Chalcogen Or Nitrogen Attached Indirectly To The Hetero Ring By Acyclic Nonionic Bonding Patents (Class 549/407)
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Publication number: 20030233002Abstract: Novel processes for producing enantiomerically enriched and enantiomerically pure compositions of 2-acyl substituted chromane compounds, and 2-acylchromane compounds that are intermediates for producing platelet aggregation inhibitors and/or are themselves potent platelet aggregation inhibitors are disclosed. Further disclosed are processes for producing salts such as acid addition salts for such enantiomerically enriched compositions.Type: ApplicationFiled: May 6, 2003Publication date: December 18, 2003Inventors: James Kanter, John J.G. Mullins, Anjali Pandey, Robert Scarborough
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Patent number: 6660871Abstract: Substituted 4H-chromene derivatives are a new class of compounds that bind to Bcl-2 protein and induce apoptosis in tumor cells. The present invention is directed to an efficient synthetic method for the preparation of these compounds from salicylaldehyde derivatives and alkyl cyanoacetates under solid phase.Type: GrantFiled: February 1, 2002Date of Patent: December 9, 2003Assignee: Thomas Jefferson UnversityInventor: Ziwei Huang
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Patent number: 6653488Abstract: A first process for producing a benzopyran carboxamide represented by the general formula [1] includes reacting 3-aminopropionitrile.½ sulfate, N≡CCH2CH2NH2.½(H2SO4), with a benzopyran carboxylic halide represented by the general formula [2], in the presence of a base. A second process for producing the benzopyran carboxamide includes the steps of (a) reacting 3-aminopropionitrile.½ sulfate with a base, thereby forming 3-aminopropionitrile; and (b) reacting the 3-aminopropionitrile with the benzopyran carboxylic halide [2], thereby producing the benzopyran carboxamide. A process for stabilizing 3-aminopropionitrile includes turning the 3-aminopropionitrile into a sulfate of the 3-aminopropionitrile. where R is a straight-chain or non-straight-chain perfluoroalkyl group represented by CnF2n+1 where n is an integer of 1-10; and X is fluorine, chlorine, bromine or iodine.Type: GrantFiled: August 8, 2002Date of Patent: November 25, 2003Assignee: Central Glass Company, LimitedInventors: Takeo Komata, Matsue Kawamura, Nariaki Ii
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Patent number: 6653472Abstract: New intermediates of the formula (II)B described below for the synthesis of amidine derivatives of (−)-6-hydroxy-2,5,7,8-tetramethylchromane-2-carboxylic acid, such as for example (S)-N-{4-[4-[(3,4-dihydro-6-hydroxy-2,5,7,8-tetramethyl-2H-1-benzopyran-2-yl)-carbonyl]-1-piperazinyl]phenyl}-2-thiophenecarboximidamide wherein A′ is X is —Z1—CO; &rgr; is a bond or a heterocycle selected from the group consisting of piperidine, piperazine, homopiperazine, 2-methylpiperazine, 2,5-dimethyl-piperazine and 4-aminopiperidine; Y is —Z2— or —NR3—Z2, R3 is hydrogen, alkyl of 1 to 6 carbon atoms or —COR4, R4 is alkyl of 1 to 6 carbon atoms; Z1 and Z2 independently are a single bond or alkylene of 1 to 6 carbon atoms; and R6 is hydrogen or OH.Type: GrantFiled: April 26, 2002Date of Patent: November 25, 2003Assignee: Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S.)Inventors: Christine Le Breton, Eric Manginot, Jean-Bernard Cazaux
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Patent number: 6646136Abstract: Chroman derivatives of the formula I in which R1 is acyl having 1-6 C atoms, —CO—R5 or an amino protective group, R2 is H or alkyl having 1-6 C atoms, R3, R4 in each case independently of one another are H, alkyl having 1-6 C atoms, CN, Hal or COOR2, R5 is phenyl which is unsubstituted or mono- or disubstituted by alkyl having 1-6 C atoms, OR2 or Hal, X is H, H or O, Hal is F, Cl, Br or I, and their salts, are suitable as intermediates in the synthesis of medicaments.Type: GrantFiled: February 28, 2002Date of Patent: November 11, 2003Assignee: Merck Patent GmbHInventors: Heinz-Herman Bokel, Peter Mackert, Christoph Müramann, Nobert Schweickert
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Patent number: 6638972Abstract: The present invention provides a compound of formula I and the use thereof for the therapeutic treatment of disorders relating to or affected by the 5-HT6 receptor.Type: GrantFiled: October 3, 2002Date of Patent: October 28, 2003Assignee: WyethInventors: Michael Gerard Kelly, Lynne Padilla Greenblatt, Gan Zhang, Yvette L. Palmer, Steven Edward Lenicek
