Chalcogen In Chain Between The Hetero Ring And The Cyclopentanohydrophenanthrene Ring System Patents (Class 540/113)
  • Patent number: 9487500
    Abstract: Novel compounds and their synthesis are described. Methods for using these compounds in the prevention or treatment of cancer, a bacterial infection or a viral infection in a subject are also described.
    Type: Grant
    Filed: October 4, 2013
    Date of Patent: November 8, 2016
    Assignee: INHIBIKASE THERAPEUTICS, INC.
    Inventors: Rhushikesh C. Deokar, Sundeep H. Dugar, Dinesh Mahajan, Milton H. Werner
  • Patent number: 9456971
    Abstract: Provided is a moisturizer having hygroscopicity and water retention ability, and also provided is a composition superior in antiseptic property and feeling on application, in addition to moisturizing property, and free of coloration and odorization. A moisturizer containing acylproline represented by the formula (1) wherein an acyl group represented by R1—CO— is an acyl group derived from a saturated or unsaturated fatty acid having 3-23 carbon atoms, or a salt thereof, and a composition containing (A) acylproline represented by the above formula (1) or a salt thereof and (B) bisphosphonate.
    Type: Grant
    Filed: December 29, 2014
    Date of Patent: October 4, 2016
    Assignee: AJINOMOTO CO., INC.
    Inventors: Takanori Sugimoto, Nana Haraya, Masatoshi Saito
  • Patent number: 9321804
    Abstract: Disclosed are the general structural formula of LQC-Y as well as the synthesis and use thereof. Pharmacological experiments demonstrated the marked antitumor effect of such compounds. Single day administration of LQC-Y3 to mice at a maximum dose of 6000 mg/kg showed no toxicity response during the 14-day continuous observation period, indicating the high safety of the compounds, and the compounds can be used to prepare medicaments for preventing and treating carcinomas such as liver cancer, lung cancer.
    Type: Grant
    Filed: September 4, 2013
    Date of Patent: April 26, 2016
    Assignee: 3D MEDICINES, LTD.
    Inventor: Haimin Lei
  • Patent number: 8969328
    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: Grant
    Filed: February 8, 2011
    Date of Patent: March 3, 2015
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Wolfgang Schwede, Ulrich Klar, Carsten Möller, Andrea Rotgeri, Wilhelm Bone, Christoph Huwe
  • Patent number: 8921568
    Abstract: Iminosugar compounds are described that have inbuilt delivery features by virtue of covalent incorporation of a tocopherol moiety, or alternative moieties that are analogs of tocopherol or select analogs of cholesterol, or its antagonist “Ezitimibe”; and are likely to have broad spectrum antiviral activity. The compounds differ from previous iminosugar compounds, even lipophillic ones, being more hydrophobic and resembling fats and oils in their partition behavior in vivo into lipid phases of lipoproteins, cellular lipid droplet organelles and biological membranes. These features confer a number of unique delivery attributes in vivo, favorable to the therapy of virus infections involving cells of the lymphoid system and the liver, in particular, but these features are also favorable in general for the treatment of virus infections of man and animals.
    Type: Grant
    Filed: June 5, 2013
    Date of Patent: December 30, 2014
    Assignees: Unither Virology, LLC, The Chancellor, Masters and Scholars of The University of Oxford
    Inventors: J. L. Kiappes, Peter Laing, Raymond Dwek, Nicole Zitzmann, Stephanie Pollock
  • Publication number: 20140155362
    Abstract: Embodiments of the present disclosure provide for BHQ-conjugates and protected BHQ-conjugate precursor compounds, methods of making BHQ-conjugates and protected BHQ-conjugate precursor compounds, methods of using BHQ-conjugates and protected BHQ-conjugate precursor compounds, and the like.
    Type: Application
    Filed: June 28, 2012
    Publication date: June 5, 2014
    Inventors: Timothy M. Dore, James D. Lauderdale, Adam C. Rea, Adna Muliawan, Duncan McLain
  • Publication number: 20140121367
    Abstract: The present invention relates to the synthesis and application of novel chiral/achiral substituted methyl formyl reagents to modify pharmaceutical agents and/or biologically active substances to modify the physicochemical, biological and/or pharmacokinetic properties of the resulting compounds from the unmodified original agent.
