The Chalcogen, X, Is In A -c(=x)- Group Patents (Class 544/399)
  • Publication number: 20100010222
    Abstract: A pharmaceutical composition for topical administration for prevention and/or treatment of diseases associated with decrease in bone mass comprising an EP4 agonist as an active ingredient. An EP4 agonist, in which includes a compound possessing prostaglandin skeleton as a representative, possesses promoting action on bone formation, so it is useful for prevention and/or treatment of diseases associated with decrease in bone mass (bone diseases such as primary osteoporosis, secondary osteoporosis, bone metastasis of cancer, hypercalcemia, Paget's disease, bone loss and bone necrosis, postoperative osteogenesis, alternative therapy for bone grafting).
    Type: Application
    Filed: August 27, 2009
    Publication date: January 14, 2010
    Inventors: Toru MARUYAMA, Kaoru Kobayashi, Tohru Kambe, Takayuki Maruyama, Hideyuki Yoshida, Akio Nishiura, Nobutaka Abe
  • Publication number: 20090298819
    Abstract: The present invention provides novel piperazine derivatives which can be advantageously used for treating schizophrenia and related psychoses such as acute manic, bipolar disorder, autistic disorder and depression.
    Type: Application
    Filed: May 27, 2009
    Publication date: December 3, 2009
    Inventors: Laxminarayan Bhat, Prabhu Prasad Mohapatra, Kouacou Adiey
  • Publication number: 20090299064
    Abstract: The invention relates to new processes for the manufacture of N-{5-[4-(4-methyl-piperazino-methyl)-benzoylamido]-2-methylphenyl}4-(3-pyridyl)-2-pyrimidine-amine (compound of formula I, new processes for the manufacture of metabolites of N-{5-[4-(4-methyl-piperazino-methyl)-benzoylamido]-2-methylphenyl}-4-(3-pyridyl)-2-pyrimidine-amine observed after administration of the compound to warm-blooded animals as well as to intermediates used in said processes. New starting materials as well as processes for the preparation thereof are likewise the subject of this invention. The processes described herein are especially suitable to furnish said compounds having isotopic labeling. The such obtained labeled compounds are in particular suitable to track and to investigate into the metabolism of N-{5-[4-(4-methyl-piperazino-methyl)-benzoylamido]-2-methylphenyl}4-(3-pyridyl)-2-pyrimidine-amine and its pharmaceutically acceptable salts in clinical and pre-clinical studies.
    Type: Application
    Filed: June 13, 2006
    Publication date: December 3, 2009
    Inventors: Rhys Salter, Maria Ines Rodriguez Perez, Thomas Moenius, Rolf Voges, Hendrik Andres, Kirk Bordeaux
  • Patent number: 7626024
    Abstract: The present invention provides novel processes for the preparation of a cyclopentanone of Formula II and a lactone of Formula I, which are useful in the production of prostaglandins: wherein Z, R2, R3, X1, X2, and are as defined in the specification. The invention also provides novel enantiomerically enriched compounds.
    Type: Grant
    Filed: October 9, 2007
    Date of Patent: December 1, 2009
    Assignee: Irogate International Inc.
    Inventors: Shih-Yi Wei, Yu-Chih Yeh
  • Publication number: 20090264651
    Abstract: Amines and amine derivatives that improve the buffering range, and/or reduce the chelation and other negative interactions of the buffer and the system to be buffered. The reaction of amines or polyamines with various molecules to form polyamines with differing pKa's will extend the buffering range, derivatives that result in polyamines that have the same pKa yields a greater buffering capacity. Derivatives that result in zwitterionic buffers improve yield by allowing a greater range of stability.
    Type: Application
    Filed: May 8, 2009
    Publication date: October 22, 2009
    Inventor: Thomas Daly
  • Patent number: 7589094
    Abstract: Disclosed are compounds of the formula (I): useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.
    Type: Grant
    Filed: December 7, 2005
    Date of Patent: September 15, 2009
    Assignee: Elan Pharmaceuticals, Inc.
