Z Contains A Cyclopentyl Or Cyclopentene Ring Patents (Class 514/530)
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Patent number: 6291522Abstract: The invention relates to the use of cyclopentane heptan(ene)oic acid, 2-thiocarbamoyloxy and carbamoyloxy as therapeutic agents e.g. as ocular hypotensives.Type: GrantFiled: September 27, 2000Date of Patent: September 18, 2001Assignee: Allergan Sales, Inc.Inventor: Robert M. Burk
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Patent number: 6291516Abstract: The present invention makes available methods and reagents for inhibiting aberrant growth states resulting from hedgehog gain-of-function, ptc loss-of-function or smoothened gain-of-function comprising contacting a cell with a compound, such as a polypeptide or small molecule in an amount sufficient to control the aberrant growth state, e.g., to agonize a normal ptc pathway or antagonize smoothened or hedgehog activity. The present invention further makes available methods and reagents for ameliorating the consequences of hedgehog loss-of-function, ptc gain-of-function, or smoothened loss-of-function comprising contacting a cell with a compound, such as a polypeptide or small molecule, in an amount sufficient to ameliorate the In certain embodiments, the subject compounds, e.g., a cAMP analog, adenylate cyclase agonist, or cAMP phosphodiesterase inhibitor, regulate cAMP levels, which in turn modulates activity of the hedgehog pathway.Type: GrantFiled: October 14, 1999Date of Patent: September 18, 2001Assignee: Curis, Inc.Inventors: Henryk Dudek, Benxiu Ji
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Patent number: 6291521Abstract: The present invention provides an anti-portal hypertensive agent comprising a 15-keto-prostaglandin compound as an active ingredient.Type: GrantFiled: June 14, 1999Date of Patent: September 18, 2001Assignee: R-Tech Ueno, Ltd.Inventor: Ryuji Ueno
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Patent number: 6288113Abstract: An angiogenesis promoter containing a compound of the following formula (I) wherein R1 is acyl, R2 is alkyl, R3 and R4 are the same or different and each is hydrogen atom or hydroxy protecting group and R5 is alkyl, as an active ingredient. This compound itself not only has an angiogenesis promoting effect but also potentiates the angiogenic effect by a drug (e.g., b-FGF) having such effect. Therefore, it can express the angiogenesis promoting effect more effectively in the ischemic tissues and the site under different disease state, where b-FGF has locally increased.Type: GrantFiled: June 21, 2000Date of Patent: September 11, 2001Assignees: Welfide Corporation, Seikagaku CorporationInventors: Yasuhiro Egi, Yoshiji Kubo, Satoru Inoue, Hideaki Kido, Masakuni Nishikawa, Kazutaka Hayashi
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Patent number: 6274570Abstract: A liquid pesticidal composition, which is substantially free of water, comprising a hydrophobic pesticide or mixture of pesticides dissolved in an organic solvent and comprising as surfactants (a) a castor oil ethoxylate having 30-50 mol ethoxylate, (b) a branched C8-C18 alcohol ethoxylate having 5-10 mol ethoxylate, and (c) a tristyrenephenol-ethoxylate having 8-30 mol ethoxylate, or its phosphate or salt thereof. The compositions also include gels having a viscosity of 500 to 20,000 mPas and comprising additionally a gelling agent.Type: GrantFiled: December 22, 1998Date of Patent: August 14, 2001Assignee: Syngenta Crop Protection, Inc.Inventors: Manfred Vogt, William Baettig
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Patent number: 6274623Abstract: Alkoxy and/or acyloxy disubstituted and polysubstituted aralkyl and aralkenyl bis-quaternary ammonium derivatives of cyclic alkanol diesters have neuromuscular relaxant properties.Type: GrantFiled: October 25, 1999Date of Patent: August 14, 2001Assignee: Newlaxant LLCInventors: Laszlo Gyermek, Chingmuh Lee, Young-Moon Cho
