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序号 专利名 申请号 申请日 公开(公告)号 公开(公告)日 发明人
41 A PRODRUG COMPRISING BETA-KETO CARBOXYLIC ACID, BETA-KETO CARBOXYLIC ACID SALT OR BETA-KETO CARBOXYLIC ACID ESTER FOR DRUG DELIVERY EP10764738.0 2010-04-13 EP2419398A1 2012-02-22 ANDERSSON, Martin
There is provided a prodrug of a pharmaceutically active agent, said prodrug comprising a beta-keto carboxylic acid, a beta-keto carboxylic acid salt or a beta-keto carboxylic acid ester functional group, to a pharmaceutical composition comprising the prodrug, and to the use of the prodrug or composition for treatment of a mammalian subject suffering from a condition which can be cured or alleviated by administration of said pharmaceutically active agent. There is further provided a method of inhibiting decarboxylation of a compound comprising a beta-keto carboxylic acid or a salt thereof with a monovalent cation, characterized in that a dry salt of said beta-keto carboxylic acid with a divalent or polyvalent cation is prepared.
42 Verfahren zur Herstellung von Alpha, Alpha-Dialkyl-Alpha-Hydroxymethyl-Carbonsäurederivaten EP05025658.5 2005-11-24 EP1666447A1 2006-06-07 Böhm, Andreas, Dr.; Petersen, Hermann, Dr.; Stohrer, Jürgen, Dr.

Die Erfindung betrifft ein neues Verfahren zur Hydroxymethylierung von nichtzyklischen α,α-Dialkyl-Carbonsäurederivaten mit Formaldehyd unter Verwendung von Amid-Basen bei Temperaturen von -40°C bis zum Siedepunkt des verwendeten Lösungsmittels oder Lösungsmittelgemisches.

43 CYCLOOCTADIENE DERIVATIVE EP95907819.7 1995-02-01 EP0742196A1 1996-11-13 NAKAJIMA, Yasuyuki, Nissan Chemical Industries,; WATANABE, Hisayuki, Nissan Chemical Industries,; ADACHI, Michiaki, Nissan Chemical Industries, Ltd.; TAGAWA, Michito, Nissan Chemical Industries, Ltd.; FUTAGAWA, Mitsugu, Nissan Chemical Industries, Ltd; FURUSATO, Takashi, Nissan Chemical Industries, Ltd; OHYA, Hiroshi, Nissan Chemical Industries, Ltd.; NISHIOKA, Masanori, Nissan Chemical Industries Ltd

Cyclooctadiene derivative of the following formula (1): wherein A1, A2, A3 and A4 each independently represent COOR5 (where R5 represents a hydrogen atom, a C1-C10 alkyl group, a phenyl group, a C7-C12 aralkyl group or CONR6R7 (where R6 and R7 each independently represent a hydrogen atom, a C1-C10 alkyl group or a phenyl group), or A1 and A2, and/or A3 and A4 may be combined together to represent group(s) of: in which X represents an oxygen atom or NR8 {where R8 represents a hydrogen atom, a C1-C10 alkyl group or a phenyl group),

R0, R1 , R2, R3 and R4 each independently represent a hydrogen atom, a halogen atom, a hydroxyl group and an C1-C10 alkyl group,

the symbol --- represents a single or double bond, and when it is a double bond, then R1 and R3 each independently may represent an oxygen atom;

provided that the case where all of R0, R1, R2, R3 and R4 represent hydrogen atoms at the same time is excluded, and agrohorticultural fungicides, antimold agents and antithrombocytic agents containing said derivatives.

The compounds have superior fungicidal activity, antimold activity and activity for preventing platelet aggregation, and are useful as an agrohorticultural fungicide, an antimold agent and an antithrombocytic agent.

