Additional Hetero Ring Attached Directly Or Indirectly By Nonionic Bonding To The Seven-membered Hetero Ring Patents (Class 514/212.08)
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Patent number: 6579867Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.Type: GrantFiled: July 27, 2001Date of Patent: June 17, 2003Assignees: Athena Neurosciences, Inc., Eli Lilly & CompanyInventors: Jing Wu, Jay S. Tung, Eugene D. Thorsett, Michael A. Pleiss, Jeffrey S. Nissen, Jeffrey Neitz, Lee H. Latimer, Varghese John, Stephen Freedman, Thomas C. Britton, James A. Audia, Jon K. Reel, Thomas E. Mabry, Bruce A. Dressman, James J. Droste, Steven S. Henry, Stacey L. McDaniel, Russell D. Stucky, Warren J. Porter
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Publication number: 20030109517Abstract: The present invention is directed to non-peptidic factor Xa inhibitors which are useful for the treatment of arterial and venous thrombotic occlusive disorders, inflammation, cancer, and neurodegenerative diseases.Type: ApplicationFiled: September 16, 2002Publication date: June 12, 2003Applicant: 3-Dimensional Pharmaceuticals, Inc.Inventors: Scott C. Miller, Juan Jose Marugan Sanchez, Kristin D. Haslow, Jonathan Hall
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Patent number: 6573293Abstract: 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: GrantFiled: February 15, 2001Date of Patent: June 3, 2003Assignees: Sugen, Inc., Pharmacia & Upjohn Co.Inventors: Peng Cho Tang, Todd A. Miller, Xiaoyuan Li, Li Sun, Chung Chen Wei, Shahrzad Shirazian, Congxin Liang, Tomas Vojkovsky, Asaad S. Nematalla, Michael Hawley
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Patent number: 6566358Abstract: This invention provides compounds of Formula (I): wherein R1 and R2 may be single substituents or fused to form spirocyclic or hetero-spirocyclic rings; R3 is H, OH, NH2, C1 to C6 alkyl, substituted C1 to C6 alkyl, C3 to C6 alkenyl, substituted C1 to C6 alkenyl, alkynyl, or substituted alkynyl, CORC; RC is H, C1 to C3 alkyl, substituted C1 to C3 alkyl, aryl, substituted aryl, C1 to C3 alkoxy, substituted C1 to C3 alkoxy, C1 to C3 aminoalkyl, or substituted C1 to C3 aminoalkyl; R4 is H, halogen, CN, NO2, C1 to C6 alkyl, substituted C1 to C6 alkyl, alkynyl, or substituted alkynyl, C1 to C6 alkoxy, substituted C1 to C6 alkoxy, amino, C1 to C6 aminoalkyl, or substituted C1 to C6 aminoalkyl; and R5 is selected from a trisubstituted benzene ring of a five or six membered ring with 1, 2, or 3 heteroatoms from the group including O, S, SO, SO2 or NR6 and containing one or two independent substituents from the group including H, halogen, CN, NO2, amino, and C1 to C3 alky, C1 to C3 alkoxy, C1 to C3 aType: GrantFiled: September 6, 2001Date of Patent: May 20, 2003Assignees: Wyeth, Ligand Pharmaceuticals, Inc.Inventors: Puwen Zhang, Eugene A. Terefenko, Andrew Fensome, Jay E. Wrobel, Horace Fletcher, III, Lin Zhi, Todd K. Jones, James P. Edwards, Christopher M. Tegley
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Patent number: 6559141Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.Type: GrantFiled: July 27, 2001Date of Patent: May 6, 2003Assignees: Athena Neurosciences, Inc., Eli Lilly & CompanyInventors: Jing Wu, Jay S. Tung, Eugene D. Thorsett, Michael A. Pleiss, Jeffrey S. Nissen, R. Jeffrey Neitz, Lee H. Latimer, Varghese John, Stephen Freedman, Thomas C. Britton, James A. Audia, Jon K. Reel, Thomas E. Mabry, Bruce A. Dressman, Cynthia L. Cwi, James J. Droste, Steven S. Henry, Stacey L. McDaniel, William Leonard Scott, Russell D. Stucky, Warren J. Porter
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Patent number: 6555533Abstract: The present invention relates to certain substituted caprolactam compounds, pharmaceutical compositions containing said compounds, the use of said compounds in treating tumors and to a process for making said compounds.Type: GrantFiled: March 12, 2001Date of Patent: April 29, 2003Assignee: Novartis AGInventors: Frederick Ray Kinder, Jr., Kenneth Walter Bair, Christopher Turchik Jagoe, Richard William Versace, Sompong Wattanasin
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Publication number: 20030078253Abstract: The present invention provides a compound represented by Formula: 1Type: ApplicationFiled: June 3, 2002Publication date: April 24, 2003Inventors: Toshiro Yamashita, Hiroshi Nara, Masayuki Takizawa, Koji Yoshimura
