Z Contains A Cyclopentyl Or Cyclopentene Ring Patents (Class 514/530)
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Patent number: 6958146Abstract: Various exemplary compounds, compositions and methods are disclosed. An exemplary composition includes an insecticide comprising a formula weight greater than approximately 220 and a compound comprising an insect stimulant and a formula weight less than approximately 220. An exemplary method includes applying an insecticide comprising a formula weight greater than approximately 220 and applying a compound comprising an insect stimulant and a formula weight less than approximately 220. Exemplary compounds optionally include semiochemicals of insects, plants and/or animals. Other exemplary compounds, compositions and/or methods are also disclosed.Type: GrantFiled: May 28, 2003Date of Patent: October 25, 2005Assignee: Bug Buster Ltd.Inventors: Leonard R. Askham, Charles F. Dunham, Leonard D. Felix, Jr.
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Patent number: 6956056Abstract: The present invention relates to a novel method for providing a cathartic effect to a patient in need of cathartic induction, which comprises administering to the patient a cathartic-inducing effective amount of halogenated bioactive lipid comprising the following partial structure (I): The method is useful for relieving or preventing constipation, and also for cleansing the gastrointestinal tract.Type: GrantFiled: May 20, 2002Date of Patent: October 18, 2005Assignee: Sucampo AGInventor: Ryuji Ueno
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Patent number: 6956057Abstract: 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 which is a EP4 agonist.Type: GrantFiled: September 26, 2003Date of Patent: October 18, 2005Assignee: Allergan, Inc.Inventors: David F. Woodward, Achim H. Krauss, Robert M. Burk, Mark Holoboski, Mari F. Posner
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Patent number: 6933289Abstract: This invention relates to a method of reducing an irritating or adverse side effect associated with the topical use of an active ophthalmic drug comprising incorporating an effective amount of a cyclodextrin or cyclodextrin derivative into a formulation to complex the active drug such that the concentration of the free active drug is reduced below a tolerable threshold, and incorporating an effective amount of a viscosity increasing agent in said formulation such that the bioavailability of said drug is high enough to be therapeutically effective, wherein the cyclodextrin or cyclodextrin derivative is not required to solubilize the active drug. Another aspect of this invention relates to topical ophthalmic formulations comprising an active drug, a cyclodextrin or cyclodextrin derivative, and a viscosity-enhancing agent, in effective amounts as stated above.Type: GrantFiled: July 1, 2003Date of Patent: August 23, 2005Assignee: Allergan, Inc.Inventors: Robert T. Lyons, James N. Chang
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Patent number: 6921774Abstract: The invention provides novel compounds of the formula I below: wherein the meaning of each substituent is defined in the application. The compounds are useful as inhibitors of the glycine transporter and useful in the treatment of diseases responsive to the inhibition of the glycine transporter. The invention provides a pharmaceutical composition comprising a compound of Formula I as defined above and the use of compounds as above for the manufacture of medicaments for treatment of diseases responsive to ligands of the glycine transporter.Type: GrantFiled: January 17, 2003Date of Patent: July 26, 2005Assignee: H. Lundbeck A/SInventors: Ejner Knud Moltzen, Paul Garrick Smith, Christian Krog-Jensen, Klaus Peter Bøgesø
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Patent number: 6884819Abstract: The present invention provides a neurodegenerative disease therapeutic agent containing as its active ingredient a (15R)-isocarbacycline derivative indicated by the following formula [I] or a 15-deoxy-isocarbacycline derivative indicated by the following formula [III]: (wherein, R1 represents a C1-C6 alkylene group, and R2 represents a hydrogen atom, a C1-C7, alkyl group or protective group); or, (wherein, R1 and R2 are the same as those defined in formula [I]).Type: GrantFiled: August 4, 2000Date of Patent: April 26, 2005Assignees: Teijin Limited, Osaka Bioscience InstituteInventors: Yorimasa Suwa, Noboru Yoshioka, Takami Arai, Katsutoshi Sakurai, Jun Suzuki, Yasuyoshi Watanabe, Masaaki Suzuki, Takumi Satoh, Yumiko Watanabe, Yosuke Kataoka
