Additional Hetero Ring Containing Patents (Class 546/187)
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Publication number: 20100179118Abstract: 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: ApplicationFiled: September 7, 2007Publication date: July 15, 2010Applicant: DAINIPPON SUMITOMO PHARMA CO., LTD.Inventors: Michinori Ozawa, Tomoya Shiro, Takaaki Sumiyoshi, Mari Itoh
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Patent number: 7745479Abstract: 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: GrantFiled: November 27, 2006Date of Patent: June 29, 2010Assignee: Hoffmann-La Roche Inc.Inventors: Matthias Nettekoven, Jean-Marc Plancher, Hans Richter, Olivier Roche, Valerie Runtz-Schmitt, Sven Taylor
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Publication number: 20100160318Abstract: 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: ApplicationFiled: December 3, 2007Publication date: June 24, 2010Applicant: JIANGSU SIMCERE PHARMACEUTICAL R&D CO., LTD.Inventors: Feng Tang, Han Shen, Qiu Jin, Lei Ding, Jie Yang, Xiaojin Yin, Shiyue Lu
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Publication number: 20100152188Abstract: 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: ApplicationFiled: August 4, 2006Publication date: June 17, 2010Inventors: Akella Satya Surya Visweswara Srinivas, Kasinathan Mathiyazhagan, Duddu Savaraiah Sharada, Thanasekaran Ponpandian, Kulasekharan Revathy, Gaddam Om Reddy, Mani Kamarai, Sriram Raiagopal
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Publication number: 20100144716Abstract: 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: ApplicationFiled: February 18, 2010Publication date: June 10, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Stephan Georg MUELLER, Klaus RUDOLF, Philipp LUSTENBERGER, Dirk STENKAMP, Marco SANTAGOSTINO, Fabio PALEARI, Gerhard SCHAENZLE, Kirsten ARNDT, Henri DOODS
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Publication number: 20100145043Abstract: Disclosed herein are 2,4-disubstituted-5-aminocarbonyl-1,3-thiazole derivatives, a preparation method thereof, and a therapeutic agent for treating inflammatory diseases induced by SPC, which contains the derivative as an active ingredient. The anti-inflammatory effect of the 2,4-disubstituted-5-aminocarbonyl-1,3-thiazole derivatives was analyzed through a test employing human dermal cells and an animal test using mice and, as a result, it was found that the derivatives showed excellent inhibitory activity on SPC receptor compared to thiazole derivatives known in the prior art. Thus, the 2,4-disubstituted-5-aminocarbonyl-1,3-thiazole derivatives or pharmaceutically acceptable salts thereof are useful as active ingredients in therapeutic agents for treating inflammatory diseases, such as inflammation, pruritus and skin infection, which appear in atopic dermatitis and other diseases induced by SPC activity. wherein R1, R2, R3 and R4 are as defined in the specification.Type: ApplicationFiled: September 30, 2009Publication date: June 10, 2010Applicant: KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGYInventors: Young-Dae Gong, Taeho Lee, Moon-Kook Jeon, Heeyeong Cho, Jae Yang Kong, Gildon Choi, Dae Young Jeong, Soon-Hee Hwang
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Publication number: 20100137325Abstract: 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: ApplicationFiled: February 3, 2010Publication date: June 3, 2010Applicant: Theravance, Inc.Inventors: Yu-Hua Ji, Craig Husfeld, Mathai Mammen, YongQi Mu, Eric L. Stangeland
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Patent number: 7723526Abstract: Benzoimidazole compounds, compositions, and methods of using them in leukocyte recruitment inhibition, in modulating H4 receptor, and in treating conditions such as inflammation, H4 receptor-mediated conditions, and related conditions.Type: GrantFiled: August 26, 2008Date of Patent: May 25, 2010Assignee: Janssen Pharmaceutica NVInventors: James P. Edwards, Michael D. Hack, David E. Kindrachuk, Jennifer D. Venable
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Patent number: 7723325Abstract: 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: GrantFiled: June 29, 2009Date of Patent: May 25, 2010Assignee: Hoffman-La Roche Inc.Inventors: Matthias Nettekoven, Jean-Marc Plancher, Hans Richter, Olivier Roche, Sven Taylor
