Four Or More Ring Hetero Atoms In The Polycyclo Ring System Patents (Class 544/184)
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Patent number: 8217169Abstract: The present invention is directed to compounds of the formula: or salts thereof or N-oxides and their use in peptide synthesis.Type: GrantFiled: October 11, 2010Date of Patent: July 10, 2012Assignee: University of MassachusettsInventors: Louis A. Carpino, Jusong Xia, Chongwu Zhang, Calin Dan Sferdean
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Publication number: 20120157458Abstract: The present invention provides imidazotriazinone compounds which are inhibitors of phosphodiesterase 9. The present invention further provides processes, pharmaceutical compositions, pharmaceutical preparations and pharmaceutical use of the compounds in the treatment of PDE9 associated diseases or disorders in mammals, including humans.Type: ApplicationFiled: September 20, 2011Publication date: June 21, 2012Inventors: Amy Ripka, Gideon Shapiro, Andrew J. McRiner
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Publication number: 20120149662Abstract: The invention provides compounds of formula (I): or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula (I), processes for preparing compounds of formula (I), intermediates useful for preparing compounds of formula (I) and therapeutic methods for suppressing an immune response or treating cancer or a hematologic malignancy using compounds of formula (I).Type: ApplicationFiled: August 27, 2010Publication date: June 14, 2012Applicant: BioCryst Pharmaceuticals, Inc.Inventors: Yarlagadda S. Babu, Pravin L. Kotian, V. Satish Kumar, Minwan Wu, Tsu-Hsing Lin
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Publication number: 20120142681Abstract: The invention relates to compounds of formula (I) and salts thereof: wherein the substituents are as defined in the specification; a compound of formula (I) for use in the treatment of the human or animal body, in particular with regard to c-Met tyrosine kinase mediated diseases or conditions; the use of a compound of formula (I) for manufacturing a medicament for the treatment of such diseases; pharmaceutical compositions comprising a compound of the formula (I), optionally in the presence of a combination partner, and processes for the preparation of a compound of formula (I).Type: ApplicationFiled: August 10, 2010Publication date: June 7, 2012Applicant: NOVARTIS AGInventors: Feng He, Miao Dai, Xingnian Fu, Yue Li, Lei Liu, Yuan Mi, Yao-chang Xu, Guoliang Xun, Zhengtian Yu, Ji Yue Zhang
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Patent number: 8188272Abstract: Compounds having the formula (I), and enantiomers, and diastereomers, pharmaceutically-acceptable salts, thereof, [PLEASE INSERT CHEMICAL STRUCTURE HERE] (I) are useful as kinase modulators, including Btk modulation, wherein R1, R2, R4, Q, Y, A and D are as defined herein.Type: GrantFiled: March 20, 2008Date of Patent: May 29, 2012Assignee: Bristol-Myers Squibb CompanyInventors: Chunjian Liu, Katerina Leftheris, Andrew J. Tebben
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Patent number: 8143251Abstract: The present invention is directed to [1,2,4]triazolo[4,3-b][1,2,4]triazines, and pharmaceutical compositions thereof, which are inhibitors of kinases such as c-Met and are useful in the treatment of cancer and other diseases related to the dysregulation of kinase pathways.Type: GrantFiled: February 24, 2011Date of Patent: March 27, 2012Assignee: Incyte CorporationInventors: Jincong Zhuo, Colin Zhang, Meizhong Xu, Ding-Quan Qian, Wenqing Yao, Ravi Kumar Jalluri
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Patent number: 8143237Abstract: Selenopheno triazene analogs, their compositions, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, and pharmaceutically acceptable salts and mixtures thereof are useful for the treatment of metastatic malignant melanoma and other cancers. The selenopheno triazene analogs have the general formulae (I) or (II): wherein the substituents R1, R2, R3, R6, and R7 are as described in the specification. Other cancers include which may be treated with these compounds include, but are not limited to, malignant melanoma, leukemia, lymphomas (Hodgkins and non-Hodgkins), sarcomas (Ewing's sarcoma), brain tumors, central nervous system (CNS) metastases, gliomas, carcinomas such as breast cancer, prostate cancer, lung cancer (small cell and non-small cell), colon cancer, pancreatic cancer, Head and Neck cancers and oropharyngeal squamous cell carcinoma.Type: GrantFiled: April 26, 2010Date of Patent: March 27, 2012Assignee: Kasina Laila Innova Pharmaceuticals Private LimitedInventors: Ganga Raju Gokaraju, Sudhakar Kasina, Rama Raju Gokaraju, Venkata Kanaka Ranga Raju Gokaraju, Venkateswarlu Somepalli, Trimurtulu Golakoti, Kiran Bhupathiraju, Sengupta Krishanu, Venkata Krishna Raju Alluri
