Polycyclo Ring System Having The Hetero Ring As One Of The Cyclos Patents (Class 514/443)
  • Patent number: 6982348
    Abstract: The present invention provides a pharmaceutical agent having cholesteryl ester transfer protein inhibitory action and useful as a blood lipid lowering agent and the like. The present invention relates to a compound represented by the formula wherein Ar1 is an aromatic ring group optionally having substituents, Ar2 is an aromatic ring group having substituents, OR? is an optionally protected hydroxyl group, R is an acyl group, R? is a hydrogen atom or a hydrocarbon group optionally having substituents, or a salt thereof, and a pharmaceutical composition containing a compound of the formula (I) or a salt thereof or a prodrug thereof.
    Type: Grant
    Filed: January 25, 2002
    Date of Patent: January 3, 2006
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Masakuni Kori, Kazumasa Hamamura, Hiromitsu Fuse, Toshihiro Yamamoto
  • Patent number: 6967216
    Abstract: Compounds of formula (I): wherein: X is a group of formula (A) or (B): and R1, R2, R3, R4, n, x, y and z are as defined within are described. Processes for their preparation and their use in the treatment of disorders mediated by the neuropeptide Y5 receptor in a warm-blooded animal, such as a human being are also described.
    Type: Grant
    Filed: May 1, 2001
    Date of Patent: November 22, 2005
    Assignee: AstraZeneca AB
    Inventors: Michael Howard Block, Craig Samuel Donald, David Robert Brittain, Kevin Michael Foote
  • Patent number: 6964980
    Abstract: Disclosed are methods of reducing serum glucose and triglyceride levels and for inhibiting angiogenesis, the methods comprising administration of substituted indolealkanoic acids to patients in need of such treatment. Also disclosed are such compounds useful in the treatment of angiogenesis, hyperglycemia, hyperlipidemia and chronic complications arising from diabetes mellitus. Also disclosed are pharmaceutical compositions containing the compounds.
    Type: Grant
    Filed: March 26, 2003
    Date of Patent: November 15, 2005
    Assignee: The Institute for Pharmaceutical Discovery, Inc.
    Inventors: Janet Sredy, Jorge Jacot
  • Patent number: 6962929
    Abstract: The invention provides methods and compositions relating to novel pentafluorophenylsulfonamide derivatives and analogs and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly cancer, vascular restenosis, microbial infections, and psoriasis, or as lead compounds for the development of such agents.
    Type: Grant
    Filed: October 11, 2002
    Date of Patent: November 8, 2005
    Assignee: Tularik Inc.
    Inventors: John A. Flygare, Julio Cesar Medina, Bei Shan, David Louis Clark, Terry J. Rosen
  • Patent number: 6958358
    Abstract: Compounds of general formula (I): wherein R1, Y, (X)o, (W)n, (V)m, Z and U are as defined in the specification, are inhibitors of cruzipain and other cysteine protease inhibitors and are useful as therapeutic agents, for example in Chagas' disease, or for validating therapeutic target compounds.
    Type: Grant
    Filed: January 17, 2002
    Date of Patent: October 25, 2005
    Assignee: Amura Therapeutics Limited
    Inventors: Martin Quibell, Manoj Kumar Ramjee
  • Patent number: 6958348
    Abstract: Disclosed is an anti-cancer compound represented by Structural Formula (I): The variables in Structural Formula (I) are described hereinbelow. Also disclosed is a pharmaceutical composition comprising a pharmaceutically acceptable carrier or diluent and a compound represented by Structural Formula (I) (preferably an effective amount). Also disclosed is a method of treating a subject with cancer by administering to the subject an effective amount of a compound represented by Structural Formula (I).
    Type: Grant
    Filed: August 29, 2002
    Date of Patent: October 25, 2005
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Keizo Koya, Lijun Sun, Mitsunori Ono, Guiqing Liang, David James, Hao Li, Zhi-Qiang Xia
  • Patent number: 6956054
    Abstract: Treatment of warm-blooded animals having a tumor or non-malignant hypervascularation, by administering a sufficient amount of a cytotoxic agent formulated into a phosphate prodrug form having substrate specificity for microvessel phosphatases, so that microvessels are destroyed preferentially over other normal tissues, because the less cytotoxic prodrug form is converted to the highly cytotoxic dephosphorylated form.