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Publication number: 20030069204Abstract: The present invention relates to ester, ether and N-alkylcarbamoyl derivatives of compound (Ia) and pharmaceutically acceptable salts thereof. These compounds exhibit excellent antibacterial activity and are useful for the treatment or prevention of bacterial infections.Type: ApplicationFiled: March 12, 2002Publication date: April 10, 2003Applicant: SANKYO COMPANY LIMITEDInventors: Masatoshi Inukai, Masakatsu Kaneko, Toshio Takatsu, Hitoshi Hotoda, Masatoshi Arai, Shunichi Miyakoshi, Masaaki Kizuka, Yasumasa Ogawa
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Patent number: 6544978Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.Type: GrantFiled: July 27, 2001Date of Patent: April 8, 2003Assignees: Athena Neurosciences, Inc., Eli Lilly & CompanyInventors: Jing Wu, Jay S. Tung, Eugene D. Thorsett, Michael A. Pleiss, Jeffrey S. Nissen, R. Jeffrey Neitz, Lee H. Latimer, Varghese John, Stephen Freedman, Thomas C. Britton, James A. Audia, Jon K. Reel, Thomas E. Mabry, Bruce A. Dressman, Cynthia L. Cwi, James J. Droste, Steven S. Henry, Stacey L. McDaniel, William Leonard Scott, Russell D. Stucky, Warren J. Porter
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Patent number: 6544981Abstract: Lactam inhibitors are provided which have the structure including pharmaceutically acceptable salts thereof and all stereoisomers thereof, and prodrug esters thereof, wherein n is 1 to 5; and and R1, R2, R3, R4, R5 , R6, R7, R8, R9, R10, R10a, R11 and R12 are as defined herein. These compounds are inhibitors of Factor Xa and thus are useful as anticoagulants. A method for treating cardiovascular diseases associated with thromboses is also provided.Type: GrantFiled: June 5, 2001Date of Patent: April 8, 2003Assignee: Bristol-Myers Squibb CompanyInventors: Philip D. Stein, Stephen P. O'Connor, Yan Shi, Chi Li
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Patent number: 6541467Abstract: The present invention provides compounds having a lactam ring at P3 and at P1 have a six-membered heterocyclic ring having two ring nitrogen ring atoms and the remainder of the ring atoms carbon atoms. These compounds have biological activity as active and potent inhibitors of thrombin. Their pharmaceutically acceptable salts, pharmaceutical compositions thereof and methods of using these compounds and pharmaceutical compositions comprising these compounds as therapeutic agents for treatment of disease states in mammals which are characterized by abnormal thrombosis are also described.Type: GrantFiled: April 14, 2000Date of Patent: April 1, 2003Assignee: Corvas International, Inc.Inventors: Jonathan Zhanqi Ho, Joseph Edward Semple
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Patent number: 6541466Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.Type: GrantFiled: July 27, 2001Date of Patent: April 1, 2003Assignees: Athena Neurosciences, Inc., Eli Lilly & CompanyInventors: Jing Wu, Jay S. Tung, Eugene D. Thorsett, Michael A. Pleiss, Jeffrey S. Nissen, R. Jeffrey Neitz, Lee H. Latimer, Varghese John, Stephen Freedman, Thomas C. Britton, James A. Audia, Jon K. Reel, Thomas E. Mabry, Bruce A. Dressman, Cynthia L. Cwi, James J. Droste, Steven S. Henry, Stacey L. McDaniel, William Leonard Scott, Russell D. Stucky, Warren J. Porter
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Publication number: 20030055041Abstract: The present invention relates to certain substituted caprolactam carbonate and ether compounds, pharmaceutical compositions containing said compounds, the use of said compounds in treating tumors and to a process for making said compounds.Type: ApplicationFiled: May 17, 2002Publication date: March 20, 2003Inventors: Frederick Ray Kinder, Richard William Versace, Kenneth Walter Bair
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Publication number: 20030055037Abstract: Benzimidazole and indole derivatives that act as selective modulators of CRF 1 receptors are provided. These compounds are useful in the treatment of a number of CNS and periphereal disorders, particularly stress, anxiety, depression, cardiovascular disorders, and eating disorders. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also provided.Type: ApplicationFiled: October 5, 2001Publication date: March 20, 2003Inventors: Stephane DeLombaert, Ping Ge, Raymond F. Horvath, Taeyoung Yoon
