Bicyclo Ring System Which Contains The Hetero Ring As One Of The Cyclos Patents (Class 540/523)
  • Publication number: 20110009386
    Abstract: A first aspect of the invention relates to a compound of formula (I), or a pharmaceutically acceptable salt, hydrate, complex or pro-drug thereof, wherein: one of R3 and R4 is H, and the other is selected from C1-6-alkyl, C1-6-haloalkyl, C1-6-alkoxy, and C6-12-aralkyl; or R3 and R4 are each independently selected from C1-6-alkyl and halo; R9 is a substituted 5 or 6-membered aryl or heteroaryl group or a 6,5- or 6,6-fused biaryl or heterobiaryl group. Compounds of formula (I) exhibit surprisingly high efficacies for human cathepsin S, excellent selectivity verses other mammalian cathepsins and are useful for treatment of diseases such as rheumatoid arthritis, multiple sclerosis, myasthenia gravis, transplant rejection, diabetes, Sjogrens syndrome, Grave's disease, systemic lupus erythematosis, osteoarthritis, psoriasis, idiopathic thrombocytopenic purpura, allergic rhinitis, asthma, atherosclerosis, obesity, chronic obstructive pulmonary disease and chronic pain.
    Type: Application
    Filed: August 9, 2010
    Publication date: January 13, 2011
    Applicant: Amura Therapeutics Limited
    Inventors: Martin Quibell, John P. Watts, Nicholas S. Flinn
  • Patent number: 7867997
    Abstract: A ?-crystalline form of ivabradine hydrochloride of formula (I): characterised by its powder X-ray diffraction data. Medicinal products containing the same which are useful as bradycardics.
    Type: Grant
    Filed: August 27, 2009
    Date of Patent: January 11, 2011
    Assignee: Les Laboratoires Servier
    Inventors: Stephane Horvath, Marie-Noelle Auguste, Gerard Damien
  • Patent number: 7867994
    Abstract: Process for the synthesis of ivabradine of formula (I): addition salts thereof with a pharmaceutically acceptable acid and hydrates thereof. ? crystalline form of ivabradine hydrochloride. Medicinal products containing ? crystalline form of ivabradine hydrochloride, which are useful as bradycardics.
    Type: Grant
    Filed: January 18, 2007
    Date of Patent: January 11, 2011
    Assignee: Les Laboratoires Servier
    Inventors: Jean-Michel Lerestif, Jean-Pierre Lecouve, Jean-Claude Souvie, Daniel Brigot, Stephane Horvath, Marie-Noelle Auguste, Gerard Damien
  • Patent number: 7867995
    Abstract: A ?d-Crystalline form of ivabradine hydrochloride of formula (I): characterised by its powder X-ray diffraction data. Medicinal products containing the same which are useful as bradycardics.
    Type: Grant
    Filed: August 27, 2009
    Date of Patent: January 11, 2011
    Assignee: Les Laboratoires Servier
    Inventors: Stephane Horvath, Marie-Noelle Auguste, Gerard Damien
  • Patent number: 7867996
    Abstract: A ?-Crystalline form of ivabradine hydrochloride of formula (I): characterised by its powder X-ray diffraction data. Medicinal products containing the same which are useful as bradycardics.
    Type: Grant
    Filed: August 27, 2009
    Date of Patent: January 11, 2011
    Assignee: Les Laboratories Servier
    Inventors: Stephane Horvath, Marie-Noelle Auguste, Gerard Damien
  • Publication number: 20100305099
    Abstract: The present invention encompasses compounds of general formula (1) wherein A, B, R1-R3, Rx and n are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and their use for preparing a medicament having the above-mentioned properties.
    Type: Application
    Filed: December 2, 2008
    Publication date: December 2, 2010
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Ioannis Sapountzis, Juergen Braunger, Daniel Kuhn
  • Patent number: 7838517
    Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.
