cas 30532-36-6, 4-Pyridinepropanamine | Articles data

Articles about 30532-36-6Total 16 be found

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Synthesis, SAR and selectivity of 2-acyl- and 2-cyano-1-hetarylalkyl- guanidines at the four histamine receptor subtypes: A bioisosteric approach
In the search for potential bioisosteres of the 4-imidazolyl ring in acylguanidines (e.g. UR-AK24), known to possess affinity to several histamine receptor subtypes (HxR, x = 1-4), and cyanoguanidine-type H 4R agonists (e.g. UR-PI376
Geyer, Roland,Igel, Patrick,Kaske, Melanie,Elz, Sigurd,Buschauer, Armin
p. 72 - 81
(2014/01/06)

THIENO[3,2-D]PYRIMIDINE-6-CARBOXAMIDES AND ANALOGUES AS SIRTUIN MODULATORS
Provided herein are novel substituted thieno[3,2-d]pyrimidine-6-carboxamide sirtuin inhibitors and methods of use thereof. The sirtuin inhibitors may be used for inhibiting a sirtuin-mediated biological process, and, e.g. for treating and/or preventing diseases and disorders including, but not limited to cancer, neurodegenerative disease and inflammation. Also provided herein are pharmaceutical compositions comprising these sirtuin inhibitors and compositions comprising a sirtuin inhibitor in combination with another therapeutic agent.
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(2014/09/29)

Discovery of thieno[3,2-d ]pyrimidine-6-carboxamides as potent inhibitors of SIRT1, SIRT2, and SIRT3
The sirtuins SIRT1, SIRT2, and SIRT3 are NAD+ dependent deacetylases that are considered potential targets for metabolic, inflammatory, oncologic, and neurodegenerative disorders. Encoded library technology (ELT) was used to affinity screen a 1
Disch, Jeremy S.,Evindar, Ghotas,Chiu, Cynthia H.,Blum, Charles A.,Dai, Han,Jin, Lei,Schuman, Eli,Lind, Kenneth E.,Belyanskaya, Svetlana L.,Deng, Jianghe,Coppo, Frank,Aquilani, Leah,Graybill, Todd L.,Cuozzo, John W.,Lavu, Siva,Mao, Cheney,Vlasuk, George P.,Perni, Robert B.
p. 3666 - 3679
(2013/06/27)

Syntheses and biological activities of structurally stiff rhodacyanines as novel antimalarial candiadates
New classes of rhodacyanine as structurally stiff derivatives were designed and synthesized. The synthetic compounds were evaluated the antimalarial activity and cytotoxicity in vitro.
Takasu, Kiyosei,Morisaki, Daiki,Kaiser, Marcel,Brun, Reto,Ihara, Masataka
p. 161 - 166
(2007/10/03)

INDANE DERIVATES AS MUSCARINIC RECEPTOR AGONISTS
The present invention relates to compounds of Formula I: I which are agonists of the M-1 muscarinic receptor.
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Page 30

(2010/02/10)

PYRIDO[2,3-D]PYRIMIDINE-2,4-DIAMINES AS PDE 2 INHIBITORS
The invention provides compounds of formula (I) prodrugs thereof, and the pharmaceutically acceptable salts of the compounds or prodrugs, wherein n, X, and Y are as defined herein; pharmaceutical compositions thereof; combinations thereof; and uses thereo
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Page/Page column 28

(2010/02/12)

Tnf-alpha production inhibitors
A purpose of the present invention is to provide TNF-α production inhibitors being useful as therapeutic agents for autoimmune diseases such as rheumatoid arthritis. Novel compounds having the structure represented by the general formula [1] or salts ther
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(2008/06/13)

Bicyclic fibrinogen antagonists
This invention relates to compounds of the formulae: wherein A1is O, S, N—R1or CHR1; A4is N—R4or CHR4; R2is a sidechain containing an acid or ester group; R1, R4and R5are substituents such as H, alkyl and aryl alkyl, and R6is a sidechain containing a nitrogen group; and pharmaceutically acceptable salts thereof, which are effective for inhibiting platelet aggregation, pharmaceutical compositions for effecting such activity, and a method for inhibiting platelet aggregation.
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(2008/06/13)

