Plural Piperidine Rings Patents (Class 514/316)
  • Pyrrolidine aryl-ether as NK3 receptor antagonists
    Patent number: 7812021
    Abstract: The invention relates to a compound of general formula wherein Ar, R1, R2, R3, R4, n, o, p, s, X and are as defined herein or to a pharmaceutically active salt thereof, including all stereoisomeric forms, individual diastereoisomers and enantiomers of the compound of formula (I) as well as racemic and non-racemic mixtures thereof. The compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).
    Type: Grant
    Filed: August 21, 2008
    Date of Patent: October 12, 2010
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Philippe Jablonski, Kenichi Kawasaki, Henner Knust, Anja Limberg, Matthias Nettekoven, Hasane Ratni, Claus Riemer, Xihan Wu
  • INDOL-3-YL-CARBONYL-PIPERIDIN-BENZOIMIDAZOL DERIVATIVES
    Publication number: 20100256140
    Abstract: The present invention relates to Indol-3-yl-carbonyl-piperidin-benzoimidazol derivatives which act as V1a receptor antagonists and which are represented by Formula I: wherein the residues R1 to R7 are as defined herein. The invention further relates to pharmaceutical compositions containing such compounds, their use in treating dysmenorrhea, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephritic syndrome, obsessive compulsive disorder, anxiety and depressive disorders, and methods of preparation thereof.
    Type: Application
    Filed: June 21, 2010
    Publication date: October 7, 2010
    Inventors: Caterina Bissantz, Christophe Grundschober, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider
  • CRYSTALLINE FORMS OF A BIPHENYL COMPOUND
    Publication number: 20100256185
    Abstract: The invention provides crystalline forms of biphenyl-2-ylcarbamic acid 1-(2-{[4-(4-carbamoylpiperidin-1-ylmethyl)benzoyl]methylamino}ethyl)piperidin-4-yl ester, and pharmaceutically acceptable solvates thereof. The crystalline form can be a freebase, or a salt such as a diphosphate, monosulfate or dioxalate salt. The invention also provides pharmaceutical compositions comprising these crystalline compounds or prepared using these compounds; processes and intermediates for preparing the crystalline compounds; and methods of using these compounds to treat a pulmonary disorder.
    Type: Application
    Filed: June 17, 2010
    Publication date: October 7, 2010
    Applicant: THERAVANCE, INC.
    Inventors: Sabine Axt, Timothy J. Church
  • Azole derivatives and fused bicyclic azole derivatives as therapeutic agents
    Publication number: 20100256119
    Abstract: This invention provides certain compounds, methods of their preparation, pharmaceutical compositions comprising the compounds, and their use in treating human or animal disorders. The compounds of the invention are useful as modulators of the interaction between the receptor for advanced glycated end products (RAGE) and its ligands, such as advanced glycated end products (AGEs), S100/calgranulin/EN-RAGE, ?-amyloid and amphoterin, and for the management, treatment, control, or as an adjunct treatment for diseases in humans caused by RAGE. Such diseases or disease states include acute and chronic inflammation, the development of diabetic late complications such as increased vascular permeability, nephrdpathy, atherosclerosis, and retinopathy, the development of Alzheimer's disease, erectile dysfunction, and tumor invasion and metastasis.
    Type: Application
    Filed: May 5, 2010
    Publication date: October 7, 2010
    Inventors: Adnan M.M. Mjalli, Robert C. Andrews, Ramesh Gopalaswamy, Anitha Hari, Kwasi S. Avor, Ghassan Qabaja, Xiao-Chuan Guo, Suparna Gupta, David R. Jones, Xin Chen
  • PIPERIDINE DERIVATIVES AS NK3 RECEPTOR ANTAGONISTS
    Publication number: 20100256126
    Abstract: The present application relates to compounds of formula wherein the definitions are as described herein. The present compounds are high potential NK-3 receptor antagonists that are useful for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).
    Type: Application
    Filed: March 11, 2010
    Publication date: October 7, 2010
    Inventors: Henner Knust, Anja Limberg, Matthias Nettekoven, Hasane Ratni, Claus Riemer, Walter Vifian
  • Amido Compounds And Their Use As Pharmaceuticals
    Publication number: 20100256114
    Abstract: The present invention relates to inhibitors of 11-? hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-? hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess.
