Substituent On Ring Carbon Of The Bicyclo Ring System Contains The Additional Hetero Ring Patents (Class 548/467)
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Patent number: 7968591Abstract: 1,3-disubstituted 4-methyl-1H-pyrrole-2-carboxamides corresponding to formula I methods for their production, pharmaceutical compositions containing them, and the use thereof for noradrenalin receptor regulation, particularly for inhibiting noradrenalin reuptake, and/or for 5-HT receptor regulation, particularly for inhibiting 5-hydroxy tryptophan reuptake, and/or for opioid receptor regulation and/or for batrachotoxin (BTX) receptor regulation and/or for treating or inhibiting pain and other conditions.Type: GrantFiled: December 9, 2008Date of Patent: June 28, 2011Assignee: Gruenenthal GmbHInventors: Stefan Oberboersch, Bernd Sundermann, Corinna Sundermann, Edward Bijsterveld, Hagen-Heinrich Hennies
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Publication number: 20110152797Abstract: The present invention relates to cyclopentane heptenoic acid-5-cis-2-(3?-hydroxy or lower alkyloxy-5-thienylpentyl)-3,5-dihydroxy, [1?, 2?, 3?, 5?] compounds, lower alkyl, hydroxyl lower alkyl and indole lower alkyl amides and esters thereof as potent ocular hypotensives that are particularly suited for the management of glaucoma.Type: ApplicationFiled: December 17, 2010Publication date: June 23, 2011Applicant: ALLERGAN, INC.Inventor: Robert M. Burk
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Publication number: 20110144090Abstract: Indole compounds are disclosed. Also disclosed are methods for using the compounds to treat human and animal disease, pharmaceutical compositions of the compounds, and kits including the compounds.Type: ApplicationFiled: August 10, 2010Publication date: June 16, 2011Inventors: Amy Elder, Geraldine Harriman, Silvana Leit, Jie Li, Howard Sard, Yiliang Zhang, Doug Wilson
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Patent number: 7951940Abstract: The present invention features inhibitors of nitric oxide synthase (NOS), particularly those that selectively inhibit neuronal nitric oxide synthase (nNOS) in preference to other NOS isoforms. The NOS inhibitors of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing conditions such as, for example, stroke, reperfusion injury, neurodegeneration, head trauma, CABG, migraine headache with and without aura, migraine with allodynia, central post-stroke pain (CPSP), neuropathic pain, morphine/opioid induced tolerance and hyperalgesia.Type: GrantFiled: March 13, 2008Date of Patent: May 31, 2011Assignee: NeurAxon, Inc.Inventors: Shawn Maddaford, Jailall Ramnauth, Suman Rakhit, Joanne Patman, Paul Renton, Subhash C. Annedi
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Patent number: 7943784Abstract: The present invention encompasses a method for the preparation of Almotriptan and its pharmaceutically acceptable salts comprises, i) Methylation of 3-[5-(1-Pyrrolidinyl sulfonyl methyl)1H-indol-yl]ethane amine ii) Treating crude Almotriptan with a hydroxy benzoic acid yields hydroxy benzoic acid addition salt of Almotriptan iii) Converting Almotriptan hydroxy benzoic acid addition salt to Almotriptan and iv) Salification of Almotriptan to its pharmaceutically acceptable salts.Type: GrantFiled: July 21, 2006Date of Patent: May 17, 2011Assignee: Matrix Laboratories LimitedInventors: Satyanarayana Chava, Seeta Ramanjaneyulu Gorantla, Ramdas Chavakula, Babu Rao Konudula
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Patent number: 7915260Abstract: The invention is directed to Urotensin II antagonists. More specifically, the present invention relates to certain novel compounds, methods for preparing compounds, compositions, intermediates and derivatives thereof and methods for treating Urotensin-II mediated disorders. Pharmaceutical and veterinary compositions and methods of treating cardiovascular disorders and various other disease states or conditions using compounds of the invention are also described.Type: GrantFiled: January 10, 2007Date of Patent: March 29, 2011Inventors: Bruce E. Maryanoff, William A. Kinney, Edward C. Lawson, Diane K. Luci, Nikolay Marchenko, Sergey Sviridov, Shyamali Ghosh
