C07C57/30

CO-CRYSTAL OF KETOPROFEN AND ITS PREPARATION, PHARMACEUTICAL COMPOSITIONS COMPRISING THE SAME AND USES THEREOF
20230002302 · 2023-01-05 ·

The present invention refers to a eco-crystal of Ketoprofen Lysine named Form 4, a pharmaceutical composition comprising said co-crystal, a process for its preparation and to its use in the treatment of pain and Inflammatory diseases.

CO-CRYSTAL OF KETOPROFEN AND ITS PREPARATION, PHARMACEUTICAL COMPOSITIONS COMPRISING THE SAME AND USES THEREOF
20230002302 · 2023-01-05 ·

The present invention refers to a eco-crystal of Ketoprofen Lysine named Form 4, a pharmaceutical composition comprising said co-crystal, a process for its preparation and to its use in the treatment of pain and Inflammatory diseases.

Process for preparing 2,6-dialkylphenylacetic acids

The invention relates to a multi-stage process for preparing 2,6-dialkylphenylacetic acids of the general formula (I) by reacting 2,6-dialkylbromobenzenes with (1) magnesium, (2) a formamide, (3) an acid, (4) hydrogenation of the benzaldehyde obtained, (5) activation of the benzyl alcohol obtained, (6) cyanation of the activated benzyl alcohol and (7) hydrolysis of the nitrile obtained.

Process for preparing 2,6-dialkylphenylacetic acids

The invention relates to a multi-stage process for preparing 2,6-dialkylphenylacetic acids of the general formula (I) by reacting 2,6-dialkylbromobenzenes with (1) magnesium, (2) a formamide, (3) an acid, (4) hydrogenation of the benzaldehyde obtained, (5) activation of the benzyl alcohol obtained, (6) cyanation of the activated benzyl alcohol and (7) hydrolysis of the nitrile obtained.

STRENGTHENING OXIDATION SYSTEM OF EXTERNAL MICRO-INTERFACIAL UNIT FOR PRODUCING PTA WITH PX

A strengthening oxidation system of the external micro-interfacial unit for producing PTA with PX is provided, including: a reactor, a circulating heat exchange device and a micro-interfacial unit. The reactor includes an outer casing and an inner cylinder disposed concentrically inside the outer casing. The circulating heat exchange device is disposed at an exterior of the reactor, and is connected with the outer casing and the inner cylinder respectively, for regulating reaction temperatures of the first reaction zone, the second reaction zone and the third reaction zone inside the reactor in a reaction process of producing PTA with PX. the micro-interfacial unit is connected between the reactor and the circulating heat exchange device, and connected with an external feed pipe of the reactor, for crushing a gas phase material into micro bubbles with a diameter greater than or equal to 1 μm and less than 1 mm and for mixing the micro bubbles with a liquid phase material to form an emulsion at the exterior of the reactor before a reaction material enters each of the reaction zones inside the reactor.

STRENGTHENING OXIDATION SYSTEM OF EXTERNAL MICRO-INTERFACIAL UNIT FOR PRODUCING PTA WITH PX

A strengthening oxidation system of the external micro-interfacial unit for producing PTA with PX is provided, including: a reactor, a circulating heat exchange device and a micro-interfacial unit. The reactor includes an outer casing and an inner cylinder disposed concentrically inside the outer casing. The circulating heat exchange device is disposed at an exterior of the reactor, and is connected with the outer casing and the inner cylinder respectively, for regulating reaction temperatures of the first reaction zone, the second reaction zone and the third reaction zone inside the reactor in a reaction process of producing PTA with PX. the micro-interfacial unit is connected between the reactor and the circulating heat exchange device, and connected with an external feed pipe of the reactor, for crushing a gas phase material into micro bubbles with a diameter greater than or equal to 1 μm and less than 1 mm and for mixing the micro bubbles with a liquid phase material to form an emulsion at the exterior of the reactor before a reaction material enters each of the reaction zones inside the reactor.