    Type: Grant
    Filed: August 14, 2002
    Date of Patent: October 18, 2005
    Assignees: Baylor University, OXiGENE, Inc.
    Inventors: Ronald W. Pero, David Sherris, Kevin G. Pinney, Vani P. Mocharla, Zhi Chen
  • Patent number: 6951869
    Abstract: A method of preventing or treating either scarring or capsular contractures in subjects in need of such treatment comprising the administration of leukotriene receptor antagonists to said subject in need of treatment.
    Type: Grant
    Filed: June 14, 2002
    Date of Patent: October 4, 2005
    Inventor: Stephen L. Schlesinger
  • Patent number: 6951878
    Abstract: The present invention provides novel compounds, novel compositions, methods of their use, and methods of their manufacture, where such compounds are pharmacologically useful inhibitors of Protein Tyrosine Phosphatases (PTPase's) such as PTP1B, CD45, SHP-1, SHP-2, PTP?, LAR and HePTP or the like. The compounds are useful in the treatment of type I diabetes, type II diabetes, impaired glucose tolerance, insulin resistance, obesity, immune dysfunctions including autoimmunity diseases with dysfunctions of the coagulation system, allergic diseases including asthma, osteoporosis, proliferative disorders including cancer and psoriasis, diseases with decreased or increased synthesis or effects of growth hormone, diseases with decreased or increased synthesis of hormones or cytokines that regulate the release of/or response to growth hormone, diseases of the brain including Alzheimer's disease and schizophrenia, and infectious diseases.
    Type: Grant
    Filed: May 28, 2002
    Date of Patent: October 4, 2005
    Assignee: Novo Nordisk A/S
    Inventors: Niels Peter Hundahl Møller, Henrik Sune Andersen, Lars Fogh Iversen, Ole Hvilsted Olsen, Sven Branner, Daniel Dale Holsworth, Farid Bakir, Luke Milburn Judge, Frank Urban Axe, Todd Kevin Jones, William Charles Ripka, Yu Ge, Roy Teruyuki Uyeda
  • Patent number: 6946462
    Abstract: New compounds represented by the formula or pharmaceutically acceptable salts or prodrugs thereof, wherein X1 and X2 are each independently selected from a CH group or a nitrogen atom; and R is an optionally substituted five or six membered nonaromatic carbocyclic ring or a nonaromatic or aromatic heterocyclic ring, whereby the ring is optionally condensed with a 6-membered, optionally substituted carbocyclic aromatic ring.
    Type: Grant
    Filed: April 13, 2004
    Date of Patent: September 20, 2005
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Rainer Haag, Ulrike Leser-Reiff, Anja Limberg, Michael Weidner, Gerd Zimmermann
  • Patent number: 6933317
    Abstract: Compounds of the general formula (I) which are metabolically stable and have an antagonistic activity against PGD2 receptor: ? wherein Y is bicyclic ring; R1 is optionally substituted heteroaryl; R2 is hydrogen, etc.; R3 is —CH2—CH2—CH2—CH2—CH?CH—COOR4, —CH2—CH2—CH2—CH2—X1—CH2—COOR4, —CH2—CH?CH—CH2—X1—CH2—COOR4 or —CH2—CH2—CH2—COOR4; R4 is hydrogen, etc.; X1 is —O—, etc.
    Type: Grant
    Filed: October 26, 2001
    Date of Patent: August 23, 2005
    Assignee: Shionogi & Co. Ltd.