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Patent number: 6638970Abstract: Novel compounds of the general formula: and pharmaceutically acceptable acid addition salts thereof, wherein the compounds are useful in therapy to protect skeletal muscles against damage resulting from trauma or to protect skeletal muscles subsequent to muscle or systemic diseases such as intermittent claudication, to treat shock conditions, to preserve donor tissue and organs used in transplants, in the treatment of cardiovascular diseases including atrial and ventricular arrhythmias, Prinzmetal's (variant) angina, stable angina, and exercise induced angina, congestive heart disease, and myocardial infarction.Type: GrantFiled: February 22, 2001Date of Patent: October 28, 2003Assignee: CV Therapeutics, Inc.Inventors: Elfaith Elzein, Jeff Zablocki, Tim Marquart
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Patent number: 6635634Abstract: This invention relates to new propanolamine derivatives or salts thereof represented by the following formula [I]: Wherein each symbol is as defined in the specification or salts thereof which have gut selective sympathomimetic, anti-ulcerous, anti-pancreatitis, lipolytic, anti-urinary incontinence and anti-pollakiuria activities, to processes for the preparation thereof, to a pharmaceutical composition comprising the same and to a method for the prevention and/or treatment diseases indicated in the specification to a human being or an animal.Type: GrantFiled: February 14, 2002Date of Patent: October 21, 2003Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Kiyoshi Taniguchi, Minoru Sakurai, Naoaki Fujii, Kumi Hosoi, Yasuyo Tomishima, Hisashi Takasugi, Hajime Sogabe, Hirofumi Ishikawa, Naomi Hanioka
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Patent number: 6635650Abstract: The invention relates to compounds of formula (I): A-G1-Cy-G2-Cy-G3-B (I) wherein: A represents NR1C(Q)R2, C(Q)NR2R3 or NR1C(Q)NR2R3, B represents NR1C(Q)R2, C(Q)NR2R3, NR1C(Q)NR2R3, C(Q)OR1, NR1C(Q)OR2 or NR2R3, G1 and G3 represent an optionally substituted alkylene chain, Cy represents a ring structure G2 represents a chain and medicinal products containing the same which are useful in treating or in preventing melatoninergic disorders.Type: GrantFiled: August 8, 2001Date of Patent: October 21, 2003Assignee: Les Laboratoires ServierInventors: Daniel Lesieur, Said Yous, Carole Descamps-Francois, François Lefoulon, Gérald Guillaumet, Marie-Claude Viaud, Caroline Bennejean, Philippe Delagrange, Pierre Renard
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Patent number: 6620947Abstract: Novel processes and intermediates useful in the preparation of 11-oxa prostaglandin analogs are disclosed.Type: GrantFiled: August 26, 2002Date of Patent: September 16, 2003Assignee: Alcon, Inc.Inventors: Pete Delgado, Raymond E. Conrow, William D. Dean, Michael S. Gaines
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Patent number: 6599933Abstract: The object of the present invention is to provide a tocotrienol derivative which is highly water-soluble and shows high bioavailability in the living body and &ggr;-CEHC delivering agent. (A tocotrienolcarboxylic acid ester derivative represented by the general formula (I). (wherein R2 means a carboxylic acid residue having a nitrogen substituent, and R1 and R3 mean a hydrogen atom or a methyl group.Type: GrantFiled: March 2, 2001Date of Patent: July 29, 2003Assignees: Kenko CorporationInventors: Jiro Takata, Takeshi Fukushima, Kazuhiro Imai, Yoshiharu Karube, Kazuhisa Matsunaga, Michihiro Fujiwara, Akihiro Hattori, Ryoji Hidaka, Katsunori Iwasaki, Kenichi Mishima, Shizuko Kobayashi
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Publication number: 20030125571Abstract: The present invention includes a compound having the following general formula (1): 1Type: ApplicationFiled: June 13, 2002Publication date: July 3, 2003Inventors: SungDae Park, HeeAn Kwon, HongKi Kim, PilSu Ho, Kazumi Morikawa, Yoshitake Kanbe, Masahiro Nishimoto, MyungHwa Kim
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Publication number: 20030078258Abstract: This invention is related to novel di-substituted aminomethyl chroman derivatives which are useful in the treatment of beta-3 receptor-mediated conditions.Type: ApplicationFiled: December 7, 2001Publication date: April 24, 2003Inventors: Gaetan H. Ladouceur, William H. Bullock, Steven R. Magnuson, Stephen J. O'Connor, Roger A. Smith, Quanrong Shen, Qingjie Liu, Ning Su, Emil J. Velthuisen, Ann-Marie Campbell, Paul P. Ehrlich
