- DEGRADATION OF ANDROGEN RECEPTOR (AR) BY CONJUGATION OF AR ANTAGONISTS WITH E3 LIGASE LIGAND AND METHODS OF USE
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Provided herein are novel bifunctional compounds formed by conjugating AR antagonist moieties with E3 ligase Ligand moieties, which function to recruit targeted proteins to E3 Ubiquitin ligase for degradation, and methods of preparation and uses thereof.
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Paragraph 0138-0140
(2021/04/02)
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- KRAS G12C INHIBITORS
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The present invention relates to compounds that inhibit KRas G12C. In particular, the present invention relates to compounds that irreversibly inhibit the activity of KRas G12C, pharmaceutical compositions comprising the compounds and methods of use therefor.
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Paragraph 0701-0702
(2019/05/24)
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- KRAS G12C INHIBITORS
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The present invention relates to compounds that inhibit KRas G12C. In particular, the present invention relates to compounds that irreversibly inhibit the activity of KRas G12C, pharmaceutical compositions comprising the compounds and methods of use therefor.
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Paragraph 0416
(2017/12/18)
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- ANTI-ANGIOGENESIS COMPOUND, INTERMEDIATE AND USE THEREOF
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Disclosed are an anti-abnormal proliferation of angiogenesis compound represented by formula I, use and intermediate thereof. The compound has good effect against abnormal proliferation of angiogenesis, and the activity of the compound is produced by inhibiting VEGFR2. The compound can be used for treating diseases, such as wet macular degeneration, inflammation, malignant tumor and the like, caused by abnormity of angiogenesis and protein kinases such as VEGFR2, FGFR2 and the like.
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- ANTI-ANGIOGENESIS COMPOUND, INTERMEDIATE AND USE THEREOF
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Disclosed are an anti-abnormal proliferation of angiogenesis compound represented by formula I, use and intermediate thereof. The compound has good effect against abnormal proliferation of angiogenesis, and the activity of the compound is produced by inhibiting VEGFR2. The compound can be used for treating diseases, such as wet macular degeneration, inflammation, malignant tumor and the like, caused by abnormity of angiogenesis and protein kinases such as VEGFR2, FGFR2 and the like.
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- Discovery of Oral VEGFR-2 Inhibitors with Prolonged Ocular Retention That Are Efficacious in Models of Wet Age-Related Macular Degeneration
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The benefit of intravitreal anti-VEGF therapy in treating wet age-related macular degeneration (AMD) is well established. Identification of VEGFR-2 inhibitors with optimal ADME properties for an ocular indication provides opportunities for dosing routes beyond intravitreal injection. We employed a high-throughput in vivo screening strategy with rodent models of choroidal neovascularization and iterative compound design to identify VEGFR-2 inhibitors with potential to benefit wet AMD patients. These compounds demonstrate preferential ocular tissue distribution and efficacy after oral administration while minimizing systemic exposure.
- Meredith, Erik L.,Mainolfi, Nello,Poor, Stephen,Qiu, Yubin,Miranda, Karl,Powers, James,Liu, Donglei,Ma, Fupeng,Solovay, Catherine,Rao, Chang,Johnson, Leland,Ji, Nan,Artman, Gerald,Hardegger, Leo,Hanks, Shawn,Shen, Siyuan,Woolfenden, Amber,Fassbender, Elizabeth,Sivak, Jeremy M.,Zhang, Yiqin,Long, Debby,Cepeda, Rosemarie,Liu, Fang,Hosagrahara, Vinayak P.,Lee, Wendy,Tarsa, Peter,Anderson, Karen,Elliott, Jason,Jaffee, Bruce
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p. 9273 - 9285
(2015/12/23)
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- P2X7 MODULATORS
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The present invention is directed to a compound of Formula (I) The invention also relates to pharmaceutical compositions comprising compounds of Formula (I). Methods of making and using the compounds of Formula (I) are also within the scope of the invention.
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Paragraph 0156
(2014/09/30)
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- The Role of the acidity of N-heteroaryl sulfonamides as inhibitors of Bcl-2 family protein-protein interactions
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Overexpression of the antiapoptotic members of the Bcl-2 family of proteins is commonly associated with cancer cell survival and resistance to chemotherapeutics. Here, we describe the structure-based optimization of a series of N-heteroaryl sulfonamides t
- Touré, B. Barry,Miller-Moslin, Karen,Yusuff, Naeem,Perez, Lawrence,Doré, Michael,Joud, Carol,Michael, Walter,Dipietro, Lucian,Van Der Plas, Simon,McEwan, Michael,Lenoir, Francois,Hoe, Madelene,Karki, Rajesh,Springer, Clayton,Sullivan, John,Levine, Kymberly,Fiorilla, Catherine,Xie, Xiaoling,Kulathila, Raviraj,Herlihy, Kara,Porter, Dale,Visser, Michael
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p. 186 - 190
(2013/04/10)
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- SULFONAMIDES AS INHIBITORS OF BCL-2 FAMILY PROTEINS FOR THE TREATMENT OF CANCER
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The present invention includes novel compound and methods of treating a disease or disorder by antagonizing Bcl-2 family proteins, particularly compounds of Formula (I) or pharmaceutically acceptable salt thereof, as well as methods of treating a disease,
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- Pyridyloxyindoles Inhibitors of VEGF-R2 and Use Thereof for Treatment of Disease
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The invention relates to novel organic compounds of formula (I), and their use in the treatment of the animal or human body, to pharmaceutical compositions comprising a compound of formula I and to the use of a compound of formula I for the preparation of pharmaceutical compositions for use in the treatment of protein kinase dependent diseases, especially of proliferative diseases, such as in the treatment of tumour diseases and ocular neovascular diseases.
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Page/Page column 112
(2010/06/22)
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