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Publication number: 20010011104Abstract: Tannate compositions consisting essentially of carbetapentane tannate, phenylephrine tannate and chlorpheniramine tannate which are effective when administered orally for the symptomatic relief of coryza associated with the common cold, sinusitis, allergic rhinitis and upper respiratory tract conditions are disclosed.Type: ApplicationFiled: December 11, 1998Publication date: August 2, 2001Inventor: STEVEN A. GORDZIEL
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Patent number: 6268395Abstract: An antiviral agent comprising as an active ingredient a phorbol derivative of formula (I): (wherein R1, R2, R3, R4, and R5, independently one another, represent a hydrogen atom, an aliphatic carboxylic acid residue, or an aromatic carboxylic acid residue) having a ratio r=CC0/IC100, i.e., ratio of concentration CC0 at which survival of MT-4 cells is decreased upon cell proliferation tests to concentration IC100 at which HIV-1-induced cytopathic effect (CPE) on MT-4 cells is inhibited by 100%, of 2 or more and having a protein kinase C(PKC) activation of 30% or less at a concentration of 10 ng/mL. The agent is useful as an anti-HIV agent.Type: GrantFiled: May 3, 2000Date of Patent: July 31, 2001Assignee: Lead Chemical Co., Ltd.Inventor: Masao Hattori
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Patent number: 6265440Abstract: The novel 13,14-dihydro-15-keto prostaglandins E of the invention have remarkable preventive effects against ulcers. Further, the novel 13,14-dihydro-15-keto-prostaglandins E of the invention have an advantage that they have none of side effects which prostaglandin E intrinsically has, or can remarkably reduce such effects of the prostaglandin E. Therefore, the novel 13,14-dihydro-15-keto prostaglandins E of the invention are effective for animal and human use for treatment and prevention of ulcers, such as duodenal ulcer and gastric ulcer.Type: GrantFiled: May 6, 1998Date of Patent: July 24, 2001Assignee: R-Tech Ueno, Ltd.Inventors: Ryuzo Ueno, Ryuji Ueno, Ichie Kato, Tomio Oda
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Patent number: 6262105Abstract: Methods and compositions for stimulating the growth of hair are disclosed containing prostaglandins, derivatives or analogues thereof for use in treating the skin or scalp of a human or non-human animal. Prostaglandins of the A2, F2&agr; and E2 types are preferred for this treatment method.Type: GrantFiled: August 3, 1999Date of Patent: July 17, 2001Inventor: Murray A. Johnstone
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Patent number: 6258844Abstract: The invention relates to the use of omega chain modified prostaglandins as ocular hypotensive. The derivatives used in accordance with the invention are encompassed by the following structure formula I: wherein the hatched segments represent &agr; bonds; the wavy segment represents an &agr; or &bgr; bond; dashed lines represent a double bond or a single bond; X is selected from the group consisting of —OR and N(R2); Y is=O or represents 2 hydrogen radicals, provided that Y represents 2 hydrogen radicals when X is OH; R is hydrogen or a lower alkyl radical having up to six carbon atoms; R1 is=O or hydroxy; m is 0, 2, 4 or 6, provided that m is not 4 when the wavy segment represents a &bgr; bond; n is 0, 2, 4 or 6; x and y are 0 or 1, provided that x is 1 when y is 0 and y is 1 when x is 0; or 9, 11 and/or 15 ester derivatives of said compound of formula I, e.g. a C1 to C6 alkyl ester derivative; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: November 24, 1998Date of Patent: July 10, 2001Assignee: Allergan Sales, Inc.Inventors: Michael E. Garst, Michael B. Roof, Ming F. Chan, David F. Woodward, Robert M. Burk, Todd S. Gac, Steven W. Andrews
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Patent number: 6251436Abstract: Topical gelled compositions comprising a drug which causes vasodilation, and optionally prostaglandin E1, dispersed within a polymer matrix, and methods of treating sexual dysfunction, including both male and female sexual dysfunction, using said compositions.Type: GrantFiled: September 8, 1998Date of Patent: June 26, 2001Assignee: L.A.M. Pharmaceutical CorporationInventors: Alan Drizen, Peter Rothbart, Gary M. Nath