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Publication number: 20030078260Abstract: This invention relates to novel 2,6-substituted chroman derivatives which are useful in the treatment of beta-3 adrenoreceptor-mediated conditions.Type: ApplicationFiled: April 22, 2002Publication date: April 24, 2003Inventors: Stephen J. O'Connor, Gaetan H. Ladouceur, William H. Bullock, Ann-Marie Campbell, Miao Dai, Robert Dally, Jacques Dumas, Holia N. Hatoum-Mokdad, Uday Khire, Wendy Lee, Qingjie Liu, Derek B. Lowe, Steven R. Magnuson, Ning Qi, Tatiana E. Shelekhin, Quanrong Shen, Roger A. Smith, Ming Wang
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Patent number: 6541669Abstract: Disclosed are multibinding compounds which are &bgr;2 adrenergic receptor agonists and are useful in the treatment and prevention of respiratory diseases such as asthma, bronchitis. They are also useful in the treatment of nervous system injury and premature labor.Type: GrantFiled: June 2, 1999Date of Patent: April 1, 2003Assignee: Theravance, Inc.Inventors: Edmund J. Moran, Seok-Ki Choi
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Patent number: 6518264Abstract: Disclosed are azetidine derivatives of formula: their optical isomers, their salts, their preparation and medicaments containing them.Type: GrantFiled: March 9, 2001Date of Patent: February 11, 2003Assignee: Aventis Pharma S.A.Inventors: Daniel Achard, Hervé Bouchard, Jean Bouquerel, Marc Capet, Serg Grisoni, Jean-Luc Malleron, Serge Mignani, Augustin Hittinger
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Publication number: 20030027857Abstract: The object of the present invention is to provide a tocotrienol derivative which is highly water-soluble and shows high bioavailability in the living body and &ggr;-CEHC delivering agent.Type: ApplicationFiled: March 2, 2001Publication date: February 6, 2003Applicant: Jiro TakataInventors: Jiro Takata, Takeshi Fukushima, Kazuhiro Imai, Yoshiharu Karube, Kazuhisa Matsunaga, Michihiro Fujiwara, Akihiro Hattori, Ryoji Hidaka, Katsunori Iwasaki, Kenichi Mishima, Shizuko Kobayashi
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Patent number: 6495546Abstract: Propanolamine derivatives represented by the following formula (I): These derivatives may be &bgr;3 agonists and exert sympathomimetic, anti-ulcerous, anti-pancreatitis, lipolytic and anti-urinary incontinence and anti-pollakiuria activities. Pharmaceutical compositions containing such propanolamine derivatives, methods for the prevention and/or treatment diseases using these propanolamine derivatives, and processes for their preparation are also described.Type: GrantFiled: November 22, 2000Date of Patent: December 17, 2002Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Kiyoshi Taniguchi, Minoru Sakurai, Naoaki Fujii, Kumi Hosoi, Yasuyo Tomishima, Hisashi Takasugi, Hajime Sogabe, Hirofumi Ishikawa, Naomi Hanioka
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Patent number: 6482950Abstract: Squarylium compounds of the formula: wherein Q1 and Q2 are each independently a pyrylium, thiopyrylium, selenopyrylium, benzpyrylium, benzthiopyrylium or benzselenopyrylium nucleus, and R1 and R2 are each independently an aliphatic or cycloaliphatic group, can be prepared by reacting a squaric acid derivative of the formula: with a compound of the formula Q2CH2R2 in the presence of a base. The derivatives of Formula II may be prepared by condensing a 2,3,4,4-tetrahalocyclobut-2-en-1-one with a compound of the formula Q1CH2R1 in the presence of a base to produce a compound of the formula: wherein Q1 and R1 are as defined above, and X represents chlorine or bromine, and hydrolyzing the compound of Formula III.Type: GrantFiled: June 6, 1995Date of Patent: November 19, 2002Assignee: Polaroid CorporationInventors: Paulina P. Garcia, John W. Lee, John L. Marshall, Donald A. McGowan, Anthony J. Puttick, Thomas K. Spencer, Stephen G. Stroud, Stephen J. Telfer, Michael J. Zuraw
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Patent number: 6479540Abstract: Tocol-based compositions of charged amphiphilic and water soluble pharmaceutically active compounds or their charged precursors are prepared by forming a tocol-soluble ion pair with an oppositely charged ion-pair forming compound capable of forming a tocol-soluble ion-pair with the active compound. Also disclosed are novel compounds tocopherolsuccinate-aspartate and tocopherolsuccinate-glutamate, which are useful as ion-pair forming compounds.Type: GrantFiled: September 27, 2000Date of Patent: November 12, 2002Assignee: Sonus Pharmaceuticals, Inc.Inventors: Panayiotis P. Constantinides, Karel J. Lambert, Alexander K. Tustian, Andrew M. Nienstedt