    Inventors: Andrea Gailunas, John A. Tucker, Ruth TenBrink, John Mickelson
  • Publication number: 20090221823
    Abstract: The present invention is related to 1-[(4-chlorophenyl)-phenylmethyl]-4-(2,2,2-trichloroethoxycarbonyl)-piperazine of the Formula (IV) and optically isomers thereof, process for preparation thereof and the use of the compound of the Formula (IV) in the preparation of 1-(4-chlorophenyl)-phenylmethyl-piperazine and optical isomers and salts thereof. 1-(4-chlorophenyl)-phenylmethyl-piperazine and optical isomers thereof are important intermediates in the preparation of non-sedating antihistamine-type active pharmaceutical ingredients.
    Type: Application
    Filed: December 8, 2006
    Publication date: September 3, 2009
    Inventors: Tibor Mezei, Eniko Molnar, Peter Trinka, Ferenc Bartha, Zoltan Katona, Gyorgyi Vereckeyne Donath, Kalman Nagy, Laszlo Pongo, Gyula Lukacs, Marta Porcs-Makkay, Zsuzsanna Evinger, Gyula Simig
  • Patent number: 7572790
    Abstract: Compound of formula (I): or pharmaceutically acceptable derivatives thereof, and their use as pharmaceuticals, particularly as p38 kinase inhibitors.
    Type: Grant
    Filed: April 7, 2004
    Date of Patent: August 11, 2009
    Assignee: SmithKline Beecham Corporation
    Inventors: Nicola Mary Aston, Paul Bamborough, Katherine Louise Jones, Vipulkumar Kantibhai Patel, Stephen Swanson, Ann Louise Walker
  • Patent number: 7569690
    Abstract: If an organic solvent with a water content of 15% or less is used when an oxycarbonyl-substituted piperazine derivative is produced from a piperazine derivative, the piperazine derivative can be oxycarbonylated.
    Type: Grant
    Filed: September 2, 2003
    Date of Patent: August 4, 2009
    Assignee: Toray Fine Chemicals Co., Ltd.
    Inventors: Masao Morimoto, Haruyo Sato
  • Publication number: 20090176984
    Abstract: In some embodiments, this invention pertains to isotopically enriched N-substituted piperazine acetic acids. In some embodiments, this invention pertains to methods for the preparation of isotopically enriched N-substituted piperazine acetic acids.
    Type: Application
    Filed: February 29, 2008
    Publication date: July 9, 2009
    Inventors: Subhakar Dey, Darryl J.C. Pappin, Subhasish Purkayastha, Sasi Pillai, James M. Coull
  • Publication number: 20090118480
    Abstract: The present invention relates to novel quaternized polymers, especially of chitin/chitosan type, and to carbohydrate polymers carrying quaternized ammonium groups, especially piperazinium groups. Such polymers are characterized i.a. by improved solubility characteristics.
    Type: Application
    Filed: August 31, 2006
    Publication date: May 7, 2009
    Applicant: FENNOPHARMA OY
    Inventors: Jukka Holappa, Tomi Jarvinen, Tapio Nevalainen, Jouko Savolainen, Rustam Safin
  • Patent number: 7514436
    Abstract: Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I): where x, y, W, V, R2, R3, R4, R5, R6, R6a, R7, R7a, R8, R8a, R9 and R9a are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.
    Type: Grant
    Filed: July 29, 2004
    Date of Patent: April 7, 2009
    Assignee: Xenon Pharmaceuticals Inc.
    Inventors: Heinz W. Gschwend, Vishnumurthy Kodumuru, Shifeng Liu, Rajender Kamboj
  • Publication number: 20090080074
    Abstract: A polymer film includes: a wavelength dispersion regulator represented by formula (I): wherein R1 and R2 each independently represents a hydrogen atom, an alkyl group or an aryl group, provided that both R1 and R2 are not hydrogen atoms at the same time; and R3 and R4 each independently represents an electron-withdrawing substituent, and R1 and R2, or R3 and R4 may be bonded together to form a ring, and wherein the polymer film has a retardation value that satisfies the following formulae (1) and (2): 70 nm?Rth(548)?300 nm??Formula (1) Rth(628)<Rth(548)<Rth(446)??Formula (2) wherein Rth(?) represents a retardation value expressed in nm in a film thickness direction measured at a wavelength of ? nm.
    Type: Application
    Filed: September 4, 2008
    Publication date: March 26, 2009
    Applicant: FUJIFILM Corporation
    Inventors: Nobutaka Fukagawa, Masaki Noro, Teruki Niori
  • Publication number: 20090023925
    Abstract: The present invention provides N?-(2-halobenzylidene)sulfonylhydrazides of formula I Compounds of formula I are useful for the manufacture of 1-arylsulfonylindazole 5-HT6 ligands.