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Patent number: 6534495Abstract: The invention relates to a compound having the formula (I): R1SO2—B—X—Z—C(O)—Y, B is a bond, an amino acid of the formula —NR—CH[(CH2)pC(O)OH]—C(O)— or an ester derivative thereof wherein p is 1, 2, or 3, Gly, D-1-Piq, D-3-Piq, D-1-Tiq, D-3-Tiq, D-Atc, Aic, or a L- or D-amino acid having a hydrophobic, basic or neutral side chain; X is an amino acid with a hydrophobic side chain, glutamine, serine, theronine, a cyclic amino acid optionally containing an additional heteroatom selected from N, O or S, and optionally substituted with (1-6C)alkyl, (1-6C)alkoxy, benzyloxy or oxo, or X is 2-amino-isobutyric acid, —NR2—CH2—C(O)— or the fragment (I) or (II), wherein n is 2, 3, or 4, W is CH or N and R3 is H, (1-6C)alkyl or phenyl which groups may optionally be substituted with hydroxy, (1-6C)alkoxy, COOH, COO(1-6C)alkyl, CONH2, or halogen; Z is lysine or 4-aminocyclohexylglycine.Type: GrantFiled: October 26, 1999Date of Patent: March 18, 2003Assignee: Akzo NebelInventor: Anton Egbert Peter Adang
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Patent number: 6511973Abstract: Compound of the formula are inhibitors of the enzyme Factor Xa. These compounds are useful as anticoagulants in the treatment of cardiovascular diseases associated with thromboses.Type: GrantFiled: July 27, 2001Date of Patent: January 28, 2003Assignee: Bristol-Myers Squibb Co.Inventors: Philip D. Stein, Yan Shi, Stephen P. O'Connor, Chi Li
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Patent number: 6509330Abstract: Hydroxamic acids are provided which are ACE and/or NEP inhibitors and have the structure wherein R*, R and R1 are as defined herein and A is a dipeptide preferably derived from an amino acid, or is a conformationally restricted dipeptide mimic.Type: GrantFiled: February 9, 2001Date of Patent: January 21, 2003Assignee: Bristol-Myers Squibb CompanyInventor: Jeffrey A. Robl
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Patent number: 6500818Abstract: Compounds having the following formula wherein L, M, R2, R3, R4, R5, R6, R7, X1 and X2 are as defined in the specification, pharmaceutically-acceptable salt thereof, useful for treating depression, anxiety, asthma, rheumatoid arthritis, Alzheimer's disease, cancer, schizophrenia, oedema, allergic rhinitis, inflammation, pain, gastrointestinal-hypermotility, emesis, Huntington's disease, psychoses, hypertension, migraine, bladder hypermotility, or urticaria, compositions including such compounds and processes for making such compounds.Type: GrantFiled: March 30, 2001Date of Patent: December 31, 2002Assignee: Astrazeneca ABInventors: Peter Robert Bernstein, Robert Frank Dedinas, Cyrus John Ohnmacht, Keith Russell
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Patent number: 6497886Abstract: The present invention relates to a 1,3-bis-(N-lactamyl)propane of general formula (I), wherein radicals R1, R2, R3, R4, R5 and R6 independently stand for hydrogen, alkyl, cycloalkyl, aryl or aralkyl and at least one of said radicals does not stand for hydrogen, (NLac) and (NLac′) are the same or different and stand for N-lactamyl radicals. The invention also relates to the use of said substances as a solvent in pharmaceutical and cosmetic agents. Disclosed are novel compounds of formula (I), wherein R1 and methyl and R2-R6 stand for hydrogen.Type: GrantFiled: April 1, 1999Date of Patent: December 24, 2002Assignee: BASF AktiengesellschaftInventors: Jörg Breitenbach, Siegfried Lang, Detlef Kratz
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Patent number: 6495540Abstract: This invention relates to novel lactams having the Formula (I): to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of A&bgr;-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to &bgr;-amyloid production such as Alzheimer's disease and Down's Syndrome.Type: GrantFiled: March 27, 2001Date of Patent: December 17, 2002Assignee: Bristol - Myers Squibb Pharma CompanyInventor: Lorin A. Thompson
