Nitrogen Containing Hetero Ring Attached Indirectly To The Cyclopentanohydrophenanthrene Ring System By Nonionic Bonding Patents (Class 540/107)
  • Patent number: 10529934
    Abstract: Provided is a metal complex which is excellent in quantum yield and full width at half maximum of a light emission spectrum. The metal complex is represented by the following formula (1): wherein M represents an iridium atom or the like, n1 represents 1 to 3, n2 represents 0 to 2, X1 to X8 represent a carbon atom or the like, R1 to R8 represent a hydrogen atom or the like, one of Xa and Xb is a single bond, and the other is a group represented by —CR11R12—CR13R14—, R11 to R14 represent an alkyl group or the like, ring A represents a heteroaromatic ring, and A1-G1-A2 represents an anionic bidentate ligand.
    Type: Grant
    Filed: September 9, 2015
    Date of Patent: January 7, 2020
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Takakazu Saito, Yusuke Ishii, Kazuei Ohuchi, Nobuhiko Akino, Rui Ishikawa
  • Patent number: 9382288
    Abstract: The present invention relates to compounds derived from steroids of the general formula (I) wherein L represents a linker and R# represents a steroid residue, the use of compounds of the general formula (I) in medicine and for the prophylaxis and/or the treatment of infectious diseases. Furthermore described are pharmaceutical compositions containing at least one compound of the general formula (I). A further aspect of the invention relates to the synthesis of said compounds of the general formula (I).
    Type: Grant
    Filed: October 6, 2011
    Date of Patent: July 5, 2016
    Assignee: Justus-Liebig-Universitat Giessen
    Inventors: Katja Becker, Reimar Krieg, Bruno Schönecker
  • Patent number: 9067966
    Abstract: The invention relates to novel lupeol-type triterpene derivatives and related compounds, and pharmaceutical compositions useful for therapeutic treatment of viral diseases and particularly HIV mediated diseases.
    Type: Grant
    Filed: July 2, 2010
    Date of Patent: June 30, 2015
    Assignee: HETERO RESEARCH FOUNDATION, HETERO DRUGS LTD.
    Inventors: Bandi Parthasaradhi Reddy, Vedula Manohar Sharma, Kura Rathnakar Reddy, Musku Madhanmohan Reddy, Nelli Yella Reddy, Lanka VL Subrahmanyam
  • Publication number: 20140088053
    Abstract: The present application discloses 17? hydroxy steroid dehydrogenase (17? HSD) type 1, 3, 10 inhibitors and use thereof (alone and in combination) in the treatment of cancer and other afflictions. 17? HSD1 inhibitors include estradiol derivatives with a nieta-carbamoylbenzyl substituent at C 16. 17? HSD3/HSD10 inhibitors include androsterone derivatives substituted at the C3 position with a sulfonamide piperazine. Also disclosed are compounds that are inhibitors of both 17? HSD1 and 17? HSD3 that have a spiro-morpholine substituent at C20.
    Type: Application
    Filed: March 26, 2012
    Publication date: March 27, 2014
    Applicant: UNIVERSITÉ LAVAL
    Inventors: Donald Poirier, René Maltais, Jenny Roy
  • Patent number: 8524694
    Abstract: Sterol derivatives of formula (I) and a method for the production of the compounds, a medicament using one of the compounds and a pharmaceutical composition comprising the medicament.
    Type: Grant
    Filed: April 1, 2011
    Date of Patent: September 3, 2013
    Assignee: Institut National de la Sante et de la Recherche Medicale (INSERM)
    Inventors: Marc Poirot, Philippe De Medina, Sandrine Poirot
  • Patent number: 8435973
    Abstract: Substituted steroid compounds which represent selective inhibitors of 17?-hydroxysteroid dehydrogenase type I (17?-HSD1) and, in addition, which may represent inhibitors of the steroid sulfatase, salts thereof, pharmaceutical preparations containing these compounds, and a process for the preparation of these compounds. Also disclosed is a therapeutic method of using such substituted steroid compounds, particularly in the treatment, inhibition, prophylaxis or prevention of steroid hormone dependent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring the inhibition of 17?-hydroxysteroid dehydrogenase type I and/or steroid sulfatase enzymes and/or requiring lowering of the endogenous 17?-estradiol concentration.
