Patent classifications
C07C233/61
Cool-sensation imparter composition containing 2,2,6-trimethylcyclohexanecarboxylic acid derivative
A cooling agent composition contains a 2,2,6-trimethylcyclohexanecarboxylic acid derivative represented by the following general formula (1). The symbol * represents an asymmetric carbon atom. X represents NH, N(ZAr.sup.2), O or S, Z represents a single bond or an alkylene group having 1 to 3 carbon atoms which may have a substituent, Ar.sup.2 represents an aryl group having 6 to 20 carbon atoms which may have a substituent or an aromatic heterocyclic group having 2 to 15 carbon atoms which may have a substituent. Y each independently represents a methylene group which may have a substituent, and n represents an integer of 0 to 3. Ar.sup.1 represents an aryl group having 6 to 20 carbon atoms which may have a substituent or an aromatic heterocyclic group having 2 to 15 carbon atoms which may have a substituent. ##STR00001##
ORTHO-PHTHALALDEHYDE CONTAINING LINKERS AND USE FOR PREPARATION OF ANTIBODY-DRUG CONJUGATE
Provided herein are novel ortho-Phthalaldehyde (OPA) containing linkers (OPA-L) and the use of OPA-L for the preparation of Antibody-drug conjugate (ADC) via the formation of Phthalimidine through the reaction of primary amine on antibody (e.g., residue of Lysine) and ortho-Phthalaldehyde. The advantage of this OPA-L is high reactivity and can be applied in different types of antibodies to form stably-linked conjugates. The use of OPA-L for the preparation of ADC is advantageous for mild and wide condition of conjugation, for instance, low percentage of organic solvent required, wide range of pH and temperature can be used.
ORTHO-PHTHALALDEHYDE CONTAINING LINKERS AND USE FOR PREPARATION OF ANTIBODY-DRUG CONJUGATE
Provided herein are novel ortho-Phthalaldehyde (OPA) containing linkers (OPA-L) and the use of OPA-L for the preparation of Antibody-drug conjugate (ADC) via the formation of Phthalimidine through the reaction of primary amine on antibody (e.g., residue of Lysine) and ortho-Phthalaldehyde. The advantage of this OPA-L is high reactivity and can be applied in different types of antibodies to form stably-linked conjugates. The use of OPA-L for the preparation of ADC is advantageous for mild and wide condition of conjugation, for instance, low percentage of organic solvent required, wide range of pH and temperature can be used.
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.
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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.
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Methods and compositions for genome editing via haploid induction
Methods and compositions for improved plant breeding using gene editing and haploid induction are provided.
SUBSTITUTED AMIDE COMPOUNDS USEFUL AS FARNESOID X RECEPTOR MODULATORS
Disclosed are compounds of Formula (I) or a stereoisomer, a tautomer, or a pharmaceutically acceptable salt or solvate thereof, wherein Q is a 5-membered heterocyclyl or 5-membered heteroaryl having 1 to 4 heteroatoms independently selected from N, O, and S, substituted with zero to 4 R.sup.1; and A, X.sup.1, X.sup.2, X.sup.3, X.sup.4, Z.sup.1, Z.sup.2, R.sup.1, R.sup.2, R.sup.3a, R.sup.3b, a, b, and d are defined herein. Also disclosed are methods of using these compounds to modulate the activity of farnesoid X receptor (FXR); pharmaceutical compositions comprising these compounds; and methods of treating a disease, disorder, or condition associated with FXR dysregulation, such as pathological fibrosis, transplant rejection, cancer, osteoporosis, and inflammatory disorders, by using the compounds and pharmaceutical compositions.
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SUBSTITUTED AMIDE COMPOUNDS USEFUL AS FARNESOID X RECEPTOR MODULATORS
Disclosed are compounds of Formula (I) or a stereoisomer, a tautomer, or a pharmaceutically acceptable salt or solvate thereof, wherein Q is a 5-membered heterocyclyl or 5-membered heteroaryl having 1 to 4 heteroatoms independently selected from N, O, and S, substituted with zero to 4 R.sup.1; and A, X.sup.1, X.sup.2, X.sup.3, X.sup.4, Z.sup.1, Z.sup.2, R.sup.1, R.sup.2, R.sup.3a, R.sup.3b, a, b, and d are defined herein. Also disclosed are methods of using these compounds to modulate the activity of farnesoid X receptor (FXR); pharmaceutical compositions comprising these compounds; and methods of treating a disease, disorder, or condition associated with FXR dysregulation, such as pathological fibrosis, transplant rejection, cancer, osteoporosis, and inflammatory disorders, by using the compounds and pharmaceutical compositions.
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Isotope-enriched 3-amino-1-propanesulfonic acid derivatives and uses thereof
There are provided isotope-enriched compounds of Formula (I) and pharmaceutically acceptable salts or esters thereof, as well as pharmaceutical compositions thereof and methods of use thereof for prevention and treatment of amyloid- related diseases, such as Alzheimer's disease.
R.sup.1R.sup.2XCR.sub.2CH.sub.2CH.sub.2SO.sub.3H(I)
COOL-SENSATION IMPARTER COMPOSITION CONTAINING 2,2,6-TRIMETHYLCYCLOHEXANECARBOXYLIC ACID DERIVATIVE
A cooling agent composition contains a 2,2,6-trimethylcyclohexanecarboxylic acid derivative represented by the following general formula (1). The symbol * represents an asymmetric carbon atom. X represents NH, N(ZAr.sup.2), O or S, Z represents a single bond or an alkylene group having 1 to 3 carbon atoms which may have a substituent, Ar.sup.2 represents an aryl group having 6 to 20 carbon atoms which may have a substituent or an aromatic heterocyclic group having 2 to 15 carbon atoms which may have a substituent. Y each independently represents a methylene group which may have a substituent, and n represents an integer of 0 to 3. Ar.sup.1 represents an aryl group having 6 to 20 carbon atoms which may have a substituent or an aromatic heterocyclic group having 2 to 15 carbon atoms which may have a substituent.
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