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Patent number: 6875787Abstract: 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 the dashed line indicates the presence or absence of a bond, the hatched wedge indicates the ? (down) configuration, and the solid triangle indicates the ? (up) configuration; B is a single, double, or triple covalent bond; n is 0-6; X is CH2, S or O; Y is any pharmaceutically acceptable salt of CO2H, or CO2R, CONR2, NHCH2CH2OH, N(CH2CH2OH)2, CH2OR, P(O)(OR)2, CONRSO2R, SONR2, or R is H, C1-6 alkyl or C2-6 alkenyl; R2 and R3 are C1-6 linear alkyl which may be the same or different, and may be bonded to each other such that they form a ring incorporating the carbon to which they are commonly attached; R4 is hydrogen, R, C(?O)R, or any group that is easily removed under physiological conditions such that R4 is effectively hydrogen; R5 is hydrogenType: GrantFiled: February 11, 2003Date of Patent: April 5, 2005Assignee: Allergan, Inc.Inventor: Yariv Donde
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Patent number: 6858650Abstract: The present invention concerns highly pure, crystalline, stable compounds of novel derivatives of 3,3-diphenylpropylamines in the form of their salts, a method for the manufacture and highly pure, stable intermediate products. The method is in particular characterized by regio- and chemoselectivity and high yield. Salts of phenolic monoesters of 3,3-diphenylpropylamines are provided, that are particularly well-suited for use in pharmaceutical formulations. Preferred compounds are R-(+)-2-(3-diisopropylamino-1-phenyl-propyl)-4-hydroxymethylphenylisobutyrate ester hydrogen fumarate and R-(+)-2-(3-diisopropylamino-1-phenylpropyl)-4-hydroxymethylphenylisobutyrate ester hydrochloride hydrate. Furthermore, stable, crystalline intermediate products that are essential for obtaining the abovementioned salts are provided. A preferred intermediate product is R-(?)-3-(3-diisopropylamino-phenyl-propyl)-4-hydroxy-benzoic acid methyl ester.Type: GrantFiled: November 15, 2000Date of Patent: February 22, 2005Assignee: Schwarz Pharma AGInventor: Claus Meese
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Patent number: 6852880Abstract: The present invention relates to a process for effectively preparing prostaglandin derivatives and to a stereospecific alkyl halide containing 15S-alcohol group as a starting material.Type: GrantFiled: May 7, 2002Date of Patent: February 8, 2005Assignee: Yonsung Fine Chemical Co.Inventors: Won-Hun Ham, Chang-Young Oh, Kee-Young Lee, Yong-Hyun Kim, Yiu-Suk Lee
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Patent number: 6849649Abstract: The invention relates to compounds of formula (I) for treating for example sexual dysfunction, wherein R1 is optionally substituted C1-6alkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl, hydrogen, C1-6alkoxy, —NR2R3 or —NR4SO2R5; X is the linkage —(CH2)n— or —(CH2)q—O— (wherein Y is attached to the oxygen); wherein one or more hydrogen atoms in linkage X may be replaced independently by C1-4alkoxy; hydroxy; hydroxy(C1-3alkyl); C3-7cycloalkyl; carbocyclyl; heterocyclyl; or by C1-4alkyl optionally substituted by one or more fluoro or phenyl groups; n is 3, 4, 5, 6 or 7; and q is 2, 3, 4, 5 or 6; and Y is phenyl or pyridyl, each of which may be substituted; or two R8 groups on adjacent carbon atoms together with the interconnecting carbon atoms may form a fused optionally substituted 5- or 6-membered carbocyclic or heterocyclyic ring.Type: GrantFiled: October 28, 2003Date of Patent: February 1, 2005Assignee: Pfizer Inc.Inventors: Stephen Challenger, Andrew Simon Cook, Adam Thomas Gillmore, Donald Stuart Middleton, David Cameron Pryde, Alan Stobie
