Additional Hetero Ring Containing Patents (Class 540/524)
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Patent number: 8247404Abstract: The present invention relates to derivatives of 4-{2-[phenyl-3,6-dihydropyridin-1-yl]-2-oxoalkyl}-1-piperazin-2-one and 4-{2-[phenyl-2,5-dihydropyrrol-1-yl]-2-oxoalkyl}-1-piperazin-2-one having general formula (I): in which A, B, m, R3 and n are as defined herein. The invention also relates to the preparation thereof and to the therapeutic use thereof.Type: GrantFiled: December 13, 2010Date of Patent: August 21, 2012Assignee: SanofiInventors: Marco Baroni, Francoise Bono, Sandrine Delbary-Gossart
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Publication number: 20120208794Abstract: The present invention provides a fused heterocycle derivative having a strong Smo inhibitory activity, and use thereof. Specially, the present invention relates to a compound represented by the formula wherein each symbol is as defined in the specification, or salt thereof, and a medicament containing the compound or a prodrug thereof, which is an Smo inhibitor or an agent for the prophylaxis or treatment of cancer.Type: ApplicationFiled: August 25, 2010Publication date: August 16, 2012Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Satoshi Sasaki, Yuta Tanaka
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Publication number: 20120201816Abstract: The present application describes lactam-containing compounds and derivatives thereof of Formula I: P4—P-M-M4??I or pharmaceutically acceptable salt forms thereof, wherein ring P, if present is a 5-7 membered carbocycle or heterocycle and ring M is a 5-7 membered carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.Type: ApplicationFiled: April 12, 2012Publication date: August 9, 2012Applicant: BRISTOL-MYERS SQUIBB COMPANYInventors: Donald J. P. Pinto, Mimi L. Quan, Michael J. Orwat, Yun-Long Li, Wei Han, Jennifer X. Qiao, Patrick Y. S. Lam, Stephanie L. Koch
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Publication number: 20120171245Abstract: Methods of inhibiting the replication of influenza viruses in a biological sample or patient, of reducing the amount of influenza viruses in a biological sample or patient, and of treating influenza in a patient, comprises administering to said biological sample or patient an effective amount of a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (IA) are as described herein. A compound is represented by Structural Formula (IA) or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (IA) are as described herein. A pharmaceutical composition comprises an effective amount of such a compound or pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, adjuvant or vehicle.Type: ApplicationFiled: December 15, 2011Publication date: July 5, 2012Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Paul S. Charifson, Michael P. Clark, Upul K. Bandarage, Randy S. Bethiel, John J. Court, Hongbo Deng, Ioana Davies, John P. Duffy, Luc J. Farmer, Huai Gao, Wenxin Gu, Dylan H. Jacobs, Joseph M. Kennedy, Mark W. Ledeboer, Brian Ledford, Francois Maltais, Emanuele Perola, Tiansheng Wang, M. Woods Wannamaker, Randal Byrn, Yi Zhou, Chao Lin, Min Jiang, Steven Jones, Ursula A. Germann
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Publication number: 20120157443Abstract: The present invention provides compounds useful as inhibitors of Btk, compositions thereof, and methods of using the same.Type: ApplicationFiled: September 3, 2010Publication date: June 21, 2012Applicants: SUNESIS PHARMACEUTICALS, INC., BIOGEN IDEC MA INC.Inventors: Minna Bui, Patrick Conlon, Julio H. Cuervo, Daniel A. Erlanson, Junfa Fan, Bing Guan, Brian T. Hopkins, Tracy J. Jenkins, Gnanasambandam Kumaravel, Alexey A. Lugovskoy, Doug Marcotte, Noel Powell, Daniel Scott, Laura Silvian, Art Taveras, Deping Wang, Min Zhong
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Patent number: 8203001Abstract: The present invention encompasses compounds of general formula (1) wherein R1, M1, L1 and Q are defined as in claim 1, which are suitable for the treatment of diseases characterized by excessive or anomalous cell proliferation, and the use thereof for preparing a pharmaceutical composition with the above-mentioned properties.Type: GrantFiled: June 13, 2007Date of Patent: June 19, 2012Assignee: Boehringer Ingelheim International GmbHInventors: Ulrich Reiser, Peter Ettmayer, Oliver Kraemer, Peter Sennhenn, Walter Spevak
