- Discovery of CYR715: A novel carboxylic acid-containing soluble guanylate cyclase stimulator
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Soluble guanylate cyclase (sGC) is a clinically validated therapeutic target in the treatment of pulmonary hypertension. Modulators of sGC have the potential to treat diseases that are affected by dysregulation of the NO-sGC-cGMP signal transduction pathw
- Rennie, Glen R.,Barden, Timothy C.,Bernier, Sylvie G.,Carvalho, Andrew,Deming, Renee,Germano, Peter,Hudson, Colleen,Im, G-Yoon J.,Iyengar, Rajesh R.,Jia, Lei,Jung, Joon,Kim, Elise,Lee, Thomas W.-H.,Mermerian, Ara,Moore, Joel,Nakai, Takashi,Perl, Nicholas R.,Tobin, Jenny,Zimmer, Daniel P.,Renhowe, Paul A.
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- NOVEL PROCESSES AND INTERMEDIATES FOR THE PREPARATION OF SOLUBLE GUANYLATE CYCLASE STIMULATORS
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The present disclosure relates to novel processes for the preparation of compounds of Formula I. Some of these compounds are useful as stimulators of soluble guanylate cyclase (sGC). Others are useful intermediates towards the preparation of said stimulat
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- SOLID DISPERSIONS COMPRISING A SGC STIMULATOR
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The present invention relates to solid dispersions of amorphous 1,1,1,3,3,3-hexafluoro-2-(((5-fluoro-2-(1-(2-fluorobenzyl)-5-(isoxazol-3-yl)-1H-pyrazol-3-yl)pyrimidin-4-yl)amino)methyl)propan-2-ol (Compound I) or a pharmaceutically acceptable salt thereof. It also relates to pharmaceutical compositions and pharmaceutical oral dosage unit forms comprising them, and their uses thereof.
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- PYRAZOLE DERIVATIVES AS SGC STIMULATORS
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There are described imidazole and pyrazole derivatives which are useful as stimulators of sGC, particularly NO-independent, heme-dependent stimulators. These compounds are also useful for treating, preventing or managing various disorders that are herein disclosed.
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- Discovery of IWP-051, a Novel Orally Bioavailable sGC Stimulator with Once-Daily Dosing Potential in Humans
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In recent years, soluble guanylate cyclase (sGC, EC 4.6.1.2) has emerged as an attractive therapeutic target for treating cardiovascular diseases and diseases associated with fibrosis and end-organ failure. Herein, we describe our design and synthesis of
- Nakai, Takashi,Perl, Nicholas R.,Barden, Timothy C.,Carvalho, Andrew,Fretzen, Angelika,Germano, Peter,Im, G-Yoon J.,Jin, Hong,Kim, Charles,Lee, Thomas W.-H.,Long, Kimberly,Moore, Joel,Rohde, Jason M.,Sarno, Renee,Segal, Chrissie,Solberg, Erik O.,Tobin, Jenny,Zimmer, Daniel P.,Currie, Mark G.
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supporting information
p. 465 - 469
(2016/06/01)
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- SGC STIMULATORS
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The present patent application discloses at least the compounds according to Formula I' shown below, or pharmaceutically acceptable salts thereof, Formula (I) wherein ring D, ring A, ring E, JB, n, JD, J, X, Z, Z1, RC
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Paragraph 00295
(2016/04/20)
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- sGC STIMULATORS
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The present patent application discloses at least the compounds according to Formula (Ia) and Formula (Ib) shown below, or pharmaceutically acceptable salts thereof, wherein ring D, ring A, JB, n, J, RC1, RC2, Z1, Z2, W, X, Y1, Y2, JF and R9 are as defined herein.
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Paragraph 00314
(2016/04/09)
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- SGC STIMULATORS
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Compounds of Formulae (I') and (I) are described, which are useful as stimulators of sGC, particularly NO-independent, heme-dependent stimulators. These compounds are also useful for treating, preventing or managing various disorders that are herein disclosed.
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Paragraph 00274
(2014/09/29)
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- 2 - BENZYL, 3 - (PYRIMIDIN- 2 -YL) SUBSTITUTED PYRAZOLES USEFUL AS SGC STIMULATORS
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2-Benzyl, 3 - (pyrimidin- 2 -YL) substituted pyrazoles are described. They are useful as stimulators of sGC, particularly NO - independent, heme - dependent stimulators. These compounds may be useful for treating, preventing or managing various disorders that are herein disclosed.
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Page/Page column 105
(2013/07/19)
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