Polycyclo Ring System Having The Hetero Ring As One Of The Cyclos Patents (Class 549/220)
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Patent number: 6270695Abstract: Novel heterocyclic compounds which generate chemiluminescence on reaction with a phosphatase enzyme are provided as well as a process for their preparation and intermediates useful therein. The compounds comprise a nitrogen, oxygen or sulfur-containing heterocyclic ring system bearing an exocyclic carbon-carbon double bond. The double bond is further substituted at the distal carbon with a phosphate group and an oxygen or sulfur atom-containing group. Novel compositions further comprising a cationic aromatic compound (CAC) in addition to the heterocyclic phosphate compound are provided. The addition of the CAC in the composition greatly increases the production of chemiluminescence and provides improved detection sensitivity. Compositions further comprising an anionic surfactant and a non-ionic surfactant provide additional improvements in detection sensitivity.Type: GrantFiled: July 21, 1999Date of Patent: August 7, 2001Assignee: Lumigen, Inc.Inventors: Hashem Akhavan-Tafti, Zahra Arghavani, Renuka DeSilva
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Patent number: 6211167Abstract: The invention provides compounds, compositions and methods relating to novel arylsulfonanilide derivatives and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly cancer, psoriasis, vascular restenosis, infrections, atherosclerosis and hypercholesterolemia, or as lead compounds for the development of such agents.Type: GrantFiled: June 14, 2000Date of Patent: April 3, 2001Assignee: Tularik Inc.Inventor: Jonathan B. Houze
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Patent number: 6162929Abstract: A process for the manufacture of bisphosphine oxide compounds and bisphosphonates as intermediates for the production of bisphosphine ligands, in which in a single step processa) a phosphine oxide compound is reacted in an organic solvent at -70.degree. C. to 20.degree. C. with 0.5-3 eq. of a lithium or magnesium amide compound,b) 0.5-3 eq. of oxidatively-acting metal salt or metal salt complex are added to the suspension obtained in stage a) in a temperature range of -70.degree. C. to 20.degree. C., with a racemate of a bisphosphine oxide compound being obtained;c) a racemate cleavage is carried out if desired; andd) the bisphosphonates obtained in stage b) or c) are converted into bisphosphine oxides.Type: GrantFiled: December 15, 1998Date of Patent: December 19, 2000Assignee: Hoffmann-La Roche Inc.Inventors: Joseph Foricher, Rudolf Schmid
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Patent number: 6110962Abstract: This invention provides compounds of Formula I having the structure ##STR1## wherein A is hydrogen, halogen, or OH;B and D are each, independently, hydrogen, halogen, CN, alkyl of 1-6 carbon atoms, aryl, aralkyl of 6-12 carbon atoms, nitro, amino or OR;R is hydrogen, alkyl of 1-6 carbon atoms, --COR.sup.1, --CH.sub.2 CO.sub.2 R.sup.1, --CH(R.sup.1a)CO.sub.2 R.sup.1, or --SO.sub.2 R.sup.1 ;R.sup.1 and R.sup.1a are each, independently, hydrogen, alkyl of 1-6 carbon atoms, aralkyl of 6-12 carbon atoms or aryl;E is S, SO, SO.sub.2, O;X is hydrogen, halogen, alkyl of 1-6 carbon atoms, CN, perfluoroalkyl of 1-6 carbon atoms, alkoxy of 1-6 carbon atoms, aryloxy, arylalkoxy of 6-12 carbon atoms, nitro, amino, alkylsulfanyl of 1-6 carbon atoms, arylsulfanyl, pyridylsulfanyl, 2-N,N-dimethylaminoethylsulfanyl, or --OCH.sub.2 CO.sub.2 R.sup.1b ;R.sup.1b is hydrogen or alkyl of 1-6 carbon atoms;Y and Z are each, independently, hydrogen or OR.sup.2 ;R.sup.Type: GrantFiled: May 10, 1999Date of Patent: August 29, 2000Assignee: American Home Products CorporationInventors: Jay E. Wrobel, Arlene J. Dietrich, Zenan Li
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Patent number: 6090951Abstract: Novel methods for the preparation of sidechain-bearing taxanes, comprising the preparation of an oxazoline compound, coupling the oxazoline compound with a taxane having a hydroxyl group directly bonded at C-13 thereof to form an oxazoline sidechain-bearing taxane, and opening the oxazoline ring of the oxazoline sidechain-bearing taxane so formed. Novel compounds prepared by the methods of the present invention are also provided.Type: GrantFiled: August 25, 1997Date of Patent: July 18, 2000Inventors: Michael A. Poss, Jerome L. Moniot, Ivan D. Trifunovich, David J. Kucera, John K. Thottahil, Shu-Hui Chen, Jianmei Wei
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Patent number: 6087347Abstract: Estratriene derivatives of the following formula have a powerful inhibitory effect on estrone sulfatase and are hence useful for the prophylaxis or treatment of diseases caused by estrogens, such as breast cancer, uterine cancer, ovarian cancer, endometriosis, adenomyosis uteri and mastopathy. ##STR1## wherein one of A and B represents C.dbd.O or CH.sub.2 and the other represents O or NH; and R represents --SO.sub.2 NR.sup.1 R.sup.2 or --PO(OM).sub.2 in which R.sup.1 and R.sup.2 each independently represent a hydrogen atom or a lower alkyl group and M represents a hydrogen atom or an alkali metal; provided that, when one of A and B represents NH, the other represents C.dbd.O.Type: GrantFiled: March 12, 1999Date of Patent: July 11, 2000Assignee: Teikoku Hormone Mfg. Co., Ltd.Inventors: Naoyuki Koizumi, Shigehiro Takegawa, Shigeki Iwashita, Tomoko Kawachi, Mamoru Mieda, Tomohito Fujii
