- IMIDAZOPYRAZINE DERIVATIVES AS ANTIBACTERIAL AGENTS
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The invention provides novel imidazopyrazine derivatives having the general formula (I), wherein A and R1 to R11 are as described herein NA (I) and pharmaceutically acceptable salts thereof.5 Further provided are pharmaceutical compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds as medicaments, in particular methods of using the compounds as antibiotics for the treatment or prevention of bacterial infections and resulting diseases.
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Page/Page column 44; 250-251
(2020/07/14)
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- IMIDAZOPYRAZINE DERIVATIVES AS ANTIBACTERIAL AGENTS
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The invention provides novel imidazopyrazine derivatives having the general formula (I), wherein A and R1 to R11 are as described herein formula (I) and pharmaceutically acceptable salts thereof. Further provided are pharmaceutical compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds as medicaments, in particular methods of using the compounds as antibiotics for the treatment or prevention of bacterial infections and resulting diseases.
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Page/Page column 299
(2020/07/14)
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- NOVEL IMIDAZOPYRAZINE DERIVATIVES AS ANTIBACTERIALS
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The invention provides novel imidazopyrazine derivatives having general formula (I), wherein R1 to R11 are as described herein, and pharmaceutically acceptable salts thereof. Further provided are pharmaceutical compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds as medicaments, in particular methods of using the compounds as antibiotics for the treatment or prevention of bacterial infections and related diseases.
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Page/Page column 88; 324
(2020/07/14)
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- IMIDAZOPYRAZINE DERIVATIVES AS ANTIBACTERIALS
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The invention provides novel imidazopyrazine derivatives having the general formula (I), wherein A and R1 to R14 are as described herein (I) and pharmaceutically acceptable salts thereof. Further provided are pharmaceutical compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds as medicaments, in particular methods of using the compounds as antibiotics for the treatment or prevention of bacterial infections and resulting diseases.
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Page/Page column 245
(2020/07/14)
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- NOVEL IMIDAZOPYRAZINE DERIVATIVES
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The invention provides novel imidazopyrazine derivatives having the general formula (I), wherein A and R1 to R11 are as described herein (I) and pharmaceutically acceptable salts thereof. Further provided are pharmaceutical compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds as medicaments, in particular methods of using the compounds as antibiotics for the treatment or prevention of bacterial infections and related diseases.
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Page/Page column 264
(2020/07/14)
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- Flow Photo-Nazarov Reactions of 2-Furyl Vinyl Ketones: Cyclizing a Class of Traditionally Unreactive Heteroaromatic Enones
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Nazarov reactions of 2-furyl vinyl ketones and related heteroaromatic enones, to produce furan-fused cyclopentanones using a flow photochemical approach, are described. Compounds possessing this connectivity between heterocycle and ketone (2-furyl, 2-benzofuryl, 2-thiophene-yl, and 2-benzothiophene-yl) have traditionally proven difficult or impossible to cyclize with typical Br?nsted and Lewis acid mediated methods. Using mild flow photochemistry conditions and acetic acid (AcOH) or hexafluoroisopropanol (HFIP) as solvent, these compounds were found to cyclize in 45-97% yields, with typical UV exposure times of 3.4-6.8 min. In all cases, 2-furyl and 2-thiophene-yl enones cyclized, whereas 2-benzofuryl and 2-benzothiophene-yl enones exhibited divergent properties with reactivity patterns tied to the identity of the vinyl group. This report discloses the first photo-Nazarov reactions of tetrahydropyridine-substituted 2-furyl ketones, providing a direct approach to the corresponding fused heterocyclic motifs built around a central cyclopentanone. These motifs constitute the core structures of biologically active natural products, including the marine alkaloid nakadomarin A.
- Ashley, William L.,Timpy, Evan L.,Coombs, Thomas C.
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p. 2516 - 2529
(2018/03/09)
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- Discovery of potent iminoheterocycle BACE1 inhibitors
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The synthesis of a series of iminoheterocycles and their structure-activity relationships (SAR) as inhibitors of the aspartyl protease BACE1 will be detailed. An effort to access the S3 subsite directly from the S1 subsite initially yielded compounds with sub-micromolar potency. A subset of compounds from this effort unexpectedly occupied a different binding site and displayed excellent BACE1 affinities. Select compounds from this subset acutely lowered Aβ40 levels upon subcutaneous and oral administration to rats.