    Type: Grant
    Filed: September 28, 2010
    Date of Patent: May 7, 2013
    Assignee: Abbott Products GmbH
    Inventors: Josef Messinger, Heinrich-Hubert Thole, Bettina Husen, Michael Weske, Pasi Koskimies, Lila Pirkkala
  • Publication number: 20130072464
    Abstract: The invention relates to 17-hydroxy-17-pentafluoroethyl-estra-4,9(10)-dien-11-aryl derivatives of formula I with progesterone-antagonizing action and methods of production thereof, use thereof for the treatment and/or prevention of diseases and use thereof for producing medicinal products for the treatment and/or prevention of diseases, in particular uterine fibroids (myomata, uterine leiomyomata), endometriosis, heavy menstrual bleeding, meningiomata, hormone-dependent breast cancers and menopause-associated complaints or for fertility control and emergency contraception.
    Type: Application
    Filed: February 8, 2011
    Publication date: March 21, 2013
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Wolfgang Schwede, Ulrich Klar, Carsten Möller, Andrea Rotgeri, Wilhelm Bone, Christoph Huwe
  • Publication number: 20130029953
    Abstract: Described herein are compounds which either act as pure antiprogestins or as antiprogestins with partial agonistic activity and methods of treating cancer using such compounds.
    Type: Application
    Filed: July 28, 2011
    Publication date: January 31, 2013
    Inventors: Klaus Nickisch, Kesavaram Narkunan, Baishakhi Debnath, Bindu Santhamma
  • Publication number: 20130018027
    Abstract: The subject matter of the instant invention is pertinent to the field of treatment of hormone-dependent conditions. New compounds and methods for treating these conditions are disclosed. Embodiments of the instant invention disclose methods for treating endometriosis, dysmenorrhea, breast cancer, uterine fibroids and endometrial hyperproliferation.
    Type: Application
    Filed: December 23, 2010
    Publication date: January 17, 2013
    Applicant: REPROS THERAPEUTICS INC.
    Inventors: Joseph S. Podolski, Ronald D. Wiehle
  • Publication number: 20130005697
    Abstract: The invention relates to 17-hydroxy-17-pentafluoroethyl-estra-4,9(10)-dien-11-aryl derivatives of the formula I with a progesterone antagonising effect and processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and also their use for producing medicaments for the treatment and/or prophylaxis of diseases, in particular of uterus fibroids (myomas, uterine leiomyomas), endometriosis, heavy menstrual bleeding, meningiomas, hormone-dependent breast cancers and troubles associated with the menopause or for monitoring fertility and emergency contraception.
    Type: Application
    Filed: February 8, 2011
    Publication date: January 3, 2013
    Applicant: Bayer Intellectual Property GmbH
    Inventors: Wolfgang Schwede, Ulrich Klar, Carsten Möller, Andrea Rotgeri, Wilhelm Bone, Christoph Huwe
  • Publication number: 20120316145
    Abstract: The invention relates to 17-hydroxy-17-pentafluoroethylestra-4,9(10)-diene 11-benzylidene derivatives of the formula I, in which Y and X are each as defined in the claims and the description, to a process for preparation thereof and to the use thereof as medicaments.
    Type: Application
    Filed: July 7, 2010
    Publication date: December 13, 2012
    Applicant: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Ulrich Klar, Wolfgang Schwede, Carsten Möller, Andrea Rotgeri, Wilhelm Bone
  • Publication number: 20120258941
    Abstract: The invention relates to 17-hydroxy-17-pentafluoroethylestra-4,9(10)-diene 11-aryl derivatives of the formula I with progesterone-antagonising action and to processes for preparation thereof, to use thereof for treatment and/or prophylaxis of disorders and to the use thereof for production of medicaments for treatment and/or prophylaxis of disorders, especially of fibroids of the uterus (myomas, uterine leiomyomas), endometriosis, heavy menstrual bleeds, meningiomas, hormone-dependent breast cancers and complaints associated with the menopause, or for fertility control and emergency contraception.