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Patent number: 6001659Abstract: Chemiluminescent electron-rich aryl-substituted 1,2-dioxetane compounds are disclosed in which the aryl group is poly-substituted with suitable electron-donating groups such that the light-emitting pattern of the molecule results in a very high luminescent count, thus providing for a sensitive and precise assay for haptens, analytes, polynucleotides and the like. These substituted aryl-containing 1,2-dioxetane compounds can be used as direct labels in an immunoassay or when derivatized with an appropriate leaving group, can be used as a substrate for a enzyme immunoassay. The unusual chemiluminescence of the compounds allows the timing of the luminescent reaction to be exactly controlled.Type: GrantFiled: May 9, 1995Date of Patent: December 14, 1999Assignee: Abbott LaboratoriesInventors: Nai-Yi Wang, Roger C. Hu
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Patent number: 6001561Abstract: Chemiluminescent electron-rich aryl-substituted 1,2-dioxetane compounds are disclosed in which the aryl group is poly-substituted with suitable electron-donating groups such that the light-emitting pattern of the molecule results in a very high luminescent count, thus providing for a sensitive and precise assay for haptens, analytes, polynucleotides and the like. These substituted aryl-containing 1,2-dioxetane compounds can be used as direct labels in an immunoassay or when derivatized with an appropriate leaving group, can be used as a substrate for a enzyme immunoassay. The unusual chemiluminescence of the compounds allows the timing of the luminescent reaction to be exactly controlled.Type: GrantFiled: May 9, 1995Date of Patent: December 14, 1999Assignee: Abbott LaboratoriesInventors: Nai-Yi Wang, Roger C. Hu
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Patent number: 5985856Abstract: The present invention is drawn to water soluble derivatives aliphatic acid aromatic secondary and tertiary amine containing drugs. The present invention is further drawn to methods of making water soluble derivatives of aliphatic and aromatic secondary and tertiary amine containing drugs.Type: GrantFiled: December 30, 1998Date of Patent: November 16, 1999Assignee: University of KansasInventors: Valentino Stella, Jeffrey P. Krise, Jan J. Zygmunt, Ingrid Gunda Georg
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Patent number: 5981514Abstract: Disclosed herein are compounds of the formula ##STR1## or the pharmaceutically acceptable salts thereof wherein R.sub.1 is alkyl of 1-6 carbon atoms;A is alkylene having from 2-5 carbon atoms, each of which carbon atoms is substituted with R.sub.2, where each R.sub.2 is independently hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.3 is C.sub.1 -C.sub.6 alkyl;Y and Y.sub.1 are hydrogen or halogen; andR.sub.4 is hydrogen or --PO.sub.3 H,which compounds are water soluble and can be used for the treatment of arrhythmias.Type: GrantFiled: February 12, 1999Date of Patent: November 9, 1999Inventor: John C. Somberg
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Patent number: 5981768Abstract: A new class of stable dioxetanes bears a polycyclic stabilizing group and aryloxy moiety, the oxygen atom of which is provided with a protective group which can be removed by an enzymatic or chemical trigger admixed with the dioxetane. The polycyclic stabilizing group is preferably spiroadamantane. The group further bears an alkoxy, aryloxy, aralkyloxy or cycloalkyloxy moiety which is partially or completely substituted with halogens, particularly fluorine and chlorine. Proper selection of electron active groups on the stabilizing moiety, the aryl group and the OR group yields enhanced enzyme kinetics, superior light intensity and excellent detection sensitivity in various assays.Type: GrantFiled: September 21, 1998Date of Patent: November 9, 1999
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Patent number: 5973160Abstract: Novel methods for the preparation of sidechain-bearing taxanes, comprising the preparation of an oxazoline compound, coupling the oxazoline compound with a taxane having a hydroxyl group directly bonded at C-13 thereof to form an oxazoline sidechain-bearing taxane, and opening the oxazoline ring of the oxazoline sidechain-bearing taxane so formed. Novel compounds prepared by the methods of the present invention are also provided.Type: GrantFiled: February 13, 1996Date of Patent: October 26, 1999Inventors: Michael A. Poss, Jerome L. Moniot, Ivan D. Trifunovich, David J. Kucera, John K. Thottahil, Shu-Hui Chen, Jianmei Wei
