- AMINO ALCOHOL DERIVATIVE, PHARMACEUTICAL COMPOSITION AND APPLICATION THEREOF
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The present invention belongs to the field of medicine, and specifically discloses an amino alcohol derivative represented by Formula I, a pharmaceutically acceptable salt, solvate, polymorph or prodrug thereof. In addition, the present invention also discloses a pharmaceutical composition comprising the above substances, and a use of the substance in the preparation of a medicament for the prevention and treatment of an immune inflammatory disease, or a disease or condition associated with immunological competence such as multiple sclerosis, ALS, CIDP, systemic lupus erythematosus, rheumatoid arthritis, ulcerative colitis, psoriasis, polymyositis, etc.
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Paragraph 0169; 0171; 0172
(2021/11/13)
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- 3-cyano-4-alcoholate benzoate synthesis method
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The invention discloses a 3-cyano-4-alcoholate benzoate synthesis method. The general formula for the reaction is shown in the description, wherein R1 is isopropyl or other alkyls, and R2 is alkyl. The reaction condition of the method is mild, the raw materials are easy to get, the yield is high, the post-processing is simple, and the method provides an important reference for the industrial production.
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Paragraph 0025; 0032-0034
(2018/07/30)
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- OXADIAZOLE MODULATORS OF S1P METHODS OF MAKING AND USING
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The invention is directed to Compounds of Formula (I): wherein each variable is defined herein, as well as methods of making and using the compounds as agonists of S1P1 and/or S1P5 for instance for treating graft versus host disease and autoimmune diseases.
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Paragraph 0158
(2017/01/23)
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- Preparation method of 3-cyano-4-isopropoxy methyl benzoate
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The invention discloses a preparation method of 3-cyano-4-isopropoxy methyl benzoate. The preparation method comprises the following steps: step I, preparing 3-aldehyde-4-methyl hydroxybenzoate from methyl p-hydroxybenzoate; step II, preparing 3-cyano-4-m
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Paragraph 0012; 0019
(2017/08/29)
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- Method for preparing 3-cyano-4-isopropoxybenzoic acid
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The invention discloses a method for preparing 3-cyano-4-isopropoxybenzoic acid. A first step, 3-formyl-4-methyl hydroxybenzoate is prepared with methyl parahydroxybenzoate; a second step, 3-cyano-4-methyl hydroxybenzoate is prepared with the 3-formyl-4-methyl hydroxybenzoate; a third step, 3-cyano-4-methyl isopropoxybenzoate is prepared with the 3-cyano-4-methyl hydroxybenzoate; a fourth step, the 3-cyano-4-isopropoxybenzoic acid is prepared with the 3-cyano-4-methyl isopropoxybenzoate. The preparation method of the 3-cyano-4-isopropoxybenzoic acid, which is provided by the invention, has the advantages that 1) the use of the cuprous cyanide of hypertoxic cyanide in a previous process is avoided, and the method is more suitable for industrialization; 2) cyano is prepared by formyl, and the method is high-efficiency and direct, and is suitable for quantity production; 3) all raw materials are cheap and easily obtained, and the cost advantage is obvious.
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Paragraph 0021
(2017/08/29)
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- DEUTERIUM-SUBSTITUTED OXADIAZOLES
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Described are deuterated modulators of S1P1 receptors, pharmaceutical compositions thereof, and methods of use thereof.
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Paragraph 0142
(2016/10/31)
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- OXADIAZOLE SUBSTITUTED INDAZOLE DERIVATIVES FOR USE AS SPHINGOSINE 1-PHOSPHATE 1 (S1P1) RECEPTOR AGONISTS
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Oxadiazole substituted indazole derivatives of formula (I) or pharmaceutical salts thereof having pharmacological activity, processes for their preparation, pharmaceutical compositions containing them and their uses in the treatment of various disorders mediated by S1P1 receptors are disclosed.
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Page/Page column 17
(2012/11/13)
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- TRICYCLIC HETEROCYCLIC COMPOUNDS
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Disclosed are compounds of Formula (I) or stereoisomers or salts thereof, wherein: X1, X2, X3, W, Q1, Q2, and G2 are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
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Page/Page column 142
(2011/06/16)
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- OXADIAZOLE SUBSTITUTED INDAZOLE DERIVATIVES FOR USE AS SPHINGOSINE 1-PHOSPHATE 1 (S1P1) RECEPTOR AGONISTS
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Oxadiazole substituted indazole derivatives of formula (I) or pharmaceutical salts thereof having pharmacological activity, processes for their preparation, pharmaceutical compositions containing them and their uses in the treatment of various disorders mediated by S1P1 receptor are disclosed.
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Page/Page column 16; 25-26
(2011/07/07)
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- Modulators of S1P and Methods of Making And Using
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The invention is directed to Compounds of Formula I: as well as methods of making and using the compounds.
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Page/Page column 60-61
(2010/10/19)
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- CERTAIN CHEMICAL ENTITIES, COMPOSITIONS, AND METHODS
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Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of one or more mitotic kinesins are disclosed.
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Page/Page column 52-53
(2010/11/27)
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- CERTAIN CHEMICAL ENTITIES, COMPOSITIONS, AND METHODS
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Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of one or more mitotic kinesins are disclosed.
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Page/Page column 194-220
(2008/06/13)
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- (3,4-DISUBSTITUTED)PROPANOIC CARBOXYLATES AS S1P (EDG) RECEPTOR AGONISTS
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The present invention encompasses compounds of Formula A: A as well as the pharmaceutically acceptable salts thereof. The compounds are S1P1/Edg1 receptor agonists and thus have immunosuppressive, anti-inflammatory and hemostatic activities by modulating leukocyte trafficking, sequestering lymphocytes in secondary lymphoid tissues, and enhancing vascular integrity. The invention is also directed to pharmaceutical compositions containing such compounds and methods of treatment or prevention.
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Page/Page column 46-47
(2008/06/13)
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- Tetrahydronaphthyridinyl-carboxamides having anti-convulsant activity
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Compounds of formula (I) and pharmaceutically acceptable salts and solvates: where R1is hydrogen, C1-6alkyl (optionally substituted by hydroxy or C1-4alkoxy), phenyl-C1-4alkyl-, C1-6alkenyl, C1-6
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- Substituted isoquinoline derivatives and their use as anticonvulsivants
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This invention relates to novel substituted isoquinoline derivatives and their use as anticonvulsants.
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