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Publication number: 20040258730Abstract: A sustained release film preparation for local administration to the region of diseases associated with decrease in bone mass, which comprises, as an active ingredient thereof, (11&agr;,13E,15&agr;)-9-oxo-11,15-dihydroxy-16-(3-methoxymethylphenyl)-17,18,19,20-tetranor-5-thiaprost-13-enoic acid methyl ester having the following formula (I) or a non-toxic salt thereof: 1Type: ApplicationFiled: May 11, 2004Publication date: December 23, 2004Inventors: Yasuhiko Tabata, Akio Nishiura
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Publication number: 20040242615Abstract: Compounds having an activity to enhance the expression of apoAI are provided.Type: ApplicationFiled: April 19, 2004Publication date: December 2, 2004Inventors: Teruo Yamamori, Kiyoshi Nagata, Natsuki Ishizuka, Kunio Hayashi
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Patent number: 6825232Abstract: The topical use of HETE compounds to treat ophthalmic inflammatory disorders involving cytokines is disclosed.Type: GrantFiled: April 9, 2003Date of Patent: November 30, 2004Assignee: Alcon, Inc.Inventor: Daniel A. Gamache
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Patent number: 6780874Abstract: Enamine derivatives of formula (1) are described: wherein R1 is a group Ar1L2Ar2Alk- in, which Ar1 is an aromatic or heteroaromatic group, L2 is a covalent bond or a linker atom or group, Ar2 is an arylene or heteroarylene group and Alk is a chain —CH2—CH(R)—, —CH═C(R)— or in which R is a carboxylic acid or a derivative or biostere thereof; R2 is a hydrogen atom or a C1-6alkyl group; Cy is a cycloaliphatic or heterocycloaliphatic ring in which X is a N atom or a C(Rw) group; Rx is a oxo, thioxo, or imino group; Rw and Rz is each a hydrogen atom or optional substituent; provided that Cy is not a cyclobutenedione group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders, or disorders involving the inappropriate growth or migration of cells.Type: GrantFiled: June 10, 2003Date of Patent: August 24, 2004Assignee: Celltech R & D LimitedInventors: Timothy John Norman, John Robert Porter, Brian Woodside Hutchinson, Andrew James Ratcliffe, John Clifford Head, Rikki Peter Alexander, Barry John Langham, Graham John Warrellow, Sarah Catherine Archibald, Janeen Marsha Linsley
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Patent number: 6770675Abstract: An improved ophthalmic composition, including docosanoid active agents, which is especially useful in lowering intraocular pressure associated with glaucoma. Improvements in IOP reduction efficacy, preservative efficacy and reduced additive concentrations are achieved by utilizing the disclosed compositions which include a docosanoid active agent (e.g., isopropyl unoprostone), in conjunction with selected non-ionic surfactants, preservatives, and non-ionic tonicity adjusting agents.Type: GrantFiled: March 19, 2001Date of Patent: August 3, 2004Assignee: Novartis AGInventors: Kenneth Warren Reed, Shau Fong Yen, Mary Sou, Regina Flinn Peacock
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Patent number: 6767920Abstract: 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 hatched lines represent the &agr; configuration, a triangle represents the &bgr; configuration, a wavy line represents the &agr; configuration or the &bgr; configuration and a dotted line represents the presence or absence of a double bond; A and B are independently selected from the group consisting of O, S and CH2; provided that at least one of A or B is S; D represents a covalent bond or CH2, O, S or NH; X is CO2R, CONR2, CH2OR, P(O)(OR)2, CONRSO2R SONR2 or Y is O, OH, OCOR2, halogen or cyano; Z is CH2 or a covalent bond; R is H or R2; R1 is H, R2, phenyl, or COR2; R2 is C1-C5 lower alkyl or alkenyl and R3 is benzothienyl, benzofuranyl, naphthyl or substituted derivatives thereof, wherein the substituents mayType: GrantFiled: January 16, 2003Date of Patent: July 27, 2004Assignee: Allergan, Inc.Inventors: Robert M. Burk, Mark Holoboski, Mari F. Posner
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Publication number: 20040115290Abstract: A natural formulation of compounds that would to modulate inflammation is disclosed. The formulation would also inhibit expression of COX-2, inhibit synthesis of prostaglandins selectively in target cells, and inhibit inflammatory response selectively in target cells. The compositions containing at least one fraction isolated or derived from hops.Type: ApplicationFiled: June 18, 2003Publication date: June 17, 2004Inventors: Matthew L. Tripp, John G. Babish, Jeffrey S. Bland, Gary K. Darland, Robert Lerman, Daniel O. Lukaczer, DeAnn J. Liska, Terrence Howell