    Type: Grant
    Filed: May 15, 2009
    Date of Patent: November 23, 2010
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Ronald Knegtel, Jean-Damien Charrier, Steven Durrant, Guy Brenchley, Michael Mortimore
  • Publication number: 20100292157
    Abstract: The invention relates generally to novel compositions and methods comprising a cyclohexanehexol and a secretase inhibitor. The compositions and methods provide beneficial effects, in particular sustained beneficial effects, in the treatment of diseases involving a disorder in protein folding and/or aggregation, and/or amyloid formation, deposition, accumulation, or persistence, such as Alzheimer's disease and related neurodegenerative disorders.
    Type: Application
    Filed: November 22, 2007
    Publication date: November 18, 2010
    Inventor: Antonio Cruz
  • Publication number: 20100267692
    Abstract: The present invention relates to compounds conformationally constrained mimetics of Smac with function as inhibitors of Inhibitor of Apoptosis Proteins (IAPs), the invention also relates to the use of these compounds in therapy, wherein the induction of apoptotic cell death is beneficial, especially in the treatment of cancer, alone or in combination with other active ingredients.
    Type: Application
    Filed: November 5, 2008
    Publication date: October 21, 2010
    Inventors: Carlo Scolastico, Leonardo Pierpaolo Manzoni, Pierfausto Seneci, Laura Belvisi, Domenico Delia, Martino Bolognesi, Eloise Mastrangelo, Mario Milani, Ilaria Motto, Carmelo Drago
  • Publication number: 20100249396
    Abstract: The present invention relates to a benzazepinone compound represented by the following formula (I): wherein R1 represents a C1-C6 alkyl group or halogeno C1-C6 alkyl group, R2 represents a carboxyl group which may be protected, and Y represents a group represented by the formula (II): wherein Z represents CH or a nitrogen atom, or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: November 14, 2008
    Publication date: September 30, 2010
    Inventors: Naoto Suzuki, Yasunori Tsuzaki, Kimihiko Yoshimura, Masahiko Hagihara, Yukinori Wada, Masao Maruyama, Nobuyoshi Fujii, Yasuhiro Aga
  • Publication number: 20100249398
    Abstract: Process for the synthesis of ivabradine of formula (I): and addition salts thereof with a pharmaceutically acceptable acid.
    Type: Application
    Filed: March 29, 2010
    Publication date: September 30, 2010
    Applicant: LES LABORATOIRES SERVIER
    Inventors: Jean-Louis Peglion, Aimée Dessinges, Bernard Serkiz
  • Publication number: 20100249397
    Abstract: Process for the synthesis of ivabradine of formula (I): and addition salts thereof with a pharmaceutically acceptable acid.
    Type: Application
    Filed: March 29, 2010
    Publication date: September 30, 2010
    Applicant: LES LABORATOIRES SERVIER
    Inventors: Jean-Louis Peglion, Aimée Dessinges, Bernard Serkiz
  • Publication number: 20100234350
    Abstract: Novel compounds of formulae (I) to (VIII), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylsulfonamide derivatives which are effective platelet ADP receptor inhibitors. These derivatives may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also relates to a method for preventing or treating thrombosis in a mammal comprising the step of administering a therapeutically effective amount of a compound of formulae (I) to (VIII), or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: September 14, 2009
    Publication date: September 16, 2010
    Applicant: Portola Pharmaceuticals, Inc.
    Inventors: Robert M. Scarborough, Wolin Huang, Charles K. Marlowe, Kim A. Kane-McGuire, Hans-Michael Jantzen, David M. Sedlock
  • Publication number: 20100222326
    Abstract: The present invention relates to new compounds, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.
    Type: Application
    Filed: April 24, 2008
    Publication date: September 2, 2010
    Applicant: UCB PHARMA, S.A.
    Inventors: Benoit Kenda, Laurent Turet, Yannick Quesnel, Philippe Michel, Ali Ates
  • Publication number: 20100222320
    Abstract: Compounds of formula I: Selectively attenuate production of A?(1-42) and hence find use in treatment or prevention of diseases associated with deposition of A? in the brain, in particular Alzheimer's disease.