    Inventors: Norihiko Tanimoto, Yoshiharu Hiramatsu, Tsunetoshi Honma, Masanao Inagaki
  • Patent number: 6921774
    Abstract: The invention provides novel compounds of the formula I below: wherein the meaning of each substituent is defined in the application. The compounds are useful as inhibitors of the glycine transporter and useful in the treatment of diseases responsive to the inhibition of the glycine transporter. The invention provides a pharmaceutical composition comprising a compound of Formula I as defined above and the use of compounds as above for the manufacture of medicaments for treatment of diseases responsive to ligands of the glycine transporter.
    Type: Grant
    Filed: January 17, 2003
    Date of Patent: July 26, 2005
    Assignee: H. Lundbeck A/S
    Inventors: Ejner Knud Moltzen, Paul Garrick Smith, Christian Krog-Jensen, Klaus Peter Bøgesø
  • Patent number: 6921756
    Abstract: The invention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel ?-lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic ?-lactamase inhibitors presently available, and which do not require a ?-lactam pharmacophore. The invention also provides pharmaceutical compositions and methods for inhibiting bacterial growth.
    Type: Grant
    Filed: April 8, 2003
    Date of Patent: July 26, 2005
    Assignee: MethylGene, Inc.
    Inventors: Jeffrey M. Besterman, Jubrail Rahil, Arkadii Vaisburg
  • Patent number: 6906086
    Abstract: The current invention provides methods and pharmaceutical formulations that are useful for inhibiting the loss of bone. These methods and formulations can be used without the associated adverse effects of estrogen therapy, and thus serve as an effective and acceptable treatment for osteoporosis.
    Type: Grant
    Filed: May 27, 2003
    Date of Patent: June 14, 2005
    Assignee: Eli Lilly and Company
    Inventor: Larry J. Black
  • Patent number: 6906092
    Abstract: The present invention relates to a method of inhibiting matrix metalloproteinases using compounds that are dibenzofuran sulfonamide derivatives having the Formula I More particularly, the present invention relates to a method of treating diseases in which matrix metalloproteinases are involved such as multiple sclerosis, atherosclerotic plaque rupture, restenosis, aortic aneurism, heart failure, periodontal disease, corneal ulceration, burns, decubital ulcers, chronic ulcers or wounds, cancer metastasis, tumor angiogenesis, arthritis, or other autoimmune or inflammatory diseases dependent upon tissue invasion by leukocytes.
    Type: Grant
    Filed: June 25, 2003
    Date of Patent: June 14, 2005
    Assignee: Warner-Lambert Company
    Inventors: Patrick Michael O'Brien, Joseph Armand Picard, Drago Robert Sliskovic, Andrew David White
  • Patent number: 6887869
    Abstract: The invention concerns novel mikanolide derivatives, their preparation method and their therapeutic uses, in particular as anti-cancer and anti-viral agents.
    Type: Grant
    Filed: January 11, 2002
    Date of Patent: May 3, 2005
    Assignee: Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S.)
    Inventors: Olivier Lavergne, Christophe Lanco, Grégoire Prevost, Beng Poon Teng
  • Patent number: 6884791
    Abstract: The intention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel ?-lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic ?-lactamase inhibitors presently available, and which do not require a ?-lactam pharmacophore. The invention also provides pharmaceutical compositions and methods for inhibiting bacterial growth.
    Type: Grant
    Filed: November 22, 2002
    Date of Patent: April 26, 2005
    Assignee: MethylGene, Inc.
    Inventors: Jeffrey M. Besterman, Jubrail Rahil, Arkadii Vaisburg
  • Patent number: 6875787
    Abstract: The present invention provides a method of treating ocular hypertension or glaucoma which comprises administering to an animal having ocular hypertension or glaucoma therapeutically effective amount of a compound represented by the general formula I; wherein the dashed line indicates the presence or absence of a bond, the hatched wedge indicates the ? (down) configuration, and the solid triangle indicates the ? (up) configuration; B is a single, double, or triple covalent bond; n is 0-6; X is CH2, S or O; Y is any pharmaceutically acceptable salt of CO2H, or CO2R, CONR2, NHCH2CH2OH, N(CH2CH2OH)2, CH2OR, P(O)(OR)2, CONRSO2R, SONR2, or R is H, C1-6 alkyl or C2-6 alkenyl; R2 and R3 are C1-6 linear alkyl which may be the same or different, and may be bonded to each other such that they form a ring incorporating the carbon to which they are commonly attached; R4 is hydrogen, R, C(?O)R, or any group that is easily removed under physiological conditions such that R4 is effectively hydrogen; R5 is hydrogen
    Type: Grant
    Filed: February 11, 2003
    Date of Patent: April 5, 2005
    Assignee: Allergan, Inc.