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Patent number: 6750364Abstract: This invention provides compounds of the formula: wherein X is (CH2)n, O, S, SO, SO2 or CR1R2; n is 1 or 2; R1 and R2 are H, halogen, hydroxy, alkyl of 1 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms, or R1 and R2, taken together form cycloalkyl of 3 to 6 carbon atoms, an alkylidene of up to 6 carbon atoms or a carbonyl; R3, R4 and R5 are H or alkyl of 1 to 6 carbon atoms; Z is H, alkyl of 1 to 6 carbon atoms, alkanoyl of 1 to 6 carbon atoms or alkoxycarbonyl of 2 to 7 carbon atoms; or a pharmaceutically acceptable salt thereof, as well as pharmaceutical compositions and methods for their use in treating or preventing characterized by glutamate hypofunction, including schizophrenia, schizoaffective disorder and schizophreniform disorder, and for the treatment of cognitive deficits due to aging, stroke, Alzheimer's disease or other neurodegenerative diseases.Type: GrantFiled: June 27, 2002Date of Patent: June 15, 2004Assignee: WyethInventors: Gary Paul Stack, John Dunlop, Alexander Alexei Greenfield, Jonathan Laird Gross
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Patent number: 6740772Abstract: A prostaglandin derivative represented by the formula: wherein X is a halogen atom in the &agr;- or &bgr;-position, Y is an ethylene group, a vinylene group or an ethynylene group, A is a group represented by the formula: O(CH2)n, S(O)p(CH2)n, O(CH2)qO(CH2)r, O(CH2)qS(O)p(CH2)r, S(O)p(CH2)qS(O)p(CH2)r or S(O)p(CH2)qO(CH2)r (wherein n is an integer of 1 to 5, p is 0, 1 or 2, q is an integer of 1 to 3, and r is 0 or 1), R1 is a C3-10 cycloalkyl group, a C1-4 alkyl-C3-10 cycloalkyl group, a C3-10 cycloalkyl-C1-4 alkyl group, a C5-10 alkyl group, a C5-10 alkenyl group, a C5-10 alkynyl group or a bridged cyclic hydrocarbon group, R2 is a hydrogen atom, a C1-10 alkyl group or a C3-10 cycloalkyl group, and m is 0, 1 or 2], a pharmaceutically acceptable salt thereof or a hydrate thereof. The present invention is to provide novel PG derivatives having an excellent PGD2-like agonistic activity and a sleep-inducing action.Type: GrantFiled: March 11, 2002Date of Patent: May 25, 2004Assignees: Taisho Pharmaceutical Co., Ltd., Fumie SatoInventors: Fumie Sato, Tohru Tanami, Hideo Tanaka, Naoya Ono, Makoto Yagi, Hitomi Hirano
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Patent number: 6723748Abstract: Disclosed is the use of cloprostenol and fluprostenol analogues in combination with carbonic anhydrase inhibitors for the treatment of glaucoma and ocular hypertension and ophthalmic compositions therefor.Type: GrantFiled: February 5, 2002Date of Patent: April 20, 2004Assignee: Alcon Manufacturing, Ltd.Inventors: Peter G. Klimko, John E. Bishop, Verney L. Sallee, Paul W. Zinke
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Patent number: 6716876Abstract: The invention relates to 7-[5-hydroxy-2-(hydroxyhydrocarbyl or heteroatom-substituted hydroxy hydrocarbyl)-3-hydroxy-cyclopentyl(enyl)] heptanoic or heptenoic acids and derivatives of said acids, wherein one or more of said hydroxy groups are replaced by an ether group. The compounds of the present invention are potent ocular hypotensives, and are particularly suitable for the management of glaucoma.Type: GrantFiled: February 28, 2002Date of Patent: April 6, 2004Assignee: Allergan, Inc.Inventor: Robert M. Burk
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Patent number: 6713464Abstract: The invention concerns novel derivatives of 3,3-diphenylpropylamines, methods for their preparation, pharmaceutical compositions containing the novel compounds, and the use of the compounds for preparing drugs. More particularly, the invention relates to novel prodrugs of antimuscarinic agents with superior pharmacokinetic properties compared to existing drugs such as oxybutynin and tolterodine, methods for their preparation, pharmaceutical compositions containing them, a method of using said compounds and compositions for the treatment of urinary incontinence, gastrointestinal hyperactivity (irritable bowel syndrome) and other smooth muscle contractile conditions.Type: GrantFiled: January 2, 2001Date of Patent: March 30, 2004Assignee: Schwarz Pharma AGInventors: Claus Meese, Bengt Sparf
