Polycyclo-carbocyclic Ring System Having At Least Three Cyclos Patents (Class 546/285)
  • Patent number: 7365196
    Abstract: A class of compounds is disclosed, comprising sulphonamido-substituted bridged bicycloalkyl structures. The compounds are inhibitors of gamma-secretase, and hence are useful in the treatment of and/or prevention of Alzheimer's disease.
    Type: Grant
    Filed: March 15, 2001
    Date of Patent: April 29, 2008
    Assignees: Merck Sharp & Dohme Ltd., Merck Frosst Canada & Co.
    Inventors: Patrice Charles Belanger, Ian James Collins, Joanne Claire Hannam, Timothy Harrison, Stephen John Lewis, Andrew Madin, Edward Giles McIver, Alan John Nadin, Joseph George Neduvelil, Mark Steven Shearman, Adrian Leonard Smith, Timothy Jason Sparey, Graeme Irvine Stevenson, Martin Richard Teall
  • Patent number: 7338961
    Abstract: The invention relates to substituted adamantane compounds, pharmaceutical compositions thereof, processes for their preparation, and methods for inhibiting sphingosine kinase and for treating or preventing hyperproliferative disease, inflammatory disease, or angiogenic disease.
    Type: Grant
    Filed: June 15, 2006
    Date of Patent: March 4, 2008
    Assignee: Apogee Biotechnology Corporation
    Inventors: Charles D. Smith, Kevin J. French, Yan Zhuang
  • Patent number: 7335659
    Abstract: This invention provides a compound, or its possible salt, having the formula, wherein: Re and ?Re are OH, optionally independently etherified or esterified; Z is —CH2CH2— or —C(R4,R5)—, wherein R4 and R5 are independently H, (1C-2C)alkyl or form together a spiro(3C-5C)cycloalkyl; R1 is H, halogen, CF3, or (1C-4C)alkyl; R2 and R3 are independently H, halogen, —CF3, —OCF3, (1C-8C)alkyl, hydroxy, (1C-8C)alkyloxy, aryloxy, aryl(1C-8C)alkyl, halo(1C-8C)alkyl, —O(CH2)mX, wherein X is halogen or phenyl and m=2-4; —O(CH2)mNRaRb, —S(CH2)mNRaRb or —(CH2)mNRaRb, wherein m=2-4 and wherein Ra, Rb are independently (1C-8C)alkyl, (2C-8C)alkenyl, (2C-8C)alkynyl, or aryl, which alkyl, alkenyl and aryl can optionally be substituted with halogen, —CF3, —OCF3, —CN, —NO2, —OH, (1C-8C)alkoxy, aryloxy, carboxyl, (1C-8C)alkylthio, carboxylate, (1C-8C)alkyl, aryl, aryl(1C-8C)alkyl or halo(1C-8C)alkyl; or Ra and Rb form a 3-8 membered ring structure, optionally substituted with halogen, —CF3, —OCF3, —CN, —NO2, hydroxy, hydroxy(1C-
    Type: Grant
    Filed: February 14, 2003
    Date of Patent: February 26, 2008
    Assignee: N.V. Organon
    Inventors: Hubert Jan Jozef Loozen, Markus Wagener, Gerrit Veeneman, Eduard Willem Zwart
  • Patent number: 7326696
    Abstract: Aminomethyl substituted tetracycline compounds, pharmaceutical compositions, and methods of use thereof are discussed.
    Type: Grant
    Filed: December 15, 2003
    Date of Patent: February 5, 2008
    Assignee: Paratek Pharmaceuticals, Inc.
