Patents Issued in April 1, 2004
  • Publication number: 20040063740
    Abstract: (20) esters of camptothecin analogs are provided. The compounds are (20) esters of an aminoalkanoic acid or an imidoalkanoic acid and homocamptothecin, which is optionally substituted at the 7, 9, 10, 11, and 12 positions of the homocamptothecin ring. The compounds are useful for treating cancer.
    Type: Application
    Filed: June 3, 2003
    Publication date: April 1, 2004
    Inventor: Li-Xi Yang
  • Publication number: 20040063741
    Abstract: The present invention relates to the preparation of the optical isomer (R)-(+)-8,9-dihydroxy-2,3,7,11b-tetrahydro-1H-napth[1,2,3-de]isoquinoline. This invention also relates to the use of pharmaceutical compositions comprising (R)-(+)-8,9-dihydroxy-2,3,7,11b-tetrahydro-1H-napth[1,2,3-de]isoquinoline for use for the treatment of movement disorders.
    Type: Application
    Filed: April 2, 2003
    Publication date: April 1, 2004
    Inventor: Sing-Yuen Sit
  • Publication number: 20040063742
    Abstract: This invention relates to the use of the combined action of a compound with neurotrophic activity and a compound enhancing the dopamine activity for the treatment of Parkinson's disease.
    Type: Application
    Filed: October 23, 2003
    Publication date: April 1, 2004
    Inventors: Dan Peters, Lars Christian Ronn, Gunnar M. Olsen, Arne Moller
  • Publication number: 20040063743
    Abstract: The invention relates to a process for the synthesis of 1H-imidazo[4,5-c] quinoline 4-cyano and 1H-imidazo[4,5-c] quinoline 4-carboxamide intermediates useful in preparing 1H-imidazo[4,5-C] quinoline 4-amines, a process for preparing 1H-imidazo[4,5-C] quinoline 4-amines using such intermediates; and, to the 1H-imidazo[4,5-c] quinoline 4-cyano and 1H-imidazo[4,5-c] quinoline 4-carboxamide intermediates. More particularly, the invention relates to a process for the preparation of 1-isobutyl-1H-imidazo[4,5-C] quinoline 4-amine (Imiquimod) using two intermediates, 1-isobutyl-1H-imidazo[4,5-c] quinoline 4-cyano and 1-isobutyl-1H-imidazo[4,5-c] quinoline 4-carboxamide, and to the said intermediates.
    Type: Application
    Filed: July 28, 2003
    Publication date: April 1, 2004
    Inventors: Valeriano Merli, Silvia Mantovani, Bianchi Stefano
  • Publication number: 20040063744
    Abstract: This invention provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with new piperidine 4-alkenyl derivatives that possess unique antiviral activity. More particularly, the present invention relates to compounds useful for the treatment of HIV and AIDS.
    Type: Application
    Filed: April 29, 2003
    Publication date: April 1, 2004
    Inventors: Tao Wang, John F. Kadow, Nicholas A. Meanwell, Kap-Sun Yeung, Zhongxing Zhang, Zhiwei Yin, Zhilei Qiu, Daniel H. Deon, Clint A. James, Edward H. Ruediger, Carol Bachand
  • Publication number: 20040063745
    Abstract: Therapeutically active thiazole derivatives of formula (I) wherein R1, R2, X and X′ are as defined in the specification, processes for the preparation thereof, the use thereof in therapy, particularly in the treatment or prophylaxis of disorders characterized by overexpression of transforming growth factor &bgr;(TAG-&bgr;), and pharmaceutical compositions for use in such therapy.
    Type: Application
    Filed: July 31, 2003
    Publication date: April 1, 2004
    Inventors: Francoise Jeanne Gellibert, Charles David Hartley, Neil Mathews, James Michael Woolven
  • Publication number: 20040063746
    Abstract: This invention provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with ureido and thioureido piperazine derivatives of Formula I. These compounds possess unique antiviral activity, whether used alone or in combination with other antivirals, antiinfectives, immunomodulators or HIV entry inhibitors. More particularly, the present invention relates to the treatment of HIV and AIDS.
