Nitrogen Containing Hetero Ring Patents (Class 514/176)
  • 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: 20130005699
    Abstract: The invention provides a method of treating a disease or condition mediated by vascular hyperpermeability in an animal. The method comprises administering an amount of a danazol compound effective to inhibit vascular hyperpermeability and an amount of a second drug effective to treat the disease or condition. The invention further provides a method of inhibiting vascular hyperpermeability when it is a side effect caused by administration of a drug to, or another treatment of, an animal. The method comprises administration of an amount of a danazol compound effective to inhibit the vascular hyperpermeability. The invention also provides a method of modulating the cytoskeleton of endothelial cells in an animal comprising administering an amount of a danazol compound and an amount of a second drug effective to modulate the cytoskeleton. The present invention also relates to pharmaceutical compositions and kits comprising a danazol compound and a second drug.
    Type: Application
    Filed: September 7, 2012
    Publication date: January 3, 2013
    Applicant: DMI ACQUISITION CORP.
    Inventor: David Bar-Or
  • Patent number: 8338587
    Abstract: The present invention provides named compounds of formula (I) and pharmaceutical compositions containing them and their use in therapy.
    Type: Grant
    Filed: March 30, 2010
    Date of Patent: December 25, 2012
    Assignee: AstraZeneca AB
    Inventors: Frank Burkamp, Peter Hansen, Balint Gabos, Håkan Bladh
  • Patent number: 8334280
    Abstract: The invention relates to novel ligands of the estrogen receptors ? and ? of general formula II, which are useful as an active substance of pharmaceuticals, for example pharmaceutical compositions useful for hormone replacement therapy, as well as for the treatment of tumors and inflammatory diseases. The invention also relates to a novel preparation method of these ligands comprising cyclotrimerization of ethynylestradiol with the appropriate diyne in an organic solvent. Further, the invention relates to pharmaceuticals comprising the novel compounds according to the invention.
    Type: Grant
    Filed: May 5, 2009
    Date of Patent: December 18, 2012
    Assignees: Ustav Molekularni Genetikv AV CR, V.V.I., Ustav Organicke Chemie A Biochemie AV CR, V.V.I., Univerzita Karlova V Praze, Prirodovedecka Fukulta UK
    Inventors: Petr Novak, David Sedlak, Petr Bartunek, Martin Kotora
  • 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: 20120309722
    Abstract: The invention features pharmaceutical compositions and dosing regimens for the treatment of immunoinflammatory disorders.
    Type: Application
    Filed: August 16, 2012
    Publication date: December 6, 2012
    Inventor: Mahesh Padval
  • Publication number: 20120309730
    Abstract: This invention relates, e.g., to compositions comprising oxysterol compounds represented by Formula I or Formula II, e.g., comprising one or more of Oxy 16, Oxy 22, Oxy30, Oxy 31, Oxy35, Oxy37, Oxy43, Oxy44, Oxy45 or Oxy47. The compounds are shown to be Hedgehog pathway inhibiting, and to act as agonists for liver X receptor (LXR). Also disclosed are methods of using compositions of the invention to inhibit Hedgehog signaling effects, such as cell proliferation, including treating subjects in need thereof, and pharmaceutical compositions and kits for implementing methods of the invention.
    Type: Application
    Filed: February 16, 2011
    Publication date: December 6, 2012
    Applicants: The Johns Hopkins University, The Regents of the University of California
    Inventors: Farhad Parhami, Michael Jung, Khanhlinh Nguyen, Dongwon Yoo, VIncente Meliton
  • 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: 20120302534
    Abstract: The present invention relates to a compound characterized by the following Formula I: or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, X, and Y are as described herein. Compounds of the present invention are useful for the treatment of HIV-1.
