C07C273/18

Enantiomerically pure binaphthol derivatives and method for preparing the same

The present invention relates to compounds 1, 1a (S-enantiomer) and 1b (R-enantiomer) of the following formula 1, and a method for preparing the same. [formula 1] The novel compound of the formula 1 is used as an important intermediate for preparing compounds 6, 6a (S-enantiomer) and 6b (R-enantiomer) of the following formula 6, which are 2,2-binaphthol-3-aldehyde derivatives. Also, the present invention provides a method for preparing the compound of formula 1 with a very safe method at low cost. [formula 6]

Solid drug form of N-(2,6-bis(1-methylethyl)phenyl)-N′-((1-(4-(dimethylamino)phenyl)cyclopentyl)methyl)urea hydrochloride and compositions, methods and kits related thereto

A novel solid drug form of N-(2,6-bis(1-methylethyl)phenyl)-N-((1-(4-(dimethylamino)phenyl)cyclopentyl)methyl)urea hydrochloride (also referred to ATR-101) suitable for oral dosing, and to compositions, methods and kits relating thereto. ATR-101 has particular utility in the treatment of, for example, aberrant adrenocortical cellular activity, including adrenocortical carcinoma (ACC), congenital adrenal hyperplasia (CAH) and Cushing's syndrome.

METHOD FOR PRODUCING AMIDES OR POLYAMIDES BY USING AROMATIC CARBAMATES BY WAY OF ISOCYANATES AS PRECURSORS THROUGH CATALYZED THERMAL PROCESSES AND METHOD FOR PRODUCING AROMATIC CARBAMATE PRECURSORS FROM AROMATIC AMINES
20180186731 · 2018-07-05 ·

The present invention is directed to a process for preparing amides or polyamides by replacing isocyanate starting materials of a catalyzed thermal reaction with aromatic carbamates. Through the catalyzed thermal process involving a non-isocyanate precursor of the present invention, efficiency for producing amides or polyamides can be significantly improved, and the impure side products produced from a side reaction of isocyanate can be greatly curtailed. Hence, amides or polyamides of high purity and yield can be achieved. The invention also relates to a process for preparing aromatic carbamates, the new non-isocyanate precursors for amides or polyamides.

UREAURETHANES FOR RHEOLOGY CONTROL

The present invention relates to ureaurethanes of the following formula (I)

##STR00001##

in which at least one of the R.sup.1 or R.sup.2 radicals is a mono- or polyunsaturated, branched or unbranched alkenyl or alkynyl radical having 12 to 24 carbon atoms, n is an integer 1, where the upper limit for n arises from the maximum number average molecular weight M.sub.n of the ureaurethanes of the general formula (I), which is 65 000 g/mol, and which is determined by means of gel permeation chromatography to DIN 55672-2 using a polymethyl methacrylate standard, R.sup.3 is a xylylene radical or a hydrogenated xylylene radical and R.sup.4 is a tolylene radical or various other radicals. The invention also relates to ureaurethane compositions comprising the ureaurethanes of the invention and to the preparation of both. The invention further relates to the use of the ureaurethanes or ureaurethane compositions as rheology control agent and anti-settling agent. The invention further provides liquid formulations from the group consisting of coating compositions, polymer formulations, pigment pastes, sealant formulations, cosmetics, ceramic formulations, drilling fluids, adhesive formulations, potting compounds, construction material formulations, lubricants, spackling compounds, printing inks and other inks, comprising the ureaurethanes and ureaurethane compositions.

