817-71-0Relevant articles and documents
COMPLEMENT MODULATORS AND RELATED METHODS
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Paragraph 0497, (2020/10/20)
The present disclosure presents compounds and compositions that interact with complement components. Some compounds inhibit complement activity. Included are small molecule compounds and compositions that function as C5 inhibitor compounds. Methods for inhibiting complement activity and methods of treating complement-related indications with the C5 inhibitor compounds and compositions are provided.
Synthesis of 5-aminolevulinic acid with nontoxic regents and renewable methyl levulinate
Zai, Yuxia,Feng, Yunchao,Zeng, Xianhai,Tang, Xing,Sun, Yong,Lin, Lu
, p. 10091 - 10093 (2019/04/10)
Synthesis of 5-aminolevulinic acid (5-ALA) was presented with novel bromination of biobased methyl levulinate (ML), followed by ammoniation and hydrolysis. Copper bromide (CuBr2) was employed as the bromination reagent with higher selectivity and activity instead of the conventional liquid bromine (Br2). 5-ALA was obtained in a high yield (64%) and purity (>95%) by optimum design, which is of great potential in industrialization.
VISUAL CYCLE MODULATORS
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Paragraph 00155, (2018/09/19)
A method of treating an ocular disorder in a subject in need thereof includes administering to the subject a therapeutically effective amount of a retinal sequestering compound of formula (I).
Rational tuning of visual cycle modulator pharmacodynamics
Kiser, Philip D.,Zhang, Jianye,Palczewski, Krzysztof,Badiee, Mohsen,Tochtrop, Gregory P.,Peachey, Neal S.,Kinoshita, Junzo
, p. 131 - 145 (2017/06/29)
Modulators of the visual cycle have been developed for treatment of various retinal disorders. These agents were designed to inhibit retinoid isomerase [retinal pigment epithelium-specific 65 kDa protein (RPE65)], the rate-limiting enzyme of the visual cy
INHIBITING THE TRANSIENT RECEPTOR POTENTIAL A1 ION CHANNEL
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Page/Page column 129; 130, (2016/04/09)
The present invention relates to pharmaceutical compounds of the Formula (I), or a pharmaceutically acceptable salt or composition thereof, and methods of their use for the treatment of pain, respiratory conditions, as well as inhibiting the Transient Receptor Potential Al ion channel (TRPA1).
CXCR4 Receptor Antagonists
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Paragraph 0125; 0126, (2013/11/06)
Disclosed are compounds that are antagonists of the CXCR4 receptor.
Bromination of enamines from tertiary amides using the petasis reagent: A convenient one-pot regioselective route to bromomethyl ketones
Kobeissi, Marwan,Cherry, Khalil,Jomaa, Wissam
supporting information, p. 2955 - 2965 (2013/09/02)
An original one-pot synthesis of bromomethyl ketones is achived using the Petasis reagent (dimethyltitanocene) as a key for enamine generation. Several amides were used to test the limits of the procedure by changing either the alkyl chain R or the amino portion of the starting materials. The enamines generated in situ were allowed to react with bromine at low temperature followed by hydrolysis to yield bromomethyl ketones in excellent yields (85 to 95%). Mechanistic details and optimum conditions for the reaction are briefly discussed. The present approach offers several advantages such as regioselectivity in enamine formation, good yields, mild reaction conditions, and ease of experimentation.
CXCR4 RECEPTOR ANTAGONISTS
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Page/Page column 34-35, (2012/05/04)
The compounds of formula (I) are antagonists of the CXCR4 receptor Wherein R1, X, Y and R2 are as defined in the claims.
Discovery of imidazo[1,2-a]pyridines as potent MCH1R antagonists
Kishino, Hiroyuki,Moriya, Minoru,Sakuraba, Shunji,Sakamoto, Toshihiro,Takahashi, Hidekazu,Suzuki, Takao,Moriya, Ryuichi,Ito, Masahiko,Iwaasa, Hisashi,Takenaga, Norihiro,Ishihara, Akane,Kanatani, Akio,Sato, Nagaaki,Fukami, Takehiro
scheme or table, p. 4589 - 4593 (2010/04/25)
A series of imidazo[1,2-a]pyridine derivatives was identified and evaluated for MCH1R binding and antagonistic activity. Introduction of a methyl substituent at the 3-position of imidazo[1,2-a]pyridine provided compounds with a significant improvement in MCH1R affinity. Representative compounds in this series exhibited good potency and brain exposure in rats.
A mild and efficient procedure for α-bromination of ketones using N-bromosuccinimide catalysed by ammonium acetate
Tanemura, Kiyoshi,Suzuki, Tsuneo,Nishida, Yoko,Satsumabayashi, Koko,Horaguchi, Takaaki
, p. 470 - 471 (2007/10/03)
Cyclic ketones reacted with N-bromosuccinimide (NBS) catalysed by NH 4OAc in Et2O at 25°C to give the corresponding α-brominated ketones in good yields, while acyclic ketones were efficiently brominated in CCl4 at 80°C.