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Publication number: 20110071132Abstract: The invention relates to novel oxindol derivative of general formula (I), wherein substituents R1, R2, A, B and Y are such as defined in a claim 1. Drugs containing said derivatives and the use thereof for preventing and/or treating vassopress- and/or oxytocin-dependent-diseases are also disclosed.Type: ApplicationFiled: July 30, 2010Publication date: March 24, 2011Applicant: Abbott GmbH & Co. KGInventors: Thorsten Oost, Wilfried Lubisch, Wolfgang Wernet, Andrea Hager-Wernet, Wilfried Hornberger, Liliane Unger
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Publication number: 20110046195Abstract: Compounds which modulate quorum sensing in quorum sensing bacteria. Compounds of the invention inhibit quorum sensing and/or activate quorum sensing in various bacteria. Compounds that inhibit quorum sensing are particularly useful for inhibition of detrimental bacterial biofilm formation. Compounds that activate quorum sensing are particularly useful for promoting growth and biofilm formation of beneficial bacterial.Type: ApplicationFiled: June 24, 2010Publication date: February 24, 2011Inventors: Helen E. BLACKWELL, Christine E. McInnis
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Patent number: 7868008Abstract: The present invention is directed to compounds of formula I: wherein R1, R2, R3, R4, R5, R6, R7, R8, R9 and n are as defined for formula I in the description. The invention also relates to processes for the preparation of the compounds and to new intermediates employed in the preparation, pharmaceutical compositions containing the compounds, and to the use of the compounds in therapy.Type: GrantFiled: February 15, 2006Date of Patent: January 11, 2011Assignee: AstraZeneca ABInventors: Bradford Van Wagenen, Radhakrishnan Ukkiramapandian, Joshua Clayton, Ian Egle, James Empfield, Methvin Isaac, Fupeng Ma, Abdelmalik Slassi, Gary Steelman, Rebecca Urbanek, Sally Walsh
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Patent number: 7868035Abstract: A compound comprising or a pharmaceutically acceptable salt or a prodrug thereof; wherein X and Y are described herein.Type: GrantFiled: January 31, 2006Date of Patent: January 11, 2011Assignee: Allergan, Inc.Inventors: David F. Woodward, Robert M. Burk
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Publication number: 20100331312Abstract: Amide derivatives of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the histamine H3 receptor. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of histamine H3-associated disorders, such as cognitive disorders, epilepsy, brain trauma, depression, obesity, disorders of sleep and wakefulness such as excessive daytime sleepiness, narcolepsy, shift-work sleep disorder, drowsiness as a side effect from a medication, maintenance of vigilance to aid in the completion of tasks and the like, cataplexy, hypersomnia, somnolence syndrome, jet lag, sleep apnea and the like, attention deficit hyperactivity disorder (ADHD), schizophrenia, allergies, allergic responses in the upper airway, allergic rhinitis, nasal congestion, dementia, Alzheimer's disease, pain and the like.Type: ApplicationFiled: February 18, 2009Publication date: December 30, 2010Applicant: ARENA PHARMACEUTICALS, INC.Inventors: Vincent J. Santora, Brian J. Hofilena, Michelle Pulley, Graeme Semple, Yun Shan, Brian M. Smith
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Publication number: 20100311795Abstract: The present invention relates to novel 1,3-dioxane carboxylic acids of the general formula (I), their tautomeric forms, their stereoisomers, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, methods for their preparation, use of these compounds in medicine and the intermediates involved in their preparation.Type: ApplicationFiled: February 19, 2007Publication date: December 9, 2010Inventors: Harikishore Pingali, Pankaj Maganlal Makadia, Braj Bhushan Lohray
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Publication number: 20100305182Abstract: The present invention provides compositions and methods for modulating the communication and virulence of quorum sensing bacteria. In various exemplary embodiments, the invention provides a combinatorial library of quorum sensing compounds including synthetic analogs of naturally occurring and non-naturally occurring acyl-homoserine lactone (AHL) analogs, and methods of synthesizing and using these compounds.Type: ApplicationFiled: December 17, 2009Publication date: December 2, 2010Inventors: Helen E. BLACKWELL, Grant D. Geske, Rachel Wezeman