    Inventors: Mark L. Nelson, Kwasi Ohemeng, Roger Frechette, Paul Abato, Victor Amoo, Haregewein Assefa, Joel Berniac, Beena Bhatia, Todd Bowser, Jackson Chen, Laura Honeyman, Mohamed Y. Ismail, Oak Kim, Rachid Mechiche, N. Laxma Reddy, Atul K. Verma, Peter Viski, Tadeusz Warchol, Ivan Yanachkov
  • Patent number: 7320993
    Abstract: The invention relates to new pyridylalkane, alkene, and alkine acid amides substituted with an aryl and/or heteroaryl residue according to the general formula (I), with a saturated or one or several-fold unsaturated hydrocarbon residue in the carboxylic acid group, methods for the synthesis of these compounds, medicaments containing these and their production as well as their therapeutic use, especially as cytostatic agents and immunosuppressive agents, for example in the treatment or prevention of various types of tumors and control of immune reactions such as autoimmune diseases.
    Type: Grant
    Filed: June 16, 2000
    Date of Patent: January 22, 2008
    Assignee: Astellas Deutschland GmbH
    Inventors: Elfi Biedermann, Max Hasmann, Roland Löser, Benno Rattel, Friedemann Reiter, Barbara Schein, Klaus Seibel, Klaus Vogt, Katja Wosikowski, Isabel Schemainda
  • Patent number: 7317024
    Abstract: The invention relates to a class of novel non-steroidal compounds which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-?B activity including obesity, diabetes, inflammatory and immune diseases, and have the structure of formula (I) or stereoisomers or prodrugs or solvates or pharmaceutically acceptable salts thereof, wherein Z, R, R4, R5, Ra, Rb, Rc, and Rd, are defined herein. Also provided are pharmaceutical compositions and methods of treating obesity, diabetes and inflammatory or immune associated diseases comprising said compounds.
    Type: Grant
    Filed: January 12, 2006
    Date of Patent: January 8, 2008
    Assignee: Bristol-Myers Squibb Co.
    Inventor: Bingwei V. Yang
  • Publication number: 20070257603
    Abstract: A novel fluorene compound is provided which has at least one fluorene group represented by the following general formula [III] or [IV]:
    Type: Application
    Filed: January 29, 2007
    Publication date: November 8, 2007
    Applicant: CANON KABUSHIKI KAISHA
    Inventors: Koichi Suzuki, Kazunori Ueno, Hiroshi Tanabe, Satoru Shiobara
  • Publication number: 20070236137
    Abstract: The present invention relates to aromatic amine derivatives having a specific structure; and organic electroluminescent devices comprising a cathode, an anode and one or plural organic thin film layers including at least a light emitting layer which are sandwiched between the cathode and the anode wherein at least one of the organic thin film layers contains the above aromatic amine derivatives in the form of a single substance or a component of a mixture. There are provided the organic electroluminescent devices exhibiting a long life and a high efficiency of light emission which are capable of emitting a blue light having a high color purity, as well as the aromatic amine derivatives capable of realizing such organic electroluminescent devices.
    Type: Application
    Filed: March 2, 2007
    Publication date: October 11, 2007
    Applicant: Idemitsu Kosan Co., Ltd.
    Inventor: Masakazu FUNAHASHI
  • Publication number: 20070228941
    Abstract: An amino compound for an organic light-emitting device of general formula [1]: wherein X1 is bonded to the pair of fluorenyl groups at meta-positions to each other and is substituted or unsubstituted aromatic ring, fused polycyclic ring, or heterocyclic ring; Y1 and Y2 are each substituted or unsubstituted alkyl, aryl, or heterocyclic and are the same or different; Z1 to Z4 are each hydrogen, halogen, or substituted or unsubstituted alkyl, aralkyl, alkenyl, alkynyl, alkoxy, aryl, or heterocyclic and are the same or different; R1 to R4 are each hydrogen, halogen, or substituted or unsubstituted alkyl, aryl, or heterocyclic and are the same or different; a and d are each 1 to 4; and b and c are each 1 to 3.
    Type: Application
    Filed: March 23, 2007
    Publication date: October 4, 2007
    Applicant: CANON KABUSHIKI KAISHA
    Inventors: Shigemoto Abe, Akihiro Senoo, Naoki Yamada, Chika Negishi
  • Publication number: 20070205412
    Abstract: The present invention provides a novel anthracene derivative and an organic electronic device using the same. The organic electronic device according to the present invention shows excellent characteristics in efficiency, drive voltage, and life time.