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Publication number: 20120148514Abstract: Described is a class of symmetrical and asymmetrical N-alkyl lactam ethers. One preferred ether is bis-N-ethyl pyrrolidone ether. Preferred compositions and uses of the ethers are in performance chemicals, personal care, and pharmaceutical fields, where they function a variety of roles, including as a solvent, solubilizer, freezing point depressor, diluent, extracting agent, cleaning agent, degreaser, absorbent and/or dispersion agent.Type: ApplicationFiled: November 15, 2011Publication date: June 14, 2012Applicant: ISP INVESTMENTS INC.Inventors: Osama M. Musa, Kolazi S. Narayanan
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Publication number: 20120142671Abstract: The present invention is directed to compounds of formula I and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of Syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition Syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by Syk kinase activity, such as Non Hodgkin's Lymphoma.Type: ApplicationFiled: November 1, 2011Publication date: June 7, 2012Applicant: Portola Pharmaceuticals, Inc.Inventors: Zhaozhong J. Jia, Yonghong Song, Qing Xu, Brian Kane, Shawn M. Bauer, Anjali Pandey
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Publication number: 20120142673Abstract: There is provided a compound of formula I: or a pharmaceutically acceptable salt thereof. There are also provided processes for the manufacture of a compound of Formula 1, and the use of a compound of Formula 1 as a medicament and in the treatment of cancer.Type: ApplicationFiled: November 30, 2011Publication date: June 7, 2012Applicant: KuDOS PHARMACEUTICALS LIMITEDInventors: Heather Mary Ellen Duggan, Frederic Georges Marie Leroux, Karine Malagu, Niall Morrison Barr Martin, Keith Allan Menear, Graeme Cameron Murray Smith
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Publication number: 20120135977Abstract: The present invention is directed to ether benzotriazole derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors 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 metabotropic glutamate receptors are involved.Type: ApplicationFiled: September 28, 2011Publication date: May 31, 2012Inventors: Douglas C. Beshore, Vadim Dudkin, Robert M. Garbaccio, Adam W. Johnson, Scott D. Kuduk, Jason W. Skudlarek, Cheng Wang, Mark E. Fraley
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Patent number: 8148363Abstract: The present invention relates to novel heterocyclic compounds of Formulae I-III; as disclosed herein or a pharmaceutically acceptable salt, solvate, ester, prodrug or stereoisomer thereof. Also disclosed are pharmaceutical compositions comprising said compounds, and methods for using said compounds for treating or preventing a thromboembolic disorder.Type: GrantFiled: May 18, 2009Date of Patent: April 3, 2012Assignee: Schering CorporationInventors: Martin C. Clasby, William J. Greenlee, Yan Xia, Tin-Yau Chan, Mariappan V. Chelliah, Samuel Chackalamannil, Haiyan Pu, Keith A. Eagen, Henry Vaccaro, Brian A. McKittrick, Liyuan Wang, Xiaobang Gao
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Publication number: 20120040964Abstract: 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: ApplicationFiled: October 24, 2011Publication date: February 16, 2012Applicant: INCYTE CORPORATIONInventors: Wenqing Yao, Meizhong Xu, Colin Zhang, Yanlong Li, Jincong Zhuo, Brian W. Metcalf
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Publication number: 20120028959Abstract: The invention relates to compounds of formula (I) wherein R1, R2, X1, X2, Y, Ra, Rb, Q have the meanings given in claim 1. The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple sclerosis and also in the treatment of cancer disorders.Type: ApplicationFiled: March 26, 2010Publication date: February 2, 2012Applicant: MERCK SERONO S.A.Inventors: Siva Sanjeeva Rao Thunuguntla, Hosahalli Subramanya, Satish Reddy Kunnam, Sekhar Reddy Sanivaru Vijay, Chakrapani Bingi, Raviraj Kusanur, Matthias Schwarz, Michael Arlt
