Cyclopentyl In Acid Moiety (e.g., Prostaglandins, Etc.) Patents (Class 560/121)
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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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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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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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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: 6642274Abstract: The present invention relates to methods, compositions, devices and kits for the prevention and treatment of prostate disorders in mammals, including, but not limited to, benign prostatic hypertrophy, carcinoma of the prostate, prostadynia, prostatitis, and chronic prostatitis. The present invention provides methods for preventing and treating prostate disorders in mammals by administration of a therapeutic compound to mucosal membranes in the lower urinary tract of the mammal. The present invention also provides devices for administering a therapeutic compound to mucosal membranes in the lower urinary tract of the mammal.Type: GrantFiled: September 8, 2000Date of Patent: November 4, 2003Inventor: Gary W. Neal
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Patent number: 6632958Abstract: An alkene (1) is added to cyclopentenone (2) under the action of an alkyl lithium and an organic copper reagent to form an adduct, said adduct is reacted with e.g.Type: GrantFiled: December 4, 2000Date of Patent: October 14, 2003Assignee: Mitsubishi Pharma CorporationInventors: Masahiro Urushihara, Yoshitomi Morizawa
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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: 6576786Abstract: The invention relates to a process for preparing substituted cyclopentane derivatives represented by the formula (I) wherein R1, R2, R3, R4, X and Y are as described in the specification, and pharmaceutically acceptable salts thereof. The invention further relates to a process for purifying the compound of formula (Ia) and novel crystalline forms of the compound of formula (Ia).Type: GrantFiled: November 26, 2001Date of Patent: June 10, 2003Assignee: Biocryst Pharmaceuticals Inc.Inventors: Ahmed F. Abdel-Magid, Hans-Ulrich Bichsel, Daniel J. Korey, Gunther G. Laufer, Erja A. Lehto, Sebastiano Mattei, Max Rey, Thomas W. Schultz, Cynthia Maryanoff
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Publication number: 20030100791Abstract: Acrylic esters containing fluorine at &agr;-position and having an alkoxymethyl group introduced into the ester side chain thereof are novel. Polymers obtained from the acrylic esters are improved in transparency, acid elimination and substrate adhesion and are used to formulate chemically amplified resist compositions for lithographic microfabrication.Type: ApplicationFiled: November 27, 2002Publication date: May 29, 2003Inventors: Yuji Harada, Jun Hatakeyama, Yoshio Kawai, Masaru Sasago, Masayuki Endo, Shinji Kishimura, Kazuhiko Maeda, Michitaka Ootani, Haruhiko Komoriya
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Patent number: 6541655Abstract: Complexes of a selected class of chiral ligands with molybdenum, tungsten or chromium, preferably molybdenum, are effective as catalysts in highly enantioselective and regioselective alkylation of allylic substrates.Type: GrantFiled: September 7, 2001Date of Patent: April 1, 2003Assignee: The Board of Trustees of the Leland Stanford Junior UniversityInventors: Barry M. Trost, Iwao Hachiya
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Patent number: 6531485Abstract: This invention relates to prostaglandin agonists, methods of using such prostaglandin agonists, pharmaceutical compositions containing such prostaglandin agonists and kits containing such prostaglandin agonists. The prostaglandin agonists are useful for the treatment of bone disorders including osteoporosis.Type: GrantFiled: December 16, 1999Date of Patent: March 11, 2003Assignee: Pfizer Inc.Inventors: Kimberly O. Cameron, Paul A. DaSilva-Jardine
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Patent number: 6528688Abstract: An improved method is described for making 9-deoxy-PGF1-type compounds. In contrast to the prior art, the method is stereoselective and requires fewer steps than the known methods for making these compounds.Type: GrantFiled: February 15, 2002Date of Patent: March 4, 2003Assignee: United Therapeutics CorporationInventors: Robert M. Moriarty, Raju Penmasta, Liang Guo, Munagala S. Rao, James P. Staszewski