    Type: Application
    Filed: February 9, 2011
    Publication date: November 29, 2012
    Inventors: Daxin Gao, Nianhe Han, Zhimin Jin, Fangxian Ning, Jun Tang, Yongyong Wu, Heping Yang
  • Publication number: 20120289471
    Abstract: The present invention is directed to novel therapeutic compounds comprised of an amino acid bonded to a medicament or drug having a hydroxy, amino, carboxy or acylating derivative thereon. These high therapeutic index derivatives have the same utility as the drug from which they are made, and they have enhanced pharmacological and pharmaceutical properties. In fact, the novel drug derivatives of the present invention enhance at least one therapeutic quality, as defined herein. The present invention is also directed to pharmaceutical compositions containing same.
    Type: Application
    Filed: April 18, 2012
    Publication date: November 15, 2012
    Applicant: SIGNATURE R&D HOLDINGS, LLC
    Inventor: V. Ravi Chandran
  • Publication number: 20120289463
    Abstract: Compositions for antagonizing phosphorylation and subsequent degradation of glycogen synthase kinase 3 beta (GSK3?) in epidermal cells are disclosed. GSK3? phosphorylation antagonists include molecules that function to inhibit or reduce the binding activity or enzymatic activity of an upstream signaling molecule leading to GSK3? phosphorylation, or by downregulating the expression of one or more upstream signaling molecules involved in regulating GSK3? phosphorylation. Methods of using the GSK3? phosphorylation antagonists to inhibit or reduce the phosphorylation and degradation of GSK3? in epidermal cells are provided. The methods are useful to promote epithelialization and closure of wounds, such as chronic non-healing wounds.
    Type: Application
    Filed: December 29, 2010
    Publication date: November 15, 2012
    Applicant: New York University
    Inventors: Marjana Tomic-Canic, Harold Brem
  • Publication number: 20120282331
    Abstract: Described herein, in certain embodiments, are steroidal derivatives, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds to treat androgen receptor mediated diseases or conditions.
    Type: Application
    Filed: November 9, 2010
    Publication date: November 8, 2012
    Applicant: TOKAI PHARMACEUTICALS, INC.
    Inventors: Scott C. Chappel, David S. Casebier
  • Publication number: 20120276196
    Abstract: The present invention relates to pharmaceutical compositions of the neuroactive steroid 3?-hydroxy-3?-methoxymethyl-21-(1?-imidazolyl)-5?-pregnan-20-one or a pharmaceutically-acceptable salt or solvate thereof, with properties desirable for use in treating mood disorders and the like. The pharmaceutical compositions provide sustained therapeutic plasma levels of 3?-hydroxy-3?-methoxymethyl-21-(1?-imidazolyl)-5?-pregnan-20-one. The present invention also relates to methods of treating these disorders by administering the pharmaceutical compositions.
    Type: Application
    Filed: May 4, 2012
    Publication date: November 1, 2012
    Applicant: Euro-Celtique S.A.
    Inventor: Richard M. WOODWARD
  • Publication number: 20120271275
    Abstract: Improved medical devices and methods are provided comprising an anabolic agent for wound healing. These improved medical devices and methods can enhance wound healing in wounds from cuts, abrasions, lesions, burns including sunburn, surgical incisions, pressure ulcers, diabetic ulcers, traumatic wounds, or other injuries or maladies, which can be chronic or non-chronic in origin. In some embodiments, the medical device comprises a drug depot that releases the anabolic agent over at least 3 days to enhance wound healing.
    Type: Application
    Filed: April 25, 2011
    Publication date: October 25, 2012
    Applicant: WARSAW ORTHOPEDIC, INC.
    Inventors: Danielle L. Biggs, Jared T. Wilsey
  • Publication number: 20120258939
    Abstract: The present invention provides a method for preparing a sterile suspension of a glucocorticosteroid. The glucocorticosteroids used in the invention are preferably antiinflammatory glucocorticosteroids. By making the last stage of product preparation be the sterilization process, the potential for contamination during manufacture and heat degradation of products is greatly reduced.