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Publication number: 20100292290Abstract: The present invention relates to a novel process for the preparation of almotriptan and pharmaceutically acceptable salts thereof, which affords product conveniently and efficiently with commercially acceptable yields and purity. The present invention also relates to a novel synthetic intermediate used in the process.Type: ApplicationFiled: August 1, 2008Publication date: November 18, 2010Inventors: Vinayak Gore, Mahesh Gadkar, Kiran Pokharkar
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Publication number: 20100292187Abstract: The present invention provides compounds, pharmaceutical compositions, and methods of using such compounds or compositions for treating infection by a virus, or for affecting viral IRES activity.Type: ApplicationFiled: June 14, 2010Publication date: November 18, 2010Applicant: PTC THERAPEUTICS, INC.Inventors: Gary M. Karp, Peter Seongwoo Hwang, James J. Takasugi, Hongyu Ren, Richard Gerald Wilde, Anthony A. Turpoff, Alexander Arefolov, Guangming Chen, Jeffrey A. Campbell, Chunshi Li, Steven Paget, Nanjing Zhang, Xiaoyan Zhang, Jin Zhu
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Publication number: 20100286118Abstract: The present invention provides compounds of formula (I) in which y, m, n, R1, R2 and Q are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: ApplicationFiled: May 6, 2010Publication date: November 11, 2010Inventors: Rhonan Ford, Andrew Mather, Antonio Mete, Ian Millichip
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Publication number: 20100280091Abstract: Novel 3,6-disubstituted pyrans, optionally with a further substituent at the 4-position, are monoamine reuptake inhibitors with activity profiles of anti-depressants.Type: ApplicationFiled: July 15, 2010Publication date: November 4, 2010Applicant: WAYNE STATE UNIVERSITYInventor: Aloke K. Dutta
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Publication number: 20100273835Abstract: The invention provides compounds of general formula (I) or a pharmaceutically acceptable salt, polymorph or solvate thereof, including all tautomers and stereoisomers thereof, wherein K, W, X; Y and Z are described throughout the description and claims. The compounds of the present invention are useful as inhibitors of prolyl endopeptidase (PEP, EC 3.4.21.26) and/or IL-6.Type: ApplicationFiled: July 10, 2008Publication date: October 28, 2010Applicant: PROBIODRUG AGInventors: Ulrich Heiser, Andre J. Niestroj, Ingo Schulz
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Publication number: 20100267688Abstract: The present invention comprises compounds of Formula (I). wherein: X, R1, R2, R3, and R4 are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula (I).Type: ApplicationFiled: April 15, 2010Publication date: October 21, 2010Inventors: Xuqing Zhang, Heather Rae Hufnagel, Chaozhong Cai, James C. Lanter, Thomas P. Markotan, Zhihua Sui
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Patent number: 7816393Abstract: Novel isoindoline compounds are disclosed. Methods of treating, preventing and/or managing cancer, diseases and disorders associated with, or characterized by, undesired angiogenesis, and diseases and disorders mediated by PDE 4, using the compounds are also disclosed.Type: GrantFiled: August 4, 2009Date of Patent: October 19, 2010Assignee: Celgene CorporationInventors: George W. Muller, Hon-Wah Man
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Patent number: 7812017Abstract: The present invention relates to novel compounds of formula (I): wherein m, n, R0, R1, R2, R3 and R4 are as described herein, to pharmaceutical compositions comprising the compounds, to processes for their preparation, as well as to the use of the compounds for the preparation of a medicament against 5-HT6 receptor-related disorders.Type: GrantFiled: July 3, 2007Date of Patent: October 12, 2010Assignee: Biovitrum AB (publ.)Inventors: Johan Angbrant, Rune Ringom, Kristin Hammer, Erik Ringberg, Bengt Lindqvist, Gary Johansson, Peter Brandt, Katarina Beierlein, Björn M Nilsson
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Patent number: 7799933Abstract: The invention is concerned with novel sulfonamide derivatives of formula (I) wherein R1, R2, R3, X and Y are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit L-CPT1 and can be used as medicaments.Type: GrantFiled: December 6, 2007Date of Patent: September 21, 2010Assignee: Hoffman-La Roche Inc.Inventors: Simona M. Ceccarelli, Odile Chomienne, Patrizio Mattei, Ulrike Obst Sander
