- Benzylamine derivatives and its application on the medicament
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The invention provides novel benzylamine derivatives or stereoisomers, geometric isomers, tautomers, nitrogen oxides, hydrates, solvates, metabolites and pharmaceutically acceptable salts or pro-drugs thereof for treating Alzheimer diseases. The invention also provides a medicine composition containing a compound provided by the invention and a method for treating the Alzheimer diseases by using the compound or the medicine composition of the compound provided by the invention.
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Paragraph 0164; 0166; 0167
(2017/08/25)
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- Substituted heterocyclic compound and its application on the medicament
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The invention provides a novel substituted heterocyclic compound or stereisomers, stereomers, tautomers, oxynitrides, hydrates, solvates, metabolites, and pharmaceutically acceptable salts or prodrugs thereof. The novel substituted heterocyclic compound i
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Paragraph 0205; 0206; 0207; 0208
(2016/10/09)
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- A new fluorescent "turn-on" chemodosimeter for cyanide based on dual reversible and irreversible deprotonation of NH and CH groups
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A new fluorescent "turn-on" cyanide chemodosimeter 5 was developed for the first time based on the irreversible deprotonation/oxidation of the CH group followed by the reversible deprotonation of the NH group, with high selectivity and dramatic red-shifted absorption (≈263 nm). The photoinduced electron transfer (PET) is prevented by the irreversible process, which results in coplanar geometry between indole and naphthalimide causing enhancement of fluorescence.
- Zhang, Chuanxiu,Liu, Chuanxiang,Li, Baiyun,Chen, Jinju,Zhang, Hua,Hu, Zhou,Yi, Fengping
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p. 1968 - 1973
(2015/03/18)
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- TETRACYCLIC AUTOTAXIN INHIBITORS
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Described herein are compounds that are autotaxin inhibitors, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with autotaxin activity.
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Paragraph 00395
(2015/06/08)
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- FSH RECEPTOR ANTAGONISTS
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The invention relates to FSH receptor antagonist according to general formula (I) or a pharmaceutically acceptable salt thereof and to a pharmaceutical composition containing the same. The compounds can be used for the treatment and prevention of endometriosis, for the treatment and prevention of pre-menopausal and peri-menopausal hormone-dependent breast cancer, for contraception, and for the treatment of uterine fibroids and other menstrual-related disorders
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Page/Page column 31
(2013/04/10)
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- Synthesis of the tetracyclic core skeleton of the lundurines by a gold-catalyzed cyclization
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The 1H-azocino[5,4-b]indole skeleton of the lundurines has been prepared by the 8-endo-dig cyclization of an alkynylindole using AuCl3 or other gold complexes as catalysts.
- Ferrer, Catalina,Escribano-Cuesta, Ana,Echavarren, Antonio M.
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experimental part
p. 9015 - 9020
(2009/12/24)
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- Discovery of XL335 (WAY-362450), a highly potent, selective, and orally active agonist of the farnesoid X receptor (FXR)
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Azepino[4,5-b]indoles have been identified as potent agonists of the farnesoid X receptor (FXR). In vitro and in vivo optimization has led to the discovery of 6m (XL335, WAY-362450) as a potent, selective, and orally bioavailable FXR agonist (EC50 = 4 nM, Eff = 149%). Oral administration of 6m to LDLR-/- mice results in lowering of cholesterol and triglycerides. Chronic administration in an atherosclerosis model results in significant reduction in aortic arch lesions.
- Flatt, Brenton,Martin, Richard,Wang, Tie-Lin,Mahaney, Paige,Murphy, Brett,Gu, Xiao-Hui,Foster, Paul,Li, Jiali,Pircher, Parinaz,Petrowski, Mary,Schulman, Ira,Westin, Stefan,Wrobel, Jay,Yan, Grace,Bischoff, Eric,Daige, Chris,Mohan, Raju
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supporting information; experimental part
p. 904 - 907
(2009/12/24)
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- AZEPINOINDOLE DERIVATIVES AS PHARMACEUTICAL AGENTS
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The present invention relates to compounds of formula I, which exhibit affinity for the farnesoid X receptor.
