C07D231/06

NOVEL ARYL-CYANOGUANIDINE COMPOUNDS

The present invention relates to protein-lysine N-methyltransferase SMYD2 (SET and MYND domain-containing protein 2) inhibitors, in particular SMYD2-inhibitory substituted cyanoguanidine-pyrazolines of general formula (I) wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, X and r have the meaning as described and defined herein, as well as to pharmaceutical compositions comprising compounds according to the invention and to their prophylactic and therapeutic use for hyper-proliferative disorders, in particular for cancer, respectively tumour disorders. The present invention furthermore relates to the use of SMYD2 inhibitors for benign hyperplasias, atherosclerotic disorders, sepsis, autoimmune disorders, vascular disorders, viral infections, neurodegenerative disorders, inflammatory disorders, atherosclerotic disorders and the control of male fertility.

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Modulators of GTPases and their use

The present invention relates to molecules which function as modulators (i.e., inhibitors and agonists) of the Ras-homologous (Rho) family of small GTPases (e.g. Rac, Cdc42 and Rho GTPases) and their use to treat diseases, including cancers (including solid tumors-medulloblastoma, ovarian, breast, head and neck, testicular, prostate among others and hematologic malignancies-B cell lymphoma, where these GTPases are overexpressed or hyperactivated), sporadic and genetic diseases where activation of Rho GTPases plays a pivotal role (Menkes disease, rheumatoid arthritis, atherosclerosis, diabetes (type I), Huntington's disease and Alzheimer's disease) which are mediated through these proteins. Compounds according to the present invention may also be used as a therapy for the treatment of Entamoeba spp. or Acanthamoeba spp. infections, especially including Entamoeba histolytica.

Modulators of GTPases and their use

The present invention relates to molecules which function as modulators (i.e., inhibitors and agonists) of the Ras-homologous (Rho) family of small GTPases (e.g. Rac, Cdc42 and Rho GTPases) and their use to treat diseases, including cancers (including solid tumors-medulloblastoma, ovarian, breast, head and neck, testicular, prostate among others and hematologic malignancies-B cell lymphoma, where these GTPases are overexpressed or hyperactivated), sporadic and genetic diseases where activation of Rho GTPases plays a pivotal role (Menkes disease, rheumatoid arthritis, atherosclerosis, diabetes (type I), Huntington's disease and Alzheimer's disease) which are mediated through these proteins. Compounds according to the present invention may also be used as a therapy for the treatment of Entamoeba spp. or Acanthamoeba spp. infections, especially including Entamoeba histolytica.

Solid Dispersions of Amorphous 3,4-Diphenyl-4,5-Dihydro-1H-Pyrazole Derivatives, Compositions Comprising them and Uses Thereof as Cannabinoid CB1 Receptor Inhibitors

Amorphous compounds of Formula I, solid dispersions of amorphous compounds of Formula I, pharmaceutical compositions comprising the same and their use in the treatment and prevention of diseases and disorders associated with cannabinoid CB.sub.1 receptor are described. The solid dispersions comprise a compound of Formula I dispersed in a solid matrix comprising a pharmaceutically acceptable polymer having a glass transition temperature of at lest 50° C.

Solid Dispersions of Amorphous 3,4-Diphenyl-4,5-Dihydro-1H-Pyrazole Derivatives, Compositions Comprising them and Uses Thereof as Cannabinoid CB1 Receptor Inhibitors

Amorphous compounds of Formula I, solid dispersions of amorphous compounds of Formula I, pharmaceutical compositions comprising the same and their use in the treatment and prevention of diseases and disorders associated with cannabinoid CB.sub.1 receptor are described. The solid dispersions comprise a compound of Formula I dispersed in a solid matrix comprising a pharmaceutically acceptable polymer having a glass transition temperature of at lest 50° C.

ETHOXY/PROPOXY MODIFIED PYRAZOLINE ORGANIC MATTER, APPLICATION THEREOF, PHOTOCURABLE COMPOSITION, AND PHOTORESIST
20230167066 · 2023-06-01 ·

An ethoxy/propoxy modified pyrazoline organic matter, an application thereof, a photocurable composition, and a photoresist. The introduction of —CH.sub.2—CH.sub.2—O(EO) and/or —CH(CH.sub.3)—CH.sub.2—O(PO) enables an EO/PO modified pyrazoline organic matter to have excellent compatibility with other components in a photocuring system, and the organic matter is solid, and is easy to add and use. In addition, the ethoxy/propoxy modified pyrazoline organic matter has an absorption band of 360-400 nm, and is thus particularly suitable for use as a sensitizer in the photocuring system (such as a system containing a bisimidazole photoinitiator), thereby greatly improving the sensitivity of the photocuring system. On this basis, the EO/PO modified pyrazoline organic matter has high sensitivity enhancement, features low usage, is solid, and is easy to add and use.

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ETHOXY/PROPOXY MODIFIED PYRAZOLINE ORGANIC MATTER, APPLICATION THEREOF, PHOTOCURABLE COMPOSITION, AND PHOTORESIST
20230167066 · 2023-06-01 ·

An ethoxy/propoxy modified pyrazoline organic matter, an application thereof, a photocurable composition, and a photoresist. The introduction of —CH.sub.2—CH.sub.2—O(EO) and/or —CH(CH.sub.3)—CH.sub.2—O(PO) enables an EO/PO modified pyrazoline organic matter to have excellent compatibility with other components in a photocuring system, and the organic matter is solid, and is easy to add and use. In addition, the ethoxy/propoxy modified pyrazoline organic matter has an absorption band of 360-400 nm, and is thus particularly suitable for use as a sensitizer in the photocuring system (such as a system containing a bisimidazole photoinitiator), thereby greatly improving the sensitivity of the photocuring system. On this basis, the EO/PO modified pyrazoline organic matter has high sensitivity enhancement, features low usage, is solid, and is easy to add and use.

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HETEROCYCLIC COMPOUNDS AS PESTICIDES

The present application relates to the use of heterocyclic compounds for controlling animal pests including arthropods, insects and nematodes, to novel heterocyclic compounds, to processes for their preparation and to intermediates for preparing the heterocyclic compounds.

HETEROCYCLIC COMPOUNDS AS PESTICIDES

The present application relates to the use of heterocyclic compounds for controlling animal pests including arthropods, insects and nematodes, to novel heterocyclic compounds, to processes for their preparation and to intermediates for preparing the heterocyclic compounds.

Organic Scintillators Derived from Pyrazoline

Pyrazoline-based fluorophores and plastic scintillators incorporating the fluorophores are described. The fluorophores include 1,3,5-triaryl substituted pyrazolines. A fluorophore of a plastic scintillator can be a 1-phenyl-4,5-1H-dihydroyrazole having the structure:

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in which R.sub.1 and R.sub.2 are independently selected from a heteroaryl group including one or more of an oxygen, selenium or sulfur atom in the ring; an aryl halide group; or a phenyl alkyl including a C1 to C18 saturated or unsaturated alkyl that optionally includes a reactive functionality.