    Type: Application
    Filed: June 27, 2008
    Publication date: January 22, 2009
    Applicant: Wyeth
    Inventors: Anita Wai-Yin Chan, Mahmut Levent, David Place, Panolil Raveendranath, Sanjay Raveendranth, Vijay Raveendranath, Girija Raveendranath, Xinxu Shi, Charles Wu
  • Publication number: 20080300261
    Abstract: Compounds of formula I are useful in treatment of diseases associated with the deposition of ?-amyloid in the brain.
    Type: Application
    Filed: July 19, 2005
    Publication date: December 4, 2008
    Inventors: Peter Blurton, Frank Burkamp, Ian Churcher, Timothy Harrison, Joseph Neduvelil
  • Patent number: 7452921
    Abstract: Compounds of formula (I) where: {R1 is methyl, ethyl, cycloalkyl or optionally substituted aryl; Z is arylene or a group of formula —(CHR4)n-, where R4 is hydrogen, hydroxy or alkyl, and n is a number from 0 to 6; Y is carbonyl or a —CH2— group; Q is a residue of a mono- or poly-hydroxyl compound having from I to 6 hydroxy groups; and x is a number from I to 6; and esters thereof} are useful as sensitizers for use in radiationcurable compositions.
    Type: Grant
    Filed: July 2, 2004
    Date of Patent: November 18, 2008
    Assignee: Sun Chemical Corporation
    Inventors: Shaun Lawrence Herlihy, Brian Rowett, Robert Stephen Davidson
  • Patent number: 7452891
    Abstract: The present invention discloses compounds which, are novel antagonists for melanin-concentrating hormone (MCH), as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such MCH antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.
    Type: Grant
    Filed: January 28, 2005
    Date of Patent: November 18, 2008
    Assignee: Schering Corporation
    Inventors: John W. Clader, Hubert B. Josien, Anandan Palani, Tin Yau Chan
  • Patent number: 7442692
    Abstract: A compound selected from those of formula (I): wherein: R3 represents a hydrogen atom, and R1 and R2 together with the carbon atoms carrying them form a benzene, naphthalene or quinoline ring structure, each of the ring structures being optionally substituted, or R1 represents a hydrogen atom, and R2 and R3 together with the carbon atoms carrying them form a benzene, naphthalene or quinoline ring structure, each of the ring structures being optionally substituted, n represents 1 or 2, —X— represents a group selected from —(CH2)m—O-Ak-, —(CH2)m—NR4-Ak-, —(CO)—NR4-Ak- and —(CH2)m—NR4-(CO)—, m represents an integer between 1 and 6 inclusive, Ak represents an optionally substituted alkylene chain, and R4 represents a hydrogen atom or an alkyl group, Ar represents an aryl or heteroaryl group, its enantiomers, diasteroisomers, and addition salts thereof with a pharmaceutically acceptable acid.
    Type: Grant
    Filed: March 29, 2006
    Date of Patent: October 28, 2008
    Assignee: Les Laboratoires Servier
    Inventors: Guillaume De Nanteuil, Bernard Portevin, Philippe Gloanec, Mark Millan, Jean-Claude Ortuno, Clotilde Mannoury La Cour, Alain Gobert
  • Publication number: 20080200474
    Abstract: Disclosed herein are novel salts of flunarizine with improved properties. Also described herein are novel pharmaceutical compositions comprising such flunarizine salts, methods of making, and related methods of treatment.
    Type: Application
    Filed: January 17, 2008
    Publication date: August 21, 2008
    Inventors: Matthew Peterson, Julius Remenar, Carlos Sanrame
  • Publication number: 20080177071
    Abstract: The present invention relates to a process for the manufacture of 2-{2-[4-(bis(4-fluorophenyl)methyl)-1-piperazinyl]ethoxy}acetic acids, amides or related derivatives, of the general formula (I) wherein: Y represents hydroxy or —NR1R2; R1 and R2 each independently represent hydrogen or C?1-4#191 alkyl; m is 1 or 2, and n is 1 or 2, as well as the non-toxic, pharmaceutically acceptable salts and mixtures thereof. The present invention concerns also a polymorphic form of efletirizine.