    Type: Application
    Filed: June 17, 2010
    Publication date: October 7, 2010
    Applicant: INCYTE CORPORATION
    Inventors: Wenqing Yao, Jincong Zhuo, Meizhong Xu, Brian W. Metcalf, Chunhong He, Ding-Quan Qian, Colin Zhang
  • Selected CGRP-antagonists, process for preparing them and their use as pharmaceutical compositions
    Publication number: 20100249114
    Abstract: The present invention relates to the CGRP antagonists of general formula wherein A, X, D, E, G, M, Q and R1 to R3 are defined as in claim 1, the tautomers, the isomers, the diastereomers, the enantiomers, the hydrates thereof, the mixtures thereof and the salts thereof and the hydrates of the salts, particularly the physiologically acceptable salts thereof with inorganic or organic acids, pharmaceutical compositions containing these compounds, the use thereof and processes for the preparation thereof.
    Type: Application
    Filed: February 25, 2010
    Publication date: September 30, 2010
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Stephan Georg MUELLER, Klaus RUDOLF, Philipp LUSTENBERGER, Dirk STENKAMP, Alexander DREYER, Kirsten ARNDT, Henri DOODS, Gerhard SCHAENZLE, Marco SANTAGOSTINO, Fabio PALEARI
  • BENZIMIDAZOLE-CARBOXAMIDE COMPOUNDS AS 5-HT4 RECEPTOR AGONISTS
    Publication number: 20100249186
    Abstract: The invention relates to benzimidazole-carboxamide 5-HT4 receptor agonist compounds of formula (I) wherein R1 and X are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The invention also relates to pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HT4 receptor activity, and processes and intermediates useful for preparing such compounds.
    Type: Application
    Filed: June 9, 2010
    Publication date: September 30, 2010
    Inventors: Robert Murray McKinnell, Roland Gendron, Lan Jiang, Seoki-ki Choi, Daniel D. Long, Paul R. Fatheree, Daniel Marquess
  • OXYPIPERIDINE DERIVATIVES AND METHODS OF USE THEREOF
    Publication number: 20100249098
    Abstract: The present invention relates to novel Oxypiperidine Derivatives, pharmaceutical compositions comprising the Oxypiperidine Derivatives and the use of the Oxypiperidine Derivatives for treating or preventing treating allergy, an allergy-induced airway response, congestion, hypotension, a cardiovascular disease, a gastrointestinal disorder, obesity, a sleep disorder, pain, diabetes, a diabetic complication, impaired glucose tolerance, impaired fasting glucose or a central nervous system (CNS) disorder.
    Type: Application
    Filed: September 25, 2008
    Publication date: September 30, 2010
    Inventors: Jianhua Chao, Robert G. Aslanian
  • MULTI-RING COMPOUNDS AND USES THEREOF
    Publication number: 20100249111
    Abstract: Chemical agents, such as derivatives of hydroxy benzene moieties, and similar heterocyclic ring structures, including salts thereof, that act as anti-cancer and anti-tumor agents, especially where such agents modulate the activity of enzymes and structural polypeptides present in cells, such as cancer cells, or where the agents modulate levels of gene expression in cellular systems, including cancer cells, are disclosed, along with methods for preparing such agents, as well as pharmaceutical compositions containing such agents as active ingredients and methods of using these as therapeutic agents.
    Type: Application
    Filed: April 25, 2008
    Publication date: September 30, 2010
    Applicant: AVALON PHARMACEUTICALS
    Inventors: Norman E. Ohler, Jeffrey W. Watthey, Jeffrey Strovel, Sheela K. Chellappan
  • Multimodal Abuse Resistant and Extended Release Opioid Formulations
    Publication number: 20100249045
    Abstract: The present invention is in the field of oral, abuse resistant pharmaceutical compositions of opioid agonists, extended release pharmaceutical compositions of opioid agonists and extended release abuse resistant pharmaceutical compositions of opioid agonists and the use thereof. The present invention is also directed to extended release pharmaceutical compositions and the use thereof for preventing or minimizing the risk of abuse and/or toxicity from either intentional or unintentional tampering. The present invention is further directed at a method of preventing or minimizing the risk of abuse and/or toxicity from either intentional or unintentional tampering.
    Type: Application
    Filed: April 26, 2008
    Publication date: September 30, 2010
    Applicant: THERAQUEST BIOSCIENCES, INC.
    Inventor: Najib Babul
  • ABCG2 INHIBITOR
    Publication number: 20100249089
    Abstract: The present invention relates to a breast cancer resistance protein (BCRP/ABCG2) inhibitor. The invention provides an acrylonitrile derivative represented by formula (1): (wherein A represents an optionally substituted 3- to 8-membered heterocyclic ring) or a salt thereof.
