104706-47-0Relevant articles and documents
A PROCESS FOR PREPARATION OF (2S, 5R)-7-OXO-N-[(3S)-PYRROLIDIN-3-YLOXY]-6-(SULFOOXY)-1,6-DIAZABICYCLO [3.2.1]OCTANE-2-CARBOXAMIDE
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Page/Page column 14, (2015/08/06)
A process for preparation of a compound of Formula (I) is disclosed.
DIAMINOPYRIMIDINE DERIVATIVES AND PROCESSES FOR THE PREPARATION THEREOF
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Page/Page column 55, (2012/09/11)
The present invention provides a diaminopyrimidine derivative or its pharmaceutically acceptable salt, a process for the preparation thereof, a pharmaceutical composition comprising the same, and a use thereof. The diaminopyrimidine derivative or its pharmaceutically acceptable salt functions as a 5-HT4 receptor agonist, and therefore can be usefully applied for preventing or treating dysfunction in gastrointestinal motility, one of the gastrointestinal diseases, such as gastroesophageal reflux disease (GERD), constipation, irritable bowel syndrome (IBS), dyspepsia, post-operative ileus, delayed gastric emptying, gastroparesis, intestinal pseudo-obstruction, drug-induced delayed transit, or diabetic gastric atony.
PREPARATION OF DARIFENACIN AND ITS SALTS
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Page/Page column 15; 32-33, (2008/12/08)
Provided are various processes and compounds related to darifenacin and/or its salts. For example, there is provided a process for preparing a free base of darifenacin: Formula, or the salt thereof, the process including reacting 3-(S)-(cyanodiphenylmethyl)-1-[2-(2,3-dihydrobenzofuran-5-yl) ethyl] pyrrolidine of the Formula (IV), or a salt thereof: Formula (IV) with a base effective to convert the nitrile group of the compound of the Formula (IV) to the amide group of the darifenacin in an organic solvent, the reaction being carried out in the organic solvent, with a proviso that the solvent is not 2-methyl-butan-2-ol, and with further proviso that the reaction produces less than about 0.5 % of the compound of the Formula (Ic): Formula (Ic) in the reaction mass, as measured by HPLC. Various embodiments and variants are provided.
Pteridinone derivatives as PI3-kinases inhibitors
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Page/Page column 20, (2008/12/07)
New compounds of formula 1 are provided which by virtue of their pharmaceutical activity as PI3-kinase modulators may be used in the therapeutic field for the treatment of inflammatory or allergic diseases. Examples of these include inflammatory and allergic respiratory complaints, inflammatory diseases of the gastro-intestinal tract and motor apparatus, inflammatory and allergic skin diseases, inflammatory eye diseases, diseases of the nasal mucosa, inflammatory or allergic conditions involving autoimmune reactions or inflammations of the kidney.
1-SUBSTITUTED-3-PYRROLIDINE DERIVATIVES AS MUSCARINIC RECEPTOR ANTAGONISTS
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Page 14, (2008/06/13)
This invention generally relates to the derivatives of 1 -substituted-3 -pyrroli dines having the structure of Formula (I): The compounds of this invention can function as..muscarinic receptor antagonists, and can be used for the treatment of various diseases of the respiratory, urinary and gastrointestinal systems mediated through muscarinic receptors. The invention also relates to a process for the preparation of the compounds of the present invention. pharmaceutical compositions containing the compounds of the present invention and the methods for treating the diseases mediated through muscarinic receptors.
Novel processes for the preparation of adenosine compounds and intermediates thereto
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, (2008/06/13)
Novel processes for the preparation of adenosine compounds and intermediates thereto. The adenosine compounds prepared by the present processes may be useful as cardiovascular agents, more particularly as antihypertensive and anti-ischemic agents, as cardioprotective agents which ameliorate ischemic injury or myocardial infarct size consequent to myocardial ischemia, and as an antilipolytic agents which reduce plasma lipid levels, serum triglyceride levels, and plasma cholesterol levels. The present processes may offer improved yields, purity, ease of preparation and/or isolation of intermediates and final product, and more industrially useful reaction conditions and workability.