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Patent number: 7723527Abstract: Benzoimidazole compounds, compositions, and methods of using them in leukocyte recruitment inhibition, in modulating H4 receptor, and in treating conditions such as inflammation, H4 receptor-mediated conditions, and related conditions.Type: GrantFiled: August 26, 2008Date of Patent: May 25, 2010Assignee: Janssen Pharmaceutica NVInventors: Kristen L. Arienti, James G. Breitenbucher, Daniel J. Buzard, James P. Edwards, Michael D. Hack, Alice Lee-Dutra
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Publication number: 20100113776Abstract: A novel pyrazole derivative of the following formula having a histamine H3 receptor antagonistic effect: or a pharmaceutically acceptable salt thereof or a pharmaceutical preparation comprising the same as an active ingredient is effective for prevention or treatment of dementia, Alzheimer's disease, attention-deficit hyperactivity disorder, schizophrenia, eating disorders, obesity, diabetes, hyperlipidemia, sleep disorders, narcolepsy, sleep apnea syndrome, circadian rhythm disorder, depression, allergic rhinitis or other diseases.Type: ApplicationFiled: December 14, 2007Publication date: May 6, 2010Applicant: TAISHO PHARMACEUTICAL CO.,LTD.Inventors: Toshio Nakamura, Dai Nozawa, Makoto Tatsuzuki, Hiroahi Ohta, Takeshi Kuwada, Tomoko Ishizaka, Tomoko Tamita, Seiji Masuda
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Publication number: 20100099708Abstract: The present invention relates to 4-[3-(1,1-difluoroethyl)-5-methyl-4H-1,2,4-triazol-4-yl]-1-{(1R,3R)-3-(3,5-difluorophenyl)-1-methyl-3-[1-(methylsulfonyl)?iperidin-4-yl]propyl}piperidine formula (I): or a pharmaceutically acceptable salt thereof, as well as processes for the preparation of this compound and its use in the treatment of CCR5 disease states.Type: ApplicationFiled: December 10, 2007Publication date: April 22, 2010Inventors: Alan Wellington Faull, Steven Swallow
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Patent number: 7700598Abstract: 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: GrantFiled: October 6, 2008Date of Patent: April 20, 2010Assignee: Boehringer Ingelheim International GmbHInventors: Stephan Georg Mueller, Klaus Rudolf, Philipp Lustenberger, Dirk Stenkamp, Alexander Dreyer, Kirsten Arndt, Henri Doods, Gerhard Schaenzle, Marco Santagostino, Fabio Paleari
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Patent number: 7700628Abstract: This application relates to a compound of formula (I) (or a pharmaceutically acceptable salt of the compound or prodrug thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa and/or thrombin, as well as a process for its preparation and intermediates therefor. An example of a compound of formula (I) is (a).Type: GrantFiled: November 10, 2005Date of Patent: April 20, 2010Assignee: Eli Lilly and CompanyInventors: Ankush Baburao Argade, Theodore Goodson, Jr., David Kent Herron, Sajan Joseph, Salvatore Donato Lepore, Angela Lynn Marquart, John Joseph Masters, David Mendel, Leander Merritt, Andrew Michael Ratz, Gerald Floyd Smith, Anne Louise Tebbe, Michael Robert Wiley, Ying Kwong Yee
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Publication number: 20100093795Abstract: The present invention relates to 4-{(1R,3R)-1-(3,5-difluorophenyl)-3-[4-(3-ethyl-5-isopropyl-4H-1,2,4-triazol-4-yl)piperidin-1-yl]butyl}-1-(methylsulfonyl)piperidine formula (I): or a pharmaceutically acceptable salt thereof, as well as to processes for preparing such a compound, to pharmaceutical compositions comprising such a compound and to the use of such a compound in the treatment of CCR5 mediated disease states.Type: ApplicationFiled: December 10, 2007Publication date: April 15, 2010Inventors: Dearg Sutherland Brown, Alan Wellington Faull, Steven Swallow
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Publication number: 20100075960Abstract: The present invention provides bezimidazole thiophene compounds pharmaceutical compositions containing the same, processes for preparing the same and their use as pharmaceutical agents.Type: ApplicationFiled: May 29, 2007Publication date: March 25, 2010Inventors: Kevin Kuntz, Kyle Allen Emmitte, Tara Renae Rheault, Stephon Smith, Keith Hornberger, Hamilton Dickson, Mui Cheung