    Inventor: Yariv Donde
  • Patent number: 6872746
    Abstract: The present invention is directed to novel fused pyrrolocarbazoles and isoindolones, including pharmaceutical compositions, diagnostic kits, assay standards or reagents containing the same, and methods of using the same as therapeutics. The invention is also directed to intermediates and processes for making these novel compounds.
    Type: Grant
    Filed: April 24, 2003
    Date of Patent: March 29, 2005
    Assignee: Cephalon, Inc.
    Inventor: Robert L. Hudkins
  • Patent number: 6872730
    Abstract: The present invention relates to novel substituted benzofurans and benzothiophenes compounds that are antagonists of alpha V (?v) integrins, for example ?v?3 and ?v?5 integrins, their pharmaceutically acceptable salts, and pharmaceutical compositions thereof. The compounds may be used in the treatment of pathological conditions mediated by ?v?3 and ?v?5 integrins, including such conditions as tumor growth, metastasis, restenosis, osteoporosis, inflammation, macular degeneration, diabetic retinopathy, and rheumatoid arthritis. The compounds have the general formula I: where R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, m, n, i, j and k are defined herein.
    Type: Grant
    Filed: April 26, 2002
    Date of Patent: March 29, 2005
    Assignee: 3-Dimensional Pharmaceuticals, Inc.
    Inventors: Beth M. Anaclerio, Juan J. Marugan Sanchez, Victor J. Marder, David C. U'Prichard, Bruce E. Tomczuk
  • Patent number: 6869972
    Abstract: The subject invention pertains to novel compounds (and salts thereof), and compositions comprising the compounds, for the treatment of cardiac arrhythmias. The subject invention further concerns methods of making the novel compounds. The novel compounds are rapidly metabolized analogs of amiodarone, having the distinct and advantageous characteristic of being metabolized to a less lipophilic compound. This results in an improved safety profile. The new compounds have particular utility for treating life-threatening ventricular tachyarrhythmias, especially in patients with congestive heart failure (CHF). The compounds also provide effective management for ventricular arrhythmias and supraventricular arrhythmias, including atrial fibrillation and re-entrant tachyarrhythmias involving accessory pathways.
    Type: Grant
    Filed: March 11, 2004
    Date of Patent: March 22, 2005
    Assignee: ARYx Therapeutics
    Inventor: Pascal Druzgala
  • Patent number: 6869953
    Abstract: New compounds represented by the formula or pharmaceutically acceptable salts or prodrugs thereof, wherein X1 and X2 are each independently selected from a CH group or a nitrogen atom; and R is an optionally substituted five or six membered nonaromatic carbocyclic ring or a nonaromatic or aromatic heterocyclic ring, whereby the ring is optionally condensed with a 6-membered, optionally substituted carbocyclic aromatic ring.
    Type: Grant
    Filed: August 6, 2002
    Date of Patent: March 22, 2005
    Assignee: Hoffman-La Roche Inc.
    Inventors: Rainer Haag, Ulrike Leser-Reiff, Anja Limberg, Michael Weidner, Gerd Zimmermann
  • Patent number: 6864254
    Abstract: An inhibitor for 20-hydroxyeicosatetraenoic acid production which comprises as the active ingredient a specific hydroxyformamidine derivative or a pharmacologically acceptable salt thereof. It is useful especially as a remedy for kidney diseases, cerebrovascular diseases, or circulatory diseases. The novel hydroxyformamidine derivative or pharmacologically acceptable salt thereof is also provided.