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Publication number: 20110306599Abstract: Provided is an agent for the treatment or prophylaxis of inflammatory diseases, allergic diseases, autoimmune diseases, transplant rejection or the like. A compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, or a solvate thereof: wherein each symbol is as described in the specification.Type: ApplicationFiled: November 24, 2010Publication date: December 15, 2011Applicant: JAPAN TOBACCO INC.Inventors: Teruhiko INOUE, Tetsudo KAYA, Shinichi KIKUCHI, Koji MATSUMURA, Ritsuki MASUO, Motoya SUZUKI, Michihide MAEKAWA
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Publication number: 20110301109Abstract: The present invention relates to a class of phenylpyrimidone compounds, the pharmaceutical composition, the preparation method and the use thereof. More specifically, the present invention relates to a type of phenylpyrimidone compounds of the following formula I, the pharmaceutically acceptable salts or solvates thereof and to the pharmaceutical composition as well as the preparation method of the compounds. The compounds of formula I according to the present invention can effectively inhibit type V phosphodiesterase (PDE5), and thus can be used for the treatment of various vascular disorders, such as male erectile dysfunction, pulmonary hypertension and the like.Type: ApplicationFiled: December 10, 2009Publication date: December 8, 2011Applicants: TOPHARMAN SHANGHAI CO., LTD.Inventors: Zheng Liu, Jianfeng Li, Xiaojun Yang, Zhen Wang, Jinfeng Zhang, Yi Zhu, Guanghui Tian, Qing Jin, Jingkang Shen, Weiliang Zhu, Hualiang Jiang, Jingshan Shen
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Patent number: 8071600Abstract: 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: GrantFiled: August 31, 2006Date of Patent: December 6, 2011Assignee: Otsuka Pharmaceutical Co., Ltd.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
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Patent number: 8039458Abstract: The invention encompasses a series bicyclic pyrimidinone compounds of Formula I which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions and methods for treating those infected with HIV.Type: GrantFiled: October 31, 2006Date of Patent: October 18, 2011Assignee: Bristol-Myers Squibb CompanyInventors: B. Narasimhulu Naidu, Yasutsugu Ueda, John D. Matiskella, Michael A. Walker, Jacques Banville, Francis Beaulieu, Carl Ouellet, Serge Plamondon
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Publication number: 20110245205Abstract: The present invention provides novel pyrimidine amines of formula (I) which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD and rheumatoid arthritis.Type: ApplicationFiled: December 15, 2010Publication date: October 6, 2011Inventors: Michael D. Altman, Brian M. Andresen, Kenneth L. Arrington, Sathesh Bhat, Jason Burch, Kaleen Konrad Childers, Bernard Cote, Maria Emilia Di Francesco, Anthony Donofrio, Kristina Dupont-Gaudet, John Michael Ellis, Christian Fischer, Jean-Francois Fournier, Jacques Yves Gauthier, Jonathan Grimm, Daniel Guay, David Joseph Guerin, Andrew M. Haidle, Solomon Kattar, Sandra Lee Knowles, Chaomin Li, Jongwon Lim, Michelle R. Machacek, Matthew L. Maddess, Alan B. Northrup, Brendan M. O'Boyle, Ryan D. Otte, Alessia Petrocchi, Michael H. Reutershan, Joel S. Robichaud, Eric Romeo, Adam J. Schell, Tony Siu, Kerrie B. Spencer, Brandon M. Taoka, B. Wesley Trotter, Hyun Chong Woo, Hua Zhou
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Publication number: 20110237791Abstract: A 2-pyridone compound represented by the formula [1]: {wherein in the formula [1], the ring represented by A represents a benzene ring or a pyridine ring, X represents any of the structures represented by the formulas [3] shown below: V represents a single bond or a lower alkylene group, and W represents a single bond, an ether bond or a lower alkylene group (wherein the lower alkylene group may contain an ether bond)}, a tautomer or stereoisomer of the compound, a pharmaceutically acceptable salt thereof, or a solvate thereof is a compound that has an excellent GK activating effect and is useful as a pharmaceutical.Type: ApplicationFiled: April 6, 2011Publication date: September 29, 2011Applicants: TAISHO PHARMACEUTICAL CO., LTD, NISSAN CHEMICAL INDUSTRIES, LTD.Inventors: Takanori KAWAGUCHI, Kengo WATATANI, Keiko FUSEGI, Masahiro BOHNO, Hajime ASANUMA, Shoichi KURODA, Yudai IMAI, Tomomichi CHONAN, Nagaaki SATO, Shigeru TOKITA, Shigetada SASAKO, Takumi OKADA, Keishi HAYASHI, Shin ITOH, Noriko SAITO, Rui JIBIKI, Seishi ISHIYAMA, Hirofumi OTA
