C07D225/02

CHIMERIC COMPOUNDS TARGETING PROTEINS, COMPOSITIONS, METHODS, AND USES THEREOF

The present invention provides chimeric compounds that modulate protein function, to restore protein homeostasis, including cytokine, aiolos, and/or ikaros activity, TNF-alpha activity, CK1-alpha activity and cell-cell adhesion. The invention provides methods of modulating protein-mediated diseases, such as cytokine-mediated diseases, disorders, conditions, or responses. Compositions, including in combination with other cytokine and inflammatory mediators, are provided. Methods of treatment, amelioration, or prevention of protein-mediated diseases, disorders, and conditions, such as cytokine-mediated diseases, disorders, and conditions, including inflammation, fibromyalgia, rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, psoriasis, psoriatic arthritis, inflammatory bowel diseases, Crohn's disease, ulcerative colitis, uveitis, inflammatory lung diseases, chronic obstructive pulmonary disease, Alzheimer's disease, organ transplant rejection, and cancer, are provided.

HETEROCYCLIC P2Y14 RECEPTOR ANTAGONISTS

Disclosed are compounds for treating or preventing a disease or disorder responsive to antagonism of a P2Y.sub.14R receptor agonist in a mammal in need thereof, for example, compounds of formulas (I) and (II), wherein R.sup.1.sub.-R.sup.8, X, Y, Z, X, Y, Z, and A are as defined herein, that are useful in treating an inflammatory such as asthma, cystic fibrosis, and sterile inflammation of the kidney.

##STR00001##

HETEROCYCLIC P2Y14 RECEPTOR ANTAGONISTS

Disclosed are compounds for treating or preventing a disease or disorder responsive to antagonism of a P2Y.sub.14R receptor agonist in a mammal in need thereof, for example, compounds of formulas (I) and (II), wherein R.sup.1.sub.-R.sup.8, X, Y, Z, X, Y, Z, and A are as defined herein, that are useful in treating an inflammatory such as asthma, cystic fibrosis, and sterile inflammation of the kidney.

##STR00001##

Method for reactivation of a homogeneous oxidation catalyst
20190232271 · 2019-08-01 · ·

The present invention relates to a method for the reactivation of homogeneous catalyst systems from organic reaction mixtures. The catalyst systems are suitable for the oxidation of organic compounds such as, for example, cyclododecene. The reactivation is carried out using an aqueous base.

Method for reactivation of a homogeneous oxidation catalyst
20190232271 · 2019-08-01 · ·

The present invention relates to a method for the reactivation of homogeneous catalyst systems from organic reaction mixtures. The catalyst systems are suitable for the oxidation of organic compounds such as, for example, cyclododecene. The reactivation is carried out using an aqueous base.

Cationic lipid

Provided are a cationic lipid which facilitates the introduction of a nucleic acid into, for example, a cell or the like; a composition containing the cationic lipid and a nucleic acid; a method for introducing a nucleic acid into a cell by using a composition containing the cationic lipid and the nucleic acid; and the like. The cationic lipid is, for example, a cationic lipid represented by formula (A): formula (A): ##STR00001##
(wherein R.sup.1 is alkenyl or the like, R.sup.2 is alkenyl or the like, R.sup.3 and R.sup.4 are each alkyl, or are combined together to form alkylene, or R.sup.3 and R.sup.5 are combined together to form alkylene, R.sup.5 is a hydrogen atom or the like, or is combined together with R.sup.3 to form alkylene, X.sup.1 is alkylene, and X.sup.2 is a single bond or alkylene).

CYCLIC KETO-AMIDE COMPOUNDS AS CALPAIN MODULATORS AND METHODS OF PRODUCTION AND USE THEREOF

The present technology relates to cyclic keto-amide compounds of general formulae I to XXXII, compositions and kits thereof as calpain modulators and methods useful for the treatment of various diseases or disorders such as fibrotic disease or cancer which are associated or mediated, by calpains, such as CAPN1, CAPN2, and/or CAPN9. The present technology is also applicable to cyclic keto-amide compounds which inhibit myofibroblast differentiation.

CYCLIC KETO-AMIDE COMPOUNDS AS CALPAIN MODULATORS AND METHODS OF PRODUCTION AND USE THEREOF

The present technology relates to cyclic keto-amide compounds of general formulae I to XXXII, compositions and kits thereof as calpain modulators and methods useful for the treatment of various diseases or disorders such as fibrotic disease or cancer which are associated or mediated, by calpains, such as CAPN1, CAPN2, and/or CAPN9. The present technology is also applicable to cyclic keto-amide compounds which inhibit myofibroblast differentiation.

Process for preparing polymers from monomers comprising laurolactam

Polymers can be prepared from monomers comprising laurolactam, by a process including a. Beckmann rearrangement of cyclododecanone oxime to give laurolactam in the presence of a Beckmann rearrangement catalyst, b. removal of impurities from the laurolactam to obtain purified laurolactam, and c. polymerization of monomers comprising purified laurolactam. For avoidance of discolouration or yellowing under ageing conditions, prior to the polymerization, polycyclic substances containing 24 carbon atoms and at least one heteroatom selected from oxygen and nitrogen and having a molar mass between 300 and 380 g/mol are limited to 500 ppm, based on laurolactam.

Non-chromatographic purification of macrocyclic peptides by a resin catch and release

The disclosure is directed to the synthesis and improved methods for purifying macrocyclic peptides produced by solid phase peptide synthesis. The synthesized peptide is capped with an alkyne-functionalized or azide-functionalized compound of formula (I): ##STR00001##
prior to cleavage of the peptide from the solid phase support.