- Structurally Diverse Synthesis of Five-, Six-, and Seven-Membered Benzosultams through Electrochemical Cyclization
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We have developed a metal- and oxidant-free approach to structurally diverse synthesis of benzosultams from aryl sulfonamides through an electrochemical cyclization. Upon variation of the ortho substituent on aryl sulfonamides, five-, six-, and seven-memb
- Liu, Aiyun,Guo, Tiantian,Zhang, Shuangshuang,Yang, Han,Zhang, Qi,Chai, Yonghai,Zhang, Shengyong
-
supporting information
p. 6326 - 6331
(2021/08/23)
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- Copper-Catalyzed Intermolecular Alkynylation and Allylation of Unactivated C(sp3)-H Bonds via Hydrogen Atom Transfer
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We describe Cu-catalyzed intermolecular alkynylation and allylation of unactivated C(sp3)-H bonds with singly occupied molecular orbital-philes (SOMO-philes) via hydrogen atom transfer (HAT). Employing N-fluoro-sulfonamide as a HAT reagent, a set of subst
- Liang, Lei,Guo, Ge,Li, Chen,Wang, Song-Lin,Wang, Yue-Hui,Guo, Hai-Ming,Niu, Hong-Ying
-
supporting information
p. 8575 - 8579
(2021/11/13)
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- Copper-Catalyzed Intermolecular Functionalization of Unactivated C(sp3)-H Bonds and Aliphatic Carboxylic Acids
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Intermolecular functionalization of C(sp3)-H bonds and aliphatic carboxylic acids enables the efficient synthesis of high value-added organic compounds from readily available starting materials. Although methods involving hydrogen atom transfer have been developed for such functionalization, these methods either work for only activated C(sp3)-H bonds or bring in a narrow set of functional groups. Here we describe a Cu-catalyzed process for the diverse functionalization of both unactivated C(sp3)-H bonds and aliphatic carboxylic acids. The process is enabled by the trapping of alkyl radicals generated through hydrogen atom abstraction by arylsulfonyl-based SOMO-philes, which introduces a large array of C, N, S, Se, and halide-based functional groups. The chemoselectivity can be switched from C-H functionalization to decarboxylative functionalization by matching the bond dissociation energy of the hydrogen atom transfer reagent with that of the target C-H or O-H bond.
- Mao, Runze,Bera, Srikrishna,Turla, Aurélya Christelle,Hu, Xile
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supporting information
p. 14667 - 14675
(2021/09/18)
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- Synthesis of amino-diamondoid pharmacophores: Via photocatalytic C-H aminoalkylation
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We report a direct C-H aminoalkylation reaction using two light-activated H-atom transfer catalyst systems that enable the introduction of protected amines to native adamantane scaffolds with C-C bond formation. The scope of adamantane and imine reaction partners is broad and deprotection provides versatile amine and amino acid building blocks. Using readily available chiral imines, the enantioselective synthesis of the saxagliptin core and rimantadine derivatives is also described.
- Weigel, William K.,Dang, Hoang T.,Yang, Hai-Bin,Martin, David B. C.
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supporting information
p. 9699 - 9702
(2020/09/03)
-
- MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR
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This disclosure provides modulators of Cystic Fibrosis Transmembrane Conductance Regulator (CFTR), pharmaceutical compositions containing at least one such modulator, methods of treatment of cystic fibrosis using such modulators and pharmaceutical composi
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-
Paragraph 00221
(2019/10/29)
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- Sulfonamide Synthesis through Electrochemical Oxidative Coupling of Amines and Thiols
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Sulfonamides are key motifs in pharmaceuticals and agrochemicals, spurring the continuous development of novel and efficient synthetic methods to access these functional groups. Herein, we report an environmentally benign electrochemical method which enables the oxidative coupling between thiols and amines, two readily available and inexpensive commodity chemicals. The transformation is completely driven by electricity, does not require any sacrificial reagent or additional catalysts and can be carried out in only 5 min. Hydrogen is formed as a benign byproduct at the counter electrode. Owing to the mild reaction conditions, the reaction displays a broad substrate scope and functional group compatibility.