    Type: Application
    Filed: July 8, 2010
    Publication date: October 11, 2012
    Applicant: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Ulrich Klar, Wolfgang Schwede, Carsten Möller, Andrea Rotgeri, Wilhelm Bone
  • Publication number: 20120190660
    Abstract: The invention relates to 17-hydroxy-17-pentafluoroethylestra-4,9(10)-diene 11-ethynylphenyl derivatives of the formula I, in which R1 and X are each as defined in the claims and the description, and to a process for preparation thereof and to the use thereof as medicaments.
    Type: Application
    Filed: July 8, 2010
    Publication date: July 26, 2012
    Applicant: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Ulrich Klar, Wolfgang Schwede, Carsten Möller, Andrea Rotgeri, Wilhelm Bone
  • Publication number: 20120157421
    Abstract: The invention relates to 17?-alkyl-17?-oxy-oestratrienes of the formula (I), to processes for their preparation, to the use of the 17?-alkyl-17?-oxy-oestratrienes for preparing pharmaceuticals and to pharmaceutical preparations comprising these compounds.
    Type: Application
    Filed: May 26, 2010
    Publication date: June 21, 2012
    Applicant: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Rolf Bohlmann, Nikolaus Heinrich, Jan Hübner, Georg Kettschau, Hermann Künzer, Philip Lienau, Michael Gerisch, Silke Köhr, Dieter Lang, Karsten Denner, Michael Sander, Jens Hoffmann, Tim Wintermantel
  • Patent number: 8119619
    Abstract: Steroid compounds possessing a hydrogen donor in 3beta position, either in the form of a hydroxy- or a sulfate group, function as efficient blockers of the 3alpha-hydroxy-pregnan-steroid action and thus have utility as therapeutic substances for the prevention and/or treatment of steroid related CNS disorders. Treatment methods based on the administration of these substances are disclosed, and these substances either alone or in combination are also suggested for the manufacture of pharmaceuticals for the treatment of many specific steroid induced CNS disorders.
    Type: Grant
    Filed: January 7, 2011
    Date of Patent: February 21, 2012
    Assignee: Umecrine AB
    Inventors: Torbjörn Bäckström, Per Lundgren, Ming-De Wang, Inga-Maj Johansson
  • Patent number: 8088758
    Abstract: 3,15-substituted estrone compounds which act as inhibitors of 17?-hydroxysteroid dehydrogenase type I (17?-HSD1), salts thereof, pharmaceutical preparations containing such compounds, processes for preparing such compounds, and therapeutic uses of such compounds, particularly in the treatment or inhibition of steroid hormone dependent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring the inhibition of 17?-hydroxysteroid dehydrogenase type I enzymes and/or requiring the lowering of the endogenous 17?-estradiol concentration, as well as the general use of selective 17?-hydroxysteroid dehydrogenase type 1 inhibitors which possess in addition no or only pure antagonistic binding affinities to the estrogen receptor for the treatment or inhibition of benign gynecological disorders, particularly endometriosis.
    Type: Grant
    Filed: November 9, 2004
    Date of Patent: January 3, 2012
    Assignee: Abbott Products GmbH
    Inventors: Josef Messinger, Heinrich-Hubert Thole, Bettina Husen, Bartholomeus Johannes Van Steen, Gyula Schneider, Johannes Bernardus Everardus Hulshof, Pasi Koskimies, Nina Johansson, Jerzy Adamski
  • Patent number: 7998935
    Abstract: The present invention provides quinaldine-based semisquaraines, symmetrical and unsymmetrical squaraine dyes represented by the general formulae 1, 2 and 3 and/or pharmaceutically acceptable derivatives thereof as sensitizers for photodynamic therapeutical and industrial applications. These symmetrical and unsymmetrical squaraine dyes posses absorption which extends well into the photodynamic window (650-800 nm) and hence are useful for the treatment of deep seated tumors. The absorption of these dyes can be tuned by changing the substituents on the quinaldine moiety thereby enabling the development of a library of dyes which have absorption ranging from 650 to 800 nm. They also exhibited fluorescence emission in the long wavelength region making them useful as near infrared fluorescence sensors for the detection of tumors. These dyes are non-toxic in the dark and exhibit good photocytotoxicity.