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Patent number: 6248783Abstract: 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 or OCOR3; 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: September 20, 2000Date of Patent: June 19, 2001Assignee: Allergan Sales, Inc.Inventors: Robert M. Burk, Mark Holoboski, Mari F. Posner
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Patent number: 6242485Abstract: An endothelin antagonist comprising as the active ingredient a prostanoic acid derivative wherein the &agr;-chain has eight or more skeletal carbon atoms.Type: GrantFiled: April 13, 1998Date of Patent: June 5, 2001Assignee: R-Tech UenoInventor: Ryuji Ueno
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Patent number: 6242482Abstract: Prostaglandin and analogs thereof which include protective groups attached to at least one site which are pharmaceutically acceptable and which are capable of slowing the metabolic rate of the active groups for administration to a warm blooded animal for the treatment of congestive heart failure.Type: GrantFiled: June 5, 2000Date of Patent: June 5, 2001Assignee: United Therapeutics CorporationInventors: Robert Shorr, Martine Rothblatt, Michael D. Bentley, Xuan Zhao
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Patent number: 6235780Abstract: (wherein R1 is OH etc.; X is Cl, F; R2 is H, C1-8 alkyl, C2-8 alkenyl, C2-8 alkynyl which may be substituted; n is 0-4.), non-toxic salts thereof or cyclodextrin clathrates thereof can strongly bind on EP2 subtype receptor. Therefore, they are useful for the prevention and/or treatment of immunological diseases (autoimmune diseases, post-transplantation graft rejection etc.), asthma, abnormal bone formation, neuronal cell death, hepatopathy, abortion, premature birth or retina neuropathy (e.g. glaucoma) etc.Type: GrantFiled: July 19, 1999Date of Patent: May 22, 2001Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Shuichi Ohuchida, Kousuke Tani
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Patent number: 6235781Abstract: A pharmaceutical product comprising an aqueous prostaglandin formulation and a polypropylene container are disclosed. Aqueous prostaglandin formulations are more stable in polypropylene containers than polyethylene containers.Type: GrantFiled: January 20, 2000Date of Patent: May 22, 2001Assignee: Alcon Laboratories, Inc.Inventors: Alan L. Weiner, Subhash C. Airy, Cody Yarborough, Julia A. Clifford, William E. McCune
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Patent number: 6235779Abstract: Cis-&Dgr;4 analogs of prostaglandins and methods of their use in treating glaucoma and ocular hypertension are disclosed.Type: GrantFiled: June 2, 1999Date of Patent: May 22, 2001Assignee: Alcon Laboratories, Inc.Inventors: Peter G. Klimko, Paul W. Zinke
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Patent number: 6232343Abstract: An ophthalmic preparation which exhibits excellent pharmacological effects for various ophthalmic diseases is disclosed. The ophthalmic preparation according to the present invention contains a 4,8-inter-m-phenylene prostaglandin I2 derivative represented by the formula (I): or a pharmaceutically acceptable salt thereof as an effective ingredient.Type: GrantFiled: March 9, 1998Date of Patent: May 15, 2001Assignee: Toray Industries, Inc.Inventors: Takashi Ikari, Yuzuru Matsumura, Tsutomu Nakamura, Motoyuki Yajima, Hajimu Kurumatani, Ayako Kawashima, Masafumi Isogaya, Hisanori Wakita
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Patent number: 6232344Abstract: 13-Oxa analogs of certain prostaglandins and methods of their use in treating glaucoma and ocular hypertension are disclosed.Type: GrantFiled: May 21, 1999Date of Patent: May 15, 2001Assignee: Alcon Laboratories, Inc.Inventors: Zixia Feng, Mark R. Hellberg