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Publication number: 20100056514Abstract: Thienopyrazoles, their preparation, pharmaceutical compositions comprising these compounds, and their pharmaceutical uses in the treatment of disease states capable of being modulated by the inhibition of the protein kinases, in particular interleukin-2 inducible tyrosine kinase (ITK).Type: ApplicationFiled: March 26, 2009Publication date: March 4, 2010Applicant: AVENTIS PHARMACEUTICALS INC.Inventors: John Gerard JURCAK, Matthieu BARRAGUE, Timothy Alan GILLESPY, Michael Louis EDWARDS, Kwon Yon MUSICK, Philip Marvin WEINTRAUB, Yan DU, Ramalinga M. DHARANIPRAGADA, Ashfaq Ahmad PARKAR
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Publication number: 20100055090Abstract: The present invention relates to novel Anilinopiperazine Derivatives of formula (I), compositions comprising the Anilinopiperazine Derivatives, and methods for using the Anilinopiperazine Derivatives for treating or preventing a proliferative disorder, an anti-proliferative disorder, inflammation, arthritis, a central nervous system disorder, a cardiovascular disease, alopecia, a neuronal disease, an ischemic injury, a viral disease, a fungal infection, or a disorder related to the activity of a protein kinase.Type: ApplicationFiled: October 29, 2007Publication date: March 4, 2010Inventors: Gerald W. Shipps, JR., Cliff C. Cheng, Xiaohua Huang, Thierry O. Fischmann, Jose S. Duca, Matthew Richards
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Publication number: 20100048583Abstract: The present invention relates to compounds of the general formula (I) and salts and physiologically functional derivatives thereof, wherein R1 is independently hydrogen, alkyl, cycloalkyl, hydroxyalkyl, haloalkyl, haloalkyloxy, aryl, substituted aryl, heteroaryl, substituted heteroaryl, arylalkyl or substituted arylalkyl; R2 is independently —NR3R4, R3 is independently alkyl, cycloalkyl, alkoxy, alkylamine, —OH, —SH, alkylthio, hydroxyalkyl, haloalkyl, haloalkyloxy, aryl or heteroaryl, R4 is independently alkyl, cycloalkyl, alkoxy, alkylamine, alkylthio, hydroxyalkyl, haloalkyl, haloalkyloxy, aryl or heteroaryl; R5 is independently H, COR6, CO2R6, SOR6, SO2R6, SO3R6, alkyl, cycloalkyl, alkoxy, —NH2, alkylamine, —NR7COR6, halogen, —OH, —SH, alkylthio, hydroxyalkyl, haloalkyl, haloalkyloxy, aryl or heteroaryl; R6 is independently H, alkyl, cycloalkyl, —NH2, alkylamine, aryl or heteroaryl; R7 is independently H, alkyl, cycloalkyl, alkoxy, —OH, —SH, alkylthio, hydroxyalkyl, aryl, or heteroaryl; p is 0,Type: ApplicationFiled: August 24, 2009Publication date: February 25, 2010Applicant: 4SC AGInventors: Johann LEBAN, Harald Schmitt, Kristina Wolf, Stefano Pegoraro, Andreas Wuzik
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Publication number: 20100041701Abstract: The invention provides compounds of formula I: wherein a, b, c, d, n, R1, R2, R3, R6, R7, W, and A 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: ApplicationFiled: October 21, 2009Publication date: February 18, 2010Applicant: THERAVANCE, INC.Inventors: Yu-Hua Ji, Craig Husfeld, Li Li, Mathai Mammen, YongQi Mu, Eric L. Stangeland
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Patent number: 7662816Abstract: Disclosed are compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1 is R is —C(O)—N(R27)(R28) or and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are pharmaceutical compositions and methods of treating cognitive or neurodegenerative diseases comprising the compounds of formula I in combination with a ?-secretase inhibitor other than those of formula I, an HMG-CoA reductase inhibitor, a gamma-secretase inhibitor, a non-steroidal anti-inflammatory agent, an N-methyl-D-aspartate receptor antagonist, a cholinesterase inhibitor or an anti-amyloid antibody.Type: GrantFiled: August 4, 2004Date of Patent: February 16, 2010Assignee: Schering CorporationInventors: Jared N. Cumming, Ulrich Iserloh, Andrew Stamford, Corey Strickland, Johannes H. Voigt, Yusheng Wu, Ying Huang, Yan Xia, Samuel Chackalamannil, Tao Guo, Douglas W. Hobbs, Thuy X. H. Le, Jeffrey F. Lowrie, Kurt W. Saionz, Suresh D. Babu
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Publication number: 20100029946Abstract: The invention provides crystalline forms of the novel benzimidazole-carboxamide 5-HT4 receptor agonist compound, 4-(4-{[(2-isopropyl-1H-benzoimidazole-4-carbonyl)amino]methyl}-piperidin-1-ylmethyl)piperidine-1-carboxylic acid methyl ester. The invention also provides pharmaceutical compositions comprising the crystalline compound, methods of using the compound to treat diseases associated with 5-HT4 receptor activity, and processes useful for preparing crystalline forms of the compound.Type: ApplicationFiled: October 13, 2009Publication date: February 4, 2010Applicant: THERAVANCE, INC.Inventors: Sean M. Dalziel, Kirsten M. Phizackerley