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Patent number: 7790832Abstract: A method for purifying a 2-aryl-3,3-bis(hydroxyaryl)phthalimidine comprises contacting a crude 2-aryl-3,3-bis(hydroxyaryl)phthalimidine with a purification agent, removing a 2-aryl-3-(aminoaryl)-3-(hydroxyaryl)phthalimidine compound from the crude 2-aryl-3,3-bis(hydroxyaryl)phthalimidine, and producing a purified 2-aryl-3,3-bis(hydroxyaryl)phthalimidine product comprising less than 200 parts per million of the 2-aryl-3-(aminoaryl)-3-(hydroxyaryl)phthalimidine compound. The purification agent is selected from the group consisting of an acidic material, an organic acid chloride, an organic anhydride, or a combination thereof. The 2-aryl-3-(aminoaryl)-3-(hydroxyaryl)phthalimidine compound has a formula: wherein each R1 is independently selected from a group consisting of a hydrocarbyl radical, a nitro radical, and a halogen atom; “a” is an integer from 0 to 4; and Ar1 and Ar2 are independently at each occurrence an aromatic radical.Type: GrantFiled: September 4, 2007Date of Patent: September 7, 2010Assignee: Sabic Innovative Plastics IP B.V.Inventors: Balakrishnan Ganesan, Pradeep Jeevaji Nadkarni, Kumar Arun Satyanarayana, Venkata Rama Narayanan Ganapathy Bhotla, Suresh Shanumgam, Gurram Kishan, Ravindra Vikram Singh
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Publication number: 20100222322Abstract: Indole compounds of Formula (I) are HIV reverse transcriptase inhibitors, wherein R1, R2, R3, R4 and R5 are defined herein. The compounds of Formula (I) and their pharmaceutically acceptable salts are useful in the inhibition of HIV reverse transcriptase, the prophylaxis and treatment of infection by HIV and in the prophylaxis, delay in the onset, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: ApplicationFiled: June 23, 2006Publication date: September 2, 2010Applicant: MERCK & CO., INC.Inventors: Scott E. Wolkenberg, Zhijian Zhao, Craig W. Lindsley
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Publication number: 20100222363Abstract: New bicyclic derivatives of formula (I); wherein the meanings for the various substituents are as disclosed in the description. These compounds are useful as p38 kinase inhibitors.Type: ApplicationFiled: June 28, 2006Publication date: September 2, 2010Applicant: PALAU PHARMA, S.A.Inventors: Carmen Almansa Rosales, Marina Virgili Bernadó
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Publication number: 20100209391Abstract: The embodiments provide compounds of the general Formula II, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments also provide treatment methods, including methods of treating a hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.Type: ApplicationFiled: April 28, 2010Publication date: August 19, 2010Applicant: INTERMUNE, INC.Inventors: SCOTT SEIWERT, LEONID BEIGELMAN, LAWRENCE M. BLATT, TIMOTHY KERCHER, APRIL L. KENNEDY, STEVEN W. ANDREWS
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Publication number: 20100173898Abstract: The present invention discloses and claims a series of substituted N-phenyl-pyrrolidinylmethylpyrrolidine amides of formula (I). Wherein R, R1, R2, R3 and R4 are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this invention also discloses methods of preparation of substituted pyrrolidinylmethylpyrrolidine amides and intermediates therefor.Type: ApplicationFiled: March 15, 2010Publication date: July 8, 2010Applicant: SANOFI-AVENTISInventors: Werngard CZECHTIZKY, Zhongli GAO, William J. HURST, Lothar SCHWINK, Siegfried STENGELIN
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Publication number: 20100173897Abstract: The present invention discloses and claims a series of substituted N-phenyl-bipyrrolidine carboxamides of formula (I). Wherein R, R1, R2, R3 and R4 are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this invention also discloses methods of preparation of substituted N-phenyl-bipyrrolidine carboxamides and intermediates therefor.Type: ApplicationFiled: March 15, 2010Publication date: July 8, 2010Applicant: SANOFI-AVENTISInventors: Werngard CZECHTIZKY, Zhongli GAO, William J. HURST, Lothar SCHWINK, Siegfried STENGELIN
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Publication number: 20100167936Abstract: The invention relates to the use of at least one ascorbic acid derivative for the functionalisation of matrices, and to specific ascorbic acid derivatives and processes for the preparation thereof.Type: ApplicationFiled: June 27, 2007Publication date: July 1, 2010Inventors: Thomas Rudolph, Philipp Buehle, Herwig Buchholz