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Patent number: 6225348Abstract: A method of treating age-related macular degeneration in an eye is described, comprising contacting the eye with a therapeutic amount of a prostaglandin F2&agr; derivative. The preferred prostaglandin F2&agr; derivative is latanoprost, and the preferred dosage is between about 1.5 &mgr;g and about 4.5 &mgr;g per day per eye.Type: GrantFiled: August 19, 1999Date of Patent: May 1, 2001Inventor: Alfred W. Paulsen
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Patent number: 6225347Abstract: The invention relates to 9-halogen-(Z) prostane derivatives of formula I in which Z represents the radicals Hal represents a chlorine or fluorine atom in the alpha or beta position, R1 represents the radical with R2 meaning a hydrogen atom, an alkyl, cycloalkyl, aryl or heterocyclic radical or R1 represents the radical with R3 meaning an acid radical or the radical R2 and A represents a —CH2—CH2—, a trans-CH═CH or —C≡C group, W represents a free or a functionally modified group, and the respective OH groups can be in the alpha or beta position, D and E together represent a direct bond or D represents a straight-chain alkylene group with 1-10 C atoms, a branched-chain alkylene group with 2-10 C atoms or an annular alkylene group with 3-10 C atoms, which optionally can be substituted by fluorine atoms, and E represents an oxygen or sulfur atom, a direct bond, a C≡C bond or aType: GrantFiled: September 27, 1994Date of Patent: May 1, 2001Assignee: Schering AktiengesellschaftInventors: Bernd Buchmann, Werner Skuballa, Helmut Vorbrueggen, Bernd Raduechel, Olaf Loge, Walter Elger, Claus-Steffen Stuerzebecher, Karl-Heinz Thierauch
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Patent number: 6214872Abstract: A compound of the formula wherein X, Y, R1 and R2 are as defined above, useful in the treatment of arthritis or cancer and other diseases involving selective inhibition of matrix metaloproteinase-13.Type: GrantFiled: August 26, 1999Date of Patent: April 10, 2001Assignee: Pfizer Inc.Inventor: Ralph Pelton Robinson
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Patent number: 6187813Abstract: The invention relates to ophthalmological compositions for topical treatment of glaucoma or ocular hypertension comprising an effective intraocular pressure reducing amount of a prostaglandin derivative of PGA, PGB, PGD, PGE or PGF, in which the omega chain contains a ring structure, in an ophthalmologically compatible carrier. The invention further relates to the preparation of said compositions and their use for treatment of glaucoma or ocular hypertension.Type: GrantFiled: May 10, 1999Date of Patent: February 13, 2001Assignee: Pharmacia & Upjohn AktiebolagInventors: Johan Wilhelm Stjernschantz, Bahram Resul
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Patent number: 6184250Abstract: Disclosed is the use of cloprostenol and fluprostenol analogues and combinations thereof with other medicaments for the treatment of glaucoma and ocular hypertension and ophthalmic compositions therefor. Also disclosed are methods of treating optic nerve disorders using the cloprostenol and fluprostenol analogues.Type: GrantFiled: March 30, 1999Date of Patent: February 6, 2001Assignee: Alcon Laboratories, Inc.Inventors: Peter G. Klimko, John E. Bishop, Verney L. Sallee, Paul W. Zinke, Tom R. Dean, George E. Barnes, Michael L. Chandler
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Patent number: 6177464Abstract: Methods for performing ring-opening cross-metathesis reactions on solid support are disclosed. Substituted cyclic compounds, libraries of the compounds, and methods of using the compounds to treat bacterial infections are also disclosed.Type: GrantFiled: March 14, 1997Date of Patent: January 23, 2001Assignee: Sepracor, Inc.Inventors: Gregory D. Cuny, Jingrong Cao, James R. Hauske
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Patent number: 6172109Abstract: 13-thia prostaglandins are useful in the treatment of glaucoma and ocular hypertension. Also disclosed are ophthalmic, pharmaceutical compositions comprising said prostaglandins.Type: GrantFiled: June 3, 1998Date of Patent: January 9, 2001Assignee: Alcon Laboratories, Inc.Inventors: Paul W. Zinke, Mark R. Hellberg