    Type: Application
    Filed: July 18, 2003
    Publication date: April 1, 2004
    Inventors: Alicia Regueiro-Ren, Qiufen May Xue, John F. Kadow, Malcolm Taylor
  • Publication number: 20040063747
    Abstract: Methods of reversing local anesthesia are disclosed. The methods comprise administering a local anesthetic and alpha adrenergic receptor agonist to induce local anesthesia followed by reversing anesthesia with a low dose of an alpha adrenergic receptor antagonist. Also disclosed are kits comprising a local anesthetic, an alpha adrenergic receptor agonist and a low dose of an alpha adrenergic receptor antagonist.
    Type: Application
    Filed: September 24, 2003
    Publication date: April 1, 2004
    Inventors: Eckard Weber, Howard I. Katz
  • Publication number: 20040063748
    Abstract: There is provided an aminophenoxyacetic acid derivative of the following formula (I): 1
    Type: Application
    Filed: March 24, 2003
    Publication date: April 1, 2004
    Inventors: Hirokazu Annoura, Naohiro Takemoto, Hiroshi Uramoto
  • Publication number: 20040063749
    Abstract: The present invention provides compounds of Formula I or Formula II, or the pharmaceutically acceptable salts or prodrugs thereof, pharmaceutical compositions comprising compounds or Formula I or Formula II, and methods for treating neurological disorders and neurodegenerative diseases, particularly migraine.
    Type: Application
    Filed: June 25, 2003
    Publication date: April 1, 2004
    Inventors: Thomas John Bleisch, Sandra Ann Filla, Paul Leslie Ornstein
  • Publication number: 20040063750
    Abstract: A novel high-density lipoprotein (HDL)-cholesterol level elevating agent containing a compound which has a squalene synthase inhibitory activity.
    Type: Application
    Filed: May 6, 2003
    Publication date: April 1, 2004
    Inventors: Tomoyuki Nishimoto, Ryuichi Tozawa, Masakuni Kori, Yuichiro Amano
  • Publication number: 20040063751
    Abstract: A method of treating, preventing, or inhibiting ALS, in a subject in need of such treatment, inhibition or prevention. The method comprises administering to a subject one or more cyclooxygenase-2 selective inhibitor(s) or isomer(s) or pharmaceutically acceptable salt(s), ester(s), or prodrug(s) thereof, in combination with one or more second drugs, wherein the amount of the cyclooxygenase-2 selective inhibitor(s) or isomer(s) or pharmaceutically acceptable salt(s), ester(s), or prodrug(s) thereof in combination with the amount of second drug(s) constitutes an ALS treatment, inhibition or prevention effective amount.
    Type: Application
    Filed: May 23, 2003
    Publication date: April 1, 2004
    Applicant: Pharmacia Corporation
    Inventor: Peter C. Isakson
  • Publication number: 20040063752
    Abstract: A method of treating, preventing, or inhibiting ALS, in a subject in need of such treatment, inhibition or prevention. The method comprises administering to a subject one or more cyclooxygenase-2 selective inhibitor(s), or isomer(s), or pharmaceutically acceptable salt(s), ester(s), or prodrug(s) thereof, wherein the amount of the cyclooxygenase-2 selective inhibitor(s), isomer(s), ester(s), salt(s) or prodrug(s) thereof constitutes an ALS treatment, inhibition or prevention effective amount of the COX 2 inhibitor(s).
    Type: Application
    Filed: May 23, 2003
    Publication date: April 1, 2004
    Applicant: Pharmacia Corporation
    Inventor: Peter C. Isakson
  • Publication number: 20040063753
    Abstract: Compounds of formula (I): are inhibitors of the enzyme Lp-PLA2 and are of use in therapy, in particular for treating atherosclerosis.