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Patent number: 6479670Abstract: This invention relates to new selective retinoid acid receptor agonists of formula I wherein the symbols are as defined in the specification to their pharmaceutically acceptable salts, individual isomers or to a racemic or non-racemic mixture; to pharmaceutical compositions containing them, and to methods for their use as therapeutic agents.Type: GrantFiled: July 12, 2000Date of Patent: November 12, 2002Assignee: Hoffmann-La Roche Inc.Inventors: Paula Nanette Belloni, Peter Mohr
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Publication number: 20020164498Abstract: The present invention discloses a novel compound useful as the material for a red organic EL device. The novel compound is produced by connecting a benzene ring at the positions 2 and 3 of withdrawing group 2,5-dimethyl-4-(2,2-dicyano)pyrane, and connecting a conjugated donating group at position 5. Using this compound, the EL emission is shifted to the red spectral region, and a higher purity in color for red EL elements is obtained. The synthesis of the compound is easy and the product yield is improved compared to the prior art. Moreover, the red organic EL devices fabricated using the compound have properties that conform with existing NTSC standards.Type: ApplicationFiled: March 19, 2001Publication date: November 7, 2002Inventors: Liang-Jyi Chen, Wen-Kuo Weng, Chun-Neng Ku, Po-Yen Lu
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Publication number: 20020146588Abstract: The present invention discloses a novel compound useful as the material for a red organic EL device. The novel compound is produced by connecting a benzene ring at the positions 2 and 3 of withdrawing group 2, 5-dimethyl-4-(2,2-dicyano)pyrane, and connecting a conjugated donating group at position 5. Using this compound, the EL emission is shifted to the red spectral region, and a higher purity in color for red EL elements is obtained. The synthesis of the compound is easy and the product yield is improved compared to the prior art. Moreover, the red organic EL devices fabricated using the compound have properties that conform with existing NTSC standards.Type: ApplicationFiled: May 16, 2001Publication date: October 10, 2002Inventors: Liang-Jyi Chen, Wen-Kuo Weng, Chun-Neng Ku, Po-Yen Lu
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Publication number: 20020128495Abstract: The present application relates to carboxylic acid amides of general formula 1Type: ApplicationFiled: December 19, 2001Publication date: September 12, 2002Inventors: Henning Priepke, Norbert Hauel, Klaus Damm, Andreas Schnapp
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Patent number: 6429320Abstract: Processes for purifying compounds are disclosed which include reacting (i) a mixture of at least one tocopherol compound or sterol compound, and an alcohol having from about 10 to 30 carbons with (i) one or more boron-containing compounds to form a second mixture of orthoborate esters, wherein the mole ratio of tocopherol, sterol and alcohol to boron is at least about 2.5:1; heating the second mixture to form a residue containing the orthoborate esters; contacting the residue with a compound capable of solvolyzing the orthoborate esters to form a third mixture including the boron-containing compound(s), the alcohol and the tocopherol and/or sterol compound(s); and recovering the tocopherol and/or sterol compound(s).Type: GrantFiled: August 3, 2001Date of Patent: August 6, 2002Assignee: Cognis CorporationInventors: Patrick M. McCurry, Jr., Stephen W. Turner, Carl Pickens
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Patent number: 6403638Abstract: Compounds having the formulas below, where R is H, lower alkyl, or a pharmaceutically acceptable salt, and where R1 represents i-propyl, t-butyl or n-butyl groups, have selective RXR retionoid agonist activity.Type: GrantFiled: March 21, 2000Date of Patent: June 11, 2002Assignee: Allergan Sales, Inc.Inventors: Vidyasagar Vuligonda, Kwok Yin Tsang, Jayasree Vasudevan, Roshantha A. Chandraratna