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Publication number: 20020187193Abstract: The present invention relates to the use of quinolone carboxylic acid formulations in the treatment of ocular and periocular infections. The present invention also relates to sustained release compositions comprising specific quinolone carboxylic acid compounds. The invention also relates to quinolone carboxylic acid compositions and methods of preparing the same.Type: ApplicationFiled: April 25, 2001Publication date: December 12, 2002Inventors: Samir Roy, Santosh Kumar Chandrasekaran, Katsumi Imamori, Takemitsu Asaoka, Akihiro Shibata, Masami Takahashi, Lyle M. Bowman
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Publication number: 20020182255Abstract: The present invention relates to the use of quinolone carboxylic acid formulations in the treatment of ocular and periocular infections. The present invention also relates to sustained release compositions comprising specific quinolone carboxylic acid compounds. The invention also relates to quinolone carboxylic acid compositions and methods of preparing the same.Type: ApplicationFiled: April 22, 2002Publication date: December 5, 2002Inventors: Samir Roy, Santosh Kumar Chandrasekaran, Katsumi Imamori, Takemitsu Asaoka, Akihiro Shibata, Masami Takahashi, Lyle M. Bowman
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Patent number: 6476016Abstract: Cyclic oxyguanidine pyrazinone compounds are described, including compounds of the Formula I: wherein R3, R4, R5, W, and A are as set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof. The compounds of the invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin. Compositions for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation are described.Type: GrantFiled: July 17, 2001Date of Patent: November 5, 2002Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Aihua Wang, Bruce Edward Tomczuk, Tianbao Lu, Richard M. Soll, John Curtis Spurlino, Roger Francis Bone
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Patent number: 6476019Abstract: One aspect of the present invention relates to spirocyclic compounds. Another aspect of the present invention relates to the use of the spirocyclic compounds as ligands for mammalian G-protein-coupled receptors or sigma receptors. The present invention also relates to methods of modulating the activity of a G-protein-coupled receptor or a sigma receptor in a mammal using the spirocyclic compounds of the present invention. The present invention also relates to methods of treating various diseases in a mammal using the spirocyclic compounds of the present invention.Type: GrantFiled: August 7, 2000Date of Patent: November 5, 2002Assignee: Sepracor Inc.Inventors: Heike Radeke, Paul E. Persons, James R. Hauske
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Publication number: 20020147188Abstract: The present invention provides 4-amino-azepan-3-one protease inhibitors and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, novel intermediates of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia of malignancy; and metabolic bone disease, comprising inhibiting said bone loss or excessive cartilage or matrix degradation by administering to a patient in need thereof a compound of the present invention.Type: ApplicationFiled: February 13, 2002Publication date: October 10, 2002Applicant: SmithKline Beecham CorporationInventors: Robert Wells Marquis, Yu Ru, Daniel Frank Veber, Maxwell David Cummings, Scott Kevin Thompson, Dennis Shinji Yamashita
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Publication number: 20020128474Abstract: The present invention relates to an improved process for preparing certain substituted caprolactam compounds which comprises acylating an aminocaprolactam compound with a lactone compound in the presence of a weak base and a polar, organic solvent, and hydrolyzing the resultant diamide compound in a mixture of solvents to obtain the desired caprolactam compound.Type: ApplicationFiled: March 11, 2002Publication date: September 12, 2002Inventors: David Daqiang Xu, Wenming Liu