    Type: Grant
    Filed: November 1, 2000
    Date of Patent: March 8, 2005
    Assignee: Taisho Pharmaceutical Co., Ltd.
    Inventors: Masakazu Sato, Noriyuki Miyata, Takaaki Ishii, Yuko Kobayashi, Hideaki Amada
  • Patent number: 6861444
    Abstract: Compounds of the general formula (I): or a salt thereof, wherein R1 is hydrogen, hydroxyl or halogen; R2 is NHSO2CH3, SO2NHCH3 or the like; R5 and R6 each independently is hydrogen, C1-6 alkyl, optionally substituted phenyl or optionally substituted benzyl; X is NH, sulfur, oxygen or methylene; Y is oxygen, NR7, sulfur, methylene or a bond; and * represents an asymmetric carbon atom. The compounds are useful as a medicine for treating or preventing diabetes, obesity, hyperlipidemia, digestive diseases, depression or urinary disturbances.
    Type: Grant
    Filed: April 25, 2001
    Date of Patent: March 1, 2005
    Assignee: Asahi Kasei Pharma Corporation
    Inventors: Shunichi Ikuta, Shiro Miyoshi, Kohei Ogawa
  • Patent number: 6838477
    Abstract: Described herein are compounds related to lactacystin and lactacystin ?-lactone, pharmaceutical compositions containing the compounds, and methods of use.
    Type: Grant
    Filed: August 8, 2001
    Date of Patent: January 4, 2005
    Assignee: President and Fellows of Harvard College
    Inventors: Stuart L. Schreiber, Robert F. Standaert, Gabriel Fenteany, Timothy F. Jamison
  • Publication number: 20040266850
    Abstract: The invention relates to novel fungicidally active compound combinations of
    Type: Application
    Filed: May 7, 2004
    Publication date: December 30, 2004
    Inventors: Ulrike Wachendorff-Neumann, Thomas Seitz, Herbert Gayer, Ulrich Heinemann, Bernd-Wieland Kruger, Wolfgang Kramer, Lutz Assmann
  • Publication number: 20040234623
    Abstract: The present invention provides improved treatment methods by the administration of both an inhibitor of indoleamine-2,3-dioxygenase in addition to the administration of an additional therapeutic agent.
    Type: Application
    Filed: February 17, 2004
    Publication date: November 25, 2004
    Applicant: Medical College of Georgia Research Institute, Inc.
    Inventors: David Munn, Andrew Mellor
  • Patent number: 6818660
    Abstract: The present invention features calcilytic compounds. “Calcilytic compounds” refer to compounds able to inhibit calcium receptor activity. Also described are the use of calcilytic compounds to inhibit calcium receptor activity and/or achieve a beneficial effect in a patient; and techniques which can be used to obtain additional calcilytic compounds.
    Type: Grant
    Filed: October 19, 2001
    Date of Patent: November 16, 2004
    Assignee: NPS Pharmaceuticals, Inc.
    Inventors: Eric G. Del Mar, Robert M. Barmore, Derek Sheehan, Bradford C. Van Wagenen, James F. Callahan, Richard M. Keenan, Nikesh R. Kotecha, Maria Amparo Lago, Linda Sue Southall, Mervyn Thompson
  • Patent number: 6818666
    Abstract: Bi-aromatic compounds linked via a heteroethynylene radical are provided along with pharmaceutical and cosmetic compositions containing these compounds and methods for their use.
    Type: Grant
    Filed: August 9, 2002
    Date of Patent: November 16, 2004
    Assignee: Galderma Research & Development
    Inventors: Jean-Michel Bernardon, Philippe Diaz
  • Publication number: 20040225006
    Abstract: Compounds of formula (I) wherein R is hydrogen, alkyl, alkenyl, alkynyl, aryl, heteroaryl or heterocyclyl; and R1 is bicyclyl or heterobicyclyl; are useful in the treatment and prophylaxis of conditions mediated by s-CD23 or TNF.
    Type: Application
    Filed: May 14, 2004
    Publication date: November 11, 2004
    Applicant: SmithKline Beecham p.l.c.