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Patent number: 8138337Abstract: Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins as well as their prodrugs are disclosed. Such reverse-turn mimetic structures and prodrugs have utility over a wide range of fields, including use as diagnostic and therapeutic agents. Libraries containing the reverse-turn mimetic structures of this invention are also disclosed as well as methods for screening the same to identify biologically active members. The invention also relates to the use of such compounds and prodrugs for inhibiting or treating disorders modulated by Wnt-signaling pathway, such as cancer, especially colorectal cancer, restenosis associated with angioplasty, polycystic kidney disease, aberrant angiogenesis disease, rheumatoid arthritis disease, tuberous sclerosis complex, Alzheimer's disease, excess hair growth or loss, or ulcerative colitis.Type: GrantFiled: December 29, 2009Date of Patent: March 20, 2012Assignee: Choongwae Pharma CorporationInventors: Sung Hwan Moon, Jae Uk Chung, Sung Chan Lee, Masakatsu Eguchi, Michael Kahn, Kwang Won Jeong, Cu Nguyen, Soo Jin Lee
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Publication number: 20120059000Abstract: Chemical compounds that modulate kinase activity, including PI3 kinase activity, and chemical compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including P13 kinase activity, are described herein.Type: ApplicationFiled: May 20, 2011Publication date: March 8, 2012Inventors: Pingda Ren, Yi Liu, Liansheng Li, Katrina Chan, Alfredo C. Castro, Catherine A. Evans
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Patent number: 8106049Abstract: Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins are disclosed. Such reverse-turn mimetic structures have utility as diagnostic and therapeutic agents for inhibiting or treating disorders modulated by Wnt-signaling pathway, such as cancer, especially colorectal cancer, restenosis associated with angioplasty, polycystic kidney disease, aberrant angiogenesis disease, rheumatoid arthritis disease, tuberous sclerosis complex, Alzheimer's disease, excess hair growth or loss, or ulcerative colitis. In one embodiment, these reverse-term mimetics have a general structure of formula (VI): wherein Ra, Rb, Rc, X1, X2 and X3 are defined as provided herein.Type: GrantFiled: September 3, 2009Date of Patent: January 31, 2012Assignee: Choongwae Pharma CorporationInventors: Sung Hwan Moon, Jae Uk Chung, Sung Chan Lee, Masakatsu Eguchi, Michael Kahn, Kwang Won Jeong, Cu Nguyen
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Publication number: 20120022046Abstract: Methods and pharmaceutical compositions for treating viral infections, by administering certain thienopyridine derivative compounds in therapeutically effective amounts are disclosed. Methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by flavivirus is disclosed, i.e., including but not limited to, Dengue virus, West Nile virus, yellow fever virus, Japanese encephalitis virus, and tick-borne encephalitis virus.Type: ApplicationFiled: February 24, 2010Publication date: January 26, 2012Inventors: Chelsea M. Byrd, Dongcheng Dai, Robert Jordan, Dennis E. Hruby
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Patent number: 8101751Abstract: Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins are disclosed. Such reverse-turn mimetic structures have utility over a wide range of fields, including use as diagnostic and therapeutic agents. Libraries containing the reverse-turn mimetic structures of this invention are also disclosed as well as methods for screening the same to identify biologically active members. The invention also relates to the use of such compounds for inhibiting or treating disorders modulated by Wnt-signaling pathway, such as cancer, especially colorectal cancer, restenosis associated with angioplasty, polycystic kidney disease, aberrant angiogenesis disease, rheumatoid arthritis disease, tuberous sclerosis complex, Alzheimer's disease, excess hair growth or loss, or ulcerative colitis.Type: GrantFiled: August 14, 2009Date of Patent: January 24, 2012Assignee: Choongwae Pharma CorporationInventors: Sung Hwan Moon, Jae Uk Chung, Sung Chan Lee, Masakatsu Eguchi, Michael Kahn, Kwang Won Jeong, Cu Nguyen