    Type: Application
    Filed: September 9, 2003
    Publication date: April 1, 2004
    Inventors: Deirdre Mary Bernadette Hickey, Robert John Ife, Colin Andrew Leach, John Liddle, Ivan Leo Pinto, Stephen Allan Smith, Steven James Stanway
  • Publication number: 20040063754
    Abstract: 3-(1-Aminocycloalkyl)pyrrolidinyl-substituted-6-dehalodeno(hydrogen-substituted)quinolon carboxylic acid derivatives having specific substitunets as represented by the following formula (I), its salts, and hydrates thereof exhibit a broad and potent antibacterial activity on gram-negative and gram-positive bacteria, in particular, resistant bacteria typified by gram-positive cocci, including MRSA, PRSP and VRE. Thus these compounds are usable as drugs.
    Type: Application
    Filed: May 19, 2003
    Publication date: April 1, 2004
    Inventors: Hisashi Takahashi, Rie Miyauchi, Masao Itoh, Makoto Takemura, Isao Hayakawa
  • Publication number: 20040063755
    Abstract: The invention provides novel &bgr;2 adrenergic receptor agonist compounds of formula (I): 1
    Type: Application
    Filed: August 18, 2003
    Publication date: April 1, 2004
    Inventors: Edmund J. Moran, John R. Jacobsen, Michael R. Leadbetter, Matthew B. Nodwell, Sean G. Trapp, James Aggen, Timothy J. Church
  • Publication number: 20040063756
    Abstract: The present invention is related to compounds of formula (I), 1
    Type: Application
    Filed: June 12, 2003
    Publication date: April 1, 2004
    Inventors: Christine A. Collins, Ju Gao, Philip R. Kym, Jared C. Lewis, Andrew J. Souers, Anil Vasudevan, Dariusz Wodka
  • Publication number: 20040063757
    Abstract: The present invention relates to quinolines, pharmaceutical compositions containing them and their use as antagonists of urotensin II.
    Type: Application
    Filed: July 25, 2003
    Publication date: April 1, 2004
    Inventors: Dashyant Dhanak, Steven D. Knight, Gregory L. Warren
  • Publication number: 20040063758
    Abstract: The present invention provides methods of synthesizing and screening inhibitors of bacterial NAD synthetase enzyme, compounds thereof, and methods of treating bacterial and microbial infections with inhibitors of bacterial NAD synthetase enzyme.
    Type: Application
    Filed: October 25, 2002
    Publication date: April 1, 2004
    Inventors: Wayne J. Brouillette, Donald Muccio, Mark J. Jedrzejas, Christie G. Brouillette, Yancho Devedjiev, Walter Cristofoli, Lawrence J. DeLucas, Jose Gabriel Garcia, Laurent Schmitt, Sadanandan E. Velu
  • Publication number: 20040063759
    Abstract: A compound of the formula 1
    Type: Application
    Filed: July 8, 2003
    Publication date: April 1, 2004
    Applicant: Pfizer Inc.
    Inventors: Laura C. Blumberg, Matthew F. Brown, Matthew M. Hayward, Christopher S. Poss
  • Publication number: 20040063760
    Abstract: The invention provides sodium channel modulating compounds which are useful for treating diseases or conditions associated with sodium channel activity, such as neuropathic pain. The invention also provides pharmaceutical compositions comprising a compound of the present invention, as well as therapeutic methods comprising administering such a compound or salt to a mammal (e.g. a human).
    Type: Application
    Filed: September 11, 2003
    Publication date: April 1, 2004
    Inventors: Seok-Ki Choi, Paul R. Fatheree, David C. Green, Daniel Marquess
  • Publication number: 20040063761
    Abstract: Compounds disclosed herein are bradykinin B1 antagonist compounds useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway.
    Type: Application
    Filed: August 5, 2003
    Publication date: April 1, 2004
    Inventors: Scott D. Kuduk, Mark G. Bock, Dong-Mei Feng, Jenny Miu-Chun Wai
  • Publication number: 20040063762
    Abstract: Compounds are provided which are useful as antidiabetic agents and antiobesity agents and have the structure 1
    Type: Application
    Filed: July 8, 2003
    Publication date: April 1, 2004
    Inventors: Peter T. W. Cheng, Sean Chen, Charles Z. Ding, Timothy F. Herpin
  • Publication number: 20040063763
    Abstract: The present invention provides 2-methoxyimino-2-(pynrdinyloxymetilyl,) phenyl acetamides according to formula (I) as well as their use as fungicidal compounds.