    Type: Grant
    Filed: January 8, 2007
    Date of Patent: August 16, 2011
    Assignee: Council of Scientific and Industrial Research
    Inventors: Danaboyina Ramaiah, Jyothish Kuthanapillil, Kalliat Thazhathveetil Arun
  • Patent number: 7960367
    Abstract: Steroid compounds processing a hydrogen donor in 3beta position, either in the form of a hydroxy- or a sulfate group, function as efficient blockers of the 3alpha-hydroxy-pregnan-steroid action and thus have utility as therapeutic substances for the prevention and/or treatment of steroid related CNS disorders. Treatment methods based on the administration of these substances are disclosed, and these substances either alone or in combination are also suggested for the manufacture of pharmaceuticals for the treatment of many specific steroid induced CNS disorders.
    Type: Grant
    Filed: December 20, 2002
    Date of Patent: June 14, 2011
    Assignee: Umecrine AB
    Inventors: Torbjorn Backstrom, Per Lundgren, Ming-De Wang, Inga-Maj Johansson
  • Patent number: 7888340
    Abstract: Steroid compounds processing a hydrogen donor in 3beta position, either in the form of a hydroxy- or a sulfate group, function as efficient blockers of the 3alpha-hydroxy-pregnan-steroid action and thus have utility as therapeutic substances for the prevention and/or treatment of steroid related CNS disorders. Treatment methods based on the administration of these substances are disclosed, and these substances either alone or in combination are also suggested for the manufacture of pharmaceuticals for the treatment of many specific steroid induced CNS disorders.
    Type: Grant
    Filed: December 20, 2002
    Date of Patent: February 15, 2011
    Assignee: Umecrine AB
    Inventors: Torbjorn Backstrom, Per Lundgren, Ming-De Wang, Inga-Maj Johansson
  • Publication number: 20100324004
    Abstract: This application is directed to the use of steroid compounds for the selective inhibition of the enzyme PTP1B in a mammal for the treatment of diabetes.
    Type: Application
    Filed: September 8, 2008
    Publication date: December 23, 2010
    Inventors: Michael McLane, Inez Ruiz-White, Henry Wolfe
  • Patent number: 7816348
    Abstract: Compounds of formula I: wherein X, R2, R3, R5 and R6 are defined herein, are useful as inhibitors of the hepatitis C virus NS5B polymerase.
    Type: Grant
    Filed: January 29, 2007
    Date of Patent: October 19, 2010
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Rene Coulombe, Gulrez Fazal, Jean Rancourt, Timothy Stammers, Bounkham Thavonekham
  • Patent number: 7691836
    Abstract: The subject invention provides a compound according to Formula I, wherein each of the substituents is given the definition as set forth in the specification and claims, or a pharmaceutically acceptable salt and/or hydrate form and/or prodrug thereof.
    Type: Grant
    Filed: March 18, 2005
    Date of Patent: April 6, 2010
    Assignee: N.V. Organon
    Inventors: Johannes Antonius Maria Hamersma, Johannes Bernardus Maria Rewinkel
  • Patent number: 7687486
    Abstract: Compositions and methods for treating a cancer in mammals by administering selective estrogen receptor modulators particularly compounds represented by: or any other of the structures contained herein, or of a stereoisomer, enantiomer, rotomer, tautomer or pharmaceutically acceptable salt form thereof.
    Type: Grant
    Filed: March 5, 2005
    Date of Patent: March 30, 2010
    Assignee: Florida Agricultural & Mechanical University
    Inventor: John S. Cooperwood
  • Patent number: 7662838
    Abstract: The invention relates to the use of a deoxynojirimycin derivative, or pharmaceutically acceptable salt thereof, for the preparation of a medicament for the treatment of insulin resistance, hyperpigmentation and/or inflammatory processes in the skin, a fungal disease, overweight and obesity, or a microbacterial infection.