UREAURETHANES FOR RHEOLOGY CONTROL

The present invention relates to ureaurethanes of the following formula (I)

##STR00001##

in which at least one of the R.sup.1 or R.sup.2 radicals is a mono- or polyunsaturated, branched or unbranched alkenyl or alkynyl radical having 12 to 24 carbon atoms, n is an integer 1, where the upper limit for n arises from the maximum number average molecular weight M.sub.n of the ureaurethanes of the general formula (I), which is 65 000 g/mol, and which is determined by means of gel permeation chromatography to DIN 55672-2 using a polymethyl methacrylate standard, R.sup.3 is a xylylene radical or a hydrogenated xylylene radical and R.sup.4 is a tolylene radical or various other radicals. The invention also relates to ureaurethane compositions comprising the ureaurethanes of the invention and to the preparation of both. The invention further relates to the use of the ureaurethanes or ureaurethane compositions as rheology control agent and anti-settling agent. The invention further provides liquid formulations from the group consisting of coating compositions, polymer formulations, pigment pastes, sealant formulations, cosmetics, ceramic formulations, drilling fluids, adhesive formulations, potting compounds, construction material formulations, lubricants, spackling compounds, printing inks and other inks, comprising the ureaurethanes and ureaurethane compositions.

Process for preparing low-viscosity allophanates containing actinically curable groups
09988485 · 2018-06-05 · ·

The present invention provides a process for preparing radiation-curing allophanates having residual monomer contents of less than 0.5% by weight and an NCO content of less than 1% by weight, wherein (A) compounds containing isocyanate groups, (B) hydroxy-functional compounds which contain groups which react, with polymerization, with ethylenically unsaturated compounds on exposure to actinic radiation (radiation-curing groups) and (C) optionally further compounds containing NCO-reactive groups, also optionally in the presence of a catalyst, are used to form NCO-group-containing urethanes having radiation-curing groups, which are subsequently reacted, without further addition of compounds containing isocyanate groups, in the presence of an allophanatization catalyst, the ratio of NCO groups of the compounds from A) to the OH groups of the compounds from B) and, where used, C) being 1.45:1.0 to 1.1:1.0.

NOVEL KCNQ POTASSIUM CHANNEL AGONIST, AND PREPARATION METHOD THEREFOR AND USE THEREOF

The present invention provides a compound represented by general formula I or a pharmaceutical acceptable salt thereof, the preparation method therefor and the use thereof in preparing a medicine for treating a neurological disease, such as epilepsy, convulsion, neuropathic pain, acute ischemic stroke, and a neurodegenerative disease. The compound according to present invention has a better absorption in brain tissue when compared with RTG. In addition, the compound provided by present invention has not only a greatly enhanced efficacy, but also a neurotoxicity greatly lower than that of RTG, and thus possesses a wider safety window.

##STR00001##

NOVEL KCNQ POTASSIUM CHANNEL AGONIST, AND PREPARATION METHOD THEREFOR AND USE THEREOF

The present invention provides a compound represented by general formula I or a pharmaceutical acceptable salt thereof, the preparation method therefor and the use thereof in preparing a medicine for treating a neurological disease, such as epilepsy, convulsion, neuropathic pain, acute ischemic stroke, and a neurodegenerative disease. The compound according to present invention has a better absorption in brain tissue when compared with RTG. In addition, the compound provided by present invention has not only a greatly enhanced efficacy, but also a neurotoxicity greatly lower than that of RTG, and thus possesses a wider safety window.

##STR00001##

6-amino-5,6,7,8-tetrahydronaphthalen-2-yl or 3-aminochroman-7-yl derivatives

The present invention relates to compounds TAAR receptor antagonists of formula I wherein X, R, L, Ar and R.sup.1 are as described herein, compositions containing compounds of formula I, methods of manufacture of compounds of formula I and methods of treating psychiatric disorders with compounds of formula I. ##STR00001##

Solid drug form of N-(2,6-bis(1-methylethyl)phenyl)-N′-((1-(4-(dimethylamino)phenyl)cyclopentyl)methyl)urea hydrochloride and compositions, methods and kits related thereto

A novel solid drug form of N-(2,6-bis(1-methylethyl)phenyl)-N-((1-(4-(dimethylamino)phenyl)cyclopentyl)methyl)urea hydrochloride (also referred to ATR-101) suitable for oral dosing, and to compositions, methods and kits relating thereto. ATR-101 has particular utility in the treatment of, for example, aberrant adrenocortical cellular activity, including adrenocortical carcinoma (ACC), congenital adrenal hyperplasia (CAH) and Cushing's syndrome.