- VASCULAR ADHESION PROTEIN-1 (VAP-1) MODULATORS AND THERAPEUTIC USES THEREOF
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Disclosed herein are small molecule Vascular Adhesion Protein- 1 (VAP-1) modulator compositions, pharmaceutical compositions, the use and preparation thereof.
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Paragraph 0221
(2020/01/24)
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- Imidazo ring PAR4 antagonist and medical applications thereof
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The invention relates to an imidazo ring compound represented by formula (I) or formula (II), or a pharmaceutically acceptable salt or ester or solvate thereof. The compound disclosed by the inventioncan be used for preparing medicines for preventing or treating thromboembolic diseases.
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Paragraph 0259; 0261; 0264
(2020/01/12)
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- TRICYCLIC INHIBITORS OF THE BCL6 BTB DOMAIN PROTEIN-PROTEIN INTERACTION AND USES THEREOF
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The present application relates to compounds of Formula (I) or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, to compositions comprising these compounds or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, and various uses in the treatment of diseases, disorders or conditions that are treatable by inhibiting interactions with BCL6 BTB, such as cancer.
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Paragraph 00251
(2019/07/13)
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- INHIBITORS OF THE BCL6 BTB DOMAIN PROTEIN-PROTEIN INTERACTION AND USES THEREOF
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The present application relates to compounds of Formula I (I) or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, to compositions comprising these compounds or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, and various uses in the treatment of diseases, disorders or conditions that are treatable by inhibiting interactions with BCL6 BTB, such as cancer.
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Paragraph 00302
(2019/08/29)
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- CONFORMATIONALLY-CONSTRAINED BIOISOSTERES OF CAFFEIC ACID, AND SYNTHESIS AND THERAPEUTIC USES
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A method of treating a disease condition in a mammal comprising administering a pharmacologically effective amount of a therapeutic, wherein the therapeutic includes a bioisosteres of caffeic acid. A pharmaceutical composition for treating a disease condition in a mammal comprising a first therapeutic that includes a bioisosteres of caffeic acid, wherein the condition may be breast cancer, and the pharmaceutical composition may include a second therapeutic for the disease condition that is not a bioisosteres of caffeic acid.
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Paragraph 0044
(2019/08/22)
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- C70 Fullerene-Catalyzed Metal-Free Photocatalytic ipso-Hydroxylation of Aryl Boronic Acids: Synthesis of Phenols
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A metal-free C70 fullerene-catalyzed method has been developed for the ipso-hydroxylation of aryl and heteroaryl boronic acids to corresponding phenols under photocatalytic conditions. The reaction proceeds under oxygen atmosphere and the mechanistic study revealed that C70 plays a critical role in the generation of reactive oxygen species in the presence of blue light. Reactions in the presence of 18O-labelled water and oxygen confirmed the generation of reactive oxygen species from oxygen molecule. Amine used as a reductant could be recovered in the form of imine. The current method is also applicable to the synthesis of aryl ethers in one-pot two-step process. (Figure presented.).
- Kumar, Inder,Sharma, Ritika,Kumar, Rakesh,Kumar, Rakesh,Sharma, Upendra
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supporting information
p. 2013 - 2019
(2018/04/02)
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- Novel use of amine compounds
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The invention provides a preparation method and novel use of amine compounds. Specifically, the invention provides compounds shown in the formula A or their optical isomers, racemes, solvates or pharmaceutically acceptable salts and a medical use thereof. The above compounds can be used for preparation of a pharmaceutical composition or a preparation. The pharmaceutical composition or preparationis used for (a) inhibiting a transient receptor potential channel protein TRPA1 and (b) treating diseases associated with the transient receptor potential channel protein, wherein each group is defined in the specification.
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Paragraph 0190; 0191; 0193; 0210; 0211; 0212; 0213
(2018/06/28)
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- The palladium/norbornene-catalyzed: Ortho -silylmethylation reaction: A practical protocol for ortho -functionalized one-carbon homologation of aryl iodides
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A palladium/norbornene-catalyzed ortho-silylmethylation reaction using of (iodomethyl)cyclohexyloxydimethylsilane as the electrophile was reported. The ((cyclohexyloxy)dimethylsilyl)methyl group was readily oxidized using the Fleming-Tamao process or by ceric ammonium nitrate to give benzylic alcohol derivatives. This method was successfully applied in a concise synthesis of a biaryl analogue of schisandrins.
- Sui, Xianwei,Ding, Linlin,Gu, Zhenhua
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supporting information
p. 13999 - 14002
(2016/12/09)
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- HETEROCYCLIC COMPOUNDS AS INHIBITORS OF CXCR2
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The present invention relates to compounds of formula (I) wherein R1, R2, X, Y and Z are as defined in the specification.