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Patent number: 8080657Abstract: Conformationally constrained compounds that are novel and mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins and having bicyclic framework are disclosed, as well as their prodrugs. Such reverse-turn mimetic structures and prodrugs have utility over a wide range of fields, including use as diagnostic and therapeutic agents. The invention also relates to a use of such compounds for the preparation of a medicament for treating or preventing cancer including an acute myeloid leukemia.Type: GrantFiled: October 15, 2008Date of Patent: December 20, 2011Assignee: Choongwae Pharma CorporationInventors: Jae Uk Chung, Kyung-Yun Jung, Min-Wook Jeong, Hee-Kyung Jung, Hyun-Ju La
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Patent number: 8071764Abstract: Conformationally constrained compounds that are novel and mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins and having bicyclic frame-work are disclosed, as well as their prodrugs. Such reverse-turn mimetic structures and prodrugs have utility over a wide range of fields, including use as diagnostic and therapeutic agents. The invention also relates to the use of such compounds for the preparation of a medicament for treating or preventing cancer including an acute myeloid leukemia.Type: GrantFiled: October 15, 2008Date of Patent: December 6, 2011Assignee: Choongwae Pharma CorporationInventors: Jae Uk Chung, Kyung-Yun Jung, Sang-Hwi Lee, Myoung-Joo Kang
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Publication number: 20110294797Abstract: Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins are disclosed. Such reverse-turn mimetic structures have utility over a wide range of fields, including use as diagnostic and therapeutic agents. Libraries containing the reverse-turn mimetic structures of this invention are also disclosed as well as methods for screening the same to identify biologically active members. The invention also relates to the use of such compounds for inhibiting or treating disorders modulated by Wnt-signaling pathway, such as cancer, especially colorectal cancer, restenosis associated with angioplasty, polycystic kidney disease, aberrant angiogenesis disease, rheumatoid arthritis disease, tuberous sclerosis complex, Alzheimer's disease, excess hair growth or loss, or ulcerative colitis.Type: ApplicationFiled: July 29, 2011Publication date: December 1, 2011Applicant: Choongwae Pharma CorporationInventors: Sung Hwan Moon, Jae Uk Chung, Sung Chan Lee, Masakatsu Eguchi, Michael Kahn, Kwang Won Jeong, Cu Nguyen
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Patent number: 8049008Abstract: Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins as well as their prodrugs are disclosed. Such reverse-turn mimetic structures and prodrugs have utility over a wide range of fields, including use as diagnostic and therapeutic agents. Libraries containing the reverse-turn mimetic structures of this invention are also disclosed as well as methods for screening the same to identify biologically active members. The invention also relates to the use of such compounds and prodrugs for inhibiting or treating disorders modulated by Wnt-signaling pathway, such as cancer, especially colorectal cancer, restenosis associated with angioplasty, polycystic kidney disease, aberrant angiogenesis disease, rheumatoid arthritis disease, tuberous sclerosis complex, Alzheimer's disease, excess hair growth or loss, or ulcerative colitis.Type: GrantFiled: April 7, 2010Date of Patent: November 1, 2011Assignee: Choongwae Pharma CorporationInventors: Jae Uk Chung, Masakatsu Eguchi