MUSCARINIC RECEPTOR ANTAGONISTS
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, (2008/06/13)
A series of novel 3-phenyl-3-[1-(cyclicalkyl)pyrrolidin-3-yl] glutarimide derivatives have been prepared, including their pharmaceutically acceptable salts. The cyclic moiety present in these compounds is derived from either benzene or a heteroaryl such as benzofuran or 2,3-dihydrobenzofuran, or it is derived from an aromatic heterocyclic such as pyridine, pyrazine or thiophene, and it is attached to the adjacent alkyl group of the molecule by means of one of the available ring carbon atoms situated in the aromatic ring of the aforementioned cyclic ring moiety. These particular compounds are useful in therapy as selective muscarinic receptor antagonists, which are selective for smooth muscle muscarinic sites over cardiac muscarinic sites and therefore, are of value in the treatment of diseases associated with altered motility and/or smooth muscle tone as found in the gut, trachea and bladder. Methods for preparing these compounds from known starting materials are provided.
Muscarinic receptor antagonists
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, (2008/06/13)
Muscarinic receptor antagonists of formula (I), and their pharmaceutically acceptable salts, wherein Y is --CH 2 --, --(CH 2) 2 --, --CH 2 O--, --(CH 2) 2 O-- or --CH 2 S--; R is --CH or --CONH 2 ; and R 1 is a group of formula (a), where R 2 and R 3 are each independently H, C 1 -C 4 alkyl, C 1 -C 4 alkoxy, --(CH 2) n OH, halo, trifluoromethyl, cyano, --(CH 2) n NR 4 R 5, --CO(C 1 -C 4 alkyl), --OCO(C 1 -C 4 alkyl), --CH(OH)(C 1 -C 4 alkyl), --C(OH)(C 1 -C 4 alkyl 2, --SO 2 NH 2, --(CH 2) n CONR 6 R 7 or --(CH 2) n COO(C 1 -C 4 alkyl); R 4 is H or C 1 -C 4 alkyl; R 5 is H, C 1 -C 4 alkyl or C 1 -C 4 alkysulphonyl; R 6 and R 7 are each independently H or C 1 -C 4 alkyl; and n is 0, 1 or 2. The compounds are particularly useful in treating irritable bowel syndrome.
Quinolone antibacterial agents. Synthesis and structure-activity relationships of a series of amino acid prodrugs of racemic and chiral 7-(3- amino-1-pyrrolidinyl)quinolones. Highly soluble quinolone prodrugs with in vivo pseudomonas activity
Sanchez,Domagala,Heifetz,Priebe,Sesnie,Trehan
, p. 1764 - 1773 (2007/10/02)
A series of amino acid prodrugs of racemic and chiral 7-(3-amino-1- pyrrolidinyl)-6-fluoro-1,8-naphthyridine-3-carboxylic acids, 1-cyclopropyl- 6,8-difluoro-3-quinolinecarboxylic acids, 1-cyclopropyl-6-fluoro-3- quinolinecarboxylic acids, and 5-amino-1-cyclopropyl-6,8-difluoro-3- quinolinecarboxylic acids have been prepared and evaluated for comparative antibacterial activity. Compounds were prepared by acylation of the 3-amino group of the pyrrolidine with common amino acids using standard peptide chemistry. This series has been compared with the parent compounds for antibacterial activity in vitro and in vivo as well as for comparative solubility. The amino acid analogues were less active in vitro, but had equal or increased efficacy in vivo. Indeed, it was proven that these compounds, which were stable to acid and base under the reaction conditions for their preparation, were rapidly cleaved in serum to give the parent quinolones. The amino acid derivatives showed a 3-70 times improved solubility when compared to the parent compounds. The most active compound of the series was [S- (R*,R*)]-7-[3-[(2-amino-1-oxopropyl)-amino]-1-pyrrolidinyl]-1-cyclopropyl- 6-fluoro-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acid (PD 131112).
