- COMPLEMENT MODULATORS AND RELATED METHODS
-
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.
- -
-
Paragraph 0497
(2020/10/20)
-
- Synthesis of 5-aminolevulinic acid with nontoxic regents and renewable methyl levulinate
-
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.
- Zai, Yuxia,Feng, Yunchao,Zeng, Xianhai,Tang, Xing,Sun, Yong,Lin, Lu
-
p. 10091 - 10093
(2019/04/10)
-
- VISUAL CYCLE MODULATORS
-
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).
- -
-
Paragraph 00155
(2018/09/19)
-
- Rational tuning of visual cycle modulator pharmacodynamics
-
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
- Kiser, Philip D.,Zhang, Jianye,Palczewski, Krzysztof,Badiee, Mohsen,Tochtrop, Gregory P.,Peachey, Neal S.,Kinoshita, Junzo
-
p. 131 - 145
(2017/06/29)
-
- INHIBITING THE TRANSIENT RECEPTOR POTENTIAL A1 ION CHANNEL
-
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).
- -
-
Page/Page column 129; 130
(2016/04/09)
-
- Bromination of enamines from tertiary amides using the petasis reagent: A convenient one-pot regioselective route to bromomethyl ketones
-
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.
- Kobeissi, Marwan,Cherry, Khalil,Jomaa, Wissam
-
supporting information
p. 2955 - 2965
(2013/09/02)
-
- CXCR4 Receptor Antagonists
-
Disclosed are compounds that are antagonists of the CXCR4 receptor.
- -
-
Paragraph 0125; 0126
(2013/11/06)
-
- CXCR4 RECEPTOR ANTAGONISTS
-
The compounds of formula (I) are antagonists of the CXCR4 receptor Wherein R1, X, Y and R2 are as defined in the claims.
- -
-
Page/Page column 34-35
(2012/05/04)
-
- Discovery of imidazo[1,2-a]pyridines as potent MCH1R antagonists
-
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.
- 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 mild and efficient procedure for α-bromination of ketones using N-bromosuccinimide catalysed by ammonium acetate
-
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.
- Tanemura, Kiyoshi,Suzuki, Tsuneo,Nishida, Yoko,Satsumabayashi, Koko,Horaguchi, Takaaki
-
p. 470 - 471
(2007/10/03)
-
- Induction period in the BrO3 -, Ce(III), H2SO4, oxalic acid and ketone oscillating reaction
-
Contrary to what has been thought, systems classified as bromine- hydrolysis-controlled (BHC) show an induction period. In studies on the effect of a family of ketones upon this type of oscillators, it was found that an induction period appears in an interval of concentrations of the ketone, or in an interval of the value of the enolization constant. Simulations of the processes involved and a corresponding explanation are shown in this paper.
- Berenstein, Igal,Agreda, Jesus,Barragan, Daniel
-
p. 4601 - 4603
(2007/10/03)
-
- Selective bromination of ketones. A convenient synthesis of 5-aminolevulinic acid
-
Bromination of unsymmetrical ketones with Br2 in methanol proceeded regioselectively in good yield at the less substituted methyl carbon. The bromination of levulinic acid using this method was followed by azidation and amination to lead to an efficient three-step synthesis of 5-aminolevulinic acid in 36% overall yield.
- Ha,Lee,Ha,Park
-
p. 2557 - 2562
(2007/10/02)
-
- Phenoxypropanolamine compounds
-
Compounds of the formula (I): STR1 wherein R1 is hydrogen or fluoro and R2 is hydrogen or C1-6 alkyl and salts thereof are described as agents for the treatment of obesity and related conditions. Processes for their preparation and intermediates are described.
- -
-
-
- ANTI-EMETIC QUINUCLIDINYL BENZAMIDES
-
Novel substituted benzamides of the formula STR1 wherein R. sup.1, R 2, R 3, R 4, R 5 and A are as defined herein are useful in the treatment of emesis, and particularly chemotherapy-induced emesis in cancer patients. Some of the compounds are also useful
- -
-
-
- Synthesis of three retinal models, including the 10-s-cis-locked retinal, all-E-12,19-methanoretinal
-
All-E-12,19-methanoretinal (1) is distinguished by the presence of the locked 10-s-cis conformation in the cyclohexadiene ring in the conjugated chain. 1 has been prepared together with its 13-Z isomer in an overall yield of 0.5percent. 1 and 13-Z-1 photochemically interconvert in a clean way.In this system, only photoisomerization around the C13=C14 double bond is observed.In the photostationary state, the 13-Z isomer is predominant.All-E-12-ethyl-19-methylretinal (2) and all-E-12-ethylretinal (3) were prepared in good overall yields (20percent and 30percent) from β-ionone using the novel synthon, 3-methyl-4-(diethylphosphono)-2-hexenenitrile (11).The photochemistry of these retinal derivatives is very similar to that of retinal.The 9-Z, 11-Z and 13Z isomers of 2 and 3 were photochemically prepared.The 13C NMR spectra of these new compounds gave information about the structural elements of alkyl groups in conjugated systems and about the conformation of the conjugated chain.
- Groesbeek, M.,Steen, R. van der,Vliet, J. C. van,Vertegaal, L. B. J.,Lugtenburg, J.
-
p. 427 - 436
(2007/10/02)
-
- Alkyne Formation in the Reaction of α-Bromo Ketones with Arylsulfonylhydrazines
-
Alkynes can be produced by treating some α-bromo ketones with arylsulfonylhydrazines.The reaction is acid-catalysed and mesitylsulfonylhydrazine was the most efficient hydrazine reagent examined.The mechanism of the reaction has not been elucidated although it is shown not to proceed via an α-bromo mesitylsulfonylhydrazone.
- Bryant, Michael W.,Smith, Robin A. J.,Wong, Lisa
-
p. 2529 - 2540
(2007/10/02)
-