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Publication number: 20110257185Abstract: Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins are disclosed. Such reverse-turn mimetic structures have utility over a wide range of fields, including use as diagnostic and therapeutic agents. Libraries containing the reverse-turn mimetic structures of this invention are also disclosed as well as methods for screening the same to identify biologically active members. The invention also relates to the use of such compounds for inhibiting or treating disorders modulated by Wnt-signaling pathway, such as cancer, especially colorectal cancer, restenosis associated with angioplasty, polycystic kidney disease, aberrant angiogenesis disease, rheumatoid arthritis disease, tuberous sclerosis complex, Alzheimer's disease, excess hair growth or loss, or ulcerative colitis.Type: ApplicationFiled: June 29, 2011Publication date: October 20, 2011Applicant: CHOONGWAE PHARMA CORPORATIONInventors: SUNG HWAN MOON, JAE UK CHUNG, SUNG CHAN LEE, MASAKATSU EGUCHI, MICHAEL KAHN, KWANG WON JEONG, CU NGUYEN
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Patent number: 8022207Abstract: The invention relates to a compound which has affinity with amyloid, shows sufficiently rapid clearance from normal tissues and is suppressed in toxicity such as mutagenicity, and also relates to a low-toxic diagnostic agent for Alzheimer's disease containing the compound. The compound is represented by the following formula (1) or a salt thereof: wherein A1, A2, A3 and A4 independently represent a carbon or a nitrogen, and R3 is a group represented by the following formula: wherein R1 is a radioactive halogen substituent; m is an integer of 0 to 4; and n is an integer of 0 or 1, provided that at least one of A1, A2, A3 and A4 represents a carbon, and R3 binds to a carbon represented by A1, A2, A3 or A4.Type: GrantFiled: April 26, 2007Date of Patent: September 20, 2011Assignee: Nihon Medi-Physics Co., Ltd.Inventors: Shigeyuki Tanifuji, Daisaku Nakamura, Shinya Takasaki
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Publication number: 20110224195Abstract: The present invention is directed to substituted six-membered heterocyclic compounds of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as obesity and diabetes, particularly Type 2 diabetes. 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 dipeptidyl peptidase-IV enzyme is involved.Type: ApplicationFiled: August 18, 2008Publication date: September 15, 2011Inventors: Tesfaye Biftu, Danqing Feng, Ann E. Weber, Jason M. Cox, Xiaoxia Qian, Jinyou Xu
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Publication number: 20110218183Abstract: Compounds represented by Formula (I) or a pharmaceutically acceptable salt thereof, are inhibitors of mTOR and useful in the treatment of cancer.Type: ApplicationFiled: May 13, 2011Publication date: September 8, 2011Inventors: Xin Chen, Heather Coate, Andrew Philip Crew, Han-Qing Dong, Ayako Honda, Mark Joseph Mulvihill, Paula A.R. Tavares, Jing Wang, Douglas S. Werner, Kristen Michelle Mulvihill, Kem W. Siu, Bijoy Panicker, Apoorba Bharadwaj, Lee D. Arnold, Meizhong Jin, Brian Volk, Qinghua Weng, James David Beard
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Publication number: 20110212967Abstract: The present invention relates to imidazo[1,2-b][1,2,4]triazines that are inhibitors of c-Met and are useful in the treatment of c-Met associated diseases including cancer.Type: ApplicationFiled: February 2, 2011Publication date: September 1, 2011Applicant: INCYTE CORPORATIONInventors: Jincong Zhuo, Chunhong He, Wenqing Yao
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Patent number: 8008315Abstract: The present invention is directed to compounds which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.Type: GrantFiled: May 3, 2010Date of Patent: August 30, 2011Assignee: Merck, Sharp & Dohme Corp.Inventors: Philippe G. Nantermet, Hemaka Anthony Rajapakse, Harold G. Selnick
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Publication number: 20110190496Abstract: Compounds represented by Formula (I) or a pharmaceutically acceptable salt thereof, are inhibitors of mTOR and useful in the treatment of cancer.Type: ApplicationFiled: April 13, 2011Publication date: August 4, 2011Inventors: Xin Chen, Heather Coate, Andrew Philip Crew, Han-Qing Dong, Ayako Honda, Mark Joseph Mulvihill, Paula A.R. Tavares, Jing Wang, Douglas S. Werner, Kristen Michelle Mulvihill, Kam W. Siu, Bijoy Panicker, Apoorba Bharadwaj, Lee D. Arnold, Meizhong Jin, Brian Volk, Quinghua Weng, James David Beard