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Publication number: 20100029939Abstract: The present invention discloses a novel process to prepare ketone amides, which are useful intermediates for the preparation of antagonists of CCR5 receptor and therefore useful for the treatment of HIV virus infected mammals. It specifically discloses a novel process to synthesize 1-(2,4-dimethylpyrimidine-5-carbonyl)-4-piperidone, 1-[(2,4-dimethyl-3-pyridinyl)carbonyl]-4-piperidone and related compounds. A salient feature of the invention is the use of a three-phase reaction medium with an organic phase and a buffer salt slurry.Type: ApplicationFiled: September 22, 2009Publication date: February 4, 2010Inventors: SHEN-CHUN KUO, David Jieh-Shyh Tsai, Hongbiao Liao
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Publication number: 20100029688Abstract: Bipiperidinyl compounds of the formula I, are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. Pharmaceutically acceptable salts and solvates are included as well. The compounds are useful as agonists of the g-protein coupled receptor GPR-119.Type: ApplicationFiled: December 14, 2007Publication date: February 4, 2010Inventors: Harold B. Wood, Alan D. Adams, Stanley Freeman, Jason W. Szewezyk, Conrad Santini, Yong Huang
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Publication number: 20100022539Abstract: Certain isoxazole compounds are histamine H3 modulators useful in the treatment of histamine H3 receptor mediated diseases.Type: ApplicationFiled: September 15, 2009Publication date: January 28, 2010Inventors: Nicholas I. Carruthers, Chandravadan R. Shah, Devin M. Swanson
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Patent number: 7652142Abstract: In its many embodiments, the present invention provides a novel class of bipiperidinyl compounds as inhibitors of the CCR5 receptors, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with CCR5 using such compounds or pharmaceutical compositions. The invention also relates to the use of a combination of a compound of this invention and one or more antiviral or other agents useful in the treatment of Human Immunodeficiency Virus (HIV). The invention further relates to the use of a compound of this invention, alone or in combination with another agent, in the treatment of solid organ transplant rejection, graft v. host disease, arthritis, rheumatoid arthritis, inflammatory bowel disease, atopic dermatitis, psoriasis, asthma, allergies or multiple sclerosis.Type: GrantFiled: November 1, 2004Date of Patent: January 26, 2010Assignee: Schering CorporationInventors: Michael W. Miller, Jack D. Scott
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Publication number: 20100010007Abstract: Compounds of formula (I): compositions comprising them, processes for preparing them and their use in medical therapy (for example modulating CCR5 receptor activity in a warm blooded animal).Type: ApplicationFiled: September 18, 2009Publication date: January 14, 2010Applicant: AstraZeneca ABInventors: Alan Faull, Howard Tucker
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Publication number: 20090325980Abstract: The present invention is concerned with novel piperidine or piperazine substituted tetrahydro-naphthalene-1-carboxylic acid derivatives having apoB secretion/MTP inhibiting activity and concomitant lipid lowering activity. The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use of said compounds as a medicine for the treatment of atherosclerosis, pancreatitis, obesity, hypertriglyceridemia, hypercholesterolemia, hyperlipidemia, diabetes and type II diabetes.Type: ApplicationFiled: October 22, 2007Publication date: December 31, 2009Inventors: Lieven Meerpoel, Joannes Theodorus Maria Linders, Libuse Jaroskova, Marcel Viellevoye, Leo Jacobus Jozef Backx, Didier Jean-Claude Berthelot, Guuske Frederike Busscher
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Patent number: 7638631Abstract: The present invention relates to novel methylene dipiperidine derivatives having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of neurological and psychiatric disorders.Type: GrantFiled: September 16, 2005Date of Patent: December 29, 2009Assignee: Glaxo Group LimitedInventors: Gordon Bruton, Vicky Johnstone, Barry Sidney Orlek