    Type: Application
    Filed: March 6, 2007
    Publication date: September 6, 2007
    Inventors: Jae-Soon Bae, Dae-Woong Lee, Dong-Hoon Lee, Jun-Gi Jang, Sang-Young Jeon, Ji-Eun Kim
  • Patent number: 7220783
    Abstract: The present invention provides a selective suppressor of the IgE production comprising a compound which suppresses the IgE production in a process from a differentiation of a mature B cell into an antibody-producing cell to the production of an antibody and which does not suppress or weakly suppresses the production of IgG, IgM and/or IgA which are produced at the same time, a compound of the formula (I): wherein R1–R13 are hydrogen, halogen, lower alkyl, lower alkoxy or the like, X is —O—, —CH2—, —NR14— or —S(O)p- and Y is lower alkyl, lower alkenyl or the like, a process for producing the same and a pharmaceutical composition comprising the same.
    Type: Grant
    Filed: November 12, 2003
    Date of Patent: May 22, 2007
    Assignee: Shionogi & Co., Ltd.
    Inventors: Kenji Kawada, Mitsuaki Ohtani, Ryuji Suzuki, Akinori Arimura
  • Patent number: 7173131
    Abstract: An anthryl derivative group substituted compound having a specific chemical structure is provided. This compound is used for producing an organic luminescent device which can emit luminescent hues with a very high purity and effect light emission with a high luminescence efficiency and a long lifetime.
    Type: Grant
    Filed: June 25, 2004
    Date of Patent: February 6, 2007
    Assignee: Canon Kabushiki Kaisha
    Inventors: Akihito Saitoh, Koichi Suzuki, Akihiro Senoo, Kazunori Ueno, Keiji Okinaka
  • Patent number: 7160907
    Abstract: Pleuromutilin compounds of the formula: are of use in anti-bacterial therapy.
    Type: Grant
    Filed: December 3, 2004
    Date of Patent: January 9, 2007
    Assignee: SmithKline Beecham P.L.C.
    Inventors: John Stephen Elder, Andrew Keith Forrest, Richard Lewis Jarvest, Robert John Sheppard
  • Patent number: 7157477
    Abstract: The invention involves a methods and compositions for use in photodynamic therapy. Novel perylenequinone derivatives, conjugates comprising perylenequinone derivatives and a binding agent, and methods of treatment using these compositions are disclosed. The present invention relates to the field of photosensitizers possessing photodynamic activities. They possess high photodynamic activities and low dark toxicities, which makes them as more potent photodynamic agents than HPD against cancer and AIDS virus.
    Type: Grant
    Filed: October 24, 2001
    Date of Patent: January 2, 2007
    Assignees: Altachem Pharma Ltd., Institute of Photographic Chemistry Academia Sinica
    Inventors: Manhua Zhang, Shangjie Xu, Tao Wu, Shen Chen, Tao Shen
  • Patent number: 7138406
    Abstract: The present invention provides compounds of the formula wherein A is of the formula and X, Y, n, R1–R25 are as described in the specification which are modulators of the glucocorticoid receptor and are thus useful for the treatment of animals requiring glucocorticoid receptor agonist therapy. Glucocorticoid receptor modulators are useful in the treatment of certain inflammatory conditions.
    Type: Grant
    Filed: July 8, 2003
    Date of Patent: November 21, 2006
    Assignees: Pfizer, Inc., Pfizer Products, Inc.
    Inventors: Yves A. Chantigny, Edward F. Kleinman, Ralph P. Robinson
  • Patent number: 7101915
    Abstract: The present invention provides a selective suppressor of the IgE production comprising a compound which suppresses the IgE production in a process from a differentiation of a mature B cell into an antibody-producing cell to the production of an antibody and which does not suppress or weakly suppresses the production of IgG, IgM and/or IgA which are produced at the same time, a compound of the formula (I): wherein R1–R13 are hydrogen, halogen, lower alkyl, lower alkoxy or the like, X is —O—, CH2—, —NR14— or —S(O)p— and Y is lower alkyl, lower alkenyl or the like, a process for producing the same and a pharmaceutical composition comprising the same.
