- An improved synthesis of 4-chloro-7H-pyrrolo[2,3-d]pyrimidine
-
[Figure not available: see fulltext.] An improved seven-step synthesis of 4-chloro-7H-pyrrolo[2,3-d]pyrimidine from dimethyl malonate with 31% overall yield is described. The procedure is operationally simple and practical for the synthesis of the 4-chloro-7H-pyrrolo[2,3-d]pyrimidine building block.
- Zhang, Yu-Liu,Xu, Cheng-Tao,Liu, Ting,Zhu, Yong,Luo, Yu
-
p. 638 - 642
(2018/08/17)
-
- ATROPISOMERISM FOR ENHANCED KINASE INHIBITOR SELECTIVITY
-
The invention provides a series of conformationally stable and selective kinase inhibitors, and methods of using the kinase inhibitors. The effect of atropisomerism on kinase selectivity was assessed, finding improved selectivity compared to rapidly inter
- -
-
Page/Page column 33
(2019/01/10)
-
- Exploiting Atropisomerism to Increase the Target Selectivity of Kinase Inhibitors
-
Many biologically active molecules exist as rapidly interconverting atropisomeric mixtures. Whereas one atropisomer inhibits the desired target, the other can lead to off-target effects. Herein, we study atropisomerism as a possibility to improve the sele
- Smith, Davis E.,Marquez, Isaac,Lokensgard, Melissa E.,Rheingold, Arnold L.,Hecht, David A.,Gustafson, Jeffrey L.
-
supporting information
p. 11754 - 11759
(2015/10/05)
-
- CYCLOLIC HYDRAZINE DERIVATIVES AS HIV ATTACHMENT INHIBITORS
-
Compounds of Formula I are provided, including pharmaceutically acceptable salts thereof: wherein A is selected from the group consisting of: wherein Z is selected from the group consisting of: which are useful as HIV attachment inhibitors.
- -
-
Page/Page column 61
(2013/09/26)
-
- Discovery of 6,7-dihydro-5H-pyrrolo[2,3-a]pyrimidines as orally available g protein-coupled receptor 119 agonists
-
GPR119 is a 7-transmembrane receptor that is expressed in the enteroendocrine cells in the intestine and in the islets of Langerhans in the pancreas. Indolines and 6,7-dihydro-5H-pyrrolo[2,3-a]pyrimidines were discovered as G protein-coupled receptor 119
- Katamreddy, Subba R.,Carpenter, Andrew J.,Ammala, Carina E.,Boros, Eric E.,Brashear, Ron L.,Briscoe, Celia P.,Bullard, Sarah R.,Caldwell, Richard D.,Conlee, Christopher R.,Croom, Dallas K.,Hart, Shane M.,Heyer, Dennis O.,Johnson, Paul R.,Kashatus, Jennifer A.,Minick, Doug J.,Peckham, Gregory E.,Ross, Sean A.,Roller, Shane G.,Samano, Vicente A.,Sauls, Howard R.,Tadepalli, Sarva M.,Thompson, James B.,Xu, Yun,Way, James M.
-
p. 10972 - 10994
(2013/02/25)
-
- FUSED BICYCLIC PYRIMIDINE DERIVATIVES AND METHODS OF USE THEREOF
-
The present invention relates to Fused Bicyclic Pyrimidine Derivatives, compositions comprising a Fused Bicyclic Pyrimidine Derivative, and methods of using the Fused Bicyclic Pyrimidine Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a G-protein coupled receptor (GPCR) in a patient.