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Publication number: 20090318668Abstract: This invention relates to novel analogs of the DNA-binding alkylating agent CC-1065 and to their conjugates. Furthermore this invention concerns intermediates for the preparation of said agents and their conjugates. The conjugates are designed to release their (multiple) payload after one or more activation steps and/or at a rate and time span controlled by the conjugate in order to selectively deliver and/or controllably release one or more of said DNA alkylating agents. The agents, conjugates, and intermediates can be used to treat an illness that is characterized by undesired (cell) proliferation. As an example, the agents and the conjugates of this invention may be used to treat a tumor.Type: ApplicationFiled: February 2, 2007Publication date: December 24, 2009Inventors: Patrick Henry Beusker, Franciscus Marinus Hendrikus De Groot, Lutz F. Tietze, Felix Major, Johannes Albertus Frederikus Joosten, Henri Johannes Spijker
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Publication number: 20090318498Abstract: The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R4, R5 and X are as defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is uveitis, including acute, recurring or chronic uveitis. 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: June 19, 2009Publication date: December 24, 2009Inventors: Chaozhong Cai, Zhihua Sui
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Publication number: 20090318467Abstract: The invention is concerned with novel heteroaryl carboxamide derivatives of formula (I), wherein m, X, Y, R1, R2, R3 and R4 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds are antagonists of CCR-2 receptor, CCR-5 receptor and/or CCR-3 receptor and can be used as medicaments.Type: ApplicationFiled: June 15, 2009Publication date: December 24, 2009Inventors: Jean-Michel Adam, Johannes Aebi, Alferd Binggeli, Luke Green, Guido Hartmann, Hans P. Maerki, Patrizio Mattei, Fabienne Ricklin, Olivier Roche
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Patent number: 7635705Abstract: Disclosed are novel compounds of the formula or a pharmaceutically acceptable salt thereof, wherein: M1 and M3 are CH or N; M2 is CH, CF or N; Y is —C(?O)—, —C(?S)—, —(CH2)q—, —C(?NOR7)— or —SO1-2—; Z is a bond or optionally substituted alkylene or alkenylene; R1 is H, or alkyl, cycloalkyl, aryl, heteroaryl, heterocycloalkyl, all optionally substituted, or a group of the formula: where ring A is a heteroaryl ring; R2 is optionally substituted alkyl, alkenyl, aryl, heteroaryl, cycloalkyl or heterocycloalkyl; R3 is H, —C(O)NH2, or alkyl, aryl, cycloalkyl, heterocycloalkyl or heteroaryl, all optionally substituted; and the remaining variables are as defined in the specification; compositions and methods of treating allergy-induced airway responses, congestion, obesity, metabolic syndrome, alcoholic fatty liver disease, hepatic steatosis, nonalcoholic steatohepatitis, cirrhosis, hepatacellular carcinoma and cognition deficit disorders using said compounds, alone or in combination with othType: GrantFiled: June 19, 2006Date of Patent: December 22, 2009Assignee: Schering CorporationInventors: Robert G. Aslanian, Michael Y. Berlin, Christopher W. Boyce, Jianhua Chao, Manuel de Lera Ruiz, Pietro Mangiaracina, Kevin D. McCormick, Stuart B. Rosenblum, Neng-Yang Shih, Daniel M. Solomon, Wing C. Tom, Henry A. Vaccaro, Junying Zheng, Xiaohong Zhu, Mwangi W. Mutahi
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Patent number: 7632949Abstract: The instant invention relates to a process for the preparation of stabilizers for polymers, especially for polyamides, by condensation of isophthalic acic dichloride (IPC) with sterically hindered amines of the type tetraalkylpiperidine. By using organic solvents or mixtures of organic solvents with water and by an optimized combination of temperature and pressure the yield is much higher than by using water alone. The organic load of the waste water could be significantly reduced.Type: GrantFiled: August 15, 2003Date of Patent: December 15, 2009Assignee: Clariant Produkte (Deutschland) GmbHInventor: Mathias Mehrer
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Patent number: 7629338Abstract: Compounds of formula I: (wherein variables A1, A2, A3, A4, m, n, J, Q, R4, Ea, Eb, Ec, R6, R7, Re, Rf, RPG and Y are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. 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 CGRP is involved.Type: GrantFiled: May 7, 2007Date of Patent: December 8, 2009Assignee: Merck & Co., Inc.Inventors: Michael R. Wood, Steven N. Gallicchio, Harold G. Selnick, C. Blair Zartman, Ian M. Bell, Craig A. Stump