    Type: Application
    Filed: June 9, 2008
    Publication date: September 2, 2010
    Inventors: Christian Fischer, Ben Munoz, Susan Zultanski, Joey Methot, Hua Zhou, W. Colby Brown
  • Patent number: 7786105
    Abstract: The invention relates to pyrimidine compounds of general formula (I), and to the use of these compounds of general formula (I) and of the physiologically compatible acid addition salts of compounds (I) for producing a pharmaceutical agent for treating diseases, which respond to the influence of dopamine D3 receptor antagonists or agonists.
    Type: Grant
    Filed: June 3, 2005
    Date of Patent: August 31, 2010
    Assignee: Abbott GmbH & Co. KG
    Inventors: Herve Geneste, Andreas Haupt, Wilfried Braje, Wilfried Lubisch, Gerd Steiner
  • Publication number: 20100190688
    Abstract: Compounds, compositions and methods for treatment of hyperproliferative diseases, such as cancer are provided.
    Type: Application
    Filed: July 12, 2005
    Publication date: July 29, 2010
    Inventors: Bin Chao, Thomas L. Deckwerth, Paul S. Furth, Steven D. Linton, Alfred P. Spada, Brett R. Ullman, Michael I. Weinhouse
  • Publication number: 20100179316
    Abstract: The present invention encompasses a process for the preparation of highly pure ivabradine hydrochloride by treating ivabradine with alcoholic hydrogen chloride. The invention further encompasses amorphous ivabradine hydrochloride and process for its preparation using suitable acid addition salts of ivabradine.
    Type: Application
    Filed: May 29, 2008
    Publication date: July 15, 2010
    Applicant: IND-SWIFT LABORATORIES LIMITED
    Inventors: Satyendra Pal Singh, Gajendra Singh, Lalit Wadhwa
  • Publication number: 20100160628
    Abstract: Process for the synthesis of ivabradine of formula (I): and addition salts thereof with a pharmaceutically acceptable acid.
    Type: Application
    Filed: December 23, 2009
    Publication date: June 24, 2010
    Applicant: LES LABORATOIRES SERVIER
    Inventors: Jean-Louis Peglion, Aimée Dessinges, Bernard Serkiz, Jean-Michel Lerestif, Jean-Pierre Lecouve
  • Patent number: 7723384
    Abstract: The invention relates to novel keto lactam compounds, hydrogenated derivatives and tautomers thereof. These compounds have valuable therapeutic properties and are particularly suited for treating diseases that respond to the modulation of the dopamine D3 receptor.
    Type: Grant
    Filed: December 10, 2004
    Date of Patent: May 25, 2010
    Assignee: Abbott GmbH & Co. KG.
    Inventors: Wilfried Lubisch, Andreas Haupt, Wilfried Braje, Herve Geneste
  • Patent number: 7709471
    Abstract: There is provided a compound of formula (I): processes for the manufacture thereof, pharmaceutical compositions thereof and uses in therapy.
    Type: Grant
    Filed: July 5, 2007
    Date of Patent: May 4, 2010
    Assignee: AstraZeneca AB
    Inventors: Christopher Thomas Halsall, David Alan Rudge, Iain Simpson, Richard Andrew Ward
  • Publication number: 20100056495
    Abstract: Compounds, compositions, and methods of using such compounds to modulate apoptosis including IAP antagonists are provided herein. Compositions including mimetics of the invention and, optionally, secondary agents, may be used to treat proliferative disorders such as, cancer and autoimmune diseases.
    Type: Application
    Filed: July 24, 2007
    Publication date: March 4, 2010
    Applicant: TETRALOGIC PHARMACEUTICALS CORPORATION
    Inventor: Stephen M. Condon
  • Publication number: 20100056778
    Abstract: Process for the optical resolution of the compound of formula (I): by chiral chromatography. Application in the synthesis of ivabradine, of its addition salts with a pharmaceutically acceptable acid and of their hydrates.
    Type: Application
    Filed: August 24, 2009
    Publication date: March 4, 2010
    Inventors: Jean-Michel Lerestif, Jean-Pierre Lecouve, Daniel Dron, Eric Gojon, Maryse Phan
  • Publication number: 20100041640
    Abstract: ?-Crystalline form of ivabradine of formula (I): characterised by its powder X-ray diffraction diagram. Medicinal products containing the same which are useful as bradycardics.