    Type: Application
    Filed: April 9, 2012
    Publication date: May 1, 2014
    Inventors: Sundeep Dugar, Dinesh Mahajan, Frank Peter Hollinger
  • Publication number: 20130331578
    Abstract: Iminosugar compounds are described that have inbuilt delivery features by virtue of covalent incorporation of a tocopherol moiety, or alternative moieties that are analogues of tocopherol or select analogues of cholesterol, or its antagonist “Ezitimibe”; and are likely to have broad spectrum antiviral activity. The compounds differ from previous iminosugar compounds, even lipophillic ones, being more hydrophobic and resembling fats and oils in their partition behavior in vivo into lipid phases of lipoproteins, cellular lipid droplet organelles and biological membranes. These features confer a number of unique delivery attributes in vivo, favorable to the therapy of virus infections involving cells of the lymphoid system and the liver, in particular, but these features are also favorable in general for the treatment of virus infections of man and animals.
    Type: Application
    Filed: June 5, 2013
    Publication date: December 12, 2013
    Inventors: J. L. Kiappes, Peter Laing, Raymond Dwek, Nicole Zitzmann, Stephanie Pollock
  • Publication number: 20130245253
    Abstract: The present disclosure provides modified neuroactive steroids. The modified neuroactive steroids may comprise, consist of, or consist essentially of a therapeutic agent and/or a modifying moiety. The modified neuroactive steroid can have modified characteristics as compared to native neuroactive steroids that do not include a modifying moiety and/or therapeutic agent. The modified neuroactive steroid may be, for example, modified pregnenolone, pregnenolone metabolites, allopregnanolone, and/or allopregnanolone metabolites. The modified neuroactive steroids can be used to treat, prevent and/or ameliorating a phenotypic state of interest in a subject.
    Type: Application
    Filed: March 28, 2011
    Publication date: September 19, 2013
    Applicants: DEPARTMENT OF VETERANS AFFAIRS, DUKE UNIVERSITY
    Inventors: Christine Marx, Robert Mook
  • Publication number: 20130072438
    Abstract: Disclosed herein are opioid peptide conjugates (for example, opioid peptide esters). In some embodiments, the disclosed conjugates include an opioid peptide consisting of two to six amino acids and a moiety conjugated to the opioid peptide by an ester bond. In some examples, the moiety is an alcohol, a sugar, a lipid, or dehydroascorbic acid. Also disclosed are methods of altering nociception including administering an effective amount of one or more disclosed opioid peptide conjugates to a subject (such as a human subject).
    Type: Application
    Filed: September 13, 2012
    Publication date: March 21, 2013
    Inventor: Joel S. Goldberg
  • Publication number: 20120309698
    Abstract: The disclosure generally relates to the novel compounds of formula I, including their salts, which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions and methods for treating those infected with HIV.
    Type: Application
    Filed: December 6, 2011
    Publication date: December 6, 2012
    Inventors: Yasutsugu Ueda, Timothy P. Connolly, Barry L. Johnson, Chen Li, B. Narasimhulu Naidu, Manoj Patel, Kevin Peese, Margaret E. Sorenson, Michael A. Walker, Michael S. Bowsher, Rongti Li
  • Publication number: 20120253032
    Abstract: The instant invention provides for novel cationic lipids with short lipid chains that can be used in combination with other lipid components such as cholesterol and PEG-lipids to form lipid nanoparticles with oligonucleotides, to facilitate the cellular uptake and endosomal escape, and to knockdown target mRNA both in vitro and in vivo while decreasing inflammatory toxicities.
    Type: Application
    Filed: September 20, 2010
    Publication date: October 4, 2012
    Inventors: Mark Cameron, Jennifer R. Davis, Weimin Wang
  • Publication number: 20120245110
    Abstract: The present disclosure relates to a novel vascular leakage inhibitor. The novel vascular leakage inhibitor of the present disclosure inhibits the apoptosis of vascular endothelial cells, inhibits the formation of actin stress fibers induced by VEGF, enhances the cortical actin ring structure, and improves the stability of the tight junctions (TJs) between vascular cells, thereby inhibiting vascular leakage. The vascular leakage inhibitor of the present disclosure has the activity of not only reducing vascular permeability but also recovering the integrity of damaged blood vessels. Accordingly, the vascular leakage inhibitor of the present disclosure can prevent or treat various diseases caused by vascular leakage. Since the vascular leakage inhibitor of the present disclosure is synthesized from commercially available or easily synthesizable cholesterols, it has remarkably superior feasibility of commercial synthesis.