    Type: Grant
    Filed: October 29, 2004
    Date of Patent: February 16, 2010
    Assignee: Genzyme Corporation
    Inventor: Johannes Maria Franciscus Gerardus Aerts
  • Patent number: 7601706
    Abstract: This invention is directed to compounds that provide for sustained systemic concentrations of therapeutic or prophylactic agents following administration to animals. This invention is also directed to pharmaceutical compositions including and methods using such compounds.
    Type: Grant
    Filed: March 24, 2006
    Date of Patent: October 13, 2009
    Assignee: XenoPort, Inc.
    Inventors: Kenneth C. Cundy, Mark A. Gallop, Cindy X. Zhou
  • Patent number: 7498321
    Abstract: There are provided according to the invention compounds of formula (I) wherein R1 represents C1-6 alkyl or C1-6 haloalkyl; R2 represents —C(?O)-aryl or —C(?O)-heteroaryl; R3 represents hydrogen, methyl (which may be in either the ? or ? configuration) or methylene; R4 and R5 are the same or different and each represents hydrogen or halogen; and——represents a single or a double bond; and salts and solvates thereof. There are also provided processes for preparing compounds of formula (I) and use of the compounds in therapy especially in the treatment of inflammatory and allergic conditions.
    Type: Grant
    Filed: August 3, 2001
    Date of Patent: March 3, 2009
    Assignee: Glaxo Group Limited
    Inventors: Keith Biggadike, Paul Jones, Jeremy John Payne
  • Publication number: 20080255075
    Abstract: Substituted estratriene compounds of formula (I) useful in therapy, especially in the treatment or inhibition of a steroid hormone dependent disorder requiring the inhibition of a 17?-hydroxysteroid dehydrogenase (17?-HSD) type 1, type 2 and/or type 3 enzyme, as well as their salts, pharmaceutical compositions containing such compounds and processes for preparing such compounds.
    Type: Application
    Filed: November 29, 2007
    Publication date: October 16, 2008
    Applicant: Solvay Pharmaceuticals GmbH
    Inventors: Josef MESSINGER, Uwe Schoen, Heinrich-Hubert Thole, Bettina Husen, Pasi Koskimies, Mikko Unkila
  • Patent number: 7407947
    Abstract: An amphoteric compound based on a sterol skeleton, the 3-position of the sterol ring system being substituted by one or more amphoteric groups having an isoelectric point of between about 4 and 9, together with liposomes containing such compounds and their uses.
    Type: Grant
    Filed: February 21, 2002
    Date of Patent: August 5, 2008
    Assignee: Novosom AG
    Inventors: Steffen Panzner, Gerold Endert, Stefan Fankhaenel, Nasr El-Mokdad
  • Publication number: 20080113017
    Abstract: A sterol derivative with a pKa value of between 3.5 and 8, according to the general formula cation-spacer 2-Y-spacer 1-X-sterol, wherein Y and X represent linking groups, is suggested, as well as liposomes comprising such sterol derivatives.
    Type: Application
    Filed: November 2, 2007
    Publication date: May 15, 2008
    Applicant: NOVOSOM AG
    Inventors: STEFFEN PANZNER, Gerold Endert, Stefan Fankhanel, Anja Behrens
  • Patent number: 7312206
    Abstract: Disclosed is a sterol derivative having a pKa value of 3.5-8 according to the general formula cation-spacer 2-Y-spacer 1-X-sterol, wherein Y and X represent bonding groups. The invention also relates to liposomes containing said sterol derivatives.
    Type: Grant
    Filed: February 21, 2002
    Date of Patent: December 25, 2007
    Assignee: Novosom AG
    Inventors: Steffen Panzner, Gerold Endert, Stefan Fankhänel, Anja Behrens
  • Publication number: 20070207989
    Abstract: The present invention relates to useful diterpenes and pharmaceutical compositions containing them of the formula: for use in the treatment of cardiovascular and inflammatory diseases and for cancers susceptible to an NF-?B inhibitor and an endothelin receptor inhibitor. The present invention also relates to compounds and methods useful to inhibit cell proliferation and for the induction of apoptosis.