    Type: Grant
    Filed: July 30, 1997
    Date of Patent: September 5, 2006
    Assignee: Shionogi & Co., Ltd.
    Inventors: Kenji Kawada, Mitsuaki Ohtani, Ryuji Suzuki, Akinori Arimura
  • Patent number: 7087599
    Abstract: The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including: bone loss, bone fractures, osteoporosis, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, cerebral degenerative disorders, restinosis, gynacomastia, vascular smooth muscle cell proliferation, obesity, incontinence, and cancer, in particular of the breast, uterus and prostate.
    Type: Grant
    Filed: February 14, 2001
    Date of Patent: August 8, 2006
    Assignee: Merck & Co., Inc.
    Inventors: Dann LeRoy Parker, Jr., Ronald W. Ratcliffe, Robert R. Wilkening, Kenneth J. Wildonger
  • Patent number: 7074536
    Abstract: The present invention provides an alkylenebisnaphthol derivative represented by formula [I]: and a salt thereof. The compound of the present invention has an excellent triboelectric charge property and useful as charge control agent for electrophotographic toners.
    Type: Grant
    Filed: July 30, 2002
    Date of Patent: July 11, 2006
    Assignee: Kabushiki Kaisha Ueno Seiyaku Oyo Kenkyujo
    Inventors: Ryuzo Ueno, Masaya Kitayama, Kenji Minami, Hiroyuki Wakamori, Nobuhiro Yonetani
  • Patent number: 7074836
    Abstract: The present invention provides a selective suppressor of the IgE production comprising a compound which suppresses the IgE production in a process from a differentiation of a mature B cell into an antibody-producing cell to the production of an antibody and which does not suppress or weakly suppresses the production of IgG, IgM and/or IgA which are produced at the same time, a compound of the formula (I): wherein R1–R13 are hydrogen, halogen, lower alkyl, lower alkoxy or the like, X is —O—, —CH2—, NR14— or —S(O)p— and Y is lower alkyl, lower alkenyl or the like, a process for producing the same and a pharmaceutical composition comprising the same.
    Type: Grant
    Filed: November 12, 2003
    Date of Patent: July 11, 2006
    Assignee: Shionogi & Co., Ltd.
    Inventors: Kenji Kawada, Mitsuaki Ohtani, Ryuji Suzuki, Akinori Arimura
  • Patent number: 7037632
    Abstract: 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 the formula is described in the especification; and ?(b) a charge generating compound.
    Type: Grant
    Filed: September 25, 2003
    Date of Patent: May 2, 2006
    Assignee: Samsung Electronics Co. Ltd.
    Inventors: Nusrallah Jubran, Zbigniew Tokarski, Kam W. Law
  • Patent number: 7011917
    Abstract: 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, halogen, carboxyl, hydroxyl, thiol, cyano, nitro, aldehyde group, ketone group, an ether group, an ester group, a carbonyl group, 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 can be 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, 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— gr
    Type: Grant
    Filed: September 25, 2003
    Date of Patent: March 14, 2006
    Assignee: Samsung Electronics Co. Ltd.
    Inventors: Nusrallah Jubran, Zbigniew Tokarski, Kam W. Law
  • Patent number: 6995181
    Abstract: Novel non-steroidal compounds are provided which are glucocorticoid receptor modulators which are useful in treating diseases requiring glucocorticoid receptor agonist or antagonist therapy such as obesity, diabetes, inflammatory and immune disorders, and have the structure where Z is CONR1R2 or CH2NR1R2 and where R, Ra, Rb, Rc, Rd, Z, A and B are defined herein.
    Type: Grant
    Filed: July 17, 2003
    Date of Patent: February 7, 2006
    Assignee: Bristol-Myers Squibb Co.