    Type: Application
    Filed: October 29, 2010
    Publication date: September 27, 2012
    Inventors: Young-Guen Kwon, Young-Ger Suh
  • Publication number: 20120238740
    Abstract: The present invention provides novel and advantageous processes for preparing and purifying pharmaceuticals The processes comprise a nucleophilic reaction wherein a modified leaving group LM, which has increased lipophilicity, of a vector in a nucleophilic reaction which offers a convenient and time-saving way to purify the product from non-reacted precursors vector-LM and by-products LM.
    Type: Application
    Filed: July 6, 2010
    Publication date: September 20, 2012
    Applicant: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Keith Graham, Mathias Berndt, Dae Yoon Chi, Byoung Se Lee, Sandip S. Shinde, Hee Seup Kil, Sang Ju Lee, Jin-Sook Ryu, Seung Jun Oh
  • Publication number: 20120232042
    Abstract: The invention relates to 17-hydroxy-13-methyl-17-pentafluoroethyl-11-acyloxyalkylenephenyldodecahydrocyclopenta[a]phenanthren-3-one 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 7, 2010
    Publication date: September 13, 2012
    Applicant: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Ulrich Klar, Wolfgang Schwede, Carsten Moller, Andrea Rotgeri, Ursula Krenz
  • Patent number: 8258328
    Abstract: The subject of the invention is a method for preparing compounds of general formula (I): in which A, Z, R3 are as defined in the description, and the intermediate compounds for carrying out this method.
    Type: Grant
    Filed: October 29, 2010
    Date of Patent: September 4, 2012
    Assignee: Aventis Pharma S.A.
    Inventors: Denis Prat, Christian Moratille, Francoise Benedetti, Lahlou Nait-Bouda
  • 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: 20120177634
    Abstract: This disclosure concerns novel demethylpenclomedine analogs. Also disclosed are pharmaceutical compositions and methods for using such compositions to treat hyperproliferative disorders.
    Type: Application
    Filed: February 22, 2012
    Publication date: July 12, 2012
    Inventor: Lee Roy Morgan
  • Publication number: 20120149894
    Abstract: The instant invention provides for novel cationic lipids that can be used in combination with other lipid components such as cholesterol and PEG-lipids to form lipid nanoparticles with siRNA, to facilitate the cellular uptake and endosomal escape, and to knockdown target mRNA both in vitro and in vivo.
    Type: Application
    Filed: August 18, 2010
    Publication date: June 14, 2012
    Inventors: Mark Cameron, Jennifer R. Davis, Andrea R. Geiser, Matthew G. Stanton, Vladislav V. Telyatnikov, Lu Tian, Weimin Wang
  • Publication number: 20120135065
    Abstract: An amphoteric liposome composed of a mixture of lipids, said mixture comprising a cationic amphiphile, an anionic amphiphile and optionally one or more neutral amphiphiles, at least one of said cationic and anionic amphiphiles being chargeable and the respective amounts of said cationic and anionic amphiphiles being selected such there is a stoichiometric excess of positively charged cationic amphiphile at a first lower pH, a stoichiometric excess of negatively charged anionic amphiphile at a second higher pH and said mixture has an isoelectric point intermediate said first and second pHs; characterised in that said positively charged cationic and negatively charged anionic amphiphiles are adapted to form a lipid salt with one another at said isoelectric point. Also disclosed are methods of predicting the fusogenicity of an amphoteric liposome at a given pH, formulating an amphoteric liposome and loading an amphoteric liposome with a cargo moiety.
