549532-08-3

Upstream product

• 109431-87-0 (R)-tert-butyl 3-hydroxypyrrolidine-1-carboxylate 
• 74-88-4 methyl iodide 
• 24424-99-5 di-tert-butyl dicarbonate 
• 77-78-1 dimethyl sulfate 

Downstream Products

• 120099-60-7 (3R)-3-methoxypyrrolidine 
• 474707-30-7 (3R)-3-methoxypyrrolidine hydrochloride 

Relevant academic research and scientific papers

4-PYRIDONE COMPOUND OR SALT THEREOF, AND PHARMACEUTICAL COMPOSITION AND FORMULATION INCLUDING SAME

An object of the present invention is to provide a compound or a salt thereof having anti-HBV activity, a pharmaceutical composition, an anti-hepatitis B virus agent, a production inhibitor of DNA of a hepatitis B virus, and a production or secretion inhibitor of a hepatitis B surface antigen. According to the present invention, provided are a compound represented by General Formula [1] or a salt thereof: (in the formula, R1 represents a benzothiazolyl group which may be substituted (in which a carbon atom constituting the 6-membered ring of the benzothiazolyl group of R1 is bonded to the nitrogen atom of the pyridone ring); R2 represents a C2-6 alkenyl group which may be substituted, or the like; and R3 represents a hydrogen atom or the like).

COMPOUNDS AND THEIR METHODS OF USE

The present invention is directed to, in part, fused heteroaryl compounds and compositions useful for preventing and/or treating a disease or condition relating to aberrant function of a voltage-gated, sodium ion channel, for example, abnormal late/persistent sodium current. Methods of treating a disease or condition relating to aberrant function of a sodium ion channel including Dravet syndrome or epilepsy are also provided herein.

AMINOPYRIMIDINE HETEROCYCLIC COMPOUND WITH ADENOSINE RECEPTOR ANTAGONISTIC ACTIVITY

Disclosed hereinis an aminopyrimidine heterocyclic compound with adenosine receptor antagonistic activity, comprising a compound of the general formula (I), or a pharmaceutically acceptable salt thereof. The aminopyrimidine heterocyclic compound with adenosine receptor antagonistic activitydisclosed herein can be used as an effective adenosine receptor antagonist, and can be used for the treatment or prevention of disorders caused by abnormal level of adenosine.

Protecting-group-free catalytic asymmetric total synthesis of (-)-rosmarinecine

The protecting-group-free asymmetric total synthesis of (-)-rosmarinecine was achieved in only four steps from the commercially available (±)-3-hydroxypyrrolidine hydrochloride (2a). The key steps include the direct oxidation of (±)-2a to (±)-3-hydroxy-1-pyrroline N-oxide (1a) using the Davis reagent and the domino reaction; viz., the lipase-catalyzed dynamic kinetic resolution of (±)-1a with 1-ethoxyvinyl ethyl maleate followed by the intramolecular [3+2] dipolar cycloaddition reaction of the generated optically active ester. Some insights into the mechanism of the racemization of the optically active 1a, observed during the enzymatic process, were also obtained.

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.

5,7-DIAMINOPYRAZOLO [4,3-d] PYRIMIDINES WITH PDE-5 INHIBITING ACTIVITY

This invention relates to compounds of formula (I).

PYRAZOLO`4,3-D! PYRIMIDINES

This invention relates to compounds of formula (I).

PYRAZOLE DERIVATIVE

Not available

5,7-DIAMINOPYRAZOLO`4,3-D!PYRIMIDINES USEFUL IN THE TREATMENT OF HYPERTENSION

This invention relates to compounds of formula (I).

TRIAZOLE COMPOUNDS FOR THE TREATMENT OF DYSMENORRHOEA

A compound of formula (I), a pharmaceutically acceptable salt or solvate thereof, wherein R' represents C,-C6 alkyl,-(CH2)c-[C3-C8 cycloalkyl]-,-(CH2)C-W or-(CH2)C-Z-(CH2)dW; W represents C1-C6 alkyl, C1-C6 alkyloxy,-C02[C1-C6 alkyl],-CONR4R5, an optionally substituted phenyl group, NR4R5, het2 or het3; Z represents O or S(O)g; g represents 0, 1 or 2; R2 represents a phenyl group, optionally fused to a 5-or 6-membered aryl or heterocyclic group which may contain one or more heteroatoms selected from N, O or S; the phenyl group and the optionally fused group being optionally substituted; Ring A represents a 4-, 5-or 6-membered saturated heterocyclic group containing at least one N; Ring B represents a phenyl group or het1, each group being optionally substituted; R7 independently represents H1 C1-C6alkyl, OR3,-(CH2)e-R3 or-(CH2)f-O-(CH2)e-R3; at each occurrence R3 independently represents H1 C1-C6 alkyl optionally substituted by Y,-(CH2)g [C3-C8 cycloalkyl], phenyl, benzyl, pyridyl or pyrimidyl; at each occurrence R4 and R5independently represent H1 Cl-C6 alkyl (optionally substituted with Cl-C6alkyloxy), (CH2)gC02-[C1-C6 alkyl],-S02Me,-(CH2)g[C3-C8 cycloalkyl], S02Me, phenyl, benzyl, pyridyl or pyrimidyl; or R4 and R5 together with the N atom to which they are attached represent a heterocyclic group of from 3 to 8 atoms; Y independently represents a phenyl group, NR4R5 or het4, the phenyl group being optionally substituted; het1 represents a 4-, 5-or 6-membered saturated, or unsaturated, heterocyclic group containing at least one N (but which may also contain one or more O or S atoms); het2 and het4 represent an optionally substituted 4-, 5-, 6-or 7-membered saturated, or unsaturated, heterocyclic group containing at least one N (but which may 5 also contain one or more O or S atoms); het3 represents an optionally substituted 4-, 5-, 6-or 7-membered saturated, or unsaturated, heterocyclic group containing at least one O (but which may also contain one or mare N or S atoms); at each occurrence R6 independently represents H1 C1-C6 alkyl optionally substituted by Y, =(CH2)g [C3-C8 cycloalkyl], phenyl, benzyl, pyridyl or pyrimidyl; a and b independently represent 0 or 1; c,, d, a end g independently represent 0, 1, 2, 3 or 4; . f índeperldently represents 1, 2, 3 or 4; provided that: (i) a + b cannot equal 0; and províded,that,when R1 represents-(CH2)c-Z-(CH2)d-W and W represents.NR4R5 or any N linked heterocyclic, group then d must not be, 0 or 1; and (iii), provided that when R2 represents a phenyl group substituted by a group of, formula-(CH2)eOR3,-(CH2)e-OCOR3 or-(CH2)e,OCOR3 ;or het1,and/or het2 are substituted by a group of formula-(CH2)eOR3, (CH2),-CO2R3 or-(CH2)eOCOR3; or when R7 represents-OR3 or-(CH2)f-0-(CH2)e-R3 and e is 0; or when W represents a phenyl group substituted with-OR3 or-C02R3 and R3 represents an alkyl group substituted with Y, and Y represents NR4R5 or an N-Finked het3; then, R3, must,represent,C2-C6 alkyl substituted with. Y. are useful in the treatment of dysmenorrhoea.