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Publication number: 20030027853Abstract: 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; 1Type: ApplicationFiled: June 14, 2001Publication date: February 6, 2003Applicant: Allergan Sales, Inc.Inventors: Robert M. Burk, Mark Holoboski, Mari F. Posner
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Patent number: 6512139Abstract: The invention relates to the use of an oxidation inhibitor, i.e. active carbon, for ambient air in industrial manufacturing, especially in the processing of prostane derivatives, whereby the oxidation inhibitor removes ozone from the process air before contact with said prostane derivatives. The concentration of decomposition products is reduced.Type: GrantFiled: March 7, 2001Date of Patent: January 28, 2003Assignee: Schering AktiengesellschaftInventors: Torsten Wagner, Martin Wessel, Ralph Lipp, Bernd Iffert, Heinrich Michel, Jürgen Westermann, Helmut Dahl, Werner Skuballa
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Publication number: 20030008895Abstract: This invention relates to prostaglandin agonists, methods of using such prostaglandin agonists, pharmaceutical compositions containing such prostaglandin agonists and kits containing such prostaglandin agonists. The prostaglandin agonists are useful for the treatment of bone disorders including osteoporosis.Type: ApplicationFiled: December 16, 1999Publication date: January 9, 2003Inventors: KIMBERLY O CAMERON, PAUL A. DASILVA-JARDINE
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Patent number: 6495725Abstract: The present invention provides a simplified and convenient process for the preparation of an optically active enone such as 7,7-dimethyl-6,8-dioxabicyclo-[3,3,0]oct-3-en-2-one. The invention further provides novel optically active intermediate compounds.Type: GrantFiled: December 15, 2000Date of Patent: December 17, 2002Assignee: Chisso CorporationInventor: Kunio Ogasawara
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Publication number: 20020161045Abstract: Novel acetyloxymethyl esters are disclosed. Methods of treating an illness, including cancer, hemological disorders and inherited metabolic disorders, and treating or ameliorating other conditions using these compounds are also disclosed. The compounds are effective in the inhibition of histone deacetylase.Type: ApplicationFiled: December 21, 2000Publication date: October 31, 2002Inventors: Hsuan-Yin Lan-Hargest, Norbert L. Wiech
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Publication number: 20020143205Abstract: This invention encompasses a process for making a compound of Formula A 1Type: ApplicationFiled: January 17, 2002Publication date: October 3, 2002Inventors: Cheng Yi Chen, Weirong Chen, Paul O'Shea, Lushi Tan, Richard Tillyer, Feng Xu, Philippe Dagneau
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Publication number: 20020137793Abstract: The invention relates to compositions and methods for the treatment of dry eye and related diseases utilizing 6-keto-PGF1&agr; and its analogs, according to formula (I); wherein A,B,D,Q9, Q11, R1, X and Y have the meanings given in the description. Some of these compounds are novel.Type: ApplicationFiled: March 23, 2001Publication date: September 26, 2002Inventor: Peter G. Klimko
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Patent number: 6455584Abstract: To provide a prostaglandin derivative represented by the formula: wherein A is an ethylene group, a vinylene group, an ethynylene group, O(CH2)q or S(O)r(CH2)q, R1 is a C3-10 cycloalkyl group, a C1-4 alkyl-C3-10 cycloalkyl group, a C3-10 cycloalkyl-C1-4 alkyl group, a C1-10 alkyl group, a C1-10 alkyl group substituted with hydroxyl group(s) or C1-4 alkoxy group(s), a C2-10 alkenyl group, a C2-10 alkenyl group substituted with hydroxyl group(s) or C1-4 alkoxy group(s), a C2-10 alkynyl group, a C2-10 alkynyl group substituted with hydroxyl group(s) or C1-4 alkoxy group(s) or a bridged cyclic hydrocarbon group, R2 is a hydrogen atom, a C1-10 alkyl group or a C3-10 cycloalkyl group, m is an integer of 1 to 5, n is an integer of 1 to 4, p is 0, 1 or 2, q is an integer of 1 to 5 and r is 0, 1 or 2; a pharmaceutically acceptable salt thereof or a hydrate thereof exhibit excellent action in inhibiting the growth of vascular smooth muscle and is useful as a drug for inhibition of restenosis after perType: GrantFiled: January 4, 2002Date of Patent: September 24, 2002Assignees: Taisho Pharmaceutical Co., Ltd.Inventors: Fumie Sato, Tohru Tanami, Hideo Tanaka, Naoya Ono, Makoto Yagi, Hitomi Hirano
