Polycyclo Ring System Patents (Class 562/466)
  • Publication number: 20040092748
    Abstract: Derivatives of C2-substituted indan-1-ol compounds of formula I: 1
    Type: Application
    Filed: October 27, 2003
    Publication date: May 13, 2004
    Applicant: Aventis Pharma Deutschland GmBH
    Inventors: Gerhard Jaehne, Volker Krone, Martin Bickel, Matthias Gossel
  • Publication number: 20040092749
    Abstract: Polysubstituted indan-1-ol compounds, methods for their preparation; and methods for their use are disclosed herein.
    Type: Application
    Filed: October 27, 2003
    Publication date: May 13, 2004
    Applicant: Aventis Pharma Deutschland GmBH
    Inventors: Gerhard Jaehne, Volker Krone, Martin Bickel, Matthias Gossel
  • Publication number: 20040063963
    Abstract: The present invention provides a binaphthol compound represented by formula [1]: 1
    Type: Application
    Filed: July 1, 2003
    Publication date: April 1, 2004
    Inventors: Ryuzo Ueno, Masaya Kitayama, Kenji Minami, Hiroyuki Wakamori
  • Publication number: 20040042981
    Abstract: The present invention relates to novel compounds, termed serpentemycins, of the formula (I) 1
    Type: Application
    Filed: June 27, 2003
    Publication date: March 4, 2004
    Applicant: Aventis Pharma Deutschland GmbH
    Inventors: Laszlo Vertesy, Michael Kurz, Joachim Wink
  • Patent number: 6686386
    Abstract: The present invention relates to pharmaceutical and cosmetic compositions comprising at least one agonist ligand, which is specific for receptors of the RAR-&ggr; type, which are characterized as inducers of apoptosis in at least one cell population in which apoptosis can be induced by activating receptors of the RAR-&ggr; type. In one aspect of the present invention, there is provided a method of combating photoinduced or chronological ageing of skin, said method comprising administering an effective amount of at least one agonist ligand which is specific for receptors of the RAR-&ggr; type to combat photoinduced or chronological aging of skin, wherein the agonist ligand has a ratio R which is equal to or greater than 10.
    Type: Grant
    Filed: November 2, 1999
    Date of Patent: February 3, 2004
    Assignee: Galderma Research & Development S.N.C.
    Inventors: Laszlo Fesus, Zsuzsa Szondy, Uwe Reichert
  • Patent number: 6683111
    Abstract: The present invention relates to compounds of the general formula (I) The compounds are useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR).
    Type: Grant
    Filed: October 25, 2001
    Date of Patent: January 27, 2004
    Assignees: Novo Nordisk A/S, Dr. Reddy's Research Foundation
    Inventors: Lone Jeppesen, Paul Stanley Bury, Per Sauerberg
  • Publication number: 20030220315
    Abstract: Alkenyldiarylmethane (ADAM) compounds have been found effective as anti-HIV agents. Novel ADAM compounds, their pharmaceutical formulations and a method of using same to treat viral infections are described.
    Type: Application
    Filed: May 27, 2003
    Publication date: November 27, 2003
    Inventors: Mark S. Cushman, Agustin Casimiro-Garcia, William G. Rice
  • Publication number: 20030212293
    Abstract: A method for transferring amino acid into ketone acid (ester) may obtain ketone acid (ester) at low cost. The method uses sodium hypochlorous acid as oxidizing agent and proceeds oxidation reaction with amino acid or its derivatives so as to obtain ketone acid and its derivatives. The sodium hypochlorous acid is easily to get with low cost and the conditions of the reaction are mild so that the method meets the needs of the industry.
    Type: Application
    Filed: May 10, 2002
    Publication date: November 13, 2003
    Inventor: Chung-Jang Chang
  • Patent number: 6632963
    Abstract: Novel pharmaceutically/cosmetically-active bicyclic aromatic compounds have the structural formula (I): in which Ar1 is a radical having one of the structural formulae (a)-(c): Ar2 is a radical having one of the following formulae (d)-(h): and X is a radical having one of the following formulae (i)-(l): and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.
    Type: Grant
    Filed: March 29, 1999
    Date of Patent: October 14, 2003
    Assignee: Galderma Research & Development S.N.C.