    Type: Application
    Filed: January 13, 2012
    Publication date: May 31, 2012
    Inventors: Steffen Panzner, Silke Lutz, Evgenios Siepi, Claudia Müller
  • Publication number: 20120071453
    Abstract: A compound with general formula I for treatment of various diseases of the central nervous system, in treatment of neuropsychiatric disorders related to imbalance of glutamatergic neurotransmitter system, ischemic damage of CNS, neurodegenerative changes and disorders of CNS, affective disorders, depression, PTSD and other diseases related to stress, anxiety, schizophrenia and psychotic disorders, pain, addictions, multiple sclerosis, epilepsy and gliomas.
    Type: Application
    Filed: May 28, 2010
    Publication date: March 22, 2012
    Inventors: Hana Chodounska, Eva Stastna, Vojtech Kapras, Ladislav Kohout, Jirina Borovska, Ladislav Vyklicky, Karel Vales, Ondrej Cais, Lukas Rambousek, Ales Stuchlik, Vera Valesova
  • Publication number: 20110200582
    Abstract: Disclosed are formulation and optimization protocols for delivery of therapeutically effective amounts of biologically active agents to liver, tumors, and/or other cells or tissues. Also provided are compositions and uses for cationic lipid compounds of formula (I). The invention also relates to compositions and uses for stealth lipids of formula (XI). Also provided are processes for making such compounds, compositions, and formulations, plus methods and uses of such compounds, compositions, and formulations to deliver biologically active agents to cells and/or tissues.
    Type: Application
    Filed: December 21, 2010
    Publication date: August 18, 2011
    Applicant: NOVARTIS AG
    Inventors: Jeremy BARYZA, Keith BOWMAN, Andrew GEALL, Tanzina LABONTE, Cameron LEE, Chandra VARGEESE, Laura WEST, Junping ZHAO
  • Publication number: 20110046599
    Abstract: Compositions and methods for modifying biologically active substances to achieve multi-day delivery of such substances, particularly through oral or parenteral administration, are disclosed. The compositions include the biologically active substance conjugated to a carrier having a suitably long half life, typically more than one day, wherein the conjugate optionally contains a spacer linking the carrier to the biologically active substance. Pharmaceutical formulations of the conjugates are also disclosed, as are methods of extending delivery of a single dose of a biologically active substance for more than one day.
    Type: Application
    Filed: June 26, 2008
    Publication date: February 24, 2011
    Inventor: Agis Kydonieus
  • Patent number: 7875712
    Abstract: This invention provides caspase inhibitors of formula I: wherein Z is oxygen or sulfur; R1 is hydrogen, —CHN2, R, CH2OR, CH2SR, or —CH2Y; ?between R3 and R4 represents a single or double bond; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; R3 is a group capable of fitting into the S2 subsite of a caspase enzyme; R4 is a hydrogen or C1-6 alkyl or R3 and R4 taken together form a ring; Ring A and Ring B are each heterocyclic rings, and R and R5 are as described in the specification. The compounds are effective inhibitors of apoptosis and IL-1? secretion.
    Type: Grant
    Filed: September 23, 2008
    Date of Patent: January 25, 2011
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Michael Mortimore, Andrew Miller, John Studley, Jean-Damien Charrier
  • Publication number: 20100324003
    Abstract: New aminooxime derivatives at position 3 of 2- and/or 4-substituted androstanes and androstenes, processes for their preparation, and to pharmaceutical compositions containing them for the treatment of cardiovascular disorders, such as heart failure and hypertension. In particular compounds having the general formula (I) are described, where the radicals have the meanings described in detail in the application.
    Type: Application
    Filed: September 18, 2008
    Publication date: December 23, 2010
    Applicant: SIGMA-TAU INDUSTRIE FARMACEUTICHE RIUNITE S.P.A.
    Inventors: Alberto Cerri, Giuseppe Bianchi, Giorgio Fedrizzi, Patrizia Ferrari, Mauro Gobbini, Giuseppe Marazzi, Marco Torri, Walter Cabri
  • Publication number: 20090286973
    Abstract: This invention relates composition and methods for making and using chemically modified oligonucleotides agents for inhibiting gene expression.
    Type: Application
    Filed: July 2, 2009
    Publication date: November 19, 2009
    Applicant: ALNYLAM PHARMACEUTICALS, INC.