    Inventors: Gordon Bruton, Andrew Faller, Barry Sidney Orlek, Kishore Kalidas Rana, Graham Walker
  • Publication number: 20040220251
    Abstract: The synthesis and study of biological activity of a series of new molecules with potential antimicrobial activity are described. The molecules are bicyclic carbohydrates, based on furanose sugars. Their antimicrobial activity against viruses is demonstrated, next to cytostatic effects. Significantly, a high and selective activity against Cytomegalovirus was observed.
    Type: Application
    Filed: January 20, 2004
    Publication date: November 4, 2004
    Inventors: Benedikt Sas, Johan Van hemel, Jan Vandenkerckhove, Eric Peys, Johan Van der Eycken, Steven Van Hoof
  • Patent number: 6812243
    Abstract: The invention relates to tyrosine kinase inhibitors of the bis-indolyl compound type of the general formula I: pharmaceuticals containing them and their use for the treatment of malignant and other diseases based on pathological cell proliferation.
    Type: Grant
    Filed: May 3, 2002
    Date of Patent: November 2, 2004
    Assignee: Zentaris AG
    Inventors: Siavosh Mahboobi, Sabine Kuhr, Herwig Pongratz, Alfred Popp, Harald Hufsky, Frank-D Bohmer, Steffen Teller, Andrea Uecker, Thomas Beckers
  • Patent number: 6803378
    Abstract: Novel diketoacid compounds of Formula I are provided which are useful as HIV integrase inhibitors and for the treatment of AIDS or ARC.
    Type: Grant
    Filed: September 25, 2002
    Date of Patent: October 12, 2004
    Assignee: Bristol-Myers Squibb Company
    Inventors: Michael A. Walker, Timothy D. Johnson, Nicholas A. Meanwell, Jacque Banville
  • Patent number: 6800656
    Abstract: The present invention provides a compound of the formula and pharmaceutically acceptable salts having useful antiviral activity against viruses of the herpes family. Wherein: X=O, (CH2)m, S, SO, SO2, NH, NR8; Y=O, (CH2)m, S, SO, SO2, NH, NR8 or a chemical bond; Z=NH, O, NR8, S, SO, SO2; The remaining substituents are described in the specification.
    Type: Grant
    Filed: July 5, 2002
    Date of Patent: October 5, 2004
    Assignee: Warner Lambert Company
    Inventors: Richard John Booth, Vara Prasad Venkata Nagendra Josyula, Annette Lynn Meyer, Bruce Allan Steinbaugh
  • Publication number: 20040192744
    Abstract: New compounds represented by the formula 1
    Type: Application
    Filed: April 13, 2004
    Publication date: September 30, 2004
    Inventors: Rainer Haag, Ulrike Leser-Reiff, Anja Limberg, Michael Weidner, Gerd Zimmermann
  • Patent number: 6797693
    Abstract: This invention provides methods for utilizing a PTPase inhibiting compounds and one or more insulins in methods for use in control and maintenance of type II diabetes in a mammal, for improving the cardiovascular and cerebrovascular risk profiles, reduction of hyperlipidemia, lowering low density lipoprotein blood levels, lowering free fatty acid blood levels and triglyceride levels and inhibition, prevention or reduction of atherosclerosis in a type II diabetic, or the risk factors thereof.
    Type: Grant
    Filed: June 6, 2002
    Date of Patent: September 28, 2004
    Assignee: Wyeth
    Inventors: John Thomas Gwynne, Philippe John Robert Vitou
  • Patent number: 6797726
    Abstract: An N-alkoxyalkyl-N,N-dialkylamine derivative represented by the following general formula [1]: wherein the ring D represents a 5- or 6-membered heterocyclic ring or hydrocarbon ring; R3 and R4, which are the same or different, represent an unsubstituted or substituted alkyl, cycloalkyl or aralkyl group; and R1, R2, R5, R6, R7, R8, m and n are as defined in the specification, or a salt thereof has an anti-hypoxic activity, a nerve-protecting activity and a nerve regeneration promoting activity and is useful for the treatment of neurodegenerative diseases.
