Patents Examined by Andrea M. D'Souza
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Patent number: 6387906Abstract: The present invention concerns novel compounds of formula a N-oxide form, a pharmaceutically acceptable acid addition salt or a stereochemically isomeric form thereof, wherein n is zero, 1, 2 or 3; X is N or CH; each R1 independently is halo, nitro, cyano, amino, hydroxy, C1-4alkyl, C1-4alkyloxy or trifluoromethyl; R2 is hydrogen; C3-7alkenyl; C3-7alkynyl, aryl; C3-7cycloalkyl; optionally substituted C1-6alkyl R3 and R4 each independently are hydrogen, C1-6alkyl, C3-7cycloalkyl or aryl; or R3 and R4 taken together form a bivalent radical —R3—R4— of formula: wherein R5a, R5b, R5c, R5d each independently are hydrogen, C1-6alkyl or aryl; and aryl is optionally substituted phenyl; as antifungals; their preparation, compositions containing them and their use as a medicine.Type: GrantFiled: January 7, 2000Date of Patent: May 14, 2002Inventors: Lieven Meerpoel, Jan Heeres, Frank Christopher Odds, Hugo Florent Adolf Vanden Bossche, Louis Jozef Elisabeth Van der Veken
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Patent number: 6380213Abstract: This invention relates to novel phenyl oxazoles, thiazoles, oxazolines, oxadiazoles and benzoxazoles useful as neuro-protective agents.Type: GrantFiled: November 17, 2000Date of Patent: April 30, 2002Assignee: Eli Lilly and CompanyInventors: Jill Ann Panetta, John Kevin Shadle, Lawrence Joseph Heinz, Michael LeRoy Phillips, John Robert Rizzo, Benjamin Alan Anderson, John Allan Rieck, III, David Lee Varie
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Patent number: 6365757Abstract: This invention relates to a process for the production of a compound (+) catechin penta acetate of formula I from Taxus wallichiana tissue cultures which comprises : (a) inoculation of explants on different media compositions supplemented with combinations of auxins (1-5 mg/l) and cytokinins (0.1-1.0 mg/l); (b) incubation of the cultures under continuous light or dark conditions for 4-6 weeks for callus cultures followed by subculturing at 4-6 weeks intervals; (c) harvesting of the calli at different growth phases ranging from 12-36 months; (d) extraction of fresh pulverized calli with polar solvents at room temperature; (e) evaporating the solvent to give a residue; and partitioning of the residue between water and chlorinated solvents and evaporating the solvent to a semisolid mass; (f) subjecting the resultant mass to column chromatography over suitable adsorbent and (g) eluting with organic solvent/mixtures of organic solvents to get (+) catechin penta acetate.Type: GrantFiled: March 28, 2000Date of Patent: April 2, 2002Assignee: Council of Scientific and Industrial ResearchInventors: Sunil Kumar Chattopadhyay, Suchitra Banerjee, Shipra Agarwal, Koneni Venkata Sashidhara, Vinayak Tripathi, Arun Kumar Kukreja, Sushil Kumar, Manish Kulshrestha, Ram Prakash Sharma, Vijay Kumar Mehta
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Patent number: 6353116Abstract: Novel pyrroles, pyrazoles and triazoles, pharmaceutical compositions containing these compounds and their use as endothelin receptor antagonists are described.Type: GrantFiled: December 14, 1999Date of Patent: March 5, 2002Assignee: SmithKline Beecham CorporationInventors: Juan Ignacio Luengo, John Duncan Elliott
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Patent number: 6348604Abstract: Described are novel photochromic 2H-naphtho[1,2-b]pyran compounds essentially characterized by having two adjacent moderate to strong electron donor substituents at the 8 and 9 positions or a fused heterocyclic group formed by the substituents coming together, weak to moderate electron donors at the 2 position and a rating of at least 80 in the Relative &Dgr;OD at Saturation Test. The compounds also have certain substituents at the 5 position and optionally at the 6 position of the naphtho portion of the compound. These compounds may be represented by the following graphic formula: Also described are polymeric organic host materials that contain or that are coated with such compounds. Optically clear articles such as ophthalmic lenses or adjacent plastic transparencies that incorporate the novel naphthopyran compounds or combinations thereof with complementary photochromic compounds, e.g.Type: GrantFiled: September 6, 2000Date of Patent: February 19, 2002Assignee: PPG Industries Ohio, Inc.Inventors: Clara M. Nelson, Anu Chopra, David B. Knowles, Barry Van Gemert, Anil Kumar
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Patent number: 6344569Abstract: The present invention provides a process which can produce an important intermediate for the production of the HMG coenzyme A reductase inhibitor atrovastatin, 6-cyanomethyl-1,3-dioxane-4-acetic acid derivatives, with ease industrially and in good yields, wherein a 3,5-dihydroxy-6-halohexanoic acid derivative is used as the starting material, and which comprises cyanation by reaction with a cyanating agent for substitution of a cyano group for the halogen atom and an acetal formation reaction of the diol moiety with an acetal forming reagent in the presence of an acid catalyst.Type: GrantFiled: January 2, 2001Date of Patent: February 5, 2002Assignee: Kaneka CorporationInventors: Masaru Mitsuda, Makoto Miyazaki, Kenji Inoue