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Patent number: 6710081Abstract: Therapeutic agents for erectile dysfunction containing as the active ingredient prostaglandin derivatives of formula (I) (wherein symbols have the same meanings as described in the description), nontoxic salts thereof, or cyclodextrin clathrate compounds thereof.Type: GrantFiled: April 8, 2002Date of Patent: March 23, 2004Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Masami Narita, Kouzou Yoshida
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Publication number: 20040054003Abstract: Compounds of the general formula (I) which are metabolically stable and have an antagonistic activity against PGD2 receptor: 1Type: ApplicationFiled: April 18, 2003Publication date: March 18, 2004Inventors: Norihiko Tanimoto, Yoshiharu Hiramatsu, Tsunetoshi Honma
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Patent number: 6689901Abstract: The present invention is a novel intermediate, compound of the formula (VI) and salts thereof. In addition, the invention includes a process for the preparation of a 15(S)-prostaglandin intermediates compounds (IV) and (XVIII) which comprises (1) contacting a the corresponding enone with (−)-chlorodiisopinocampheylborane while maintaining the reaction mixture temperature in the range of from about −50° to about 0° and (2) contacting the reaction mixture of step (1) with a boron complexing agent.Type: GrantFiled: June 25, 2002Date of Patent: February 10, 2004Assignee: Pharmacia & Upjohn CompanyInventor: Kevin E. Henegar
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Patent number: 6689906Abstract: The invention is a novel series of cyclic amino acids which are useful in the treatment of epilepsy, faintness attacks, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, gastrointestinal disorders such as irritable bowel syndrome (IBS), and inflammation, especially arthritis. A pharmaceutical composition containing a compound of the invention as well as methods of preparing the compounds and novel intermediates useful in the preparation of the final compounds are included.Type: GrantFiled: April 19, 2002Date of Patent: February 10, 2004Assignee: Warner-Lambert CompanyInventors: Justin Stephen Bryans, David Clive Blakemore, Simon Andrew Osborne, Jean-Marie Receveur
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Patent number: 6683071Abstract: This invention relates to a method for the initiation of oestrus and ovulation early postpartum, especially but not exclusively, in dairy cows which comprises supplying a prostaglandin post partum and subsequently treating with a progesterone.Type: GrantFiled: July 17, 2002Date of Patent: January 27, 2004Assignees: The University of Nottingham, Milk Development CouncilInventor: George Eric Lamming
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Patent number: 6680339Abstract: 15-fluoro substituted analogs of PGF2&agr; and methods of their use in treating glaucoma and ocular hypertension are disclosed.Type: GrantFiled: March 18, 2002Date of Patent: January 20, 2004Assignee: Alcon Manufacturing, Ltd.Inventors: Peter G. Klimko, Mark R. Hellberg, Paul W. Zinke
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Patent number: 6680337Abstract: The present invention provides cyclopentane heptanoic acid, 2 heteroaryl alkyl or alkenyl derivatives which may be substituted in the 1-position with hydroxyl, alkyloxy, amino and amido groups, e.g. 1-OH cyclopentane heptanoic acid, 2 heteroarylalkenyl derivatives. In particular, these derivatives are 7-[5-hydroxy-2-(heteroatom-substituted hydroxyhydrocarbyl)-3-hydroxycyclopentyl] heptanoic or heptenoic acids and amine, amide, ether, ester and alchohol derivatives of said acids wherein one or more of said hydroxy groups are replaced with an ether group. These compounds are potent ocular hypotensive and are particularly suited for the management of glaucoma.Type: GrantFiled: March 7, 2003Date of Patent: January 20, 2004Assignee: Allergan, Inc.Inventor: Robert M. Burk
