Polycyclo Ring System Patents (Class 568/326)
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Patent number: 6166251Abstract: Disclosed are labeling reagents containing fluorescent compounds represented by the general formula ##STR1## where R is a group capable of combining with proteins, Ar is a conjugated double bond system, and n is a whole number. These labeling reagents have high fluorescence emission intensities, give high synthesis yields, permit both solid-phase measurements and liquid-phase measurements in immunoassays, and require less measuring steps.Type: GrantFiled: December 31, 1998Date of Patent: December 26, 2000Assignees: Kazuko Matsumoto, Suzuki Motor CorporationInventors: Kazuko Matsumoto, Jingli Yuan
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Patent number: 6139770Abstract: An oxygen scavenging composition or system is provided comprising an oxygen scavenging material, a photoinitiator, and at least one catalyst effective in catalyzing an oxygen scavenging reaction, wherein the photoinitiator comprises a benzophenone derivative containing at least two benzophenone moieties. A film, a multi-phase composition, a multi-layer composition, a multi-layer film, an article comprising the oxygen scavenging composition, a method for preparing the oxygen scavenging composition, and a method for scavenging oxygen are also provided. Non-extractable benzophenone derivative photoinitiators and methods for preparing same are also provided.Type: GrantFiled: May 16, 1997Date of Patent: October 31, 2000Assignees: Chevron Chemical Company LLC, Cryovac, Inc.Inventors: Kiyoshi Katsumoto, Ta Yen Ching, Joseph L. Goodrich, Drew Ve Speer
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Patent number: 6114493Abstract: This invention relates to methods for preparing novel, solid-phase transfer reagents, specifically phosgenated oxime resins and non-symmetrical ureas, that are useful as supports in combinatorial synthesis for the creation of libraries of compounds for lead identification.Type: GrantFiled: December 22, 1998Date of Patent: September 5, 2000Assignee: E. I. du Pont de Nemours and CompanyInventor: Mark Andrew Scialdone
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Patent number: 6111118Abstract: A procedure for oxidizing organic compounds having allylic hydrogen atom(s) involving the steps of reactively contacting the organic compound with a combination of a periodic acid or metal periodate and an alkyl hydroperoxide under conditions of normal as well as elevated pressure of a suitable gas like air. The reaction can conveniently be conducted at temperatures between about 0-65.degree. C. in a cosolvent system of water and organic solvent(s).Type: GrantFiled: January 11, 1999Date of Patent: August 29, 2000Assignee: Humanetics CorporationInventors: Padma Marwah, Henry A. Lardy
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Patent number: 6080739Abstract: The present invention relates to colchicine and thiocolchicine derivatives which can be obtained from these molecules by functionalization of the C-7 to ketone or functionalization of the amino group. Said compounds have a marked antiblastic activity both on the normal cancer cells and on the chemoresistant phenotype. The compounds of the invention can be administered both by injection and orally.Type: GrantFiled: November 24, 1998Date of Patent: June 27, 2000Assignee: Indena S.p.A.Inventor: Ezio Bombardelli
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Patent number: 6048877Abstract: Tetralone derivatives of the formula ##STR1## where R.sup.1 is halo, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, (aryl)alkenyl, (aryl)alkynyl, alkoxy, O-alkenyl, O-aryl, O-alkyl(heterocyclo), COO-alkyl,alkanoyl, CO-amino, CO-substituted amino, alkyl-CO-amino, alkyl-CO-substituted amino, NHCO-alkyl, NHCO-aryl, NHCO-alkyl(heterocyclo), N(alkyl)CO-alkyl, N(alkyl)CO-aryl, N(alkyl)CO-heterocyclo, N(alkyl)CO-alkyl(heterocyclo);R.sup.2 is hydrogen, alkyl, halo, aryl, alkoxy, amino, substituted amino;R.sup.3 is oxo, hydroxy, alkoxy, O--COalkyl, --O--COaryl, --O--COheterocyclo, NOH, NO-alkyl, N-amino, N-substituted amino, N-NHCONHalkyl, N-NHSO.sub.2 alkyl, N-NHSO.sub.2 aryl, amino, substituted amino, NHCO-alkyl, NHCO-aryl, NHCO-heterocyclo, spiroheterocyclo;R.sup.4 is hydrogen, alkyl, alkyl(COalkyl), alkyl(COOalkyl); orR.sup.3 and R.sup.4 taken together with the atoms to which they are attached form a five- to seven-membered ring which can contain up to three heteroatoms selected from oxygen, nitrogen and sulfur;R.sup.Type: GrantFiled: January 20, 1998Date of Patent: April 11, 2000Assignee: Bristol-Myers Squibb CompanyInventors: Saleem Ahmad, Philip D. Stein, Francis N. Ferrara, Karnail S. Atwal
