- PHARMACEUTICAL COMPOUNDS
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This invention relates to compounds that are agonists of the muscarinic M1 receptor or M1 and M4 receptors and which are useful in the treatment of muscarinic M1 or M1/M4 receptor mediated
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Paragraph 0567; 0652; 0653; 0655; 0867
(2018/04/26)
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- 8-Amino-2-Oxo-1,3-Diaza-Spiro-[4.5]-Decane Derivatives
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The invention relates to 8-amino-2-oxo-1,3-diaza-spiro-[4.5]-decane derivatives, their preparation and their use in medicine, particularly in the treatment of pain.
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Paragraph 0205; 0207
(2017/08/01)
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- 3-(Carboxyethyl)-8-Amino-2-Oxo-1,3-Diaza-Spiro-[4.5]-Decane Derivatives
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The invention relates to 3-(carboxyethyl)-8-amino-2-oxo-1,3-diazaspiro-[4.5]-decane derivatives, their preparation and their use in medicine, particularly in the treatment of pain.
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Paragraph 0245; 0247
(2017/08/01)
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- 3-((HETERO-)ARYL)-8-AMINO-2-OXO-1,3-DIAZA-SPIRO-[4.5]-DECANE DERIVATIVES
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The invention relates to 3-((hetero-)aryl)-8-amino-2-oxo-1,3-diaza-spiro-[4.5]-decane derivatives, their preparation and their use in medicine, particularly in the treatment of pain.
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Paragraph 0149; 0152; 0153
(2017/08/07)
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- 3-(Carboxymethyl)-8-Amino-2-Oxo-1,3-Diaza-Spiro-[4.5]-Decane Derivatives
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The invention relates to 3-(carboxymethyl)-8-amino-2-oxo-1,3-diaza-spiro-[4.5]-decane derivatives, their preparation and their use in medicine, particularly in the treatment of pain.
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Paragraph 0206; 0208
(2017/08/01)
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- 3-((HETERO-)ARYL)-ALKYL-8-AMINO-2-OXO-1,3-DIAZA-SPIRO-[4.5]-DECANE DERIVATIVES
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The invention relates to 3-((hetero-)aryl)-alkyl-8-amino-2-oxo-1,3-diaza-spiro-[4.5]-decane derivatives, their preparation and their use in medicine, particularly in the treatment of pain.
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Paragraph 0152; 0155-0156
(2017/09/02)
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- SUBSTITUTED AZASPIRO(4.5)DECANE DERIVATIVES
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The invention relates to substituted spirocyclic cyclohexane derivatives which have an affinity for the μ opioid receptor and/or the ORL1 receptor, processes for the preparation thereof, medicaments containing these compounds and the use of these compounds for the preparation of medicaments.
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Page/Page column 63
(2016/02/10)
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- Optimization of novel di-substituted cyclohexylbenzamide derivatives as potent 11β-HSD1 inhibitors
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Novel 4,4-disubstituted cyclohexylbenzamide inhibitors of 11β-HSD1 were optimized to account for liabilities relating to in vitro pharmacokinetics, cytotoxicity and protein-related shifts in potency. A representative compound showing favorable in vivo pharmacokinetics was found to be an efficacious inhibitor of 11β-HSD1 in a rat pharmacodynamic model (ED50 = 10 mg/kg).
- McMinn, Dustin L.,Rew, Yosup,Sudom, Athena,Caille, Seb,DeGraffenreid, Michael,He, Xiao,Hungate, Randall,Jiang, Ben,Jaen, Juan,Julian, Lisa D.,Kaizerman, Jacob,Novak, Perry,Sun, Daqing,Tu, Hua,Ursu, Stefania,Walker, Nigel P.C.,Yan, Xuelei,Ye, Qiuping,Wang, Zhulun,Powers, Jay P.
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scheme or table
p. 1446 - 1450
(2010/01/16)
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- SUBSTITUTED ISOQUINOLINES AND ISOQUINOLINONES AS RHO KINASE INHIBITORS
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The invention relates to substituted isoquinoline and isoquinolinones of the formula (I) useful for the treatment and/or prevention of diseases associated with Rho-kinase and/or Rho-kinase mediated phosphorylation of myosin light chain phosphatase, and compositions containing such compounds.
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Page/Page column 75
(2010/01/30)
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- Benzamide derivatives and uses related thereto
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Benzamide derivatives of formula I are described and have therapeutic utility, particularly in the treatment of diabetes, obesity and related conditions and disorders: wherein R1, R2, R3, R4, R5, R6, R7, R8, and n are as defined herein.
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Page/Page column 59
(2008/06/13)
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