- Caldwell, John P.,Mazzola, Robert D.,Durkin, James,Chen, Joseph,Chen, Xia,Favreau, Leonard,Kennedy, Matthew,Kuvelkar, Reshma,Lee, Julie,McHugh, Nansie,McKittrick, Brian,Orth, Peter,Stamford, Andrew,Strickland, Corey,Voigt, Johannes,Wang, Liyang,Zhang, Lili,Zhang, Qi,Zhu, Zhaoning
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p. 5455 - 5459
(2015/01/08)
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- Iridium-catalyzed enantioselective hydrogenation of unsaturated heterocyclic acids
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Spiral binding: A highly enantioselective hydrogenation of unsaturated heterocyclic acids has been developed by using chiral iridium/spirophosphino oxazoline catalysts (see scheme; BArF-=tetrakis[3,5- bis(trifluoromethyl)phenyl]borate, Boc=tert-butoxycarbonyl). This reaction provided an efficient method for the preparation of optically active heterocyclic acids with excellent enantioselectivities. Copyright
- Song, Song,Zhu, Shou-Fei,Pu, Liu-Yang,Zhou, Qi-Lin
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p. 6072 - 6075
(2013/07/05)
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- Synthesis of 3-azabicyclo [4.1.0]heptane-1-carboxylic acid
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A full study on the synthesis of 3-azabicyclo[4.1.0]heptane-1-carboxylic acid is described.Three different approaches were investigated in order to achieve an efficient synthesis of this unnatural aminoacid.The optimized synthetic route relies upon three key steps: (i) diazomalonate insertion on 4-phtalimido 1-butene, (ii) intramolecular cyclization and (iii) chemoselective reduction of the resulting lactam.Due to its bicyclic nature and conformational constraints, this aminoacid may be an useful building block in medicinal chemistry.
- Napolitano, Carmela,Borriello, Manuela,Cardullo, Francesca,Donati, Daniele,Paio, Alfredo,Manfredini, Stefano
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experimental part
p. 5492 - 5497
(2010/08/07)
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- NOVEL OXADIAZOLE DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF METABOTROPIC GLUTAMATE RECEPTORS
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The present invention relates to new compounds which are Oxadiazole derivatives of formula (I) wherein B, P, Q,W, R1 and R2 are defined in the description. Invention compounds are useful in the prevention or treatment of central or p
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Page/Page column 23
(2008/06/13)
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- THERAPEUTIC COMPOUNDS AND USES THEREOF
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Compounds of formula (I) are described herein The compounds can be used, for example, to modulate growth hormone secretagogue receptor (GHS-R). In some instances, the compounds can be used to treat obesity.
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Page/Page column 95; 96
(2008/06/13)
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- Carbamoyl tetrahydropyridine derivatives
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Carbamoyl tetrahydropyridine derivatives represented by the formula: [in the formula, R1and R2are identical or different, and each represents a hydrogen atom, a C1-C5alkyl group, or the like; Y1-Y2represents (R4)C═C(R5), (R6)C═N, N═N, (R7)N—CO, or N═C(R8); X1, X2, and X3are identical or different, and each represents a hydrogen atom, a halogen atom, or the like; R3, R4, R5, and R6are identical or different, and each represents a hydrogen atom or an alkyl group; R7represents a hydrogen atom, a C1-C5alkyl group, or the like; and R8represents a hydrogen atom or a carbamoyl group] or a pharmaceutically acceptable salt thereof, and intermediates for the preparation thereof are provided. The derivatives described above are effective for diseases which are believed to involve CRF.
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- CARBAMOYL TETRAHYDROPYRIDINE DERIVATIVES
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Carbamoyl tetrahydropyridine derivatives represented by the formula: [in the formula, R1 and R2 are identical or different, and each represents a hydrogen atom, a C1-C5 alkyl group, or the like; Y1-Y
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- Synthesis of the sialidase inhibitor siastatin B.
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[structure] The resolved piperidinecarboxylate (R)-7 was converted to siastatin B (1) by an efficient and stereoselective sequence that includes a bromo-beta-lactonization and an N-acyliminium azidation. Two analogues (3 and 4) of siastatin were also prepared.
- Knapp,Zhao
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p. 4037 - 4040
(2007/10/03)
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- New carbamoylpiperidines as human platelet aggregation inhibitors
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A series of 3-carbamoylpiperidines (nipecotamides) are designed, synthesized and tested for their inhibitory action against adenosine diphosphate (ADP)-induced aggregation of human platelets. A structure- activity analysis of the bis(nipecotamido)aralkane type showed that a substituent on the piperidine ring should preferably be an amide and that the electronegativity of the carbonyl oxygen and the orientation of the amide group affected activities. Based on the knowledge of factors influencing platelet activation and aggregation, a nitric ester moiety which could release nitric oxide (NO) in situ, is incorporated into the nipecotamide structure. These compounds exhibit increased activity compared to those having no -ONO2 function. They also show stereoselectivity, with the meso isomer being approximately twice as potent as the synthetic diastereomeric mixture. Replacement of the -ONO2 function with hydroxyl, ester or alkyl groups considerably diminishes aggregation-inhibitory potential. Nipecotamides are shown here to inhibit the basal and collagen-induced rise in platelet inositol trisphosphate (IP3) levels, as well as phosphoinositide turnover. A comprehensive mechanism of action is proposed taking earlier results into consideration. (C) 2000 Elsevier Science Ltd.
- Guo, Zhengming,Zheng, Xiaozhang,Thompson, Walter,Dugdale, Marion,Gollamudi, Ram
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p. 1041 - 1058
(2007/10/03)
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- Heterocyclic compounds
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Novel piperidine compounds are provided, and those compounds are useful in the treatment and/or prevention of diabetes, and especially non-insulin dependent diabetes (NIDDM or type 2 diabetes) including overnight or meal treatment and treatment or prevention of longterm complications, such as retinopathy, neuropathy, nephropathy, and micro- and macroangiopathy; treatment of hyperglycemia, hypercholesterolemia, hypertension, hyperinsulinemia, hyperlipidemia, atherosclerosis or myocardial ischemia.
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