    Type: Application
    Filed: October 29, 2007
    Publication date: July 24, 2008
    Inventors: Ousmane Diouf, John Surtees
  • Patent number: 7365076
    Abstract: The present invention is directed to substituted aryl cycloalkanoyl derivatives, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal and genitourinary disorders, chronic fatigue syndrome, fibromylagia syndrome, nervous system disorders, and combinations thereof, particularly those conditions selected from the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibromyalgia, pain, diabetic neuropathy, and combinations thereof.
    Type: Grant
    Filed: October 12, 2004
    Date of Patent: April 29, 2008
    Assignee: Wyeth
    Inventors: Eugene John Trybulski, Joseph Peter Sabatucci, An Thien Vu, Stephen Todd Cohn, Arthur Attilio Santilli, Lori Krim Gavrin, Fei Ye, Paige Erin Mahaney
  • Patent number: 7355045
    Abstract: In some embodiments, this invention pertains to isotopically enriched N-substituted piperazine acetic acids. In some embodiments, this invention pertains to methods for the preparation of isotopically enriched N-substituted piperazine acetic acids.
    Type: Grant
    Filed: January 5, 2004
    Date of Patent: April 8, 2008
    Assignee: Applera Corporation
    Inventors: Subhakar Dey, Darryl J. C. Pappin, Subhasish Purkayastha, Sasi Pillai, James M. Coull
  • Patent number: 7335788
    Abstract: Dithiocarbonate derivatives are disclosed, along with a process for preparing the same. The dithiocarbonate compounds can be utilized as initators, chain transfer agents and/or terminators in controlled free radical polymerizations. The dithiocarbonates can be used to produce polymers having narrow molecular weight distribution. Advantageously, the compounds of the present invention can also introduce functional groups into the resulting polymers. The dithiocarbonate compounds have low odor and are substantially colorless.
    Type: Grant
    Filed: October 8, 2003
    Date of Patent: February 26, 2008
    Assignee: Lubrizol Advanced Materials, Inc.
    Inventor: John Ta-Yuan Lai
  • Publication number: 20080027075
    Abstract: The present invention provides novel quaternary amino-functional chalcone derivatives and analogues exhibiting interesting antibacterial activity. The compounds have the general formula (Y1)m—Ar1(X1)—C(=O)VAr2(X2)?(Y2)p (I), wherein V designates —CH2—CH2—, —CH?CH— or —C?C—; Ar1 and Ar2 independently are aryl and heteroaryl; m=0, 1, 2, p=0, 1, 2, m+p>0; each Y1 and Y2 independently is -Z—N+(R1)(R2)R4 Q? (A); —NR3-Z—N+(R1)(R2)R4 Q? (B), or —O-Z—N+(R1)(R2)R4 Q? (C), R1, R2, R3, R4, X1, X2 are substituents, and Q? is an anion. The present invention also relates to the compounds for use as pharmaceutically active agents, in particular against bacterial infections (such as Gram-negative and Gram-positive bacteria, including antibiotic-sensitive or resistant strains), and in the medical treatment of bacterial infections in mammals.
    Type: Application
    Filed: October 28, 2004
    Publication date: January 31, 2008
    Applicant: Lica Pharmaceuticals A/S
    Inventor: Simon Feldbaek Nielsen
  • Patent number: 7307169
    Abstract: In some embodiments, this invention pertains to isotopically enriched N-substituted piperazines. In some embodiments, this invention pertains to methods for the preparation of isotopically enriched N-substituted piperazines.
    Type: Grant
    Filed: January 5, 2004
    Date of Patent: December 11, 2007
    Assignee: Applera Corporation
    Inventors: Darryl J. C. Pappin, Sasi Pillai, James M. Coull
  • Patent number: 7273952
    Abstract: Substituted C-cyclohexylmethylamine derivatives, methods for the production thereof, pharmaceuticals containing said compounds, the use of substituted C-cyclohexylmethylamine derivatives for producing pharmaceuticals, and method of pain treatment using the pharmaceuticals.
    Type: Grant
    Filed: March 31, 2003
    Date of Patent: September 25, 2007
    Assignee: Gruenenthal GmbH
    Inventors: Bernd Sundermann, Corinna Maul, Helmut Buschmann, Michael Finkam, Babette-Yvonne Koegel
  • Patent number: 7229803
    Abstract: The invention relates to methods for reacting (di)amines as substrates in the presence of a lysine oxidase arid a reducing agent, resulting in alcohols, diols or cyclic secondary amines. In a particular embodiment, the invention is directed to methods of preparing cyclic secondary amines suitable for ultimately synthesizing piperidine-2-carboxylic acid and proline derivatives, useful, for example as thrombin inhibitors.