    Inventor: Jean-Michel Bernardon
  • Publication number: 20030176506
    Abstract: The present invention provides compounds that are inducers or inhibitors of apoptosis or apoptosis preceded by cell-cycle arrest. In addition, the present invention provides pharmaceutical compositions and methods for treating mammals with leukemia or other forms of cancer or for treating disease conditions caused by apoptosis of cells.
    Type: Application
    Filed: December 2, 2002
    Publication date: September 18, 2003
    Inventors: Marcia J. Dawson, Joseph A. Fontana, Xiao-kun Zhang, Mark Leid, Ling Jong, Peter D. Hobbs
  • Patent number: 6610883
    Abstract: Compounds, compositions, and methods for modulating processes mediated by Retinoid X Receptors using retinoid-like compounds which have activity selective for members of the subclass of Retinoid X Receptors (RXRs), in preference to members of the subclass of Retinoic Acid Receptors (RARs). Examples of such compounds are bicyclic benzyl, pyridinyl, thiophene, furanyl, pyrrole, and polyenoic acid derivatives including carbocyclic polyenoic acids. The disclosed methods employ compounds for modulating processes selectively mediated by Retinoid X Receptors.
    Type: Grant
    Filed: July 13, 1998
    Date of Patent: August 26, 2003
    Assignee: Ligand Pharmaceuticals, Inc.
    Inventors: Marcus F. Boehm, Richard A. Heyman, Lin Zhi, Chan Kou (Jack) Hwang, Steve White, Alex Nadzan
  • Patent number: 6610877
    Abstract: Compounds of the formula wherein R1 is a residue of the formula and R2-R10 have the significance given in the specification can be used as pharmaceuticals, particularly for the repair of photodamaged skin, other dermatological conditions, and oncological indications.
    Type: Grant
    Filed: August 1, 1997
    Date of Patent: August 26, 2003
    Assignee: Hoffman-La Roche Inc.
    Inventors: Michael Klaus, Peter Mohr
  • Patent number: 6603040
    Abstract: Compounds useful as surface coating agents, including compounds of the formula: wherein X1 comprises a first photoreactive species; X2 comprises a second photoreactive species; Y comprises a nonpolymeric core molecule comprising an aromatic group; and Z comprises at least one charged group. The Y core can include an aromatic group such as a benzene radical, the charged groups Z can be independently selected from the organic acids that include sulfonic acid, carboxylic acid, and phosphoric acid, and the photoreactive species of X1 and X2 can independently be aryl ketones, such as those selected from the group acetophenone, benzophenone, anthraquinone, anthrone, and anthrone-like heterocycles, and their substituted derivatives.
    Type: Grant
    Filed: June 25, 2001
    Date of Patent: August 5, 2003
    Assignee: SurModics, Inc.
    Inventor: Dale G. Swan
  • Patent number: 6603012
    Abstract: New compounds containing bicyclic fused rings, one of which being a phenyl moiety connected by an aliphatic chain to a cycloalkyl or aryl moiety, and pharmaceutically active salts thereof are useful as RAR selective retinoid agonists. Furthermore, such retinoic acid receptor agonists, particularly retinoic acid receptor &ggr; (RAR&ggr;) selective agonists, are useful for the treatment of emphysema and associated pulmonary diseases, as well as for the therapy and prophylaxis of dermatological disorders, for the therapy and prophylaxis of malignant and premalignant epithelial lesions, tumors and precancerous changes of the mucous membrane in the mouth, tongue, larynx, esophagus, bladder, cervix and colon.
    Type: Grant
    Filed: April 23, 2001
    Date of Patent: August 5, 2003
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Paula Nanette Belloni, Synese Jolidon, Michael Klaus, Jean-Marc Lapierre
  • Publication number: 20030139473
    Abstract: Novel compounds of the general formula (I), the use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds may be useful in the treatment and/or prevention of conditions mediated by Peroxisome Proliferator-Activated Receptors (PPAR), in particular the PPAR&dgr; suptype.
