Patents Examined by Andrea M. D'Souza
  • Patent number: 6387906
    Abstract: 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: Grant
    Filed: January 7, 2000
    Date of Patent: May 14, 2002
    Inventors: Lieven Meerpoel, Jan Heeres, Frank Christopher Odds, Hugo Florent Adolf Vanden Bossche, Louis Jozef Elisabeth Van der Veken
  • Patent number: 6380213
    Abstract: This invention relates to novel phenyl oxazoles, thiazoles, oxazolines, oxadiazoles and benzoxazoles useful as neuro-protective agents.
    Type: Grant
    Filed: November 17, 2000
    Date of Patent: April 30, 2002
    Assignee: Eli Lilly and Company
    Inventors: 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
  • Patent number: 6365757
    Abstract: 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: Grant
    Filed: March 28, 2000
    Date of Patent: April 2, 2002
    Assignee: Council of Scientific and Industrial Research
    Inventors: 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
  • Patent number: 6353116
    Abstract: Novel pyrroles, pyrazoles and triazoles, pharmaceutical compositions containing these compounds and their use as endothelin receptor antagonists are described.
    Type: Grant
    Filed: December 14, 1999
    Date of Patent: March 5, 2002
    Assignee: SmithKline Beecham Corporation
    Inventors: Juan Ignacio Luengo, John Duncan Elliott
  • Patent number: 6348604
    Abstract: 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: Grant
    Filed: September 6, 2000
    Date of Patent: February 19, 2002
    Assignee: PPG Industries Ohio, Inc.
    Inventors: Clara M. Nelson, Anu Chopra, David B. Knowles, Barry Van Gemert, Anil Kumar
  • Patent number: 6344569
    Abstract: 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: Grant
    Filed: January 2, 2001
    Date of Patent: February 5, 2002
    Assignee: Kaneka Corporation
    Inventors: Masaru Mitsuda, Makoto Miyazaki, Kenji Inoue
  • Patent number: 6342516
    Abstract: 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: Grant
    Filed: January 26, 2001
    Date of Patent: January 29, 2002
    Assignee: Nippon Soda Co., Ltd.
    Inventors: Nobuhiro Umeda, Nobuo Mochizuki, Seiichi Uchida, Tadayuki Nishibe, Hirokazu Yamada, Kunihito Ito, Hiromi Horikoshi
  • Patent number: 6340701
    Abstract: 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: Grant
    Filed: November 22, 2000
    Date of Patent: January 22, 2002
    Assignee: Immunogen INC
    Inventors: Ravi V. J. Chari, Walter A. Blättler
  • Patent number: 6339153
    Abstract: 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: Grant
    Filed: August 4, 2000
    Date of Patent: January 15, 2002
    Assignee: Baker Hughes Incorporated
    Inventors: Gordon T. Rivers, James Hackerott
  • Patent number: 6339163
    Abstract: 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: Grant
    Filed: August 11, 2000
    Date of Patent: January 15, 2002
    Assignee: Institut Francais du Petrole
    Inventors: Bruno Delfort, Stéphane Joly, Thierry Lacôme, Patrick Gateau, Fabrice Paille
  • Patent number: 6326363
    Abstract: 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: Grant
    Filed: July 12, 2000
    Date of Patent: December 4, 2001
    Assignee: Leiras Oy
    Inventors: Esko Pohjala, Heikki Nupponen, Leena Laurén, Ritva Hannuniemi, Jouko Vepsäläinen, Jouni Kähkönen, Tomi Järvinen, Marko Ahlmark
  • Patent number: 6323230
    Abstract: 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: Grant
    Filed: April 24, 2000
    Date of Patent: November 27, 2001
    Assignee: Geange Ltd.
    Inventor: Carla Rossi
  • Patent number: 6323345
    Abstract: 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: Grant
    Filed: February 27, 2001
    Date of Patent: November 27, 2001
    Assignee: Pfizer Inc.
    Inventor: Charles K. F. Chiu
  • Patent number: 6323228
    Abstract: 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: Grant
    Filed: September 15, 2000
    Date of Patent: November 27, 2001
    Assignee: Abbott Laboratories
    Inventors: Nwe Y. BaMaung, Richard A. Craig, Megumi Kawai, Jieyi Wang
  • Patent number: 6320059
    Abstract: 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: Grant
    Filed: March 7, 2000
    Date of Patent: November 20, 2001
    Assignee: American Cyanamid Company
    Inventor: Venkataraman Kameswaran
  • Patent number: 6320060
    Abstract: 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: Grant
    Filed: September 29, 2000
    Date of Patent: November 20, 2001
    Assignee: Shionogi & Co., Ltd.
    Inventors: Tsunetoshi Honma, Yoshiharu Hiramatsu
  • Patent number: 6316451
    Abstract: 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: Grant
    Filed: September 26, 2000
    Date of Patent: November 13, 2001
    Assignee: Pharmacia & Upjohn S.p.A.
    Inventors: Sergio Mantegani, Gabriella Traquandi, Tiziano Bandiera, Jacqueline Lansen, Mario Varasi
  • Patent number: 6310215
    Abstract: 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: Grant
    Filed: April 4, 2000
    Date of Patent: October 30, 2001
    Assignee: Hoya Healthcare Corporation
    Inventor: Hidetoshi Iwamoto
  • Patent number: 6307092
    Abstract: 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: Grant
    Filed: May 8, 2001
    Date of Patent: October 23, 2001
    Assignee: Allergan Sales, Inc.
    Inventors: Robert M. Burk, Mark Holoboski, Mari F. Posner
  • Patent number: 6307059
    Abstract: 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: Grant
    Filed: August 30, 2000
    Date of Patent: October 23, 2001
    Assignee: LG Chemical, LTD
    Inventors: Jay Hyok Chang, Won Sup Kim, Tae Hee Lee, Kwang Yul Moon