    Type: Grant
    Filed: December 11, 2001
    Date of Patent: September 28, 2004
    Assignee: Toyama Chemical Co., Ltd.
    Inventors: Satoshi Ono, Akihito Saitoh, Noboru Iwakami, Masaya Nakagawa, Sumie Yamaguchi
  • Publication number: 20040176437
    Abstract: The subject invention pertains to novel compounds (and salts thereof), and compositions comprising the compounds, for the treatment of cardiac arrhythmias. The subject invention further concerns methods of making the novel compounds. The novel compounds are rapidly metabolized analogs of amiodarone, having the distinct and advantageous characteristic of being metabolized to a less lipophilic compound. This results in an improved safety profile. The new compounds have particular utility for treating life-threatening ventricular tachyarrhythmias, especially in patients with congestive heart failure (CHF). The compounds also provide effective management for ventricular arrhythmias and supraventricular arrhythmias, including atrial fibrillation and re-entrant tachyarrhythmias involving accessory pathways.
    Type: Application
    Filed: March 11, 2004
    Publication date: September 9, 2004
    Inventor: Pascal Druzgala
  • Publication number: 20040176435
    Abstract: There is provided a heretoaryloxy 3-substituted propanamine compound of formula (I): wherein A is selected from —O— and —S—; X is selected from phenyl optionally substituted with up to 5 substituents selected from halo, C1-C4 alkyl and C1-C4 alkoxy, and thienyl optionally substituted with up to 3 substituents selected from halo and C1-C4 alkyl; Y is selected from benzothienyl, indolyl and benzofuranyl, optionally substituted with up to 5 substituents selected from halo, C1-C4 alkyl, C1-C4 alkoxy, nitro, acetyl and cyano; and when Y is indolyl it may be substituted or further substituted by an N-substituent selected from C1-C4 alkyl; R1 and R2 are each independently H or C1-C4 alkyl; and pharmaceutically acceptable salts thereof.
    Type: Application
    Filed: October 23, 2003
    Publication date: September 9, 2004
    Inventors: Peter Gallagher, Richard Edmund Rathmell, Maria Ann Fagan
  • Patent number: 6787559
    Abstract: This invention relates to certain sulfonamide derivatives that are inhibitors of procollagen C-proteinase, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.
    Type: Grant
    Filed: October 9, 2002
    Date of Patent: September 7, 2004
    Assignee: Syntex (U.S.A.) LLC.
    Inventors: Roland Joseph Billledeau, Chris Allen Broka, Jeffrey Allen Campbell, Jian Jeffrey Chen, Sharon Marie Dankwardt, Nancy Delaet, Leslie Ann Robinson, Keith Adrian Murray Walker
  • Patent number: 6784299
    Abstract: This invention relates to a series of substituted aromatic ethers of the formula I wherein ring A and X and Y are defined as in the specification, that exhibit activity as glycine transport inhibitors, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, and their use for the enhancement of cognition and the treatment of the positive and negative symptoms of schizophrenia and other psychoses in mammals, including humans.
    Type: Grant
    Filed: April 16, 2003
    Date of Patent: August 31, 2004
    Assignee: Pfizer Inc.
    Inventor: John A. Lowe, III
  • Publication number: 20040162304
    Abstract: The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including: bone loss, bone fractures, osteoporosis, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, cerebral degenerative disorders, restenosis, gynecomastia, vascular smooth muscle cell proliferation, obesity, incontinence, and cancer, in particular of the breast, uterus and prostate.
    Type: Application
    Filed: October 14, 2003
    Publication date: August 19, 2004
    Inventors: Timothy Allen Blizzard, Milton Lloyd Hammond, Jerry Dwain Morgan, Ralph Troy Mosley
  • Publication number: 20040157841
    Abstract: Mono-acylated o-phenylendiamines derivatives of formula I 1
    Type: Application
    Filed: February 3, 2004
    Publication date: August 12, 2004
    Inventors: Georg Fertig, Frank Herting, Manfred Kubbies, Anja Limberg, Ulrike Reiff, Michael Weidner
  • Publication number: 20040147580
    Abstract: Compounds are disclosed which are Fab I inhibitors and are useful in the treatment of bacterial infections.