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Patent number: 6037361Abstract: Fluorinated butyric acid compounds and derivatives are described as well as acid methods for the preparation and pharmaceutical compositions of same, which are useful as inhibitors of matrix metalloproteinases, particularly gelatinase A (72 kD gelatinase) and stromelysin-1, and also collagenase, matrilysin, and MMP-13, and for the treatment of multiple sclerosis, atherosclerotic plaque rupture, aortic aneurism, heart failure, restenosis, periodontal disease, corneal ulceration, treatment of burns, decubital ulcers, wound healing, cancer, inflammation, pain, arthritis, or other autoimmune or inflammatory disorders dependent upon tissue invasion by leukocytes or other activated migrating cells, acute and chronic neurodegenerative disorders including stroke, head trauma, spinal cord injury, Alzheimer's disease, amyotrophic lateral sclerosis, cerebral amyloid angiopathy, AIDS, Parkinson's disease, Huntington's disease, prion diseases, myasthenia gravis, and Duchenne's muscular dystrophy.Type: GrantFiled: March 9, 1998Date of Patent: March 14, 2000Assignee: Warner-Lambert CompanyInventors: Bruce David Roth, Patrick Michael O'Brien, Drago Robert Sliskovic
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Patent number: 6017470Abstract: This invention provides a compound having the structure: ##STR1## wherein rings A and B represent independent electron accepting ring systems and wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7 and R.sub.8 are the same or different and are H, substituted or unsubstituted, saturated or unsaturated alkyl, alkenyl, cycloalkyl, aryl, or arylalkyl, --SR, --NRR', --OR, --OC(O)R, SC(O)R, --SCR, wherein R and R' are independently substituted or unsubstituted, saturated or unsaturated alkyl, alkenyl, cycloalkyl, aryl, or arylalkyl.This invention also provides thin films comprising a compound having the above structure or suitable derivatives thereof.This invention further provides liquid crystal display devices and non-linear optical devises comprising a compound having the above structure or a suitable derivative thereof.Type: GrantFiled: April 12, 1996Date of Patent: January 25, 2000Assignee: The Trustees of Columbia University in the City of New YorkInventors: Thomas J. Katz, Colin P. Nuckolls
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Patent number: 5993700Abstract: This invention provides an aggregate of a compound capable of forming helical structures such that the aggregate is capable of achieving a specific rotation of at least 100,000.degree. for plane polarized light having a wavelength of 589 nm.Type: GrantFiled: July 18, 1997Date of Patent: November 30, 1999Assignee: The Trustees of Columbia University in the City of New YorkInventors: Thomas J. Katz, Colin P. Nuckolls
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Patent number: 5968482Abstract: The invention relates to the use of .alpha.-hydroxyketoalkyl derivatives as light protection filters for cosmetic or pharmaceutical products, the .alpha.-hydroxyketoalkyl group being linked, if appropriate via a spacer, to a chromophoric group which has an absorption maximum in a wavelength range of between 280 and 400 nm and has a conjugated .pi.-electron system of at least 8 .pi.-electrons, and to new .alpha.-hydroxyalkyl derivatives, processes for their preparation and pharmaceutical and cosmetic formulations comprising these derivatives as light protection substances.Type: GrantFiled: September 20, 1996Date of Patent: October 19, 1999Assignee: Merck Patent Gesellschaft MIT Beschrankter HaftungInventors: Roland Martin, Ingeborg Stein, Ulrich Heywang, Michael Schwarz, Thekla Kurz
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Patent number: 5942641Abstract: The present invention provides a novel fluorenone derivatives represented by the formula: ##STR1## wherein R.sup.a -R.sup.g are defined in the specification, and a method for repairing and protecting central or peripheral nerve degeneration comprising use of a fluorenone derivative represented by the formula: ##STR2## wherein R.sup.1, R.sup.2 p and q are as defined in the specification as an active component.Type: GrantFiled: February 7, 1995Date of Patent: August 24, 1999Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Tatsuyoshi Tanaka, Yohji Sakurai, Nobutaka Fujisawa, Osamu Hongoh, Takao Nishi
