460748-80-5

Usage

Uses

Used in Pharmaceutical Industry:
(R)-2-ethylpyrrolidine hydrochloride is used as a reagent for the synthesis of 6-(4-pyrimidinyl)-1H-indazole derivatives. These derivatives serve as PDK1 kinase inhibitors, which are useful in the treatment of cancer, immune, metabolic, and other kinase-mediated diseases. (R)-2-ethylpyrrolidine hydrochloride's role in this application is crucial for developing potential therapeutic agents that can target specific kinases involved in these diseases.
Used in Medicinal Chemistry:
(R)-2-ethylpyrrolidine hydrochloride is also used as a reagent in the synthesis of aryloxazole derivatives. These derivatives act as histamine H3 receptor antagonists or inverse agonists, which have potential applications in the treatment of various conditions, such as cognitive disorders, sleep-wake regulation, and other histamine-related pathologies. (R)-2-ethylpyrrolidine hydrochloride's involvement in this synthesis process highlights its importance in the development of novel drugs targeting histamine receptors.

Upstream product

• 86661-32-7 (S)-tert-butyl 2-((tosyloxy)methyl)pyrrolidine-1-carboxylate 
• 69610-40-8 N-(tert-butoxycarbonyl)-L-prolinol 
• 1227910-54-4 phenylmethyl (2R)-2-ethyl-1-pyrrolidinecarboxylate 
• 876617-06-0 tert-butyl (2R)-2-ethylpyrrolidine-1-carboxylate 

Relevant academic research and scientific papers

2-ACYLAMINOTHIAZOLE DERIVATIVE OR SALT THEREOF

To provide a compound useful as an active ingredient of a pharmacological composition for the treatment of urinary storage symptoms, dysuria, lower urinary tract diseases, and the like. [Solution] The inventors perfected the present invention after discov

2-ACYLAMINOTHIAZOLE DERIVATIVE AND SALT THEREOF

[Problem] A compound which is useful as an active ingredient of a pharmaceutical composition for treating storage dysfunctions, voiding dysfunctions, and lower urinary tract diseases is provided. [Means for Solution] The present inventors have found that a thiazole derivative having pyrazine-2-carbonylamino substituted at the 2-position is an excellent muscarinic M3 receptor positive allosteric modulator, and is useful as an agent for preventing and/or treating bladder or urinary tract diseases, related to bladder contraction by a muscarinic M3 receptor, thereby completing the present invention. The 2-acylaminothiazole derivative or a salt thereof of the present invention can be used as an agent for preventing and/or treating bladder or urinary tract diseases, related to bladder contraction by a muscarinic M3 receptor, for example, voiding dysfunctions such as underactive bladder.

2-ACYLAMINOTHIAZOLE DERIVATIVE AND SALT THEREOF

[Problem] A compound which is useful as an active ingredient of a pharmaceutical composition for treating storage dysfunctions, voiding dysfunctions, and lower urinary tract diseases is provided. [Means for Solution] The present inventors have found that a thiazole derivative having pyrazine-2-carbonylamino substituted at the 2-position is an excellent muscarinic M 3 receptor positive allosteric modulator, and is useful as an agent for preventing and/or treating bladder or urinary tract diseases, related to bladder contraction by a muscarinic M 3 receptor, thereby completing the present invention. The 2-acylaminothiazole derivative or a salt thereof of the present invention can be used as an agent for preventing and/or treating bladder or urinary tract diseases, related to bladder contraction by a muscarinic M 3 receptor, for example, voiding dysfunctions such as underactive bladder.

CHEMICAL COMPOUNDS

The invention is directed to to substituted indazole derivatives. Specifically, the invention is directed to compounds according to Formula I: wherein R1 - R6 and X are defined herein. The compounds of the invention are inhibitors of PDK1 and can be useful in the treatment of disorders characterized by constitutively activated ACG kinases such as cancer and more specifically leukemia and cancers of the breast, colon, and lung. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting PDK1 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.

OXAZOLE DERIVATIVES AS HISTAMINE H3 RECEPTOR AGENTS, PREPARATION AND THERAPEUTIC USES

The present invention discloses novel aryl oxazole compounds of Formula I (I), or pharmaceutically acceptable salts thereof, which have histamine-H3 receptor antagonist or inverse agonist activity, as well as methods for preparing and using such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I as well as methods of using these compositions to treat obesity, cognitive deficiencies, narcolepsy, and other histamine H3 receptor-related diseases. Formula I (I) or a pharmaceutically acceptable salt thereof, wherein: m is independenlly at each occurrence 1, 2, or 3, Z independently represents carbon (substituted with hydrogen or the optional substituents indicated herein) or nitrogen, provided that when Z is nitrogen then R6 is not attached to Z; R1 and R2 are independently -(C1-C7) alkyl(optionally substituted with one to three halogens), or R1 and R2 and the nitrogen to which they are attached form an azetidinyl ring, a pyrrolidinyl ring, or a piperidinyl ring, wherein further the azetidinyl, pyrrolidinyl, or piperidinyl ring so formed may be optionally substituted one to three times with R5; R6 is independently at each occurrence -H, -halogen, or -CH3.