    Type: Application
    Filed: July 19, 2002
    Publication date: July 24, 2003
    Inventors: Lone Jeppesen, Paul Stanley Bury, John Patrick Mogensen, Ingrid Pettersson, Per Sauerberg
  • Patent number: 6586463
    Abstract: Compounds having the general structure: which are useful for the treatment of a variety of diseases and conditions, such as bone disorders.
    Type: Grant
    Filed: September 4, 2001
    Date of Patent: July 1, 2003
    Assignee: The Procter & Gamble Company
    Inventors: Mitchell Anthony deLong, David Lindsey Soper, John August Wos, Biswanath De
  • Patent number: 6562998
    Abstract: Granular product of 2-hydroxynaphthalene-3-carboxylic acid with well-suppressed dusting tendency, and process for preparing the same is provided. Granular product of 2-hydroxynaphthalene-3-carboxylic acid having an average particle size of 150 &mgr;m or more and a hardness of 70-3000 g, and a process for preparing the same comprising the steps of dry compressing powdery 2-hydroxynaphthalene-3-carboxylic acid to give compressed material and pulverizing and classifying the same.
    Type: Grant
    Filed: June 26, 2001
    Date of Patent: May 13, 2003
    Assignee: Kabushiki Kaisha Ueno Seiyako Oyo Kenkyujo
    Inventors: Ryuzo Ueno, Masaya Kitayama, Nobutaka Izumichi, Syungo Nara, Masaharu Kittaka
  • Patent number: 6555577
    Abstract: The present invention relates to compounds of the general formula (I) The compounds are useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR).
    Type: Grant
    Filed: January 26, 2001
    Date of Patent: April 29, 2003
    Assignee: Novo Nordisk A/S
    Inventors: John Patrick Mogensen, Per Sauerberg, Paul Stanley Bury, Lone Jeppesen, Ingrid Pettersson
  • Patent number: 6555704
    Abstract: A method is provided for the preparation of alpha-aryl-propionic acids such as ibuprofen by carbonylating the corresponding 1-arylethyl halide in an acidic aqueous medium containing a palladium catalyst. In the preparation of ibuprofen, 1-(4′-isobutylphenyl)ethyl halide is reacted with carbon monoxide in an acidic aqueous medium containing a palladium catalyst.
    Type: Grant
    Filed: May 22, 1995
    Date of Patent: April 29, 2003
    Assignee: BASF Corporation
    Inventor: Varadaraj Elango
  • Patent number: 6521646
    Abstract: Compounds of the formula (I) and their physiologically acceptable salts and solvates are useful as integrin-inhibiting substances. They are especially useful in the prophylaxis and treatment of cardiovascular disorders, of thrombosis, cardiac infarction, coronary heart diseases, arteriosclerosis, osteoporosis, in pathological conditions that are caused or propagated by angiogenesis and in tumor therapy.
    Type: Grant
    Filed: October 15, 2001
    Date of Patent: February 18, 2003
    Assignee: Merck Patent GmbH
    Inventors: Wolfgang Stähle, Rudolf Gottschlich, Simon Goodman
  • Publication number: 20030018207
    Abstract: The present invention relates to certain phenalkyloxy-phenyl derivatives of formula (I) and analogs, to a process for preparing such compounds, having the utility in clinical conditions associated with insulin resistance, to methods for their therapeutic use and to pharmaceutical compositions containing them.
    Type: Application
    Filed: June 3, 2002
    Publication date: January 23, 2003
    Inventors: Jonas Fagerhag, Lanna Li, Eva-Lotte Linstedt Alstermark
  • Publication number: 20030008882
    Abstract: The present invention relates to compounds and pharmaceutical compositions which are proteomimetic and to methods for inhibiting the interaction of an alpha-helical protein with another protein or binding site. Methods for treating diseases or conditions which are modulated through interactions between alpha helical proteins and their binding sites are other aspects of the invention.