    Type: Application
    Filed: February 27, 2003
    Publication date: April 1, 2004
    Inventors: Neil Vincent Kirby, Jenifer Lynn Adamski Butz, Brent Jeffrey Rieder, James M Renga, Jeannie Rachel Phillips Cetusic, Irene Mae Morrison, John Todd Mathieson, Gary David Gustafson
  • Publication number: 20040063764
    Abstract: Compounds of the general formula (III), prodrugs thereof, pharmaceutically acceptable salts of both, or solvates of them and exhibiting thrombopoietin receptor agonism: 1
    Type: Application
    Filed: July 25, 2003
    Publication date: April 1, 2004
    Inventors: Hiroshi Takemoto, Masami Takayama, Takeshi Shiota
  • Publication number: 20040063765
    Abstract: The present invention relates to the use of compounds of the general Formula (I): 1
    Type: Application
    Filed: May 6, 2003
    Publication date: April 1, 2004
    Applicant: 4 SC AG
    Inventors: Aldo Ammendola, Katharina Aulinger-Fuchs, Astrid Gotschlich, Bernd Kramer, Martin Lang, Wael Saeb, Udo Sinks, Andreas Wuzik
  • Publication number: 20040063766
    Abstract: The invention relates to the use of aminoacetonitrile compounds of formula 1
    Type: Application
    Filed: October 2, 2003
    Publication date: April 1, 2004
    Inventors: Pierre Ducray, Jacques Bouvier
  • Publication number: 20040063767
    Abstract: The present invention relates to new, efficient processes for the preparation of 5-(-2-oxyazolylalkylthio)-2-azacycloalkanoylaminothiazole compounds of formula I 1
    Type: Application
    Filed: August 12, 2003
    Publication date: April 1, 2004
    Inventors: Bang-Chi Chen, Kyoung S. Kim, S. David Kimball, Raj N. Misra, Mark E. Salvati, Joseph E. Sundeen, Hai-Yun Xia, Rulin Zhao
  • Publication number: 20040063768
    Abstract: The present invention relates to compounds of Formula (I) and pharmaceutically acceptable salts or solvates thereof and pharmaceutically acceptable formulations comprising said compounds 1
    Type: Application
    Filed: September 15, 2003
    Publication date: April 1, 2004
    Inventors: Derek John Denhart, Jonathan L. Ditta, Dalton King, John E. Macor, Lawrence R. Marcin, Ronald J. Mattson, Zhaoxing Meng
  • Publication number: 20040063769
    Abstract: The invention features a method for treating a patient having a cancer or other neoplasm, by administering to the patient (i) a benzimidazole or a metabolite or analog thereof; and (ii) pentamidine or a metabolite or analog thereof simultaneously or within 14 days of each other in amounts sufficient to inhibit the growth of the neoplasm.
    Type: Application
    Filed: October 2, 2003
    Publication date: April 1, 2004
    Inventors: Alexis Borisy, Curtis Keith, Michael A. Foley, Brent R. Stockwell
  • Publication number: 20040063770
    Abstract: The present invention provides methods and compositions for inhibiting A&bgr; synthesis and for treating Alzheimer's disease by administering a farnesyl transferase inhibitor of the formula: 1
    Type: Application
    Filed: September 26, 2003
    Publication date: April 1, 2004
    Applicant: Warner-Lambert Company
    Inventors: Kyunghye Ahn, Mark Richard Emmerling, Taraneh Haske, Donald J. Hupe, Judith Sebot-Leopold, Harry LeVine, Jeffrey David Scholten
  • Publication number: 20040063771
    Abstract: Bis-sulfonamido hydroxyethylamino compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Application
    Filed: April 17, 2003
    Publication date: April 1, 2004
    Applicant: G.D. Searle & Co.
    Inventors: John N. Freskos, Daniel P. Getman, John J. Talley, James A. Sikorski
  • Publication number: 20040063772
    Abstract: The present application describes intermediates for nitrogen containing heteroaromatics and derivatives thereof of formula I: 1
    Type: Application
    Filed: June 24, 2003
    Publication date: April 1, 2004
    Inventors: Mimi L. Quan, Renhua Li
  • Publication number: 20040063773
    Abstract: The present invention relates to pyrrole substituted 2-indolinone compounds and their pharmaceutically acceptable salts which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related cellular disorders such as cancer.