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Patent number: 5869709Abstract: A procedure for oxidizing organic compounds having allylic hydrogen atom(s) involving the steps of reactively contacting the organic compound with a combination of an alkali metal periodate and an alkyl hydroperoxide. The reaction can conveniently be conducted under ambient temperature and pressure conditions, and is conveniently conducted in a cosolvent system of water and organic solvent(s).Type: GrantFiled: May 7, 1997Date of Patent: February 9, 1999Assignee: Humanetics CorporationInventors: Padma Marwah, Henry A. Lardy
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Patent number: 5859297Abstract: Disclosed are labeling reagents containing fluorescent compounds represented by the general formula ##STR1## where R is a group capable of combining with proteins, Ar is a conjugated double bond system, and n is a whole number. These labeling reagents have high fluorescence emission intensities, give high synthesis yields, permit both solid-phase measurements and liquid-phase measurements in immunoassays, and require less measuring steps.Type: GrantFiled: October 23, 1996Date of Patent: January 12, 1999Assignees: Kazuko Matsumoto, Suzuki Motor CorporationInventors: Kazuko Matsumoto, Jingli Yuan
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Patent number: 5852160Abstract: This invention relates to methods for preparing novel, solid-phase transfer reagents, specifically phosgenated oxime resins and non-symmetrical ureas, that are useful as supports in combinatorial synthesis for the creation of libraries of compounds for lead identification.Type: GrantFiled: August 19, 1997Date of Patent: December 22, 1998Assignee: E. I. du Pont de Nemours and CompanyInventor: Mark Andrew Scialdone
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Patent number: 5849956Abstract: The present invention relates to phytocassanes which are novel diterpene compounds exhibiting an antifungal activity against rice blast fungus, Pyricularia oryzae (Magnaporthe grisea) and rice sheath blight fungus, Rhizoctonia solani, and more specifically, it relates to phytocassanes A, B, C, D, and EL and a process for producing phytocassanes or momilactones, antifungal diterpene compounds, at a high yield.Type: GrantFiled: August 8, 1997Date of Patent: December 15, 1998Assignee: Plant Biological Defense System LaboratoriesInventors: Jinichiro Koga, Toyozo Yamauchi, Masaru Shimura, Yoko Ogasawara, Nagakatsu Ogasawara, Jyunko Suzuki
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Patent number: 5840661Abstract: The present invention relates to novel 2-aryl-3-hydroxy-cyclopent-2-en-1-one derivatives of the formula (I) ##STR1## in which X represents halogen, nitro, cyano, alkyl, alkoxy, alkenyloxy, alkylthio, alkylsulphinyl, alkylsulphonyl, halogenoalkyl or halogenoalkoxy,Y represents hydrogen, halogen, nitro, cyano, alkyl, alkoxy, alkenyloxy, alkylthio, alkylsulphinyl, alkylsulphonyl, halogenoalkyl or halogenoalkoxy,Z represents halogen, nitro, cyano, alkyl, alkoxy or halogenoalkoxy andA, B, D.sup.1, D.sup.2, G and n have the meaning given in the description,several processes for their preparation and their use as compositions for controlling pests and as herbicides.Type: GrantFiled: December 31, 1996Date of Patent: November 24, 1998Assignee: Bayer AktiengesellschaftInventors: Reiner Fischer, Jacques Dumas, Thomas Bretschneider, Christoph Erdelen, Ulrike Wachendorff-Neumann, Hans-Joachim Santel, Markus Dollinger, Andreas Turberg, Norbert Mencke
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Patent number: 5834521Abstract: Tetracyclic compounds having the following structure are described: ##STR1## wherein R.sub.1 -R.sub.10 are as defined. The tetracyclic compounds are capable of potent effects on steroid sensitive tissues and have demonstrated increased uterine weight, antiovulatory effects and potent steroid receptor binding. The compounds have therapeutic utility in reproductive applications such as fertility control, labor induction, ovulation induction and spermatogenesis. Methods for preparing the tetracyclic compounds from substituted indanones are also described.Type: GrantFiled: August 5, 1996Date of Patent: November 10, 1998Assignee: Ortho Pharmaceutical CorporationInventors: John H. Dodd, Lisa A. Dixon, James L. Bullington, Charles F. Schwender