- Laudadio, Gabriele,Barmpoutsis, Efstathios,Schotten, Christiane,Struik, Lisa,Govaerts, Sebastian,Browne, Duncan L.,No?l, Timothy
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supporting information
(2019/04/16)
-
- Sulfonamide Synthesis through Electrochemical Oxidative Coupling of Amines and Thiols
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Sulfonamides are key motifs in pharmaceuticals and agrochemicals, spurring the continuous development of novel and efficient synthetic methods to access these functional groups. Herein, we report an environmentally benign electrochemical method which enables the oxidative coupling between thiols and amines, two readily available and inexpensive commodity chemicals. The transformation is completely driven by electricity, does not require any sacrificial reagent or additional catalysts and can be carried out in only 5 min. Hydrogen is formed as a benign byproduct at the counter electrode. Owing to the mild reaction conditions, the reaction displays a broad substrate scope and functional group compatibility.
- Laudadio, Gabriele,Barmpoutsis, Efstathios,Schotten, Christiane,Struik, Lisa,Govaerts, Sebastian,Browne, Duncan L.,No?l, Timothy
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supporting information
p. 5664 - 5668
(2019/04/17)
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- Cobalt-Catalyzed Asymmetric Allylation of Cyclic Ketimines
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A CoII/Box-catalyzed [Box=bis(oxazoline)] enantioselective addition of potassium allyltrifluoroborate to cyclic ketimines was developed, providing the corresponding chiral α-tertiary amines in high yields and with good enantioselectivity values. Alkoxycarbonyl- and alkyl-substituted saccharin-derived ketimines are suitable substrates for this allylation reaction. The product can be converted to complex molecules over several simple steps, including a precursor of MK-0371, which is a kinesin spindle protein inhibitor. In addition, this catalytic system showed a strong positive nonlinear effect.
- Wu, Liang,Shao, Qihang,Yang, Guoqiang,Zhang, Wanbin
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supporting information
p. 1241 - 1245
(2017/12/15)
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- Copper(II)-Catalyzed Asymmetric Photoredox Reactions: Enantioselective Alkylation of Imines Driven by Visible Light
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Asymmetric photoredox catalysis offers exciting opportunities to develop new synthetic approaches to chiral molecules through novel reaction pathways. Employing the first-row transition metal complexes as the chiral photoredox catalysts remains, however, a formidable challenge, although these complexes are economic, environmentally friendly, and often exhibit special reactivities. We report in this Article the development of one class of highly efficient asymmetric/photoredox bifunctional catalysts based on the copper(II) bisoxazoline complexes (CuII-BOX) for the light-induced enantioselective alkylation of imines. The reactions proceed under very mild conditions and without a need for any other photosensitizer. The simple catalytic system and readily tunable chiral ligands enable a significantly high level of enantioselectivity for the formation of chiral amine products bearing a tetrasubstituted carbon stereocenter (36 examples, up to 98% ee). Overall, the CuII-BOX catalysts initiate the radical generation, and also govern the subsequent stereoselective transformations. This strategy utilizing chiral complexes comprised of a first-row transition metal and a flexible chiral ligand as the asymmetric photoredox catalysts provides an effective platform for the development of green asymmetric synthetic methods.
- Li, Yanjun,Zhou, Kexu,Wen, Zhaorui,Cao, Shi,Shen, Xiang,Lei, Meng,Gong, Lei
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supporting information
p. 15850 - 15858
(2018/11/23)
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- Copper (II)/RuPHOX-Catalyzed Enantioselective Mannich-Type Reaction of Glycine Schiff Bases with Cyclic Ketimines
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A Cu(II)/RuPHOX-catalyzed enantioselective Mannich-type reaction of glycine Schiff bases with cyclic ketimines was developed, affording chiral α,?-diamino acid derivatives in good yields with moderate to good ee and dr values. This provides an efficient methodology for furnishing chiral Cβ-tetrasubstituted α,β-diamino acid precursors. The catalytic system is compatible with a series of substrates. In addition, an interesting nonlinear effect of the catalyst's enantiomeric composition on reaction enantioselectivity was observed. (Figure presented.).