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Publication number: 20100168101Abstract: The present invention is related to the use of oxindole hydrazide derivatives of formula (I) for the treatment and/or prevention of metabolic disorders mediated by insulin resistance or hyperglycemia, comprising diabetes type I and/or II, inadequate glucose tolerance, insulin resistance, hyperlipidemia, hypertriglyceridemia, hypercholesterolemia, obesity, polycystic ovary syndrome (PCOS). In particular, the present invention is related to the use of oxindole hydrazide derivatives of formula (I) to modulate, notably to inhibit the activity of PTPs, in particular of PTP1B, TC-PTP, SHP and GLEPP-1. The present invention is furthermore related to novel oxindole hydrazide derivatives and method of preparation thereof.Type: ApplicationFiled: December 23, 2009Publication date: July 1, 2010Applicant: APPLIED RESEARCH SYSTEMS ARS HOLDING N.V.Inventors: Agnes BOMBRUN, Patrick Gerber, Dennis Church
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Patent number: 7741359Abstract: The present invention relates to derivatives of non-steroidal anti-inflammatory drugs (NSAIDs) having improved anti-inflammatory properties useful in the treatment of inflammation, pain and fever. More particularly, NSAIDs are derivatized with a hydrogen sulfide (H2S) releasing moiety to produce novel anti-inflammatory compounds having reduced side effects.Type: GrantFiled: July 18, 2007Date of Patent: June 22, 2010Assignee: Antibe Therapeutics Inc.Inventors: John Wallace, Giuseppe Cirino, Vincenzo Santagada, Giuseppe Caliendo
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Patent number: 7741360Abstract: The present invention relates to substituted indoles of Formula (I) useful as pharmaceutical compounds for treating respiratory disorders.Type: GrantFiled: May 25, 2007Date of Patent: June 22, 2010Assignee: AstraZeneca ABInventors: Roger Victor Bonnert, Timothy Jon Luker, John Cumming
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Publication number: 20100137583Abstract: The present invention relates to peptidomimetic compounds useful as protease inhibitors, particularly as serine protease inhibitors and more particularly as hepatitis C NS3 protease inhibitors; intermediates thereto; their preparation including novel steroselective processes to intermediates. The invention is also directed to pharmaceutical compositions and to methods for using the compounds for inhibiting HCV protease or treating a patient suffering from an HCV infection or physiological condition related to the infection. Also provided are pharmaceutical combinations comprising, in addition to one or more HCV serine protease inhibitors, one or more interferons exhibiting anti-HCV activity and/or one or more compounds having anti HCV activity and a pharmaceutically acceptable carrier, and methods for treating or preventing a HCV infection in a patient using the compositions. The present invention is also directed to a kit or pharmaceutical pack for treating or preventing HCV infection in a patient.Type: ApplicationFiled: September 8, 2008Publication date: June 3, 2010Inventors: Robert Edward Babine, Shu-Hui Chen, Jason Eric Lamar, Nancy June Snyder, Xicheng Sun, Mark Joseph Tebbe, Frantz Victor, Q. May Wang, Yvonne Yee Mai Yip, Ivan Collado, Cristina Garcia-Paredes, Raymond Samuel Parker, III, Ling Jin, Deqi Guo, John Irvin Glass
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Publication number: 20100130581Abstract: This invention relates to derivatives of an endomorphin, or of an endomorphin analog, comprising at least one moiety selected from a lipid moiety, a cyclitol moiety and a saccharide moiety.Type: ApplicationFiled: March 30, 2007Publication date: May 27, 2010Inventors: Istvan Toth, Yasuko Koda, Mark Pasqualino Del Borgo, Joanne Therese Blanchfield
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Publication number: 20100119479Abstract: Disclosed herein are compounds represented by a formula: Therapeutic methods, compositions, medicaments, and dosage forms related thereto are also disclosed.Type: ApplicationFiled: October 14, 2009Publication date: May 13, 2010Applicant: INTERMUNE, INC.Inventors: BRAD BUCKMAN, VLADIMIR SEREBRYANY, SCOTT SEIWERT, LEONID BEIGELMAN, ANTITSA STOYCHEVA