    Type: Grant
    Filed: April 8, 2002
    Date of Patent: June 12, 2007
    Assignee: BASF Aktiengesellschaft
    Inventors: Thomas Friedrich, Norbert Zimmermann, Rainer Stürmer
  • Patent number: 7195751
    Abstract: This invention pertains to methods, mixtures, kits and/or compositions for the determination of analytes by mass analysis using unique labeling reagents or sets of unique labeling reagents. The labeling reagents can be isomeric or isobaric and can be used to produce mixtures suitable for multiplex analysis of the labeled analytes.
    Type: Grant
    Filed: January 27, 2004
    Date of Patent: March 27, 2007
    Assignee: Applera Corporation
    Inventors: Darryl J. C. Pappin, Michael Bartlet-Jones
  • Patent number: 7166605
    Abstract: Probucol derivatives and pharmaceutical compositions containing the same to be employed in treatment or prophylaxis of diseases.
    Type: Grant
    Filed: March 19, 2003
    Date of Patent: January 23, 2007
    Assignee: Nicox, S.A.
    Inventors: Piero Del Soldato, Giancarlo Santus, Ennio Ongini
  • Patent number: 7115610
    Abstract: Disclosed are novel substituted heterocyclic derivatives having the structure of Formula I: The compounds are useful for the treatment of various disease states, in particular cardiovascular diseases such as atrial and ventricular arrhythmias, intermittent claudication, Prinzmetal's (variant) angina, stable and unstable angina, exercise induced angina, congestive heart disease, diabetes, and myocardial infarction.
    Type: Grant
    Filed: December 17, 2004
    Date of Patent: October 3, 2006
    Assignee: CV Therapeutics, Inc.
    Inventors: Elfatih Elzein, Prabha Ibrahim, Venkata Palle, Kenneth Rehder, Jeffrey Zablocki
  • Patent number: 7078402
    Abstract: The invention relates to novel aminothiol ester compounds having the general formula (I): and to a method for preparing them and to their use in pharmaceutical compositions intended for use in human or veterinary medicine (cancers and precancers, dermatological, rheumatic and ophthalmological complaints in particular) or in cosmetic compositions. The invention also relates to a pharmaceutical or cosmetic composition, characterized in that it comprises, as active agent, a compound of general formula (I) in combination with a pharmaceutically or cosmetically acceptable support.
    Type: Grant
    Filed: May 31, 2001
    Date of Patent: July 18, 2006
    Assignee: Centre National de la Recherche Scientifique (CNRS)
    Inventors: Guy Fournet, Gerard Anthony Quash, Jacques Gore
  • Patent number: 7074820
    Abstract: There is provided compounds of formula I, wherein R1, R2, R3, Y, n and B have meanings given in the description which are useful as competitive inhibitors of trypsin-like proteases, such as thrombin, and in particular in the treatment of conditions where inhibition of thrombin is required (e.g. thrombosis) or as anticoagulants.
    Type: Grant
    Filed: April 23, 2001
    Date of Patent: July 11, 2006
    Assignee: AstraZeneca AB
    Inventor: Thomas Antonsson
  • Patent number: 7019007
    Abstract: The invention provides compounds of Formula (I): wherein: R1–R4, A, D, and L have any of the values defined in the specification that are CCR-3 receptor antagonists, pharmaceutical compositions containing them, methods for their use, and methods and intermediates useful for preparing them.
    Type: Grant
    Filed: November 27, 2002
    Date of Patent: March 28, 2006
    Assignee: Syntex (U.S.A.) LLC
    Inventors: Daisy Joe Du Bois, Beihan Wang
  • Patent number: 6972287
    Abstract: The present invention provides a method of treating Alzheimer's disease using a compound of Formula (I). Also provided is a method of inhibiting the aggregation of amyloid proteins using a compound of the Formula (I) and a method of imaging amyloid deposits, as well as new compounds of Formula (I).
    Type: Grant
    Filed: May 31, 2000
    Date of Patent: December 6, 2005
    Assignee: Pfizer Inc.