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Patent number: 5770763Abstract: Novel difunctionalized cyclobutabenzene monomers of the general formula: ##STR1## wherein Z can be hydrogens or a cyclobutane ring; and X and Y are carboxyl, amino, alcohol, isocyanate, acid halide, or bis-acyl halide groups. Exemplary difunctional bitricyclodecatriene monomers are ?2,2'-bidicyclo?2.4.0!octa-1,3,5-triene!-5,5'-dicarboxylic acid (BXTA) and ?2,2'-bitricyclo?6.2.0.0!deca-1,3,(6),7-triene!-7,7'-dicarboxylic acid (QXTA). The difunctionalized bitricyclodecatriene monomers can form part of a polymer backbone chain in which the multiple butane ring functionalities can be easily opened to produce strong, three-dimensional covalent bond crosslinking between polymer chains. The crosslinking can be induced simply by heating the polymer to a temperature in excess of 250.degree. C.Type: GrantFiled: August 30, 1996Date of Patent: June 23, 1998Assignee: The Board of Regents of the Univ. of MichiganInventors: David C. Martin, Jeffrey S. Moore, Larry J. Markoski, Kenneth A. Walker, Gary E. Spilman
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Patent number: 5760092Abstract: Disclosed are allocolchinones, which are anti-mitotic agents. Allocolchinones bind to tubulin reversibly and are more effective at inhibiting microtubule formation than colchicine. 7-Acetamido-allocolchinone inhibits the growth of a number of tumor cell lines at concentrations about 100 times lower than colchicine. Also disclosed is a method of treating an individual with cancer by administering a composition which comprises a therapeutically effective amount of an allocolchinone which inhibits microtubule assembly. Administering a therapeutically effective amount of a composition which comprises an allocolchinone which inhibits microtubule assembly can also be used for treating inflammatory diseases, multiple sclerosis, primary biliary cirrhosis, Alzheimer's Disease and Behcet's Disease.Type: GrantFiled: March 11, 1996Date of Patent: June 2, 1998Assignee: Brandeis UniversityInventors: Serge M. Timasheff, Marina J. Gorbunoff, Bernardo Perez-Ramirez
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Patent number: 5741814Abstract: Cyclooctadiene derivative of the following formula (1): ##STR1## wherein A.sup.1, A.sup.2, A.sup.3 and A.sup.4 each independently represent COOR.sup.5 (where R.sup.5 represents a hydrogen atom, a C.sub.1 -C.sub.10 alkyl group, a phenyl group, a C.sub.7 -C.sub.12 aralkyl group or CONR.sup.6 R.sup.7 (where R.sup.6 and R.sup.7 each independently represent a hydrogen atom, a C.sub.1 -C.sub.10 alkyl group or a phenyl group), or A.sup.1 and A.sup.2, and/or A.sup.3 and A.sup.4 may be combined together to represent group(s) of: ##STR2## in which X represents an oxygen atom or NR.sup.8 {where R.sup.8 represents a hydrogen atom, a C.sub.1 -C.sub.10 alkyl group or a phenyl group),R.sup.0, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 each independently represent a hydrogen atom, a halogen atom, a hydroxyl group and an C.sub.1 -C.sub.10 alkyl group,the symbol ------ represents a single or double bond, and when it is a double bond, then R.sup.1 and R.sup.Type: GrantFiled: September 3, 1996Date of Patent: April 21, 1998Assignee: Nissan Chemical Industries, Ltd.Inventors: Yasuyuki Nakajima, Hisayuki Watanabe, Michiaki Adachi, Michito Tagawa, Mitsugu Futagawa, Takashi Furusato, Hiroshi Ohya, Masanori Nishioka
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Patent number: 5726325Abstract: The present invention relates to tricyclic compounds represented by general formula (I) which are useful as therapeutic agents for urinary incontinence: ##STR1## wherein R.sup.1 represents hydrogen and the like; --X.sup.1 --X.sup.2 --X.sup.3 -- represents --CR.sup.2 .dbd.CR.sup.3 --CR.sup.4 .dbd.CR.sup.5 -- (wherein R.sup.2, R.sup.3, R.sup.4, and R.sup.5 represent hydrogen and the like) and the like; and Y represents --CH.sub.2 O-- and the like.Type: GrantFiled: June 6, 1997Date of Patent: March 10, 1998Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Makoto Yoshida, Shin-ichi Sasaki, Shigeru Aono, Shigeki Fujiwara, Haruki Takai, Tsuyoshi Yamagata, Ken Nagashima, Akira Karasawa
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Patent number: 5705704Abstract: Novel tricyclic compounds of formula I as defined in the specification, a process for their preparation and their use for the preparation of optically active or racemic colchicine and thiocolchicine derivatives.Type: GrantFiled: March 1, 1996Date of Patent: January 6, 1998Assignee: Roussel UclafInventors: Francis Brion, Bernadette Chappert, Christian Diolez, Christian Marie, Alain Mazurie, Michel Middendorp, Didier Pronine, Edmond Toromanoff