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Patent number: 6436943Abstract: The invention relates to dihydropyrimidines of the general formula and to the use of dihydropyrimidines as medicaments for the treatment and prophylaxis of hepatitis B. The invention further relates to a process for the preparation of medicaments comprising the corresponding dihydropyrimidines.Type: GrantFiled: October 18, 2000Date of Patent: August 20, 2002Assignee: Bayer AktiengesellschaftInventors: Jürgen Stoltefuss, Siegfried Goldmann, Arnold Paessens, Erwin Graef, Stefan Lottmann
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Publication number: 20020107239Abstract: The present invention relates to cyclized amide derivatives for treating or preventing neuronal damage associated with neurological diseases. The invention also provides compositions comprising the compounds of the present invention and methods of utilizing those compositions for treating or preventing neuronal damage.Type: ApplicationFiled: January 3, 2002Publication date: August 8, 2002Inventors: David Lauffer, Michael Mullican, Brian Ledford
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Patent number: 6413954Abstract: The present invention relates to certain substituted caprolactam carbonate and ether compounds, pharmaceutical compositions containing said compounds, the use of said compounds in treating tumors and to a process for making said compounds.Type: GrantFiled: May 8, 2001Date of Patent: July 2, 2002Assignee: Novartis AGInventors: Frederick Ray Kinder, Jr., Richard William Versace, Kenneth Walter Bair
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Publication number: 20020061874Abstract: This invention relates to novel lactams having the Formula (I): 1Type: ApplicationFiled: April 3, 2001Publication date: May 23, 2002Inventors: Michael G. Yang, Hong Liu
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Publication number: 20020061875Abstract: This invention provides a method of providing contraception which comprises administering to a female of child bearing age a combination of a non-uterotrophic anti-estrogen and a progestin for 28 days per 28-day menstrual cycle.Type: ApplicationFiled: November 21, 2001Publication date: May 23, 2002Applicant: American Home Products CorporationInventors: Michael J. Gast, Christopher P. Miller
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Patent number: 6384035Abstract: This invention relates a to a series of heterocyclic substituted piperazines of Formula I pharmaceutical compositions containing them and intermediates used in their manufacture. The compounds of the invention selectively inhibit binding to the &agr;-1a adrenergic receptor, a receptor which has been implicated in benign prostatic hyperplasia. As such the compounds are potentially useful in the treatment of this disease.Type: GrantFiled: October 9, 1998Date of Patent: May 7, 2002Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Richard H. Hutchings, Haripada Khatuya, Gee-Hong Kuo, Xiaobing Li, William V. Murray, Catherine Prouty, Frank Villani, Nelson C. F. Yim, Cynthia Maryanoff
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Patent number: 6376485Abstract: Compounds of formula I in which R1, R2, R3 and A have the meaning set forth in the specification, are selective cyclic nucleotide phosphodiesterase (PDE) inhibitors useful as therapeutics in human and veterinary medicine. They are distinguished by low toxicity, good enteral absorption (high bioavailability), a wide therapeutic breadth and absence of significant side effects.Type: GrantFiled: January 3, 2001Date of Patent: April 23, 2002Assignee: Byk Gulden Lomberg Chemische Fabrik GmbHInventor: Thomas Martin
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Publication number: 20020045616Abstract: Compound of the formula 1Type: ApplicationFiled: July 27, 2001Publication date: April 18, 2002Inventors: Philip D. Stein, Yan Shi, Stephen P. O'Connor, Chi Li
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Publication number: 20020042398Abstract: The present application describes novel lactams and derivatives thereof of formula I: 1Type: ApplicationFiled: July 10, 2001Publication date: April 11, 2002Inventors: Thomas P. Maduskuie, Jingwu Duan, Stephen E. Mercer
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Publication number: 20020025957Abstract: Lactam inhibitors are provided which have the structure 1Type: ApplicationFiled: June 5, 2001Publication date: February 28, 2002Inventors: Philip D. Stein, Stephen P. O'Connor, Yan Shi, Chi Li