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Patent number: 5969015Abstract: Compositions, comprising (i) a halogen-containing polymeric material, and(ii) at least one phosphite of formula I ##STR1## wherein n is a number from 1 to 6,R is a divalent linking group of formulae as defined herein as well as of novel compounds of formula I and their use as stabilisers.Type: GrantFiled: September 10, 1997Date of Patent: October 19, 1999Assignee: Witco Vinyl Additives GmbHInventors: Horst Zinke, Karl Josef Kuhn, Wolfgang Wehner
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Patent number: 5962438Abstract: A novel estrogen derivative represented by the formula: ##STR1## is useful for treating or preventing diseases caused by estrogen deficiency.Type: GrantFiled: October 17, 1997Date of Patent: October 5, 1999Assignee: Sumitomo Pharmaceuticals Company, LimitedInventors: Michihiro Yamamoto, Akira Sasaki, Takashi Katsumata, Naomi Tsushima, Hideyuki Harada
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Patent number: 5958905Abstract: Phosphoramidates and phosphinic amides and related compounds are provided. Also provided are methods that use the compounds for modulating the activity of the endothelin family of peptides are provided. In particular, compounds having formula: ##STR1## in which A, B, R.sup.1 and R.sup.2 are as described are provided. Also provided are methods for treating endothelin-mediated disorders by administering effective amounts of one or more of these compounds or prodrugs thereof. Methods for elucidating the physiological and pathophysiological roles of endothelin, as well as isolating endothelin receptors are also provided.Type: GrantFiled: March 26, 1996Date of Patent: September 28, 1999Assignee: Texas Biotechnology CorporationInventors: Ming Fai Chan, Erik Joel Verner
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Patent number: 5955453Abstract: Membrane-permeant phosphoinositides, including phosphatidylinositol phosphate esters, are described. A membrane-permeant phosphoinositide includes groups that neutralize the charges of the phosphate moieties of the phosphoinositide. A cell can be treated with the membrane-permeant phosphoinositide, which is then absorbed into the cell. The neutralizing groups can be removed intracellularly to afford the charged phosphoinositide.Type: GrantFiled: April 24, 1998Date of Patent: September 21, 1999Assignee: The Regents of the University of CaliforniaInventors: Roger Y. Tsien, Tao Jiang
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Patent number: 5948631Abstract: The subject matter of the invention is a stable mixture for the detection of alkaline phosphatase, wherein it contains the N-methylglucamine salt of o-cresolphthalein monophosphoric acid and N-methylglucamine as well as an analytical element for the detection of alkaline phosphatase with a matrix that carries this mixture. In addition the invention concerns a method for the determination of alkaline phosphatase using a salt of o-cresolphthalein monophosphoric acid, wherein the sample is brought into contact with a mixture according to the invention or an analytical element according to the invention and a change in color is observed in the presence of alkaline phosphatase.A subject matter of the invention is also a salt of o-cresolphthalein monophosphoric acid with N-methylglucamine as well as a process for producing such a salt.Type: GrantFiled: August 7, 1997Date of Patent: September 7, 1999Assignee: Roche Diagnostics GmbHInventors: Rolf Nagel, Steffen Bossert-Reuther, Thomas Zeibig
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Patent number: 5910600Abstract: A bisphosphite compound of the following formula (A): ##STR1## wherein --Ar--Ar-- is a bisarylene group represented by any one of the formulae (A-I) to (A-III) defined in the specification, and each of Z.sub.1 to Z.sub.4 is a C.sub.4-20 aromatic or heteroaromatic group which may have a substituent, wherein each of substituents on carbon atoms of an aromatic ring adjacent to the carbon atom bonded to the oxygen atom in each of Z.sub.1 to Z.sub.4, is a C.sub.0-2 group, and each pair of Z.sub.1 and Z.sub.2, and Z.sub.3 and Z.sub.4, are not bonded to each other.Type: GrantFiled: April 28, 1997Date of Patent: June 8, 1999Assignee: Mitsubishi Chemical CorporationInventors: Hisao Urata, Hiroaki Itagaki, Eitaro Takahashi, Yasuhiro Wada, Yoshiyuki Tanaka, Yasukazu Ogino
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Patent number: 5872273Abstract: A novel diphosphine compound of the formula (I): ##STR1## where R.sup.1 and R.sup.2 represent independently cycloalkyl, unsubstituted or substituted phenyl, or a five-membered heteroaromatic ring. The compound is useful as a ligand for an asymmetric reaction, in particular, as an asymmetric hydrogenation catalyst.Type: GrantFiled: December 22, 1997Date of Patent: February 16, 1999Assignee: Takasago International CorporationInventors: Takao Saito, Tohru Yokozawa, Xiaoyaong Zhang, Noburo Sayo