Substituted aromatic compounds and related method for the treatment of fibrosis

The present invention relates to compounds of: ##STR00001##
or a pharmaceutically acceptable salt thereof, wherein A is C.sub.5 alkyl, C.sub.6 alkyl, C.sub.5 alkenyl, C.sub.6 alkenyl, C(O)—(CH.sub.2).sub.n—CH.sub.3 or CH(OH)—(CH.sub.2).sub.n—CH.sub.3 wherein n is 3 or 4; R.sub.1 is H, F or OH; R.sub.2 is C.sub.5 alkyl, C.sub.6 alkyl, C.sub.5 alkenyl, C.sub.6 alkenyl, C(O)—(CH.sub.2).sub.n—CH.sub.3 or CH(OH)—(CH.sub.2).sub.n—CH.sub.3 wherein n is 3 or 4; R.sub.3 is H, F, OH or CH.sub.2Ph; R.sub.4 is H, F or OH; Q is 1) (CH.sub.2).sub.mC(O)OH wherein m is 1 or 2, 2) CH(CH.sub.3)C(O)OH, 3) C(CH.sub.3).sub.2C(O)OH, 4) CH(F)—C(O)OH, 5) CF.sub.2—C(O)OH, or 6) C(O)—C(O)OH;
and compositions comprising the same and the method using the same for the prevention or treatment of various fibrotic diseases and conditions in subjects, including pulmonary fibrosis, liver fibrosis, skin fibrosis, renal fibrosis, pancreas fibrosis, systemic sclerosis, cardiac fibrosis or macular degeneration.

Substituted aromatic compounds and related method for the treatment of fibrosis

The present invention relates to compounds of: ##STR00001##
or a pharmaceutically acceptable salt thereof, wherein A is C.sub.5 alkyl, C.sub.6 alkyl, C.sub.5 alkenyl, C.sub.6 alkenyl, C(O)—(CH.sub.2).sub.n—CH.sub.3 or CH(OH)—(CH.sub.2).sub.n—CH.sub.3 wherein n is 3 or 4; R.sub.1 is H, F or OH; R.sub.2 is C.sub.5 alkyl, C.sub.6 alkyl, C.sub.5 alkenyl, C.sub.6 alkenyl, C(O)—(CH.sub.2).sub.n—CH.sub.3 or CH(OH)—(CH.sub.2).sub.n—CH.sub.3 wherein n is 3 or 4; R.sub.3 is H, F, OH or CH.sub.2Ph; R.sub.4 is H, F or OH; Q is 1) (CH.sub.2).sub.mC(O)OH wherein m is 1 or 2, 2) CH(CH.sub.3)C(O)OH, 3) C(CH.sub.3).sub.2C(O)OH, 4) CH(F)—C(O)OH, 5) CF.sub.2—C(O)OH, or 6) C(O)—C(O)OH;
and compositions comprising the same and the method using the same for the prevention or treatment of various fibrotic diseases and conditions in subjects, including pulmonary fibrosis, liver fibrosis, skin fibrosis, renal fibrosis, pancreas fibrosis, systemic sclerosis, cardiac fibrosis or macular degeneration.

SPECIFICALLY SUBSTITUTED 3-PHENYL-5-SPIROCYCLOPENTYL-3-PYRROLIN-2-ONES AND THEIR USE AS HERBICIDES

The present invention relates to novel herbicidally active pyrrolin-2-ones of the general formula (I) or agrochemically acceptable salts thereof and to their use for controlling broad-leaved weeds and weed grasses in crops of useful plants.

SPECIFICALLY SUBSTITUTED 3-PHENYL-5-SPIROCYCLOPENTYL-3-PYRROLIN-2-ONES AND THEIR USE AS HERBICIDES

The present invention relates to novel herbicidally active pyrrolin-2-ones of the general formula (I) or agrochemically acceptable salts thereof and to their use for controlling broad-leaved weeds and weed grasses in crops of useful plants.