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Publication number: 20020025955Abstract: This invention relates to novel lactams of Formula (I): 1Type: ApplicationFiled: April 11, 2001Publication date: February 28, 2002Inventors: Qi Han, Hong Liu, Richard E. Olson, Michael G. Yang
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Patent number: 6344450Abstract: Lactam inhibitors are provided which have the structure X is wherein Y is O or S and R4 is R7O— or R8 and R1, R2, R3, R5, R6, R7, and R8, are as defined herein. These compounds are inhibitors of Factor Xa and thus are useful as anticoagulants, and are inhibitors of tryptase and thus are useful in treating asthma. Methods for treating cardiovascular diseases associated with thromboses and for treating asthma and related diseases are also provided.Type: GrantFiled: August 7, 2000Date of Patent: February 5, 2002Assignee: Bristol-Myers Squibb CompanyInventors: Gregory S. Bisacchi, Steven M. Seiler, R. Michael Lawrence, James C. Sutton, Jr., William A. Slusarchyk, Guohua Zhao
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Patent number: 6326379Abstract: Compounds of the formulas are useful as inhibitors of cGMP PDE, especially type V.Type: GrantFiled: September 10, 1999Date of Patent: December 4, 2001Assignee: Bristol-Myers Squibb Co.Inventors: John E. Macor, Guixue Yu
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Publication number: 20010046986Abstract: There is provided a method for controlling flies, that live in or come flying to livestock pens or poultry houses, by using a compound or salt thereof with an affinity for a nicotinic acetylcholine receptor of insects. Since having a very high activity against flies, the compound or salt thereof helps quickly and efficiently to control flies that live in or come flying to livestock pens or poultry houses. Also, since having an excellent control effect on flies that are resistant to conventional chemicals including a organo-phosphoric pesticide and a pyrethroid, the compound or salt thereof helps to prevent propagation, caused by flies, of various diseases to livestock, poultry and humans, and reduce discomfort of workers engaged in the livestock and poultry farming and a community. Still, it is possible with the present invention to keep livestock pens or poultry houses in a hygienic condition, which may greatly contribute to the development of the livestock and poultry farming.Type: ApplicationFiled: April 25, 2001Publication date: November 29, 2001Inventors: Hiroyuki Miura, Atsuo Akayama
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Publication number: 20010044433Abstract: The present invention relates to certain substituted caprolactam compounds, pharmaceutical compositions containing said compounds, the use of said compounds in treating tumors and to a process for making said compounds.Type: ApplicationFiled: March 12, 2001Publication date: November 22, 2001Inventors: Frederick Ray Kinder, Kenneth Walter Bair, Christopher Turchik Jagoe, Richard William Versace, Sompong Wattanasin
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Patent number: 6316438Abstract: Compounds of the formula are useful as inhibitors of cGMP PDE especially Type 5.Type: GrantFiled: March 15, 2000Date of Patent: November 13, 2001Assignee: Bristol-Myers Squibb Co.Inventors: Guixue Yu, John Macor, Soojin Kim, Hyei-Jha Chung, Michael Humora, Kishta Katipally, Yizhe Wang
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Patent number: 6310058Abstract: Compounds represented by the formula [1] R1 is H or a substituent; R2 and R3 are C1-C3 alkyl; R4 is siderophore group e.g. CH3—(CH2)n—C(O)—N(OH)—(CH2)m— with n=10-22, m=2-6; X is O, S, or NH; X1 is O or NH; Y is H or alkyl; Z is H or substituted amino, e.g., t-BocNH or CbzNH, and r is 2-4; are useful in the method provided for treating tuberculosis. [1] is prepared by coupling [7], wherein HX1 is HO— or H2N—, with [4] obtained as the free acid after saponification of the methyl ester.Type: GrantFiled: May 25, 2000Date of Patent: October 30, 2001Assignee: University of Notre Dame du LacInventors: Marvin J. Miller, Yanping Xu