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Patent number: 5858995Abstract: This invention relates to a novel heterocyclic compound represented by formula (I), wherein each symbol is as defined in the specification and a pharmaceutically acceptable salt thereof which are the inhibitors of bone resorption and bone metabolism, to processes for preparation thereof, to a pharmaceutical composition comprising the same and to a method for the treatment of diseases caused by abnormal bone metabolism in human being or an animal.Type: GrantFiled: October 25, 1996Date of Patent: January 12, 1999Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Yoshio Kawai, Hitoshi Yamazaki, Natsuko Kayakiri, Kousei Yoshihara, Takumi Yatabe, Teruo Oku
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Patent number: 5847161Abstract: A new class of stable dioxetanes bears a polycyclic stabilizing group and aryloxy moiety, the oxygen atom of which is provided with a protective group which can be removed by an enzymatic or chemical trigger admixed with the dioxetane. The polycyclic stabilizing group is preferably spiroadamantane. The group further bears an alkoxy, aryloxy, aralkyloxy or cycloalkyloxy moiety which is partially or completely substituted with halogens, particularly fluorine and chlorine. Proper selection of electron active groups on the stabilizing moiety, the aryl group and the OR group yields enhanced enzyme kinetics, superior light intensity and excellent detection sensitivity in various assays.Type: GrantFiled: June 13, 1997Date of Patent: December 8, 1998
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Patent number: 5840925Abstract: Described herein are novel trioxane dimers of structure ##STR1## which possess antiproliferative and antitumor activities.Type: GrantFiled: December 2, 1996Date of Patent: November 24, 1998Assignee: Hauser, Inc.Inventors: Qun Y. Zheng, Christopher Murray, Randall J. Daughenbaugh, Poonsakdi Ploypradith, Gary H. Posner
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Patent number: 5840919Abstract: Novel 1,2-dioxetanes with improved chemiluminescent properties, such as signal intensity, S/N ratio, T1/2, etc. are provided by spiroadamantyl 1,2-dioxetanes, wherein the remaining carbon atom of the ring bears an alkoxy, aryloxy, or arylalkoxy substituent, and either a phenyl or naphthyl ring, this aromatic ring bearing, at the meta position on the phenyl group, or a non-conjugated position on the naphthyl ring, a OX moiety wherein X is an enzyme-cleavable group, which when removed from the dioxetane, leaves the oxyanion which decomposies with chemiluminescence, the aryl ring further bearing an electron active substituent Z. The nature and placement of the Z substituent, at a position not adjacent the point of attachment to the dioxetane ring, strongly influences the properties of the dioxetane. Assays, as well as kits for the performance of those assays, include the dioxetane, an enzyme capable of cleaving the X group, and in certain cases, membranes and chemiluminscent enhancement agents.Type: GrantFiled: October 17, 1995Date of Patent: November 24, 1998
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Patent number: 5840917Abstract: A phosphorylamide derivative represented by the general formula (I): ##STR1## wherein R represents an amino group that may be substituted, or a salt thereof, possesses potent antibacterial activity against Helicobacter bacterium, especially Helicobacter pylori, and is useful for prevention or treatment of digestive diseases caused by Helicobacter bacterium, solely or in combination with an antacid or an acid secretion inhibitor.Type: GrantFiled: December 6, 1996Date of Patent: November 24, 1998Assignee: Takeda Chemical Industries, Ltd.Inventors: Satoru Oi, Hideaki Nagaya, Nobuhiro Inatomi, Masafumi Nakao, Hidefumi Yukimasa
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Patent number: 5837669Abstract: The invention relates to compounds of formula: ##STR1## The invention also relates to a process for the preparation of the said compounds, which consists in:a) reacting dianhydro-1,4:3,6-D-glucitol with a compound of formula RCOOR' or RCH.sub.2 Y in the presence of a catalyst to form compounds of formula: ##STR2## in which: Y represents a halogen or an alkyl or arylsulfonic radical,R' represents a hydrogen atom or an alkyl radical having from 1 to 6 carbon atoms,R represents a saturated or unsaturated linear or branched alkyl radical containing from 5 to 21 carbon atoms,x represents CO or CH.sub.2 ;b) reacting the product of step a) with phosphorus oxychloride, a base and an anhydrous solvent, to form the compounds of formula (I) and/or (II), and optionally in separating them.The compounds which form the subject of the invention can be used in the field of surfactants, in particular for the preparation of cosmetic or hair compositions.Type: GrantFiled: March 26, 1997Date of Patent: November 17, 1998Assignee: Ceca S.A.Inventors: Serge Petit, Stephane Fouquay, Daniel Bernard
