- Muscarinic acetylcholine receptor binding affinities of pethidine analogs
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A series of pethidine analogs were synthesized and their affinities for the [3H]N-methyl-scopolamine (NMS) binding site on muscarinic acetylcholine receptors (mAChRs) were determined using M1, M3 or M5 human mAChRs expressed by Chinese hamster ovary (CHO) cell membranes. Compound 6b showed the highest binding affinities at M1, M3 and M5 mAChRs (Ki = 0.67, 0.37, and 0.38 μM, respectively).
- Lee, Na-Ra,Zhang, Xuan,Darna, Mahesh,Dwoskin, Linda P.,Zheng, Guangrong
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p. 5032 - 5035
(2015/11/09)
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- HETEROCYCLIC COMPOUNDS, MEDICAMENTS CONTAINING SAID COMPOUNDS, USE THEREOF AND PROCESSES FOR THE PREPARATION THEREOF
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The present invention relates to compounds of general formula (I) and the tautomers and the salts thereof, particularly the pharmaceutically acceptable salts thereof with inorganic or organic acids and bases, which have valuable pharmacological properties, particularly an inhibitory effect on epithelial sodium channels, and the use thereof for the treatment of diseases, particularly diseases of the lungs and airways.
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Paragraph 0339; 0341
(2013/05/09)
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- DRUG COMBINATIONS CONTAINING PDE4 INHIBITORS AND NSAIDS
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The present invention relates to new drug combinations which contain in addition to one or more PDE4-inhibitors at least one NSAID (=non-steroidal anti-inflammatory drug) (2), processes for preparing them and their use in treating in particular respiratory complaints such as for example COPD, chronic sinusitis and asthma. The invention particularly relates to those drug combinations which contain, in addition to one or more, preferably one PDE4 inhibitor of general formula 1 wherein X is SO or SO2, but preferably SO, and wherein R1, R2, R3 and R4 have the meanings given in claim 1, at least one NSAID (2), the preparation thereof and the use thereof for the treatment of respiratory complaints.
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- Design and synthesis of a new class of malonyl-CoA decarboxylase inhibitors with anti-obesity and anti-diabetic activities
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A new series of thiazole-substituted 1,1,1,3,3,3-hexafluoro-2-propanols were prepared and evaluated as malonyl-CoA decarboxylase (MCD) inhibitors. Key analogs caused dose-dependent decreases in food intake and body weight in obese mice. Acute treatment with these compounds also led to a drop in elevated blood glucose in a murine model of type II diabetes.
- Tang, Haifeng,Yan, Yan,Feng, Zhe,De Jesus, Reynalda K.,Yang, Lihu,Levorse, Dorothy A.,Owens, Karen A.,Akiyama, Taro E.,Bergeron, Raynald,Castriota, Gino A.,Doebber, Thomas W.,Ellsworth, Kenneth P.,Lassman, Michael E.,Li, Cai,Wu, Margaret S.,Zhang, Bei B.,Chapman, Kevin T.,Mills, Sander G.,Berger, Joel P.,Pasternak, Alexander
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scheme or table
p. 6088 - 6092
(2010/11/18)
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- METHODS AND COMPOSITIONS FOR TREATING AMYLOID-RELATED DISEASES
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Methods, compounds, pharmaceutical compositions and kits are described for treating or preventing amyloid-related disease.
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Page 170; 171
(2008/06/13)
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- Spirohydantoin compounds and uses thereof
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Spirohydantoin compounds and their pharmaceutically acceptable salts are disclosed. The synthesis of these compounds and their use as alpha 1a adrenergic receptor antagonists is also described. One application of these compounds is in the treatment of ben
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- Phenylacetamides as selective α-1A adrenergic receptor antagonists
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A novel class of potent and selective α-1a receptor antagonists has been identified. The structures of these antagonists were derived from truncating the 4-aryl dihydropyridine subunit present in known α-1a antagonists. The design principles which led to the discovery of substituted phenylacetamides, the synthesis and SAR of key analogues, and the results of select in vitro and in vivo studies are described. (C) 2000 Elsevier Science Ltd. All rights reserved.
- Patane, Michael A.,DiPardo, Robert M.,Newton, Randall C.,Price, RoseAnn P.,Broten, Theodore P.,Chang, Raymond S.L.,Ransom, Richard W.,Di Salvo, Jerry,Nagarathnam, Dhanapalan,Forray, Carlos,Gluchowski, Charles,Bock, Mark G.
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p. 1621 - 1624
(2007/10/03)
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