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Patent number: 8026233Abstract: Compounds of formula (I): in which A, B, X, Ar1, R8 and R4 have any of the meanings given in the specification, are inhibitors of p38 useful in the treatment and prevention of various disorders mediated by p38.Type: GrantFiled: March 27, 2007Date of Patent: September 27, 2011Assignee: Array BioPharma Inc.Inventors: Mark C. Munson, Kevin W. Hunt, Christopher T. Clark, Ganghyeok Kim, Laurence E. Burgess, James P. Rizzi
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Publication number: 20110230468Abstract: Fused heterocylic compounds of the following Formula wherein R1, R2, R5, Z, J1 and J2 are described herein, and analogs thereof are provided which are useful in treating leukocyte activation-associated disorders.Type: ApplicationFiled: June 1, 2011Publication date: September 22, 2011Inventors: Joseph Barbosa, William J. Pitts, Junqing Guo
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Publication number: 20110230467Abstract: [Problem] The present invention provides a 4,6-diaminonicotinamide compound which is useful as an active ingredient of a pharmaceutical composition, in particular, a pharmaceutical composition for treating diseases caused by undesirable and/or abnormal cytokine signal transduction. [Means for Solution] The present inventors have extensively studied compounds having a JAK3 inhibitory action, and as a result, they have found that a 4,6-diaminonicotinamide compound which is the compound of the present invention has an excellent JAK3 inhibitory action and is useful as an agent for preventing or treating diseases caused by undesirable and/or abnormal cytokine signal transduction, thereby completing the present invention.Type: ApplicationFiled: November 20, 2009Publication date: September 22, 2011Applicant: Astellas Pharma Inc.Inventors: Shohei Shirakami, Fumie Takahashi, Yutaka Nakajima, Hirofumi Omura, Naohiro Aoyama, Hiroshi Sasaki, Takeshi Hondo, Hiroaki Tominaga
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Publication number: 20110218187Abstract: The invention relates to compounds of formula wherein the substituents R1, R2 and R4 have the meaning as set forth and explained in the description of the invention, to processes for the preparation of these compounds, pharmaceutical compositions containing same, the use thereof optionally in combination with one or more other pharmaceutically active compounds for the therapy of a disease which responds to an inhibition of protein kinase activity, especially a neoplastic disease, in particular leukaemia, and a method for the treatment of such a disease.Type: ApplicationFiled: May 12, 2011Publication date: September 8, 2011Inventors: Werner BREITENSTEIN, Pascal FURET, Sandra JACOB, Paul William MANLEY
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Publication number: 20110218188Abstract: The present invention relates to phenyl-pyrimidinyl-amino derivatives of formula (I) wherein Q1 and p, Ra to Rc, L1, Y, L2 and Q2 represent various substituents, their process of preparation, preparation intermediate compounds, their use as fungicide active agents, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.Type: ApplicationFiled: November 12, 2009Publication date: September 8, 2011Inventors: Christian Beier, Jurgen Benting, Isabelle Christian, Pierre-Yves Coqueron, Peter Dahmen, Ralf Dunkel, Jorg Greul, Marie-Claire Grosjean-Cournoyer, Hiroyuki Hadano, Philippe Rinolfi, Arnd Voerste, Jean-Pierre Vors, Ulrike Wachendorff-Neumann
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Publication number: 20110212941Abstract: The present invention is directed to imidazoisoindole compounds which are antagonists of neuropeptide S receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which the neuropeptide S receptor is 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 the neuropeptide S receptor is involved.Type: ApplicationFiled: November 3, 2009Publication date: September 1, 2011Inventors: Peter J. Manley, Kausik K. Nanda, B. Wesley Trotter
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Publication number: 20110212930Abstract: The present application describes lactam-containing compounds and derivatives thereof of Formula I: P4—P-M-M4??I or pharmaceutically acceptable salt forms thereof, wherein ring P, if present is a 5-7 membered carbocycle or heterocycle and ring M is a 5-7 membered carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.Type: ApplicationFiled: May 5, 2011Publication date: September 1, 2011Applicant: BRISTOL-MYERS SQUIBB COMPANYInventors: Donald J.P. Pinto, Mimi L. Quan, Michael J. Orwat, Yun-Long Li, Wei Han, Jennifer X. Qiao, Patrick Y.S. Lam, Stephanie L. Koch