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Patent number: 5814657Abstract: Compounds of the formula ##STR1## wherein the variables are defined as in the specification, are capable of lowering introaocular pressure in the eye of a mammal.Type: GrantFiled: November 21, 1997Date of Patent: September 29, 1998Assignee: AllerganInventors: Robert M. Burk, David F. Woodward
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Patent number: 5808162Abstract: A novel chiral unsymmetric diphosphine compound of formula (I): ##STR1## wherein Ar.sup.1 and Ar.sup.2, which are different from each other, each represent a substituted or unsubstituted phenyl group, a substituted or unsubstituted naphthyl group, a pyridyl group, a quinolyl group, an isoquinolyl group, a furfuryl group, a benzofurfuryl group, a thienyl group, or a benzothienyl group, and a transition metal complex containing the diphosphine compound as a ligand. The complex catalyzes various asymmetric synthesis reactions, e.g., asymmetric hydrogenation or asymmetric hydrosilylation, exhibiting excellent performance in selectivity, conversion and catalytic activity, to provide a product of desired absolute configuration at high optical purity and in high yield.Type: GrantFiled: July 18, 1996Date of Patent: September 15, 1998Assignee: Takasago International CorporationInventors: Noboru Sayo, Xiaoyong Zhang, Tatsuya Omoto, Tohru Yokozawa, Tetsuro Yamasaki, Hidenori Kumobayashi
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Patent number: 5808102Abstract: Novel methods for the preparation of sidechain-bearing taxanes, comprising the preparation of an oxazoline compound, coupling the oxazoline compound with a taxane having a hydroxyl group directly bonded at C-13 thereof to form an oxazoline sidechain-bearing taxane, and opening the oxazoline ring of the oxazoline sidechain-bearing taxane so formed. Novel compounds prepared by the methods of the present invention are also provided.Type: GrantFiled: August 22, 1997Date of Patent: September 15, 1998Assignee: Bristol-Myers Squibb CompanyInventors: Michael A. Poss, Jerome L. Moniot, Ivan D. Trifunovich, David J. Kucera, John K. Thottahil, Shu-Hui Chen, Jianmei Wei
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Patent number: 5795981Abstract: Squarylium compounds of the formula: ##STR1## (in which Q.sup.1 and Q.sup.2 are each a chromophoric group having an aromatic unsaturated system conjugated with the squarylium ring and such that in the compounds of formulae Q.sup.1 CH.sub.2 R.sup.1 and Q.sup.2 CH.sub.2 R.sup.2 the methylene hydrogens are active hydrogens, R.sup.1 and R.sup.2 are each independently a hydrogen atom or an aliphatic or cycloaliphatic group, and R.sup.3 and R.sup.4 are each independently a hydrogen atom, or an acyl, aliphatic, cycloaliphatic, aromatic or heterocyclic group, subject to the proviso that one of R.sup.3 and R.sup.4 may be an amino or substituted amino group, or one of R.sup.3 and R.sup.4 is a hydrogen atom and the other is an organosulfonyl group, or R.sup.3 and R.sup.4 together with the intervening nitrogen atom form a nitrogenous heterocyclic ring) are useful as near infra-red absorbers.Type: GrantFiled: December 16, 1996Date of Patent: August 18, 1998Assignee: Polaroid CorporationInventors: John W. Lee, Donald A. McGowan, Mark R. Mischke, Socorro M. Ramos, Stephen J. Telfer
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Patent number: 5756770Abstract: A novel synthesis of 1,2-dioxetane phosphate alkali metal salts and novel intermediates employed in this synthesis are disclosed. A hydroxyaryl enol ether alkali metal salt having the formula: ##STR1## wherein T can be an unsubstituted or substituted adamant-2'-ylidene group, R.sup.3 can be a methyl group, Y can be a phenyl group and M.sup.+ can be a sodium cation, is reacted with a phosphorohalidate to give the corresponding enol ether ethylene phosphate, which is then reacted with an alkali metal cyanide to give the corresponding enol ether cyanoethyl phosphate diester alkali metal salt intermediate. Singlet oxygen addition to this enol ether cyanoethyl phosphate diester alkali metal salt intermediate to give the corresponding 1,2-dioxetane cyanoethyl phosphate diester alkali metal salt, followed by .beta.-elimination of the cyanoethyl group using an alkali metal hydroxide or the like, gives the corresponding 1,2-dioxetane phosphate alkali metal salt.Type: GrantFiled: December 20, 1990Date of Patent: May 26, 1998
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Patent number: 5750516Abstract: This invention provides a phosphoric diester of formula (I) which is available on di-esterification of phosphoric acid with L-ascorbic acid involving its 5-hydroxyl group and tocopherol involving its hydroxyl group or a pharmacologically acceptable salt thereof. ##STR1## The compound of the invention can be used with advantage as an antioxidant (radical-scavenging) agent and a prophylactic and therapeutic agent for ischemic organ disorders (e.g. myocardial infarction, heart failure, arrhythmia, cerebral infarction, stroke (cerebral apoplexy), renal failure, etc.).Type: GrantFiled: September 30, 1996Date of Patent: May 12, 1998Assignee: Senju Pharmaceutical Co., Ltd.Inventors: Masayuki Nakamura, Kazumi Ogata, Takahiro Sakaue, Noriko Saito, Masahito Iemura