    Type: Application
    Filed: October 21, 2009
    Publication date: February 18, 2010
    Applicant: LES LABORATOIRES SERVIER
    Inventors: Stéphane Horvath, Marie-Noëlle Auguste, Gérard Damien
  • Publication number: 20100009965
    Abstract: This invention relates to novel cyclic malonamides having the formula (I): to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of A?-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to ?-amyloid production such as Alzheimer's disease and Down's Syndrome.
    Type: Application
    Filed: September 2, 2009
    Publication date: January 14, 2010
    Applicant: BRISTOL-MYERS SQIBB PHARMA COMPANY
    Inventors: Richard E. Olson, Michael G. Yang
  • Publication number: 20100009966
    Abstract: This invention relates to novel lactams of Formula (I): having drug and bio-affecting properties, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of A?-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to ?-amyloid production such as Alzheimer's disease and Down's Syndrome.
    Type: Application
    Filed: September 15, 2009
    Publication date: January 14, 2010
    Applicant: BRISTOL-MYERS SQUIBB PHARMA COMPANY
    Inventors: Qi HAN, Hong Liu, Richard E. Olson, Michael G. Yang
  • Publication number: 20090318420
    Abstract: A ?d-Crystalline form of ivabradine hydrochloride of formula (I): characterised by its powder X-ray diffraction data. Medicinal products containing the same which are useful as bradycardics.
    Type: Application
    Filed: August 27, 2009
    Publication date: December 24, 2009
    Applicant: LES LABORATOIRES SERVIER
    Inventors: Stéphane Horvath, Marie-Noëlle Auguste, Gérard Damien
  • Publication number: 20090318682
    Abstract: Process for the synthesis of the compound of formula (I): Application in the synthesis of ivabradine, addition salts thereof with a pharmaceutically acceptable acid and hydrates thereof.
    Type: Application
    Filed: June 17, 2009
    Publication date: December 24, 2009
    Applicant: LES LABORATOIRES SERVIER
    Inventors: Jean-Michel Lerestif, Jean-Pierre Lecouve, Daniel Brigot
  • Publication number: 20090318419
    Abstract: A ?-crystalline form of ivabradine hydrochloride of formula (I): characterised by its powder X-ray diffraction data. Medicinal products containing the same which are useful as bradycardics.
    Type: Application
    Filed: August 27, 2009
    Publication date: December 24, 2009
    Applicant: LES LABORATOIRES SERVIER
    Inventors: Stéphane Horvath, Marie-Noëlle Auguste, Gérard Damien
  • Publication number: 20090318418
    Abstract: A ?d-crystalline form of ivabradine hydrochloride of formula (I): characterised by its powder X-ray diffraction data. Medicinal products containing the same which are useful as bradycardics.
    Type: Application
    Filed: August 27, 2009
    Publication date: December 24, 2009
    Applicant: LES LABORATOIRES SERVIER
    Inventor: Stephane Horvath
  • Publication number: 20090318417
    Abstract: A ?-Crystalline form of ivabradine hydrochloride of formula (I): characterised by its powder X-ray diffraction data. Medicinal products containing the same which are useful as bradycardics.
    Type: Application
    Filed: August 27, 2009
    Publication date: December 24, 2009
    Applicant: LES LABORATOIRES SERVIER
    Inventors: Stephane Horvath, Marie-Noelle Auguste, Gerard Damien
  • Publication number: 20090318416
    Abstract: A ?d-Crystalline form of ivabradine hydrochloride of formula (I): characterised by its powder X-ray diffraction data. Medicinal products containing the same which are useful as bradycardics.
    Type: Application
    Filed: August 27, 2009
    Publication date: December 24, 2009
    Applicant: LES LABORATOIRES SERVIER
    Inventors: Stéphane Horvath, Marie-Noëlle Auguste, Gérard Damien
  • Publication number: 20090306369
    Abstract: This invention provides a process for preparing benzazepine compounds of the formula (1): wherein X1 is a halogen atom, R1 and R2 are a lower alkyl group, or salts thereof as well as intermediate benzoic acid compounds in high yield and high purity on industrial scale, which are useful as an intermediate for preparing a pharmaceutically active 2,3,4,5-tetrahydro-1H-1-benzazepine compound having vasopressin antagonistic activity.