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Patent number: 5705169Abstract: The invention relates to ketotricyclo?5.2.1.0!decane derivatives of the formula I ##STR1## wherein Phe is a phenylene group which is unsubstituted or substituted by 1 to 4 hydroxyl, alkyl or alkoxy groups having 1 to 10 C atoms,and their preparation and use as UV filters, in particular in cosmetic or pharmaceutical preparations.Type: GrantFiled: July 24, 1995Date of Patent: January 6, 1998Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Inge Stein, Michael Schwarz, Ulrich Heywang
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Patent number: 5698595Abstract: Application of a compound having at least one sulfonic acid functional group which is at least partially non-neutralized, in a cosmetic or dermatological composition, to the skin is useful for treating intrinsic ageing of the skin.Type: GrantFiled: December 19, 1996Date of Patent: December 16, 1997Assignee: L'OrealInventors: Jean Paul Boelle, Jean-Pierre Laugier, Serge Forestier
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Patent number: 5519027Abstract: New D-homo-(16-ene)-11.beta.-aryl-4-estrenes of general formula I ##STR1## as well as their pharmaceutically compatible addition salts with acids are described in whichX stands for an oxygen atom, the hydroxyimino grouping >N.about.OH or two hydrogen atoms,R.sup.1 stands for a hydrogen atom or a methyl group,R.sup.2 stands for an hydroxy group, a C.sub.1 -C.sub.10 alkoxy or C.sub.1 -C.sub.10 acyloxy group,R.sup.11 stands for a fluorine, chlorine or bromine atom, and then R.sup.12 and R.sup.13 together mean an additional bond orR.sup.11 stands for a straight-chain or branched-chain C.sub.1 -C.sub.4 -alkyl radical or a hydrogen atom, and then R.sup.12 and R.sup.13 each mean a hydrogen atom or together mean an additional bond,and R.sup.3 and R.sup.4 have the usual meanings indicated in the description for competitive progesterone antagonists.Type: GrantFiled: February 25, 1994Date of Patent: May 21, 1996Assignee: Schering AktiengesellschaftInventors: Wolfgang Schwede, Eckhard Ottow, Arwed Cleve, Walter Elger, Krzysztof Chwalisz, Martin Schneider
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Patent number: 5514675Abstract: This invention provides methods of treating a physiological disorder associated with an excess of bradykinins in a mammal which comprises administering to a mammal in need of said treatment a compound selected from a series of substituted dihydronaphthalenes and naphthalenes.Type: GrantFiled: October 20, 1994Date of Patent: May 7, 1996Assignee: Eli Lilly and CompanyInventors: Robert F. Bruns, Jr., Donald R. Gehlert, J. Jeffry Howbert, William H. W. Lunn
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Patent number: 5500156Abstract: Compositions for use in non-linear optical devices. The compositions have first molecular electronic hyperpolarizability (.beta.) either positive or negative in sign and therefore display second order non-linear optical properties when incorporated into non-linear optical devices.Type: GrantFiled: April 11, 1994Date of Patent: March 19, 1996Assignee: California Institute of TechnologyInventors: Seth R. Marder, Chin-Ti Chen, Lap-Tak Cheng
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Patent number: 5492917Abstract: Novel compounds of the general structural formula I: ##STR1## have endothelin antagonist activity and are therefore useful in treating cardiovascular disorders, such as hypertension, pulmonary hypertension, postischemic renal failure, vasospasm, cerebral and cardiac ischemia, myocardial infarction, endotoxic shock, inflammatory diseases including Raynaud's disease and asthma.Type: GrantFiled: September 29, 1993Date of Patent: February 20, 1996Assignee: Merck & Co., Inc.Inventors: Ralph A. Rivero, Peter D. Williams, Daniel F. Veber
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Patent number: 5488180Abstract: This invention relates to complex hydrophobe compounds and to alkoxylation products, i.e., condensation reaction products of alkylene oxides and complex hydrophobe compounds having at least one active hydrogen. This invention also relates to alkoxylation products that have beneficial, narrow molecular weight ranges.Type: GrantFiled: May 29, 1992Date of Patent: January 30, 1996Assignee: Union Carbide Chemicals & Plastics Technology CorporationInventors: Richard D. Jenkins, David R. Bassett, Danny E. Smith, John N. Argyropoulos, James E. Loftus, Gregory D. Shay
