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.
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.
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
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.
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
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
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
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.
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
Abstract: A novel high-density lipoprotein (HDL)-cholesterol level elevating agent containing a compound which has a squalene synthase inhibitory activity.
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.
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).
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.
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
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
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
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
Abstract: Compounds of the general formula (III), prodrugs thereof, pharmaceutically acceptable salts of both, or solvates of them and exhibiting thrombopoietin receptor agonism: 1
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
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
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
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
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
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
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.
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
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
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.
Abstract: Pharmaceutical preparations for type II diabetes comprising as active ingredients thereof biguanide derivatives represented by the following general formula (1): 1
Abstract: A new crystalline form of bicalutamide (form II) is disclosed. Bicalutamide form II is useful as a pharmaceutical and has antiandrogenic activity.
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.
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
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.
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.
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