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Patent number: 7714019Abstract: This invention provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with amido piperazine derivatives. These compounds possess unique antiviral activity, whether used alone or in combination with other antivirals, antiinfectives, immunomodulators or HIV entry inhibitors. More particularly, the present invention relates to the treatment of HIV and AIDS.Type: GrantFiled: April 2, 2009Date of Patent: May 11, 2010Assignee: Bristol-Myers Squibb CompanyInventors: John F. Kadow, Qiufen May Xue, Tao Wang, Zhongxing Zhang, Nicholas A. Meanwell
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Patent number: 7705035Abstract: The invention is directed to indoline amide derivatives of formula I as EP4 receptor ligands, antagonists or agonists, useful for the treatment of EP4 mediated diseases or conditions, such as acute and chronic pain, osteoarthritis, rheumatoid arthritis, cancer and glaucoma. Pharmaceutical compositions and methods of use are also included.Type: GrantFiled: June 8, 2007Date of Patent: April 27, 2010Assignee: Merck Frosst Canada Ltd.Inventors: Michael Boyd, John Colucci
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Publication number: 20100087659Abstract: The present invention provided a norbornene compound with cross-linkable groups and their derivative polymers, wherein said cross-linkable groups were olefin or epoxy groups. Norbornene polymers with cross-linkable side chain and their block copolymers as well as modified derivatives were prepared via living ring-open metathesis polymerization method. The resulting polymers with excellent solubility and optic properties had narrow molecular weight distribution, well-controlled molecular weight, small refraction index and high transparency. They were also suitable for preparing hybrid materials with high thermal stability and chemical resistance.Type: ApplicationFiled: September 8, 2009Publication date: April 8, 2010Inventors: Der-Jang Liaw, Ching-Cheng Huang, Shou-Mau Hong, Ming-Hung Huang
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Patent number: 7692005Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.Type: GrantFiled: July 12, 2006Date of Patent: April 6, 2010Assignee: Allergan, Inc.Inventors: Julie A. Wurster, Edward H. Wang, Richard C. Yee
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Publication number: 20100076202Abstract: The present invention provides an advantageous method for producing an intermediate which is useful for production of a compound which exhibits excellent VLA-4 inhibitory effect and safety. An intermediate (14) is produced through the following reaction scheme.Type: ApplicationFiled: December 1, 2009Publication date: March 25, 2010Applicant: DAIICHI PHARMACEUTICAL CO., LTD.Inventors: Yoshihiro TAKAYANAGI, Toshihide Yamada, Yukito Furuya, Yoshiyuki Yoneda
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Patent number: 7655641Abstract: The present invention is directed to a compound of Formula (I): and pharmaceutically acceptable salts, solvates, hydrates or stereoisomers thereof, which are useful in treating or preventing disorders mediated by a peroxisome proliferator activated receptor (PPAR) such as syndrome X, type II diabetes, hyperglycemia, hyperlipidemia, obesity, coagaulopathy, hypertension, arteriosclerosis, and other disorders related to syndrome X and cardiovascular diseases.Type: GrantFiled: February 10, 2004Date of Patent: February 2, 2010Assignee: Eli Lilly and CompanyInventors: Scott Eugene Conner, Lynn Stacy Gossett, Jonathan Edward Green, Winton Dennis Jones, Jr., Nathan Bryan Mantlo, Donald Paul Matthews, Daniel Ray Mayhugh, Daryl Lynn Smith, Jennifer Ann Vance, Xiaodong Wang, Alan M Warshawsky, Leonard Larry Winneroski, Jr., Yanping Xu, Guoxin Zhu
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Publication number: 20100022783Abstract: The present invention provides a VLA-4 inhibitor having high water-solubility and excellent long-term stability; i.e., sodium trans-4-[1-[2,5-dichloro-4-[(1-methyl-1H-3-indolylcarbonyl)amino]phenylacetyl]-(4S)-methoxy-(2S)-pyrrolidinylmethoxy]cyclohexanecarboxylate pentahydrate.Type: ApplicationFiled: October 7, 2009Publication date: January 28, 2010Applicant: DAIICHI PHARMACEUTICAL CO., LTD.Inventors: Makoto ONO, Shigeru Noguchi
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Patent number: 7652153Abstract: The present invention provides a compound of formula I: wherein the variables are as defined herein. The present invention also provides processes for preparing the compounds of formula I, and intermediates thereof, pharmaceutical compositions comprising those compounds, and methods of using the compounds and compositions.Type: GrantFiled: February 28, 2005Date of Patent: January 26, 2010Inventors: Jean Damien Charrier, Steven Durrant, Michael Mortimore, Michael O'Donnell, Alistair Rutherford, Sharn Ramaya, John Studley, Martin Trudeau, Adam Looker