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Patent number: 5480913Abstract: Disclosed are novel classes of anti-androgens including dihydrophenanthrene derivatives, their method of synthesis and their use in treating disorders associated with excessive androgenic activities.Type: GrantFiled: May 3, 1993Date of Patent: January 2, 1996Assignee: Arch Development CorporationInventors: Shutsung Liao, John Pataki, Ronald G. Harvey
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Patent number: 5478862Abstract: The invention is drawn to 17-oxo-15,16-seco-19-nor steroids which are useful as intermediates in the production of various 15,16-seco-19-nor progestins. These progestins display elevated progestational activity with a minimum of ancillary hormonal activity and are thus useful in the suppression of ovulation in the human female.Type: GrantFiled: May 13, 1994Date of Patent: December 26, 1995Assignee: SRI InternationalInventors: Richard H. Peters, Masato Tanabe
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Patent number: 5476860Abstract: Diaromatic compounds, characterized in that they correspond to the following general formula: ##STR1## in which: R.sub.1 is --CH.sub.3, --CH.sub.2 OH, --COR.sub.8 or --CH.sub.2 OCOR.sub.9, R.sub.8 is H, OH, --OR.sub.10, --N(rr') or alkyl, R.sub.10 is alkyl, alkenyl, aryl or aralkyl, r and r' being H, alkyl, aryl, aralkyl, etc., r and r' together form a heterocycle, R.sub.9 is alkyl, alkenyl or a sugar residue, R.sub.2 and R.sub.3 are --OR.sub.11 or --OCOR.sub.11, R.sub.11 is H, alkyl, fluoroalkyl, aryl or aralkyl, R.sub.3 in addition being H, R.sub.4 is H, OH, alkyl, alkoxy, F, Cl or --CF.sub.3, R.sub.5 and R.sub.7 are H, OH, alkoxy, .alpha.-substituted alkyl or .alpha.,.alpha.'-disubstituted alkyl, etc., R.sub.6 is H, OH, alkyl, alkoxy, cycloalkyl, etc., R.sub.5 and R.sub.7 cannot simultaneously be OH or alkoxy and R.sub.4, R.sub.5, R.sub.6 and R.sub.7 cannot simultaneously be H, R.sub.5 and R.sub.6 or R.sub.6 and R.sub.Type: GrantFiled: December 8, 1993Date of Patent: December 19, 1995Assignee: Centre International de Recherches Dermatologiques (CIRD Galderma)Inventor: Jean-Michel Bernardon
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Patent number: 5457108Abstract: The invention relates to substituted 5-oxo-di-benzo[a,d]cyclohepta-1,4-dienes of the formula (I) ##STR1## processes for their preparation and their use as retroviral agents.Type: GrantFiled: September 17, 1993Date of Patent: October 10, 1995Assignee: Bayer AktiengesellschaftInventors: Hanno Wild, Jutta Hansen, Jorg Lautz, Arnold Paessens
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Patent number: 5457239Abstract: A process for the preparation of a formylated aromatic compound comprising contacting an aromatic compound with (i) a halogenated compound in the presence of a Lewis acid, and (ii) a base, is described. The subject process provides an efficient and effective means of preparing formylated compounds which may be useful in a wide variety of applications.Type: GrantFiled: May 25, 1994Date of Patent: October 10, 1995Assignee: Union Camp CorporationInventors: Walter C. Frank, Richard L. Veazey, John J. Mahurter, Mark J. Jenkins, Neil R. Fairfax
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Patent number: 5405948Abstract: A compound of formula (I): selected from 1,5-diyne-3-cyclodecene and undecene compounds. ##STR1## in which: R represents a hydrogen atom, a straight-chain or branched (C.sub.1 -C.sub.6) acyl radical or a glycoside radical,R' represents a hydrogen atom ##STR2## n is 1 or 2, and R.sub.1 and R.sub.2 simultaneously represent two hydrogen atoms or, together with the two carbon atoms and the double bond to which they are attached, form a phenyl ring.Type: GrantFiled: September 30, 1992Date of Patent: April 11, 1995Assignee: Adir et CompagnieInventors: Jean-Marie Beau, Christophe Crevisy, Ghanem Atassi, Alain Pierre
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Patent number: 5380718Abstract: Arthropodicidal tetrahydropyridazines of Formulae I and II, ##STR1## wherein Q,X,X.sup.1 Y, and G are as defined in the text, compositions containing them and their use in the control of arthropods.Type: GrantFiled: November 12, 1992Date of Patent: January 10, 1995Assignee: E. I. Du Pont de Nemours and CompanyInventors: Charles R. Harrison, George P. Lahm, Thomas M. Stevenson