- Shao, Qihang,Wu, Liang,Chen, Jianzhong,Gridnev, Ilya D.,Yang, Guoqiang,Xie, Fang,Zhang, Wanbin
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supporting information
p. 4625 - 4633
(2018/11/10)
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- Highly Enantioselective Ferrocenyl Palladacycle-Acetate Catalysed Arylation of Aldimines and Ketimines with Arylboroxines
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Benzylic N-substituted stereocenters constitute a frequent structural motif in drugs. Their highly enantioselective generation is hence of technical importance. An attractive strategy is the arylation of imines with organoboron reagents. Chiral Rh complexes have reached a high level of productivity for this reaction type. In this article we describe that an electron rich PdIIcatalyst also performs well in the arylation of aldimines, comparable to the best Rh catalysts. The ferrocenyl palladacycle-acetate catalyst allows for a broad substrate scope and very high enantioselectivities. Commonly observed side reactions like aryl–aryl homocouplings and imine hydrolysis could be blocked. Mechanistic studies implicate that a) the acetate ligand is crucial for transmetallation, b) the active catalyst is most likely a palladacycle-OAc monomer, c) the rate limiting step is probably the product release. By added KOAc the arylation could also be applied to ketimines.
- Schrapel, Carmen,Frey, Wolfgang,Garnier, Delphine,Peters, René
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supporting information
p. 2448 - 2460
(2017/02/23)
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- Copper-catalyzed asymmetric alkynylation of cyclic: N -sulfonyl ketimines
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A Cu-catalyzed asymmetric alkynylation of cyclic N-sulfonyl ketimines was developed, providing the corresponding chiral α-tertiary amines with up to 98% ee. The method tolerates some variations in cyclic N-sulfonyl ketimine and alkyne scope. These products could be used in several transformations, in particular, the products of 6-membered cyclic N-sulfonyl ketimines could be easily converted to linear chiral α-tertiary amines. This asymmetric alkynylation provides an efficient, gram-scale, low-cost transition-metal catalyzed synthesis of chiral α-tetrasubstituted propargylamines.
- Ling, Zheng,Singh, Sonia,Xie, Fang,Wu, Liang,Zhang, Wanbin
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supporting information
p. 5364 - 5367
(2017/07/06)
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- A synthetic method of the compound benzenesulfonyl amine
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The invention relates to a method for preparing benzene sulfonamide compounds. In the method, a ternary catalyzing system of ethyltriphenylphosphonium bromide-silver compounds-porphyrin is adopted; the method for preparing N-tert-Butylbenzenesulfenamide from the reaction of methyl tertiary butyl ether with a weak reactivity and benzene sulfonamide compounds is realized; remarkably technical effects of preferable reaction temperature, high yield and good universality are achieved; moreover, as appropriate additives are added in the reaction, the collision between molecules is promoted and the reaction time is shortened; the method has favorable industrialization perspective and industrialized production value.
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-
Paragraph 0036; 0037; 0038; 0039; 0040
(2017/03/08)
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- A general iodine-mediated synthesis of primary sulfonamides from thiols and aqueous ammonia
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A general and efficient methodology for preparing primary sulfonamides has been developed. In the presence of iodine as the catalyst and TBHP (70% in water) as the oxidant, a wide range of primary sulfonamides were prepared from the corresponding thiols and aqueous ammonia in moderate to good yields.
- Feng, Jian-Bo,Wu, Xiao-Feng
-
supporting information
p. 6951 - 6954
(2016/07/30)
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- The Construction of 3-Methyl-4-arylpiperidines via a trans- Perhydroindolic Acid-Catalyzed Asymmetric Aza-Diels-Alder Reaction
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An efficient trans-perhydroindolic acid-catalyzed asymmetric aza-Diels-Alder reaction of cyclic 1-azadienes and propanal was developed for the synthesis of chiral 3-methyl-4-aryldehydropiperidine derivatives (up to 98% yield and 99% ee). Such scaffolds are often found in bioactive compounds and medicines. A gram-scale reaction was carried out with a low catalyst loading to give the desired product in high yield and with excellent enantioselectivity. The resulting dehydropiperidine derivatives can be further transformed to chiral 3-methyl-4-aryl-substituted piperidines with high efficiency.