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Page/Page column 30
(2009/10/21)
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- Studies on the narciclasine alkaloids: Total synthesis of (+)- narciclasine and (+)-pancratistatin
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Enantioselective total syntheses of the antimmor alkaloids, (+)- narciclasine and (+)-pancratistatin, are reported. These syntheses feature a stereo- and regiocontrolled aryl enamide photocyclization to construct a common, advanced intermediate possessing a transfused BC substructure. Differential functional group interchange in the C-ring of this phenanthridone core structure allows for the production of the two target natural products in enantiomerically pure form.
- Rigby, James H.,Maharoof, Umar S. M.,Mateo, Mary E.
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p. 6624 - 6628
(2007/10/03)
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- Naphthalene anti-psoriatic agents
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Naphthalenes of the formula: STR1 wherein: m is 1 or 2; n is 1, 2, or 3; R1 is alkyl of one to seven carbon atoms or an optionally substituted phenyl; R2 is hydrogen, lower alkyl, lower alkoxy, optionally substituted phenyl, optionally substituted phenyl-lower-alkyl, optionally substituted phenyl-lower-alkoxy, amino, lower alkylamino, lower dialkylamino, halo, cyano, hydroxy, or lower alkylthio are useful in relieving psoriasis.
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- Benzylamine derivative
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There is provided a novel benzylamine derivative of the formula I: STR1 wherein R1 represents a hydrogen atom or a methyl group, X represents a hydrogen atom, a methyl group or a tosyl group, and Y represents a hydrogen atom, a methyl group or STR2 in which R2 and R3 being identical or different from each other represent independently a lower alkyl group.
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- Derivatives of 1,3-Benzdioxoles, 48. Preparation and Reactions of 1,3-Benzdioxole-4,7-quinones
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We describe the preparation of a substituted 1,3-benzdioxole-4,7-quinone complex (2) by reaction of 4-hydroxy-1,3-benzdioxole (1) with potassiumnitrosodisulfonate.The quinones 4a-d can be obtained by treatment of the 4-hydroxy-7-methoxy-1,3-benzdioxoles 3a-d with ammoniumcerium(IV)nitrate.Reaction of 2 with several cyclophiles gives the addition compounds resp. the dehydrogenation-products 6b-d in partly high yields. - Keywords: 1,3-Benzdioxol-4,7-chinon, 6,7-Dimethyl-naphtho-1,3-dioxol-4,9-chinon, 6-Hydroxy-naphtho-1,3-dioxol-4,9-chinon
- Dallacker, Franz,Holtmann, Bodo,Coerver, Wim
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p. 392 - 397
(2007/10/02)
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- SYNTHESE TOTALES DE LA (+/-) ISO β-PELTATINE ET DE SES ANALOGUES
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α-Hydroxyalkylation of a β-(2-alkoxy 3,4-methylenedioxy benzyl)-γ-butyrolactone (17 or 25) with 3,4,5-trimethoxybenzaldehyde or syringaldehyde 27, followed by cyclisation, afforded good yields of the corresponding (+/-) isopeltatins.
- Brown, Eric,Loriot, Michel,Robin, Jean-Pierre
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p. 949 - 952
(2007/10/02)
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- The Constituents of Schizandra chinensis BAILL. IX. The Cleavage of the Methylenedioxyl Moiety with Lead Tetraacetate in Benzene, and the Structure of Angeloylgomisin Q
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A procedure for selective cleavage of the methylenedioxyl moiety with lead tetraacetate in dry benzene is described.Piperonylic acid methyl ester (5), 4-nitro-1,2-methylenedioxybenzene (6), 3,4-methylenedioxytoluene (7), 2,3-methylenedioxyanisole (8) and gomisin A (9) afforded protocatechuic acid (12), 4-nitrocatechol (13), 3,4-dihydroxytoluene(14), 2,3-dihydroxyanisole (15) and compound 16, respectively.The structure of angeloylgomisin Q isolated from the fruits of Schizandra chinensis BAILL. (Schizandraceae), was elucidated as 1 by using the above reaction.Keywords--cleavage of methylenedioxyl moiety; lead tetraacetate; Schizandra chinensis BAILL.; Schizandraceae; dibenzocyclooctadiene; lignan; angeloylgomisin Q
- Ikeya, Yukinobu,Taguchi, Heihachiro,Yoshioka, Itiro
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p. 2893 - 2898
(2007/10/02)
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- THE CONSTITUENTS OF SCHIZANDRA CHINENSIS BAILL. VI. 13C NUCLEAR MAGNETIC RESONANCE SPECTROSCOPY OF DIBENZOCYCLOOCTADIENE LIGNANDS.
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The 13C NMR spectra of thirteen dibenzocyclooctadiene lignans, isolated from the truits of Schizandra chinensis BAILL. (Schizandraceae), were analyzed and their carbon shifts assigned.Several important chemical shift trends are described.Keywords - Schizandra chinesis BAILL.; Schizandraceae; dibenzocyclooctadiene; lignans; Gomisins; 13C NMR
- Ikeya, Yukinobu,Taguchi, Heihachiro,Sasaki, Hiroshi,Nakajima, Kaoru,Yosioka, Itiro
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p. 2414 - 2421
(2007/10/02)
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