- SOMATOSTATIN MODULATORS AND USES THEREOF
-
Described herein are compounds that are somatostatin modulators, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders that would benefit from modulation of somatostatin activity.
- -
-
Paragraph 00376; 00378
(2019/08/29)
-
- Design and synthesis of potent and orally active GPR4 antagonists with modulatory effects on nociception, inflammation, and angiogenesis
-
GPR4, a G-protein coupled receptor, functions as a proton sensor being activated by extracellular acidic pH and has been implicated in playing a key role in acidosis associated with a variety of inflammatory conditions. An orally active GPR4 antagonist 39c was developed, starting from a high throughput screening hit 1. The compound shows potent cellular activity and is efficacious in animal models of angiogenesis, inflammation and pain.
- Miltz, Wolfgang,Velcicky, Juraj,Dawson, Janet,Littlewood-Evans, Amanda,Ludwig, Marie-Gabrielle,Seuwen, Klaus,Feifel, Roland,Oberhauser, Berndt,Meyer, Arndt,Gabriel, Daniela,Nash, Mark,Loetscher, Pius
-
supporting information
p. 4512 - 4525
(2017/07/22)
-
- Syntheses of two potential food mutagens
-
The syntheses of the potential heterocyclic amine food mutagens 1,4,6-trimethyl-2-aminoimidazo[4,5-c]pyridine and 1,5,7-trimethyl-2 -aminoimidazo [4,5-b]pyridine are described.
- Tanga,Bradford,Bupp,Kozocas
-
p. 569 - 573
(2007/10/03)
-
- PYRIDYL IMIDAZOLE DERIVATIVES AND PROCESSES FOR THE PREPARATION THEREOF
-
Substituted pyridyl imidazole derivatives of formula (I) inhibit effectively the action of angiotensin II and have a superior anti-hypertensive activity. STR1
- -
-
-
- 3N-Methylbiphenylsulfonylurea and -carbamate substituted imidazo[4,5-b]pyridines. Potent antagonists of the ANG II AT1 receptors
-
The synthesis and the SAR study of imidazo[4,5-b]pyridine biphenyl sulfonylureas and -carbamates as highly potent AT1-seIective ANG II receptor antagonists are described. Several members of this new class of antagonists efficiently inhibited the ANG II-induced presser response in pithed rats after iv and intraduodenal (id) administration.
- Heitsch, Holger,Becker, Reinhard H.A.,Kleemann, Heinz-Werner,Wagner, Adalbert
-
p. 673 - 678
(2007/10/03)
-
- Innovative approaches to the imidazo[4,5-b]pyridine ring system. Development of an efficient process for industrial-scale production of a key intermediate for potent angiotensin II receptor antagonists
-
Two syntheses of 2-ethyl-5,7-dimethyl-3H-imidazo[4,5-b]pyridine (3), an important intermediate for the synthesis of several potent angiotensin II antagonists, have been investigated. The first route involves conversion of 1,1-bis(methylthio)-2-nitroethene (17) to 2-ammo-4,6-dimethyl-3-nitropyridine (6); catalytic hydrogenation of 6 in propionic acid gave 3 in high yield. In the second synthesis, propionitrile is converted to imidate hydrochloride 15·HCl which is neutralised and reacted with aminoacetonitrile in the presence of acetylacetone to give 3 in 55% overall yield. The propionitrile route was scaled up to produce 3 in the pilot plant.
- Stucky, Gerhard C.,Roduit, Jean-Paul,Schmidt, Beat
-
p. 280 - 282
(2007/10/03)
-
- Substituted imidazo-fused 6-membered heterocycles as angiotensin II antagonists
-
Substituted Imidazo-fused 6-membered heterocycles of structural formula: STR1 wherein A, B, C, and D are independently carbon atoms or nitrogen atoms are angiotensin II antagonists useful in the treatment of hypertension and congestive heart failure.
- -
-
-
- Diaminopyridine compounds and methods of use
-
The present invention relates to compositions and method for inhibiting nonenzymatic cross-linking (protein aging) which contain diaminopyridines and derivates thereof. Accordingly, a composition is disclosed which comprises an agent capable of inhibiting the formation of advanced glycosylation endproducts of target proteins by reacting with the carbonyl moiety of the early glycosylation product of such target proteins formed by their initial glycosylation. The method comprises contacting the target protein with the composition. Both industrial and therapeutic applications for the invention are envisioned, as food spoilage and animal protein aging can be treated.
- -
-
-
- ANGIOTENSIN II ANTAGONISTS INCORPORATING A SUBSTITUTED PYRIDOIMIDAZOLYL RING
-
Substituted heterocycles attached through a methylene bridge to novel substituted phenyl derivatives of the Formula I are useful as angiotensin II antagonists. STR1
- -
-
-
- Angiotensin II antagonists incorporating a substituted thiophene or furan
-
There are disclosed substituted thiophene and furan derivatives of Formula I which are useful as angiotensin II antagonists. STR1
- -
-
-
- SUBSTITUTED IMIDAZO-FUSED 6-MEMBERED HETEROCYCLCES AS ANGIOTENSIN II ANTAGONISTS
-
Substituted Imidazo-fused 6-membered heterocycles of structural formula: STR1 wherein A, B, C, and D are independently carbon atoms or nitrogren atoms are angiotensin II antagonists useful in the treatment of hypertension and congestive heart failure.
- -
-
-
- Angiotensin II antagonists incorporating a nitrogen containing six membered ring heterocycle
-
There are disclosed compounds, containing a pyridine, pyrazine or pyrimidine functionality on the lower ring of Formula I, which are useful as angiotensin II antagonists. STR1
- -
-
-
- Microbial transformation process for antihypertensive products
-
Fermentation of the microorganism Streptomyces sp. MA6751 (ATCC No. 55043) in the presence of the Angiotensin II (A II) receptor antagonist yields an N2-tetrazole β-glucuronide analog which is also an A II antagonist useful in the treatment of hypertension and congestive heart failure and other indications known to respond to A II antagonists.
- -
-
-
- ANGIOTENSIN II ANTAGONISTS INCORPORATING AN INDOLE OR DIHYDROINDOLE
-
There are disclosed substituted indoles and dihydroindoles of Formula I which are useful as angiotensin II antagonists. STR1
- -
-
-
- MICROBIAL TRANSFORMATION PROCESS FOR PREPARING ANTI-HYPERTENSIVE PRODUCTS
-
Fermentation of the microorganism Streptomyces sp. (MA6750) ATTC No. 55042 in the presence of the Angiotensin II (A II) receptor antagonist STR1 yields three analogs, each having a shikimate sugar-like moiety attached to the tetrazole, which are also A II antagonists useful in the treatment of hypertension and congestive heart failure and other indications known to respond to A II antagonists.
- -
-
-
- Anti-hypersensitive N2-tetrazole-β-glucuronide analog
-
Fermentation of the microorganism Streptomyces sp. MA6751 in the presence of STR1 yields an anti-hypertensive compound of the structure STR2
- -
-
-
- Antihypertensive products, a process for their preparation and pharmaceutical compositions containing them.
-
Fermentation of the microorganism Actinoplanacete sp. in the presence of the Angiotensin II (A II) receptor antagonist yields a 5-hydroxymethyl and a 7-hydroxymethyl analog, both of which are also A II antagonists useful in the treatment of hypertension and congestive heart failure and other indications known to respond to A II antagonists.
- -
-
-