- An, Qianjin,Shen, Jiefeng,Butt, Nicholas,Liu, Delong,Liu, Yangang,Zhang, Wanbin
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supporting information
p. 3627 - 3638
(2016/01/25)
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- Simple branched sulfur-olefins as chiral ligands for Rh-catalyzed asymmetric arylation of cyclic ketimines: Highly enantioselective construction of tetrasubstituted carbon stereocenters
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New, simple, sulfinamide-based branched olefin ligands have been developed and successfully used in Rh-catalyzed asymmetric arylations of cyclic ketimines, providing efficient and highly enantioselective access to valuable benzosultams and benzosulfamidat
- Wang, Hui,Jiang, Tao,Xu, Ming-Hua
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supporting information
p. 971 - 974
(2013/04/10)
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- BENZOXAZEPIN COMPOUNDS SELECTIVE FOR PI3K P110 DELTA AND METHODS OF USE
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Benzoxazepin Formula I compounds, including stereoisomers, geometric isomers, tautomers, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting the delta isoform of PI3K, and for treating disorders mediated by lipid kinases such as inflammation, immunological disorders, and cancer. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
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Page/Page column 133
(2012/10/08)
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- Design and synthesis of cyclic sulfonamides and sulfamates as new calcium sensing receptor agonists
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The design, synthesis and calcimimetic properties of various cyclic sulfonamides and sulfamates are described. The latter were prepared from the corresponding o-alkenylarenesulfonamides via copper- or rhodium-catalyzed intramolecular aziridination. The si
- Kiefer, Lionel,Gorojankina, Tatiana,Dauban, Philippe,Faure, Hélène,Ruat, Martial,Dodd, Robert H.
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scheme or table
p. 7483 - 7487
(2011/02/21)
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- Copper-catalyzed formation of sulfur-nitrogen bonds by dehydrocoupling of thiols with amines
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Copper-catalyzed formation of sulfur-nitrogen bonds can be performed by a dehydrocoupling of aryl thiols with amines. Sulfenamides or sulfonamides can be produced by the use of a copper catalyst in air or under oxygen atmosphere. Furthermore, a reaction involving the combination of a palladium catalyst and a copper catalyst selectively afforded sulfinamides.
- Taniguchi, Nobukazu
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experimental part
p. 2670 - 2673
(2010/07/18)
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- Structure-based design, synthesis, and biological evaluation of 1,1-dioxoisothiazole and benzo[b]thiophene-1,1-dioxide derivatives as novel inhibitors of hepatitis C virus NS5B polymerase
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A novel series of HCV NS5B polymerase inhibitors comprising 1,1-dioxoisothiazoles and benzo[b]thiophene-1,1-dioxides were designed, synthesized, and evaluated. SAR studies guided by structure-based design led to the identification of a number of potent NS
- Kim, Sun Hee,Tran, Martin T.,Ruebsam, Frank,Xiang, Alan X.,Ayida, Benjamin,McGuire, Helen,Ellis, David,Blazel, Julie,Tran, Chinh V.,Murphy, Douglas E.,Webber, Stephen E.,Zhou, Yuefen,Shah, Amit M.,Tsan, Mei,Showalter, Richard E.,Patel, Rupal,Gobbi, Alberto,LeBrun, Laurie A.,Bartkowski, Darian M.,Nolan, Thomas G.,Norris, Daniel A.,Sergeeva, Maria V.,Kirkovsky, Leo,Zhao, Qiang,Han, Qing,Kissinger, Charles R.
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supporting information; scheme or table
p. 4181 - 4185
(2009/04/16)
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- Selective angiotensin II AT2 receptor agonists: Benzamide structure-activity relationships
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In the investigation of the structure-activity relationship of nonpeptide AT2 receptor agonists, a series of substituted benzamide analogues of the selective nonpeptide AT2 receptor agonist M024 have been synthesised. In a second ser
- Wallinder, Charlotta,Botros, Milad,Rosenstr?m, Ulrika,Guimond, Marie-Odile,Beaudry, Hélène,Nyberg, Fred,Gallo-Payet, Nicole,Hallberg, Anders,Alterman, Mathias
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p. 6841 - 6849
(2008/12/22)
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- THIOUREAS AS FACTOR Xa INHIBITORS
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The present invention is directed to compounds represented by Formula (I) and pharmaceutically acceptable salts, solvates, hydrates, and prodrugs thereof which are inhibitors of Factor Xa. The present invention is also directed to and intermediates used in making such compounds, pharmaceutical compositions containing such compounds, methods to prevent or treat a number of conditions characterized by undesired thrombosis and methods of inhibiting the coagulation of a blood sample.