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Page/Page column 110; 111; 117
(2008/06/13)
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- NOVEL TRICYCLIC HETEROCYCLE COMPOUND
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―The present invention relates to the compound represented by formula (I) ????????A―X―Y―Z―B?????(I) (wherein A is a cyclic group which may have a substituent(s); X is a single bond or a spacer; Y is a single bond or a spacer; Z is a single bond or a spacer; B is a hydrocarbon group which may have a substituent(s) or a cyclic group which may have a substituent(s)), a salt thereof, a solvate thereof or a prodrug thereof. The compound represented by formula (I), a salt thereof, a solvate thereof or a prodrug thereof is useful for preventive and/or therapeutic agent for a disease caused by stress.
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Page/Page column 58
(2008/06/13)
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- Azepinoindole derivatives as pharmaceutical agents
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Compounds, compositions and methods for modulating the activity of receptors are provided. In particular, compounds and compositions are provided for modulating the activity of receptors and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder directly or indirectly related to the activity of the receptors.
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- Structure-activity relationship study of novel necroptosis inhibitors
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Necroptosis is a regulated caspase-independent cell death mechanism that results in morphological features resembling necrosis. It can be induced in a FADD-deficient variant of human Jurkat T cells treated with TNF-α. 5-(1H-Indol-3-ylmethyl)-2-thiohydantoins and 5-(1H-indol-3-ylmethyl)hydantoins were found to be potent necroptosis inhibitors (called necrostatins). A SAR study revealed that several positions of the indole were intolerant of substitution, while small substituents at the 7-position resulted in increased inhibitory activity. The hydantoin ring was also quite sensitive to structural modifications. A representative member of this compound class demonstrated moderate pharmacokinetic characteristics and readily entered the central nervous system upon intravenous administration.
- Teng, Xin,Degterev, Alexei,Jagtap, Prakash,Xing, Xuechao,Choi, Sungwoon,Denu, Regine,Yuan, Junying,Cuny, Gregory D.
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p. 5039 - 5044
(2007/10/03)
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- Beta-carbolines useful for treating inflammatory disease
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This invention provides beta-carboline compounds of formula III-A-aa: wherein Q, G, R1, R2, R3, and R6b are as described in the specification. The compounds are useful for treating diseases such as inflammatory diseases and cancer.
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Page/Page column 99
(2010/02/14)
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- BETA-CARBOLINES USEFUL FOR TREATING INFLAMMATORY DISEASE
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This invention provides beta-carboline compounds of formula (I) wherein Ring A is a substituted pyridinyl, pyrimidinyl, morpholinyl, piperidinyl, piperazinyl, pyrrolidinyl, pyranyl, tetrahydrofuranyl, cyclohexyl, cyclopentyl or thiomorpholinyl ring and R1, R2 and R3 are as described in the specification. The compounds are IKK-2 inhibitors that are useful for treating IKK-2 mediated diseases such as inflammatory diseases and cancer.
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- Kinase inhibitors
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Compounds having the formula are useful for inhibiting protein kinases. Also disclosed are compositions which inhibit protein kinases and methods of inhibiting protein kinases in a patient.
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- Kinase inhibitors
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Compounds having the formula are useful for inhibiting protein kinases. Also disclosed are compositions which inhibit protein kinases and methods of inhibiting protein kinases in a patient.
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Page/Page column 28
(2010/01/31)
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- AZEPINOINDOLE AND PYRIDOINDOLE DERIVATIVES AS PHARMACEUTICAL AGENTS
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The present invention is directed to compounds of formula (I) and formula (II): formula (I) and (II), wherein R1-R8, A and n are as described in the description. These compounds are used in pharmaceutical compositions and methods for modulating the activity of orphan nuclear receptors.
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Page 131-132
(2008/06/13)
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- Conformationally constrained amino-acids: Synthesis of novel β, β-, 2,3-, and 3,4-cyclised tryptophans
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The synthesis of novel, conformationally constrained tryptophan mimetics is described.
- Horwell, David C.,McKiernan, Mary J.,Osborne, Simon
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p. 8729 - 8732
(2007/10/03)
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