- 6-HETEROARYLOXY BENZIMIDAZOLES AND AZABENZIMIDAZOLES AS JAK2 INHIBITORS
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The present disclosure provides 6-heteroaryloxy benzimidazole and azabenzimidazole compounds and compositions thereof useful for inhibiting JAK2.
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Paragraph 0434; 0437
(2021/11/13)
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- Enantioselective Construction of Sulfur-Containing Tetrasubstituted Stereocenters via Asymmetric Functionalizations of α-Sulfanyl Cyclic Ketones
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Asymmetric functionalizations of α-sulfanyl cyclic ketones were realized via chiral phosphoric acid catalyzed enantioselective addition reactions with aldimines, azodicarboxylates and allenamides. A series of chiral organosulfur compounds possessing sulfur-containing tetrasubstituted stereocenters were accessed via these methods, with excellent regioselectivities and high stereoselectivities. (Figure presented.).
- Ye, Xueqian,Pan, Yongkai,Chen, Yunrong,Yang, Xiaoyu
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supporting information
p. 3374 - 3379
(2020/07/16)
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- Discovery of cycloalkyl-fused N-thiazol-2-yl-benzamides as tissue non-specific glucokinase activators: Design, synthesis, and biological evaluation
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Glucokinase (GK) activators are being developed for the treatment of type 2 diabetes mellitus (T2DM). However, existing GK activators have risks of hypoglycemia caused by over-activation of GK in islet cells and dyslipidemia caused by over-activation of intrahepatic GK. In the effort to mitigate risks of hypoglycemia and dyslipidemia while maintaining the promising efficacy of GK activator, we investigated a series of cycloalkyl-fused N-thiazol-2-yl-benzamides as tissue non-specific partial GK activators, which led to the identification of compound 72 that showed a good balance between in vitro potency and enzyme kinetic parameters, and protected β-cells from streptozotocin-induced apoptosis. Chronic treatment of compound 72 demonstrated its potent activity in regulation of glucose homeostasis and low risk of dyslipidemia with diabetic db/db mice in oral glucose tolerance test (OGTT). Moreover, acute treatment of compound 72 did not induce hypoglycemia in C57BL/6J mice even at 200 mg/kg via oral administration.
- Wang, Zhengyu,Shi, Xiaofan,Zhang, Huan,Yu, Liang,Cheng, Yanhua,Zhang, Hefeng,Zhang, Huibin,Zhou, Jinpei,Chen, Jing,Shen, Xu,Duan, Wenhu
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p. 128 - 152
(2017/08/10)
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- Cyclic Urea Derivatives As Androgen Receptor Antagonists
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The present invention is directed to compounds of formula (I) wherein R1, R2, R3, and A are defined herein. The present invention also provides for pharmaceutical compositions comprising a compound of formula (I) as well as to the use of such compounds as androgen receptor antagonists for the treatment of diseases and conditions mediated by the androgen receptor, such as prostate cancer.
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Paragraph 0432; 0433
(2014/11/13)
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- CYCLIC UREA DERIVATIVES AS ANDROGEN RECEPTOR ANTAGONISTS
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The present invention is directed to compounds of formula (I) wherein R1, R2, R3, and A are defined herein. The present invention also provides for pharmaceutical compositions comprising a compound of formula (I) as well as to the use of such compounds as androgen receptor antagonists for the treatment of diseases and conditions mediated by the androgen receptor, such as prostate cancer.
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Page/Page column 73
(2013/06/27)
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- COMPOUNDS FOR THE REDUCTION OF β-AMYLOID PRODUCTION
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The present disclosure provides a series of compounds of the formula (I), which modulate β-amyloid peptide (β-ΑΡ) production and are useful in the treatment of Alzheimer's Disease and other conditions affected by β-amyloid peptide (β-ΑΡ) production.
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Page/Page column 74
(2012/08/08)
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- Synthesis of quinoxaline analogues
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Substituted tricyclic or tetracyclic quinoxalines, tricyclic pyridoquinoxalines and bis-quinoxalines were synthesized in high yields starting from cyclic ketones by the -bromination of cyclic ketones with N-bromosuccinimide (NBS) followed by condensation of the resulting -bromo ketones with 1,2-diaminobenzene, 3,4-diaminopyridine, or 3,3-diaminobenzidine. Georg Thieme Verlag Stuttgart New York.