    Inventors: Muthiah MANOHARAN, Venkitasamy KESAVAN, Kallanthottathil G. RAJEEV
  • 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
  • Publication number: 20090215736
    Abstract: This invention provides caspase inhibitors of formula I: wherein Z is oxygen or sulfur; R1 is hydrogen, —CHN2, R, CH2OR, CH2SR, or —CH2Y; between R3 and R4 represents a single or double bond; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; R3 is a group capable of fitting into the S2 subsite of a caspase enzyme; R4 is a hydrogen or C1-6 alkyl or R3 and R4 taken together form a ring; Ring A and Ring B are each heterocyclic rings, and R and R5 are as described in the specification. The compounds are effective inhibitors of apoptosis and IL-1? secretion.
    Type: Application
    Filed: September 23, 2008
    Publication date: August 27, 2009
    Applicant: Vertex Pharmaceuticals, Incorporated
    Inventors: Michael Mortimore, Andrew Miller, John Studley, Jean-Damien Charrier
  • Patent number: 7576055
    Abstract: This invention relates to a highly efficient artificial low-density lipoprotein (LDL) carrier system for the targeted delivery therapeutic agents across the blood-brain barrier (BBB). In particular, this invention relates to artificial LDL particles comprised of three lipid elements: phosphatidyl choline, fatty-acyl-cholesterol esters, and at least one apolipoprotein. The present invention further relates to compositions, methods and kits comprising artificial LDL particles for targeting drugs to and across the BBB for the prevention and treatment of brain diseases.
    Type: Grant
    Filed: May 21, 2007
    Date of Patent: August 18, 2009
    Assignee: Blanchette Rockefeller Neurosciences Institute
    Inventors: Thomas Nelson, Alessandro Quattrone, Daniel Alkon
  • Publication number: 20090105202
    Abstract: The disclosure provides androsterone derivatives. The derivatives of the disclosure are useful in the treatment of androgen- and estrogen-associated diseases and disorders, including breast cancer.
    Type: Application
    Filed: October 18, 2006
    Publication date: April 23, 2009
    Applicants: CALIFORNIA PACIFIC MEDICAL CENTER, CATHOLIC HEALTHCARE WEST
    Inventor: Li-Xi Yang
  • Patent number: 7449572
    Abstract: The invention relates to a process for preparing compounds of formula (I): in which R1, R2, R3, n and X are as defined in the description, and to the intermediate compounds for implementing this process.
    Type: Grant
    Filed: April 29, 2004
    Date of Patent: November 11, 2008
    Assignee: Aventis Pharma S.A.
    Inventors: Francois Nique, Christian Moratille, Patrick Roussel, Joëlle Bousquet
  • Patent number: 7442790
    Abstract: This invention provides caspase inhibitors of formula I: wherein Z is oxygen or sulfur; R1 is hydrogen, —CHN2, R, CH2OR, CH2SR, or —CH2Y; between R3 and R4 represents a single or double bond; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; R3is a group capable of fitting into the S2 subsite of a caspase enzyme; R4 is a hydrogen or C1-6 alkyl or R3 and R4 taken together form a ring; Ring A and Ring B are each heterocyclic rings, and R and R5 are as described in the specification. The compounds are effective inhibitors of apoptosis and IL-1? secretion.
    Type: Grant
    Filed: June 28, 2007
    Date of Patent: October 28, 2008
    Assignee: Vertex Pharmaceuticals, Incorporated
    Inventors: Michael Mortimore, Andrew Miller, John Studley, Jean-Damien Charrier
  • Publication number: 20080249075
    Abstract: Retrosteroidal compounds corresponding to formula I, representing progesterone receptor modulators, and their production, and pharmaceutical preparations containing these compounds. These compounds are useful in the treatment of benign gynecological disorders such as endometriosis and uterine fibroids, as well as for female birth control and for hormone replacement therapy.
    Type: Application
    Filed: March 20, 2008
    Publication date: October 9, 2008
    Applicant: Solvay Pharmaceuticals GmbH
    Inventors: Josef Messinger, Christiane Boecker, Heinrich-Hubert Thole, Bettina Husen, Maria Hinaje, Monika Buchholz
  • Publication number: 20080214514
    Abstract: Described herein are steroid derivatives of fullerene moieties, for example fullerene derivatives in which cholesterol, or a cholesterol moiety, is attached via ester, amide, or ether bonds to one of a variety of “linkers,” e.g., chemical groups including alkyl chains and aromatic groups, which are then connected to the fullerene moiety. The steroid moiety can confers useful solubility in components of biological fluids and/or pharmacologically acceptable carriers and can also affect the biodistribution of the fullerenes which makes the derivatives useful in imaging, diagnosis and the treatment or management of disease or complications of disease states.