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Patent number: 5721355Abstract: Compounds useful to attach a fluorescein label to an oligonucleotide are disclosed. To create these compounds, oxygen groups on the fluorescein moiety are protected (e.g. with acyl groups). One then links a phosphoramidite to the fluorescein moiety via an amide or thiourea linkage to an active site on the fluorescein ring. The resulting compound can then be directly linked to an oligonucleotide as it is being formed in an automated synthesizer and then deprotected using the same deprotection conditions as are used to deprotect the oligonucleotides. Such compounds are, inter alia, useful to create labelled primers for DNA sequencing.Type: GrantFiled: June 25, 1996Date of Patent: February 24, 1998Assignee: Pharmacia Biotech Inc.Inventor: Charles K. Brush
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Patent number: 5719182Abstract: Novel indane and indene derivatives are described which are endothelin receptor antagonists.Type: GrantFiled: May 16, 1995Date of Patent: February 17, 1998Assignee: SmithKline Beecham CorporationInventors: Russell Donovan Cousins, John Duncan Elliott, Maria Amparo Lago, Jack Dale Leber, Catherine Elizabeth Peishoff
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Patent number: 5714621Abstract: Compounds of the formula ##STR1## where W is (CH.sub.2).sub.n where n is 1 or 2, or n is 0 and W represents lower alkyl groups attached to each oxygen;m is an integer between 1 and 8;R.sub.1 is COOH or a pharmaceutically acceptable salt thereof, COOR.sub.4, CONR.sub.5 R.sub.6, CONR.sub.5 SO.sub.2 R.sub.7, CH.sub.2 OH, CH.sub.2 OR.sub.7, CH.sub.2 O--COR.sub.7, CH.sub.2 O--CONR.sub.5,R.sub.7, CH.sub.2 OCOOR.sub.7, CH.sub.2 NH.sub.2, CH.sub.2 NR.sub.5 R.sub.6, CH.sub.2 NR.sub.5 COR.sub.7, CHO, CH(OR.sub.8).sub.2, CHOR.sub.9 O, --COR.sub.10, CR.sub.10 (OR.sub.8).sub.2, or CR.sub.10 OR.sub.9 O, where R.sub.4 is an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5 to 10 carbons, or R.sub.4 is phenyl or lower alkylphenyl, R.sub.5 and R.sub.6 independently are hydrogen, an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5 to 10 carbons, or phenyl or lower alkylphenyl, R.sub.7 is alkyl of 1 to 10 carbons, phenyl or lower alkylphenyl, R.sub.8 is lower alkyl, and R.sub.Type: GrantFiled: February 27, 1996Date of Patent: February 3, 1998Assignee: AllerganInventors: Robert M. Burk, David F. Woodward
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Patent number: 5710288Abstract: Compounds of the formula ##STR1## where the symbols have the meaning defined in the specification, are capable of lowering intraocular pressure in the eye of a mammal.Type: GrantFiled: May 3, 1996Date of Patent: January 20, 1998Assignee: AllerganInventors: Robert M. Burk, David F. Woodward
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Patent number: 5693868Abstract: The present invention provides a method for producing novel optically active diphosphine compounds ?2,2'-bis(di-substituted phosphino)-1,1'-binaphthyl compounds! having a selectivity (chemoselectivity or enantioselectivity) and catalytic activity different from those of conventional BINAP compounds. In a method of the present invention for producing an optically active diphosphine compound (i.e., 2,2-bis(di-substituted phosphino)-1,1'-binaphthyl), 2,2'-bis(trifluoromethanesulfonyloxy)-1,1'-binaphthyl is reacted, in the presence of a transition metal-phosphine complex, with a phosphineoxide compound represented by the following general formula:A.sub.Type: GrantFiled: October 30, 1996Date of Patent: December 2, 1997Assignee: Takasago International CorporationInventors: Noboru Sayo, Xiaoyong Zhang, Tatsuya Ohmoto, Akifumi Yoshida, Tohru Yokozawa
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Patent number: 5679700Abstract: Novel phosphinic acid-containing peptidyl compounds of formula I are found to be useful inhibitors of matrix metalloendoproteinase-mediated diseases including osteoarthritis, rheumatoid arthritis, septic arthritis, tumor invasion in certain cancers, periodontal disease, corneal ulceration, proteinuria, dystrophobic epidermolysis bullosa, and coronary thrombosis associated with atherosclerotic plaque rupture. These inhibitors may also be useful in preventing the pathological sequelae following a traumatic injury that could lead to permanent disability. These compounds may also have utility as a means for birth control by preventing ovulation or implantation.Type: GrantFiled: November 9, 1995Date of Patent: October 21, 1997Assignee: Merck & Co., Inc.Inventors: Charles G. Caldwell, Philippe L. Durette, Joung L. Goulet, William K. Hagmann, Soumya P. Sahoo