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Patent number: 6369099Abstract: A method of modifying or altering the structure of a 1&agr;-hydroxylated vitamin D compound to increase its biological activity by altering the conformational equilibrium of the A-ring to favor a chair conformation that presents the 1&agr;-hydroxyl in the axial orientation. This is accomplished by either locking the A-ring chair conformation in a geometry having an axially orientated 1&agr;-hydroxyl, or by the addition of one or more substituents to the A-ring which interact with other substituents in the molecule or on the A-ring to provide a driving force to the A-ring to adopt a chair conformation which presents the 1&agr;-hydroxyl in the axial orientation.Type: GrantFiled: April 20, 2000Date of Patent: April 9, 2002Assignee: Wisconsin Alumni Research FoundationInventors: Hector F. DeLuca, Rafal R. Sicinski
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Patent number: 6369225Abstract: Compounds having Formula 8 wherein the symbols have the meaning defined in the specification are inhibitors of the cytochrome P450RAI (retinoic acid inducible) enzyme, and are used for treating diseases responsive to treatment by retinoids.Type: GrantFiled: August 29, 2000Date of Patent: April 9, 2002Assignee: Allergan Sales, Inc.Inventors: Jayasree Vasudevan, Alan T. Johnson, Dehua Huang, Roshantha A. Chandraratna
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Patent number: 6358995Abstract: The present invention provides a medicament exhibiting excellent retinoic acid receptor agonism. A Carboxylic acid derivative having a fused ring which is represented by the following formula or a pharmacologically acceptable salt thereof: {wherein the symbol represents a single bond or a double bond; X, Y, Z, P, Q, U, V and W are each a group represented by the formula: —O— or —S—, or a group represented by the formula: [wherein Rk (k: 1 to 8) is hydrogen, halogeno, optionally substituted lower alkyl or the like, with either of R7 and R8 being a group represented by the formula: (wherein A and B are each independently an optionally substituted aromatic hydrocarbon ring or an optionally substituted unsaturated heterocycle; and D is optionally protected carboxyl)]}.Type: GrantFiled: July 21, 2000Date of Patent: March 19, 2002Assignee: Eisai Co., Ltd.Inventors: Katsuya Tagami, Hiroyuki Yoshimura, Mitsuo Nagai, Shigeki Hibi, Kouichi Kikuchi, Takashi Sato, Makoto Okita, Yasushi Okamoto, Yumiko Nagasaka, Naoki Kobayashi, Takayuki Hida, Kenji Tai, Naoki Tokuhara, Seiichi Kobayashi
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Patent number: 6350754Abstract: The present invention relates to novel 3-(cycloalkano-heteroarylidenyl)-2-indolinone compounds and physiologically acceptable salts and prodrugs thereof which are expected to modulate the activity of protein tyrosine kinases and therefore to be useful in the prevention and treatment of protein tyrosine kinase related cellular disorders such as cancer.Type: GrantFiled: January 12, 2000Date of Patent: February 26, 2002Assignee: Sugen, Inc.Inventors: Peng Cho Tang, Li Sun, Gerald McMahon
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Patent number: 6350453Abstract: A source of material known as a byproduct solution of Bixa orellana seed components, which is obtained as an oily material after the bulk of annatto color, is removed from either the aqueous extract or solvent extract of annatto seeds. Further, this byproduct contains a tocotrienol component and a geranylgeraniol component and can be used as a source for the recovery of a tocotrienol component and a geranylgeraniol component.Type: GrantFiled: May 24, 2000Date of Patent: February 26, 2002Assignee: American River Nutrition, Inc.Inventors: Barrie Tan, John Foley
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Patent number: 6348605Abstract: 3-(Hydroxymethyl)chromen-4-ones of formula (I) are described and a process for preparing said compounds.Type: GrantFiled: June 14, 2001Date of Patent: February 19, 2002Assignee: Ferrer Internacional, S.A.Inventors: Rafael Foguet, Jordi Bolos, Aurelio Sacristan, Josep M. Castello, José A. Ortiz