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Publication number: 20110212920Abstract: Disclosed are N-substituted benzenesulfonamides for use in treating or preventing cognitive disorders, such as Alzheimer's Disease. In Formula (I), R1, R2, R3, R4, R3?, R10 and R11 are as described herein. The invention also encompasses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of treating cognitive disorders using compounds of Formula (I).Type: ApplicationFiled: May 9, 2011Publication date: September 1, 2011Inventors: Martin Neitzel, Michael S. Dappen, Jennifer Marugg
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Patent number: 7981881Abstract: Fused heterocylic compounds of the following Formula wherein R1, R2, R5, Z, J1 and J2 are described herein, and analogs thereof are provided which are useful in treating leukocyte activation-associated disorders.Type: GrantFiled: March 18, 2008Date of Patent: July 19, 2011Assignee: Bristol-Myers Squibb CompanyInventors: Joseph Barbosa, William J. Pitts, Junqing Guo
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Publication number: 20110172414Abstract: A pesticide, particularly an insecticide or an acaricide, including a substituted isoxazoline compound of formula (1) or a salt thereof: wherein A1, A2 and A3 independently of one another are carbon atom or nitrogen atom, G is benzene ring, etc., L is —N(R2c)—, or —CH(R2a)N(R2c)—, etc., X is halogen atom, C1-C6 haloalkyl, etc., Y is halogen atom, C1-C6alkyl, etc., R1 is —C(O)R1a, —C(O)OR1a, —C(O)NHR1a, etc., R2 is hydrogen atom, C1-C6haloalkyl, —C1-C4alkoxy C1-C4alkyl, cyano C1-C6alkyl, C3-C6alkenyl, C3-C6alkynyl, —C(O)R15, —C(O)OR15, etc., R3 is C1-C6haloalkyl, etc., m is an integer of 0 to 5, n is an integer of 0 to 4. The pesticide containing these compounds.Type: ApplicationFiled: March 28, 2011Publication date: July 14, 2011Applicant: NISSAN CHEMICAL INDUSTRIES, LTD.Inventors: Takeshi MITA, Kazushige MAEDA, Mitsuaki KOMODA, Eitatsu IKEDA, Ken-ichi TOYAMA, Motoyoshi IWASA
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Patent number: 7968708Abstract: Disclosed are compounds having the formula: wherein Z1 is an alkylene moiety; Q is a carboxylic acid derivative; and R1 and R2 are the same or different and are selected from the group consisting of alkyl, aryl, alkylcarbonyl, arylcarbonyl, hydroxycarbonyl, and alkoxycarbonyl or R1 and R2, taken together with the nitrogen atom to which they are bound, form a ring. Also disclosed are compounds having the formula: wherein Z1 is an alkylene moiety; Q is a carboxylic acid derivative; and R13 is selected from the group consisting of alkyl and aryl. The compounds can be used to modulate cell proliferation and/or apoptosis, for example, in the treatment of cancers and other proliferative diseases, disorders, and conditions.Type: GrantFiled: December 6, 2007Date of Patent: June 28, 2011Assignees: The Research Foundation of State University of New York, Health Research Inc.Inventors: David G. Hangauer, Fengzhi Li, Taher Hegab, Xiang Ling
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Patent number: 7951940Abstract: The present invention features inhibitors of nitric oxide synthase (NOS), particularly those that selectively inhibit neuronal nitric oxide synthase (nNOS) in preference to other NOS isoforms. The NOS inhibitors of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing conditions such as, for example, stroke, reperfusion injury, neurodegeneration, head trauma, CABG, migraine headache with and without aura, migraine with allodynia, central post-stroke pain (CPSP), neuropathic pain, morphine/opioid induced tolerance and hyperalgesia.Type: GrantFiled: March 13, 2008Date of Patent: May 31, 2011Assignee: NeurAxon, Inc.Inventors: Shawn Maddaford, Jailall Ramnauth, Suman Rakhit, Joanne Patman, Paul Renton, Subhash C. Annedi
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Publication number: 20110112063Abstract: The invention provides novel pyrimidine derivatives of formula I and pharmaceutical compositions thereof, and methods for using such compounds. For example, the pyrimidine derivatives of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of insulin-like growth factor (IGF-IR) or analplastic lymphoma kinase (ALK).Type: ApplicationFiled: June 24, 2009Publication date: May 12, 2011Inventors: Thomas H. Marsilje, Wenshuo Lu, Bei Chen, Xiaohui He, Christian Cho-Hua Lee, Songchun Jiang, Kunyong Yang