    Type: Application
    Filed: April 14, 2003
    Publication date: April 1, 2004
    Applicant: SUGEN, Inc. & Pharmacia & Upjohn Co.
    Inventors: Peng Cho Tang, Todd A. Miller, Xiaoyuan Li, Li Sun, Chung Chen Wei, Shahrzad Shirazian, Congxin Liang, Thomas Vojkovsky, Asaad S. Nematalla, Michael Hawley
  • Publication number: 20040063774
    Abstract: Pyrrolylquinones and indolylquinones useful for treating diseases such as neurodegenerative disease, viral infections and proliferative disease are described, along with methods of making such compounds and pharmaceutical formulations containing such compounds.
    Type: Application
    Filed: September 26, 2002
    Publication date: April 1, 2004
    Inventors: Michael C. Pirrung, Johannes Rudolph
  • Publication number: 20040063775
    Abstract: The present invention relates to a compound represented by the formula 1
    Type: Application
    Filed: September 22, 2003
    Publication date: April 1, 2004
    Inventors: Yu Momose, Tsuyoshi Maekawa, Hiroshi Imoto, Hiroyuki Odaka, Hiroyuki Kimura
  • Publication number: 20040063776
    Abstract: A medicament for therapeutic and/or prophylactic treatment of neuropathic pain, which comprises a compound represented by the general formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient: 1
    Type: Application
    Filed: October 20, 2003
    Publication date: April 1, 2004
    Inventors: Hiroshi Ueda, Munehiro Tomikawa
  • Publication number: 20040063777
    Abstract: The invention relates to compounds of Formula (I), to processes for their preparation and pharmaceutical compositions thereof, that inhibit the Ras farnesyl-protein transferase enzyme (FPTase), and may be used as an alternative to, or in conjunction with, traditional cancer therapy for the treatment of ras oncogene-dependent tumors, such as cancers of the pancreas, colon, bladder, and thyroid.
    Type: Application
    Filed: September 26, 2003
    Publication date: April 1, 2004
    Applicant: Wyeth Holdings Corporation
    Inventors: Joseph William Epstein, Semiramis Ayral-Kaloustian
  • Publication number: 20040063778
    Abstract: The present invention provides compounds having improved stability over that of natural benzolactones, and a process for synthesizing these compounds. These compounds exhibit anti-cancer activity and inhibit V-ATPase activity.
    Type: Application
    Filed: April 18, 2003
    Publication date: April 1, 2004
    Inventors: Jef Karel De Brabander, Yusheng Wu
  • Publication number: 20040063779
    Abstract: The invention relates to the use of 1-phenyl-1,2-diaminoethane derivatives of formula (I) 1
    Type: Application
    Filed: July 7, 2003
    Publication date: April 1, 2004
    Applicant: Boehringer Ingelheim Pharma GmbH & Co. KG
    Inventors: Horst Dollinger, Franz Birke, Pascale Arielle Jane-Josee Pouzet, Enzo Cereda, Monica Quai
  • Publication number: 20040063780
    Abstract: Pharmaceutical preparations for type II diabetes comprising as active ingredients thereof biguanide derivatives represented by the following general formula (1): 1
    Type: Application
    Filed: October 31, 2002
    Publication date: April 1, 2004
    Applicant: CHUGAI SEIYAKU KABUSHIKI KAISHA
    Inventors: Hiroharu Matsuoka, Naoki Taka, Hirotaka Kashiwagi, Kazuharu Ozawa
  • Publication number: 20040063781
    Abstract: 1
    Type: Application
    Filed: October 14, 2003
    Publication date: April 1, 2004
    Inventors: Benjamin Pelcman, Annika Gustafsson, Philip R Kym
  • Publication number: 20040063782
    Abstract: A new crystalline form of bicalutamide (form II) is disclosed. Bicalutamide form II is useful as a pharmaceutical and has antiandrogenic activity.