    Type: Application
    Filed: March 1, 2007
    Publication date: September 6, 2007
    Applicant: SaviPu Pharmaceuticals
    Inventors: Inderjit Kumar Dev, Ven Subbiah
  • Patent number: 7153844
    Abstract: wherein X may be —CH2—O—CH2— or —CH2—, wherein n may be 1, 2, 3, 4 or 5 when X is —CH2—O—CH2—, wherein n may be 2, 3, 4, 5, 6, 7, 8, 9 or 10 when X is —CH2—, wherein o may be 1, 2 or 3, wherein Y may be O or 17?-OH, where the dotted line represents the presence or absence of a second chemical bond, wherein R1 may be selected from the group consisting of H, straight alkyl groups of 1 to 5 carbon atoms, and branched alkyl groups of 3 to 5 carbon atoms, wherein R2 may be selected for the group consisting of H, straight alkyl groups of 1 to 4 carbon atoms, branched alkyl groups of 3 or 4 carbon atoms, F, Cl, Br, I, —CF3, —NO2, —OR1, where R1 is as defined hereinabove, —COR1, where R1 is as defined hereinabove, and —CH2OH. These compounds possess anticancer activity against hormono-dependent breast, uterus as well as ovarian cancers.
    Type: Grant
    Filed: March 27, 2003
    Date of Patent: December 26, 2006
    Inventor: Gervais Bérubé
  • Patent number: 7115758
    Abstract: The invention relates to vitamin D derivatives of general formula I, process for their production, intermediate products of the process as well as the use for the production of pharmaceutical agents.
    Type: Grant
    Filed: November 26, 2002
    Date of Patent: October 3, 2006
    Assignee: Schering AG
    Inventors: Andreas Steinmeyer, Katica Schwarz, Claudia Giesen, Martin Haberey, Marianne Fähnrich
  • Patent number: 6984634
    Abstract: This invention is directed to compounds that provide for sustained systemic concentrations of therapeutic or prophylactic agents following administration to animals. This invention is also directed to pharmaceutical compositions including and methods using such compounds.
    Type: Grant
    Filed: October 9, 2001
    Date of Patent: January 10, 2006
    Assignee: XenoPort, Inc.
    Inventors: Kenneth C. Cundy, Mark A. Gallop
  • Patent number: 6953785
    Abstract: Provided is steroid sulfatase inhibitors comprising, as the active ingredient, an estra-1,3,5(10)-triene derivative which is represented by formula (I): {wherein R1 and R2 are the same or different and represent a hydrogen atom, a lower alkyl group or, etc.; R3 represents a hydrogen atom etc.; R4 represents a hydrogen atom etc.; R5 represents a hydrogen atom etc.; R6 represents a cyano group, an amino group, COR53 (wherein R53 represents a substituted lower alkyl group etc.), a substituted or unsubstituted aryl group, a substituted or unsubstituted heterocyclic group, etc}, or pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: April 24, 2001
    Date of Patent: October 11, 2005
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Yoji Ino, Nobuyoshi Amishiro, Mayumi Miyata, Tsutomu Agatsuma, Kozue Muramatsu, Takeshi Takahashi, Shiro Akinaga, Chikara Murakata
  • Patent number: 6916921
    Abstract: The present invention relates to steroid compounds of general formula X, which may advantageously be employed to stimulate meiosis in human oocytes, the steroid being specifically characterized by amino nitrogen bonded to C17 of the steroid skeleton via a spacer A.