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Publication number: 20110190495Abstract: Disclosed are N-{1-[3-(2-ethoxy-5-(4-ethylpiperazinyl)sulfonylphenyl)-4,5-dihydro-5-oxo-1,2,4-triazin-6-yl]ethyl}butyramide (which is represented by formula III), its preparation method, intermediates during preparation procedure, preparation method for such intermediates and a method for preparing vardenafil from the compound. In the method for preparing vardenafil, a chloro-sulfonation reaction carries out in the early stage of the preparation procedure.Type: ApplicationFiled: December 28, 2007Publication date: August 4, 2011Applicant: Topharman Shanghai Co., Ltd.Inventors: Guanghui Tian, Zheng Liu, Jin Zheng, Jingshan Shen
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Patent number: 7989451Abstract: The invention relates to novel tricyclic 1,2,4-triazine-1-oxides and novel tricyclic 1,2,4-triazine-1,4-dioxides of formula I and to related analogues, to their preparation, and to their use as hypoxia-selective drugs and radiosensitizers for cancer therapy, both alone or in combination with radiation and/or other anticancer drugs.Type: GrantFiled: March 31, 2006Date of Patent: August 2, 2011Assignee: Auckland Uniservices LimitedInventors: Michael Patrick Hay, Adrian Blaser, William Alexander Denny, Kevin Owen Hicks, Ho Huat Lee, Karin Pchalek, Frederik Bastiaan Pruijn, Bronwyn Gae Siim, William Robert Wilson, Shangjin Yang
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Publication number: 20110183972Abstract: The invention belongs to pharmaceutical field. The invention relates to the compounds according to Formula I, including their optically active forms, pharmaceutically acceptable salts or hydrates, and the pharmaceutical composition comprising thereof as active ingredient; uses in the preparation of vascular endothelial growth factor receptor tyrosine kinase inhibitors, and uses in the preparation of medicament for the treatment and/or prevention of cancer.Type: ApplicationFiled: February 10, 2009Publication date: July 28, 2011Applicant: SHENYANG PHARMACEUTICAL UNIVERSITYInventors: Linxiang Zhao, Jinling Lv, Rui Wang, Dan Liu, Yongkui Jing
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Publication number: 20110172422Abstract: The present invention relates to methods of modulating the pharmacokinetic and/or pharmacodynamic properties of a compound by attaching at least one functional unit or group to the compound, thereby improving its non-specific binding characteristics and/or pharmacokinetic properties. Compounds comprising at least one functional residue are provided, as are pharmaceutical compositions comprising said compounds.Type: ApplicationFiled: February 21, 2006Publication date: July 14, 2011Applicant: SURFACE LOGIX, INC.Inventors: Stewart Campbell, David Duffy, Michael Grogan, Steven Kates, Emanuele Ostuni, Olivier Schueller, Paul Sweetnam
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Patent number: 7977478Abstract: Crystalline polymorphic forms of vardenafil and vardenafil hydrochloride, and processes for preparing them.Type: GrantFiled: September 27, 2006Date of Patent: July 12, 2011Assignees: Dr. Reddy's Laboratories Limited, Dr. Reddy's Laboratories, Inc.Inventors: Eswaraiah Sajja, Ravindar Reddy Koppera, Satyanarayana Revu, Venkata Reddy Vajrala, Vijayapal Reddy Kanumathi
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Publication number: 20110166144Abstract: The present disclosure is directed to pyrimidotriazinediones and pyrimidopyrimidinediones having a formula (I), (II), or (III), or a mixture or pharmaceutically acceptable salt or hydrate thereof, and to methods of treating cancer comprising administering the same.Type: ApplicationFiled: July 30, 2009Publication date: July 7, 2011Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGANInventors: H.D. H. Showalter, Anjanette J. Turbiak, Eric R. Fearon, Guido T. Bommer
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Publication number: 20110165183Abstract: The invention provides a compound of formula (I): wherein W is a bicyclic heteroaromatic group; or a salt thereof. The compounds and salts thereof have beneficial therapeutic properties (e.g. immunosuppressant properties).Type: ApplicationFiled: July 31, 2009Publication date: July 7, 2011Applicant: BioCryst Pharmaceuticals, Inc.Inventors: Yarlagadda S. Babu, Pooran Chand, Pravin L. Kotian, V. Satish Kumar