    Type: Application
    Filed: December 2, 2008
    Publication date: September 30, 2010
    Applicant: KABUSHIKI KAISHA YAKULT HONSHA
    Inventors: Ryuta Yamazaki, Hiroshi Hatano, Takashi Yaegashi, Yoshiaki Igarashi, Oh Yoshida, Yoshikazu Sugimoto
  • Biphenyl compounds useful as muscarinic receptor antagonists
    Patent number: 7803812
    Abstract: This invention provides compounds of formula I: wherein a, b, c, d, m, n, p, s, t, W, Ar1, R1, R2, R3, R4, R6, R7, and R8 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.
    Type: Grant
    Filed: May 8, 2009
    Date of Patent: September 28, 2010
    Assignee: Theravance, Inc.
    Inventors: Mathai Mammen, YuHua Ji, YongQi Mu, Craig Husfeld, Li Li
  • WATER-SOLUBLE THALIDOMIDE DERIVATIVES
    Publication number: 20100240651
    Abstract: A compound of formula (I), wherein R1 represents H, or a C1-4 alkyl group; R2 represents H, a C1-4 alkyl group, C(O)CHR4NR5R6, or C(O)W; or R1 and R2 taken together represent 1,3-propylene; R3 represents H, a C1-4 alkyl group, C(O)CHR4NR5R6, or C(O)W; or R2 and R3 taken together represent 1,3-propylene, 1,4-butylene, 1,5-pentylene, 1,6-hexylene, CH2OCH2, CH2SCH2 or CH2NR7CH2, wherein R7 represents H or a C1-4 alkyl group; and when one of R2 and R3 represents H, or a C1-4 alkyl group, the other one does not represent H; and R8 represents H, or a C1-4 alkyl group.
    Type: Application
    Filed: June 4, 2010
    Publication date: September 23, 2010
    Inventor: Hesheng ZHANG
  • COMPOUNDS AND COMPOSITIONS AS CHANNEL ACTIVATING PROTEASE INHIBITORS
    Publication number: 20100239551
    Abstract: The invention provides compounds and pharmaceutical compositions thereof, which are useful for modulating chan-nel activating proteases, and methods for using such compounds to treat, ameliorate or prevent a condition associated with a channel activating protease, including but not limited to prostasin, PRSS22, TMPRSS11 (e.g., TMPRSS11B, TMPRSSI1E), TMPRSS2, TMPRSS3, TMPRSS4 (MTSP-2), matriptase (MTSP-1), CAP2, CAP3, trypsin, cathepsin A, or neutrophil elastase.
    Type: Application
    Filed: January 4, 2008
    Publication date: September 23, 2010
    Applicant: IRM LLC
    Inventors: David C. Tully, Arnab K. Chatterjee, Agnes Vidal, Badry Bursulaya
  • NOVEL BENZIMIDAZOLE DERIVATIVES
    Publication number: 20100233122
    Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
    Type: Application
    Filed: March 1, 2010
    Publication date: September 16, 2010
    Inventors: Yao-Ling Qiu, Ce Wang, Xiaowen Peng, Lu Ying, Yat Sun Or
  • FATTY-ACID BASED PARTICLES
    Publication number: 20100233232
    Abstract: The present invention is directed toward fatty acid-based particles, and methods of making such particles. The particles can be associated with an additional, therapeutic agent. Also provided herein is a method of forming fatty acid particles, comprising associating a cross-linked, fatty acid-derived biomaterial with a cryogenic liquid; and fragmenting the bio material/cryogenic liquid composition, such that fatty acid particles are formed. The particles can be used for a variety of therapeutic applications.
    Type: Application
    Filed: March 10, 2009
    Publication date: September 16, 2010
    Inventors: Thomas M. SWANICK, Joseph FERRARO, Lisa ROGERS, Paul MARTAKOS
  • LINKED DIIMIDAZOLE DERIVATIVES
    Publication number: 20100226883
    Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
    Type: Application
    Filed: February 17, 2010
    Publication date: September 9, 2010
    Inventors: Yao-Ling Qiu, Lu Ying, Ce Wang, Xiaowen Peng, Yat Sun Or
  • LINKED DIIMIDAZOLE ANTIVIRALS
    Publication number: 20100226882
    Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
    Type: Application
    Filed: February 17, 2010
    Publication date: September 9, 2010
    Inventors: Yat Sun Or, Xiaowen Peng, Ce Wang, Lu Ying, Datong Tang, Yao-Ling Qiu
  • Compounds comprising an oxazole or thiazole moiety, processes for making them, and their uses
    Patent number: 7790720
    Abstract: The present invention relates to compounds comprising an oxazole or thiazole moiety of formula (I), processes for preparing them, pharmaceutical compositions comprising said compounds and their uses as H3-receptor ligands, Formula (I), wherein, A1 is CH, C(alkyl), C-halogen or N; R1 is hydrogen, halogen, C1-6 alkyl or alkoxy; R2 is, Formula (II?), A3 is O or S; R3 is hydrogen, halogen, C1-6 alkyl or alkoxy; R4 is hydrogen, halogen, C1-6 alkyl, alkoxy or —O-L; R5 is hydrogen or —O-L, wherein L is an aminoalkyl group and at least one of R4 and R5 should be —O-L.