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Page/Page column 45
(2010/11/08)
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- AMIDO COMPOUNDS AND THEIR USE AS PHARMACEUTICALS
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The present invention relates to inhibitors of 11-? hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of variou
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Page/Page column 53
(2010/02/14)
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- Benzenesulfonyl chloride with primary and secondary amines in aqueous media - Unexpected high conversions to sulfonamides at high pH
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We have determined pH-yield profiles under pseudo-first-order conditions of the reactions of benzenesulfonyl chloride with a set of primary and secondary water-soluble alkylamines, and have found with certain amines, such as dibutylamine, a profile taking the form of a sigmoid pH-yield curve with relatively high yields of the sulfonamide persisting with increasing basicity up to and including 1.0 mol/L sodium hydroxide. This behaviour is quantitatively accounted for by invoking, in addition to the usual second-order reaction of the sulfonyl chloride with the amine, two third-order terms (i) one first-order in sulfonyl chloride, amine and hydroxide anion, and (H) another first-order in sulfonyl chloride and second-order in the amine. The importance of the third-order terms correlates approximately with the total number of alkyl carbon atoms in the amine, and this in turn is regarded as related to the hydrophobic character of the amine. Experiments to test this picture included: (i) observation of a bell-shaped curve with bis(2-methoxyethyl)amine, (H) in the reaction of dibutylamine in THF-H2O (1:1), and also (iii) in the reaction of dibutylamine in 1.0 mol/L tetrabutylammonium bromide, and (iv) increase in the contributions of the third-order terms in 1.0 mol/L aqueous sodium chloride. Preparative reactions with dibutylamine, 1-octylamine, and hexamethylenimine in 1.0 mol/L aqueous sodium hydroxide with a 5% excess of benzenesulfonyl chloride gave, respectively, 94%, 98%, and 97% yields of the corresponding sulfonamides.
- King, James F.,Gill, Manjinder S.,Ciubotaru, Petru
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p. 1525 - 1535
(2007/10/03)
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- Platelet ADP receptor inhibitors
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Novel compounds of formulae (I) to (VIII), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylsulfonamide derivatives which are effective platelet ADP receptor inhibitors. These derivatives may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also relates to a method for preventing or treating thrombosis in a mammal comprising the step of administering a therapeutically effective amount of a compound of formulae (I) to (VIII), or a pharmaceutically acceptable salt thereof.
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- Inhibitors of factor Xa
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Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.
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Page column 199 - 200
(2010/02/05)
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- 5-AMIDINO-2-HYDROXYBENZENESULFONAMIDE DERIVATIVES, MEDICINAL COMPOSITIONS CONTAINING THE SAME, MEDICINAL USE THEREOF AND INTERMEDIATES IN THE PRODUCTION THEREOF
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The present invention relates to a 5-amidino-2-hydroxybenzenesulfonamide derivative represented by the general formula: wherein R1 is an optionally substituted lower alkyl group, an optionally substituted lower alkoxy group, an optionally substituted lower alkenyl group, a cycloalkyl group or a lower acyl group etc.; Q is a hydrogen atom or an optionally substituted lower alkyl group; and Z is a hydrogen atom or a hydroxy group etc., or a pharmaceutically acceptable salt thereof, which exert a potent and selective activated blood coagulation factor X inhibitory activity and is useful as an agent for the prevention or treatment of a disease occurred associating an activated blood coagulation factor X, a pharmaceutical composition comprising the same and an intermediate thereof. These compounds are useful as preventives or remedies for various diseases such as brain infarction, cerebral thrombosis, cerebral embolism, TIA, cerebral vascular jerk, Alzheimer's diseases, myocardial infarction, heart attack, heart failure, thrombosis, pulmonary infarction and pulmonary embolism.