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Publication number: 20110144113Abstract: The present invention is directed to [1,2,4]triazolo[4,3-b][1,2,4]triazines, and pharmaceutical compositions thereof, which are inhibitors of kinases such as c-Met and are useful in the treatment of cancer and other diseases related to the dysregulation of kinase pathways.Type: ApplicationFiled: February 24, 2011Publication date: June 16, 2011Inventors: Jincong Zhuo, Colin Zhang, Meizhong Xu, Ding-Quan Qian, Wenqing Yao, Ravi Kumar Jalluri
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Publication number: 20110136781Abstract: The present invention is directed to imidazo[1,2-b][1,2,4]triazines and imidazo[1,2-a]pyrimidines, and pharmaceutical compositions thereof, which are inhibitors of kinases such as c-Met and are useful in the treatment of cancer and other diseases related to the dysregulation of kinase pathways.Type: ApplicationFiled: June 10, 2010Publication date: June 9, 2011Applicant: Incyte CorporationInventors: Jincong ZHUO, Meizhong XU, Chunhong HE, Colin ZHANG, Ding-Quan QIAN, David M. BURNS, Yun-Long LI, Brian METCALF, Wenqing YAO
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Publication number: 20110124640Abstract: Compounds having the formula (I), and enantiomers, and diastereomers, pharmaceutically-acceptable salts, thereof, are useful as kinase modulators, including Btk modulation, wherein R1, R2, R3, R4, Q, A and B are as defined herein.Type: ApplicationFiled: July 23, 2009Publication date: May 26, 2011Inventors: Chunjian Liu, Katerina Leftheris, Andrew J. Tebben
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Patent number: 7943767Abstract: Compounds represented by Formula (I) or a pharmaceutically acceptable salt thereof, are inhibitors of mTOR and useful in the treatment of cancer.Type: GrantFiled: November 20, 2009Date of Patent: May 17, 2011Assignee: OSI Pharmaceuticals, Inc.Inventors: Xin Chen, Heather Coate, Andrew Philip Crew, Han-Qing Dong, Ayako Honda, Mark Joseph Mulvihill, Paula A. R. Tavares, Jing Wang, Douglas S. Werner, Kristen Michelle Mulvihill, Kam W. Siu, Bijoy Panicker, Apoorba Bharadwaj, Lee D. Arnold, Meizhong Jin, Brian Volk, Quinghua Weng, James David Beard
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Publication number: 20110105477Abstract: The present invention relates to HIV protease, and methods for inhibiting the function of HIV protease. In particular, present invention provides compounds that inhibit or block the biological activity of HIVp, thereby causing the replication of the HIV virus to be inhibited or to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and optionally other anti-viral agents as active ingredients, are suitable for treating patients or hosts infected with the HIV virus, which is known to cause AIDS. The compounds and formulations also find use in diagnostic and research settings.Type: ApplicationFiled: September 12, 2008Publication date: May 5, 2011Applicant: The Regents of the University of MichiganInventors: Heather A. Carlson, Kelly L. Damm, Kristen L. Meagher
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Patent number: 7932384Abstract: Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins are disclosed. Such reverse-turn mimetic structures have utility over a wide range of fields, including use as diagnostic and therapeutic agents. Libraries containing the reverse-turn mimetic structures of this invention are also disclosed as well as methods for screening the same to identify biologically active members. The invention also relates to the use of such compounds for inhibiting or treating disorders modulated by Wnt-signaling pathway, such as cancer, especially colorectal cancer, restenosis associated with angioplasty, polycystic kidney disease, aberrant angiogenesis disease, rheumatoid arthritis disease, tuberous sclerosis complex, Alzheimer's disease, excess hair growth or loss, or ulcerative colitis.Type: GrantFiled: July 27, 2009Date of Patent: April 26, 2011Assignee: Choongwae Pharma CorporationInventors: Sung Hwan Moon, Jae Uk Chung, Sung Chan Lee, Masakatsu Eguchi, Michael Kahn, Kwang Won Jeong, Cu Nguyen, Soo Jin Lee
