- INHIBITORS OF PROTEIN ARGININE DEIMINASES
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Provided herein are inhibitors of protein arginine deiminases (PADs), pharmaceutical compositions comprising said compounds, and methods for using said compounds for the treatment of diseases.
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Paragraph 00135
(2019/08/26)
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- Novel indazoles for the treatment and prophylaxis of respiratory syncytial virus infection
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The invention provides novel compounds having the general formula: wherein R1, R2, R3, R4, R5, R7, A1, A2 and A3 are as described herein, compositions including the compounds and methods of using the compounds.
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Paragraph 0582-0583
(2016/08/17)
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- Novel indazoles for the treatment and prophylaxis of respiratory syncytial virus infection
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The invention provides novel compounds having the general formula: wherein R1, R2, R3, R4, R5, R7, A1, A2 and A3 are as described herein, compositions including the compounds and methods of using the compounds.
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Paragraph 0581; 0582
(2015/06/17)
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- NOVEL INDAZOLES FOR THE TREATMENT AND PROPHYLAXIS OF RESPIRATORY SYNCYTIAL VIRUS INFECTION
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The invention provides novel compounds having the general formula: formula (I) wherein R1, R2, R3, R4, R5, R7, A1, A2 and A3 are as described herein, compositions including the compounds and methods of using the compounds.
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Page/Page column 119
(2014/02/15)
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- Diazine indole acetic acids as potent, selective, and orally bioavailable antagonists of chemoattractant receptor homologous molecule expressed on Th2 cells (CRTH2) for the treatment of allergic inflammatory diseases
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New classes of CRTH2 antagonists, the pyridazine linker containing indole acetic acids, are described. The initial hit 1 had good potency but poor permeability, metabolic stability, and PK. Initial optimization led to compounds of type 2 with low oxidative metabolism but poor oral bioavailability. Poor permeability was identified as a liability for these compounds. Addition of a linker between the indole and diazine moieties afforded a series with good potency, low rates of metabolism, moderate permeability, and good oral bioavailability in rodents. 32 was identified as the development track candidate. It was potent in cell based, binding, and whole blood assays and exhibited good PK profile. It was efficacious in mouse models of contact hypersensitivity (1 mg/kg b.i.d.) and house dust (20 mg/kg q.d.) when dosed orally. In sheep asthma, administration at 1 mg/kg iv completely blocked the LAR and AHR and attenuated the EAR phase.
- Kaila, Neelu,Huang, Adrian,Moretto, Alessandro,Follows, Bruce,Janz, Kristin,Lowe, Michael,Thomason, Jennifer,Mansour, Tarek S.,Hubeau, Cedric,Page, Karen,Morgan, Paul,Fish, Susan,Xu, Xin,Williams, Cara,Saiah, Eddine
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experimental part
p. 5088 - 5109
(2012/08/28)
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- HETEROCYCLIC INHIBITORS OF HISTAMINE RECEPTORS FOR THE TREATMENT OF DISEASE
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The present invention relates to compounds and methods which may be useful as inhibitors of H1R and/or H4R for the treatment or prevention of inflammatory, autoimmune, allergic, and ocular diseases.
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Page/Page column 239
(2011/10/05)
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- HETEROCYCLIC INHIBITORS OF HISTAMINE RECEPTORS FOR THE TREATMENT OF DISEASE
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The present invention relates to compounds and methods which may be useful as inhibitors of H1R and/or H4R for the treatment or prevention of inflammatory, autoimmune, allergic, and ocular diseases.
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Page/Page column 116
(2010/06/11)
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- INDAN-AMIDE DERIVATIVES WITH GLYCOGEN PHOSPHORYLASE INHIBITORY ACTIVITY
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A compound of the formula (1) or a pharmaceutically-acceptable salt: (A chemical formula should be inserted here - please see paper copy enclosed herewith) (1) possess glycogen phosphorylase inhibitory activity and accordingly have value in the treatment
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Page/Page column 56
(2008/06/13)
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