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- Substituted aryl and heteroaryl derivatives, the preparation thereof and the use therof as pharmaceutical compositions
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The present invention relates to new substituted aryl and heteroaryl derivatives of general formula wherein A, Ar, n, X, Y1, Y2, Y3, Y4, R1 and R5 are defined as in claim 1, the prodrugs, t
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- Sultams: Solid phase and other synthesis of anti-HIV compounds and compositions
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Biologically active sultams are disclosed which have potent anti-HIV activity. A combinational method of synthesis, which uses a solid support and variants thereof, are described. Biological compositions and method of treating mammals for viral infections
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-
- Platelet ADP receptor inhibitors
-
Novel compounds of formulae (I) to (VIII), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylsulfonamide derivatives which are effective platelet ADP receptor inhibitors. These derivatives may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also relates to a method for preventing or treating thrombosis in a mammal comprising the step of administering a therapeutically effective amount of a compound of formulae (I) to (VIII), or a pharmaceutically acceptable salt thereof.
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-
- Inhibitors of factor Xa
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Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.
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-
- Design, synthesis, and SAR of amino acid derivatives as factor Xa inhibitors1
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A series of potent and selective factor Xa inhibitors was synthesized using various readily available amino acids as central templates. The most potent compound displays IC50 of 3 nM.
- Su, Ting,Wu, Yanhong,Doughan, Brandon,Jia, Zhaozhong J.,Woolfrey, John,Huang, Brian,Wong, Paul,Park, Gary,Sinha, Uma,Scarborough, Robert M.,Zhu, Bing-yan
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p. 2947 - 2950
(2007/10/03)
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- PYRAZOLE DERIVATIVES AS ANGIOTENSIN II ANTAGONISTS
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Compounds of general formula I and their salts and solvates are angiotensin II receptor antagonists and as such are useful in the treatment of hypertension, congestive heart failure and elevated intraocular pressure. Pharmaceutical compositions including these compounds and processes for their preparation are also provided.
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-
- L-162,389: A potent orally active angiotensin II receptor antagonist with balanced affinity to both AT1 and AT2 receptor subtypes
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Simple modifications made to our potent angiotensin II AT1 selective clinical candidate MK-996 provided a compound with balanced binding affinity to both the AT1 and the AT2 receptor subtype. This compound, L-162,389 is or
- Rivero,Kevin,Kivlighn,Zingaro,Chang,Greenlee
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p. 307 - 310
(2007/10/03)
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- Potent and orally active angiotensin II receptor antagonists with equal affinity for human AT1 and AT2 subtypes
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In order to block the effects induced by the interactions between angiotensin II (AII) and both AT1 and AT2 receptors, we have pursued the discovery of orally active non-peptide AII antagonists that exhibit potent and equal affinity
- Chang,Ashton,Flanagan,Chen,O'Malley,Zingaro,Kivlighn,Siegl,Lotti,Chang,Greenlee
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p. 3741 - 3758
(2007/10/03)
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- SUBSTITUTED 1,2,4-TRIAZOLIN-3-ONE COMPOUNDS BEARING ACIDIC FUNCTIONAL GROUPS AS BALANCED ANGIOTENSIN II ANTAGONISTS
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Novel substituted 1,2,4-triazolin-3-ones of the formula (I) are useful as angiotensin II antagonists. STR1
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-
- Synthesis of Spiro(oxazolidinediones): Spiro-2',3(2H),4'-triones and Spiro-2',4'-dione 1,1-Dioxides
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Members of two novel families of spiro(oxazolidinediones) have been prepared.Spiro-2',3(2H),4'-triones (4) were synthesized from the corresponding 1-hydroxy-1-carboethoxyethylisoindol-3-one (7) or (10) or their primary amide
- Wrobel, Jay,Dietrich, Arlene
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p. 1823 - 1838
(2007/10/02)
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- Spiro[1,2-benzisothiazole-3(2H),5'-oxazolidine]-2',4'-dione 1,1-dioxides as antihyperglycemic agents
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This invention relates to novel spiro[1,2-benzisothiazole-3(2H),5'-oxazolidine]-2',4'-dione 1,1-dioxides characterized by the general formula (I), STR1 wherein R is lower alkyl containing 1 to 6 carbon atoms, cycloalkyl containing 5 to 6 carbon atoms, all
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