    Type: Application
    Filed: September 1, 2006
    Publication date: December 10, 2009
    Inventors: Yasuhiro Torisawa, Kaoru Abe, Yasuaki Muguruma, Shigekazu Fujita, Hidenori Ogawa, Naoto Utsumi, Masahiro Miyake
  • Publication number: 20090264404
    Abstract: A heterocyclic compound or a salt thereof represented by the formula (1): where R2 represents a hydrogen atom or a lower alkyl group; A represents a lower alkylene group or lower alkenylene group; and R1 represents an aromatic group or a heterocyclic group. The compound of the present invention has a wide treatment spectrum for mental disorders including central nervous system disorders, no side effects and high safety.
    Type: Application
    Filed: August 31, 2006
    Publication date: October 22, 2009
    Inventors: Hiroshi Yamashita, Hideaki Kuroda, Nobuaki Ito, Shin Miyamura, Kunio Oshima, Jun Matsubara, Haruka Takahashi, Tae Fukushima, Satoshi Shimizu, Kazumi Kondo, Yohji Sakurai, Takeshi Kuroda, Shinichi Taira, Motohiro Itotani, Tatsuyoshi Tanaka
  • Patent number: 7598237
    Abstract: This invention provides progesterone receptor modulators having the structure: wherein R1 to R7, X, and Q are as defined in the specification; or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: November 28, 2007
    Date of Patent: October 6, 2009
    Assignee: Wyeth
    Inventors: Puwen Zhang, Jay Edward Wrobel, Eugene Anthony Terefenko, Jeffrey Curtis Kern
  • Publication number: 20090209473
    Abstract: Angiogenesis may be initiated or increased through the use of gamma-secretase inhibitors. The gamma-secretase inhibitor can be a dipeptide class, sulfonamide class, transition state mimic class, benzodiazepine class, or benzocaprolactam class gamma secretase inhibitor. Methods for initiating and increasing angiogenesis are used for disease prevention and treatment as well as for generating research models.
    Type: Application
    Filed: February 19, 2009
    Publication date: August 20, 2009
    Inventors: Mats Hellstrom, Linda Karlsson-Lindahl, Elisabet Wallgard
  • Publication number: 20090181945
    Abstract: The present invention relates to a novel two cyclic cinnamide compound and a pharmaceutical agent comprising the compound as an active ingredient. The two cyclic cinnamide compound represented by the general formula (I): wherein represents a single bond or a double bond; Ar1 represents a phenyl group or pyridinyl group that may be substituted with 1 to 3 substituents; R1 and R2 each represent a C1-6 alkyl group, a hydroxyl group, or the like; Z1 represents a methylene group or vinylene group, which may be substituted with 1 or 2 substituents selected from Substituent Group A1, an oxygen atom, or an imino group that may be substituted with a substituent selected from Substituent Group A1; and p, q, and r each represent an integer of 0 to 2, which has an effect of reducing A?40 and A?42 production, and thus is particularly useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by A? such as Alzheimer's disease or Down's syndrome.
    Type: Application
    Filed: March 13, 2009
    Publication date: July 16, 2009
    Inventors: Teiji Kimura, Koki Kawano, Eriko Doi, Noritaka Kitazawa, Mamoru Takaishi, Koichi Ito, Toshihiko Kaneko, Takeo Sasaki, Takehiko Miyagawa, Hiroaki Hagiwara, Yu Yoshida
  • Publication number: 20090181928
    Abstract: Compounds of the formula are inhibitors of protein tyrosine phosphatases (PTPases) and, thus, may be employed for the treatment of conditions mediated by PTPase activity. The compounds of the present invention may also be employed as inhibitors of other enzymes characterized with a phosphotyrosine binding region such as the SH2 domain. Accordingly, the compounds of formula (I) may be employed for prevention and/or treatment of insulin resistance associated with obesity, glucose intolerance, diabetes mellitus, hypertension and ischemic diseases of the large and small blood vessels, conditions that accompany type-2 diabetes, including hyperlipidemia, hypertriglyceridemia, atherosclerosis, vascular restenosis, irritable bowel syndrome, pancreatitis, adipose cell tumors and carcinomas such as liposarcoma, dyslipidemia, and other disorders where insulin resistance is indicated.