    Type: Application
    Filed: May 8, 2002
    Publication date: January 9, 2003
    Inventors: Andrew D. Hamilton, Justin Ernst, Brendan P. Orner
  • Patent number: 6495546
    Abstract: 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: Grant
    Filed: November 22, 2000
    Date of Patent: December 17, 2002
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Kiyoshi Taniguchi, Minoru Sakurai, Naoaki Fujii, Kumi Hosoi, Yasuyo Tomishima, Hisashi Takasugi, Hajime Sogabe, Hirofumi Ishikawa, Naomi Hanioka
  • Patent number: 6479549
    Abstract: A novel carnosic acid derivative for promoting the synthesis of nerve growth factor (NGF), a composition comprising the carnosic acid derivative as an effective ingredient, as well as, a method of promoting the synthesis of NGF comprising administering an effective amount of the carnosic acid derivative as an effective ingredient to a subject requiring such promotion. The carnosic acid derivative, composition and method according to the present invention can safely and efficiently promote the production of NGF in the living body, without being accompanied by a side effect such as a loss of a quantitative balance of hormones in the living body.
    Type: Grant
    Filed: February 28, 2001
    Date of Patent: November 12, 2002
    Assignee: Nagase & Company, Ltd.
    Inventors: Kunio Kosaka, Toshitsugu Miyazaki, Toshio Yokoi
  • Publication number: 20020151720
    Abstract: Novel naphthol derivatives, and various azo compounds and metal complexes prepared by using the derivatives are provided.
    Type: Application
    Filed: January 16, 2002
    Publication date: October 17, 2002
    Inventors: Ryuzo Ueno, Masaya Kitayama, Kenji Minami, Hiroyuki Wakamori
  • Publication number: 20020120153
    Abstract: A method of producing a compound of the formula: 1
    Type: Application
    Filed: February 15, 2001
    Publication date: August 29, 2002
    Inventor: M. Mahmun Hossain
  • Patent number: 6433021
    Abstract: Indane compounds of general formulae (1) to (4) and their pharmaceutical use, particularly to achieve mast cell stabilising activity and/or anti-inflammatory activity are described.
    Type: Grant
    Filed: December 3, 1999
    Date of Patent: August 13, 2002
    Assignee: Venantius Limited
    Inventors: Neil Frankish, Helen Sheridan, John Walsh, Michael Jordan
  • Patent number: 6403638
    Abstract: 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: Grant
    Filed: March 21, 2000
    Date of Patent: June 11, 2002
    Assignee: Allergan Sales, Inc.
    Inventors: Vidyasagar Vuligonda, Kwok Yin Tsang, Jayasree Vasudevan, Roshantha A. Chandraratna
  • Patent number: 6387951
    Abstract: Compounds having Formulas 5 and 6 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: Grant
    Filed: August 29, 2000
    Date of Patent: May 14, 2002
    Assignee: Allergan Sales, Inc.
    Inventors: Jayasree Vasudevan, Alan T. Johnson, Liming Wang, Dehua Huang, Roshantha A. Chandraratna
  • Publication number: 20020002290
    Abstract: 1
    Type: Application
    Filed: June 14, 2001
    Publication date: January 3, 2002
    Applicant: Secretary of State for Defence in her Britannic Majesty's Government of the United Kingdom
    Inventors: Graeme P. Nicholson, Mark J. Kan, Gareth Williams, Michael G. Drew, Paul D. Beer
  • Patent number: 6326369
    Abstract: A compound of the formula: wherein R1 and R2 each represents a lower alkyl, or R1 and R2 may be bonded together to form a ring; X represents a spacer of which the number of atoms constituting the principal chain is 1 to 15; Y represents an acyl, or a hydroxy, an amino or an aromatic group, each of which may be substituted; and ring A represents a 5- to 8-membered ring which may be further substituted apart from —X—Y, or a salt thereof is useful as a pharmaceutical composition for preventing or treating disease related to mitochondrial dysfunction.
    Type: Grant
    Filed: July 6, 1999
    Date of Patent: December 4, 2001
    Assignee: Takeda Chemicals Industries, Ltd.
    Inventors: Kaneyoshi Kato, Taiichi Ohra, Masaomi Miyamoto
  • Patent number: 6316009
    Abstract: “Biphenyl derivatives substituted with an aromatic or heteroaromatic radical, and pharmaceutical and cosmetic compositions containing them” in which: Ar represents an aromatic or a heteroaromatic radical optionally substituted, in particular, with an alkyl or a carboxyl group, R2 and R3 represent, in particular, H or alkyl, or R2 and R3, taken together, form a 5- or 6-membered ring, R4 and R5 represent, in particular, H or halogen, R6 represents, in particular, H or lower alkyl, and the salts of the compounds of formula (I). These compounds can be used in particular in the treatment of dermatological complaints associated with a keratinization disorder, and for combating ageing of the skin.