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Patent number: 7939657Abstract: Disclosed are N-substituted benzenesulfonamides for use in treating or preventing cognitive disorders, such as Alzheimer's Disease. In Formula (I), R1, R2, R3, R4, R3?, R10 and R11 are as described herein. The invention also encompasses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of treating cognitive disorders using compounds of Formula (I).Type: GrantFiled: April 23, 2007Date of Patent: May 10, 2011Assignee: Elan Pharmaceuticals, Inc.Inventors: Martin Neitzel, Michael S. Dappen, Jennifer Marugg
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Publication number: 20110105472Abstract: Use of diaminopyrimidines of the formula (I) in which R1 to R11a,b,c and X1, X2 have the meanings given in the description, and also agrochemically active salts thereof as crop protection agents. Diaminopyrimidines of the formulae (Ia), (Ib) and (Ic) in which R8a, R8b, R8c, and R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11a,b,c and X1, X2 have the meanings given in the description, and also agrochemically active salts thereof and their use for controlling animal pests and/or phytopathogenic harmful fungi.Type: ApplicationFiled: March 16, 2009Publication date: May 5, 2011Applicant: Bayer CropScience AGInventors: Jörg Nico Greul, Olive Gaertzen, Stefan Hillebrand, Amos Mattes, Ulrike Wachendorff-Neumann, Peter Dahmen, Arnd Voerste, Peter Schreier, Ulrich Görgens, Heinz Kehne, Christian Paulitz, Hiroyuki Hadano, Oliver Guth, Angela Becker, Olga Malsam
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Publication number: 20110105457Abstract: The purpose of the present invention is to provide a compound or a pharmaceutically acceptable salt thereof which inhibits the activity of PI3K to regulate many biological processes including the growth, differentiation, survival, proliferation, migration, metabolism, and the like of cells and is therefore useful for the prevention/treatment of diseases including inflammatory diseases, arteriosclerosis, vascular/circulatory diseases, cancer/tumors, immune system diseases, cell proliferative diseases, infectious diseases, and the like. This was achieved by providing a substituted 2-amino-5,6-nitrogenated fused ring compound shown in the present specification, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: April 16, 2009Publication date: May 5, 2011Inventors: Daisuke Taniyama, Kazuya Kano, Kazuya Okamoto, Masahiko Fujioka, Yasunori Mitsuoka
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Publication number: 20110077236Abstract: The present invention relates to new substituted carboxylic acid amides of general formula wherein A, B and R1 to R5 are defined as in claim 1, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties.Type: ApplicationFiled: December 2, 2010Publication date: March 31, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Henning PRIEPKE, Kai GERLACH, Roland PFAU, Norbert HAUEL, Iris KAUFFMANN-HEFNER, Georg DAHMANN, Herbert NAR, Sandra HANDSCHUH, Wolfgang WIENEN, Annette SCHULER-METZ
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Patent number: 7915251Abstract: The invention provides ?-helix mimetic structures of formula (I) with the definitions of A, B, D, E, G, W, R1 and R2 as set out in the description and a chemical library relating thereto. The compounds, pharmaceutical compositions comprising the compounds, and methods of the invention using the compounds, relate to the treatment of diseases including fibrosis, such as pulmonary fibrosis.Type: GrantFiled: March 15, 2006Date of Patent: March 29, 2011Assignee: Institute for Chemical GenomicsInventors: Michael Kahn, Masakatsu Eguchi
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Publication number: 20110065682Abstract: The present invention relates to novel heterocyclic compounds of Formulae I-III; as disclosed herein or a pharmaceutically acceptable salt, solvate, ester, prodrug or stereoisomer thereof. Also disclosed are pharmaceutical compositions comprising said compounds, and methods for using said compounds for treating or preventing a thromboembolic disorder.Type: ApplicationFiled: May 18, 2009Publication date: March 17, 2011Inventors: Martin C. Clasby, William J. Greenlee, Yan Xia, Tin-Yau Chan, Mariappan V. Chelliah, Samuel Chackalamannil, Haiyan Pu,, Keith A. Eagen, Henry Vaccaro, Brian A. McKittrick,, Liyuan Wang, Xiaobang Gao
