cas 75073-11-9, 5-IODO-6-METHYL-PYRIDIN-2-YLAMINE

Articles about 75073-11-9Total 15 be found

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Encoding Multiple Reactivity Modes within a Single Synthetic-Replicator
Establishing programmable and self-sustaining replication networks in pools of chemical reagents is a key challenge in systems chemistry. Self-replicating templates are formed from two constituent components with complementary recognition and reactive sites via a slow bimolecular pathway and a fast template-directed pathway. Here, we re-engineer one of the components of a synthetic replicator to encode an additional recognition function, permitting the assembly of a binary complex between the components that mediates replicator formation through a template-independent pathway, which achieves maximum rate acceleration at early time points in the replication process. The complementarity between recognition sites creates a key conformational equilibrium between the catalytically inert product, formed via the template-independent pathway, and the catalytically active replicator that mediates the template-directed pathway. Consequently, the rapid formation of the catalytically inert isomer kick-starts replication through the template-directed pathway. Through kinetic analyses, we demonstrate that the presence of the two recognition-mediated reactivity modes results in enhanced template formation in comparison to that of systems capable of exploiting only a single recognition-mediated pathway. Finally, kinetic simulations reveal that the conformational equilibrium and both the relative and absolute efficiencies of the recognition-mediated pathways affect the extent to which self-replicating systems can benefit from this additional template-independent reactivity mode. These results allow us to formulate the rules that govern the coupling of replication processes to alternative recognition-mediated reactivity modes. The interplay between template-directed and template-independent pathways for replicator formation has significant relevance to ongoing efforts to design programmable and adaptable replicator networks.
Kosikova, Tamara,Philp, Douglas,Robertson, Craig C.
p. 11139 - 11152
(2020)
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Sulfapyridine hapten and artificial antigen as well as preparation method and application thereof
The invention relates to sulfapyridine hapten and artificial antigen as well as a preparation method and application thereof. The structure of the sulfapyridine hapten is shown as a formula (1), wherein the R1 and R2 are hydrogen, methyl or methoxyl; m is
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Paragraph 0090; 0103; 0105

(2020/02/14)

HETEROCYCLIC COMPOUND
Provided is a compound having an antagonistic action on an NMDA receptor containing the NR2B subunit, and is useful as a prophylactic or therapeutic agent for major depression, bipolar disorder, migraine, pain, peripheral symptoms of dementia and the like
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Paragraph 0305

(2017/11/18)

SPIROCYCLIC ISOXAZOLINES AS ANTIPARASITIC AGENTS
The invention recites spirocyclic isoxazoline derivatives of Formula (1) stereoisomers thereof, veterinary or pharmaceutical acceptable salts thereof, compositions thereof, processes for making, and their use as a parasiticide in an animal. The variables
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Page/Page column 50

(2014/03/26)

Remarkable switch in the regiochemistry of the iodination of anilines by N-iodosuccinimide: Synthesis of 1,2-dichloro-3,4-diiodobenzene
Direct iodination of anilines by NIS in polar solvents (such as DMSO) affords p-iodinated products with up to >99% regioselectivity. Switching to less polar solvents (such as benzene) in the presence of AcOH inverts this outcome toward dramatically increased or preferential generation of the o-isomers, also with up to >99% regioselectivity. This finding was exploited in the synthesis of 1,2-dichloro-3,4-diiodobenzene. Georg Thieme Verlag Stuttgart - New York.
Shen, Hao,Vollhardt, K. Peter C.
supporting information; experimental part
p. 208 - 214
(2012/03/11)

5-ALKYNYL-PYRIMIDINES
The present invention encompasses compounds of general formula (1) wherein R1 to R4 R3 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a medicament having the above-mentioned properties.
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Page/Page column 9

(2012/02/06)

5-ALKYNYL-PYRIMIDINES
The present invention encompasses compounds of general formula (1) wherein R1 to R3 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a medicament having the above-mentioned properties.
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Page/Page column 8-9

(2012/02/06)

5-ALKYNYL PYRIMIDINES AND THEIR USE AS KINASE INHIBITORS
The present invention encompasses compounds of general formula (1) wherein R1 to R4 R3 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a medicament having the above-mentioned properties.
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Page/Page column 25

(2011/08/21)

Synthesis and nicotinic acetylcholine receptor binding properties of bridged and fused ring analogues of epibatidine
Epibatidine analogues 3-5, possessing the pyridine ring fused to the 2,3 position of the 7-azabicyclo[2.2.1]heptane ring, and analogue 8a, possessing a benzene ring fused to the 5,6 position, were synthesized by procedures involving key steps of trapping
Carroll, F. Ivy,Robinson, T. Philip,Brieaddy, Lawrence E.,Atkinson, Robert N.,Mascarella, S. Wayne,Damaj, M. Imad,Martin, Billy R.,Navarro, Hernán A.
p. 6383 - 6391
(2008/03/30)

(IMIDAZOLO-5-YL)-2-ANILO-PYRIMIDINES AS AGENTS FOR THE INHIBITION OF CELL PROLIFERATION
Compounds of the formula (I): wherein variable groups are as defined within and a pharmaceutically acceptable salts and in vivo hydrolysable esters are described. Also described are processes for their preparation and their use as medicaments, particularly medicaments for producing a cell cycle inhibitory (anti cell proliferation) effect in a warm blooded animal, such as man.
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Page/Page column 63-64

(2008/06/13)