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Patent number: 6452039Abstract: 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: December 30, 1999Date of Patent: September 17, 2002Inventor: Ryuji Ueno
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Patent number: 6444840Abstract: The invention provides novel prostaglandin analogs. In particular, the present invention relates to compounds having a structure according to formula (I) wherein R1, R2, R3, R4, R5, R6, W, X, Z, a, b, p and q are defined below. This invention also includes optical isomers, diastereomers and enantiomers of formula (I), 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 these compounds or the compositions containing them.Type: GrantFiled: September 28, 2000Date of Patent: September 3, 2002Assignee: The Procter & Gamble Co.Inventors: Mitchell Anthony deLong, Jack Snyder Amburgey, Jr., John August Wos, Biswanath De, David Lindsey Soper
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Patent number: 6441245Abstract: An improved method is described for making 9-deoxy-PGF1-type compounds. In contrast to the prior art, the method is stereoselective and requires fewer steps than the known methods for making these compounds.Type: GrantFiled: April 3, 2000Date of Patent: August 27, 2002Assignee: United Therapeutics CorporationInventors: Robert M. Moriarty, Raju Penmasta, Liang Guo, Munagala S. Rao, James P. Staszewski
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Publication number: 20020111499Abstract: An enantiomerically enriched compound of formula 1, 1Type: ApplicationFiled: July 3, 2001Publication date: August 15, 2002Inventors: Philip Mark Jackson, Ian Campbell Lennon
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Patent number: 6410591Abstract: The present invention provides a method of treating ocular hypertension or glaucoma which comprises administering to an animal having ocular hypertension or glaucoma a therapeutically effective amount of a 3, 7 or 3 and 7 thia or oxa prostanoic acid derivative.Type: GrantFiled: May 8, 2001Date of Patent: June 25, 2002Assignee: Allergan Sales, Inc.Inventors: Robert M. Burk, Mark Holoboski, Mari F. Posner
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Patent number: 6410780Abstract: The invention provides novel prostaglandin analogs. In particular, the present invention relates to compounds having a structure according to formula (I) wherein R1, R2, R3, R4, R5, R6, W, X, Z, a, b, p and q are defined below. This invention also includes optical isomers, diastereomers and enantiomers of formula (I), 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 these compounds or the compositions containing them.Type: GrantFiled: September 28, 2000Date of Patent: June 25, 2002Assignee: The Procter & Gamble Co.Inventors: Mitchell Anthony deLong, Jack Snyder Amburgey, Jr., John August Wos, Biswanath De, David Lindsey Soper
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Patent number: 6395786Abstract: A sleep-inducing preparation which comprises as an effective ingredient a prostaglandin derivative represented by the formula: wherein X is a halogen atom, Y is a group represented by (CH2)m, a cis-vinylene group or a phenylene group, Z is an ethylene group, a trans-vinylene group, OCH2 or S(O)nCH2, R1 is a C3-10 cycloalkyl group, a C3-10 cycloalkyl group substituted with C1-4 alkyl group(s), a C4-13 cycloalkylalkyl 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, m is an integer of 1 to 3, and n is 0, 1 or 2, a pharmaceutically acceptable salt thereof or a hydrate thereof.Type: GrantFiled: November 27, 2000Date of Patent: May 28, 2002Assignees: Taisho Pharmaceutical Co., Ltd.Inventors: Fumie Sato, Tohru Tanami, Kazuya Kameo, Kenji Yamada, Shigeru Okuyama, Naoya Ono
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Publication number: 20020061930Abstract: The invention relates to a process for preparing substituted cyclopentane derivatives represented by the 1Type: ApplicationFiled: November 26, 2001Publication date: May 23, 2002Inventors: Ahmed F. Abdel-Magid, Hans-Ulrich Bichsel, Daniel J. Korey, Gunther G. Laufer, Erja A. Lehto, Sebastiano Mattei, Max Rey, Thomas W. Schultz, Cynthia Maryanoff
