C07D307/16

SUBSTITUTED CYCLOHEXYL COMPOUNDS AS NOP INHIBITORS

Substituted cyclohexyl chemical entities of Formula (I): wherein R.sup.a, G, and R.sup.b have any of the values described herein, and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies; detection and imaging techniques; radioactive therapies; modulating and treating disorders mediated by nociceptin activity or dopamine signaling; treating neurological disorders, neurodegenerative diseases, depression, and schizophrenia; enhancing the efficiency of cognitive and motor training; and treating peripheral disorders, including renal, respiratory, gastrointestinal, liver, genitourinary, metabolic, and inflammatory disorders.

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SUBSTITUTED CYCLOHEXYL COMPOUNDS AS NOP INHIBITORS

Substituted cyclohexyl chemical entities of Formula (I):

##STR00001## wherein R.sup.a, G, and R.sup.b have any of the values described herein, and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies; detection and imaging techniques; radioactive therapies; modulating and treating disorders mediated by nociceptin activity or dopamine signaling; treating neurological disorders, neurodegenerative diseases, depression, and schizophrenia; enhancing the efficiency of cognitive and motor training; and treating peripheral disorders, including renal, respiratory, gastrointestinal, liver, genitourinary, metabolic, and inflammatory disorders.

HERBICIDAL MALONAMIDES

The invention relates to compounds of formula (I), and their use as herbicides. In said formula, R.sup.1 to R.sup.9 represent groups such as hydrogen, halogen or organic groups such as alkyl, alkenyl, alkynyl, or alkoxy; X is a bond or a divalent unit; Y is hydrogen, cyano, hydroxyl or a linear or cyclic organic group. The invention further refers to a composition comprising such compound and to the use thereof for controlling unwanted vegetation.

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PROCESSES AND INTERMEDIATES FOR THE PREPARATION OF CARBAPROSTACYCLIN ANALOGUES

The invention relates to processes for preparing carbaprostacyclin analogues and intermediates prepared from the processes. The invention also relates to cyclopentenone intermediates in racemic or optically active form.

PROCESSES AND INTERMEDIATES FOR THE PREPARATION OF CARBAPROSTACYCLIN ANALOGUES

The invention relates to processes for preparing carbaprostacyclin analogues and intermediates prepared from the processes. The invention also relates to cyclopentenone intermediates in racemic or optically active form.

CXCR6 SULFONAMIDE COMPOUNDS

Provided are sulfonamide compounds having formula (I):

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or a pharmaceutically acceptable salt thereof, wherein R, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and the subscripts n and m have the meanings provided in the specification. The compounds are useful for treating diseases and conditions associated with CXCR6 activity.

CXCR6 SULFONAMIDE COMPOUNDS

Provided are sulfonamide compounds having formula (I):

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or a pharmaceutically acceptable salt thereof, wherein R, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and the subscripts n and m have the meanings provided in the specification. The compounds are useful for treating diseases and conditions associated with CXCR6 activity.

COMPOSITIONS AND METHODS FOR IMMUNE MODULATION AND TREATMENT OF CANCER

The disclosure relates to rexinoids, including compounds of the Formula (I) and (II) or a pharmaceutically acceptable salt, polymorph, prodrug, solvate or clathrate thereof. These rexinoids are useful for increasing PD-L1 in vivo, for treatment of cancer, and for inhibiting the onset of cancer.

INTERMEDIATES IN THE SYNTHESIS OF C3-SUBSTITUTED CEPHALOSPORINS
20210261571 · 2021-08-26 ·

Disclosed herein are novel and inventive methods for preparing intermediates in the synthesis of C3-substituted cephalosporins. One preferred C3-substituted cephalosporin of clinical interest is Cefovecin. Accordingly, the present invention provides for methods of preparing reactive halogen intermediates for use in the synthesis of C3-substituted cephalosporins, such as Cefovecin. In the case of Cefovecin the reactive intermediates are of the formula:

##STR00001##

INTERMEDIATES IN THE SYNTHESIS OF C3-SUBSTITUTED CEPHALOSPORINS
20210261571 · 2021-08-26 ·

Disclosed herein are novel and inventive methods for preparing intermediates in the synthesis of C3-substituted cephalosporins. One preferred C3-substituted cephalosporin of clinical interest is Cefovecin. Accordingly, the present invention provides for methods of preparing reactive halogen intermediates for use in the synthesis of C3-substituted cephalosporins, such as Cefovecin. In the case of Cefovecin the reactive intermediates are of the formula:

##STR00001##