Syntheses of pyridine C-nucleosides as analogues of the natural nucleosides dC and dU
The syntheses of four pyrimidine C-nucleosides are described. These derivatives are designed as mimics of dC and dU, and in that respect, each can form two hydrogen bonds with complementary dG or dA residues. The minor groove O2 carbonyl in each derivativ
Sun, Zhenhua,Ahmed, Shahadat,McLaughlin, Larry W.
p. 2922 - 2925
(2007/10/03)

Synthesis of conformationally constrained spirodihydrofuropyridine analogues of epibatidine
Conformationally constrained spirofuropyridine analogues of epibatidine, syn-2 and anti-2, in which the 7-azabicyclo[2.2.1]heptane system and the 2-chloropyridine ring are held rigidly with the shorter and longer N-N distances, respectively, were synthesized from N-Boc-7-azabicyclo[2.2.1]heptan-2-one. The preliminary binding studies suggested that syn-2 has stronger binding affinity for nAChRs than anti-2.
Abe, Hideki,Arai, Yumiko,Aoyagi, Sakae,Kibayashi, Chihiro
p. 2971 - 2973
(2007/10/03)

Compounds and methods for promoting smoking cessation
Compounds and methods for promoting smoking cessation. The compounds may be used to treat a variety of other conditions and disease states.
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(2008/06/13)

4-hydroxy-1,8-naphthyridine-3-carboxamides as antiviral agents
A compound of formula IV: or a pharmaceutically acceptable salt thereof wherein, R1 is (a) Cl, (b) Br, (c) CN, (d) NO2, or (e) F; R2, R3 and R4 are independently selected from: (a) H, (b) halo, (c) aryl, (d) S(O)mR6, (e) (C═O)R6, (f) (C═O)OR9, (g) cyano, (h) het, wherein said het is bound via a carbon atom, (i) OR10, (j) Ohet, (k) NR7R8 (1) SR10, (m) Shet, (n) NHCOR12, (o) NHSO2R12, or (p) C1-7alkyl which may be partially unsaturated and optionally substituted by one or more substituents of the group R11, OR13, SR10, SR13, NR7R8, halo, (C═O)C1-7alkyl, or SOmR9; R6 is (a) C1-7alkyl, (b) NR7R8, (c) aryl, or (d) het, wherein said het is bound via a carbon atom; R7 and R8 are independently (a) H, (b) aryl, (c) C1-7alkyl which may be partially unsaturated and is optionally substituted by one or more substituents selected from NR10R10, R11, SOmR9, CONR10R10, or halo, or, (d) R7 and R8 together with the nitrogen to which they are attached form a het; R9 is (a) aryl, (b) het, (c) C3-8cycloalkyl, (d) methyl, or (e) C2-7alkyl which may be partially unsaturated and is optionally substituted by one or more substituents selected from NR10R10, R11, SH, CONR10R10, or halo; R10 is (a) H, (b) methyl, or (b) C2-7alkyl optionally substituted by OH; R11 is (a) OR10, (b) Ohet, (c) Oaryl, (d) CO2R10, (e) het, (f) aryl, or (g) CN; R12 is (a) H, (b) het, (c) aryl, (d) C3-8cycloalkyl, (e) methyl, or (f) C2-7alkyl optionally substituted by NR7R8 or R11; R13 is (a) (P═O)(OR14)2, (b) CO(CH2)nCON(CH3)-(CH2)nSO3?M+, (c) an amino acid, (d) C(═O)aryl, or (e) C(═O)C1-7alkyl optionally substituted by NR7R8, aryl, het, CO2H, or O(CH2)nCO2R14; R14 is (a) H, or (b) C1-7alkyl; each n is independently 1, 2, 3, 4 or 5; each m is independently 0, 1, or 2; M is sodium, potassium, or lithium; aryl is a phenyl radical or an ortho-fused bicyclic carbocyclic radical wherein at least one ring is aromatic; wherein any aryl is optionally substituted with one or more substituents selected from the group consisting of halo, OH, cyano, CO2R14, CF3, C1-6alkoxy, and C1-6alkyl which may be further substituted by one to three SR14, NR14R14, OR14, or CO2R14 groups; het is a four- (4), five- (5), six- (6), or seven- (7) membered saturated or unsaturated heterocyclic ring having 1, 2, or 3 heteroatoms selected from the group consisting of oxygen, sulfur, and nitrogen, which is optionally fused to a benzene ring, or any bicyclic heterocycle group; wherein any het is optionally substituted with one or more substituents selected from the group consisting of halo, OH, cyano, phenyl, CO2R14, CF3, C1-6alkoxy, oxo, oxime, and C1-6 alkyl which may be further substituted by one to three SR14, NR14R14, OR14, or CO2R14 groups; is provided. The compounds are particularly effective in the treatment or prevention of herpesviruses. Certain novel 4-hydroxy-1,8-naphthyridine-3-carboxyamides. The compounds are effective in the treatment or prevention of viral infections, particularly viral infections caused by herpes simplex viruses types 1 and 2, human herpes viruses types 6, 7 and 8, varicello zoster viruses, human cytomegaloviruses and Epstein-Barr viruses.
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(2008/06/13)

Synthesis of bridged analogs of epibatidine. 3-Chloro-5,7,8,9,9a,10-hexahydro-7,10-methanopyrrolo[1,2-b]-2,6-naphthyridine and 2-chloro-5,5a,6,7,8,10-hexahydro-5,8-methanopyrrolo[2,1-b]-1,7-naphthyridine
The synthesis of conformationally locked analogs of epibatidine are described in which the key step is an intramolecular reductive palladium-catalyzed Heck-type coupling.
Brieaddy, Lawrence E.,Wayne Mascarella,Navarro, Hernán A.,Atkinson, Robert N.,Damaj,Martin, Billy R.,Carroll
p. 3795 - 3797
(2007/10/03)