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Publication number: 20100016314Abstract: Derivatives of azabicyclo octane presented by formula (I), the method of making them, and the compositions containing the same and the uses thereof as inhibitors of dipeptidyl peptidase IV (DPP-IV), wherein the substitutes in formula (I) have the same meanings as what is mentioned in the descriptions.Type: ApplicationFiled: October 30, 2007Publication date: January 21, 2010Inventors: Pengcho Tang, Zhigang Lin, Hejun Lü, Fuqiang Zhao, Li Li
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Publication number: 20100004463Abstract: Convenient method for obtaining carbapenem by hydrogenation with Raney Nickel, as an alternative to the known catalytic hydrogenation conducted under hydrogen overpressure in the presence of Palladium, starting from corresponding protected intermediates such as p-nitrobenzylesters and with optional suitable protections of any primary and secondary amino functions structurally present.Type: ApplicationFiled: June 25, 2009Publication date: January 7, 2010Applicant: ACS DOBFAR S.p.A.Inventors: Antonio MANCA, Riccardo Ambrogio Monguzzi
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Patent number: 7642281Abstract: This invention provides a method of treating a subject suffering from a cognitive impairment or a cognitive disorder which comprises administering to the subject an amount of an indolone compound effective to treat the subject's cognitive impairment or disorder.Type: GrantFiled: December 8, 2006Date of Patent: January 5, 2010Assignee: Helicon Therapeutics, Inc.Inventor: Thomas P. Blackburn
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Publication number: 20090326011Abstract: Disclosed herein are compounds of formula (I) where G and Q are heteroaromatic groups. These compounds are useful for treating psychosis or a psychotic condition, substance abuse, premature ejaculation or cognition impairment.Type: ApplicationFiled: June 13, 2006Publication date: December 31, 2009Inventors: Luca Arista, Francesca Cardullo, Anna Checchia, Dieter Hamprecht, Fabrizio Micheli, Giovanna Tedesco, Silvia Terreni
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Publication number: 20090324581Abstract: To provide a novel compound which has S1P receptor agonistic activity, exhibits excellent immunosuppressing effect, gives less adverse side effects, and can be orally administered. The invention provides a compound represented by general formula (I) (wherein A is a single bond, —O—, or —CH2—; R1 represents a hydrogen atom or a C1-C6 alkyl group, and V represents any one group selected from among the following groups (1) to (3): (1) -G1-, (2) -G2-N(R2)-G3-, and (3) a group represented by formula 2, wherein each of Z1 and Z2 represents a hydrogen atom or a C1-C6 alkyl group, Z3 represents a hydrogen or the like, Q represents —CH2—O— or the like, and Y represents a group represented by formula 3, a salt thereof, or a solvate thereof.Type: ApplicationFiled: May 9, 2007Publication date: December 31, 2009Applicant: Daiichi Sankyo company LimitedInventors: Nobuo Machinaga, Toshiharu Yoshino, Jun Chiba, Jun Watanabe, Takashi Suzuki, Youichi Kimura
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Publication number: 20090318521Abstract: 4-bromomethyl-2?-formylbiphenyl and 4-bromomethyl-2?-hydroxymethylbiphenyl are useful starting material for the preparation various angiotenzin II antagonists, which are prepared from 4-bromomethyl-2?-cyanobiphenyl or 4?-bromomethylbiphenylcarboxyilic derivatives using selected hydride reagent.Type: ApplicationFiled: March 30, 2006Publication date: December 24, 2009Applicant: LEK PHARMACEUTICALS D.D.Inventors: Anton Copar, Ljubomic Antoncic, Matej Antoncic
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Patent number: 7635710Abstract: The present invention relates to novel pyrone-indole derivatives, pharmaceutical formulations containing them, and use of the compounds in the manufacture of Medicaments for treating or preventing various diseases.Type: GrantFiled: February 12, 2007Date of Patent: December 22, 2009Assignee: Neurim Pharmaceuticals (1991) Ltd.Inventors: Moshe Laudon, Tal Peleg-Shulman