Two Of The Cyclos Share At Least Three Ring Members (i.e., Bridged) Patents (Class 549/360)
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Patent number: 9290474Abstract: Small molecule therapeutics for the treatment of parasitic diseases, in particular, semi-synthetic derivatives of the fungally-derived natural product merulin A for the treatment of African Sleeping Sickness.Type: GrantFiled: December 17, 2014Date of Patent: March 22, 2016Assignee: The Regents of the University of CaliforniaInventors: Roger R Linington, Gabriel Navarro, Khanitha Pudhom, James McKerrow
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Publication number: 20150105453Abstract: Small molecule therapeutics for the treatment of parasitic diseases, in particular, semi-synthetic derivatives of the fugally-derived natural product merulin A for the treatment of African Sleeping Sickness.Type: ApplicationFiled: December 17, 2014Publication date: April 16, 2015Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: Roger R Linington, Gabriel Navarro, Khanitha Pudhom, James McKerrow
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Patent number: 8946455Abstract: Small molecule therapeutics for the treatment of parasitic diseases, in particular, semi-synthetic derivatives of the fugally-derived natural product merulin A for the treatment of African Sleeping Sickness.Type: GrantFiled: July 28, 2012Date of Patent: February 3, 2015Assignee: Regents of the University of CaliforniaInventors: Roger Linington, Gabriel Navarro, Khanitha Pudhom, James McKerrow
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Publication number: 20140296531Abstract: Small molecule therapeutics for the treatment of parasitic diseases, in particular, semi-synthetic derivatives of the fugally-derived natural product merulin A for the treatment of African Sleeping Sickness.Type: ApplicationFiled: July 28, 2012Publication date: October 2, 2014Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: Khanitha Pudhom, Gabriel Navarro, James McKerrow, Roger Linington
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Patent number: 8183200Abstract: The present invention is directed to novel fragrance compounds and their unexpected advantageous use in improving, enhancing or modifying a fragrance formulation through the addition of an olfactory acceptable amount of the compounds, wherein the compounds are represented by the following formula: wherein R1, R2, R3, R4, and R5 are independently selected from the group consisting of hydrogen and C1-C5 alkyl.Type: GrantFiled: December 16, 2010Date of Patent: May 22, 2012Assignee: International Flavors & Fragrances Inc.Inventors: Anubhav P. S. Narula, Richard M. Boden, James A. Lasome
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Patent number: 7169520Abstract: Improved organophotoreceptor comprises an electrically conductive substrate and a photoconductive element on the electrically conductive substrate, the photoconductive element comprising: (a) a charge transport material having the formula where n is an integer between 2 and 6, inclusive; R1 and R2 are, independently, H, an alkyl group, an alkaryl group, or an aryl group; X is a linking group having the formula —(CH2)m—, branched or linear, where m is an integer between 0 and 20, inclusive, and one or more of the methylene groups is optionally replaced by O, S, C?O, O?S?O, a heterocyclic group, an aromatic group, urethane, urea, an ester group, a NR3 group, a CHR4 group, or a CR5R6 group where R3, R4, R5, and R6 are, independently, H, hydroxyl group, thiol group, an alkyl group, an alkaryl group, a heterocyclic group, or an aryl group; Y comprises a bond, C, N, O, S, a branched or linear —(CH2)p— group where p is an integer between 0 and 10, an aromatic group, a cycloalkyl group, a heterocyclic grType: GrantFiled: October 31, 2003Date of Patent: January 30, 2007Assignee: Samsung Electronics Co., LtdInventors: Nusrallah Jubran, Zbigniew Tokarski, Juozas V. Grazulevicius, Vytautas Getautis, Jolita Ostrauskaite, Jurate Simokaitiene, Vygintas Jankauskas