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Publication number: 20110092459Abstract: Alpha-helix mimetic structures and compounds represented by the formula (I) wherein the general formula and the definition of each symbol are as defined in the specification, a compound relating thereto, and methods relating thereto, are disclosed. Applications of these compounds in the treatment of medical conditions, e.g., cancer diseases, fibrotic diseases, and pharmaceutical compositions comprising the mimetics are further disclosed.Type: ApplicationFiled: June 5, 2009Publication date: April 21, 2011Applicant: PRISM Biolab CorporationInventors: Takenao Odagami, Yuji Kogami, Hiroyuki Kouji
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Patent number: 7923555Abstract: Compounds represented by Formula (I) or a pharmaceutically acceptable salt thereof, are inhibitors of mTOR and useful in the treatment of cancer.Type: GrantFiled: December 2, 2008Date of Patent: April 12, 2011Assignee: OSI Pharmaceuticals, Inc.Inventors: Xin Chen, Heather Coate, Andrew Philip Crew, Hanqing Dong, Ayako Honda, Mark Joseph Mulvihill, Paula A. R. Tavares, Jing Wang, Douglas S. Werner, Kristen Michelle Mulvihill, Kam W. Siu, Bijoy Panicker, Apoorba Bharadwaj, Lee D. Arnold, Meizhong Jin, Brian Volk, Quinghua Weng, James David Beard
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Publication number: 20110082147Abstract: This invention relates to novel substituted imidazotriazines and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a compound showing partial-agonist activity at the GABA ?2, ?3 and ?5 subtype receptors, and antagonist activity at the al subtype receptor.Type: ApplicationFiled: July 23, 2010Publication date: April 7, 2011Applicant: CoNCERT Pharmaceuticals, Inc.Inventors: Scott L. Harbeson, Roger D. Tung, Julie F. Liu
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Patent number: 7915408Abstract: The present invention is directed to [1,2,4]triazolo[4,3-b][1,2,4]triazines, and pharmaceutical compositions thereof, which are inhibitors of kinases such as c-Met and are useful in the treatment of cancer and other diseases related to the dysregulation of kinase pathways.Type: GrantFiled: January 28, 2010Date of Patent: March 29, 2011Assignee: Incyte CorporationInventors: Jincong Zhuo, Colin Zhang, Meizhong Xu, Ding-Quan Qian, Wenqing Yao, Ravi Kumar Jalluri
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Publication number: 20110065708Abstract: The invention relates to compounds of formula (I) and salts thereof: wherein the substituents are as defined in the specification; a compound of formula (I) for use in the treatment of the human or animal body, in particular with regard to c-Met tyrosine kinase mediated diseases or conditions; the use of a compound of formula (I) for manufacturing a medicament for the treatment of such diseases; pharmaceutical compositions comprising a compound of the formula (I), optionally in the presence of a combination partner, and processes for the preparation of a compound of formula (I).Type: ApplicationFiled: August 19, 2010Publication date: March 17, 2011Applicant: NOVARTIS AGInventors: Miao DAI, Xingnian FU, Feng HE, Lei JIANG, Yue LI, Fang LIANG, Lei LIU, Yuan MI, Yao-chang XU, Guoliang XUN, Xiaoxia YAN, Zhengtian YU, Ji Yue ZHANG
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Publication number: 20110034375Abstract: The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I. Additionally, the present application provides pharmaceutical compositions containing at least one compound according to Formula I and optionally at least one additional therapeutic agent. Finally, the present application provides methods for treating a patient suffering from an MCHR-1 modulated disease or disorder such as, for example, obesity, diabetes, depression or anxiety by administration of a therapeutically effective dose of a compound according to Formula I. where R1, R1a, R1b, A, R3, R4, R5, R5b and R6 are as defined herein.Type: ApplicationFiled: October 19, 2010Publication date: February 10, 2011Inventors: William N. Washburn, Saleem Ahmad, Andres S. Hernandez
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Publication number: 20110028720Abstract: The present invention is directed to compounds of the formula: or salts thereof or N-oxides and their use in peptide synthesis.Type: ApplicationFiled: October 11, 2010Publication date: February 3, 2011Inventors: Louis A. Carpino, Jusong Xia, Chongwu Zhang, Calin Dan Sferdean