    Inventors: Wayne Vaccaro, Bingwei Vera Yang, Soong-Hoon Kim, Tram Huynh, David R. Tortolani, Kenneth J. Leavitt, Wenying Li, Arthur M. Doweyko, Xiao-Tao Chen, Lidia Doweyko
  • Patent number: 6972297
    Abstract: 2-(S)-hydroxymutilin carbamate derivatives of formula (I), in which R1 is a 5- or 6-membered optionally substituted heteroaryl group; and R2 is vinyl or ethyl, are useful in the treatment of bacterial infections
    Type: Grant
    Filed: March 29, 2001
    Date of Patent: December 6, 2005
    Assignee: SmithKline Beecham p.l.c.
    Inventors: Gerald Brooks, Eric Hunt, Steven Howard
  • Patent number: 6906046
    Abstract: Benzobicyclooctane compounds, their use in inhibiting cellular events involving TNF-? and IL-8, and in the treatment of inflammation events in general; a combinatorial library of diverse bicyclooctanes and process for their synthesis as a library and as individual compounds.
    Type: Grant
    Filed: December 11, 2001
    Date of Patent: June 14, 2005
    Assignee: Celltech R & D Inc.
    Inventors: Randy W. Jackson, Ihab Darwish, Ted A. Baughman, J. Jeffry Howbert
  • Publication number: 20040263067
    Abstract: An anthryl derivative group substituted compound having a specific chemical structure is provided. This compound is used for producing an organic luminescent device which can emit luminescent hues with a very high purity and effect light emission with a high luminescence efficiency and a long lifetime.
    Type: Application
    Filed: June 25, 2004
    Publication date: December 30, 2004
    Applicant: CANON KABUSHIKI KAISHA
    Inventors: Akihito Saitoh, Koichi Suzuki, Akihiro Senoo, Kazunori Ueno, Keiji Okinaka
  • Publication number: 20040248026
    Abstract: The present invention provides an alkylenebisnaphthol derivative represented by formula [I]: 1
    Type: Application
    Filed: July 12, 2004
    Publication date: December 9, 2004
    Inventors: Ryuzo Ueno, Masaya Kitayama, Kenji Minami, Hiroyuki Wakamori, Nobuhiro Yonetani
  • Publication number: 20040235910
    Abstract: A compound of formula 1
    Type: Application
    Filed: June 14, 2004
    Publication date: November 25, 2004
    Inventors: Gerd Ascher, Heinz Berner, Johannes Hildebrandt
  • Publication number: 20040214867
    Abstract: In one aspect, the present invention concerns the use of certain quaternary ammonium compounds as active ingredient in the manufacture of a medicament for use in the treatment and/or prevention of cough in warm-blooded animals, including humans, such as compounds of the following formula (I): Y-J-E An− wherein J is independently selected from a group represented by one of formulae (II), (III) and (IV).
    Type: Application
    Filed: February 14, 2003
    Publication date: October 28, 2004
    Inventors: Lewis Siu Leung Choi, Gregory N Beatch, Clive Page
  • Publication number: 20040152674
    Abstract: The invention includes new substituted tetracycline-type compounds that exhibit significant antibacterial activity, including against both gram-positive and gram-negative bacteria. It has been found that compounds of the invention are highly active against both gram positive and gram negative tetracycline sensitive and tetracycline resistant bacteria.
    Type: Application
    Filed: January 20, 2004
    Publication date: August 5, 2004
    Applicant: Trustees of Tufts College
    Inventors: Stuart B. Levy, Mark L. Nelson
  • Publication number: 20040138467
    Abstract: Aromatic and aromatic/heteroaromatic molecular structures with controllable electron conducting properties are derived from the incorporation of electron active substituents in selective positions.
    Type: Application
    Filed: November 25, 2003
    Publication date: July 15, 2004
    Inventors: Roger Harquail French, Ross Getty, Simona Percec
  • Publication number: 20040138262
    Abstract: The present invention provides compounds of the formula 1
    Type: Application
    Filed: July 8, 2003
    Publication date: July 15, 2004
    Applicant: Pfizer Inc.
