C07C229/30

LIPID PARTICLE, COMPOSITION COMPRISING LIPID PARTICLE, AND METHOD FOR DERIVERING ACTIVATORS TO CELL

The present embodiment provides a compound represented by the formula (1):


Q-CHR.sub.2  (1)

(Q is a nitrogen-containing aliphatic group containing two or more tertiary nitrogens but no oxygen, and R is an aliphatic group containing a biodegradable group). From the compound in combination with other lipids such as a lipid capable of reducing aggregation, lipid particles can be formed. Further, the compound can be used for a pharmaceutical composition to deliver an activator into cells.

L-PAG DERIVATIVES FOR TREATMENT OF SLEEP DISORDERED BREATHING (SDB)

Described herein are novel γ- and δ-propargyl carboxylic acids and esters. The novel compositions are antagonists of CSE and may be used to modulate of the activity of the carotid body, therefore providing therapeutic benefits for sleep-related breathing disorders and related conditions.

L-PAG DERIVATIVES FOR TREATMENT OF SLEEP DISORDERED BREATHING (SDB)

Described herein are novel γ- and δ-propargyl carboxylic acids and esters. The novel compositions are antagonists of CSE and may be used to modulate of the activity of the carotid body, therefore providing therapeutic benefits for sleep-related breathing disorders and related conditions.

POLYMERIZABLE POLAR COMPOUND, LIQUID CRYSTAL COMPOSITION, AND LIQUID CRYSTAL DISPLAY ELEMENT

Provided is a polar compound having high chemical stability, high capability of aligning liquid crystal molecules, high solubility in a liquid crystal composition, and a large voltage holding ratio when used in a liquid crystal display device. The compound is represented by formula (1):

##STR00001##

in which, for example, R.sup.1 is alkyl having 1 to 15 carbons; MES is a mesogen group having at least one ring; Sp.sup.1 is a single bond or alkylene having 1 to 10 carbons; M.sup.1 and M.sup.2 are hydrogen; and R.sup.2 is a group represented by formulas (1a) to (1c):

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in which, Sp.sup.2 and Sp.sup.a are a single bond or alkylene having 1 to 10 carbons; S.sup.1 is >CH—; S.sup.2 is >C<; and X.sup.1 is —OH.

IONIC DIOL, ANTISTATIC POLYURETHANE, AND METHOD OF MAKING THE SAME

An ionic diol has formula wherein R.sup.1 represents an alkyl group having from 6 to 18 carbon atoms; R.sup.2 and R.sup.3 independently represent alkyl groups having from 1 to 4 carbon atoms; R.sup.4 represents an alkylene group having from 2 to 8 carbon atoms; and R.sup.5 represents an alkylene group having from 1 to 8 carbon atoms. Antistatic polymers are formed by copolymerization of monomers including a diisocyanate, an ionic diol, a polyether diol, and at least one non-ionic diols. Methods of making the antistatic polyurethanes are also disclosed.

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IONIC DIOL, ANTISTATIC POLYURETHANE, AND METHOD OF MAKING THE SAME

An ionic diol has formula wherein R.sup.1 represents an alkyl group having from 6 to 18 carbon atoms; R.sup.2 and R.sup.3 independently represent alkyl groups having from 1 to 4 carbon atoms; R.sup.4 represents an alkylene group having from 2 to 8 carbon atoms; and R.sup.5 represents an alkylene group having from 1 to 8 carbon atoms. Antistatic polymers are formed by copolymerization of monomers including a diisocyanate, an ionic diol, a polyether diol, and at least one non-ionic diols. Methods of making the antistatic polyurethanes are also disclosed.

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INHIBITION OF PROLINE CATABOLISM FOR THE TREATMENT OF CANCER AND OTHER THERAPEUTIC APPLICATIONS
20170348266 · 2017-12-07 ·

In various embodiments a cancer treatment method is provided based on inhibition of proline catabolism. When combined with p53 restoration therapy and/or inhibition of glutaminase, the inhibition of proline catabolism results in a “synthetic lethal” and synergistic anticancer response. Novel suicide inhibitors that induce the degradation of proline dehydrogenase (PRODH) are also provided. Also provided is a method of assaying PRODH to identify responders/non-responders to inhibition of proline catabolism and/or glutaminase.

Process for the preparation of intermediates useful for the manufacture NEP inhibitors

The invention relates to a new process for producing useful intermediates for the manufacture of NEP inhibitors or prodrugs thereof, in particular NEP inhibitors comprising a γ-amino-δ-biphenyl-α-methylalkanoic acid, or acid ester, backbone, such as N-(3-carboxyl-1-oxopropyl)-(4S)-(p-phenylphenylmethyl)-4-amino-(2R)-methyl butanoic acid ethyl ester or salt thereof.

Process for the preparation of intermediates useful for the manufacture NEP inhibitors

The invention relates to a new process for producing useful intermediates for the manufacture of NEP inhibitors or prodrugs thereof, in particular NEP inhibitors comprising a γ-amino-δ-biphenyl-α-methylalkanoic acid, or acid ester, backbone, such as N-(3-carboxyl-1-oxopropyl)-(4S)-(p-phenylphenylmethyl)-4-amino-(2R)-methyl butanoic acid ethyl ester or salt thereof.

COMPOSITIONS COMPRISING A POLYMERIC NETWORK

The present invention relates to a composition comprising a polymeric network having at least one unit of formula (I), (II), and/or (III); (I) (II) (III) wherein said composition is obtained by contacting at least one compound A comprising at least two functions selected from the group of function of formula X—C(═O)—CHR.sup.1—C(═O)—R.sup.2, —C(═O)—C—R.sup.2; or —C(═O)—CR.sup.1═CR.sup.2—NR.sup.4R.sup.5; wherein at least 25% by weight of compounds A have a functionality ≦5, with % by weight relative to the total weight of compounds A; with at least one compound B comprising at least one NH.sub.2, or NH.sub.3.sup.+ groups; wherein X, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, L.sup.1 and L.sup.2 have the same meaning as that defined in the claims. The present invention also relates to a compound comprising at least two units and at most 5 units of formula (I), (II), and/or (III); wherein R.sup.1, R.sup.2, R.sup.3, X, L.sup.1 and L.sup.2 have the same meaning as that defined in the claims. The present invention also relates to processes for preparing said composition and said compounds, to material, articles, and polymers comprising or using said compositions and compounds, and the use thereof.

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