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Patent number: 5329050Abstract: 1-Indanones of the formula IV or IVa ##STR1## in which R.sup.1 and R.sup.7 are preferably hydrogen or alkyl, or adjacent radicals R.sup.1 to R.sup.4 form a ring, are obtained in a one-step reaction by reacting a compound I ##STR2## with a compound of the formula II or a compound III ##STR3## in liquid hydrogen fluoride.Type: GrantFiled: April 27, 1993Date of Patent: July 12, 1994Assignee: Hoechst AktiengesellschaftInventors: Laurent Weisse, Jurgen Rohrmann, Frank Kuber, Heinz Strutz
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Patent number: 5232915Abstract: 9.alpha.-Hydroxy-19,11.beta.-bridged steroids of general formula I ##STR1## are described. The more detailed meaning of A, B, R.sup.1, R.sup.2, G, Z, R.sup.4 --Y and R.sup.4' --Y' follows from the description. The steroids of general formula I have antigestagen and/or antiglucocorticoidal action and can be used for the production of pharmaceutical agents.Type: GrantFiled: January 14, 1992Date of Patent: August 3, 1993Assignee: Schering AktiengesellschaftInventors: Eckhard Ottow, Gunter Neef, Rudolf Wiechert, Walter Elger, Sybille Beier, Karl-Heinrich Fritzemeier
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Patent number: 5213709Abstract: A mesomorphic compound represented by the following formula (I): ##STR1## wherein R.sub.1 and R.sub.2 respectively denote an alkyl group having 1-16 carbon atoms optionally substituted; X.sub.1 and X.sub.3 respectively denote a single bond, --O--, ##STR2## X.sub.2 denotes a single bond, ##STR3## A.sub.1 denotes a single bond ##STR4## A.sub.3 denotes ##STR5## A.sub.2 denotes 9, 10-dihydro-2,7-phenanthrenediyl, 2,7-fluorenediyl or 2,7-fluorenonediyl; n is 0 or 1; and X.sub.4 and X.sub.5 respectively denote hydrogen, F, Cl, Br, --CH.sub.3, --CN or --CF.sub.3, with proviso that X.sub.1 is a single bond when A.sub.1 is a single bond.Type: GrantFiled: April 30, 1991Date of Patent: May 25, 1993Assignee: Canon Kabushiki KaishaInventors: Takao Takiguchi, Takashi Iwaki, Takeshi Togano, Yoko Yamada, Shinichi Nakamura
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Patent number: 5208263Abstract: Disclosed are novel classes of anti-androgen including dihydrophenanthrene derivatives, their method of synthesis and their use in treating disorders associated with excessive androgenic activities.Type: GrantFiled: September 27, 1989Date of Patent: May 4, 1993Assignee: Arch Development CorporationInventors: Shutsung Liao, John Pataki, Ronald G. Harvey
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Patent number: 5192817Abstract: Novel phenanthrene derivatives represented by the general formula (1), ##STR1## wherein the group of the formula ##STR2## is a group of the formula ##STR3## (wherein R.sup.1 is a hydrogen atom or a lower alkyl group), a group of the formula ##STR4## (wherein R.sup.2 is a hydrogen atom or a lower alkanoyl group) or a group of the formula ##STR5## (wherein R.sup.2 is the same as defined above), and salts thereof, and other compounds derived therefrom and salts thereof; processes for preparing the same; and interleukin-1 (IL-1) inhibitors containing the abovementioned novel phenanthrene derivatives as to the active ingredient(s).Type: GrantFiled: November 5, 1991Date of Patent: March 9, 1993Assignees: Otsuka Pharmaceutical Co., Ltd., Otsuka Pharmaceutical Factory, Inc.Inventors: Yoshihisa Takaishi, Kiyoto Goto, Takuji Uesako, Toshiko Kuwahara, Masaaki Takai, Yukihisa Ono, Yoshihiro Taniguchi, Sachiko Manabe, Takahiro Asakuni
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Patent number: 5185447Abstract: Ketones having formulas (1)-(3) are provided by improved methods which involve the treatment of compounds having formulas (9)-(11) with aqueous base. ##STR1## wherein R.sub.x is NO.sub.2.Type: GrantFiled: January 29, 1992Date of Patent: February 9, 1993Assignee: Du Pont Merck Pharmaceutical CompanyInventor: Edward C. Crapps
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Patent number: 5183942Abstract: Macrocyclic enediynediols and enediynediones having a ten carbon ring and open chain enediyne dihydroperoxides having eight carbons between the hydroperoxide groups that cleave DNA are disclosed, as are methods of making and using the same.Type: GrantFiled: November 5, 1991Date of Patent: February 2, 1993Assignee: The Scripps Research InstituteInventors: Kyriacos C. Nicolaou, Erik Sorensen, Chan-Kou Hwang, Robert Discordia, Robert G. Bergman, Robert E. Minto