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Patent number: 6172110Abstract: Betulin and dihydrobetulin acyl derivatives according to the present invention have been found to have potent anti-HIV activity. The compounds of the present invention have the following formulae: or pharmaceutically acceptable salts thereof, wherein R1 is a C2-C20 substituted or unsubstituted carboxyacyl, R2 is a C2-C20 substituted or unsubstituted carboxyacyl; and R3 is hydrogen, halogen, amino, optionally substituted mono- or di-alkylamino, or —OR4, where R4 is hydrogen, C1-4 alkanoyl, benzoyl, or C2-C20 substituted or unsubstituted carboxyacyl; wherein the dashed line represents an optional double bond between C20 and C29.Type: GrantFiled: March 2, 1999Date of Patent: January 9, 2001Assignees: The University of North Carolina at Chapel Hill, BBI Biotech Research Laboratories, Inc.Inventors: Kuo-Hsiung Lee, I-Chen Sun, Hui-Kang Wang, Louis Mark Cosentino
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Patent number: 6169111Abstract: Conformationally rigid aryl prostaglandins are useful in the treatment of glaucoma and ocular hypertension. Also disclosed are ophthalmic pharmaceutical compositions comprising said prostaglandins.Type: GrantFiled: May 12, 1999Date of Patent: January 2, 2001Assignee: Alcon Laboratories, Inc.Inventors: Paul W. Zinke, John E. Bishop, Thomas R. Dean, Mark R. Hellberg
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Patent number: 6166073Abstract: Compositions containing DP-agonist and FP-agonists prostaglandin agonists and methods of their use in treating glaucoma or ocular hypertension are disclosed.Type: GrantFiled: August 2, 1999Date of Patent: December 26, 2000Assignee: Alcon Laboratories, Inc.Inventors: Thomas R. Dean, Mark Hellberg, Verney L. Sallee
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Patent number: 6160012Abstract: Leukotriene-B.sub.4 derivatives of general formula (I), in which R.sub.1 represents H, CF.sub.3, CH.sub.2 OH, and R.sub.2 represents H or an organic acid radical; R.sup.3 symbolizes H, C.sub.1 -C.sub.14 alkyl, C.sub.3 -C.sub.10 cycloalkyl, or a 5- to 6-membered aromatic heterocyclic ring with at least 1 heteroatom; R.sub.4 means hydrogen, C.sub.1 -C.sub.10 alkyl, C.sub.3 -C.sub.10 cycloalkyl; A symbolizes a trans, trans--CH.dbd.CH--CH.dbd.CH, a --CH.sub.2 CH.sub.2 --CH.dbd.CH-- or a tetramethylene group; B symbolizes a C.sub.1 -C.sub.10 -- straight-chain or branched-chain alkylene group or group (a) or (b); D can mean a direct bond, oxygen, sulfur, --C.tbd.C--, --CH.dbd.CR.sub.7, or together with B can also mean a direct bond; R.sub.5 and R.sub.6 are the same or different and represent H or C.sub.1 -C.sub.4 alkyl, or R.sub.6 represents H and R.sub.5 represents C.sub.1 -C.sub.15 alkanoyl or R.sub.8 represents SO.sub.2 ; R.sub.7 means H, C.sub.1 -C.sub.5 alkyl, chlorine, bromine; R.sub.Type: GrantFiled: March 27, 2000Date of Patent: December 12, 2000Assignee: Schering AktiengesellschaftInventors: Bernd Buchmann, Wolfgang Frohlich, Claudia Giesen, Hartwig Hennekes, Stefan Jaroch, Werner Skuballa
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Patent number: 6160013Abstract: 14-Aza analogs of PGF.sub.2.alpha., PGD.sub.2, and PGE.sub.2 and methods of their use in treating glaucoma and ocular hypertension are disclosed.Type: GrantFiled: November 30, 1999Date of Patent: December 12, 2000Assignee: Alcon Laboratories, Inc.Inventor: Robert D. Selliah
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Patent number: 6156785Abstract: There is disclosed a method for increasing retinal and optic nerve head oxygen tension by application of a composition comprising carbonic anhydrase inhibitors to the eye.Type: GrantFiled: January 19, 1999Date of Patent: December 5, 2000Assignee: Merck Sharp & Dohme B.V.Inventors: Einae Stefansson, Jens Dollerup, Kurt Bang
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Patent number: 6153650Abstract: Novel gamma aminobutyric acids of formula (I) are disclosed and are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, inflammation, and gastrointestinal damage. Processes for the preparation and intermediates useful in the preparation are also disclosed.Type: GrantFiled: March 1, 1999Date of Patent: November 28, 2000Assignee: Warner-Lambert CompanyInventors: Justin Stephen Bryans, David Christopher Horwell, Clare Octavia Kneen, Andrew John Thorpe, David Juergen Wustrow
