relates to a key intermediate in the synthesis of an endothelin antagonist the synthesis of this key intermediate via an asymmetric conjugate addition reaction.Type: GrantFiled: November 24, 1999Date of Patent: March 5, 2002Assignee: Merck & Co., Inc.Inventors: Paul N. Devine, Richard D. Tillyer, Richard M. Heid, Jr., David M. Tschaen
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Publication number: 20020019401Abstract: The present invention relates to compounds of the formula 1Type: ApplicationFiled: September 27, 2001Publication date: February 14, 2002Inventors: Anton Franz Joseph Fliri, Todd William Butler
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Patent number: 6342497Abstract: This invention relates to compounds of the formula and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein R1 and R2 are as defined herein. The compounds of formula 1 are antibacterial and antiprotozoal agents that may be used to treat various bacterial and protozoal infections and disorders related to such infections. The invention also relates to pharmaceutical compositions containing the compounds of formula 1 and to methods of treating bacterial and protozoal infections by administering the compounds of formula 1.Type: GrantFiled: September 7, 1999Date of Patent: January 29, 2002Assignee: Pfizer IncInventor: Robert Gerald Linde, II
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Patent number: 6340704Abstract: The present invention provides a compound represented by the formula: wherein R1 is an amino group which may be substituted; R2 is a hydrogen atom or a lower alkyl group which may be substituted; X is a methyne group which may be substituted or N(O)m (m is 0 or 1); a ring A is a homo- or hetero-cycle which is substituted by a halogen atom, lower alkyl, lower alkoxy or lower alkylenedioxy; and a ring B is a homo- or hetero-cycle which may be substituted; or a salt thereof, which exhibits excellent cell differentiation-inducing action and cell differentiation-inducing factor action-enhancing action, and is useful in the treatment and prevention of various nerve diseases or bone/joint diseases.Type: GrantFiled: July 19, 1999Date of Patent: January 22, 2002Assignee: Takeda Chemical Industries, Ltd.Inventors: Shogo Marui, Masatoshi Hazama, Kohei Notoya, Koki Kato
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Publication number: 20010041796Abstract: The present invention relates to a novel taxol derivative having an antitumor-activity which is represented by formula (1).Type: ApplicationFiled: January 16, 2001Publication date: November 15, 2001Inventors: Hirofumi Terasawa, Tsunehiko Soga, Takashi Ishiyma
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Publication number: 20010008898Abstract: Ether and amide derivatives are disclosed, which are represented by the following formula (I) and its pharmaceutical acceptable salt, and which are useful for the treatment of diabetes.Type: ApplicationFiled: January 10, 2001Publication date: July 19, 2001Inventors: Tsuyoshi Tomiyama, Akira Tomiyama, Hiroshi Tomiyama, Keiko Kuroiwa
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Patent number: 6262084Abstract: A method for the inhibition of the binding of &agr;4&bgr;1 integrin to its receptors, for example VCAM-1 (vascular cell adhesion molecule-1) and fibronectin; compounds that inhibit this binding; pharmaceutically active compositions thereof; and the use of the compounds either as above, or in formulations for the control or prevention of diseases states in which &agr;4&bgr;1 is involved.Type: GrantFiled: October 14, 1999Date of Patent: July 17, 2001Assignee: Texas Biotechnology CorporationInventors: Ronald J. Biediger, Vanessa O. Grabbe, George W. Holland, Jamal Kassir, Karin M. Keller, Timothy P. Kogan, Shuqun Lin, Robert V. Market, Bore G. Raju, Ian L. Scott, Chengde Wu
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Patent number: 6262083Abstract: The present invention relates to novel genipin derivatives which have an excellent liver protection activity with little cytotoxicity, and these compounds are so stable in vivo that they do not induce any side effects.Type: GrantFiled: May 5, 2000Date of Patent: July 17, 2001Assignee: Choongwae Pharma CorporationInventors: Sung-Hwan Moon, Hea-Jin Choi, Su-Jin Lee, Jea-Uk Chung, Jong-Ryul Ha, Kyoung-June Lee, Se-Woong Oh, Kwang-Won Jeong
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Patent number: 6232319Abstract: The invention relates to compounds of general formula (I): in which R, R1, R2, X and Y are as defined in the description, their geometrical and/or optical isomers, and their addition salts with a pharmaceutically-acceptable acid or base, as well as to medicaments containing the same.Type: GrantFiled: June 4, 1999Date of Patent: May 15, 2001Assignee: Adir et CompagnieInventors: Christian Marazano, Delphine Compere, Bhupesh Chandra Das, Jean Lepagnol
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Patent number: 6211363Abstract: The present invention relates to a novel taxol derivative having an antitumor-activity which is represented by formula (1). [In the formula (I), R1: a phenyl group, R2: an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group or an alkoxyl group, R3: a hydrogen atom, a hydroxyl group, a halogen atom, an alkoxyl group, a group —O—R31, an acyloxy group or a group —O—CO—R31, (in which R31: an alkylamino group, an alkenyl group, an alkynyl group, a cycloalkyl group, an aryl group or a heterocyclic group), R4 and R5: a hydrogen atom, an alkyl group, an alkenyl group, an alkynyl group, an aryl group or a heterocyclic group, Z1: a hydrogen atom, a hydroxyl group, a halogen atom or an alkyl group, Z2: a hydrogen atom, a hydroxyl group, a halogen atom or an alkyl group, Z3: an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, an aryl group or a heterocyclic group].Type: GrantFiled: February 25, 2000Date of Patent: April 3, 2001Assignee: Daiichi Pharamaceutical Co., Ltd.Inventors: Hirofumi Terasawa, Tsunehiko Soga, Takashi Ishiyama
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Patent number: 6211202Abstract: The present invention provides novel 2-methoxyimino-2-(pyridinyloxymethyl)phenyl acetamide compounds with substituted ketal 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: GrantFiled: November 13, 1998Date of Patent: April 3, 2001Assignee: Dow AgroSciences LLCInventors: Emily J. Canada, Christopher S. Galka, Dave D. Johnson, Neil Kirby, Irene M. Morrison, Bassam S. Nader, Jim M. Renga
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Patent number: 6194448Abstract: A method for the inhibition of the binding of &agr;4&bgr;1 integrin to its receptors, for example VCAM-1 (vascular cell adhesion molecule-1) and fibronectin; compounds that inhibit this binding; pharmaceutically active compositions comprising such compounds; and the use of such compounds either as above, or in formulations for the control or prevention of diseases states in which &agr;4&bgr;1 is involved.Type: GrantFiled: October 14, 1999Date of Patent: February 27, 2001Assignee: Texas Biotechnology CorporationInventors: Ronald J. Biediger, Vanessa O. Grabbe, George W. Holland, Jamal M. Kassir, Timothy P. Kogan, Shuqun Lin, Robert V. Market, Bore G. Raju, Ian L. Scott, Chengde Wu
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Patent number: 6172235Abstract: This invention relates to a key intermediate in the synthesis of an endothelin antagonist and the synthesis of this key intermediate using an asymmetric conjugate addition reaction.Type: GrantFiled: April 27, 1999Date of Patent: January 9, 2001Assignee: Merck & Co., Inc.Inventors: Ulf H. Dolling, Lisa F. Frey, Richard D. Tillyer, David M. Tschaen