    Type: Application
    Filed: March 29, 2007
    Publication date: July 16, 2009
    Inventors: Alan Neubert, David Barnes, Young-Shin Kwak, Katsumasa Nakajima, Gregory Raymond Bebernitz, Gary Mark Coppola, Louise Kirman, Michael H. Serrano-Wu, Travis Stams, Sidney Wolf Topiol, Thalaththani Ralalage Vedananda, James Richard Wareing
  • Publication number: 20090181946
    Abstract: Benzazepinone compounds represented by Formula (I), or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, sodium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, epilepsy, irritable bowel syndrome, urinary incontinence, pruritis, itchiness, allergic dermatitis, depression, anxiety, multiple sclerosis, and bipolar disorder, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds.
    Type: Application
    Filed: June 5, 2007
    Publication date: July 16, 2009
    Inventors: Scott B. Hoyt, Clare London, Dong Ok, William H. Parsons
  • Publication number: 20090170831
    Abstract: Field of the Invention This invention relates to novel lactams of Formula (I): having drug and bio-affecting properties, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of A?-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to ?-amyloid production such as Alzheimer's disease and Down's Syndrome.
    Type: Application
    Filed: February 19, 2009
    Publication date: July 2, 2009
    Applicant: BRISTOL-MYERS SQUIBB PHARMA COMPANY
    Inventors: Qi Han, Hong Liu, Richard E. Olson, Michael G. Yang
  • Publication number: 20090162420
    Abstract: The invention relates to a salt of an ACE inhibitor dicarboxylic acid with an organic amine and/or an alkali compound, a transdermal therapeutic system comprising the salt, and a method of producing the transdermal therapeutic system.
    Type: Application
    Filed: December 5, 2006
    Publication date: June 25, 2009
    Inventors: Karin Klokkers, Michael Helfrich, Jörg Nink
  • Patent number: 7550453
    Abstract: The invention relates particularly to 2-alkoxy-3,4,5-trihydroxy-alkylamides, preparation thereof, compositions containing them and use thereof as a medicament, particularly as anti-cancer agents.
    Type: Grant
    Filed: May 24, 2007
    Date of Patent: June 23, 2009
    Assignee: Aventis Pharma SA
    Inventors: Jidong Zhang, Neerja Bhatnagar, Jean-Marie Ruxer
  • Patent number: 7544680
    Abstract: The invention encompasses constrained bicyclic and tricyclic CGRP-receptor antagonists, methods for identifying them, pharmaceutical compositions comprising them, and methods for their use in therapy for treatment of migraine and other headaches, neurogenic vasodilation, neurogenic inflammation, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), and other conditions the treatment of which can be effected by the antagonism of CGRP-receptors.
    Type: Grant
    Filed: April 18, 2008
    Date of Patent: June 9, 2009
    Assignee: Bristol-Myers Squibb Company
    Inventors: Prasad V. Chaturvedula, Stephen E. Mercer, Haiquan Fang
  • Publication number: 20090099152
    Abstract: The present invention relates to 2-alkoxy-3,4,5-trihydroxyalkylamide benzodiazepine compounds, to pharmaceutical compositions comprising such compounds, to methods of treatment comprising administering such compounds, to processes for the preparation of such compounds, and to intermediate precursors to such compounds.
    Type: Application
    Filed: November 10, 2008
    Publication date: April 16, 2009
    Applicant: SANOFI-AVENTIS
    Inventors: Jidong ZHANG, Frederico NARDI, Alain COMMERCON
  • Publication number: 20090082559
    Abstract: An improved process for the crystallization of benazepril hydrochloride to obtain in at least 99.8% diastereomeric purity. The process comprises making a concentrated solution of benazepril hydrochloride in ethanol and adding the resulting solution to a non-solvent diisopropyl ether.