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Patent number: 6673841Abstract: The present invention relates to a composition of topical preparation containing alprostadil alkyl ester, and more particularly, comprising an alprostadil alkyl ester, an oily vehicle, a skin permeation enhancer and an anti-irritant agent.Type: GrantFiled: December 20, 2001Date of Patent: January 6, 2004Assignee: Whan In Pharm. Co., Ltd.Inventors: Dong Soo Lee, Kye Kwan Lee, Yun Seok Rhee, Jun Hee Jang, Sun Oh Jeoung, Sang Jin Kim, Sang Cheol Chi
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Patent number: 6670394Abstract: This invention relates to a method for the prophylaxis of or for treating COPD by administering a PDE4 inhibitor which has a defined therapeutic ratio.Type: GrantFiled: August 31, 2001Date of Patent: December 30, 2003Assignee: SmithKline Beecham CorporationInventors: Siegfried B. Christensen, IV, Mary S. Barnette, Theodore J. Torphy
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Patent number: 6664290Abstract: This invention relates to a method of limiting postpartum hemorrhage comprising administering orally a single effective dose of misoprostol to a woman during the third stage of labor.Type: GrantFiled: April 15, 1997Date of Patent: December 16, 2003Assignee: University College LondonInventor: Hazem El-Rafaey
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Patent number: 6660756Abstract: The invention relates to compounds of formula (I) for treating for example sexual dysfunction, wherein R1 is optionally substituted C1-6alkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl, hydrogen, C1-6alkoxy, —NR2 R3 or —NR4SO2R5; X is the linkage —(CH2)n— or —(CH2)q—O— (wherein Y is attached to the oxygen); wherein one or more hydrogen atoms in linkage X may be replaced independently by C1-4alkoxy; hydroxy; hydroxy(C1-3alkyl); C3-7cycloalkyl; carbocyclyl; heterocyclyl; or by C1-4alkyl optionally substituted by one or more fluoro or phenyl groups; n is 3, 4, 5, 6 or 7; and q is 2, 3, 4, 5 or 6; and Y is phenyl or pyridyl, each of which may be substituted; or two R8 groups on adjacent carbon atoms together with the interconnecting carbon atoms may form a fused optionally substituted 5- or 6-membered carbocyclic or heterocyclyic ring.Type: GrantFiled: March 12, 2002Date of Patent: December 9, 2003Assignee: Pfizer Inc.Inventors: Stephen Challenger, Andrew Simon Cook, Adam Thomas Gillmore, Donald Stuart Middleton, David Cameron Pryde, Alan Stobie
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Publication number: 20030220292Abstract: Methods for the treatment of erectile dysfunction are provided comprising placing in the fossa navicularis an amount of a semi-solid vasoactive prostaglandin composition sufficient to increase blood flow in the glans penis and resulting in increased tumescence of the penis. In preferred embodiments, the method further comprises providing erotic stimuli. Another embodiment, the invention provides a method for increasing the tumescence of the glans penis. In another aspect, the invention provides compositions and articles of manufacture for the practice of the methods of the invention.Type: ApplicationFiled: February 14, 2003Publication date: November 27, 2003Applicant: NexMed (Holdings), Inc.Inventors: Koichi Okada, James L. Yeager, Nadir Buyuktimkin, Servet Buyuktimkin
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Publication number: 20030220396Abstract: The present invention provides a method for treating ocular hypertension and glaucoma, which comprises administrating an ophthalmic solution comprising as an active ingredient thereof 15-keto-prostaglandin compound having a ring structure at the end of the &ohgr; chain, wherein the intraocular pressure (IOP) lowering effect is improved by adjusting the osmolarity ratio of said solution to be within a specific range.Type: ApplicationFiled: March 27, 2003Publication date: November 27, 2003Applicant: SUCAMPO AGInventor: Ryuji Ueno
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Publication number: 20030220397Abstract: The invention is a novel series of cyclic amino acids which are useful in the treatment of epilepsy, faintness attacks, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, gastrointestinal disorders such as irritable bowel syndrome (IBS), and inflammation, especially arthritis. A pharmaceutical composition containing a compound of the invention as well as methods of preparing the compounds and novel intermediates useful in the preparation of the final compounds are included.Type: ApplicationFiled: May 30, 2003Publication date: November 27, 2003Inventors: Justin Stephen Bryans, David Christopher Horwell, Andrew John Thorpe, David Juergen Wustrow, Po-Wai Yuen