    Type: Grant
    Filed: April 6, 1999
    Date of Patent: November 13, 2001
    Assignee: Galderma Research & Development
    Inventors: Jean-Michel Bernardon, Philippe Nedoncelle
  • Patent number: 6306899
    Abstract: This invention relates to anti-viral drugs such as Helioxanthin and its analogs. The present compounds may be used alone or in combination with other drugs for the treatment of Hepatitis B virus (HBV), Hepatitis C virus (HCV), Yellow Fever, Dengue Virus, Japanese Encephalitis, West Nile virus and related flaviviruses. In addition, compounds according to the present invention can be used to prevent hepatoma secondary to virus infection as well as other infections or disease states which are secondary to the virus infection.
    Type: Grant
    Filed: August 23, 1999
    Date of Patent: October 23, 2001
    Assignees: Yale University, N. Y. Mu, N.T.U., V.G.H
    Inventors: Yung-Chi Cheng, Chen-Kung Chou, Lei Fu, Yueh-Hsiung Kuo, Sheau-Farn Yeh, Juliang Zhu, Yonglian Zhu
  • Patent number: 6248781
    Abstract: The present invention relates to compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, Ar, X, Q, A, Y and Z are as defined in the specification. These compounds are useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR).
    Type: Grant
    Filed: October 19, 1999
    Date of Patent: June 19, 2001
    Assignees: Novo Nordisk A/S, Dr. Reddy's Research Foundation
    Inventors: Lone Jeppesen, Paul Stanley Bury, Per Sauerberg
  • Patent number: 6242635
    Abstract: A process for producing a 2-aralkyl-3-hydroxypropionic acid (or its ester), comprising the steps of: reacting a 3-hydroxy-2-methylene-3-arylpropionic acid ester, easily obtained by the reaction of an arylaldehyde with an acrylic acid ester, with an acid anhydride to form a 2-aralkylidene-3-acyloxypropionic acid ester; subjecting the same to hydrolysis or alcoholysis; and reducing the resulting 2-aralkylidene-3-hydroxypropionic acid or its ester. The reduction step may be conducted in the presence of a base.
    Type: Grant
    Filed: September 18, 1998
    Date of Patent: June 5, 2001
    Assignee: Ajinomoto Co., Inc.
    Inventors: Takayuki Suzuki, Takayuki Hamada, Kunisuke Izawa
  • Patent number: 6242493
    Abstract: Compounds of formula I: as well as pharmaceutically acceptable salts, hydrates and esters thereof, are disclosed. The compounds are useful for treating or preventing prostaglandin mediated diseases. Pharmaceutical compositions containing such compounds and methods of treatment are also included.
    Type: Grant
    Filed: March 10, 1999
    Date of Patent: June 5, 2001
    Assignee: Merck Frosst Canada & Co.
    Inventors: Yves Gareau, Marc LaBelle, Helene Juteau, Michel Gallant, Nicolas LaChance, Michel Belley
  • Patent number: 6201019
    Abstract: Bi-aromatic compounds linked via a heteroethynylene radical are provided along with pharmaceutical and cosmetic compositions containing these compounds and methods for their use.
    Type: Grant
    Filed: April 8, 1999
    Date of Patent: March 13, 2001
    Assignee: Galderma Research & Development
    Inventors: Jean-Michel Bernardon, Philippe Diaz
  • Patent number: 6187933
    Abstract: Compounds of the formula where the symbols have the meaning described in the application, have retinoid-like or retinoid antagonist-like biological activity.
    Type: Grant
    Filed: January 27, 2000
    Date of Patent: February 13, 2001
    Assignee: Allergan Sales, Inc.
    Inventors: Vidyasagar Vuligonda, Min Teng, Richard L. Beard, Alan T. Johnson, Yuan Lin, Roshantha A. Chandraratna
  • Patent number: 6160175
    Abstract: A class of novel naphthyl acetamide compounds is disclosed together with the use of such compounds for inhibiting sPLA.sub.2 mediated release of fatty acids for treatment of conditions such as septic shock.