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Patent number: 6150374Abstract: The invention relates to novel substituted cycloalkenes of the formula (I), ##STR1## to a plurality of processes for their preparation, and to novel intermediates and a plurality of processes for their preparation.Type: GrantFiled: September 29, 1997Date of Patent: November 21, 2000Assignee: Bayer AktiengesellschaftInventors: Herbert Gayer, Peter Gerdes, Ralf Tiemann, Stefan Dutzmann, Klaus Stenzel
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Patent number: 6133303Abstract: The present invention provides compounds of Formula (I). The present invention also provides a method of treating cancer and treating or preventing restenosis or atherosclerosis. Also provided by the present invention is a pharmaceutically acceptable composition containing a compound of Formula (I).Type: GrantFiled: August 2, 1999Date of Patent: October 17, 2000Assignee: Warner-Lambert CompanyInventors: Jack Bikker, Ellen Myra Dobrusin, Annette Marian Doherty, Matthew Drowns, James Stanley Kaltenbronn, Juergen Kleinschroth, Dennis Joseph McNamara, John Quin, III, Joseph Thomas Repine, Marcin Stasiak
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Patent number: 6133230Abstract: A pharmaceutical composition comprising a prostaglandin such as misoprostol and TGF-B in amounts sufficient to stimulate production of chondrocyte matrix is disclosed which exhibit therapeutic synergy.Type: GrantFiled: June 19, 1997Date of Patent: October 17, 2000Assignee: Queen's University at KingstonInventor: Tassos Anastassiades
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Patent number: 6127413Abstract: This invention relates to an agent for decreasing ocular tension comprising as an effective ingredient a 4,8-inter-m-phenylene PGI.sub.2 derivative represented by the formula: ##STR1## or a pharmaceutically acceptable salt thereof. The agent for decreasing ocular tension according to the present invention is useful as a therapeutic agent for treating various high ocular tension states such as glaucoma, ocular hypertension and high ocular tension which occurs after surgery.Type: GrantFiled: October 15, 1997Date of Patent: October 3, 2000Assignee: Toray Industries, Inc.Inventors: Hajimu Kurumatani, Ayako Kawashima, Masafumi Isogaya, Hisanori Wakita
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Patent number: 6124354Abstract: This invention relates to the use of 2-(diisopropylamino)-ethyl-1-phenyl-cyclopentane-carboxylate or 2-(diisopropylamino)-ethyl-1-phenyl-cyclohexane-carboxylate, or a pharmaceutically accceptable salt thereof, for treatment of urinary incontinence or irritable bowel syndrome (IBS).Type: GrantFiled: April 12, 1999Date of Patent: September 26, 2000Assignee: Pharmacia & Upjohn ABInventors: Eva .ANG.kerblom, Martin Haraldsson, Rolf Johansson, Katarina Beierlein, Birger Sjoberg, Erik Ringberg, Birgitta Weinz
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Patent number: 6124353Abstract: The present invention provides a method of treating ocular hypertension which comprises applying to the eye an amount sufficient to treat ocular hypertension of a compound of formula (I) ##STR1## wherein the wavy line attachments indicate either alpha (.alpha.) or beta (.beta.) configuration; hatched lines indicate .alpha. configuration, solid triangles are used to indicate .beta. configuration; the dashed bonds represent a single bond or a double bond which can be in the cis or trans configuration; X is selected from the group consisting of H, R or a pharmaceutically-acceptable cation, and R is an aliphatic hydrocarbon group of about 1 to about 6 carbon atoms; one of R.sub.1 and R.sub.2 is .dbd.O, --OH or an --O(CO)R.sub.4 group, and the other one is --OH or an --O(CO)R.sub.4 group or R.sub.1 is .dbd.O and R.sub.2 is H; R.sub.3 is --OH or --O(CO)R.sub.4, wherein R.sub.4 is a saturated or unsaturated acyclic hydrocarbon group having from 1 to about 20 carbon atoms, or --(CH.sub.2).sub.n R.sub.Type: GrantFiled: November 12, 1992Date of Patent: September 26, 2000Assignee: Allergan Sales, Inc.Inventor: David F. Woodward