    Inventors: Yves A. Chantigny, Edward F. Kleinman, Ralph P. Robinson
  • Publication number: 20040127715
    Abstract: The object of the present invention is to provide a novel compound which can prepare an insulating film having a low dielectric constant and excellent in the heat resistance. This object is achieved by an adamantane compound represented by the formula (1).
    Type: Application
    Filed: July 23, 2003
    Publication date: July 1, 2004
    Applicant: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Nobutaka Kunimi, Yuji Yoshida
  • Patent number: 6756375
    Abstract: The invention provides for a non-steroidal compound having the formula wherein Re and ′Re are OH, optionally independently etherified or esterified; Z is —CH2— or —CH2CH2—; R1 is H, halogen, CF3, or (1C-4C)alkyl; R2, R3 and R4 are independently H, halogen, —CF3, —OCF3, (1C-8C)Alkyl, hydroxy, (1C-8C)alkyloxy, aryloxy, aryl(1C-8C)alkyl, halo(1C-8C)alkyl, —O(CH2)mX, wherein X is halogen or phenyl and m=2-4; —O(CH2)mNRaRb, —S(CH2)mNRaRb or —(CH2)mNRaRb, wherein m=2-4 and Ra, Rb are independently (1C-8C)alkyl, (2C-8C)alkenyl, (2C-8C)alkynyl, or aryl, optionally substituted with halogen, —CF3, —OCF3, —CN, —NO2, —OH, (1C-8C)alkoxy, aryloxy, carboxyl, (1C-8C)alkylthio, carboxylate, (1C-8C)alkyl, aryl, aryl(1C-8C)alkyl, halo(1C-8C)alkyl or Ra and Rb form a 3-8 membered ring structure, optionally substituted with halogen, —CF3, —OCF3, —CN, —NO2, hydroxy, hydroxy(1C-4C)a
    Type: Grant
    Filed: July 24, 2003
    Date of Patent: June 29, 2004
    Assignee: Akzo Nobel N.V.
    Inventors: Gerrit Herman Veeneman, Hubert JanJozef Loozen, Jordi Mestres, Eduard Willem De Zwart
  • Publication number: 20040122063
    Abstract: The invention relates a compound represented by the formula (1):
    Type: Application
    Filed: July 30, 2003
    Publication date: June 24, 2004
    Inventors: Toshiharu Yoshino, Tsutomu Nagata, Noriyasu Haginoya, Kenji Yoshikawa, Hideyuki Kanno, Masatoshi Nagamochi
  • Publication number: 20040116708
    Abstract: The present invention provides a novel carboxylic acid derivative, a salt thereof or a hydrate of them which is useful as an insulin sensitizer, and a medicament comprising the derivative as the effective ingredient. More specifically, it provides a carboxylic acid compound represented by the formula (I), a salt thereof or a hydrate of them.
    Type: Application
    Filed: August 27, 2003
    Publication date: June 17, 2004
    Inventors: Hitoshi Harada, Masanobu Shinoda, Richard Clark, Fumiyoshi Matsuura, Eita Emori, Shunji Kasai, Hideki Yoshitomi, Kazuto Yamazaki, Takashi Inoue, Sadakazu Miyashita, Taro Hihara
  • Publication number: 20040110958
    Abstract: Arylamine derivatives that can be utilized as hole transport or hole injection materials of organic electroluminescence devices, electrophotographic reactors, etc., and synthetic intermediates thereof, and processes of producing those.
    Type: Application
    Filed: September 17, 2003
    Publication date: June 10, 2004
    Applicant: TOSOH CORPORATION
    Inventors: Masakazu Nishiyama, Hiroaki Tenma, Hisao Eguchi
  • Patent number: 6737423
    Abstract: Substituted heterocyclo-norbornylaminoderivatives having: a) an exo-configuration nitrogen and an endo-fused five-membered ring or six-membered ring of the formula (I) or b) an exo-configuration nitrogen and an exo-fused five-membered ring or six-membered ring of the formula (I a), wherein Rn, Het, A, B and T have the meanings given in the claims. These compounds have a variety of uses. They can be used as antihypertensives, for the reduction or prevention of is chemically induced damage, as pharmaceuticals for surgical interventions, for the treatment of ischemia of the nervous system, including stroke and cerebral edema, for the treatment of ischemia due to shock and disturbed respiratory drive, for the treatment of snoring, as a laxative, as an agent against ectoparasites, for the prevention of gallstone formation, as an antiatherosclerotic, as an agent against diabetic late complications, cancers, fibrotic disorders, endothelial dysfunction, organ hypertrophy, and organ hyperplasia.