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Patent number: 5162588Abstract: Compound of formula ##STR1## wherein a) indexes m and n are identical and stand each for an integer number equal to zero, symbols R.sup.1 and R.sup.2 are identical and represent each a hydrogen atom, or are different and represent each a hydrogen atom or a methyl radical, symbols R.sup.5 and R.sup.8 stand each for a methyl radical, symbols R.sup.6 and R.sup.7 can be identical or different and designate each a hydrogen atom or a methyl radical and, either symbol R.sup.4 represents a methyl radical and symbol R.sup.3 stands for a hydrogen atom or a methyl radical, or symbols R.sup.3 and R.sup.4 represent each a methylene radical belonging to a ring such as indicated by the dotted line, with the proviso that the following combinations are excluded:1. R.sup.1 =R.sup.2 =R.sup.3 =R.sup.6 =R.sup.7 =H, or2. R.sup.1 =R.sup.2 =R.sup.3 =H and R.sup.6 or R.sup.7 =CH.sub.3, or3. R.sup.2 =CH.sub.3 and R.sup.3 =R.sup.6 =R.sup.7 =H, or4. R.sup.2 =CH.sub.3 and R.sup.3 =H and R.sup.6 or R.sup.7 =CH.sub.3, or5. R.sup.1 =R.sup.Type: GrantFiled: June 26, 1990Date of Patent: November 10, 1992Assignee: Firmenich S.A.Inventors: Charles Fehr, Jose Galindo
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Patent number: 5144081Abstract: The invention relates to dialkoxybenzylidene-camphor derivatives of the formula I ##STR1## in which R.sup.1 and R.sup.2, in each case independently of one another, are a straight-chain or branched alkyl radical having 1 to 10 c atoms, andX is H or SO.sub.3 H,and to a process for their preparation and their use in cosmetic and pharmaceutical preparations.Type: GrantFiled: September 4, 1991Date of Patent: September 1, 1992Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Ulrich Heywang, Roland Martin, Ingeborg Stein
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Patent number: 5140044Abstract: A UCN-1028D derivative represented by the formula: ##STR1## has protein kinase C inhibitory activity and is expected to be used as an active ingredient in anti-tumor agents, etc.Type: GrantFiled: March 27, 1990Date of Patent: August 18, 1992Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Teruo Kishi, Hiromitsu Saito, Hiroshi Sano, Isami Takahashi, Tatsuya Tamaoki
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Patent number: 5136099Abstract: 5-Hydroxy-benzo-(1',2')-cyclodeca-2,7-diyne-1-one and derivatives thereof and related fused ring diyneone macrocyclic compounds are disclosed. The compounds possess DNA-cleaving, antibiotic and tumor growth-inhibiting properties. Methods of making and using the same are also disclosed.Type: GrantFiled: August 1, 1990Date of Patent: August 4, 1992Assignee: Scripps Clinic and Research FoundationInventors: Golfo Skokotas, Kyriacos C. Nicolaou
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Patent number: 5117062Abstract: A novel synthesis of aromatic tertiary amines involves reacting an aromatic anil and an aromatic ether in a molar ratio of 1:1; adjusting the ratio to 2:1 produces novel enamines and by employing a two step process for enamine production, various unsymmetrically substituted enamines can be obtained which are readily hydrolyzed to corresponding deoxybenzoins which in turn are readily oxidized to benzils, the aromatic tertiary amines may be used to produce charge transport layers in xerography, while the benzils may be used to produce a variety of desired polymers.Type: GrantFiled: January 22, 1991Date of Patent: May 26, 1992Inventors: Allan S. Hay, Martino Paventi
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Patent number: 5100921Abstract: New angucyclinones with a therapeutic action can be prepared with the aid of a strain of the genus Streptomyces.Type: GrantFiled: April 25, 1989Date of Patent: March 31, 1992Assignee: Hoechst AktiengesellschaftInventors: Susanne Grabley, Joachim Wink, Carlo Giani, Gerhard Seibert, Wolfgang Raether, Susanne Dobreff, Axel Zeeck
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Patent number: 5095099Abstract: This invention concerns novel fluorescent compositions having the potential for absorption of visible and UV radiation and for re-emitting the radiation at longer wavelengths. The compositions comprise rare earth chelates containing a phenalenone nucleus.Type: GrantFiled: December 10, 1990Date of Patent: March 10, 1992Assignee: E. I. Du Pont de Nemours and CompanyInventors: Bruce A. Parkinson, Andrew Streitwieser, Jr., Douglas W. Wiley