    Type: Grant
    Filed: March 28, 2006
    Date of Patent: September 7, 2010
    Assignee: UCB Pharma, S.A.
    Inventors: Sylvain Celanire, Frederic Denonne
  • PIPERIDINE DERIVATIVES AS MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY
    Publication number: 20100222366
    Abstract: The present application describes modulators of MIP-1 of formula (I): or stereoisomers or pharmaceutically acceptable salts thereof, wherein m, Q, T, W, Z, R1, R3, R4, R5, R5a and R5b, are as set forth above. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis using the modulators are disclosed.
    Type: Application
    Filed: July 23, 2008
    Publication date: September 2, 2010
    Inventors: Joseph B. Santella, John Hynes, Daniel S. Gardner
  • HEPATITIS C VIRUS INHIBITORS
    Publication number: 20100221216
    Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
    Type: Application
    Filed: February 17, 2010
    Publication date: September 2, 2010
    Inventors: Yat Sun Or, Datong Tang
  • 3-Fluoro-Piperidine T-Type Calcium Channel Antagonists
    Publication number: 20100222387
    Abstract: The present invention is directed to 3-fluoro-piperidine compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which T-type calcium channels are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels are involved.
    Type: Application
    Filed: June 21, 2006
    Publication date: September 2, 2010
    Inventors: James C. Barrow, Craig W. Lindsley, William D. Shipe, Zhi-Qiang Yang
  • LINKED DIBENZIMIDAZOLE DERIVATIVES
    Publication number: 20100221214
    Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
    Type: Application
    Filed: February 9, 2010
    Publication date: September 2, 2010
    Inventors: Yat Sun Or, Ce Wang, Xiaowen Peng, Lu Ying, Yao-Ling Qiu
  • Indol-3-y-carbonyl-piperidin and piperazin-derivatives
    Patent number: 7781436
    Abstract: The present invention relates to indol-3-yl-carbonyl-piperidin and piperazin derivatives which act as V1a receptor antagonists and which are represented by Formula I: wherein the residues R1 to R3 are as defined herein. The invention also relates to pharmaceutical compositions containing such compounds, and methods for preparation of the compounds and compositions. The invention further relates to methods for treating dysmenorrhea, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, obsessive compulsive disorder, anxiety and depressive disorders.
    Type: Grant
    Filed: July 25, 2006
    Date of Patent: August 24, 2010
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Caterina Bissantz, Christophe Grundschober, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider
  • Substituted 2-phenylbenzimidazoles, the production thereof and their use
    Patent number: 7781596
    Abstract: The invention relates to novel 2-phenylbenzimidazoles of general formula (I) or (II), wherein the radicals have the meanings cited in the description, and to their tautomeric forms, possible enantiomeric and diastereomeric forms, to their prodrugs, and to possible physiologically compatible salts. The invention also relates to the production of said compounds and to their use.
    Type: Grant
    Filed: October 28, 1999
    Date of Patent: August 24, 2010
    Assignee: Abbott Laboratories
    Inventors: Wilfried Lubisch, Michael Kock, Thomas Höger
  • CARBOXAMIDE COMPOUNDS AND THEIR USE
    Publication number: 20100210633
    Abstract: Chemokine receptor antagonists, in particular, compounds of Formula (I) that act as antagonists of the chemokine CCR2 receptor, including pharmaceutical compositions and uses thereof to treat or prevent diseases associated with monocyte accumulation, lymphocyte accumulation or leukocyte accumulation are described herein.
    Type: Application
    Filed: October 12, 2007
    Publication date: August 19, 2010
    Applicant: EPIX Delaware, Inc.