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Patent number: 6121268Abstract: Compounds with fungicidal properties having formula I ##STR1## where m and n are 0 or 1 provided that m+n is 1; X is hydrogen, halo, (C.sub.1 -C.sub.4)alkyl, or (C.sub.1 -C.sub.4)alkoxy; R is an optionally-substituted alkyl, cycloalkyl, alkenyl, alkynyl, alkoxy, aryl, aralkyl, or heterocyclic group; R.sub.1 and R.sub.2 are hydrogen, optionally-substituted alkyl, cycloalkyl, cyano, carboxy alkyl, or aryl; at least one of R.sub.1 and R.sub.2 is hydrogen; and R.sub.3 is alkyl or haloalkyl.Type: GrantFiled: November 23, 1998Date of Patent: September 19, 2000Assignee: Rohm and Haas CompanyInventors: Ronald Ross, Ted Tsutomo Fujimoto, Edward Michael Szapacs, Steven Howard Shaber
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Patent number: 6121317Abstract: Compounds of formula (1), (Gibberellins), and their pharmaceutically acceptable derivatives to promote ulcer-healing, healing of surgical wounds or open fractures and treatment of bronchitis or thrombophlebitis in animals including humans or cultivation of skin cell lines in vitro ##STR1## wherein A is COOR, where R is hydrogen, unsubstituted or substituted C.sub.1-20 alkyl, allyl, aryl, arylalkyl, amidine, NR.sup.4 R.sup.5 or an unsaturated or saturated ring containing one or more hetero-atoms selected from the group consisting of nitrogen, oxygen and sulfur; R.sup.4 and R.sup.5 may or may not be the same, are hydrogen, or C.sub.1-20 alkyl, allyl, aryl, arylalkyl or an unsaturated or saturated ring containing one or more hetero-atoms selected from the group consisting of nitrogen and sulfur; B is hydrogen, hydroxyl, mercaptan, or halogen, or A and B together form a --CO--O-- linkage; R.sup.1 is hydrogen, hydroxyl, mercaptan, halogen, amino, azido, NR.sup.4 R.sup.5, unsubstituted or substituted C.sub.Type: GrantFiled: November 9, 1998Date of Patent: September 19, 2000Assignee: Australian Biomedical Company Pty. Ltd.Inventors: Minne Wu, David Shine Wu
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Patent number: 6114364Abstract: The present invention relates to a compound represented by the following general formula (1) ##STR1## (wherein X represents O, S, SO, SO.sub.2, or NH, Y is a substituted or unsubstituted hydrocarbon residue containing 1 through 6 carbon atoms and having an overall molecular weight of not less than 15 and not more than 400, and the hydrocarbon residue, when the residue is ring, may contain one or two hetero-atoms in the ring, and Z is a carboxyl group, a group derived therefrom or an aliphatic hydrocarbon residue having from 1 to 4 carbon atoms which may be substituted or unsabstituted) or a pharmacologically acceptable salt thereof (excluding (1R,2S)-2-[(2R)-(2-acetyl-amino-2-carboxyethyl)thiomethyl]-3-oxo-1-cyclope ntane-carboxylic acid (cystacyclin)), a method for production thereof and a medicinal use thereof. The compound of the present invention is useful as a neuron differentiation accelerator.Type: GrantFiled: October 5, 1998Date of Patent: September 5, 2000Assignee: Nippon Kayaku Co., Ltd.Inventors: Seiichi Saito, Tomio Morino, Kuniko Masuda
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Patent number: 6110969Abstract: A .omega.-cycloalkyl-prostaglandin E.sub.2 derivatives of the formula (I) ##STR1## wherein R is carboxy or hydroxymethyl; R.sup.1 is oxo, methylene or halogen atom; R.sup.2 is H, OH or C1-4 alkoxy; R.sup.3 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 EP.sub.2 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.Type: GrantFiled: February 4, 1998Date of Patent: August 29, 2000Assignee: Ono Pharmaceutical Co. Ltd.Inventors: Kousuke Tani, Shuichi Ohuchida