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Patent number: 5679803Abstract: A new class of stable dioxetanes bears a polycyclic stabilizing group and aryloxy moiety, the oxygen atom of which is provided with a protective group which can be removed by an enzymatic or chemical trigger admixed with the dioxetane. The polycyclic stabilizing group is preferably spiroadamantane. The group further bears an alkoxy, aryloxy, aralkyloxy or cycloalkyloxymoiety which is partially or completely substituted with halogens, particularly fluorine and chlorine. Proper selection of electron active groups on the stabilizing moiety, the aryl group and the OR group yields enhanced enzyme kinetics, superior light intensity and excellent detection sensitivity in various assays.Type: GrantFiled: October 25, 1995Date of Patent: October 21, 1997
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Patent number: 5668176Abstract: Phenoxyphenylacetic acids and derivatives of the general structural formula I ##STR1## have endothelin antagonist activity and are useful in treating cardiovascular disorders, such as hypertension, postischemic renal failure, vasospasm, cerebral and cardiac ischemia, myocardial infarction, endotoxic shock, benign prostatic hyperplasia, inflammatory diseases including Raynaud's disease and asthma.Type: GrantFiled: October 18, 1996Date of Patent: September 16, 1997Assignee: Merck & Co. Inc.Inventors: Scott W. Bagley, Theodore P. Broten, Prasun K. Chakravarty, Daljit S. Dhanoa, Kenneth J. Fitch, William J. Greenlee, Nancy Jo Kevin, Gerard R. Kieczykowski, Douglas J. Pettibone, James R. Tata, Ralph A. Rivero, Thomas F. Walsh, David L. Williams, Jr., Jay M. Matthews, Richard B. Toupence
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Patent number: 5660976Abstract: This invention provides a hepatic graft preservative composition containing a phosphoric acid diester compound of the formula: ##STR1## (wherein R.sub.1 and R.sub.2 are the same or different and each represents a hydrogen atom or a methyl group) or a pharmacologically acceptable salt thereof and a method for viable preservation of the hepatic graft using the above substance.The hepatic graft preservative composition and hepatic graft preserving method of this invention inhibit hepatic microcirculation disturbance following cold storage-reperfusion of the liver to effectively prevent necrosis of hepatocytes and is, therefore, useful for the preservation of the hepatic graft.Type: GrantFiled: June 13, 1995Date of Patent: August 26, 1997Assignee: Senju Pharmaceutical Co., Ltd.Inventors: Yuzuru Ishimura, Makoto Suematsu, Kenichi Yoshida
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Patent number: 5656750Abstract: Squarylium compounds of the formula: ##STR1## (in which Q.sup.1 and Q.sup.2 are each a chromophoric group having an aromatic unsaturated system conjugated with the squarylium ring and such that in the compounds of formulae Q.sup.1 CH.sub.2 R.sup.1 and Q.sup.2 CH.sub.2 R.sup.2 the methylene hydrogens are active hydrogens, R.sup.1 and R.sup.2 are each independently a hydrogen atom or an aliphatic or cycloaliphatic group, and R.sup.3 and R.sup.4 are each independently a hydrogen atom, or an acyl, aliphatic, cycloaliphatic, aromatic or heterocyclic group, subject to the proviso that one of R.sup.3 and R.sup.4 may be an amino or substituted amino group, or one of R.sup.3 and R.sup.4 is a hydrogen atom and the other is an organosulfonyl group, or R.sup.3 and R.sup.4 together with the intervening nitrogen atom form a nitrogenous heterocyclic ring) are useful as near infra-red absorbers.Type: GrantFiled: June 6, 1995Date of Patent: August 12, 1997Assignee: Polaroid CorporationInventors: Richard M. Allen, Peter K. Chu
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Patent number: 5650404Abstract: This invention provides a therapeutic composition for pancreatitis which comprises a phosphoric diester compound of the following formula or a pharmacologically acceptable salt thereof ##STR1## wherein R.sub.1 and R.sub.2 are the same or different and each represents hydrogen or methyl. The pharmaceutical composition of this invention can be used with advantage in the prevention and treatment of pancreatitis.Type: GrantFiled: July 18, 1995Date of Patent: July 22, 1997Assignee: Senju Pharmaceutical Co., Ltd.Inventors: Kazumi Ogata, Takahiro Sakaue, Shinya Ogino, Sachiko Matsuura, Rie Nagao
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Patent number: 5646176Abstract: The present invention concerns antitumor compounds. More particularly, the invention provides novel taxane derivatives, pharmaceutical compositions thereof, and their use as antitumor agents.Type: GrantFiled: May 19, 1995Date of Patent: July 8, 1997Assignee: Bristol-Myers Squibb CompanyInventors: Jerzy Golik, Dolatrai Vyas, John J. Wright, Henry Wong, John F. Kadow, John K. Thottathil, Wen-Sen Li, Murray A. Kaplan, Robert K. Perrone, Mark D. Wittman