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Patent number: 7629339Abstract: Alkoxy indolinone based acid and amide derivatives have enhanced and unexpected drug properties as inhibitors of protein kinases and are useful in treating disorders related to abnormal protein kinase activities such as cancer.Type: GrantFiled: September 21, 2006Date of Patent: December 8, 2009Assignee: The Scripps Research InstituteInventors: Congxin Liang, Yangbo Feng
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Patent number: 7622587Abstract: The invention provides crystalline forms of the novel benzimidazole-carboxamide 5-HT4 receptor agonist compound, 4-(4-{[(2-isopropyl-1H-benzoimidazole-4-carbonyl)amino]methyl}-piperidin-1-ylmethyl)piperidine-1-carboxylic acid methyl ester. The invention also provides pharmaceutical compositions comprising the crystalline compound, methods of using the compound to treat diseases associated with 5-HT4 receptor activity, and processes useful for preparing crystalline forms of the compound.Type: GrantFiled: May 30, 2007Date of Patent: November 24, 2009Assignee: Theravance, Inc.Inventors: Sean M. Dalziel, Kirsten M. Phizackerley
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Patent number: 7622497Abstract: The present invention is directed to novel derivatives of gambogic acid and analogs thereof. The present invention also relates to the discovery that novel derivatives of gambogic acid are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention can be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.Type: GrantFiled: December 17, 2004Date of Patent: November 24, 2009Assignee: Cytovia, Inc.Inventors: Sui Xiong Cai, Songchun Jiang, Han-Zhong Zhang
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Patent number: 7618961Abstract: The present invention relates to compounds with the formula (II) and also to pharmaceutical compositions comprising the compounds, to processes for their preparation, as well as to the use of the compounds in medicine and for the preparation of a medicament which acts on the human 11-?-hydroxysteroid dehydrogenase type 1 enzyme.Type: GrantFiled: May 22, 2001Date of Patent: November 17, 2009Assignee: Biovitrum ABInventors: Tjeerd Barf, Rikard Emond, Guido Kurz, Jerk Vallgårda, Marianne Nilsson
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Publication number: 20090281097Abstract: The object of the present invention is to provide a compound having an ACC inhibitory action, which is useful for the prophylaxis or treatment of obesity, diabetes, hypertension, hyperlipidemia, cardiac failure, diabetic complications, metabolic syndrome, sarcopenia and the like, and has superior properties such as efficacy, duration of activity, specificity, low toxicity and the like.Type: ApplicationFiled: April 13, 2007Publication date: November 12, 2009Applicant: Takeda Pharmaceutical Company LimitedInventors: Kohji Fukatsu, Makoto Kamata, Tohru Yamashita, Satoshi Endo
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Publication number: 20090281116Abstract: The invention relates to compounds having the formula (I): Wherein R1, R2, R3, R4, R5, R6, R7 and R9 and A-R9 are as defined herein. Also disclosed are the preparative methods for the compounds of formula (I) and their use in therapy.Type: ApplicationFiled: May 14, 2009Publication date: November 12, 2009Applicant: SANOFI-AVENTISInventors: Francis Barth, Christian Congy, Laurent Hortala, Murielle Rinaldi-Carmona
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Patent number: 7615555Abstract: Compounds of formula (I): compositions comprising them, processes for preparing them and their use in medical therapy (for example modulating CCR5 receptor activity in a warm blooded animal).Type: GrantFiled: April 20, 2005Date of Patent: November 10, 2009Assignee: AstraZeneca ABInventors: Alan Faull, Howard Tucker
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Publication number: 20090275609Abstract: Disclosed are carboxamide compounds, as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure in which R1, R2, R3, R4, D, J, Z, T, p, q, w and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.Type: ApplicationFiled: April 22, 2009Publication date: November 5, 2009Applicant: RIGEL PHARMACEUTICALS, INC.Inventors: Jiaxin Yu, Hui Hong, Ihab S. Darwish, Xiang Xu, Rajinder Singh