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Publication number: 20030220395Abstract: 15-keto latanoprost and other 15-keto prostaglandin analogs are used as ocularly applied intraocular pressure reducing agents.Type: ApplicationFiled: March 12, 2003Publication date: November 27, 2003Applicant: SUCAMPO, A.G.Inventor: Ryuji Ueno
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Patent number: 6649653Abstract: 15-Fluoro substituted analogs of PGF2&agr; and methods of their use in treating glaucoma and ocular hypertension are disclosed.Type: GrantFiled: June 2, 1999Date of Patent: November 18, 2003Assignee: Alcon Manufacturing, Ltd.Inventors: Peter G. Klimko, Mark R. Hellberg, Paul W. Zinke
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Patent number: 6649654Abstract: The present invention provides methods and compositions for inhibiting IKK, as well as methods and compositions for identifying compounds with activity as inhibitors of IKK, and methods and compositions for the treatment of diseases and/or conditions wherein IKK is implicated and inhibition of its activity is desired. In addition, the present invention provides methods and compositions for the improving the therapeutic activity of COX2 inhibitors, comprising administering the COX2 to a subject in combination with a compound that inhibits IKK activity. The present invention further provides compositions that comprise compounds that inhibit IKK and COX2.Type: GrantFiled: November 22, 2000Date of Patent: November 18, 2003Assignee: The Regents of the University of CaliforniaInventors: Michael Karin, Pankaj Kapahi
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Patent number: 6649655Abstract: Methods and compositions for the antagonism of FP receptor-mediated biological responses are disclosed.Type: GrantFiled: July 24, 2002Date of Patent: November 18, 2003Assignee: Alcon Manufacturing, Ltd.Inventors: Najam A. Sharif, Brenda W. Griffin
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Publication number: 20030212139Abstract: Topical application of a prostaglandin directly to the clitoris is effective for enhancing female sexual desire and responsiveness.Type: ApplicationFiled: April 11, 2003Publication date: November 13, 2003Inventor: Gary W. Neal
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Patent number: 6646001Abstract: Disclosed are methods and compositions for the treatment of glaucoma and ocular hypertension, comprising the administration of a prostaglandin FP receptor agonist and a prostaglandin synthesis inhibitor.Type: GrantFiled: January 28, 2002Date of Patent: November 11, 2003Assignee: Alcon Manufacturing, Ltd.Inventors: Mark R. Hellberg, Jon C. Nixon
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Publication number: 20030207852Abstract: Methods and formulations for treating female sexual dysfunction are provided. A pharmaceutical composition formulated so as to contain a selected vasoactive agent is administered to the vagina, vulvar area or urethra of the individual undergoing treatment. Suitable vasoactive agents are vasodilators, including naturally occurring prostaglandins, synthetic prostaglandin derivatives, endothelial-derived relaxation factors, vasoactive intestinal polypeptide agonists, smooth muscle relaxants, leukotriene inhibitors, and others. The formulations are also useful for preventing the occurrence of yeast infections, improving vaginal muscle tone and tissue health, enhancing vaginal lubrication, and minimizing excess collagen deposition. A clitoral drug delivery device is also provided.Type: ApplicationFiled: June 2, 2003Publication date: November 6, 2003Inventors: Virgil A. Place, Leland F. Wilson, Paul C. Doherty, Mark S. Hanamoto, Alfred P. Spivack, Neil Gesundheit, Sean R. Bennett
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Publication number: 20030203921Abstract: The instant invention is a method of using certain analogs of glutamic acid and gamma-aminobutyric acid in combination with an anti-viral agent to treat shingles.Type: ApplicationFiled: April 2, 2003Publication date: October 30, 2003Inventors: Leslie Magnus, Catherine Segal