    Type: Grant
    Filed: December 18, 2001
    Date of Patent: May 18, 2004
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Uwe Heinelt, Hans-Jochen Lang, Klaus Wirth, Hans-Willi Jansen
  • Publication number: 20040092557
    Abstract: The invention involves a methods and compositions for use in photodynamic therapy. Novel perylenequinone derivatives, conjugates comprising perylenequinone derivatives and a binding agent, and methods of treatment using these compositions are disclosed. The present invention relates to the field of photosensitizers possessing photodynamic activities. They possess high photodynamic activities and low dark toxicities, which makes them as more potent photodynamic agents than HPD against cancer and AIDS virus.
    Type: Application
    Filed: August 26, 2003
    Publication date: May 13, 2004
    Inventors: Manhua Zhang, Shangjie Xu, Tao Wu, Shen Chen, Tao Shen
  • Publication number: 20040067971
    Abstract: The invention relates to novel stilbene compounds having the general formula (I): 1
    Type: Application
    Filed: October 2, 2003
    Publication date: April 8, 2004
    Applicant: GALDERMA RESEARCH & DEVELOPMENT, S.N.C.
    Inventors: Jean-Michel Bernardon, Bruno Charpentier
  • Publication number: 20040062726
    Abstract: Derivatives of fluorene, including ester derivatives of cyano(9H-fluoren-9-ylidene) acetic acid, and sunscreen compositions including a mixture of a photoactive compound and an ester derivative of cyano(9H-fluoren-9-ylidene) acetic acid are disclosed herein. Also disclosed are methods for terminating a polymer chain with an ester derivative of cyano(9H-fluoren-9-ylidene) acetic acid and methods of filtering out ultra-violet light from a substrate by the use of one or more such derivatives.
    Type: Application
    Filed: June 10, 2003
    Publication date: April 1, 2004
    Inventors: Craig A. Bonda, Anna B. Pavlovic
  • Publication number: 20040058937
    Abstract: Pleuromutilin compounds of the formula: 1
    Type: Application
    Filed: October 17, 2003
    Publication date: March 25, 2004
    Inventors: Steven Aitken, Gerald Brooks, Steven Dabbs, Colin Henry Frydrych, Steven Howard, Eric Hunt
  • Publication number: 20040054232
    Abstract: A novel arylamine compound represented by the following general formula (1): 1
    Type: Application
    Filed: September 10, 2003
    Publication date: March 18, 2004
    Applicant: Idemitsu Kosan Co., Ltd.
    Inventors: Chishio Hosokawa, Masakazu Funahashi
  • Publication number: 20040049030
    Abstract: tert-Alkylphenoxy-substituted polycyclic compounds of the general formula I 1
    Type: Application
    Filed: September 23, 2003
    Publication date: March 11, 2004
    Inventors: Arno Bohm, Willi Helfer, Georg Beck, Matthias Krieger, Peter Erk
  • Publication number: 20040044062
    Abstract: A water soluble derivative of buckministerfullerene (C50) having antiviral and virucidal properties is used to inhibit human retroviral replication and infections. The derivatized fullerene is symmetrically substituted with polar organic moieties containing 1 to 20 carbon atoms and optionally further containing oxygen or nitrogen.
    Type: Application
    Filed: February 1, 2003
    Publication date: March 4, 2004
    Inventors: Simon H. Friedman, Raymond F. Schinazi, Fred Wudl, Craig L. Hill, Diane L. DeCamp, Rintje P. Sijbesma, George L. Kenyon
  • Publication number: 20040029929
    Abstract: The present invention provides novel aminoadamantane derivatives, methods of making the derivatives, compositions including the novel aminoadamantane derivatives, and methods for the treatment and prevention of neurological diseases using the derivatives and compositions.