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Publication number: 20090275613Abstract: The present invention discloses novel compounds of Formula I: (I) possessing 11?-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, cognitive disorders, and other conditions associated with 11?-HSD type 1 activity.Type: ApplicationFiled: April 25, 2007Publication date: November 5, 2009Applicant: Eli Lilly and CompanyInventors: Renhua Li, Owen Brendan Wallace, Yanping Xu
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Publication number: 20090270372Abstract: A subject of the present Application is novel derivatives of benzimidazole and imidazopyridine which have a good affinity for certain sub-types of melanocortin receptors, in particular the MC4 receptors. They are particularly useful for treating pathological conditions and diseases in which one or more melanocortin receptors are involved. The invention also relates to pharmaceutical compositions containing said products.Type: ApplicationFiled: January 21, 2009Publication date: October 29, 2009Applicant: Societe de Conseils de Recherches etInventors: Lydie POITOUT, Valerie Brault, Carole Sackur, Roubert Pierre, Pascale Plas
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Publication number: 20090264418Abstract: 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: ApplicationFiled: June 29, 2009Publication date: October 22, 2009Inventors: Matthias Nettekoven, Jean-Marc Plancher, Hans Richter, Olivier Roche, Sven Taylor
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Publication number: 20090264400Abstract: Substituted sulfonamide compounds corresponding to formula I: processes for the preparation thereof, pharmaceutical compositions containing these compounds, and the use of such substituted sulfonamide compounds in pharmaceutical compositions for the treatment and/or inhibition of pain and other conditions at least partly mediated by the bradykinin 1 receptor.Type: ApplicationFiled: April 8, 2009Publication date: October 22, 2009Applicant: Gruenenthal GmbHInventors: Stefan Oberboersch, Melanie Reich, Stefan Schunk, Michael Franz-Martin Engels, Ruth Jostock, Tieno Germann, Jean De Vry, Klaus Schiene, Sabine Hees
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Publication number: 20090264407Abstract: Substituted sulfonamide compounds corresponding to formula I: a process for their preparation, pharmaceutical compositions comprising such compounds, and the use of such substituted sulfonamide compounds in pharmaceutical compositions for the treatment of pain or other disorders or diseases that are mediated at least in part by B1R receptors.Type: ApplicationFiled: April 8, 2009Publication date: October 22, 2009Applicant: GRUENENTHAL GmbHInventors: Stefan OBERBOERSCH, Melanie REICH, Stefan SCHUNK, Michael ENGELS, Ruth JOSTOCK, Tieno GERMANN, Sabine HEES
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Publication number: 20090253656Abstract: The present invention is directed to a breast cancer resistance protein (BCRP/ABCG2) inhibitor. The BCRP inhibitor contains, as an active ingredient, an acrylonitrile derivative represented by formula (1): wherein one of R1 and R2 represents a cyano group and the other represents a hydrogen atom; Ar1 represents a group selected from among the groups represented by formulas (2) to (4): and Ar2 represents an aromatic hydrocarbon group having a condensed ring which may be substituted by a halogen atom, or a group selected from among the groups represented by the following formulas (5) to (15): or a salt thereof.Type: ApplicationFiled: March 29, 2006Publication date: October 8, 2009Applicant: Kabushiki Kaisha Yakult HonshaInventors: Ryuta Yamazaki, Yukiko Nishiyama, Tomio Furuta, Takeshi Matsuzaki, Hiroshi Hatano, Oh Yoshida, Masato Nagaoka, Ritsuo Aiyama, Shusuke Hashimoto, Yoshikazu Sugimoto
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Publication number: 20090247509Abstract: 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: ApplicationFiled: April 17, 2009Publication date: October 1, 2009Applicant: AVENTIS PHARMACEUTICALS INC.Inventors: James A. Hendrix, Horst Hemmerle, Matthias Urmann, Gregory M. Shutske, Joseph T. Strupczewski, Kenneth J. Bordeau, John G. Jurcak, Thaddeus R. Nieduzak, Sharon A. Jackson, Paul Angell, James P. Carey, George Lee, David Fink, Jean-Francois Sabuco, Yulin Chiang, Nicola Collar