    Type: Application
    Filed: March 3, 2008
    Publication date: September 4, 2008
    Applicant: Luna Innovations Incorporated
    Inventors: Darren MacFarland, Jing Zhang, Zhiguo Zhou, Robert P. Lenk, Stephen R. Wilson
  • 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
  • Patent number: 7381718
    Abstract: A process for the preparation of compounds of formula (I) in which R1, R2, R3 and n are defined as indicated in the description, use of said compounds as intermediates for the preparation of estrogen derivatives as well as the intermediates of this process.
    Type: Grant
    Filed: June 12, 2002
    Date of Patent: June 3, 2008
    Assignee: Aventis Pharma S.A.
    Inventors: Francoise Benedetti, Alain Mazurie, Francois Nique, Denis Prat, Christian Wehrey
  • 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
  • Patent number: 6921757
    Abstract: Compounds of formula (I), where R is a monovalent cyclic organic group having from 3 to 15 atoms in the ring system, useful as pharmaceuticals
    Type: Grant
    Filed: June 26, 2001
    Date of Patent: July 26, 2005
    Assignee: Novartis AG
    Inventors: Bernard Cuenoud, David Beattie, Thomas Hugo Keller, Gaynor Elizabeth Pilgrim, David Andrew Sandham, Simon James Watson
  • 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
  • Patent number: 6670348
    Abstract: Compounds having an ansamycin anitibiotic, or other moiety which binds to hsp90, coupled to a targeting moiety which binds specifically to a protein, receptor or marker can provide effective targeted delivery of the ansamycin antibiotic leading to the degradation of proteins and death of the targeted cells. These compositions may have different specificity than the ansamycin alone, allowing for a more specific targeting of the therapy, and can be effective in instances where the ansamycin alone has no effect. Thus, these compounds provide an entirely new class of targeted chemotherapy agents with application, depending on the nature of the targeting moiety, to treatment of a variety of different forms of cancer. Such agents can further be used to promote selective degradation of proteins associated with the pathogenesis of others diseases, including antigens associated with autoimmune disorders and pathogenic proteins associated with Alzheimer's disease.
    Type: Grant
    Filed: October 20, 1999
    Date of Patent: December 30, 2003
    Assignee: Sloan-Kettering Institute for Cancer Research
    Inventors: Neal Rosen, Samuel Danishefsky, Ouathek Ouerfelli, Scott D. Kuduk, Laura Sepp-Lorenzino
  • Patent number: 6583130
    Abstract: The invention relates to new C13-substituted estra-1,3,5(10)-trien-3-yl sulfamates of general formula I, wherein R1 represents an acyl residue, oxycarbonyl residue, aminocarbonyl residue, sulfonyl residue, or aminosulfonyl residue, and R15 represents ethyl, methods of preparing same, and pharmaceutical compositions containing these compounds. The compounds of the invention of general formula I inhibit the activity of steroid sulfatase (EC 3.1.6.2) and do not exhibit any estrogenic effect.
    Type: Grant
    Filed: September 6, 2000
    Date of Patent: June 24, 2003
    Assignee: Schering AG
    Inventors: Sigfrid Schwarz, Gerd Müller, Dirk Kosemund, Margit Richter, Olaf Peters, Ina Scherlitz-Hofmann, Thomas Michel, Walter Elger, Gudrun Reddersen, Birgitt Schneider
  • Patent number: 6566542
    Abstract: A process for the preparation of a compound of the formula wherein the substituents are defined as in the specification.
    Type: Grant
    Filed: June 18, 2002
    Date of Patent: May 20, 2003
    Assignee: Aventis Pharma S.A.
    Inventors: Yasmina Bouali, Jacques Mauger, Patrick Van De Velde, Francois Nique
  • Patent number: 6541464
    Abstract: Compounds of the formula Where the substituents are defined in the application.