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Patent number: 6319930Abstract: The invention relates to compounds of formula (I): A—G1—Cy—G2—Cy—G3—B (I) wherein: A represents NR1C(Q)R2, C(Q)NR2R3 or NR1C(Q)NR2R3, B represents NR1C(Q)R2, C(Q)NR2R3, NR1C(Q)NR2R3, C(Q)OR1, NR1C(Q)OR2 or NR2R3, G1 and G3 represent an optionally substituted alkylene chain, Cy represents a ring structure and G2 represents a chain and medicinal products containing the same which are useful in treating or in preventing melatoninergic disorders.Type: GrantFiled: March 24, 2000Date of Patent: November 20, 2001Assignee: Adir et CompagnieInventors: Daniel Lesieur, Said Yous, Carole Descamps-Francois, François Lefoulon, Gérald Guillaumet, Marie-Claude Viaud, Caroline Bennejean, Philippe Delagrange, Pierre Renard
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Patent number: 6313160Abstract: The invention relates to compounds of formula (I): wherein: R1, R2 and R3 are as defined in the description, X is as defined in the description, Y represents an oxygen atom, a sulphur atom, a C(H)q group, SO or SO2, n is equal to from 0 to 5, A represents a NR5R6 group, and medicinal products containing the same which are useful in treating or in preventing melatoninergic disorders.Type: GrantFiled: November 12, 1999Date of Patent: November 6, 2001Assignee: Adir et CompagnieInventors: Gérald Guillaumet, Marie-Claude Viaud, Ahmed Mamai, Isabelle Charton, Pierre Renard, Caroline Bennejean, Béatrice Guardiola, Philippe Daubos
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Patent number: 6310074Abstract: The invention relates to compound of formula (I): A—G1—Cy—G2—Cy′—G3—B (I) wherein: A represents a grouping NR1C(Q)R2, C(Q)NR2R3 or NR1C(Q)NR2R3, B represents a grouping NR1C(Q)R2, NR1C(Q)NR2R3, C(Q)NR2R3, C(Q)OR1, NR1C(Q)OR2 or NR2R3, G1 and G3 represent an optionally substituted alkylene chain, Cy and Cy′, which are different, represent a ring structure or G2 represents a chain and medicinal products containing the same are useful in treating or in preventing melatoninergic disorders.Type: GrantFiled: May 18, 2000Date of Patent: October 30, 2001Assignee: Adir et CompagnieInventors: Patrick Depreux, Said Yous, Gwenael Cheve, Gérald Guillaumet, Marie-Claude Viaud, Carlos Larraya, Caroline Bennejean, Philippe Delagrange, Pierre Renard, Carole Descamps-Francois
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Patent number: 6297273Abstract: Disclosed and claimed are cocoa extracts, compounds, combinations thereof and compositions containing the same, such as polyphenols or procyanidins, methods for preparing such extracts, compounds and compositions, as well as uses for them, especially a polymeric compound of the formula An, wherein A is a monomer of the formula: wherein n is an integer from 2 to 18, such that there is at least one terminal monomeric unit A, and one or a plurality of additional monomeric units; R is 3-(&agr;)-OH, 3-(&bgr;)-OH, 3-(&agr;)-O-sugar, or 3-(&bgr;)-O-sugar; bonding between adjacent monomers takes place at positions 4, 6 or 8; a bond of an additional monomeric unit in position 4 has alpha or beta stereochemistry; X, Y and Z are selected from the group consisting of monomeric unit A, hydrogen, and a sugar, with the provisos that as to the at least one terminal monomeric unit, bonding of the additional monomeric unit thereto (the bonding of the additional monomeric unit adjacent to the terminal monoType: GrantFiled: April 2, 1997Date of Patent: October 2, 2001Assignee: Mars, Inc.Inventor: Leo J. Romanczyk, Jr.
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Publication number: 20010021710Abstract: The present invention relates to therapeutically active compounds of formula I 1Type: ApplicationFiled: October 27, 1997Publication date: September 13, 2001Inventors: POUL JACOBSEN, SVEND TREPPENDAHL, PAUL STANLEY BURY, ANDERS KANSTRUP, LISE BROWN CHRISTIANSEN
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Patent number: 6288071Abstract: Pesticidally active cyclohexadienyl derivative compounds of the formula I that are esters, oximes or amides are claimed. These compounds may be used as fungicides, acaricides and insecticides in plant protection.Type: GrantFiled: December 10, 1998Date of Patent: September 11, 2001Assignee: Bayer AktiengesellschaftInventors: Henry Szczepanski, Martin Zeller, Ottmar Franz Hüter
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Publication number: 20010018530Abstract: The invention relates to the use of substituted aminomethyl-chromans for the treatment of neuronal degeneration and for the promotion of neuronal regeneration in cerebral injuries and chronic disorders of the nervous system.Type: ApplicationFiled: March 9, 2001Publication date: August 30, 2001Inventors: Thomas Fahrig, Irene Gerlach, Ervin Horvath, Reinhard Jork