    Type: Application
    Filed: September 12, 2003
    Publication date: April 1, 2004
    Inventor: Raymond J.H. Westheim
  • Publication number: 20040063783
    Abstract: The present invention relates to a compound of formula (I) in which X, A, T, Y, G and R are as defined in Claim (1).
    Type: Application
    Filed: April 3, 2003
    Publication date: April 1, 2004
    Inventors: Claude Lardy, Jean-Yves Nioche, Lidia Caputo, Jacques Decerprit, Jean-Yves Ortholand, Didier Festal, Daniel Guerrier
  • Publication number: 20040063784
    Abstract: The present invention is directed to methods of treating, preventing, and/or managing abnormal increases in gastrointestinal motility, and intestinal conditions that cause the same. Such conditions include, but are not limited to, irritable bowel syndrome (IBS), infectious diseases of the small and large intestines, and symptoms of any of the foregoing. In particular, the present invention discloses methods of using enriched (R)-verapamil, as well as compositions and formulations containing the same.
    Type: Application
    Filed: November 15, 2002
    Publication date: April 1, 2004
    Inventors: John Kelly, John Devane
  • Publication number: 20040063785
    Abstract: Symmetrically disubstituted aromatic compounds and pharmaceutical compositions containing such compounds that inhibit and/or modulate the activity of poly(ADP-ribose) glycohydrolase, also known as PARG, are described. The invention is also directed to the therapeutic or prophylactic use of such compounds and compositions, and to methods of treating diseases and disorders described herein, by administering effective amounts of such compounds.
    Type: Application
    Filed: August 28, 2003
    Publication date: April 1, 2004
    Applicant: Guilford Pharmaceuticals, Inc.
    Inventors: Jia-He Li, Dana Victor Ferraris, Paul W. Kletzly, Weixing Li, Eric Yanjun Wang, Amy D. Xing, Weizheng Xu, Jie Zhang
  • Publication number: 20040063786
    Abstract: The present invention is related to new vanilloid analogues containing resiniferatoxin pharmacophores, pharmaceutical compositions that have such analogues, and their uses as vanilloid receptor agonists and potent analgesics. The present invention provides a pharmaceutical composition for preventing, alleviating or treating pain, acute pain, chronic pain, neuropathic pain, post-operative pain, migraine, arthralgia, neutopathies, nerve injury, diabetic neuropathy, neurodegeneration, neurotic skin disorder, stroke, urinary bladder hypersensitiveness, irritable bowel syndrome, a respiratory disorder such as asthma or chronic obstructive pulmonary disease, irritation of skin, eye or mucous membrane, fervescence, stomach-duodenal ulcer, inflammatory bowel disease, inflammatory disease or urgent urinary incontinence.
    Type: Application
    Filed: December 18, 2002
    Publication date: April 1, 2004
    Inventor: Jee Woo Lee
  • Publication number: 20040063787
    Abstract: The invention provides compositions and methods for increasing the secretion of mucus within the reproductive tract of a female mammal.
    Type: Application
    Filed: September 19, 2002
    Publication date: April 1, 2004
    Inventor: Julie M. Villanueva
  • Publication number: 20040063788
    Abstract: The present invention relates to a novel use of abietic acid or derivatives thereof for inhibiting the growth of a cancer cell or treating a cancer, preferably, reducing the tumor size of the cancer.
    Type: Application
    Filed: September 26, 2003
    Publication date: April 1, 2004
    Applicant: Royal Dynesty Tech. Co., Ltd.
    Inventors: Chi-Hung Lin, Hsin-Shiu Chuang
  • Publication number: 20040063789
    Abstract: The instant invention is a series of novel mono- and disubstituted 3-propyl gamma aminobutyric acids of Formula I 1
    Type: Application
    Filed: September 29, 2003
    Publication date: April 1, 2004
    Inventors: Thomas Richard Belliotti, Justin Stephen Bryans, Ihoezo Victor Ekhato, Augustine Tobi Osuma, Robert Michael Schelkun, Jacob Bradley Schwarz, Andrew John Thorpe, Lawrence David Wise, David Juergen Wustrow, Po-Wai Yuen