- Chang, Meng-Yang,Lee, Tein-Wei,Hsu, Ru-Ting,Yen, Tzu-Lin
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experimental part
p. 3143 - 3151
(2011/10/30)
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- COMPOUNDS FOR THE REDUCTION OF β-AMYLOID PRODUCTION
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The present disclosure provides a series of compounds of the formula (I) which modulate β-amyloid peptide (β-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions affected by β-amyloid peptide (β-AP) production.
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Page/Page column 89-90
(2011/02/24)
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- OXOPIPERIDINYL AND PYRANYL SULFONAMIDES AS AMPA POTENTIATORS
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The invention is directed to a class of compounds, including the pharmaceutically acceptable salts of the compounds, having the structure of Formula (I) : as defined in the specification. The invention is also directed to compositions containing the compo
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Page/Page column 50-51
(2010/04/27)
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- CYCLOALKYLIDENE AND HETEROCYCLOALKYLIDENE INHIBITOR COMPOUNDS
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The present invention provides a compound of general Formula (I) having histone deacetylase (HDAC) inhibitory activity, a pharmaceutical composition comprising the compound, and a method useful to treat diseases using the compound.
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Page/Page column 93-94
(2010/02/17)
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- Azole derivatives as histamine H3 receptor antagonists, Part I: Thiazol-2-yl ethers
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Most human histamine H3 receptor (hH3R) antagonists follow a general structural blueprint, containing a basic moiety linked by a spacer to a substituted core element. In this investigation the acceptance of thiazol-2-yl ether moieties in the core region is proved with some ether derivatives showing hH3R binding affinities in the nanomolar concentration range. A diversity of structural motifs is used as substituents to enhance the in vitro hH3R binding affinity.
- Walter,Von Coburg,Isensee,Sander,Ligneau,Camelin,Schwartz,Stark
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supporting information; experimental part
p. 5879 - 5882
(2010/11/18)
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- SULFONAMIDES AND PHARMACEUTICAL COMPOSITIONS THEREOF
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The invention is directed to a class of compounds, including the pharmaceutically acceptable salts of the compounds, having the structure of formula (I), as defined in the specification. The invention is also directed to compositions containing the compounds of formula (I).
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Page/Page column 65; 110-111
(2008/12/04)
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- GUANIDINE DERIVATIVES AND USE THEREOF AS NEUROPEPTIDE FF RECEPTOR ANTAGONISTS
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The invention relates to guanidine derivatives of formula (I) where: A = a chain of 3-c6 carbon atoms, one of which can be replaced by -N(R')- or -O- and R' = H or a substituent, where the ring skeleton only contains both double bonds of the thiazole component, the pharmaceutically-acceptable acid addition salts of basic compounds of formula (I), the pharmaceutically-acceptable salts of compounds of formula (I),, comprising acid groups, with bases, the pharmaceutically-acceptable esters of hydroxy or carboxyl group containing compounds of formula (I) and the solvates or hydrates thereof, which are partly known and partly novel and exhibit a neuropeptide FF receptor antagonist effect. The above are suitable for the treatment of pain and hyperalgesia, withdrawal symptoms in alcohol, psychotropic and nicotine dependencies, for improvement or cure of said dependencies, for regulation of insulin excretion, food intake, memory functions, blood pressure, electrolyte and energy management and for treatment of urinary incontinence. The above can be produced using generally used methods and processed to give medicaments.
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- SULFONYLPHENYLPYRAZOLE COMPOUNDS USEFUL AS COX-2 INHIBITORS
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The present invention encompasses novel sulfonylphenylpyrazole compounds useful in the treatment of cyclooxygenase-2 mediated diseases.
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- Sulfonylphenylpyrazole compounds useful as COX-2 inhibitors
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The present invention encompasses novel sulfonylphenylpyrazole compounds useful in the treatment of cyclooxygenase-2 mediated diseases.
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