    Type: Application
    Filed: October 6, 2003
    Publication date: July 29, 2004
    Inventors: Walter J. Burgess, Dalia Jakas, William F Huffmann, William H Miller, Kenneth A Newlander, Mark A Seefeld, Irene N Uzinskas
  • Patent number: 6767920
    Abstract: The present invention provides a method of treating ocular hypertension or glaucoma which comprises administering to an animal having ocular hypertension or glaucoma therapeutically effective amount of a compound represented by the general formula I; wherein hatched lines represent the &agr; configuration, a triangle represents the &bgr; configuration, a wavy line represents the &agr; configuration or the &bgr; configuration and a dotted line represents the presence or absence of a double bond; A and B are independently selected from the group consisting of O, S and CH2; provided that at least one of A or B is S; D represents a covalent bond or CH2, O, S or NH; X is CO2R, CONR2, CH2OR, P(O)(OR)2, CONRSO2R SONR2 or Y is O, OH, OCOR2, halogen or cyano; Z is CH2 or a covalent bond; R is H or R2; R1 is H, R2, phenyl, or COR2; R2 is C1-C5 lower alkyl or alkenyl and R3 is benzothienyl, benzofuranyl, naphthyl or substituted derivatives thereof, wherein the substituents may
    Type: Grant
    Filed: January 16, 2003
    Date of Patent: July 27, 2004
    Assignee: Allergan, Inc.
    Inventors: Robert M. Burk, Mark Holoboski, Mari F. Posner
  • Publication number: 20040142971
    Abstract: Benzothiophene compounds such as 1
    Type: Application
    Filed: June 6, 2002
    Publication date: July 22, 2004
    Applicant: GeneSoft, Inc.
    Inventors: Roland W. Burli, Eldon E. Baird, Matthew J. Taylor, Jacob A. Kaizerman, Wenhao Hu
  • Publication number: 20040138282
    Abstract: The present invention provides compounds and methods of administering compounds to a subject taht can reduce &bgr;APP production and that is not toxic in a wide range of dosages. The present invention also provides non-carbamate compounds and methods of administering such compounds to a subject that can reduce &bgr;APP production and that is not tocix in a wide range of dosages. It has been discovered that either the racemic or enantiomerically pure non-carbamate compounds can be used to decrease &bgr;APP production.
    Type: Application
    Filed: February 6, 2004
    Publication date: July 15, 2004
    Inventors: Nigel H. Greig, Karen T. Y. Shaw, Qiang-Sheng Yu, Harold W. Holloway, Timothy T. Sencrant, Tada Utsuki, Donald K. Ingram, Arnold Brossi, Anthony Giordano, Gordon Powers, Diane Davidson, Michael Sturgess
  • Publication number: 20040127546
    Abstract: Compounds of the general formula (I): 1
    Type: Application
    Filed: January 22, 2004
    Publication date: July 1, 2004
    Applicant: ASAHI KASEI PHARMA CORPORATION
    Inventors: Shunichi Ikuta, Shiro Miyoshi, Kohei Ogawa
  • Publication number: 20040127543
    Abstract: Compounds of the Formula I: 1
    Type: Application
    Filed: September 10, 2003
    Publication date: July 1, 2004
    Inventors: Deborah Ann Evrard, Uresh Shantilal Shah, Gary Paul Stack
  • Publication number: 20040110791
    Abstract: Arylaminopropane analogues are disclosed. Also disclosed are methods for the lowering and controlling of normal or elevated intraocular pressure as well as a method for the treatment of glaucoma using compositions containing one or more of the compounds of the present invention.
    Type: Application
    Filed: November 26, 2003
    Publication date: June 10, 2004
    Inventors: Mark R. Hellberg, Abdelmoula Namil