    Type: Grant
    Filed: February 14, 2002
    Date of Patent: April 1, 2003
    Assignee: Aventis Pharma S.A.
    Inventors: Yamina Bouali, Francois Nique, Jean-Georges Teutsch, Patrick Van De Velde
  • Patent number: 6472382
    Abstract: A subject of the invention is the compounds of formula (I): in which X is a halogen atom, D represents the remainder of an optionally substituted pentagonal or hexagonal ring and optionally carrying an unsaturation, R1, R2, R3, R4, Y and n are as defined in the description, their preparation process and intermediates, their use as medicaments and the compositions containing them.
    Type: Grant
    Filed: December 8, 2000
    Date of Patent: October 29, 2002
    Assignee: Aventis Pharma S.A.
    Inventors: Yamina Bouali, Francois Nique, Jean-Georges Teutsch, Patrick Van De Velde
  • Patent number: 6436917
    Abstract: New non-estrogenic derivative compounds of estradiol, which have no estrogenic activity and comparatively high anti-oxidative activity, are disclosed. These new non-estrogenic derivative compounds are potentially useful as non-estrogenic antioxidants, especially for administration in post-menopausal women and in men. The compounds of the invention can also inhibit aromatase and sulfatase.
    Type: Grant
    Filed: June 5, 1998
    Date of Patent: August 20, 2002
    Assignee: Jenapharm GmbH & Co. KG
    Inventors: Peter Droescher, Bernd Menzenbach, Wolfgang Roemer, Birgitt Schneider, Walter Elger, Guenter Kaufmann
  • Patent number: 6423700
    Abstract: A compound of the formula wherein the substituents are as defined in the application and its non-toxic, pharmaceutically acceptable acid and base salts useful for hormone replacement for treating menopause or perimenopause without activity at the uterine level treating osteoporosis and strengthening cardiovascular protection in warm-blooded animals.
    Type: Grant
    Filed: January 5, 2001
    Date of Patent: July 23, 2002
    Assignee: Aventis Pharma S.A.
    Inventors: Yasmina Bouali, Jacques Mauger, Patrick Van De Velde, Francois Nique
  • Patent number: 6399766
    Abstract: A subject of the invention is the compounds of formula (I): in which X is a halogen atom, D represents the remainder of an optionally substituted pentagonal or hexagonal ring and optionally carrying an unsaturation, R1, R2, R3, R4, Y and n are as defined in the description, their preparation process and intermediates, their use as medicaments and the compositions containing them.
    Type: Grant
    Filed: January 10, 2001
    Date of Patent: June 4, 2002
    Assignee: Aventis Pharma S.A.
    Inventors: Yamina Bouali, Francois Nique, Jean-Georges Teutsch, Patrick Van De Velde
  • Patent number: 6355630
    Abstract: This invention provides estrogens and antiestrogens of formula I having the structure wherein X, Y, Z, and R are as defined hereinbefore in the specification, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: October 13, 1998
    Date of Patent: March 12, 2002
    Assignee: American Home Products Corporation
    Inventors: Chris P. Miller, Ivo Jirkovsky, Bach Dinh Tran
  • Patent number: 6339077
    Abstract: The invention relates to substituted 4-benzylaminoquinolines and their hetero analogs, and to the pharmaceutically acceptable salts and physiologically functional derivatives thereof. Compounds of formula I in which the radicals are defined in the specification, and their physiologically tolerated salts, physiologically functional derivatives and processes for their preparation are described. The compounds are suitable, for example, as medicines for the prophylaxis or treatment of gallstones.
    Type: Grant
    Filed: September 22, 2000
    Date of Patent: January 15, 2002
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Armin Hofmeister, Eugen Falk, Heinz-Werner Kleemann, Hans-Willi Jansen, Martin Bickel
  • Publication number: 20010039268
    Abstract: A subject of the invention is the compounds of formula (I): 1
    Type: Application
    Filed: December 8, 2000
    Publication date: November 8, 2001
    Applicant: Hoechst Marion Roussel
    Inventors: Yamina Bouali, Francois Nique, Jean-Georges Teutsch, Patrick Van De Velde