Abstract: A pyrrolesulfonamide compound having the following formula (I):
wherein the ring P represented by
is a pyrrole ring having the following structure:
wherein A represents alkylene, alkenylene or alkynylene; and Y represents a group
in which W represents CH, C═ or N; m stands for 0 or 1 when W is CH or N, or m stands for 1 when W is C═; B represents a specific divalent group; E1 and E2 each independently represents H or lower alkyl; and D represents an aromatic hydrocarbon group or heterocyclic group; l stands for 0 or 1; the dashed line indicates the presence or absence of a bond; and, when the bond is present, Z2 is not present and Z1 represents H but, when the bond is absent, Z1 represents H and Z2 represents OH or Z1 and Z2 are combined together to represent O or a group NOR5, in which R5 represents H, or alkyl, aralkyl or aryl; and R represents H, alkyl, cycloalkyl, cycloalkyl-alkyl or aralkyl.
Abstract: An E-isomeric fulleropyrrolidine compound of formula (I):
is disclosed. Also disclosed is a method for preparing and polymers prepared from such a compound.
Abstract: A &ohgr;-cycloalkyl-prostaglandin E2 derivatives of the formula (I)
wherein R is carboxy or hydroxymethyl; R1 is oxo, methylene or halogen atom; R2 is H, OH or C1-4 alkoxy; R3 is H, C1-8 alkyl, C2-8 alkenyl, C2-8 alkynyl, C1-8 alkyl, C2-8 alkenyl or C2-8 alkynyl substituted by 1-3 of substituent selected from halogen atom, C1-4 alkoxy, C3-7 cycloalkyl, phenyl, or phenyl substituted by 1-3 of substituent selected from halogen atom, C1-4 alkyl, C1-4 alkoxy, nitro, trifluoromethyl; n is 0-4;
and non-toxic salt thereof, prodrug thereof and cyclodextrin clathrate thereof can strongly bind on EP2 subtype receptor. Therefore, they are useful for prevention and/or treatment of immune disease (autoimmune disease, organ transplantation, etc.), asthma, abnormal bone formation, neuron cell death, liver damage, abortion, premature birth or retina neuropathy of glaucoma etc.
Abstract: The present invention provides a method of treating ocular hypertension or glaucoma which comprises administering to an animal having ocular hypertension or glaucoma therapeutically effective amount of a compound represented by the general formula I;
wherein X, Y, Z, D and R3 are as defined in the specification.
Type:
Grant
Filed:
May 14, 2002
Date of Patent:
June 3, 2003
Assignee:
Allergan, Inc.
Inventors:
David W. Old, Danny Thang Dinh, Robert M. Burk
Abstract: This invention pertains to DTT-based compounds having two-photon absorption property containing electron donors and/or electron acceptors and having cross section value &sgr; that is higher than compound AF-50.
Type:
Grant
Filed:
May 19, 2000
Date of Patent:
May 20, 2003
Assignee:
The United States of America as represented by the Secretary
of the Navy
Inventors:
Oh-Kil Kim, Han Young Woo, Kie-Soo Kim, Kwang-Sup Lee
Abstract: Oxazolidinones and methods for their synthesis are provided. Also provided are combinatorial libraries comprising oxazolidinones, and methods to prepare the libraries. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. The methods of library preparation include the attachment of oxazolidinones to a solid support. The methods of compound preparation in one embodiment involve the reaction of an iminophosphorane with a carbonyl containing polymeric support.
Type:
Grant
Filed:
December 28, 2001
Date of Patent:
May 13, 2003
Assignee:
Pharmacia & Upjohn Company
Inventors:
Mikhail F. Gordeev, Gary W. Luehr, Dinesh V. Patel, Zhi-Jie Ni, Eric Gordon
Abstract: The present invention relates to a novel process for making geminal bisphosphonates. The process provides for bisphosphorylation using phosphorus trihalide, phosphorous acid as a reactant/solvent, and a base as an acid acceptor/solvent.
Type:
Grant
Filed:
January 29, 2001
Date of Patent:
May 13, 2003
Assignee:
The Procter & Gamble Company
Inventors:
Frederick Dana Cazer, William Douglas Cramer, Dennis Michael Billings, Gregory Eugene Parry
Abstract: An amine compound of the formula (I):
wherein R1 represents an optionally substituted carbamoyl group, etc., R2 represents a hydrogen atom, etc., R3 represents a C1-C10 alkyl group etc., W1, W2 and W3 are the same or different and each represent a single bond or a C1-C8 alkylene group, X, Y and Q represent a sulfur atom, etc., Z represents a ═CH— group, etc., Ar represents a benzene ring, etc. and L represents a hydrogen atom, etc., or a pharmacologically acceptable salt thereof. These compounds are useful in the treatment and/or prophylaxis of diseases such as diabetes, hyperlipemia, arteriosclerosis, cancer, etc.
Abstract: The invention relates to a new class of compounds herein identified generally as “sultams”, which may be represented by the following formula V, in FIG. 1, in which numbering of the atoms is started with the sulfur atom of the isothiazole. Two of the rings (rings A and C) are aromatic, and the third is a heterocyclic ring (ring B), a cyclic sulfonamide. Of particular importance are the enantiomerically pure sultams since they are especially potent HIV-1 inhibitors.
Type:
Grant
Filed:
July 15, 1999
Date of Patent:
May 13, 2003
Assignee:
The University of Tennessee Research Corporation
Inventors:
David C. Baker, Anand Mayasundari, Jianmin Mao, Stephen C. Johnson, Shijia Yan
Abstract: Phenyl- and pyridyl-substituted thiazoline acid derivatives useful in diagnosing and treating pathological conditions associated with an excess of trivalent metals in humans and animals.