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Patent number: 6525088Abstract: Compounds represented by the following general formula (I): wherein R1, R2, R3, R4, R5, and R6 independently represent a hydrogen atom, a halogen atom, a C1-6 alkyl group, or a C1-6 alkoxyl group, R7 and R8 independently represent a C1-6 alkyl group or an aryl group which may be substituted, R9 and R10 independently represent a hydrogen atom, a C1-6 alkyl group, or a C1-6 alkoxyl group, and R11 represents a hydrogen atom or a C1-6 alkanoyl group, or salts thereof. The aforementioned compounds are substantially non-fluorescent and react with singlet oxygen under a physiological condition to give a fluorescent substance, and therefore they are useful as agents for measurement of singlet oxygen.Type: GrantFiled: January 3, 2001Date of Patent: February 25, 2003Inventors: Tetsuo Nagano, Naoki Umezawa
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Patent number: 6365610Abstract: The invention provides a urokinase production inhibitor or angiogenesis inhibitor comprising as an active component an ozonide derivative represented by the formula (1), and method of prevention or therapy using the inhibitor wherein A is an oxygen atom or N—R (wherein R is phenyl or phenyl having as a substituent lower alkyl having 1 to 6 carbon atoms, lower alkoxyl having 1 to 6 carbon atoms or a halogen atom); B is an oxo group or —R4; and (1) when A is an oxygen atom, R1 is a hydrogen atom, etc., R2 is phenyl, etc., R3 is a hydrogen atom, etc., B is an oxo group or —R4, R4 is a hydrogen atom, etc., R5 is a hydrogen atom, etc.; (2) when A is N—R, R1 is a hydrogen atom, etc., R2 is a hydrogen atom, etc., R3 is a hydrogen atom, etc., B is —R4, R4 is a hydrogen atom, etc., R5 is a hydrogen atom, etc.Type: GrantFiled: March 28, 2000Date of Patent: April 2, 2002Assignee: Taiho Pharmaceutical Company Ltd.Inventors: Takuma Sasaki, Masatomo Nojima
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Patent number: 6166065Abstract: 2,3-Dioxabicyclo[3.3.1]nonane derivatives, carrying, at position 4, a sulfur-containing functionality selected from the group consisting of sulfonyl, sulfinyl and sulfenyl, adhered to C(4) vie methylene group, represented by structural formula (A) wherein: X is hydrogen, hydroxy, alkoxy, optionally substituted by alkoxy or acyloxy, aralkoxy optionally substituted by alkoxy or aryloxy, and M is hydrogen, hydroxy, alkoxy, alkenyloxy, acyloxy, optionally substituted by acyl or acyloxy, aralokoxy, arylalkenyloxy, oxalyloxy substituted by alkoxy, di(alkyl)amino or alkyl(aryl)amino, di(aralalkyl)amino or carbonyloxy substituted by arloxy, di(alkyl)amino, di(aralkyl)amino and alkyl(aryl)amino; or X and M together represent a carbon-carbon bond or an oxygen atom; L is hydrogen or L and M together represent a carbon-carbon bond; and either Z is a radical R--S(=O).sub.n -- and Y is hydrogen, or Y is R--S(=O).sub.Type: GrantFiled: May 11, 2000Date of Patent: December 26, 2000Assignees: Yeda Research and Development Co., Ltd., Johns Hopkins UniversityInventors: Mario Bachi, Gary H. Posner, Edward Korshin
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Patent number: 6127415Abstract: The present invention relates to specific adamantyl or adamantyl group derivative containing retinoid compounds induce apoptosis of cancer cells. These adamantyl retinoid derivatives are useful for the treatment of many cancers and solid tumors, especially androgen-independent prostate cancer, skin cancer, pancreatic carcinomas, colon cancer, melanoma, ovarian cancer, liver cancer, small cell lung carcinoma, non-small cell lung carcinoma, cervical carcinoma, brain cancer, bladder cancer, breast cancer, neuroblastoma/glioblastoma, and leukemia. Also, the invention relates to novel adamantyl or adamantyl group derivative compounds which are useful as active agents for the treatment or prevention of keratinization disorders and other dermatological conditions, and other diseases.Type: GrantFiled: April 14, 1999Date of Patent: October 3, 2000Assignee: Galderma Research & Development, S.N.C.Inventors: Magnus Pfahl, Xian-Ping Lu, Darryl Rideout, Hongyue Zhang
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Patent number: 5274157Abstract: Compounds of the formula Ib ##STR1## in which R.sub.1 and R.sub.2 independently of one another are linear or branched C.sub.1 -C.sub.12 alkyl, cycloalkyl having 5 to 8 ring carbon atoms, phenylalkyl having 1 to 4 C atoms in the alkylene group, the cyclic radicals being unsubstituted or substituted by C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy, or R.sub.1 and R.sub.2 independently of one another are --SiR.sub.4 R.sub.5 R.sub.6 in which R.sub.4, R.sub.5 and R.sub.6 independently of one another are C.sub.1 -C.sub.12 alkyl, phenyl, benzyl, or phenyl or benzyl, each of which is substituted by C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy, and R.sub.3 is a bridging member which, together with the radical --OCH--CH.sub.2 --CHO-- to which it is bonded, forms a 6- to 8-membered ring. These compounds are valuable intermediates for the preparation of carbacyclic nucleosides of the natural and unnatural series and of the racemates.Type: GrantFiled: October 30, 1992Date of Patent: December 28, 1993Assignee: Ciba-Geigy CorporationInventor: Heinz Moser