    Type: Grant
    Filed: June 9, 1998
    Date of Patent: December 12, 2000
    Assignee: Eli Lilly and Company
    Inventors: Theodore Goodson, Jr., Richard W. Harper, David K. Herron
  • Patent number: 6147224
    Abstract: 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: Grant
    Filed: October 1, 1998
    Date of Patent: November 14, 2000
    Assignee: Allergan Sales, Inc.
    Inventors: Vidyasagar Vuligonda, Kwok Yin Tsang, Jayasree Vasudevan, Roshantha A. Chandraratna
  • Patent number: 6136852
    Abstract: The present invention relates to 3,4-disubstituted phenylethanolaminotetralincarboxylic acid derivatives represented by the general formula: ##STR1## [wherein Q represents a vinylene group or a group represented by the general formula:-A-(CH.sub.2).sub.m --(wherein A represents an oxygen atom or a methylene group; and m is an integer of from 1 to 6); R represents a hydrogen atom or a lower alkyl group; n is an integer of 1 or 2; the carbon atom marked with * represents a carbon atom in R configuration, S configuration or a mixture thereof; and the carbon atom marked with (S) represents a carbon atom in S configuration] and pharmaceutically acceptable salts thereof, which have a selective .beta..sub.2 -adrenergic receptor stimulating effect with relieved burdens on the heart such as tachycardia and are useful as an agent for the prevention of threatened abortion and premature labor, a bronchodilator and an agent for pain remission and promoting stone removal in urolithiasis.
    Type: Grant
    Filed: March 8, 1999
    Date of Patent: October 24, 2000
    Assignee: Kissei Pharmaceutical Co., Ltd.
    Inventors: Makio Kitazawa, Kosuke Okazaki, Tetsuro Tamai, Masaru Saito, Nobuyuki Tanaka, Hiroaki Kobayashi, Ken Kikuchi, Hideyuki Muranaka
  • Patent number: 6096920
    Abstract: Palladium-catalyzed arylation of an olefin (e.g., ethylene) with an aromatic halide (e.g., 2-bromo-6-methoxynaphthalene, m-bromobenzophenone, or 4-isobutyl-1-bromobenzene) is conducted in specified media. After a special acid or base phase separation procedure, palladium-catalyzed carbonylation of the olefinically-substituted aromatic intermediate is conducted in specified media using CO and water or an alcohol to form arylalkylcarboxylic acid or ester or substituted arylalkylcarboxylic acid or ester (e.g., racemic 2-(6-methoxy-2-naphthyl)propionic acid, 2-(3-benzoylphenyl)propionic acid, or 2-(4-isobutylphenyl)propionic acid). Catalyst recovery procedures enabling recycle of catalyst residues and efficient recovery of amine hydrogen halide scavenger and solvent used in the arylation reaction are described, as well as novel, highly efficient methods of conducting the carbonylation reaction.
    Type: Grant
    Filed: July 8, 1998
    Date of Patent: August 1, 2000
    Assignee: Albemarle Corporation
    Inventors: Robert H. Allen, R. Carl Herndon, Jr., Kannappan C. Chockalingam, W. Dirk Klobucar, Gary D. Focht, Tse-Chong Wu, Gary D. Heidebrecht, Joseph D. McLean, Yaping Zhong, Thorsten W. Brockmann, Ronny W. Lin, William J. Layman, Jr., Ranjit K. Roy
  • Patent number: 6093799
    Abstract: A substrate for solid phase synthesis of the formula: ##STR1## is disclosed. Also disclosed are processes for preparing the substrate and intermediates useful therein. Among the novel intermediates are compounds of the formula: ##STR2## wherein t is 0 or 1; n is 3-20; R is OH, an activated ester or the residue of a solid support having a plurality of amino functionalities; A is --O-- or --NH-- and Q is hydrogen or a protecting group for an amine or alcohol.
    Type: Grant
    Filed: October 20, 1999
    Date of Patent: July 25, 2000
    Assignee: Pharmacopeia, Inc.