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Patent number: 6342516Abstract: Phenylazole compounds represented by general formula (1) or pharmaceutically acceptable salts thereof and drugs for hyperlipemia which contain these compounds as the active ingredient, wherein A represents imidazolyl, pyrazolyl, etc.; B represents (1a) or (1b) (wherein R2 and R3 represent each hydrogen, C1-6 alkyl, etc; and k is 0 or an integer of 1 to 15); Y represents O, S, a bond, etc.; and Z represents an optionally substituted and saturated or unsaturated heterocycle containing 1 to 4 N, O or S atoms. Among all, compounds wherein Z is substituted chroman-2-yl, 2,3-dihydrobenzofuran-2-yl, etc. have an effect of inhibiting the formation of lipid peroxides too.Type: GrantFiled: January 26, 2001Date of Patent: January 29, 2002Assignee: Nippon Soda Co., Ltd.Inventors: Nobuhiro Umeda, Nobuo Mochizuki, Seiichi Uchida, Tadayuki Nishibe, Hirokazu Yamada, Kunihito Ito, Hiromi Horikoshi
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Patent number: 6340701Abstract: A cytotoxic agent comprising one or more taxanes linked to a cell binding agent. A therapeutic composition for killing selected cell populations comprising: (A) a cytotoxic amount of one or more taxanes covalently bonded to a cell binding agent through a linking group, and (B) a pharmaceutically acceptable carrier, diluent or excipient. A method for killing selected cell populations comprising contacting target cells or tissue containing target cells with an effective amount of a cytotoxic agent comprising one or more taxanes linked to a cell binding agent. Novel sulfur-containing taxanes.Type: GrantFiled: November 22, 2000Date of Patent: January 22, 2002Assignee: Immunogen INCInventors: Ravi V. J. Chari, Walter A. Blättler
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Patent number: 6339153Abstract: A method making sulfhydryl scavenging agents with reduced water content comprising treating the sulfhydryl scavenging agent to remove water. The sulfyhydryl scavenging agent preferably comprises an —N—C—N— moiety produced by condensation of an alkanolamine with an aldehyde. Preferred sulfhydryl scavenging agents are bisoxazolidines.Type: GrantFiled: August 4, 2000Date of Patent: January 15, 2002Assignee: Baker Hughes IncorporatedInventors: Gordon T. Rivers, James Hackerott
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Patent number: 6339163Abstract: Compositions that comprise at least one compound that corresponds to general formula (I): in which n is a number from 0 to 20; R1, R2, R3 and R4 each represent a hydrogen atom or a hydrocarbon radical, for example alkyl, with 1 to 30 carbon atoms, whereby at least one of R1, R2, R3, and R4 is a hydrocarbon radical; and m is a number from 1 to 30, can be prepared by a process that comprises the reaction of a hydroxymethylated derivative of tetrahydrofuran with ethylene oxide, then with one or more other epoxidized compounds. These compositions can be used as detergent additives for gasoline-type fuels.Type: GrantFiled: August 11, 2000Date of Patent: January 15, 2002Assignee: Institut Francais du PetroleInventors: Bruno Delfort, Stéphane Joly, Thierry Lacôme, Patrick Gateau, Fabrice Paille
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Patent number: 6326363Abstract: The object of the invention are novel halogen substituted methylenebisphosphonic acid anhydrides, ester anhydrides, amide anhydrides, and ester amide anhydrides, processes for the preparation of these novel compounds, as well as pharmaceutical preparations comprising these novel compounds.Type: GrantFiled: July 12, 2000Date of Patent: December 4, 2001Assignee: Leiras OyInventors: Esko Pohjala, Heikki Nupponen, Leena Laurén, Ritva Hannuniemi, Jouko Vepsäläinen, Jouni Kähkönen, Tomi Järvinen, Marko Ahlmark
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Patent number: 6323230Abstract: Derivatives of general chemical formula L(I) and (IV) are used in the topical treatment of diseases of the epithelial tissues, like psoriasis (epidermis) and ulcerative colitis L(lower intestine). These compounds display a high efficacy when administered for example by epicuaneous route in the case of dermatological illnesses like psoriasis, atopic dermatitis and other similar affections, or when administered by oral or rectal route in the case of diseases of the epithelia of the lower intestine like the ulcerative colitis and Crohn's disease.Type: GrantFiled: April 24, 2000Date of Patent: November 27, 2001Assignee: Geange Ltd.Inventor: Carla Rossi
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Patent number: 6323228Abstract: 3-Substituted indole carbohydrazides having the formula are useful for inhibiting angiogenesis. Also disclosed are angiogenesis-inhibiting compositions and methods of inhibiting angiogenesis in a mammal.Type: GrantFiled: September 15, 2000Date of Patent: November 27, 2001Assignee: Abbott LaboratoriesInventors: Nwe Y. BaMaung, Richard A. Craig, Megumi Kawai, Jieyi Wang