    Inventors: Corinne Elizabeth Augelli-Szafran, Mark Robert Barvian, Christopher Franklin Bigge, Shelly Ann Glase, Shunichiro Hachiya, John Steven Kiely, Takenori Kimura, Yingjie Lai, Annette Theresa Sakkab, Mark James Suto, Larry Craswell Walker, Tomoyuki Yasunaga, Nian Zhuang
  • Patent number: 6916797
    Abstract: The invention relates to new ?-arylethylpiperazine of the formula wherein Z represents 0 or S; n? represents 1 or 2; R2 represents a hydrogen atom or a methyl group; W, Ar1 and Ar2 represent various substituents as defined herein; or non-toxic pharmaceutically acceptable salt, individual optical isomer, or individual diastereoisomer thereof, which are useful as neurokinin receptor antagonists (NK1 antagonists). It also relates to processes for their preparation and use in methods for treatment of asthma and/or allergic rhinitis.
    Type: Grant
    Filed: December 14, 2000
    Date of Patent: July 12, 2005
    Assignee: UCB, S.A.
    Inventors: Françoise Stiernet, Christophe Genicot, Marie-Agnes Lassoie, Florence Moureau, Thomas Ryckmans, Thierry Taverne, Jean-Pierre Henichart, Michel Neuwels, Solo Goldstein
  • Patent number: 6887876
    Abstract: Benzamidine derivatives are useful delta-opioid receptor modulators, agonists useful as analgesics and antagonists useful as immunosuppressants, antiinflammatory agents, agents for the treatment of neurological and psychiatric conditions, medicaments for drug and alcohol abuse, agents for treating gastritis and diarrhea, cardiovascular agents and agents for the treatment of respiratory diseases.
    Type: Grant
    Filed: December 11, 2001
    Date of Patent: May 3, 2005
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventors: Ellen W. Baxter, Samuel O. Nortey, Allen B. Reitz
  • Patent number: 6881738
    Abstract: The present invention relates to novel analogs of choline and methods of use or treatment of neurodegenerative disorders and/or conditions such as Parkinson's disease, Huntington disease, Alzheimer's disease and related disorders such as amyotrophic lateral sclerosis, spinal muscular atrophy, Friedrich's ataxia, Pick's disease, Bassen-Kornzweig syndrome, Refsom's disease, retinal degeneration, Cruetzfelt-Jacob syndrome or prion disease (mad cow disease), dementia with Lewy bodies, schizophrenia, paraneoplastic cerebellar degeneration and neurodegenerative conditions caused by stroke. The present compounds are effective to treat any neurological condition where acetylcholine transmission neurons and their target cells are affected.
    Type: Grant
    Filed: July 18, 2002
    Date of Patent: April 19, 2005
    Assignees: Medical College of Georgia Research Institute, University of Georgia Research Foundation, Inc
    Inventors: Jerry J. Buccafusco, Alvin V. Terry, J. Warren Beach, Rammamohanna R. Jonnala
  • Patent number: 6875765
    Abstract: The novel arylsulfonamide ether compounds, pharmaceutical compositions and uses thereof as inhibitors of interleukin-1? converting enzyme and other cysteine proteases in the ICE family are described. In one embodiment, the compound is described by the generalized structure: and pharmaceutically acceptable salts, esters, amides, and prodrugs thereof. In addition, methods of treating stroke, inflammatory diseases, septic shock, repurfusion injury, Alzheimer's disease, and shigellosis, using a compound of the invention or a pharmaceutical composition thereof, are described.