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Patent number: 5241104Abstract: Optically active mono-esters of dicarboxylic acid of the formula III: ##STR1## being useful as intermediates for preparing optically active natural products or medicines; asymmetric synthesis process for preparing thereof being characterized by the reaction of an acid anhydride with an (R)- or (S)-arylacetic acid derivative; and the key substances therefor are also claimed.Type: GrantFiled: June 23, 1992Date of Patent: August 31, 1993Assignee: Shionogi & Co., Ltd.Inventors: Mitsuaki Ohtani, Takaharu Matsuura
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Patent number: 5233056Abstract: An optically active (S)- or (R)-chroman-2-ethanol compound of a general formula (I) ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 independently represent a hydrogen atom or a lower alkyl group having 1 to 4 carbon atoms, and a chiral central carbon atom marked with a symbol * in the formula (I) alternatively has one of an R-configuration and an S-configuration, is disclosed. Further, intermediate products of the compound of the formula (I) are also disclosed. Still further, a process for manufacturing the above compounds is disclosed. The compound of the formula (I) is easily synthesized from an easily available optically active starting material.Type: GrantFiled: November 8, 1991Date of Patent: August 3, 1993Assignee: Asahi Denka Kogyo K.K.Inventors: Seiichi Takano, Kunio Ogasawara
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Patent number: 5098929Abstract: A compound of the formula (I): ##STR1## wherein R is C.sub.2-10 alkyl, alkenyl or alkynyl, each optionally subsituted by or methyl substituted by cyano, C.sub.3-4 cycloalkyl, halo, C.sub.1-4 alkoxy or a group S(O)mR.sup.4 where R.sup.4 is C.sub.1-4 alkyl and m is O, 1 or 2, or R is C.sub.3-10 cycloalkyl, C.sub.4-10 cycloalkenyl or phenyl, each optionally substituted by C.sub.1-4 alkoxy, C.sub.1-3 alkyl, C.sub.2-4 alkynyl, halo, cyano or a group S(O)mR.sup.4 as defined hereinbefore; R.sup.1 is halo, C.sub.1-3 alkyl, C.sub.2-3 alkenyl or alkynyl each optionally substituted by halo, cyano, C.sub.1-4 alkoxy, alkyl carbalkoxy containing up to 6 carbon atoms, a group S(O)mR.sup.4 as defined hereinbefore or alkynyl substituted by tri-C.sub.1-4 alkylsilyl, or R.sup.1 is cyano, spiro-cyclopropyl, gem dimethyl, oxo or methylene optionally substituted by cyano or C.sub.1-3 alkyl optionally substituted by fluorine, or R.sup.1 and R and the carbon atoms to which they are attached form a C.sub.Type: GrantFiled: February 9, 1990Date of Patent: March 24, 1992Assignee: The Wellcome Foundation LimitedInventors: John P. Larkin, Ian H. Smith
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Patent number: 5055597Abstract: This invention provides the 4-mono-anion of myo-inositol orthoformate, and describes a process for preparing this anion as well as the use of this anion in the preparation of a variety of mono- and poly-phosphate derivatives of myo-inositol.Type: GrantFiled: January 8, 1990Date of Patent: October 8, 1991Assignee: Merck Sharp & Dohme Ltd.Inventor: David C. Billington
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Patent number: 4965257Abstract: Bicyclo-[2,2,1]-heptanes, bicyclo-[2,2,2]-octanes and bicyclo-[2,2,3]-nonanes, having 2 or 3 ring hetero atoms selected from O, S and N, substituted at the 1-position by a 4-alkynylphenyl group and at the 4-position and optionally at the 3 and/or 5-position are valuable pesticides, particularly insecticides and acaracides. The compounds may be prepared by reacting an alkyne with the corresponding 4-iodophenyl substituted compounds or by debromination of the corresponding 4-dibromomethylphenyl substituted compound.Type: GrantFiled: July 24, 1989Date of Patent: October 23, 1990Assignee: The Regents of the University of CaliforniaInventors: John E. Casida, Christopher J. Palmer, John P. Larkin, Ian H. Smith