    Inventors: Ge Li, Sian Louise Griffiths, Edward McDonald, Libo Xu
  • Patent number: 6093830
    Abstract: The invention relates to a novel non-catalytic enantioselective resolution process for the separation of enantiomer of arylpropionic acid drugs from the racemic mixture, which comprises dissolving the racemic mixture of the said drug an organic solvent, reacting this solution with an aqueous phase containing an ionic surfactant with or without a suitable co-surfactant, and an electrolyte in microemulsion/micellar/biphasic medium, reacting this mixture with an appropriate chiral amine at a temperature in the range of 0 to 70 degrees Celsius to obtain a diastereomeric salt, acid hydrolysing the diastereomeric salt to result in the pure enantiomer of the drug which is extracted by known methods.
    Type: Grant
    Filed: March 15, 1999
    Date of Patent: July 25, 2000
    Assignee: Council of Scientific and Industrial Research
    Inventors: Nirmal Kishor Yadav, Bhaskar Dattatraya Kulkarni, Ramdas Bhagvan Khomane
  • Patent number: 6093517
    Abstract: A lithographic photoresist composition is provided containing novel calixarene compounds, particularly calix[4]resorcinarenes that are partially or wholly protected with acid-labile functionalities, as dissolution inhibitors. Also provided is a process for using the composition to generate resist images on a substrate is provided, i.e., in the manufacture of integrated circuits or the like.
    Type: Grant
    Filed: July 31, 1998
    Date of Patent: July 25, 2000
    Assignee: International Business Machines Corporation
    Inventors: Hiroshi Ito, Tomonari Nakayama, Mitsuru Ueda
  • Patent number: 6087395
    Abstract: The present invention provides an apoptosis inhibitor containing a 15R-isocarbacyclin derivative or a 15-deoxy-isocarbacyclin derivative, which can be manufactured easily and economically by means of chemical synthesis.
    Type: Grant
    Filed: October 16, 1998
    Date of Patent: July 11, 2000
    Assignees: Japan Science and Technology Corporation, Atsuo Hazato
    Inventors: Yasuyoshi Watanabe, Atsuo Hazato, Masaaki Suzuki, Yumiko Watanabe, Takumi Sato
  • Patent number: 6008321
    Abstract: A substrate for solid phase synthesis of the formula: ##STR1## is disclosed. Also disclosed are processes for preparing the substrate and intermediates useful therein. Among the novel intermediates are compounds of the formula: ##STR2## wherein t is 0 or 1; n is 3-20; R is OH, an activated ester or the residue of a solid support having a plurality of amino functionalities; A is --O-- or --NH-- and Q is hydrogen or a protecting group for an amine or alcohol.
    Type: Grant
    Filed: March 16, 1998
    Date of Patent: December 28, 1999
    Assignee: Pharmacopeia, Inc.
    Inventors: Ge Li, Sian Louise Griffiths, Edward McDonald, Libo Xu
  • Patent number: 6005003
    Abstract: A subject of the invention is the compounds of general formula (I): ##STR1## in which R1=H, alkyl, acyl, R2 and R3=H, alkyl, R4=aryl, heteroaryl, X=O, CH2, Y=OH, O-alkyl or NRaRb, as well as the salts, their preparation processes, the intermediates of these processes, their use as medicaments and the pharmaceutical compositions containing them.
    Type: Grant
    Filed: May 5, 1999
    Date of Patent: December 21, 1999
    Assignee: Hoechst Marion Roussel
    Inventor: Francois Nique
  • Patent number: 5998471
    Abstract: Compounds of the formula ##STR1## the symbols have the meaning described in the specification.
    Type: Grant
    Filed: August 11, 1998
    Date of Patent: December 7, 1999
    Assignee: Allergan Sales, Inc.
    Inventors: Alan T. Johnson, Min Teng, Vidyasagar Vuligonda, Richard L. Beard, Samuel J. Gillett, Tien T. Duong, Roshantha A. Chandraratna
  • Patent number: 5985928
    Abstract: Novel pharmaceutically/cosmetically-active bicyclic aromatic compounds have the structural formula (I): ##STR1## and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.
    Type: Grant
    Filed: January 9, 1998
    Date of Patent: November 16, 1999
    Assignee: Centre International De Recherches Dermatologiques Galderma
    Inventor: Jean-Michel Bernardon