    Type: Grant
    Filed: May 10, 2002
    Date of Patent: April 5, 2005
    Assignee: Warner-Lambert Company
    Inventors: James Knobelsdorf, Sheryl Hays, Charles J. Stankovic, Kimberly S. Para, Michael K. Connolly, Paul Galatsis, William Harter, Aurash B. Shahripour, Mark Stephen Plummer, Beth Lunney, Bernd Janssen, Jay Bradford Fell
  • Patent number: 6855843
    Abstract: The present invention relates to a pharmaceutical composition comprising as an active ingredient a compound of formula (I), wherein Ring A is an aromatic or a heterocyclic ring; Q is a bond, carbonyl, lower alkylene, lower alkenylene, —O— -(lower alkylene)-, etc.; n is 0, 1 or 2; Z is oxygen or sulfur; W is oxygen, sulfur, —CH?CH—, —NH— or —N?CH—; R1, R2 and R3 are the same or different and are hydrogen, halogen, hydroxyl, a substituted or unsubstituted lower alkyl gorup, a substituted or unsubstituted lower alkoxy group, a substituted or unsubstituted amino group, etc.; R4 is tetrazolyl, carboxyl group, amide or ester; R5 is hydrogen, nitro, amino, hydroxyl, lower alkanoyl, lower alkyl, etc.; R6 is selected from (a) a substituted or unsubstituted phenyl group, (b) a substituted or unsubstituted pyridyl group, (c) a substituted or unsubstituted thienyl group, (d) a substituted or unsubstituted benzofuranyl group, etc.; or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: November 4, 2002
    Date of Patent: February 15, 2005
    Assignee: Tanabe Seiyaku Co., Ltd.
    Inventors: Ila Sircar, Kristjan S. Gudmundsson, Richard Martin
  • Patent number: 6846824
    Abstract: Compounds of formula (I) its tautomeric forms, its stereoisomers, its polymorphs, its pharmaceutically acceptable salts or its pharmaceutically acceptable solvates can be used to prevent or treat diabetes caused by insulin resistance or impaired glucose tolerance or complications of diabetes caused by insulin resistance or impaired glucose tolerance. The compounds can also be used to reduce cholesterol, body weight, blood glucose, triglycerides and free fatty acids in the blood.
    Type: Grant
    Filed: March 23, 2001
    Date of Patent: January 25, 2005
    Assignee: Dr. Reddy's Laboratories Ltd.
    Inventors: Braj Bhushan Lohray, Vidya Bhushan Lohray, Ashok Channaveerappa Bajji, Shivaramayya Kalchar, Rajagopalan Ramanujam, Ranjan Chakrabarti, Javed Iqbal, Ranga Madhavan Gurram
  • Patent number: 6844299
    Abstract: This invention generally relates to new polyol ester derivatives of polyamines for use as dispersant additives compatible in synthetic ester-based turbo oils. The dispersant additives of the present invention consist of a hydrocarbon acid, a polyol, an amine carrier such as diacid or cyclic anhydride and a polyamine. The hydrocarbon acid makes up the non-polar hydrocarbon portion of the dispersant and the polyamine functions as the polar headgroup. The diacid or cyclic anhydride provides a means for attaching the polar polyamine to the dispersant structure through an amide linkage. Different dispersant structures are obtained by varying the hydrocarbon acid, the polyol and the nature of the polyamine.
    Type: Grant
    Filed: February 20, 2003
    Date of Patent: January 18, 2005
    Assignee: BP Corporation North America Inc.
    Inventors: Paul W. Bessonette, Patrick E. Godici, Kim E. Fyfe, Jeenok T. Kim
  • Publication number: 20040267012
    Abstract: Compounds of formula (I): wherein when m is 0 to 4 R1 is selected from C1-6alkyl, C3-7cycloalkyl, C2-6alkenyl, —SO2NR4R5, —CONR4R5 and —COOR4; and when m is 2 to 4 R1 is additionally selected from C1-6alkoxy, hydroxy, NR4R5, —NR4SO2R5, —NR4SOR5, —NR4COR5, and —NR4CONR4R5; R2 is selected from hydrogen, C1-6alkyl and —(CH2)n-C3-7cycloalkyl; R3 is the group —CO—NH—(CH2)p-R6; U is selected from methyl and halogen; W is selected from methyl and chlorine; V and Y are each selected independently from hydrogen, methyl and halogen; m is selected from 0, 1, 2, 3 and 4 wherein each carbon atom of the resulting carbon chain may be optionally substituted with one or two groups selected independently from C1-6alkyl; n is selected from 0, 1, 2 and 3; p and r are independently selected from 0, 1 and 2; s is selected from 0, 1 and 2; or pharmaceutically acceptable salts or solvates thereof, and their use as pharmaceuticals, particularly as p38 kinase inhibitors
    Type: Application
    Filed: April 15, 2004
    Publication date: December 30, 2004