Type:
Grant
Filed:
March 20, 2000
Date of Patent:
May 6, 2003
Assignee:
University of Florida Research Foundation, Inc.
Abstract: The invention relates to a process for simultaneously N(2)-acylating piperazic acid or an ester thereof and forming a bicyclic ring structure. The invention also relates to the use of that process step in a method of synthesizing a bicyclic compound useful as an intermediate for the production of an inhibitor of a caspase, particularly an inhibitor of interleukin-1&bgr; converting enzyme (“ICE”).
Type:
Grant
Filed:
October 13, 2000
Date of Patent:
May 6, 2003
Assignee:
Vertex Pharmaceuticals Incorporated
Inventors:
Andrea L. C. Robidoux, Jeffrey Douglas Wilson, Petra Dieterich, Neil Storer, Stefania Leonardi
Abstract: An apoptosis inhibitor which comprises a compound of the formula:
wherein R represents a hydrocarbon group that may be substituted or a heterocyclic group that may be substituted; Y represents a group of the formula: —CO—, —CH(OH)— or —NR3— where R3 represents an alkyl group that may be substituted; m is 0 or 1; n is 0, 1 or 2; X represents CH or N; A represents a chemical bond or a bivalent aliphatic hydrocarbon group having 1 to 7 carbon atoms; Q represents oxygen or sulfur; R1 represents hydrogen or an alkyl group; ring E may have further 1 to 4 substituents, which may form a ring in combination with R1; L and M respectively represent hydrogen or may be combined with each other to form a chemical bond; or a salt thereof, or a compound having an insulin sensitivity enhancing activity.
Abstract: The decomposition of di-t-butyl dicarbonate which is a thermally unstable compound is inhibited. To achieve the object, a hydrocarbon compound such as hexane, cyclohexane, 1-hexene or toluene and/or a chain ether compound such as diisopropyl ether or t-butyl methyl ether are/is used as a decomposition inhibitor for di-t-butyl dicarbonate.
Abstract: The present invention describes novel nitrosated and/or nitrosylated H2 receptor antagonist compounds, and novel compositions comprising at least one H2 receptor antagonist compound that is optionally substituted with at least one NO and/or NO2 group, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase. The present invention also describes methods for treating and/or preventing gastrointestinal disorders; improving gastroprotective properties of H2 receptor antagonists; decreasing the recurrence of ulcers; facilitating ulcer healing; preventing and/or treating inflammations and microbial infections, ophthalmic diseases and disorders, multiple sclerosis, and viral infections; and decreasing or reducing the gastrointestinal toxicity associated with the use of nonsteroidal antiinflammatory compounds.
Type:
Grant
Filed:
November 17, 1999
Date of Patent:
April 22, 2003
Assignee:
NitroMed, Inc.
Inventors:
David S. Garvey, L. Gordon Letts, Tiansheng Wang
Abstract: Isothiazolecarboxamides of the formula:
wherein X, Y, R1, R2, R3 and R4 have the meanings given in the specification, may be used as microbicides.
Abstract: The invention relates to known and to new acylaminosalicylamides, to a plurality of processes for their preparation and to their use as pesticides. The present application furthermore relates to new intermediates, to a plurality of processes for their preparation and to their use as pesticides.
Type:
Grant
Filed:
September 21, 1999
Date of Patent:
April 15, 2003
Assignee:
Bayer Aktiengesellschaft
Inventors:
Thomas Seitz, Klaus Naumann, Ralf Tiemann, Klaus Stenzel, Gerd Hänssler, Stefan Dutzmann
Abstract: Described is a process for the preparation of a compound of formula (I) wherein R is unsubstituted or substituted C1-C12alkyl, C2-C4alkenyl, C2-C4alkynyl, C3-C6cycloalkyl, aryl or heteroaryl, or —SR1; R1 is unsubstituted or substituted C1-C12alkyl, C2-C4alkenyl, C2-C4alkynyl, cycloalkyl, aryl or heteroaryl; and X is a leaving group; which comprises: a) reacting a compound of formula (II) wherein R is as defined for formula (I), with a water-removing reagent; or b) for the preparation of a compound of formula (I) wherein X is halogen or a sulfonate, reacting a compound of the formula (III) wherein R is as defined for formula (I), with a halogenating or a sulfonylating agent; or c) for the preparation of a compound of formula (I) wherein X is halogen, reacting a compound of formula (IV) wherein R is as defined for formula (I); and wherein R2 and R3 are for example H, C1-C6alkyl, C3-C6cycloalkyl, phenyl or benzyl; with a compound of the formula halogen-C(═O)—O—C1-C8alkyl, halogen-C(═O
Type:
Grant
Filed:
June 18, 1999
Date of Patent:
April 15, 2003
Assignee:
Syngenta Crop Protection, Inc.
Inventors:
Thomas Pitterna, Henry Szczepanski, Peter Maienfisch, Ottmar Franz Hüter, Thomas Rapold, Marcel Senn, Thomas Göbel, Anthony Cornelius O'Sullivan
Abstract: The invention provides novel substituted benzylthiazolidine-2,4-dione derivatives which increase the transactivation of receptor as a ligand of human peroxisome proliferator-activated receptor (PPAR) and exhibit the blood glucose-decreasing action and lipid-decreasing action, and a process for preparing them.
The invention relates to substituted benzylthiazolidine-2,4-dione derivatives represented by the general formula (1)
[wherein A denotes a pyridyl group or cyclohexyl group], their medicinally acceptable salts, their hydrates and a process for preparing them.
Type:
Grant
Filed:
February 20, 2002
Date of Patent:
April 8, 2003
Assignee:
Kyorin Pharmaceutical Co., Ltd.
Inventors:
Shizuyoshi Fujimori, Koji Murakami, Masaki Tsunoda