C07C275/50

UREA DERIVATIVE OR PHARMACOLOGICALLY ACCEPTABLE SALT THEREOF

The present invention provides a urea compound or a pharmacologically acceptable salt thereof that has a formyl peptide receptor like 1 (hereinafter may be abbreviated as FPRL1) agonist effect, a pharmaceutical composition containing the urea compound or the pharmacologically acceptable salt thereof, and a pharmaceutical use thereof. It has been found that a urea derivative represented by the general formula (I) below or a pharmacologically acceptable salt thereof has a superior FPRL1 agonist effect. Compound (I) or a pharmacologically acceptable salt thereof is highly useful for treatment, prevention, or suppression of inflammatory diseases, chronic airway diseases, cancers, septicemia, allergic symptoms, HIV retrovirus infection, circulatory disorders, neuroinflammation, nervous disorders, pains, prion diseases, amyloidosis, immune disorders and the like.

##STR00001##

Affinity medicant conjugate
09980926 · 2018-05-29 · ·

In an embodiment of the invention, a composition for treating a cell population comprises an Affinity Medicant Conjugate (AMC). The medicant moiety can be a toxin including an acylfulvene or a drug moiety. The affinity moiety can be an antibody, a binding protein, a steroid, a lipid, a growth factor, a protein, a peptide or non peptidic. The affinity moiety can be covalently bound to the medicant via a linker. Novel linkers that can be directed to cysteine, arginine or lysine residues based on solution pH allow greater flexibility in preserving and/or generating specific epitopes in the AMC.

Method for enhancing the rate of the formation of the reaction product of a carboxylic acid and urea via acid addition
09920001 · 2018-03-20 · ·

The present invention is directed to a method for enhancing the rate of formation of the reaction products of a carboxylic acid and a urea having the formula: ##STR00001##
where R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are the same or different and are selected from the group consisting of hydrogen, substituted and unsubstituted alkyl, allyl, vinyl and alkoxyl groups having from 1-6 carbon atoms, substituted and unsubstituted phenyl groups and the halides. The rate of formation is enhanced by adding acid to a solution including the carboxylic acid and the urea. Preferably, the reaction product of the present invention is N,N-diformylurea or N,N-diacetylurea. These reaction products, e.g., diformylurea, have been found to produce significantly improved growth in a variety of agricultural products when applied to the seed, to the surrounding soil or to the foliage of the emerging plant.

Method for enhancing the rate of the formation of the reaction product of a carboxylic acid and urea via acid addition
09920001 · 2018-03-20 · ·

The present invention is directed to a method for enhancing the rate of formation of the reaction products of a carboxylic acid and a urea having the formula: ##STR00001##
where R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are the same or different and are selected from the group consisting of hydrogen, substituted and unsubstituted alkyl, allyl, vinyl and alkoxyl groups having from 1-6 carbon atoms, substituted and unsubstituted phenyl groups and the halides. The rate of formation is enhanced by adding acid to a solution including the carboxylic acid and the urea. Preferably, the reaction product of the present invention is N,N-diformylurea or N,N-diacetylurea. These reaction products, e.g., diformylurea, have been found to produce significantly improved growth in a variety of agricultural products when applied to the seed, to the surrounding soil or to the foliage of the emerging plant.

DISULFUR BRIDGE LINKERS FOR CONJUGATION OF A CELL-BINDING MOLECULE
20170209595 · 2017-07-27 · ·

The present invention relates to novel disulfur bridge linkers containing hydrazine used for the specific conjugation of compounds/cytotoxic agents to a cell-binding molecule, through bridge linking a pair of thiols on the cell-binding molecule. The invention also relates to methods of making such linkers, and of using such linkers in making homogeneous conjugates, as well as of application of the conjugates in treatment of cancers, infections and autoimmune disorders.

DISULFUR BRIDGE LINKERS FOR CONJUGATION OF A CELL-BINDING MOLECULE
20170202975 · 2017-07-20 · ·

The present invention relates to novel disulfur bridge linkers containing hydrazine used for the specific conjugation of compounds/cytotoxic agents to a cell-binding molecule, through bridge linking a pair of thiols on the cell-binding molecule. The invention also relates to methods of making such linkers, and of using such linkers in making homogeneous conjugates, as well as of application of the conjugates in treatment of cancers, infections and autoimmune disorders.

DISULFUR BRIDGE LINKERS FOR CONJUGATION OF A CELL-BINDING MOLECULE
20170151346 · 2017-06-01 · ·

The present invention relates to novel disulfur bridge linkers containing hydrazine used for the specific conjugation of compounds/cytotoxic agents to a cell-binding molecule, through bridge linking a pair of thiols on the cell-binding molecule. The invention also relates to methods of making such linkers, and of using such linkers in making homogeneous conjugates, as well as of application of the conjugates in treatment of cancers, infections and autoimmune disorders.

PYRIMIDINE COMPOUND AND MEDICAL USE THEREOF

The present invention relates to a pyrimidine compound or a pharmaceutically acceptable salt thereof represented by the following formula [I]

##STR00001##

wherein each symbol is as defined in the specification and a method of therapeutically or prophylactically treating an undesirable cell proliferation, comprising administering such a compound. The compound of the present invention has superior activity in suppressing undesirable cell proliferation, particularly, an antitumor activity, and is useful as an antitumor agent for the prophylaxis or treatment of cancer, rheumatism, and the like. In addition, the compound of the present invention can be a more effective antitumor agent when used in combination with other antitumor agents such as an alkylating agent or metabolism antagonist.

Cyclic diones as herbicidal compounds

The present invention relates to compounds of Formula (I), wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4x, R.sup.4y, m, n and G are as defined herein. The invention further relates to herbicidal compositions which comprise a compound of Formula (I), to their use for controlling weeds, in particular in crops of useful plants. ##STR00001##

Cyclic diones as herbicidal compounds

The present invention relates to compounds of Formula (I), wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4x, R.sup.4y, m, n and G are as defined herein. The invention further relates to herbicidal compositions which comprise a compound of Formula (I), to their use for controlling weeds, in particular in crops of useful plants. ##STR00001##