    Type: Application
    Filed: April 16, 2012
    Publication date: October 11, 2012
    Applicant: Norton Healthcare Limited
    Inventors: John Miller, Donald MacDonald, Martin Oliver, Matthew Pollard, Paul Ronald, Adrian Ashley, Paul Lamb
  • 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: 20120252773
    Abstract: A method is provided for treating a patient with a medical condition that involves angiogenesis or HIF-1 overexpression with a compound having the structure of formula (I) wherein Z, x, y, and R1 through R11 are as defined herein.
    Type: Application
    Filed: April 26, 2012
    Publication date: October 4, 2012
    Inventors: Khalid Amin, Joy M. Calaoagan, Wan-Ru Chao, Peter D. Hobbs, Keith R. Laderoute, Richard H. Peters, Masato Tanabe
  • 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: 20120238488
    Abstract: The invention features compounds, pharmaceutical compositions and methods useful for the treatment of neoplasia. In particular embodiments, the compounds of the invention are useful for the treatment of multidrug resistant neoplasia.
    Type: Application
    Filed: June 22, 2010
    Publication date: September 20, 2012
    Inventors: Konstantinos Alevizopoulos, Theodora Calogeropoulou, Christos Stournaras
  • Publication number: 20120237502
    Abstract: The present invention relates to a method for the prevention or treatment of certain breast cancers or ovarian cancer comprising administering to a patient in need thereof of a therapeutically effective amount of a 17,20-lyase inhibitor, wherein the breast cancer or ovarian cancer is estrogen receptor (ER) negative.
    Type: Application
    Filed: November 18, 2011
    Publication date: September 20, 2012
    Applicant: Takeda Pharmaceutical Company Limited
    Inventor: James W. Darnowski
  • Publication number: 20120234316
    Abstract: Anti-inflammatory and antiallergic compounds of the glucocorticosteroid series, according to formula (I) according to formula (I) defined herein are useful for treating diseases of the respiratory tract characterized by airway obstruction.
    Type: Application
    Filed: March 15, 2012
    Publication date: September 20, 2012
    Applicant: Chiesi Farmaceutici S.p.A.
    Inventors: Eleonora GHIDINI, Andrea Rizzi
  • Publication number: 20120238531
    Abstract: Anti-inflammatory and antiallergic compounds of the glucocorticosteroid series according to formula (I) defined herein are useful for treating diseases of the respiratory tract characterized by airway obstruction.
    Type: Application
    Filed: March 15, 2012
    Publication date: September 20, 2012
    Applicant: Chiesi Farmaceutici S.p.A.
    Inventors: Eleonora GHIDINI, Anna Maria Capelli
  • 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
  • Publication number: 20120190659
    Abstract: Compounds of Structural Formula I or pharmaceutically acceptable salts thereof, are effective inhibitors of angiogenesis:
    Type: Application
    Filed: April 16, 2010
    Publication date: July 26, 2012
    Applicants: Children's Medical Center Corporation, President and Fellows of Harvard College
    Inventors: Elias James Corey, Barbara Czakó, László Kürti, Akiko Mammoto, Donald E. Ingber
  • 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: 20120184515
    Abstract: The invention relates to 17-hydroxy-17-pentafluoroethylestra-4,9(10)-diene-11-methyleneoxyalkylenearyl derivative 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: July 19, 2012
    Applicant: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Ulrich Klar, Wolfgang Schwede, Carsten Möller, Andrea Rotgeri, Wilhelm Bone
  • Publication number: 20120178726
    Abstract: The present invention provides compounds of formula (I) wherein n, p, R1, R2, X1, X2, X3, X4, X5, R3a, R3b, R4, R5 and R6 are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Application
    Filed: March 12, 2012
    Publication date: July 12, 2012
    Applicant: ASTRAZENECA AB
    Inventors: Håkan Bladh, Frank Burkamp, Balint Gabos, Peter Hansen, Svetlana Ivanova, Karolina Lawitz
  • 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: 20120171126
    Abstract: The present invention provides compounds of Formula (I), and pharmaceutically acceptable salts, solvates, esters, prodrugs, tautomers, or isomers of said compounds), having the general structure: Formula (I) wherein L, R1, R2, R3, R4, R5, and R6 are selected independently of each other and as defined herein. The present invention also provides compounds (and salts, solvates, esters, prodrugs, tautomers, and isomers) of Formulas (H-A), (II-A1), (II-A2), (II-A2.1), (ll-A-2.2), (ll-A-2.3), (II-A4), (H-B), (H-C), (III), (IV), (V), (VI), as described herein. Also provided are pharmaceutical compositions, methods of preparing, and methods of using such compounds in the treatment and prophylaxis of a wide range of immune, autoimmune, and inflammatory diseases and conditions.