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Patent number: 6306880Abstract: A triazole compound having the formula: wherein Ar1 represents a phenyl group which may be substituted; Ar2 represents a phenyl group which may be substituted; R0 represents a hydrogen atom or a lower alkyl; R1 represents a lower alkyl; R2 to R5 each represnet a hydrogen atom or an unsubstituted or halo substituted alkyl; n represnets 0 to 2; p represents 0 or 1; q, r and s each represent 0 to 2; A represents a 4- to 7-membered carbon ring or a 4- to 7-membered heterocyclic, not including 1,3-dioxan-5-yl. The compound of the present invention exhibits an excellent antifungal activity.Type: GrantFiled: February 1, 1999Date of Patent: October 23, 2001Assignee: Sankyo Company, LimitedInventors: Sadao Oida, Teruo Tanaka, Yawara Tajima, Toshiyuki Konosu, Atsushi Somada, Takeo Miyaoka, Hiroshi Yasuda
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Patent number: 6303594Abstract: This invention relates to a series of arylsubstituted piperazines, of Formula I pharmaceutical compositions containing them and intermediates used in their manufacture. The compounds of the invention selectively inhibit binding to the &agr;-1a adrenergic receptor, a receptor which has been implicated in benign prostatic hyperplasia. As such the compounds are potentially useful in the treatment of this and other disease.Type: GrantFiled: March 15, 2000Date of Patent: October 16, 2001Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Linda Jolliffe, William Murray, Virginia Pulito, Allan Reitz, Xiaobing Li, Linda Mulcahy, Cynthia Maryanoff, Frank Villani
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Patent number: 6297233Abstract: Caprolactam inhibitors are provided which have the structure including pharmaceutically acceptable salts thereof and all stereoisomers thereof, and prodrugs thereof, wherein n is 1 to 5; and and Y R1, R2, R3, R5, R5a, R6, R7, R8, R9 and R10 are as defined herein. These compounds are inhibitors of Factor Xa and thus are useful as anticoagulants. A method for treating cardiovascular diseases associated with thromboses is also provided.Type: GrantFiled: February 2, 2000Date of Patent: October 2, 2001Assignee: Bristol-Myers Squibb CompanyInventors: Philip D. Stein, Gregory S. Bisacchi, Yan Shi, Stephen P. O'Connor, Chi Li
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Patent number: 6297232Abstract: The invention relates to triazolo[4,5-d]pyrimidin-3-yl derivatives which are useful in the treatment of platelet aggregation disorders.Type: GrantFiled: February 19, 1999Date of Patent: October 2, 2001Assignee: AstraZeneca ABInventors: Roger Victor Bonnert, Anthony Howard Ingall, Brian Springthorpe, Paul Andrew Willis
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Patent number: 6284755Abstract: The present invention is directed to azepan-2-one compounds which inhibit prenyl-protein transferase, particularly farnesyl-protein transferase (Ftase), and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.Type: GrantFiled: December 7, 1999Date of Patent: September 4, 2001Assignee: Merck & Co., Inc.Inventors: S. Jane deSolms, Samuel L. Graham, Anthony W. Shaw, Terrence M. Ciccarone, Gerald E. Stokker
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Patent number: 6262047Abstract: Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.Type: GrantFiled: October 10, 1997Date of Patent: July 17, 2001Assignee: COR Therapeutics, Inc.Inventors: Bing-Yan Zhu, Robert M. Scarborough
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Patent number: 6239127Abstract: The present invention relates to certain substituted caprolactam compounds of formula (I), where R1 is (C1-6)alkyl or (C3-6)cycloalkyl; R2 hydrogen or (C1-6)alkyl; X is (C1-12)alkynylene; (C2-12)alkynylene; m is 0 or 1; and R3 is (C3-8)cycloalkyl; or an aromatic ring system selected from (II, III, IV and V), where R4 is hydrogen, chloro, or methoxy; R5 is hydrogen, chloro, (C1-18)alkyl or (C1-18)alkoxy, and Z is oxygen, sulfur, N—H, or N—CH3; or a pharmaceutically acceptable acid addition salt thereof, where possible, pharmaceutical compositions containing said compounds, the use of said compounds in treating tumors and to a process for making said compounds.Type: GrantFiled: November 17, 1999Date of Patent: May 29, 2001Assignee: Novartis AGInventors: Frederick Ray Kinder, Jr., Kenneth Walter Bair, Christopher Turchik Jagoe, Richard William Versace, Sompong Wattanasin