44 Spiro compounds and pharmaceutical use thereof US12258033 2008-10-24 US08299296B2 2012-10-30 Takashi Shimada; Hiroshi Ueno; Kazuhiro Tsutsumi; Kouichi Aoyagi; Tomoyuki Manabe; Shin-Ya Sasaki; Susumu Katoh
The spiro compound represented by the following general formula [Ia], its pharmaceutically acceptable salt or a solvate thereof
45 Compounds US12089275 2006-10-05 US08148572B2 2012-04-03 Timothy Jon Luker; Rukhsana Tasneem Mohammed; Stephen Thom; Anil Patel
The invention relates to substituted phenylacetic acids as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their preparation.
46 T-butyl cascade polymers US12560157 2009-09-15 US08067630B1 2011-11-29 George R. Newkome; Charles N. Moorefield; Rajani K. Behera
A method for forming cascade polymers specifically utilizing the amine monomer of the formula The monomer is made by initially reacting nitromethane and CH2═CHCO2—TBu by nucleophilic addition to form the triester nitrotrialkanoate of the formula and then reducing the nitrosubstituent to afford the said amine monomer.
47 Biphenyl compound selective agonists of gamma RAR receptors US12213177 2008-06-16 US08049034B2 2011-11-01 Thibaud Biadatti; Etienne Thoreau
Biphenyl compounds having the formula (I): are useful for preventing/treating pathologies linked to a deficiency of the activation of the RAR gamma receptor, e.g., for treating a pathology linked to a cell differentiation and/or proliferation disorder, for treating acne, for treating psoriasis.
48 Synthetic bifunctional molecules containing drug moiety and pharmacokinetic modulating moiety US11011776 2004-12-13 US08044099B2 2011-10-25 Roger Briesewitz; Gerald R. Crabtree; Thomas J. Wandless
Bifunctional molecules and methods for their use are provided. The subject bifunctional molecules are conjugates of a drug moiety and a pharmacokinetic modulating moiety, where these two moieties are optionally joined by a linking group. The bifunctional molecules are further characterized in that they exhibit at least one modulated pharmacokinetic property upon administration to a host as compared to a free drug control. The subject bifunctional molecules find use in a variety of therapeutic applications.
49 Recovery of organic acids US11046206 2005-01-28 US07601865B2 2009-10-13 Dan W. Verser; Timothy J. Eggeman
A method is disclosed for the recovery of an organic acid from a dilute salt solution in which the cation of the salt forms an insoluble carbonate salt. A tertiary amine and CO2 are introduced to the solution to form the insoluble carbonate salt and a complex between the acid and an amine. A water immiscible solvent, such as an alcohol, is added to extract the acid/amine complex from the dilute salt solution to a reaction phase. The reaction phase is continuously dried and a product between the acid and the solvent, such as an ester, is formed.
50 Hydrogenation of benzene polycarboxylic acids or derivatives thereof US10535531 2003-11-18 US07595420B2 2009-09-29 Richard Henry Schlosberg; Jose Guadalupe Santiesteban; Stuart L. Soled; Andrzej Mariusz Malek; Joseph E. Baumgartner; Luo Shifang; Sabato Miseo; James Clarke Vartuli
A process for hydrogenating benzenepolycarboxylic acids or derivatives thereof, such as esters and/or anhydrides, by bringing one or more benzenepolycarboxylic acids or one or more derivatives thereof into contact with a hydrogen-containing gas in the presence of one or more catalytically active metal, such as platinum, palladium, ruthenium or mixtures thereof, deposited on a catalyst support comprising one or more ordered mesoporous materials.
51 Purification and production methods of 1-aminocyclopropanecarboxylic acid US11183858 2005-07-19 US07476760B2 2009-01-13 Ryota Hamasaki; Mitsuru Ohno
A method purifies 1-aminocyclopropanecarboxylic acid by subjecting a crude 1-aminocyclopropanecarboxylic acid to crystallization with a solvent mixture containing an organic acid having one to five carbon atoms and a poor solvent for 1-aminocyclopropanecarboxylic acid, which poor solvent is miscible with the organic acid. In the method, the solvent mixture may further contain water. Purification may be carried out by mixing the crude 1-aminocyclopropanecarboxylic acid with the organic acid having one to five carbon atoms, removing insoluble matter by filtration, and adding the poor solvent with or without water to the filtrate to thereby crystallize 1-aminocyclopropanecarboxylic acid.
52 Substituted arylalkanoic acid derivatives and use thereof US10568185 2004-08-13 US07470807B2 2008-12-30 Motoshi Shoda; Hiroshi Kuriyama
A compound represented by the formula (I): [In the formula, Link represents a saturated or unsaturated straight hydrocarbon chain having 1 to 3 carbon atoms, C2 to C6 in the aromatic ring (E) independently represent a ring-constituting carbon atom, one of the ring-constituting carbon atoms may be replaced with V, V represents nitrogen atom, or carbon atom substituted with Zx, Zx represents a saturated alkyl group having 1 to 4 carbon atoms and the like, Rs represents -D-Rx etc., D represents a single bond, oxygen atom and the like, Rx represents a saturated alkyl group having 3 to 8 carbon atoms and the like, AR represents a partially unsaturated or completely unsaturated condensed bicyclic carbon ring or a heterocyclic ring, and Y represents hydrogen atom, a lower alkyl group having 1 to 4 carbon atoms and the like] or a salt thereof. A compound having prostaglandin production-suppressing action and leukotriene production-suppressing action is provided.