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Publication number: 20030191182Abstract: The invention provides novel compounds of the Formula (I) that stimulate rates of glucose oxidation in myocardial cells.Type: ApplicationFiled: April 9, 2003Publication date: October 9, 2003Inventors: Gary David Lopaschuk, John Christopher Vederas, Jason R Dyck
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Publication number: 20030171431Abstract: The present invention relates to a 2-fluoro-2-(3-oxobicyclopentyl)acetate derivative represented by the formula (1): 1Type: ApplicationFiled: December 17, 2002Publication date: September 11, 2003Inventors: Atsuro Nakazato, Toshihito Kumagai, Kazunari Sakagami, Takeo Taguchi
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Patent number: 6610715Abstract: The present invention provides novel cathecol hydrazone derivatives of formula (I) or pharmaceutically acceptable salts thereof, wherein R1 is C1-7 alkyl or C3-7 cycloalkyl; R2 is hydrogen, hydroxy, C1-5 alkyl or —CH2CH2C(═O)NH2; R3 and R4 are independently hydrogen, C1-7 alkyl, —C(═X)—R5, or 2-, 3- or 4-pyridyl, prymidyl or phenyl substituted with one or two selected from a group consisting of halogen, C1-6 alkoxy, nitro, trifluoromethyl, C1-6 alkyl and carboxyl, or R3 and R4 are directly bonded by C3-4 containing oxygen, sulfur or nitrogen to form a heterocyclic ring, X is oxygen, sulfur or NH and R5 is C1-7 alkyl, —NHR6, CONH2 or 2-, 3- or 4-pyridyl, prymidyl or phenyl substituted with one selected from a group consisting of halogen, C1-6 alkoxy, nitrile, trifluoromethyl, C1-6 alkyl and carboxyl, and R6 is hydrogen, hydroxy, NH2, C1-5 alkoxy, C1-5 alkyl, pyridyl or phenyl.Type: GrantFiled: November 13, 2001Date of Patent: August 26, 2003Assignee: Cheil Jedang CorporationInventors: Yong Sik Youn, Myung Xik Xiang, Byoung Chol Suh, Jong Hoon Kim, Kwang Hyuk Lee, Eui Kyung Kim, Jae Kyu Shin, Chung Keun Rhee
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Patent number: 6610719Abstract: This invention is directed to methods and compositions of treating acute or chronic renal failure or dysfunction, or conditions caused thereby, comprising administering prostaglandin agonists, which are EP4 receptor selective prostaglandin agonists.Type: GrantFiled: January 29, 2001Date of Patent: August 26, 2003Assignee: Pfizer Inc.Inventors: Vishwas M. Paralkar, David D. Thompson
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Patent number: 6610700Abstract: Enamine derivatives of formula (1) are described: wherein R1 is a group Ar1 L2Ar2Alk- in which Ar1 is an aromatic or heteroaromatic group, L2 is a covalent bond or a linker atom or group, Ar2 is an arylene or heteroarylene group and Alk is a chain —CH2—CH(R)—, —CH═C(R)— or in which R is a carboxylic acid or a derivative or biostere thereof; R2 is a hydrogen atom or a C1-6alkyl group; Cy is a cycloaliphatic or heterocycloaliphatic ring in which X is a N atom or a C(Rw) group; Rx is a oxo, thioxo, or imino group; Rw and Rz is each a hydrogen atom or optional substituent; provided that Cy is not a cyclobutenedione group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders, or disorders involving the inappropriate growth or migration of cells.Type: GrantFiled: April 16, 2001Date of Patent: August 26, 2003Assignee: Celltech R & D LimitedInventors: Timothy John Norman, John Robert Porter, Brian Woodside Hutchinson, Andrew James Ratcliffe, John Clifford Head, Rikki Peter Alexander, Barry John Langham, Graham John Warrellow, Sarah Catherine Archibald, Janeen Marsha Linsley
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Patent number: 6596752Abstract: The present invention relates to small molecules according to the formula [I]: which are potent inhibitors of &agr;4&bgr;1 mediated adhesion to either VCAM or CS-1 and which can be used for treating or preventing &agr;4&bgr;1 adhesion mediated conditions in a mammal such as a human.Type: GrantFiled: July 12, 2002Date of Patent: July 22, 2003Assignees: Tanabe Seiyaku Co., Ltd., Pharmacia & Upjohn CompanyInventors: Thomas J. Lobl, Bradley R. Teegarden, Alexander Polinsky, Gilbert M. Rishton, Masafumi Yamagishi, Steven Tanis, Jed F. Fisher, Edward W. Thomas, Robert A. Chrusciel