    Inventors: Jian Lin, Dongli Chen, Steffi Koerner, Rosa E. Melendez, Pradyumma Mohanty, Efrat Ben-Zeev, Merav Fichman, Yael Marantz, Oren Becker, Dilara McCauley, Pini Orbach, Ashis K. Saha, Sharon Shacham, Michael Xie
  • ISOINDOLINE COMPOUNDS AND METHODS OF THEIR USE
    Publication number: 20100204227
    Abstract: Provided herein are isoindoline compounds, pharmaceutical compositions comprising one or more of such compounds, and methods of their use for treating, preventing, or managing various diseases.
    Type: Application
    Filed: October 29, 2009
    Publication date: August 12, 2010
    Inventors: George W. MULLER, Alexander L. Ruchelman
  • Heterocyclic substituted carbonyl derivatives and their use as dopamine Dreceptor ligands
    Patent number: 7772252
    Abstract: The invention relates to heterocyclic substituted carbonyl derivatives that display selective binding to dopamine D3 receptors. In another aspect, the invention relates to a method for treating central nervous system disorders associated with the dopamine D3 receptor activity in a patient in need of such treatment comprising administering to the subject a therapeutically effective amount of said compounds for alleviation of such disorder. The central nervous system disorders that may be treated with these compounds include Psychotic Disorders, Substance Dependence, Substance Abuse, Dyskinetic Disorders (e.g. Parkinson's Disease, Parkinsonism, Neuroleptic-Induced Tardive Dyskinesia, Gilles de la Tourette Syndrome and Huntington's Disease), Dementia, Anxiety Disorders, Sleep Disorders, Circadian Rhythm Disorders and Mood Disorders.
    Type: Grant
    Filed: April 17, 2009
    Date of Patent: August 10, 2010
    Assignee: Aventis Pharmaceuticals Inc.
    Inventors: James Hendrix, Horst Hemmerle, Matthias Urmann, Gregory M Shutske, Joseph T Strupczewski, Kenneth J Bordeau, John G Jurcak, Thaddeus Nieduzak, Sharon A. Jackson, Paul Angell, James P Carey, George Lee, David Fink, Jean-Francois Sabuco, Yulin Chiang, Nicola Collar
  • N-sulphonylated amino acid derivatives, method for the production and use thereof
    Patent number: 7772251
    Abstract: The present invention relates to N-sulfonylated amino acid derivatives, where an aryl radical is linked via the sulfonyl group N-terminally to the amino acid and a radical which comprises at least one imino group and at least one further basic group which represents an optionally modified amino, amidino or guanidino group is linked C-terminally via the carbonyl group. The invention likewise relates to processes for preparing these compounds and to their use, in particular as inhibitors of matriptase.
    Type: Grant
    Filed: May 17, 2004
    Date of Patent: August 10, 2010
    Assignee: The Medicines Company (Leipzig) GmbH
    Inventors: Jörg Stürzebecher, Torsten Steinmetzer, Andrea Schweinitz, Anne Stürzebecher, Kerstin Uhland
  • Repaglinide Substantially Free of Dimer Impurity
    Publication number: 20100197732
    Abstract: The present invention provides highly pure repaglinide substantially free of dimer impurity, and process for the preparation thereof. The present invention also relates to 2-ethoxy-N-[(1S)-3-methyl-1-[2-(1-piperidinyl)phenyl]butyl]-4-[2-[[(1S)-3-methyl-1-[2-(1-piperidinyl)phenyl]butyl]amino]-2-oxoethyl]benzamide, an impurity of repaglinide, and a process for preparing and isolating thereof. The present invention further relates to pharmaceutical compositions comprising solid particles of pure repaglinide substantially free of dimer impurity or pharmaceutically acceptable salts thereof, wherein 90 volume-percent of the particles (D90) have a size of less than about 400 microns. The present invention also provides an optical resolution method of racemic 3-methyl-1-(2-piperidino-phenyl)-1-butylamine and use thereof for the preparation of repaglinide.
    Type: Application
    Filed: June 5, 2008
    Publication date: August 5, 2010
    Applicant: ACTAVIS GROUP PTC EHF
    Inventors: Sonny Sebastian, Sasidhar Venkata Balla, Ramamurthy Katikareddy, Nitin Sharadchandra Pradhan, Jon Valgeirsson
  • NOVEL B1-ANTAGONISTS
    Publication number: 20100197664
    Abstract: Disclosed are compounds of the formula I wherein A, Y, R1, R2, R3, R4 and R5 are defined, suitable for treating diseases and symptoms of diseases caused at least to some extent by stimulation of bradykinin-B1 receptors, the preparation thereof and the use thereof.