    Type: Application
    Filed: August 4, 2003
    Publication date: February 12, 2004
    Inventors: Yuqiang Wang, Wenqing Ye, James W. Larrick, Jonathan S. Stamler, Stuart A. Lipton
  • Patent number: 6677330
    Abstract: The present invention provides a novel compound having an excellent acetylcholinesterase inhibitory effect. That is, it provides a 4-substituted piperidine compound fluoride represented by the following formula, a pharmaceutically acceptable salt thereof or hydrates thereof (provided that 1-benzyl-4-[(5,6-dimethoxy-2-fluoro-1-indanon)-2-yl]methylpiperidine, a pharmaceutically acceptable salt thereof and hydrates thereof are excluded). wherein R1 and R2 represent substituents.
    Type: Grant
    Filed: August 30, 2001
    Date of Patent: January 13, 2004
    Assignee: Eisai Co., Ltd.
    Inventors: Yoichi Iimura, Takashi Kosasa, Yoshiharu Yamanishi, Hachiro Sugimoto, Yoshio Takeuchi, Tetsuo Shibata, Emiko Suzuki
  • Publication number: 20040006235
    Abstract: In a process for the preparation of ring compounds via a combinatorial synthesis, the reaction procedure is based on a Suzuki coupling, subsequent halo-demetallation and finally a further Suzuki coupling. The Suzuki couplings are each carried out with a boronic acid or a boronic acid ester. The reaction procedure uses provides novel ring compounds and uses novel synthesis units used for this purpose. The novel ring compounds are suitable for use as constituents in liquid-crystalline mixtures.
    Type: Application
    Filed: March 17, 2003
    Publication date: January 8, 2004
    Applicant: Merck Patent GmbH
    Inventors: Detlef Pauluth, Peer Kirsch, Peter Baeuerle, Oliver Deeg
  • Patent number: 6673625
    Abstract: The present invention provides formulae for fluorescent compounds that have a number of properties which make them uniquely suited for use in sensors of analytes such as saccharides. The advantageous fluorescent properties include favorable excitation wavelengths, emission wavelengths, fluorescence lifetimes, and photostability. Additional advantageous properties include enhanced aqueous solubility, as well as temperature and pH sensitivity. The compound comprises an aryl or a substituted phenyl botonic acid that acts as a substrate recognition component, a fluorescence switch component, and a fluorophore. Fluorescent compounds are described that are excited at wavelengths greater than 400 nm and emit at wavelengths greater than 450 nm, which is advantageous for optical transmission through skin. The fluorophore is typically selected from transition metal-ligand complexes and thiazine, oxazine, oxazone, or oxazine-one as well as anthracene compounds.
    Type: Grant
    Filed: March 30, 2001
    Date of Patent: January 6, 2004
    Assignees: The Regents of the University of California, MiniMed Inc.
    Inventors: Joe H. Satcher, Jr., Stephen M. Lane, Christopher B. Darrow, Douglas R. Cary, Joe Anh Tran
  • Publication number: 20030222243
    Abstract: Fluorinated indenes and 1,7-dihydroindacenes of the general formulae (I) and (II) of negative dielectric anisotropy (&Dgr;&egr;<0) 1
    Type: Application
    Filed: April 4, 2003
    Publication date: December 4, 2003
    Applicant: Merck Patent GmbH
    Inventors: Lars Lietzau, Melanie Klasen-Memmer, Matthias Bremer
  • Publication number: 20030225091
    Abstract: Compounds that are dual aP2/k-FABP inhibitors are provided having the formula 1
    Type: Application
    Filed: November 15, 2002
    Publication date: December 4, 2003
    Inventors: David R. Magnin, Richard B. Sulsky, Jeffrey A. Robl, Thomas J. Caulfield, Rex A. Parker