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Publication number: 20110053912Abstract: A novel and excellent method for preventing and/or treating diseases related to a cannabinoid type 2 receptor, based on an agonistic action on a cannabinoid type 2 receptor. It was found that a hetero ring derivative mainly having two substituents, for example, a pyrimidine-5-carboxamide derivative having a substituent amino group at the 2-position, exhibits a potent agonistic action on a cannabinoid type 2 receptor, and can be an agent for preventing and/or treating diseases related to a cannabinoid type 2 receptor such as inflammatory diseases, pain, and the like.Type: ApplicationFiled: March 29, 2010Publication date: March 3, 2011Applicant: Astellas Pharma Inc.Inventors: Yuji Matsushima, Hirokazu Kubota, Hisao Hamaguchi, Yoshinori Okamoto, Takeshi Hondo, Fusako Nishigaki
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Patent number: 7897592Abstract: The invention encompasses a series bicyclic pyrimidinone compounds of Formula I which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions and methods for treating those infected with HIV.Type: GrantFiled: November 14, 2006Date of Patent: March 1, 2011Assignee: Bristol-Myers Squibb CompanyInventor: B. Narasimhulu Naidu
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Patent number: 7897593Abstract: The invention encompasses series bicyclic pyrimidinone compounds of Formula I which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions and methods for treating those infected with HIV.Type: GrantFiled: May 29, 2007Date of Patent: March 1, 2011Assignee: Bristol-Myers Squibb CompanyInventors: B. Narasimhulu Naidu, Margaret E. Sorenson
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Publication number: 20110034439Abstract: To provide an antitumor agent which exhibits excellent c-Met inhibitory effect and mitigates side effects by virtue of selectively affecting to tumor cells in which c-Met is specifically expressed.Type: ApplicationFiled: April 9, 2009Publication date: February 10, 2011Applicant: Taiho Pharmaceutical Co., Ltd.Inventors: Yoshimitsu Suda, Kosuke Egami, Hidenori Fujita
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Publication number: 20110003794Abstract: The present invention features compounds that are HIV integrase inhibitors and therefore are useful in the inhibition of HIV replication, the prevention and/or treatment of infection by HIV, and in the treatment of AIDS and/or ARC.Type: ApplicationFiled: August 30, 2010Publication date: January 6, 2011Inventor: Brian A Johns
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Publication number: 20110003788Abstract: The present invention provides a compound having a superior Smo inhibitory activity and lower toxicity, which is sufficiently satisfactory as a pharmaceutical product. The present invention provides a compound represented by the formula (I) wherein ring A is 5- to 7-membered ring optionally having substituent(s), where substituents are optionally bonded to each other to form a ring; X is O, S or NR1 (R1 is a hydrogen atom or a hydrocarbon group optionally having substituent(s)); R2 is carbamoyl optionally having substituent(s); and R3 is hydroxy optionally having substituent(s), or a salt thereof.Type: ApplicationFiled: February 25, 2009Publication date: January 6, 2011Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Nobuhiro Fujii, Yuya Oguro, Satoshi Sasaki, Shigeru Kondo
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Publication number: 20100323994Abstract: The invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I imidazopyridazines inhibit protein kinase activity thereby making them useful as anticancer agents.Type: ApplicationFiled: February 6, 2009Publication date: December 23, 2010Applicant: BRISTOL-MYERS SQUIBB COMPANYInventors: Brian E. Fink, Soong-Hoon Kim, Yufen Zhao, Ping Chen, Wayne Vaccaro, Litai Zhang, Ashvinikumar V. Gaval, Dharmpal S. Dodd, Libing Chen