    Type: Application
    Filed: July 23, 2008
    Publication date: August 5, 2010
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Iris Kauffmann-Hefner, Angelo Ceci, Henri Doods, Norbert Hauel, Ingo Konetzki, Annette Schuler-Metz, Rainer Walter
  • PIPERIDINE DERIVATIVES AS NK3 RECEPTOR ANTAGONISTS
    Publication number: 20100197697
    Abstract: The present invention relates to a compounds of formula I wherein A, Ar1, Ar2, R1, R2, R3, R4, R5, R6, m, n, o, p, s, t, and u are as defined herein or to a pharmaceutically active salt, a racemic mixture, an enantiomer, an optical isomer or a tautomeric form thereof. the present compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).
    Type: Application
    Filed: January 25, 2010
    Publication date: August 5, 2010
    Inventors: Henner Knust, Matthias Nettekoven, Hasane Ratni, Claus Riemer, Walter Vifian
  • NOVEL BENZENESULFONAMIDES AS CALCIUM CHANNEL BLOCKERS
    Publication number: 20100197693
    Abstract: The present application relates to calcium channel inhibitors comprising compounds of formula (I), formula (II), formula (III), or formula (IV), wherein L1, R1, R2, R3, R4, R5, R6, R7 and Rc are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.
    Type: Application
    Filed: January 14, 2010
    Publication date: August 5, 2010
    Applicant: ABBOTT LABORATORIES
    Inventors: Qingwei Zhang, Andrew O. Stewart, Zhiren Xia
  • NK 1 ANTAGONISTS
    Publication number: 20100190759
    Abstract: A compound having the general structure shown in Formula I: or pharmaceutically acceptable salts and/or solvates thereof are useful in treating diseases or conditions mediated by NK1 receptors, for example various physiological disorders, symptoms or diseases, including emesis, depression, anxiety and cough.
    Type: Application
    Filed: March 30, 2010
    Publication date: July 29, 2010
    Applicant: OPKO Health, Inc.
    Inventors: Anandan PALANI, Xianhai HUANG, Dong XIAO, Sunil PALIWAL, Hon-Chung TSUI, Michelle Laci WROBLESKI, Ashwin U. RAO, Cheng WANG, Sapna S. SHAH, Neng-Yang SHIH
  • RENIN INHIBITORS
    Publication number: 20100184805
    Abstract: Disclosed are aspartic protease inhibitors represented by the following structural formula: and pharmaceutically acceptable salts thereof. These compounds are orally active and bind to aspartic proteases to inhibit their activity. They are useful in the treatment or amelioration of diseases associated with aspartic protease activity. The present invention is also directed to pharmaceutical compositions comprising a compound described herein or enantiomers, diastereomers, or salts thereof and a pharmaceutically acceptable carrier or excipient.
    Type: Application
    Filed: June 20, 2008
    Publication date: July 22, 2010
    Inventors: John J. Baldwin, Salvacion Cacatian, David A. Claremon, Lawrence W. Dillard, Patrick T. Flaherty, Alexey V. Ishchenko, Lanqi Jia, Gerard McGeehan, Robert D. Simpson, Suresh B. Singh, Colin M. Tice, Zhenrong Xu, Jing Yuan, Wei Zhao
  • Benzimidazole-carboxamide compounds as 5-HT, receptor agonists
    Patent number: 7759363
    Abstract: The invention relates to benzimidazole-carboxamide 5-HT4 receptor agonist compounds of formula (I) wherein R1 and X are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The invention also relates to pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HT4 receptor activity, and processes and intermediates useful for preparing such compounds.
    Type: Grant
    Filed: May 24, 2006
    Date of Patent: July 20, 2010
    Assignee: Theravance, Inc.
    Inventors: Robert Murray McKinnell, Roland Gendron, Lan Jiang, Seok-ki Choi, Daniel D. Long, Paul R. Fatheree, Daniel Marquess
  • CYCLIC AMINOALKYLCARBOXAMIDE DERIVATIVE
    Publication number: 20100179118
    Abstract: The present invention relates to a compound represented by the following formula (I), which is useful as an antiallergic agent and/or an anti-inflammatory agent, or a physiologically acceptable salt thereof and the like: wherein R1 and R2 are the same or different and each is an optionally substituted aryl group and the like, R3 is a hydrogen atom, a C1-6 alkyl group and the like, R4 and R5 are the same or different and each is a hydrogen atom, a halogen atom, a hydroxy group, a C1-6 alkyl group and the like, X is a single bond or —C(R6)(R7)—, R6 and R7 are the same or different and each is a hydrogen atom, a halogen atom, an optionally substituted C1-6 alkyl group and the like, or R6 and R7 optionally form, together with the carbon atom bonded thereto, an optionally substituted C3-8 cycloalkyl group and the like, ring group A is an azetidin-1-yl group and the like, m is 0, 1 or 2, and n is 0, 1 or 2.