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Patent number: 6376699Abstract: Hydroazinecarboxylic acid ester of the formula In which R1 is an optionally substituted alkyl group, an aryl group, an arylalkyl group or a cycloalkyl group, and R3 is an optionally substituted alkyl group.Type: GrantFiled: January 26, 2001Date of Patent: April 23, 2002Assignee: Lonza AGInventor: Ulrich Veith
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Patent number: 6369194Abstract: The invention relates to compounds of formula where R is a structural diversity element selected from the group consisting of alkyl, cycloalkyl, aryl, heteroaryl, peptidyl, heteroatom-substituted alkyl, cycloalkyl, and amines; and Nu is a structural diversity element derived from a nucleophile, NuH, selected from the group consisting of amines, amino acids, peptide, water, hydrogen sulfide, alcohols, and thiols. The invention also relates to arrays and combinatorial libraries of such compounds, and to a method of preparing such compounds.Type: GrantFiled: November 9, 1998Date of Patent: April 9, 2002Assignee: Yale UniversityInventor: Harry H. Wasserman
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Patent number: 6326369Abstract: A compound of the formula: wherein R1 and R2 each represents a lower alkyl, or R1 and R2 may be bonded together to form a ring; X represents a spacer of which the number of atoms constituting the principal chain is 1 to 15; Y represents an acyl, or a hydroxy, an amino or an aromatic group, each of which may be substituted; and ring A represents a 5- to 8-membered ring which may be further substituted apart from —X—Y, or a salt thereof is useful as a pharmaceutical composition for preventing or treating disease related to mitochondrial dysfunction.Type: GrantFiled: July 6, 1999Date of Patent: December 4, 2001Assignee: Takeda Chemicals Industries, Ltd.Inventors: Kaneyoshi Kato, Taiichi Ohra, Masaomi Miyamoto
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Patent number: 6313341Abstract: A hydroxy-1-alkyne is reacted with a tin hydride compound, and the obtained (E,Z)-hydroxyvinylstannanes are separated to give the (E)-substance which is further converted to a vinylcopper complex shown by followed by the conjugate addition reaction with an &agr;, &bgr;-unsaturated cyclopentenone, and the deprotecting reaction is subsequently carried out to prepare a prostaglandin or an intermediate of prostaglandins easily, efficiently and industrially favorably.Type: GrantFiled: May 14, 1999Date of Patent: November 6, 2001Assignee: Fuji Yakuhin Kogyo Kabushiki KaishaInventors: Noriaki Murata, Atsunori Aramata, Tadashi Takeuchi
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Patent number: 6307092Abstract: The present invention provides a novel compound represented by the general formula I: wherein R is H or COR3; R1 is H, R2, phenyl, or COR3, wherein R2 is C1-C5 lower alkyl and R3 is R2 or phenyl; Z is CH2 or O; Y is OH, OCOR3 or ═O; x is 0 or 1; and X is C1-C5 n-alkyl, C3-C7 cycloalkyl, phenyl, furanyl, thienyl or substituted derivatives thereof, wherein the substituents maybe selected from the group consisting of C1-C5 alkyl, halogen, CF3, CN, NO2, NR42, CO2R4 and OR4 wherein R4 is hydrogen or C1-C5 alkyl and dotted lines represent the presence or absence of a double bond and wavy lines represent a cis or trans bond. These novel compounds are especially useful for treating elevated intraocular pressure (ocular hypertension) and glaucoma.Type: GrantFiled: May 8, 2001Date of Patent: October 23, 2001Assignee: Allergan Sales, Inc.Inventors: Robert M. Burk, Mark Holoboski, Mari F. Posner
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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: 6271408Abstract: This invention relates to trimethylsilyloxy-cyclopentane derivatives: 3-(1-Acetoxy-1-methylethyl)- 2-formyl-1-methyl-1-trimethylsilyloxy-cyclopentane; 4-[5-(1-Hydroxy-1-methylethyl)-2-methyl-2-trimethylsilyloxy-cyclopentyl]-3-buten-2-one; 5-[5-(1-Hydroxy-1-methylethyl)-2-methyl-2-trimethylsilyloxy-cyclopentyl]-3-methyl-penta-1,4-dien-3-ol and alkyl 5-[5-(1-Hydroxy-1-methylethyl)-2-methyl-2-trimethylsilyloxy-cyclopentyl]-3-methyl-penta-2,4-dienoates.Type: GrantFiled: September 13, 2000Date of Patent: August 7, 2001Assignee: Roche Vitamins Inc.Inventors: Hanspeter Pfander, Bruno Traber