Polymer bound iminodicarbonate: A new ammonia equivalent for solid-phase synthesis of primary amines
A polymer bound iminodicarbonate has been designed and its use in solid-phase synthesis of primary amines is reported. (C) Elsevier Science Ltd.
Subramanyam
p. 6537 - 6540
(2007/10/03)

Fibrinogen receptor antagonists
Fibrinogen receptor antagonists having the structure, for example, of STR1 for example STR2
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(2008/06/13)

Synthesis Of BIBN 99, A New Selective Radioligand For The In Vivo Studies Of M2 Muscarinic Receptors By Pet.
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Aubert, C.,Perrio-Huard, C.,Lasne, M. C.
p. 752 - 754
(2007/10/03)

Pyridine compounds which are useful in treating a disease state characterized by an excess of platelet activating factors
The invention relates to compounds of the formula STR1 wherein Y and Y' are hydrogen or taken together are O or S, *A is paraphenylene or *----(CH2)n --(X)s --(CH2)r ----, X is O, S or --CH=CH--, n or r, independently, are integers from 0 to 3, m is an integer from 0 to 1, s is an integer from 0 to 1, provided that when s is 1, n+m must be at least 2, t is an integer from 0 to 10, R1 and R2, independently, are lower alkyl, lower alkenyl or aryl, or one of R1 or R2 is hydrogen and the other is STR2 wherein W is STR3 --CH2 --CH2 --, --CH2 --, O, S, or STR4 and X1 is lower alkyl, phenyl unsubstituted or mono-, di- or trisubstituted by lower alkoxy, lower alkyl or halogen, and X2, X3 and X4, independently, are hydrogen, lower alkyl, lower alkoxy or halogen, R3 is hydrogen, lower alkyl or aryl, R4 is hydrogen, lower alkyl, aryl, aryl-lower alkyl or acyl, R5 is hydrogen or lower alkyl, R6 is hydrogen, lower alkyl, cycloalkyl, Het-lower alkyl or aryl, Het is a monocyclic 6-membered heteroaromatic radical containing one or two nitrogen atoms, which radical may be substituted by lower alkyl, halogen or aryl, and the asterisk denotes the point of attachment, and when R5 and R6 are different, their enantiomers and racemic mixtures thereof, when R1 and R2 are different, their geometric isomers, and pharmaceutically acceptable acid addition salts thereof.
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(2008/06/13)

Substituted n-[(pyridyl)alkyl]aryl-carboxamide
The invention relates to compounds of the formula STR1 wherein *B is STR2 Y is O or S, *A is *--(CH2)n --(X)m --(CH2)r --, n or r, independently, are integers from 0 to 3, m is an integer from 0 to 1, provided that when m is 1, then n must be at least 1, X is O or S, R1 and R4, independently, are hydrogen, lower alkyl, hydroxy or lower alkoxy, provided that when *B is other than STR3 at least one of R1 and R4, and one of R6 and R7 must be hydrogen, R2 and R3 are independently hydrogen, lower alkyl, cycloalkyl, halogen, nitro, lower alkoxy, lower alkenyl, lower alkynyl or aryl, R5 and R6, independently are hydrogen or lower alkyl, R7 is hydrogen, lower alkyl, cycloalkyl or aryl, Het is a monocyclic 5- or 6-membered hetero aromatic or a bicyclic heteroaromatic radical containing one or two hetero atoms selected from nitrogen oxygen and sulfur, which radical may be substituted by lower alkyl, halogen or aryl, and the asterisk denotes the point of attachment, and when R6 and R7 are different, their enantiomers and racemic mixtures thereof, and pharmaceutical acceptable acid addition salts thereof. The compounds of formula I exhibit activity as Platelet Activating Factor (PAF) antagonists and are, therefore, useful as agents for the prevention and treatment of vascular diseases, pulmonary diseases, dermatological disorders, transplant rejection, immunological disorders and inflammatory conditions.
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(2008/06/13)