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Patent number: 6281240Abstract: This invention provides methods of treating secretory diarrhea or cystic fibrosis in a mammal which comprises administering to a mammal in need thereof an effective amount of diarylsulfonylurea. This invention also describes specific diarylsulfonylureas for use in treating secretory diarrhea or cystic fibrosis.Type: GrantFiled: January 31, 2000Date of Patent: August 28, 2001Assignee: Eli Lilly and CompanyInventor: Bruce D Schultz
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Patent number: 6221900Abstract: The invention provides BTK inhibitors, methods for their identification and use, and pharmaceutical compositions comprising BTK inhibitors.Type: GrantFiled: October 4, 1999Date of Patent: April 24, 2001Assignee: Hughes InstituteInventors: Fatih M. Uckun, Yaguo Zheng, Sutapa Ghosh
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Patent number: 6147224Abstract: Compounds of Formula 1, Formula 2 or Formula 3 where X is O, S, or (CR.sub.1 R.sub.1).sub.n where n is 0, 1 or 2; Y is a bivalent radical having Formula 4 or Formula 5 where o is an integer from 1 to 4 ##STR1## or Y is a bivalent aryl or 5 or 6 membered heteroaryl radical having 1 to 3 heteroatoms selected from N, S and O, said aryl or heteroaryl groups being unsubstituted, or substituted with 1 to 3 C.sub.1-6 alkyl or with 1 to 3 C.sub.1-6 fluoroalkyl groups; and the remaining symbols have the meaning described in the specification, have RXR selective retinoid agonist-like activity.Type: GrantFiled: October 1, 1998Date of Patent: November 14, 2000Assignee: Allergan Sales, Inc.Inventors: Vidyasagar Vuligonda, Kwok Yin Tsang, Jayasree Vasudevan, Roshantha A. Chandraratna
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Patent number: 6136985Abstract: The present invention provides CLA esters and uses thereof. More particularly, the present invention provides a composition for topical use comprising CLA esters and a topical carrier. In addition, the present invention specifically provides tocopheryl CLA esters, ascorbyl CLA esters and retinyl CLA esters.Type: GrantFiled: December 21, 1998Date of Patent: October 24, 2000Assignee: DCV, Inc.Inventor: James R. Millis
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Patent number: 6136986Abstract: The invention relates to a process for preparing substituted chroman derivatives of the general formula VII, ##STR1## where X is the group --CN, --COOR.sup.3, --CHO, --CH.sub.2 OR.sup.7 or --CH(OR.sup.8).sub.2,R.sup.2 is a C.sub.1 -C.sub.23 -alkyl, C.sub.2 -C.sub.23 -alkenyl, C.sub.6 -C.sub.18 -aryl or C.sub.7 -C.sub.18 -aralkyl radical,R.sup.3 is hydrogen or an optionally substituted C.sub.1 -C.sub.4 -alkyl radical,R.sup.4, R.sup.5, R.sup.6 are, independently of one another, hydrogen or a C.sub.1 -C.sub.4 -alkyl radical,R.sup.7 is hydrogen or a C.sub.1 -C.sub.4 -alkyl radical,R.sup.8 is a C.sub.1 -C.sub.4 -alkyl radical, or the two radicals are a C.sub.2 -C.sub.6 -alkylene radical which links the two oxygen atoms to form a cyclic acetal and is optionally branched or may carry one or two carboxyl groups, cyclohexyl or phenyl radicals,and to the novel intermediates of the process.Type: GrantFiled: December 13, 1999Date of Patent: October 24, 2000Assignee: BASF AktiengesellschaftInventors: Rainer Sturmer, Kai-Uwe Baldenius
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Patent number: 6124347Abstract: Disclosed are chromene derivatives represented by the following formula: ##STR1## wherein R.sup.1 s represent alkyl, alkoxy or like groups, R.sup.2 represents a hydrogen atom or an alkyl group, R.sup.3 represents a substituted or unsubstituted phenyl, naphthyl or heterocyclic group, and m stands for an integer of from 0 to 4, and their salts; and pharmaceuticals containing them as effective ingredients. The chromene derivatives and their salts show excellent AGE formation inhibitory action and are useful as preventives and therapeutics for diabetic complications.Type: GrantFiled: September 29, 1998Date of Patent: September 26, 2000Assignee: SSP Co., Ltd.Inventors: Fumio Ishii, Haruyoshi Honda, Fujiko Konno, Tomomi Okada, Terumitsu Kaihoh, Yoshihiro Nagao, Susumu Sato, Hideaki Matsuda