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Patent number: 6107337Abstract: A compound of the formula ##STR1## wherein n, X, R.sup.3, R.sup.4 and Ar are as defined above, useful in the treatment of a condition selected from the group consisting of arthritis, cancer, tissue ulceration, restenosis, periodontal disease, epidermolysis bullosa, scleritis, bone resorption, loosening of artificial joint implants, atherosclerosis, multiple sclerosis, occular angiogenisis and other diseases characterized by matrix metalloproteinase activity, AIDS, sepsis, septic shock and other diseases involving the production of TNF.Type: GrantFiled: August 6, 1998Date of Patent: August 22, 2000Assignee: Pfizer Inc.Inventor: Ralph P. Robinson
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Patent number: 6107338Abstract: The invention provides novel PGF analogs. In particular, the present invention relates to compounds having a structure according to the following formula: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, X, Y, and Z are defined below. This invention also includes optical isomers, diastereomers and enantiomers of the formula above, and pharmaceutically-acceptable salts, biohydrolyzable amides, esters, and imides thereof.The compounds of the present invention are useful for the treatment of a variety of diseases and conditions, such as bone disorders and glaucoma. Accordingly, the invention further provides pharmaceutical compositions comprising these compounds. The invention still further provides methods of treatment for bone disorders and glaucoma using theses compounds or the compositions containing them.Type: GrantFiled: September 4, 1998Date of Patent: August 22, 2000Assignee: The Procter & Gamble CompanyInventors: John August Wos, Mitchell Anthony deLong, Jack S. Amburgey, Jr., Haiyan George Dai, Cynthia Jean Miley, Biswanath De
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Patent number: 6096783Abstract: Cyclobutane analogs of PGF.sub.2.alpha., PGD.sub.2, and PGE.sub.2 and methods of their use in treating glaucoma and ocular hypertension are disclosed.Type: GrantFiled: December 15, 1998Date of Patent: August 1, 2000Assignee: Alcon Laboratories, Inc.Inventor: Mark R. Hellberg
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Patent number: 6090847Abstract: The invention relates to the use of EP.sub.2 receptor agonists as neuroprotective agents. In particular said compounds are represented by the formulae: ##STR1## wherein the broken line attachment to the cyclopentane ring or the omega chain indicates the .alpha. configuration and the solid line attachment to the cyclopentane ring or the omega chain indicates the .beta. configuration, R is hydrogen or a saturated or unsaturated acyclic hydrocarbon group having from 1 to about 20 carbon atoms, or --(CH.sub.2).sub.m R.sub.1 wherein m is 0-10, and R.sub.1 is an aliphatic ring having from about 3 to about 7 carbon atoms, or an aryl or heteroaryl ring having from about 4 to about 10 carbon atoms and wherein the heteroatom is selected from the group consisting of N, O and S.Type: GrantFiled: November 3, 1998Date of Patent: July 18, 2000Assignee: Allergan Sales, Inc.Inventor: David F. Woodward
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Patent number: 6087395Abstract: The present invention provides an apoptosis inhibitor containing a 15R-isocarbacyclin derivative or a 15-deoxy-isocarbacyclin derivative, which can be manufactured easily and economically by means of chemical synthesis.Type: GrantFiled: October 16, 1998Date of Patent: July 11, 2000Assignees: Japan Science and Technology Corporation, Atsuo HazatoInventors: Yasuyoshi Watanabe, Atsuo Hazato, Masaaki Suzuki, Yumiko Watanabe, Takumi Sato
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Patent number: 6080785Abstract: The invention relates to new monofunctionalized ethylenediaminetetraacetic acid, diethylenetriaminepentaacetic acid and triethylenetetraaminehexaacetic acid derivatives, their production and their use for the production of pharmaceutical agents.Type: GrantFiled: June 29, 1998Date of Patent: June 27, 2000Assignee: Schering AktiengesellschaftInventors: Johannes Platzek, Peter Mareski, Ulrich Niedballa, Bernd Raduchel