    Type: Application
    Filed: September 7, 2007
    Publication date: July 15, 2010
    Applicant: DAINIPPON SUMITOMO PHARMA CO., LTD.
    Inventors: Michinori Ozawa, Tomoya Shiro, Takaaki Sumiyoshi, Mari Itoh
  • Diaminoalkane aspartic protease inhibitors
    Patent number: 7754737
    Abstract: Diaminoalkanes of Formula I have now been found which are orally active and bind to aspartic proteases to inhibit their activity. They are useful in the treatment or amelioration of diseases associated with elevated levels of aspartic protease activity. The invention also relates to a method for the use of the compounds of Formula I in ameliorating or treating aspartic protease related disorders in a subject in need thereof comprising administering to said subject an effective amount of a compound of Formula I.
    Type: Grant
    Filed: October 7, 2005
    Date of Patent: July 13, 2010
    Assignee: Vitae Pharmaceuticals, Inc.
    Inventors: John J. Baldwin, David A. Claremon, Colin M. Tice, Salvacion Cacatian, Lawrence W. Dillard, Alexey V. Ishchenko, Jing Yuan, Zhenrong Xu, Gerard McGeehan, Wei Zhao, Robert D. Simpson, Suresh B. Singh, Patrick T. Flaherty, Jean-Pierre Wery
  • DIARYL PIPERIDINE COMPOUNDS AS CALCIUM CHANNEL BLOCKERS
    Publication number: 20100168103
    Abstract: Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted N-type calcium channel activity are disclosed. Specifically, a series of diaryl piperidine compounds are disclosed of the general formula (I) where X is a linker and Y may be C, O, S or N.
    Type: Application
    Filed: September 14, 2007
    Publication date: July 1, 2010
    Applicant: NEUROMED PHARMACEUTICALS LTD.
    Inventors: Hassan Pajouhesh, Yanbing Ding, Hossein Pajouhesh, Richard Holland, Gabriel Hum
  • 1,5-substituted indol-2-yl amide derivatives
    Patent number: 7745479
    Abstract: The present invention relates to compounds of formula I wherein R1 to R4 and G are as defined in the description and claims and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.
    Type: Grant
    Filed: November 27, 2006
    Date of Patent: June 29, 2010
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Matthias Nettekoven, Jean-Marc Plancher, Hans Richter, Olivier Roche, Valerie Runtz-Schmitt, Sven Taylor
  • Acylated Piperidine Derivatives as Melanocortin-4 Receptor Agonists
    Publication number: 20100160306
    Abstract: Certain novel 4 alkyl substituted N acylated piperidine derivatives are ligands of the human melanocortin receptor(s) and, in particular, are selective ligands of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of MC-4R, such as obesity, diabetes, nicotine addiction, alcoholism, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.
    Type: Application
    Filed: September 26, 2006
    Publication date: June 24, 2010
    Inventors: Raman K. Bakshi, Qingmei Hong, Ravi P. Nargund
  • PYRROLIDINONE INHIBITORS OF PDE-4
    Publication number: 20100159034
    Abstract: The present invention relates to new pyrrolidinone inhibitors of PDE-4 activity, pharmaceutical compositions thereof, and methods of use thereof.
    Type: Application
    Filed: December 15, 2009
    Publication date: June 24, 2010
    Applicant: AUSPEX PHARMACEUTICALS, INC.
    Inventors: Thomas G. Gant, Sepehr Sarshar
  • 3-Pyrrolo[b]Cyclohexylene-2-Dihydroindolinone Derivatives and Uses Thereof
    Publication number: 20100160318
    Abstract: 3-pyrrolo[b]cyclohexylene-2-dihydro-indolinone derivatives of formula (I) or their pharmaceutically acceptable salts and uses thereof. The intermediates of formula (II) for preparing the above compounds. The bioassay shows that the above compounds and their pharmaceutically acceptable salts can modulate the activity of protein kinases (PKs), inhibit the activity of tyrosine kinases (PTKs) and inhibit many kinds of tumor cells as well as.