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Patent number: 5627173Abstract: Phosphonoacetic acid derivatives and their use for treating degenerative joint disorders Compounds of the formula I ##STR1## are suitable for producing pharmaceuticals for the treatment and prophylaxis of degenerative joint disorders, of rheumatic disorders accompanied by cartilage breakdown, such as rheumatoid arthritis, joint trauma and chondrolysis as a consequence of prolonged immobilization of the joint, of inflammations, septic shock, disorders with impaired leukocyte adhesion, disorders caused by an elevated concentration of tumor necrosis factor alpha, such as cachexia or Crohn's disease.Type: GrantFiled: January 23, 1996Date of Patent: May 6, 1997Assignee: Hoechst AktiengesellschaftInventors: Rolf Graeve, Werner Thorwart, Ruth Raiss, Klaus U. Weithmann, Stefan M ullner
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Patent number: 5622821Abstract: The invention provides lanthanide chelates capable of intense luminescence. The celates comprise a lanthanide chelator covalently joined to a coumarin-like or quinolone-like sensitizer. Exemplary sensitzers include 2- or 4-quinolones, 2- or 4-coumarins, or derivatives thereof e.g. carbostyril 124 (7-amino-4-methyl-2-quinolone), coumarin 120 (7-amino-4-methyl-2-coumarin), coumarin 124 (7-amino-4-(trifluoromethyl)-2-coumarin), aminomethyltrimethylpsoralen, etc.The chelates form high affinity complexes with lanthanides, such as terbium or europium, through chelator groups, such as DTPA. The chelates may be coupled to a wide variety of compounds to create specific labels, probes, diagnostic and/or therapeutic reagents, etc. The chelates find particular use in resonance energy transfer between chelate-lanthanide complexes and another luminescent agent, often a fluorescent non-metal based resonance energy acceptor.Type: GrantFiled: June 29, 1994Date of Patent: April 22, 1997Assignee: The Regents of the University of CaliforniaInventors: Paul R. Selvin, John Hearst
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Patent number: 5616729Abstract: Triggerable dioxetanes with a fluorescent substituent bonded or tethered in the dioxetane so as to produce fluorescence from the group are described. The compounds are of the formula: ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are carbon containing groups and wherein one of R.sub.1, R.sub.2 and R.sub.3 is a tethered fluorescent substitutent. The compounds are useful in immunoassays and in probes using enzymes or other chemicals for triggering the dioxetanes to produce light from the fluorescent molecule in the group as a signal.Type: GrantFiled: December 27, 1988Date of Patent: April 1, 1997Assignee: Board of Governors of Wayne State UniversityInventors: Arthur P. Schaap, Hashem Akhavan-Tafti
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Patent number: 5612370Abstract: Compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof wherein a, b and d are all carbon atoms or one of a, b and d is a nitrogen atom or --N(O)-- and the others are carbon atoms; Y is a single bond, --CH.sub.2 --, --C(O)--, --O--, --S-- or --N(R.sup.8)--; and R.sup.1 to R.sup.7 are as defined herein. These compounds have potassium channel activating activity and are useful, therefore for example, as cardiovascular agents.Type: GrantFiled: June 7, 1995Date of Patent: March 18, 1997Assignee: Bristol-Myers Squibb CompanyInventor: Karnail S. Atwal
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Patent number: 5612323Type: GrantFiled: June 7, 1995Date of Patent: March 18, 1997Assignee: Bristol-Myers Squibb CompanyInventor: Raj N. Misra
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Patent number: 5610122Abstract: The present invention relates to a new 3-aryl-4-hydroxy-.DELTA..sup.3 -dihydrofuranone derivatives of the general formula (I) ##STR1## in which the radicals A, B, G, X, Y, Z and n have the meaning given in the description, to a plurality of processes for their preparation, and to their use as pesticides.Type: GrantFiled: September 9, 1994Date of Patent: March 11, 1997Assignee: Bayer AktiengesellschaftInventors: Reiner Fischer, Thomas Bretschneider, Bernd-Wieland Kr uger, Hans-Joachim Santel, Markus Dollinger, Ulrike Wachendorff-Neumann, Christoph Erdelen
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Patent number: 5603949Abstract: Use of a tocopherol phosphate, other than alpha-tocopherol phosphate, especially in its dl or d form, or one of its esters having general formula (I) in which: R' is hydrogen atom, an alkyl radical having from 1 to 4 carbon atoms, such as the methyl or ethyl radical in particular, R'O is a tocopheryl radical; R" is a hydrogen atom, an alkyl radical having from 1 to 4 carbon atoms, such as the methyl or ethyl radical in particular, or R"O is an oxyethylene chain, of formula (a) in which R.sub.4 and R.sub.5 are independently a hydrogen atom or a methyl radical, and n is an integer of 1 or over; R.sub.1, R.sub.2 and R.sub.3 are independently a hydrogen atom or a methyl radical, it being understood that R.sub.1, R.sub.2 and R.sub.3 cannot simultaneously be a methyl radical. A represents the groups (b), or (c).Type: GrantFiled: June 5, 1995Date of Patent: February 18, 1997Assignee: LVMH RechercheInventors: Alain Meybeck, Marc Dumas, Frederic Bonte, Christian Marechal