    Type: Application
    Filed: June 15, 2010
    Publication date: July 5, 2012
    Inventors: Biju J. Purakkattle, Michael Y. Berlin, Yeon-Hee Lim, Rema D. Bitar, Kevin D. McCormick, Robert G. Aslanian, Yoon Joo Lee, Junying Zheng, Ying Huang, Walter Won
  • 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
  • Publication number: 20120141589
    Abstract: The present invention generally relates to particles for drug delivery and other applications. In one aspect, the present invention relates to a technique for reacting precursor compounds in the presence of a pharmaceutically-active agent to form product (e.g., in the form of particles) in which the agent is substantially contained within the product, and the product is soluble within typical gastric fluid of a mammal. In another aspect, the present invention is generally directed to particles comprising an inorganic pharmaceutically acceptable carrier, such as CaCO3, and an agent. In some cases, at least some of the agent contained within the particles is fluidically inaccessible from externally of the particle. For instance, the agent may be present in isolated domains within the particle. In another aspect, the present invention is generally directed to methods of creating particles.
    Type: Application
    Filed: August 23, 2011
    Publication date: June 7, 2012
    Applicants: BASF SE, President and Fellows of Harvard College
    Inventors: Ben Fan, Roland S. Koltzenburg, Jens B. Rieger, David A. Weitz
  • Publication number: 20120142653
    Abstract: Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, modified C-3 and C-28 betulinic acid derivatives that possess unique antiviral activity are provided as HIV maturation inhibitors. These compounds are useful for the treatment of HIV and AIDS.
    Type: Application
    Filed: June 2, 2011
    Publication date: June 7, 2012
    Inventors: Alicia Regueiro-Ren, Zheng Liu, Jacob Swidorski, Nicholas A. Meanwell, Sing-Yuen Sit, Jie Chen, Yan Chen, Ny Sin
  • Patent number: 8178519
    Abstract: The present invention provides a method for preparing a sterile suspension of a glucocorticosteroid. The glucocorticosteroids used in the invention are preferably antiinflammatory glucocorticosteroids. By making the last stage of product preparation be the sterilization process, the potential for contamination during manufacture and heat degradation of products is greatly reduced.
    Type: Grant
    Filed: November 16, 2005
    Date of Patent: May 15, 2012
    Assignee: Norton Healthcare Limited
    Inventors: John Miller, Paul Ronald, Adrian Ashley, Paul Lamb, Donald MacDonald, Martin Oliver, Matthew Pollard
  • Patent number: 8163724
    Abstract: The present invention provides compounds of formula (I) wherein n, p, R1, R2, X1, X2, X3, X4, X5, R3a, R3b, R4, R5 and R6 are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Grant
    Filed: October 3, 2008
    Date of Patent: April 24, 2012
    Assignee: AstraZeneca AB
    Inventors: Håkan Bladh, Frank Burkamp, Balint Gabos, Peter Hansen, Svetlana Ivanova, Karolina Lawitz
  • Publication number: 20120077777
    Abstract: The present invention relates to a compound of following formula (I): or to a pharmaceutically acceptable salt thereof, as well as to pharmaceutical compositions including same and to the use thereof as a drug, in particular for treating a proliferative disease such as cancer.