    Type: Application
    Filed: December 3, 2007
    Publication date: June 24, 2010
    Applicant: JIANGSU SIMCERE PHARMACEUTICAL R&D CO., LTD.
    Inventors: Feng Tang, Han Shen, Qiu Jin, Lei Ding, Jie Yang, Xiaojin Yin, Shiyue Lu
  • Novel Heterocyclic Compounds
    Publication number: 20100152188
    Abstract: The present invention relates to novel compounds of the general formula (I), their derivatives, their analogs, their stereoisomers, their pharmaceutically acceptable salts and compositions. The present invention more particularly provides novel heterocyclic compounds of the general formula (I).
    Type: Application
    Filed: August 4, 2006
    Publication date: June 17, 2010
    Inventors: Akella Satya Surya Visweswara Srinivas, Kasinathan Mathiyazhagan, Duddu Savaraiah Sharada, Thanasekaran Ponpandian, Kulasekharan Revathy, Gaddam Om Reddy, Mani Kamarai, Sriram Raiagopal
  • BENZIMIDAZOLE DERIVATIVES AND METHODS OF USE THEREOF
    Publication number: 20100144591
    Abstract: The present invention relates to compounds of formula (I); compositions comprising the compounds, and methods of using the compounds to treat or prevent pain, diabetes, a diabetic complication, impaired glucose tolerance (IGT) or impaired fasting glucose (IGT) in a patient.
    Type: Application
    Filed: February 27, 2008
    Publication date: June 10, 2010
    Inventors: Robert G. Aslanian, Jean E. Lachowicz, Michael Y. Berlin, Joyce J. Hwa
  • New CGRP-antagonists, process for preparing them and their use as pharmaceutical compositions
    Publication number: 20100144716
    Abstract: The present invention relates to the CGRP-antagonists of general formula I wherein R1, R2, R3, R4 and X are defined as in claim 1, the tautomers, the isomers, the diastereomers, the enantiomers, the hydrates, mixtures and salts thereof and the hydrates of the salts, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, as well as those compounds of general formula I in which one or more hydrogen atoms are replaced by deuterium, pharmaceutical compositions containing these compounds, the use thereof and processes for the preparation thereof.
    Type: Application
    Filed: February 18, 2010
    Publication date: June 10, 2010
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Stephan Georg MUELLER, Klaus RUDOLF, Philipp LUSTENBERGER, Dirk STENKAMP, Marco SANTAGOSTINO, Fabio PALEARI, Gerhard SCHAENZLE, Kirsten ARNDT, Henri DOODS
  • BIPHENYL COMPOUNDS USEFUL AS MUSCARINIC RECEPTOR ANTAGONISTS
    Publication number: 20100137325
    Abstract: The invention provides compounds of formula I: wherein a, b, c, d, f, W, Q, Y, R1, R2, and R3 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.
    Type: Application
    Filed: February 3, 2010
    Publication date: June 3, 2010
    Applicant: Theravance, Inc.
    Inventors: Yu-Hua Ji, Craig Husfeld, Mathai Mammen, YongQi Mu, Eric L. Stangeland
  • Renin Inhibitors
    Publication number: 20100130471
    Abstract: Described are compounds which bind to aspartic proteases to inhibit their activity. They are useful in the treatment or amelioration of diseases associated with aspartic protease activity. Also described are methods of use of the compounds described herein in ameliorating or treating aspartic protease related disorders in a subject in need thereof.
    Type: Application
    Filed: April 4, 2008
    Publication date: May 27, 2010
    Inventors: John J. Baldwin, Salvacion Cacatian, David Claremon, Lawrence W. Dillard, Patrick T. Flaherty, Bahman Ghavimi-Alagha, Damiamo Ghirlanda, Xiaoping Hou, Alexey V. Ishebenko, Lara S. Kallander, Beth A. Knapp-Reed, Brian Lawhorn, Qing Lu, Gerard McGeehan, Simon Semus, Robert D. Simpson, Suresh B. Singh, Lamont R. Terrell, Colin Tice, Tritin Tran, Zhenrong Xu, Jing Yuan, Jing Zhang, Wei Zhao
  • 5-amido-indole-2-carboxamide derivatives
    Patent number: 7723325
    Abstract: The present invention relates to compounds of formula I wherein G and R1 to R5 and R12 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.
    Type: Grant
    Filed: June 29, 2009
    Date of Patent: May 25, 2010
    Assignee: Hoffman-La Roche Inc.
    Inventors: Matthias Nettekoven, Jean-Marc Plancher, Hans Richter, Olivier Roche, Sven Taylor