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Patent number: 6323345Abstract: This invention provides an improved process for cis-1-{2-[4-(6-methoxy-2-phenyl-1,2,3,4-tetrahydronaphthalen-1-yl)phenoxy]ethyl}pyrrolidine which is an intermediate for the preparation of (−)cis-6-phenyl-5-[4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-5,6,7,8-tetrahydronaphthalene-2-ol which is useful for the treatment of osteoporosis.Type: GrantFiled: February 27, 2001Date of Patent: November 27, 2001Assignee: Pfizer Inc.Inventor: Charles K. F. Chiu
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Patent number: 6320059Abstract: There is provided a process for the preparation of 2-aryl-5-(perfluoroalkyl)pyrrole compounds from N-[1-chloro-1-(perfluoroalkyl)methyl]arylimidoyl chloride compounds. The 2-aryl-5-(perfluoroalkyl)pyrrole compounds are useful for the control of insect and acrid pests, and may also be used to prepare other pesticidal arylpyrrole compounds. In addition, the present invention provides compounds which are useful as intermediates in the preparation of arylpyrrole compounds.Type: GrantFiled: March 7, 2000Date of Patent: November 20, 2001Assignee: American Cyanamid CompanyInventor: Venkataraman Kameswaran
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Patent number: 6320060Abstract: Benzothiophenecarboxylic acid derivatives of the formula (I) which are useful as starting materials for producing drugs, and a process for preparing 5-hydroxybenzo[b]-thiophene-3-carboxylic acid derivatives of the formula (VI) which are specific PGD2 antagonists.Type: GrantFiled: September 29, 2000Date of Patent: November 20, 2001Assignee: Shionogi & Co., Ltd.Inventors: Tsunetoshi Honma, Yoshiharu Hiramatsu
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Patent number: 6316451Abstract: A compound of formula (1) wherein R1 is hydrogen, hydroxy, a group of formula OR5 wherein R5 is C1-C6 alkyl, C2-C6 alkenyl or C3-C8 cycloalkyl, halogen, amino which may be unsubstituted or mono or disubstituted by C1-C6 alkyl, C2-C6 alkenyl, aralkyl, acyl or trifluoroacetyl; R2 is hydrogen, hydroxy, a group NR6R7 wherein R6 and R7 independently represent hydrogen, an optionally substituted C1-C6 alkyl, C2-C6 alkenyl, C3-C8 cycloalkyl or, taken together with the nitrogen atom, represent an optionally substituted C3-C8 heterocyclic ring; R3 is hydrogen, hydroxy, R4 is a 2-substituted thiazolyl or imidazolyl system and the pharmaceutically acceptable salt thereof, is useful in the treatment of amyloidosis. Processes for the preparation and pharmaceutical compositions are also described.Type: GrantFiled: September 26, 2000Date of Patent: November 13, 2001Assignee: Pharmacia & Upjohn S.p.A.Inventors: Sergio Mantegani, Gabriella Traquandi, Tiziano Bandiera, Jacqueline Lansen, Mario Varasi
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Patent number: 6310215Abstract: Provided are novel pyrazolone compounds which have excellent copolymerizability and undergo no elution in an organic solvent when used for an ophthalmic plastic lens and which have an excellent absorption peak in visible light region and function as a reactive yellow dye.Type: GrantFiled: April 4, 2000Date of Patent: October 30, 2001Assignee: Hoya Healthcare CorporationInventor: Hidetoshi Iwamoto
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Patent number: 6307059Abstract: A process for preparing a compound of formula (1) in which P1 and P2 are protecting groups; comprising a) reaction of a compound of formula (5) wherein P1 is as defined for formula (1); with a Raney-nickel catalyst in a solvent under hydrogen to produce a compound of formula (6) wherein P1 is as defined for formula (1); b) protecting the amino group to produce a compound of formula (7) wherein P1 and P2 are as defined for formula (1); and c) selective reduction of the double bond to produce the compound of formula (1).Type: GrantFiled: August 30, 2000Date of Patent: October 23, 2001Assignee: LG Chemical, LTDInventors: Jay Hyok Chang, Won Sup Kim, Tae Hee Lee, Kwang Yul Moon
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Patent number: 6307092Abstract: The present invention provides a novel compound represented by the general formula I: wherein R is H or COR3; R1 is H, R2, phenyl, or COR3, wherein R2 is C1-C5 lower alkyl and R3 is R2 or phenyl; Z is CH2 or O; Y is OH, OCOR3 or ═O; x is 0 or 1; and X is C1-C5 n-alkyl, C3-C7 cycloalkyl, phenyl, furanyl, thienyl or substituted derivatives thereof, wherein the substituents maybe selected from the group consisting of C1-C5 alkyl, halogen, CF3, CN, NO2, NR42, CO2R4 and OR4 wherein R4 is hydrogen or C1-C5 alkyl and dotted lines represent the presence or absence of a double bond and wavy lines represent a cis or trans bond. These novel compounds are especially useful for treating elevated intraocular pressure (ocular hypertension) and glaucoma.Type: GrantFiled: May 8, 2001Date of Patent: October 23, 2001Assignee: Allergan Sales, Inc.Inventors: Robert M. Burk, Mark Holoboski, Mari F. Posner