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Publication number: 20100317848Abstract: The present invention relates to a process for the manufacturing of substituted 3-amino-tetrahydrofuran-3-carboxylic acid amides of general formula (I) and their precursors in high optical purity to the precursors of the synthesis of substituted S-Amino-tetrahydrofuran-S-carboxylic acid amides of general formula (I) in high optical purity, and to the tautomers, enantiomers, diastereomers, mixtures and salts of substituted 3-amino-tetrahydrofuran-3-carboxylic acid amides of general formula (I) in high optical purity, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties.Type: ApplicationFiled: December 21, 2007Publication date: December 16, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Zhengxu Han, Kai Gerlach, Dhileepkumar Krishnamurthy, Burkhard Matthes, Herbert Nar, Roland Pfau, Henning Priepke, Annette Schuler-Metz, Chris H. Senanayake, Peter Sieger, Wenjun Tang, Wolfgang Wienen, Yibo Xu, Nathan K. Yee
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Publication number: 20100298295Abstract: The invention provides novel pyrimidine derivatives of formula (1) and pharmaceutical compositions thereof, and methods for using such compounds. For example, the pyrimidine derivatives of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of insulin-like growth factor (IGF-1R) or anaplastic lymphoma kinase (ALK).Type: ApplicationFiled: August 27, 2008Publication date: November 25, 2010Applicant: IRM LLCInventors: Thomas H. Marsilje, Wenshuo Lu, Bei Chen, Xiaohui He, Badry Bursulaya, Christian Cho-Hua Lee, Nathanael S. Gray
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Publication number: 20100286122Abstract: An efficient synthesis for the preparation of N-[(3R,6S)-6-(2,3-difluorophenyl)-2-oxo-1-(2,2,2-trifluoroethyl)azepan-3-yl]-4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide, by coupling (3R,6S)-3-amino-6-(2,3-difluorophenyl)-1-(2,2,2-trifluoroethyl)azepan-2-one and 2-oxo-1-(4-piperidinyl)-2,3-dihydro-1H-imidazo[4,5-b]pyridine dihydrochloride with 1,1?-carbonyldiimidazole (“CDI”) as carbonyl source; an efficient preparation of the potassium salt of N-[(3R,6S)-6-(2,3-difluorophenyl)-2-oxo-1-(2,2,2-trifluoroethyl)azepan-3-yl]-4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide; efficient syntheses for the preparation of intermediates (3R,6S)-3-amino-6-(2,3-difluorophenyl)-1-(2,2,2-trifluoroethyl)azepan-2-one and 2-oxo-1-(4-piperidinyl)-2,3-dihydro-1H-imidazo[4,5-b]pyridine dihydrochloride, and the potassium salt of N-[(3R,6S)-6-(2,3-difluorophenyl)-2-oxo-1-(2,2,2-trifluoroethyl)azepan-3-yl]-4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamiType: ApplicationFiled: April 6, 2007Publication date: November 11, 2010Inventor: Kevin Belyk
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Patent number: 7829699Abstract: An efficient synthesis for the preparation of N-[(3R,6S)-6-(2,3-difluorophenyl)-2-oxo-1-(2,2,2-trifluoroethyl)azepan-3-yl]-4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1 -carboxamide, by coupling (3R,6S)-3-amino-6-(2,3-difluorophenyl)-1-(2,2,2-trifluoroethyl)azepan-2-one and 2-oxo-1-(4-piperidinyl)-2,3-dihydro-1H-imidazo[4,5-b]pyridine dihydrochloride with 1,1?-carbonyldiimidazole (“CDI”) as carbonyl source; and an efficient preparation of the potassium salt of N-[(3R,6S)-6-(2,3-difluorophenyl)-2-oxo-1-(2,2,2-trifluoroethyl)azepan-3-yl]-4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide.Type: GrantFiled: April 6, 2007Date of Patent: November 9, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Kevin Belyk, Nelo Rivera
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Patent number: 7820647Abstract: The invention relates to 2-substituted pyrimidines of the formula I in which the index n and the substituents L and R1 to R3 are as defined in the description and X is a group —CH—Ra, —N—Rb—, —O— or —S—; Ra may be hydrogen, halogen, C1-C6-alkyl, C1-C6-alkoxy, cyano or C1-C6-alkoxycarbonyl; Rb is hydrogen, C1-C6-alkyl or C3-C6-cycloalkyl; T is a group —CH—Ra—; p is an integer from 1 to 4; Y is a group —CH—Ra— or —N—Rb—, o is 0 or 1; Z is O, S or a group N(Rc) Rc is hydrogen, C1-C6-alkyl or C1-C6-alkoxy, and to processes for their preparation, to pesticidal compositions comprising them and to their use as pesticides.Type: GrantFiled: May 17, 2005Date of Patent: October 26, 2010Assignee: BASF AktiengesellschaftInventors: Anja Schwögler, Frank Schieweck, Joachim Rheinheimer, Markus Gewehr, Bernd Müller, Thomas Grote, Wassilios Grammenos, Udo Hünger, Carsten Blettner, Peter Schäfer, Oliver Wagner, Reinhard Stierl, Ulrich Schöfl, Siegfried Strathmann, Maria Scherer