55981-29-8Relevant academic research and scientific papers
ASPARAGINE ENDOPEPTIDASE (AEP) INHIBITORS, COMPOSITIONS, AND USES RELATED THERETO
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Page/Page column 4, (2020/12/11)
This disclosure relates to asparagine endopeptidase inhibitors and compositions and uses related thereto. In certain embodiments, the asparagine endopeptidase inhibitors are useful for improving memory, treating or preventing cancer, neurodegenerative diseases, and cognitive disorders. In certain embodiments, the disclosure relates to pharmaceutical compositions comprising an asparagine endopeptidase inhibitor and a pharmaceutically acceptable excipient.
Discovery of a potent thiadiazole class of histamine H3 receptor antagonist for the treatment of diabetes
Rao, Ashwin U.,Shao, Ning,Aslanian, Robert G.,Chan, Tin-Yau,Degrado, Sylvia J.,Wang, Li,McKittrick, Brian,Senior, Mary,West, Robert E.,Williams, Shirley M.,Wu, Ren-Long,Hwa, Joyce,Patel, Bhuneshwari,Zheng, Shuqin,Sondey, Christopher,Palani, Anandan
supporting information; experimental part, p. 198 - 202 (2012/04/23)
A series of novel 2-piperidinopiperidine thiadiazoles were synthesized and evaluated as new leads of histamine H3 receptor antagonists. The 4-(5-([1,4-bipiperidin]-1-yl)-1,3,4-thiadiazol-2-yl)-2-(pyridin-2-yl)morpholine (5u) displayed excellent potency and ex vivo receptor occupancy. Compound 5u was also evaluated in vivo for antidiabetic efficacy in STZ diet-induced obesity type 2 diabetic mice for 2 or 12 days. Non-fasting glucose levels were significantly reduced as compared with vehicle-treated mice. In addition, 5u dose dependently blocked the increase of HbA1c after 12 days of treatment.
Discovery of a series of potent arylthiadiazole H3 antagonists
Xiao, Dong,Palani, Anandan,Sofolarides, Michael,Huang, Ying,Aslanian, Robert,Vaccaro, Henry,Hong, Liwu,McKittrick, Brian,West Jr., Robert E.,Williams, Shirley M.,Wu, Ren-Long,Hwa, Joyce,Sondey, Christopher,Lachowicz, Jean
scheme or table, p. 861 - 864 (2011/03/18)
A series of 2-piperidinopiperidine-5-arylthiadiazoles was synthesized and subjected to a structure-activity relationship (SAR) investigation. The potency of this series was improved to the single digit nanomolar range. The key analogs were shown to be free of P450 issues, and they also maintained good ex vivo activity and brain penetration.
PYRROLIDINE, PIPERIDINE AND PIPERAZINE DERIVATIVES AND METHODS OF USE THEREOF
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Page/Page column 97, (2010/04/30)
The present invention relates to novel Pyrrolidine, Piperidine and Piperazine Derivatives, pharmaceutical compositions comprising the Pyrrolidine, Piperidine and Piperazine Derivatives and the use of these compounds for treating or preventing treating allergy, an allergy-induced airway response, congestion, a cardiovascular disease, an inflammatory disease, a gastrointestinal disorder, a neurological disoder, a metabolic disorder, obesity, an obesity-related disorder, diabetes, a diabetic complication, impaired glucose tolerance or impaired fasting glucose.
BIARYL SUBSTITUTED AZABICYCLIC ALKANE DERIVATIVES AS NICOTINIC ACETYLCHOLINE RECEPTOR ACTIVITY MODULATORS
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Page/Page column 41, (2009/06/27)
The invention relates to biaryl substituted azabicyclic alkane derivatives, compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.
Synthesis, solid structure, and optical properties of new thiophene-based alternating π-conjugated copolymers containing 4-alkyl-1,2,4-triazole or 1,3,4-thiadiazole unit as the partner unit
Yasuda, Takuma,Imase, Tatsuya,Sasaki, Shintaro,Yamamoto, Takakazu
, p. 1500 - 1503 (2007/10/03)
The synthesis, characterization, and solid-state structure of new thiophene-based alternating π-conjugated polymers containing the 4-alkyl-1,2,4-triazole or 1,2,4-thiadiazole unit as per partner unit were reported. A new thiophene-based CT type alternating copolymers was synthesized to obtain further scope about the packing structure and chemical properties of such CT type alternating π-conjugated copolymers. It was observed that the difference between the syn and anti conformations was small. It was also observed that the calculated density (1.79 g cm-3) according to the packing model agreed with the observed density (1.73 g cm-3).
Thiadiazole derivatives, process for their preparation, and their use as precursors for the production of liquid crystals
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, (2008/06/13)
Thiadiazole derivatives of the formula (I) in which the symbols and indices have the following meanings: X is Cl, Br or I; B is 1,3,4-thiadiazole-2,5-diyl; A1, A2 and A3 are identical or different and are substituted or un
