C07D281/02

2-homopiperazine-1-yl-4H-1,3-benzothiazine-4-one derivatives and process for the preparation of 2-(homo)piperazine 1,3-benzothiazine-4-one hydrochlorides

2-homopiperazine-1-yl-4H-1,3-bensothiazine-4-one derivatives of formula (I) are provided. They are useful in the treatment of bacterial infections, in particular tuberculosis, buruli ulcer and leprosy. A process for the preparation of 2-(homo)piperazine 1,3-benzothiazine-4-one hydrochlorides is also provided.

2-homopiperazine-1-yl-4H-1,3-benzothiazine-4-one derivatives and process for the preparation of 2-(homo)piperazine 1,3-benzothiazine-4-one hydrochlorides

2-homopiperazine-1-yl-4H-1,3-bensothiazine-4-one derivatives of formula (I) are provided. They are useful in the treatment of bacterial infections, in particular tuberculosis, buruli ulcer and leprosy. A process for the preparation of 2-(homo)piperazine 1,3-benzothiazine-4-one hydrochlorides is also provided.

HIV REPLICATION INHIBITOR

The present invention provides a novel compound having an antiviral activity, in particular, an HIV replication inhibiting activity, as well as a pharmaceutical composition, in particular, an anti-HIV agent.

##STR00001##

wherein ring A is substituted or unsubstituted carbocycle or substituted or unsubstituted heterocycle; R.sup.1 is substituted or unsubstituted alkyl etc.; R.sup.2 is substituted or unsubstituted alkyloxy etc.; n is 1 or 2; R.sup.3 is substituted or unsubstituted carbocyclyl or substituted or unsubstituted heterocyclyl; R.sup.4 is a hydrogen atom etc.; R.sup.6 is substituted or unsubstituted alkyl etc.

HIV REPLICATION INHIBITOR

The present invention provides a novel compound having an antiviral activity, in particular, an HIV replication inhibiting activity, as well as a pharmaceutical composition, in particular, an anti-HIV agent.

##STR00001##

wherein ring A is substituted or unsubstituted carbocycle or substituted or unsubstituted heterocycle; R.sup.1 is substituted or unsubstituted alkyl etc.; R.sup.2 is substituted or unsubstituted alkyloxy etc.; n is 1 or 2; R.sup.3 is substituted or unsubstituted carbocyclyl or substituted or unsubstituted heterocyclyl; R.sup.4 is a hydrogen atom etc.; R.sup.6 is substituted or unsubstituted alkyl etc.

Nrf2 regulators

The present invention relates to bis aryl analogs, pharmaceutical compositions containing them and their use as Nrf2 regulators.

Nrf2 regulators

The present invention relates to bis aryl analogs, pharmaceutical compositions containing them and their use as Nrf2 regulators.

TIANEPTINE OXALATE SALTS AND POLYMORPHS

Disclosed herein is an oxalate salt/co-crystal (tianeptine oxalate) of (RS)-7-(3-chloro-6-methyl-6,11-dihydrodibenzo[c,f][1,2]thiazepin-11-ylamino)heptanoic acid S,S-dioxide (tianeptine) as shown in Formula I:

##STR00001##

Identification of Novel Small Molecule Beta2 Integrin Agonists
20180319865 · 2018-11-08 ·

The application describes small molecules capable of modulating activity of beta2 family of integrins, such as integrin CD11b/CD18 (also known as Mac-1, CR3 and ?M?2). Such compounds may be used in certain embodiments for treating a disease or condition, such as inflammation, immune-related disorders, cancer, ischemia-reperfusion injury, stroke, neointimal thickening associated with vascular injury, wound-healing, organ transplantation and cardiovascular disease, among others.

2-HOMOPIPERAZINE-1-YL-4H-1,3-BENZOTHIAZINE-4-ONE DERIVATIVES AND PROCESS FOR THE PREPARATION OF 2- (HOMO)PIPERAZINE 1,3-BENZOTHIAZINE-4-ONE HYDROCHLORIDES
20180051016 · 2018-02-22 ·

2-homopiperazine-1-yl-4H-1, 3-bensothiazine-4-one derivatives of formula (I) are provided. They are useful in the treatment of bacterial infections, in particular tuberculosis, buruli ulcer and leprosy. A process for the preparation of 2-(homo)piperazine 1, 3-benzothiazine-4-one hydrochlorides is also provided.

Crystal modifications of elobixibat

The present invention relates to crystal modifications of N-{(2R)-2-[({[3,3-dibutyl-7-(methyl-thio)-1,1-dioxido-5-phenyl-2,3,4,5-tetrahydro-1,5-benzothiazepin-8-yl]oxy}acetyl)amino]-2-phenylethanolyl}glycine (elobixibat), more specifically crystal modifications I, IV, MeOH-1, EtOH-1, 1-PrOH-1 and 2-PrOH-1. The invention also relates to a process for the preparation of these crystal modifications and to a pharmaceutical composition comprising crystal modification IV.