53 Salts, aqueous liquid compositions containing salts of S-(+ )-abscisic acid and methods of their preparation US12011846 2008-01-30 US20080207454A1 2008-08-28 Daniel F. Heiman; Bala Devisetty; Peter D. Petracek; Xiaozhong Liu; John Lopez; Derek D. Woolard; Yueh Wang; Gregory D. Venburg; Prem Warrior
The present invention generally relates to salts of S-(+)-abscisic acid, aqueous liquid compositions containing salts of S-(+)-abscisic acid and methods of their preparation for agricultural use.
54 PROCESS FOR THE PREPARATION OF CETP(1) US11951444 2007-12-06 US20080154059A1 2008-06-26 Ursula Hoffmann; Bruno Lohri
The present invention relates to a process for the preparation of 1-(2-ethyl-butyl)-cyclohexanecarboxylic acid which is useful as an intermediate in the preparation of pharmaceutical active compounds.
55 Anti-inflammatory and psoriasis treatment and protein kinase inhibition by hydroxy stilbenes and novel stilbene derivatives and analogues US10893863 2004-07-15 US07321050B2 2008-01-22 Genhui Chen; John M. Webster; Jianxiong Li; Kaji Hu; Wei Liu; Jiang Zhu
The present invention provides novel diphenyl ethene compounds and pharmaceutically-acceptable salts thereof. Also provided are methods for making the compounds of the invention as well as methods for the use thereof in the treatment of immune, inflammatory, and auto-immune diseases.
56 Compounds having selective cytochrome P450RAI-1 or selective cytochrome P450RAI-2 inhibitory activity and methods of obtaining the same US11014460 2004-12-16 US07226951B2 2007-06-05 Jayasree Vasudevan; Liming Wang; Xiaoxia Liu; Kwok Yin Tsang; Ling Li; Janet A. Takeuchi; Thong Vu; Richard Beard; Smita Bhat; Vidyasagar Vuligonda; Roshantha A. Chandraratna
Compounds of formulas 1 through 17 provided in the specification specifically or selectively inhibit either the cytochrome P450RAI-1 enzyme or the cytochrome P450RAI-2 enzyme.
57 O- or S-substituted tetrahydronaphthalene derivatives having retinoid and/or retinoid antagonist-like biological activity US10269270 2002-10-11 US06855832B2 2005-02-15 Vidyasagar Vuligonda; Min Teng; Richard L. Beard; Alan T. Johnson; Yuan Lin; Roshantha A. Chandraratna
Compounds of the formula where the symbols have the meaning described in the application, have retinoid-like or retinoid antagonist-like biological activity.
58 O-or S-substituted tetrahydronaphthalene derivatives having retinoid and/or retinoid antagonist-like biological activity US923897 1997-09-04 US06051731A 2000-04-18 Vidyasagar Vuligonda; Min Teng; Richard L. Beard; Alan T. Johnson; Yuan Lin; Roshantha A. Chandraratna
Compounds of the formula ##STR1## where the symbols have the meaning described in the application, have retinoid-like or retinoid antagonist-like biological activity.
59 Oxygenated alkyl substituted bicyclo alkanes US56467 1987-06-01 US4855322A 1989-08-08 Walter J. Kasha; Chantal S. Burnison
A compound of the formula ##STR1## wherein Q is CO, CH(OR), CR(OH), or CR (OC)-lower alkyl); R is H, or C.sup.1-2 -alkyl;X is hydroxyalkyl,methoxy-C.sup.2-11 -alkyl, ethoxy-C.sup.2-11 -alkyl or oxo-C.sup.2-11 -alkyl, formyl-C.sup.2-11 -alkyl,carboxy-C.sup.2-11 -alkyl or (C.sub.1-2 -alkyl) oxycarbonyl-C.sup.2-11 -alkyl;c is 1 or 2;p or w are 0, 1 or 2 and the sum of p and w is 1 to 4;and a pharmaceutically acceptable salt thereof.
60 Process for the preparation of cyclohexanedionecarboxylic acid derivatives US008445 1987-01-29 US4803268A 1989-02-07 Hans-Georg Brunner; Urs Muller
The present invention relates to a novel, optimized process for the preparation of cyclohexanedionecarboxylic acid derivatives of formula I which can be carried out in a single vessel affording a very good yield, which process comprises heating a reactive carboxylic acid derivative of formula III ##STR1## wherein X is a halide, an alkylsulfonic or arylsulfonic acid radical or the molecular radical ##STR2## which is necessary to form an anhydride and R.sub.1 is alkyl or cycloalkyl, with an alkali metal cyanide or copper cyanide, in an inert organic solvent, to give a mixture, then adding in succession to said mixture, at a temperature in the range from 0.degree. C. to room temperature, zinc chloride, an equimolar amount, with respect to the carboxylic acid derivative of formula III, of a 3,5-cyclohexanedione-1-carboxylic acid derivative of formula II ##STR3## wherein A is an ester or amide radical, and, dropwise, an amine, and, after acidifying the reaction mixture with an aqueous acid, isolating the resultant 4-acyl-3,5-cyclohexanedione-1-carboxylic acid derivative of formula I ##STR4## by extraction. Said cyclohexanedionecarboxylic acid derivatives have herbicidal and plant growth regulating properties.
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