Cyclopropylpropenamides
The invention relates to compounds of the formula STR1 Y is O or S, *A is paraphenylene or *--(CH2)n --(X)m --(CH2)r --, X is O, S or --CH=CH--, n or r, independently, are integers from 0 to 3, s is an integer from 0 to 1, m is an integer from 0 to 1, provided that when m is 1, n+s must be at least 2, R1 and R2, independently, are hydrogen, lower alkyl, cycloalkyl, lower alkenyl, Het or aryl, *E is STR2 or --(CH2)k -- wherein k is an integer from 0 to 4, R3, R4 and R8 are independently hydrogen or lower alkyl, R5 and R6, independently are hydrogen or lower alkyl, R7 is hydrogen, lower alkyl, cycloalkyl, Het-lower alkyl or aryl, Het is a monocyclic 5- or 6-membered hetero aromatic or a bicyclic heteroaromatic radical containing one or two hetero atoms selected from nitrogen, oxygen and sulfur, which radical may be substituted by lower alkyl, halogen or aryl, and the asterisk denotes the point of attachment, and their enantiomers, diastereomers and racemic mixtures thereof, as well as when *E is STR3 their geometric isomers, and pharmaceutically acceptable acid addition salts thereof. The compounds of formula I exhibit activity as platelet activating factor (PAF) antagonists and are, therefore, useful in disease states characterized by excess platelet activating factor or for the prevention and treatment of cardiovascular diseases, pulmonary diseases, immunological disorders, inflammatory diseases, dermatological disorders, shock or transplant rejection.
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(2008/06/13)

Pentadieneamides
Compounds of the formula STR1 Y is O ir S, *A is paraphenylene or *----(CH2)n----(X)m --(CH2)r ----, X is O, S or --CH=CH--, n or r, independently, are integers from 0 to 3, s is an integer from 0 to 1, m is an integer from 0 to 1, provided that when m is 1, n+s must be at least 2, R1 and R2, independently, are hydrogen, lower alkyl, cycloalkyl, lower alkenyl, Het, aryl, R3, R4 and R8, independently, are hydrogen, lower alkyl, aryl, R5 and R6, independently, are hydrogen or lower alkyl, R7 is hydrogen, lower alkyl, cycloalkyl, Het-lower alkyl or aryl, Het is a monocyclic 5- or 6-membered hetero aromatic or a bicyclic heteroaromatic radical containing one or two hetero atoms selected from nitrogen, oxygen and sulfur, which radical may be substituted by lower alkyl, halogen or aryl, and the asterisk denotes the point of attachment, and when R6 and R7 are different, their enantiomers and racemic mixtures thereof, when R1 and R2 are different, their geometric isomers, and pharmaceutically acceptable acid addition salts thereof, are described. The compounds of formula I exhibit activity as platelet activating factor (PAF) antagonists and are, therefore, useful in disease states characerized by excess platelet activating factor or for the prevention and treatment of cardiovascular disease, pulmonary diseases, immunological disorders, inflammatory diseases, dermatological disorders, shock or transplant rejection.
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(2008/06/13)

Structural Factors Affecting the Basicity of ω-Pyridylalkanols, ω-Pyridylalkanamides and ω-Pyridylalkylamines
The present paper describes the preparation by conventional methods (when not available commercially) and the pKa-determination of the α-, β- and γ-isomers of pyridylethanamide, 3-pyridylpropanamide, 4-pyridylbutanamide, 5-pyridylpentanamide, pyridylmethanol, 2-pyridylethanol, 3-pyridylpropanol, 4-pyridylbutanol, 5-pyridylpentanol, pyridylmethylamine, 2-pyridylethylamine, 3-pyridylpropylamine, 4-pyridylbutylamine, and 5-pyridylpentylamine.While a field effect accounts for many variations in pKa as a function of chain length, marked inductive effects are operative in some methyl and ethyl homologs.The pKa-decreasing influence of an intramolecular H-bond is also apparent in some lower homologs belonging to the α-series.
Mayer, Joachim M.,Testa, Bernard
p. 1868 - 1884
(2007/10/02)