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Patent number: 7875613Abstract: The present invention concerns new compounds of formula (I), their process of preparation and their therapeutic use wherein R3, R4, R5, R6, Y, Het1, T, U, V, W, X, Ru, Rv and Rw are as defined in claim 1.Type: GrantFiled: October 30, 2006Date of Patent: January 25, 2011Assignee: Hybrigenics SAInventors: Philippe Guedat, Xavier Jacq, Frédéric Colland, Laurent Daviet, Etienne Formstecher, Jean-Christophe Rain, Matteo Colombo
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Publication number: 20110015197Abstract: Salt forms of mTOR inhibitors of the Formula (I): and methods of preparation, formulation, and use in treating disease.Type: ApplicationFiled: March 18, 2009Publication date: January 20, 2011Applicant: OSI Pharmaceuticals, Inc.Inventors: Arlindo L. Castelhano, Kristen Michelle Mulvihill, Josef A. Rechka, Gary C. Visor
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Publication number: 20110009367Abstract: The 2-phenyl-substituted imidazotriazinones having short, unbranched alkyl radicals in the 9-position are prepared from the corresponding 2-phenyl-imidazotriazinones by chlorosulphonation and subsequent reaction with the amines. The compounds inhibit cGMP-metabolizing phosphodiesterases and are suitable for use as active compounds in pharmaceuticals, for the treatment of cardiovascular and cerebrovascular disorders and/or disorders of the urogenital system, in particular for the treatment of erectile dysfunction.Type: ApplicationFiled: March 4, 2010Publication date: January 13, 2011Applicant: Bayer Schering Pharma AktiengesellschaftInventors: Ulrich Niewöhner, Maria Niewöhner, Mazen Es-Sayed, Helmut Haning, Thomas Schenke, Karl-Heinz Schlemmer, Jörg Keldenich, Erwin Bischoff, Elisabeth Perzborn, Klaus Dembowsky, Peter Serno, Marc Nowakowski
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Publication number: 20110003820Abstract: The invention relates to pyrazolopyrimidine derivatives as well as their pharmaceutically acceptable salts. The invention further relates to a process for the preparation of such compounds. The compounds of the invention are mGluR5 modulators and are therefore useful for the control and prevention of acute and/or chronic neurological disorders.Type: ApplicationFiled: January 30, 2009Publication date: January 6, 2011Applicant: MERZ PHARMA GMBH & CO. KGaAInventors: Markus Henrich, Tanja Weil, Sibylle Muller, Jens Nagel, Andreas Gravius, Valerjans Kauss, Ronalds Zemribo, Elina Erdmane
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Publication number: 20100324037Abstract: A compound of formula A having improved non-specific binding characteristics and pharmacokinetic properties is provided: or a pharmaceutically acceptable salt, stereoisomer, or hydrate thereof.Type: ApplicationFiled: August 23, 2007Publication date: December 23, 2010Applicant: SURFACE LOGIX, INC.Inventors: Stewart Campbell, David Duffy, Michael Grogan, Steven Kates, Emanuele Ostuni, Olivier Schueller, Paul Sweetnam
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Patent number: 7855206Abstract: The present invention is directed to novel substituted tricyclic heteroaromatic compounds of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. 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 dipeptidyl peptidase-IV enzyme is involved.Type: GrantFiled: November 9, 2007Date of Patent: December 21, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Jason M. Cox, Hong Dong
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Patent number: 7838672Abstract: The use of fused ring-1,2,4-benzotriazine derivatives as herbicides or plant growth regulators for the control of undesired plants or vegetation, compounds and compositions thereof, and processes for their preparation. The invention relates to the use of a compound of the formula (I) or a salt thereof: wherein A-W, X, Y, Z, R1, R2, R3 and R4 are defined in the description, as herbicides or plant growth regulators for the control of undesired plants or vegetation, to compounds and compositions thereof, and to processes for their preparation.Type: GrantFiled: July 17, 2004Date of Patent: November 23, 2010Assignee: Bayer CropScience GmbHInventors: Arnim Kohn, Wolfgang Giencke, Hendrick Helmke, Kenneth Garcia Marques, Thomas Auler, Martin Hills, Gyorgy Hajos, Zsuzsanna Riedl, Dieter Feucht