    Type: Grant
    Filed: March 26, 2002
    Date of Patent: July 12, 2005
    Assignees: Schering AG, Novo Nordisk D/S
    Inventors: Thorsten Blume, Peter Esperling, Christa Hegele-Hartung
  • Patent number: 6900193
    Abstract: The present invention relates, inter alia, to compounds having the general formula: in which: R1 is a member selected from the group consisting of —OCH3, —SCH3, —N(CH3)2, —NHCH3, —NC4H8, —NC5H10, —NC4H8O, —CHO, —CH(OH)CH3, —C(O)CH3, —O(CH2)2N(CH3)2, and —O(CH2)2NC5H10; R2 is a member selected from the group consisting of hydrogen, halogen, alkyl, acyl, hydroxy, alkoxy (e.g., methoxy, ethoxy, vinyloxy, ethynyloxy, cyclopropyloxy, etc.), acyloxy (e.g., acetoxy, glycinate, etc.), alkylcarbonate, cypionyloxy, S-alkyl, —SCN, S-acyl and —OC(O)R6, wherein R6 is a functional group including, but not limited to, alkyl (e.g., methyl, ethyl, etc.), alkoxy ester (e.g., —CH2OCH3) and alkoxy (—OCH3); R3 is a member selected from the group consisting of alkyl, hydroxy, alkoxy and acyloxy; R4 is a member selected from the group consisting of hydrogen and alkyl; and X is a member selected from the group consisting of ?O and ?N—OR5, wherein R5 is a member selected from the group consisting of hydrogen and alkyl.
    Type: Grant
    Filed: March 17, 2000
    Date of Patent: May 31, 2005
    Assignee: The United States of America as represented by the Department of Health and Human Services
    Inventors: Hyun K. Kim, Richard P. Blye, Pemmaraju N. Rao, James W. Cessac, Carmie K. Acosta, Anne Marie Simmons
  • Publication number: 20040248867
    Abstract: There are provided compounds of formula (I) wherein R1 represents C1-6 alkyl or C1-6 haloalkyl; R2 represents a 4-7 membered non-aromatic ring containing 1-3 heteroatoms selected from O, N and S optionally substituted with one or more methyl, ethyl or halogen groups; R3 represents hydrogen, methyl (which may be in either the &agr; or &bgr; configuration) or methylene; R4 and R5 are the same or different and each represents hydrogen or halogen; and (a) represents a single or a double bond; and salts and solvates thereof; processes for preparing them and their use in therapy.
    Type: Application
    Filed: June 15, 2004
    Publication date: December 9, 2004
    Inventors: Keith Biggadike, Paul Jones
  • Publication number: 20040229853
    Abstract: The subject of the invention is a method for preparing compounds of general formula (I): 1
    Type: Application
    Filed: April 29, 2004
    Publication date: November 18, 2004
    Applicant: Aventis Pharma S.A.
    Inventors: Denis Prat, Christian Moratille, Francoise Benedetti, Lahlou Nait-Bouda
  • Publication number: 20040224933
    Abstract: The invention relates to a process for preparing compounds of formula (I): 1
    Type: Application
    Filed: April 29, 2004
    Publication date: November 11, 2004
    Applicant: Aventis Pharma S.A.
    Inventors: Francois Nique, Christian Moratille, Patrick Roussel, Joelle Bousquet
  • Publication number: 20040192894
    Abstract: The present invention concerns the use of methods and/or compositions related to the synthesis and use of fatty asparagine, cysteine and/or serine derivatives. In particular, the invention concerns methods and compositions for the production of liposomes including fatty asparagine, cysteine and/or serine derivatives.
    Type: Application
    Filed: November 17, 2003
    Publication date: September 30, 2004
    Applicant: Board of Regents, The university of Texas System
    Inventors: Frederick J. Lakner, George R. Negrete
  • Publication number: 20040176340
    Abstract: Disclosed are compounds having the formula: 1
    Type: Application
    Filed: March 17, 2004
    Publication date: September 9, 2004
    Inventor: Laszlo Prokai
  • Publication number: 20040171595
    Abstract: A process for the preparation of compounds of formula (I) 1
    Type: Application
    Filed: January 12, 2004
    Publication date: September 2, 2004
    Inventors: Francoise Benedetti, Alain Mazurie, Francois Nique, Denis Prat, Christian Wehrey
  • Patent number: 6780855
    Abstract: This invention describes the new 11&bgr;-halogen-7&agr;-substituted estratrienes of general formula I in which R11 is a fluorine or chlorine atom, and the other substituents have the meanings that are explained in more detail in the description. The compounds have antiestrogenic properties or tissue-selective estrogenic properties and are suitable for the production of pharmaceutical agents.