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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: 6258975Abstract: Provided is an industrially useful process for producing an optically active 2-hydroxy-4-arylbutyric acid or its ester. An optically active acyloxysuccinic anhydride is reacted with an aromatic compound in the presence of a Lewis acid to produce an optically active 2-acyloxy-4-oxo-4-arylbutyric acid. The 2-acyloxy-4-oxo-4-arylbutyric acid is converted to an optically active 2-acyloxy-4-arylbutyric acid through catalytic reduction. The 2-acyloxy-4-arylbutyric acid is hydrolyzed in the presence of an acid or an alkali to produce an optically active 2-hydroxy-4-arylbutyric acid. The 2-hydroxy-4-arylbutyric acid is reacted with an alcohol in the presence of an acid to produce an optically active 2-hydroxy-4-arylbutyric acid ester.Type: GrantFiled: January 5, 2000Date of Patent: July 10, 2001Assignee: Ajinomoto Co., Inc.Inventors: Masahiko Kurauchi, Yoshimasa Hagiwara, Hiroyuki Matsueda, Takashi Nakano, Kunisuke Izawa
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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: 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: 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: 6197995Abstract: The present invention is concerned with a process for the manufacture of chiral succinic acid derivatives of formula (I) wherein R1 is (C1-C6) alkyl or benzyl, and the novel intermediates used therein.Type: GrantFiled: June 16, 1999Date of Patent: March 6, 2001Assignee: Hoffman-La Roche Inc.Inventor: Hans Hilpert
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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: 6156799Abstract: The present invention relates to novel methods of increasing bone volume comprising the administration of a non-naturally-occurring selective FP agonist to a subject in need of such treatment. This invention further relates to a method of treating or preventing bone disorders comprising the administration of a non-naturally-occurring selective FP agonist to a subject in need of such treatment.Type: GrantFiled: September 4, 1998Date of Patent: December 5, 2000Assignee: The Procter & Gamble CompanyInventors: James Richard Hartke, Mark Walden Lundy, Mitchell Anthony deLong
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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: 6147254Abstract: A process for the preparation of carbocyclic stereoisomers of formulae (I), (I'), (IIA'), (IIB'), (VA') and (VB'), including enantiomerically pure (IIA'), (I) and (I') utilizing fractional crystallization of salts formed with a chiral base; a reducing agent; a protecting group removing agent or a protecting group providing agent.Type: GrantFiled: August 6, 1999Date of Patent: November 14, 2000Assignee: Glaxo Wellcome Inc.Inventors: Barry Riddle Sickles, Kenneth James Ingold, Christopher John Wallis
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Patent number: 6118019Abstract: A 3-alkoxypropionic ester derivative, an olefin polymerization solid catalyst component using the same, an olefin polymerization catalyst using the same, and a process for the preparation of a polyolefin using the same. The 3-alkoxypropionic ester derivative is represented by formula (I): ##STR1## wherein R.sup.1 represents a hydrocarbon group having from 1 to 10 carbon atoms; R.sup.2 represents a hydrocarbon group having from 1 to 20 carbon atoms; R.sup.3 represents a hydrocarbon group having from 1 to 20 carbon atoms; and R.sup.4 represents a branched hydrocarbon group having 3 or more carbon atoms.Type: GrantFiled: December 29, 1998Date of Patent: September 12, 2000Assignee: Showa Denko K.K.Inventors: Masaki Fushimi, Shintaro Inazawa
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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: 6100424Abstract: Aminoacetic acid esters of formula I in which R.sup.1, R.sup.2 and R.sup.3 are identical or different hydrocarbon radicals, or any two of these radicals form a carbon ring with the carbon atom to which they are attached and R.sup.4 is hydrogen or an alkyl radical having 1-4 carbon atoms, are prepared by reacting an .alpha.-substituted malonic acid monoamide ester of formula II ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 have the meanings above, by the Hofmann degradation reaction, with a hypohalite in an amount of up to 1.5 equivalents in an aqueous-basic medium containing base in an amount of 0.8-1.5 equivalents per mol. of starting malonic acid monoamide ester II.Type: GrantFiled: July 9, 1999Date of Patent: August 8, 2000Assignee: Degussa-Huels AktiengesellschaftInventor: Wolfgang Kleemiss
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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