- -
-
Page/Page column 33-34
(2011/06/19)
-
- BICYCLIC HETEROCYCLE DERIVATIVES AND USE THEREOF AS GPR119 MODULATORS
-
The present invention relates to Bicyclic Heterocycle Derivatives of Formula (I), compositions comprising a Bicyclic Heterocycle Derivative, and methods of using the Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a metaboli
- -
-
Page/Page column 76
(2010/04/03)
-
- BICYCLIC HETEROCYCLE DERIVATIVES AND THEIR USE AS GPCR MODULATORS
-
The present invention relates to Bicyclic Heterocycle Derivatives of Formula (I), compositions comprising a Bicyclic Heterocycle Derivative, and methods of using the Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a diabetic
- -
-
Page/Page column 44
(2010/04/03)
-
- BICYCLIC HETEROCYCLE DERIVATIVES AND METHODS OF USE THEREOF
-
The present invention relates to Bicyclic Heterocycle Derivatives, compositions comprising a Bicyclic Heterocycle Derivative, and methods of using the Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a diabetic complication,
- -
-
Page/Page column 73
(2010/04/03)
-
- AZAINDOLE P2X3 AND P2X2/3 MODULATORS
-
The application discloses compounds of the Formula I: or a pharmaceutically acceptable salt thereof, wherein, X, R1, R2 R3, R4, R5, R6, R7 and R8 are as defined herein. Also provided are methods of using the compounds for treating diseases associated with the P2X3 and/or a P2X2/3 receptor antagonist and methods of making the compounds.
- -
-
Page/Page column 65-66
(2010/06/19)
-
- Facile reductive amination of aldehydes with electron-deficient anilines by acyloxyborohydrides in TFA: Application to a diazaindoline scale-up
-
A scale-up of diazaindoline 1 was achieved in four stages and 32% overall yield. The key step involved rapid reductive animation of aldehyde 8 with aniline 5 by sodium triacetoxyborohydride (STAB-H) and TFA followed by ring closure of intermediate amine 9
- Boros, Eric E.,Thompson, James B.,Katamreddy, Subba R.,Carpenter, Andrew J.
-
supporting information; experimental part
p. 3587 - 3590
(2009/09/05)
-
- GPR119 AGONISTS FOR THE TREATMENT OF DIABETES AND RELATED DISORDERS
-
The present invention relates to novel compounds that are useful in the treatment of metabolic disorders, particularly Type II diabetes mellitus and related disorders, and also to the methods for the making and use of such compounds.
- -
-
Page/Page column 63
(2010/11/29)
-
- Phosphoramidate protides of carbocyclic 2′,3′-dideoxy-2′, 3′-didehydro-7-deazaadenosine with potent activity against HIV and HBV
-
Synthesis of phosphoramidate protides of carbocyclic D- and L-2′,3′-dideoxy-2′,3′-didehydro-7-deazaadenosine by treatment of the nucleoside with phosphorochloridates in the presence of pyridine and t-BuMgCl is described. Several of these protides showed s
- Gudmundsson, Kristjan S.,Wang, Zhicheng,Daluge, Susan M.,Johnson, Lance C.,Hazen, Richard,Condreay, Lynn D.,McGuigan, Christopher
-
p. 1929 - 1937
(2007/10/03)
-
- Design, synthesis, and structure-activity relationship of 6-alkynylpyrimidines as potent adenosine kinase inhibitors
-
Adenosine (ADO) is an extracellular signaling molecule within the central and peripheral nervous system. Its concentration is increased at sites of tissue injury and inflammation. One of the mechanisms by which antinociceptive and antiinflammatory effects of ADO can be enhanced consists of inhibition of adenosine kinase (AK), the primary metabolic enzyme for ADO. Novel nonnucleoside AK inhibitors based on 4-amino-6-alkynylpyrimidines were prepared, and the importance of the length of the linker at the 5-position for high affinity AK inhibition was demonstrated. Compounds with 2- and 3-atom linkers were the most potent AK inhibitors. Optimization of their physicochemical properties led to 31a and 37a that effectively reduced pain and inflammation in animal models.
- Gomtsyan, Arthur,Didomenico, Stanley,Lee, Chih-Hung,Matulenko, Mark A.,Kim, Ki,Kowaluk, Elizabeth A.,Wismer, Carol T.,Mikusa, Joe,Yu, Haixia,Kohlhaas, Kathy,Jarvis, Michael F.,Bhagwatt, Shripad S.
-
p. 3639 - 3648
(2007/10/03)
-