    Type: Grant
    Filed: December 2, 1999
    Date of Patent: August 24, 2004
    Assignee: Schering Aktiengesellschaft
    Inventors: Rolf Bohlmann, Nikolaus Heinrich, Helmut Hofmeister, Jorg Kroll, Hermann Kunzer, Gerhard Sauer, Ludwig Zorn, Karl-Heinrich Fritzemeier, Monika Lessl, Rosemarie Lichtner, Yukishige Nishino, Karsten Parczyk, Martin Schneider
  • Publication number: 20040138446
    Abstract: The invention concerns biotin derivatives of general formula (I), wherein: R1 represents a specific compound; X1 represents a carbonaceous chain, preferably of 1 to 10 carbon atoms, substituted or not, optionally comprising one or several carbonyl or oxycarbonyl groups, and/or a —NH— group, in particular a chain of formula —HN(CH2)n—O—CO wherein n is an integer between 1 and 5 and optionally comprising one or several ether, amide and/or amino functions; Y represents a hydrocarbon chain of 1 to 5 carbon atoms, substituted or not; R2 represents a hydrogen atom, or a protecting group, in particular R2 represents an alkyl group of 1 to 5 carbon atoms. The invention is useful as vectors, in particular for implementing methods for detecting interactions between biological compounds, and in pharmaceutical compositions.
    Type: Application
    Filed: December 9, 2003
    Publication date: July 15, 2004
    Inventors: Abdelakim Kharrat, Khalil Bouayadi, Jean-Charles Faye, Emmanuelle Fourcade, Rudi Baron, Daniel Tovar, Casimir Blonski
  • Publication number: 20040138186
    Abstract: A compound of the formula 1
    Type: Application
    Filed: July 21, 2003
    Publication date: July 15, 2004
    Applicant: Inflazyme Pharmaceuticals Ltd.
    Inventors: Jeffery R. Raymond, Claudia E. Kasserra, Yaping Shen
  • Publication number: 20040131666
    Abstract: Disclosed is a sterol derivative having a pKa value of 3.5-8 according to the general formula cation-spacer 2-Y-spacer 1-X-sterol, wherein Y and X represent bonding groups. The invention also relates to liposomes containing said sterol derivatives.
    Type: Application
    Filed: February 11, 2004
    Publication date: July 8, 2004
    Inventors: Steffan Panzner, Gerold Endert, Stefan Fankhnel, Anja Behrens
  • Publication number: 20040132695
    Abstract: The present invention provides novel C24-sulfone analogs of 1&agr;,25-dihydroxy vitamin D3, compositions comprising these compounds and methods of using these compounds as selective inhibitors of CYP24. In particular, the compounds of the invention are useful for treating diseases which benefit from a modulation of the levels of 1&agr;,25-dihydroxy vitamin D3, for example, cell-proliferative disorders.
    Type: Application
    Filed: July 3, 2003
    Publication date: July 8, 2004
    Inventors: Gary H. Posner, Kenneth Crawford, Hong Woon Yang, HeungBae Jeon, Mark Hatcher, Byung-Chul Suh, Jay White, Glenville Jones
  • Publication number: 20040120997
    Abstract: The invention relates to a sterol skeleton based compound wherein one or several amphoteric groups with an isoelectric point of between 4 and 9 are substituted on the 3rd position of the ring system, in addition to liposomes containing said compounds.
    Type: Application
    Filed: February 11, 2004
    Publication date: June 24, 2004
    Inventors: Steffan Panzner, Gerold Endert, Stefan Fankhnel, Nasr El-Mokdad
  • Patent number: 6740645
    Abstract: The invention is directed to a novel class of 17&bgr;-acyl-17&agr;-propynyl steroids which exhibit potent antiprogestational activity.
    Type: Grant
    Filed: September 3, 1999
    Date of Patent: May 25, 2004
    Assignee: Research Triangle Institute
    Inventors: C. Edgar Cook, John A. Kepler, Jill M. O'Reilly