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Patent number: 6100268Abstract: The present invention is concerned with compounds of formula ##STR1## the pharmaceutically acceptable acid addition salts thereof, and the stereochemically isomeric forms thereof, wherein R.sup.1 is hydrogen or C.sub.1-6 alkyl; R.sup.2 is hydrogen or C.sub.1-6 alkyl; R.sup.3 is hydrogen or C.sub.1-6 -alkyl; R.sup.4 is hydrogen, halo, C.sub.1-6 alkyl, hydroxy, C.sub.1-6 alkyloxy, aryloxy or arylmethoxy; R.sup.5 and R.sup.6 designate R.sup.5a and R.sup.6a wherein R.sup.5a and R.sup.6a taken together form a bivalent radical; or R.sup.5 and R.sup.6 can designate R.sup.5b and R.sup.6b wherein R.sup.5b is hydrogen and R.sup.6b is a heterocycle or an optionally substituted alkenyl or alkynyl group; or R.sup.5 and R.sup.6 designate R.sup.5c and R.sup.6c, wherein R.sup.5c and R.sup.6c are hydrogen, halo, C.sub.1-6 alkyl, C.sub.3-6 alkenyl, C.sub.3-6 alkynyl, hydroxy, C.sub.1-6 alkyloxy, cyano, aminoC.sub.1-6 alkyl, carboxyl, C.sub.1-6 alkyloxycarbonyl, nitro, amino, aminocarbonyl, C.sub.Type: GrantFiled: July 28, 1998Date of Patent: August 8, 2000Assignee: Janssen Pharmaceutica, N.V.Inventors: Guy Rosalia Eugene Van Lommen, Piet Tom Bert Paul Wigerinck, Marcel Frans Leopold De Bruyn, Wim Gaston Verschueren, Marc Francis Josephine Schroven
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Patent number: 6090826Abstract: Compounds of the formula ##STR1## where R.sub.1 and R.sub.2, independently are alkyl groups having 2 to 8 carbons; R.sub.3 is hydrogen or lower alkyl; X is S, O or N--R.sub.4 where R.sub.4 is hydrogen or lower alkyl; Y is pyridyl, thienyl, furyl, pyridazinyl, pyrimidinyl, and pyrazinyl; A is (CH.sub.2).sub.n where n is 0-5, or lower branched chain alkyl, alkenyl having 2 to 6 carbons and 1 or 2 double bonds, alkynyl having 2 to 6 carbons and 1 or 2 triple bonds; B is hydrogen, COOH or a salt thereof, COOR.sub.5, CONR.sub.6 R.sub.7, --CH.sub.2 OH, CH.sub.2 OR.sub.8, CH.sub.2 OCOR.sub.8, CHO, CH(OR.sub.9).sub.2, CHOR.sub.10 O, --COR.sub.11, CR.sub.11 (OR.sub.9).sub.2, or CR.sub.11 OR.sub.10 O, where R.sub.5 is alkyl of 1 to 10 carbons, or cycloalkyl of 5 to 10 carbons, or R.sub.5 is phenyl or lower alkylphenyl, R.sub.6 and R.sub.7 independently are hydrogen, alkyl of 1 to 10 carbons, or cycloalkyl of 5 to 10 carbons, or phenyl or lower alkylphenyl, R.sub.Type: GrantFiled: February 25, 1998Date of Patent: July 18, 2000Assignee: Allergan Sales, Inc.Inventor: Roshantha A. S. Chandraratna
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Patent number: 6051722Abstract: The present invention provides, as heteroaromatic compounds made functional so as to be used for nonlinear optical materials, compounds represented by the following general formula (1), and also provides polymers obtained from these and nonlinear optical parts comprising such polymers. In the formula, Ar.sup.1 and Ar.sup.2 each represents a divalent aromatic group; R.sup.1, R.sup.2 and R.sup.3 each represents an atom or a group independently selected from a hydrogen atom or an alkyl group and an aromatic group; X.sup.1 represents a monovalent organic group; n represents an integer of 2 to 12; and Z.sup.1 and Z.sup.2 each represents a group independently selected from electron attractive functional groups.Type: GrantFiled: July 6, 1998Date of Patent: April 18, 2000Assignee: Hitachi Chemical Company, Ltd.Inventors: Yutaka Honda, Iwao Fukuchi, Kwan-Yue Alex Jen
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Patent number: 6028092Abstract: This invention relates to novel formulations of salts of certain benzopyran compounds, to compositions containing them and their use in the treatment of certain disorders.Type: GrantFiled: June 17, 1998Date of Patent: February 22, 2000Assignee: SmithKline Beecham p.l.cInventors: Christopher John Banton, Phillip Christopher Buxton
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Patent number: 6020504Abstract: Chroman derivatives of the general formula: ##STR1## in which R.sup.1 is hydrogen or C.sub.1-4 -alkyl; R.sup.2 is C.sub.1-6 -alkyl, C.sub.3-6 -cycloalkyl, optionally substituted aryl or optionally substituted aryl-C.sub.1-6 -alkyl; R.sup.3, R.sup.5 and R.sup.6 independently of one another are hydrogen, halogen, C.sub.1-4 -alkyl or optionally substituted aryl; and R.sup.4 is C.sub.1-6 -alkyl, C.sub.3-6 -cycloalkyl, (C.sub.1-6 -alkoxy)methyl, optionally substituted aryl, optionally substituted aryl-C.sub.1-6 -alkyl, C-alkanoyl or optionally substituted aroyl, are obtained from hydroquinone derivatives and alkenes in the presence of Lewis acids. The chroman derivatives (I) are intermediates in the synthesis of pharmaceutical active ingredients, for example, of hypolipidemics.Type: GrantFiled: November 10, 1998Date of Patent: February 1, 2000Assignee: Lonza AGInventor: Barry Jackson