    Type: Application
    Filed: May 20, 2010
    Publication date: March 29, 2012
    Applicants: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS), PIERRE FABRE MEDICAMENT
    Inventors: Christophe Long, Yves Guminski, Fadila Derguini, Joséphine Beck, Frédéric Cantagrel
  • Publication number: 20120077789
    Abstract: The invention provides a method of inhibiting vascular hyperpermeability in an animal in need thereof. The method comprises administering a vascular-hyperpermeability-inhibiting amount of a danazol compound to the animal. The invention also provides a method of modulating the cytoskeleton of an endothelial cell in an animal. The method comprises administering an effective amount of a danazol compound to the animal.
    Type: Application
    Filed: December 1, 2011
    Publication date: March 29, 2012
    Applicant: DMI ACQUISITION CORP.
    Inventor: David Bar-Or
  • 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
  • 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
  • Publication number: 20120040930
    Abstract: The invention concerns a triterpene alkaloid of general formula (I). The invention also concerns a method for making same and use thereof as medicine.
    Type: Application
    Filed: January 13, 2006
    Publication date: February 16, 2012
    Inventors: Catherine Guillou, Jean-Yves Lallemand, Thibault Sauvaítre, Jordi Molgo, Denyse Herlem, Daniel Guenard, Françoise Khuong-Huu
  • Publication number: 20120035147
    Abstract: The invention provides a method of inhibiting vascular hyperpermeability in an animal in need thereof. The method comprises administering a vascular-hyperpermeability-inhibiting amount of a danazol compound to the animal. The invention also provides a method of modulating the cytoskeleton of an endothelial cell in an animal. The method comprises administering an effective amount of a danazol compound to the animal.
    Type: Application
    Filed: October 19, 2011
    Publication date: February 9, 2012
    Applicant: DMI ACQUISITION CORP.
    Inventor: David Bar-Or
  • Publication number: 20120028945
    Abstract: Compound of formula (I), wherein the symbol have the meaning reported in the text; for preparing a medicament for the prevention and/or treatment of proteinuria, glomerulosclerosis or renal failure.
    Type: Application
    Filed: March 18, 2010
    Publication date: February 2, 2012
    Inventors: Patrizia Ferrari, Giuseppe Bianchi, Mara Ferrandi
  • 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
  • Publication number: 20110312924
    Abstract: Steroidal C-17 nitrogen-containing heterocycles of Formula I: wherein: the ABCD ring structure is the nucleus of a steroid, or an analog thereof; X is a group capable of coordinating a heme group of CYP17, and Y is an hydroxyl functionality, a suitable ester, or a prodrug group, for the treatment of urogenital and/or androgen-related cancers, such as castration-resistant prostate cancer. The invention provides methods of synthesizing new chemical entities and methods of using the same in treating urogenital and/or androgen-related cancers.
    Type: Application
    Filed: February 5, 2010
    Publication date: December 22, 2011
    Applicant: TOKAI PHARMACEUTICALS, INC.
    Inventor: David Casebier
  • Publication number: 20110312916
    Abstract: Prodrugs of C-17-heterocyclic-steroidal drugs providing improved oral bioavailability and pharmacokinetics are described. The drugs are inhibitors of human CYP 17 enzyme, as well as potent antagonists of both wild type and mutant androgen receptors (AR), and are useful for the treatment of urogenital and/or androgen-related cancers, diseases and/or conditions, such as human prostate cancer, breast cancer, and prostate hyperplasia. The disclosure describes methods of synthesizing and using the prodrugs in cancer therapy.
    Type: Application
    Filed: February 5, 2010
    Publication date: December 22, 2011
    Applicant: TOKAI PHARMACEUTICALS, INC.