    Inventors: Richard Martyn Angell, Nicola Mary Aston, Paul Bamborough, George Stuart Cockerill, Suzanne Joy Merrick, Kathryn Jane Smith, Ann Louise Walker
  • Publication number: 20040266782
    Abstract: This invention relates to certain cyclic amine derivatives of Formula (I) 1
    Type: Application
    Filed: November 21, 2003
    Publication date: December 30, 2004
    Inventors: Leyi Gong, Denis John Kertesz, David Bernard Smith, Francisco Xavier Talamas, Robert Stephen Wilhelm
  • Publication number: 20040259868
    Abstract: Compounds of formula (I) 1
    Type: Application
    Filed: July 6, 2004
    Publication date: December 23, 2004
    Inventors: John Walter Liebeschuetz, Christopher William Murray, Stephen Clinton Young, Nicholas Paul Camp, Stuart Donald Jones, William Alexander Wylie, John Joseph Masters, Michael Robert Wiley, Scott Martin Sheehan, David Birenbaum Engel, Brian Morgan Watson
  • Publication number: 20040258620
    Abstract: The invention relates to a novel class of ligands, complexes comprising such ligands and a metal ion, and adducts of these metal complexes and a macromolecule. Pharmaceutical compositions and methods of making and using the ligand-metal complexes are also described. The invention also relates to the use of macromolecular adducts for enhancement of diagnostic imaging. In particular, the invention relates to (ethylene)-(propylene)-triaminepentaacetic acid (EPTPA) derivatives, a process for their production, and their use for the production of pharmaceutical agents for NMR diagnosis or radiodiagnosis or radiotherapy.
    Type: Application
    Filed: August 19, 2004
    Publication date: December 23, 2004
    Inventors: Lutz Lehmann, Ulrich Niedballa, Hannelore Niedballa, Johannes Platzek, Matthias Friebe, Christoph Hilger, Andre E Merbach, Eva Jakab Toth, Robert Ruloff, Sabrina Laus
  • Publication number: 20040254166
    Abstract: Phenyl acetamide compounds are described, including compounds of Formula I: 1
    Type: Application
    Filed: April 1, 2004
    Publication date: December 16, 2004
    Inventors: Kevin D. Kreutter, Lily Lee, Tianbao Lu, Venkatraman Mohan, Sharmila Patel, Hui Huang, Guozhang Xu, Mark Fitzgerald
  • Publication number: 20040248886
    Abstract: The present invention relates to sulfonamide derivatives of formula (I) notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such sulfonamide derivatives. Said sulfonamide derivatives are useful in the treatment of neuronal disorders, autoimmune diseases, cancer and cardiovascular diseases. Furthermore, said sulfonamide derivatives are efficient modulators of the JNK pathway, they are in particular efficient and selective inhibitors of JNK2 and -3. The present invention is furthermore related to novel sulfonamide derivatives as well as to methods of their preparation. Formula (I) IAr1 is a substituted or unsubstituted aryl or heteroaryl group; X is O or S, preferably O; Ar2 a substituted or unsubstituted arylene or heteroarylene group; R1 and R2 are independently selected from the group consisting of hydrogen and a C1-C6-alkyl group.
    Type: Application
    Filed: June 30, 2004
    Publication date: December 9, 2004
    Inventors: Arthur A. Aykanian, Steve Billingsley, Philip M. Hodge, Kevin L. Simpson, John Spisak, Jim Strahan
  • Publication number: 20040248887
    Abstract: The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme. The present invention also provides methods for treating a disease state in a subject by selectively inhibiting cathepsin S.
    Type: Application
    Filed: March 23, 2004
    Publication date: December 9, 2004
    Applicant: IRM LLC
    Inventors: Hong Liu, Phil Alper, Arnab Chatterjee, David Tully, Badry Bursulaya, David Woodmansee, Robert Epple, Jennifer Leslie Harris, Jun Li
  • Publication number: 20040242572
    Abstract: The present invention relates to carboxamide compounds of general formula I 1
    Type: Application
    Filed: August 22, 2003
    Publication date: December 2, 2004
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Dirk Stenkamp, Martin Lenter, Heike-Andrea Wieland, Klaus Rudolf, Stephan George Mueller, Ralf R.H. Lotz, Kirsten Arndt, Philipp Lustenberger, Thorsten Lehmann-Lintz
  • Publication number: 20040236100
    Abstract: Compounds useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis, are disclosed.
    Type: Application
    Filed: October 14, 2003
    Publication date: November 25, 2004
    Inventors: Shalini Sharma, Reid W. von Borstel