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Patent number: 4906761Abstract: This invention provides the 4-mono-anion of myo-inositol orthoformate, and describes a process for preparing this anion as well as the use of this anion in the preparation of a variety of mono- and poly-phosphate derivatives of myo-inositol.Type: GrantFiled: June 28, 1988Date of Patent: March 6, 1990Assignee: Merck Sharpe & Dohme Ltd.Inventor: David C. Billington
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Patent number: 4792606Abstract: A process for the preparation of a dimeric aromatic acyl cyanide of the formula ##STR1## in which Ar is optionally substituted phenyl, naphthyl or hetaryl,comprising reaction an acyl halide of the formulaAr--CO--Halin whichHal is fluorine, chlorine or bromine, with an alkali metal cyanide in a two-phase system comprising water and a water-immiscible or only sparingly water-miscible aliphatic ketone, and in the presence of a phase-transfer catalyst. The products are known intermediates for pesticides.Type: GrantFiled: July 16, 1987Date of Patent: December 20, 1988Assignee: Bayer AktiengesellschaftInventors: Reinhard Lantzsch, Hermann-Dieter Krall
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Patent number: 4618686Abstract: Process for the dehalogenation of aryl and alpha-araliphatic halides comprising contacting the aryl halide or alpha-araliphatic halide with hypophosphite salt, in the presence of a catalytic amount of a noble metal catalyst. This process is useful in the field of organic synthesis and for the removal of environmentally hazardous aryl and alpha-araliphatic halides, including polychlorinated biphenyls and dibenzo-p-dioxins.Type: GrantFiled: September 27, 1984Date of Patent: October 21, 1986Assignee: Ciba-Geigy CorporationInventor: Stephen K. Boyer
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Patent number: 4578484Abstract: New process for preparing the pheromone active compound lineatin (3,3,7-trimethyl-2,9-dioxatricyclo[3,3,1,0.sup.4,7 ]-nonane), by reacting a 2,2-dimethyl-3,4-pentadienal of formula 1, in which R.sub.1 and R.sub.2 is each hydrogen or lower alkyl, with .beta.-methylallyl magnesium halide; the formed 2,5,5-trimethylocta-1,6,7-trien-4-ol derivative of formula 2 is subjected to oxidation which does not attack the double bonds; the formed 2,5,5-trimethylocta-1,6,7-trien-4-one derivative of formula 3 is subjected to pyrolysis; the formed 1,4,4-trimethyl-6-methylenebicyclo[3,2,0]heptan-3-one derivative of formula 4 is subjected to oxidation; the resulting 5,5,9-trimethyl-2,6-dioxa-7-oxo-bicyclo[4,2,0]octylspiro[2,7]-decane derivative of formula 5 is subjected to oxidation; the resulting 1,5,5-trimethyl-4-oxabicyclo[4,2,0]-octan-3,7-dione of formula 6 is reduced in a per se known manner to lineatin of formula 7. Compounds 2, 3, 4 and 5 are novel.Type: GrantFiled: November 15, 1984Date of Patent: March 25, 1986Assignee: Borregaard Industries LimitedInventors: Lars Skattebol, Yngve Stenstrom
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Patent number: 4474806Abstract: Sulfonyl or carbonyl derivatives of inositols are found to be effective phospholipase C inhibitors and thereby potent anti-inflammatory and analgesic agents. These inositol derivatives are prepared by condensation of a protected inositol with a substituted sulfonic or carboxylic acid derivative followed by removal of protecting groups.Type: GrantFiled: May 10, 1982Date of Patent: October 2, 1984Assignee: Merck & Co., Inc.Inventors: Thomas R. Beattie, Shu S. Yang
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Patent number: 4421689Abstract: Derivative compounds of 1,5-dimethylbicyclo [3,2,1] octane of the general formula ##STR1## and perfume compositions containing these derivatives, wherein X represents a C.dbd.O group, a ##STR2## group or a ##STR3## group, in which R.sub.1 and R.sub.2 are alkyl groups and R.sub.3 is an ethylene or trimethylene group which may be substituted with one or more alkyl groups. These derivative compounds may be prepared by oxidation of 1,5-dimethylbicyclo [3,2,1] octan-8-ol or an ester thereof optionally followed by reaction with an alkanol or a 1,2- or 1,3-alkane-diol.Type: GrantFiled: November 5, 1979Date of Patent: December 20, 1983Inventor: Albertus J. Mulder