    Type: Application
    Filed: May 9, 2006
    Publication date: March 26, 2009
    Applicant: Lupin Limited
    Inventors: Girij Pal Singh, Vilas Nathu Dhake, Sureshbabu Venkata Chillara, Himanshu Madhav Godbole
  • Publication number: 20090062256
    Abstract: This invention relates to novel lactams having the Formula (I): to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of A?-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to ?-amyloid production such as Alzheimer's disease and Down's Syndrome.
    Type: Application
    Filed: October 24, 2008
    Publication date: March 5, 2009
    Applicant: BRISTOL-MYERS SQUIBB PHARMA COMPANY
    Inventor: Richard E. Olson
  • Patent number: 7476675
    Abstract: The invention provides compounds of the formula: and pharmaceutically acceptable salts or prodrugs thereof, wherein m, p, q, r, A, E, X, Y, R1, R4, R5, R6, R7, R8, R9 and are as defined herein. The invention also provides methods for preparing, compositions comprising, and methods for using compounds of formula I.
    Type: Grant
    Filed: July 27, 2005
    Date of Patent: January 13, 2009
    Assignee: Roche Palo Alto LLC
    Inventors: David Bruce Repke, Russell Stephen Stabler, Ralph New Harris, III
  • Patent number: 7468365
    Abstract: The present invention provides crystalline (N)-((S)-2-hydroxy-3-methyl-butyryl)-1-(L-alaninyl)-(S)-1-amino-3-methyl-2,3,4,5-tetrahydro-1H-3-benzazepin-2-one, a crystalline anydrate and dihydrates thereof, compositions comprising (N)-((S)-2-hydroxy-3-methyl-butyryl)-1-(L-alaninyl)-(S)-1-amino-3-methyl-2,3,4,5-tetrahydro-1H-3-benzazepin-2-one, its crystalline anhydrate or dihydrate, and methods for using the same.
    Type: Grant
    Filed: January 11, 2006
    Date of Patent: December 23, 2008
    Assignees: Eli Lilly and Company, Elan
    Inventors: James Edmund Audia, Benjamin Alan Diseroad, Varghese John, Lee H. Latimer, Jeffrey Scott Nissen, Gregory Alan Stephenson, Eugene D. Thorsett, Jay S. Tung
  • Publication number: 20080293678
    Abstract: The invention describes compositions and kits comprising at least qrie organic nitric oxide enhancing salt of an angiotensin converting enzyme inhibitor, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides methods for (a) treating cardiovascular diseases; (b) treating renovascular diseases; (c) treating diabetes; (d) treating diseases resulting from oxidative stress; (e) treating endothelial dysfunctions; (f) treating diseases caused by endothelial dysfunctions; (g) treating cirrhosis; (h) treating pre-eclampsia; Q) treating osteoporosis; (k) treating nephropathy; (l) treating peripheral vascular diseases; (m) treating portal hypertension; (n) treating ophthalmic disorders; (o) treating metabolic syndrome; and (p) treating hyperlipidemia.
    Type: Application
    Filed: March 17, 2006
    Publication date: November 27, 2008
    Applicant: NitroMed, Inc.
    Inventor: David S. Garvey
  • Patent number: 7452875
    Abstract: Compounds having neutral endopeptidase (NEP) and/or human soluble endopeptidase (hSEP) inhibitory activity corresponding to the formula I, wherein the substituents R1, R2, R3 and R4 have the meanings given in the description and also pharmaceutical compositions containing these compounds, in particular pharmaceutical compositions suitable for treating or inhibiting cardiovascular diseases, sexual dysfunction and/or adverse conditions associated with apoptosis.
    Type: Grant
    Filed: August 3, 2007
    Date of Patent: November 18, 2008
    Assignee: Solvay Pharmaceuticals GmbH
    Inventors: Dagmar Hoeltje, Yvan Fischer, Dieter Ziegler, Michael Weske, Katrin Michaelis, Yasmin Karimi-Nejad, Josef Messinger, Axel Pahl, Constanze Hoefer, Hrissanthi Ikonomidou, Lechoslaw Turski