    Inventor: David Casebier
  • Publication number: 20110312926
    Abstract: Novel chemical agents are described herein. More specifically, 2-(N-substituted piperazinyl) pregnane and 2-(N-substituted piperazinyl) androstane derivatives exhibiting cytotoxicity on a variety of cancer cell lines are disclosed herein.
    Type: Application
    Filed: November 25, 2009
    Publication date: December 22, 2011
    Applicant: UNIVERSITE LAVAL
    Inventors: Donald Poirier, Jenny Roy, Rene Maltais
  • Patent number: 8080540
    Abstract: Estratrien-triazoles corresponding to formula (I) (shown below) which are useful in therapy, especially for the treatment and/or prevention or inhibition of a steroid hormone dependent disorder, preferably a steroid hormone dependent disease or disorder requiring the inhibition of a 17?-hydroxysteroid dehydrogenase (17?-HSD) such as 17?-HSD type 1, type 2 or type 3 enzyme.
    Type: Grant
    Filed: September 18, 2007
    Date of Patent: December 20, 2011
    Assignee: Abbott Products GmbH
    Inventors: Josef Messinger, Uwe Schoen, Heinrich-Hubert Thole, Bettina Husen, Pasi Koskimies, Lila Kallio nee Pirkkala
  • Publication number: 20110294770
    Abstract: Pharmaceutical drug particles of small particle size are produced by combining a solvent-non-solvent precipitate with an in-situ spray drying process. A pharmaceutical drug is dispersed in a water-miscible solvent, in particular ethanol, and heated in an infeed line under pressure to above the boiling point of the solvent until the drug dissolves. This solution collides as a fine liquid jet with a fine water jet in a gas-permeated microreactor, and the fine mist so arising vaporises rapidly. The organic solvent vaporizes first, then the water. The water may contain surface modifiers.
    Type: Application
    Filed: February 11, 2010
    Publication date: December 1, 2011
    Applicant: MJR PharmJet GmbH
    Inventors: Akif Emre Tuereli, Bernd Penth, Peter Langguth, Bernd Baumstuemmler
  • Patent number: 8067401
    Abstract: Compounds from 14 Kenyan plants, including from the root of Dovyalis abyssinica and Clutia robusta have been characterized and isolated, and their uses are disclosed.
    Type: Grant
    Filed: September 6, 2007
    Date of Patent: November 29, 2011
    Assignee: International Patent Holdings LLC
    Inventors: Paul Kiprono Chepkwony, Maria Medina, Mitchell Medina
  • Publication number: 20110275604
    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: Application
    Filed: April 1, 2011
    Publication date: November 10, 2011
    Applicant: INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE (INSERM)
    Inventors: Marc POIROT, Philippe De Medina, Sandrine Poirot
  • Publication number: 20110262368
    Abstract: The present invention provides compounds of Formula (VII) and 11-keto analogs thereof, and pharmaceutically acceptable salts, solvates, esters, prodrugs, tautomers, and isomers of said compounds and said 11-keto analogs, having the general structure formula (VII): wherein L, R1, R2, R3, R4, and R5 are selected independently of each other and as defined herein. Also provided are pharmaceutical compositions, methods of preparing, and methods of using such compounds in the treatment and prophylaxis of a wide range of immune, autoimmune, and inflammatory diseases and conditions. The novel compounds of the present invention possess useful pharmacological activity while having unexpectedly low systemic activity. Thus, the compounds of the invention represent a safer alternative to those known glucocorticoids which have poor side-effect profiles.
    Type: Application
    Filed: December 18, 2008
    Publication date: October 27, 2011
    Applicant: Schering Corporation
    Inventors: John C. Anthes, Kevin D. McCormick, John A. Hey, Robert G. Aslanian, Purakkattle J. Biju, Michael Y. Berlin, Daniel M. Solomon, Philippa H. Solomon, Hongwu Yang, Yeon-Hee Lim, Yoon Joo Lee, Rema Danielle Bitar