Patent classifications
A61K31/4166
Screening method for laminin 511 production promoting agent, basal epidermal layer stabilizing agent, and/or epidermal stem cells reduction inhibiting or proliferation promoting agent
Provided is a screening method for a laminin 511 expression promoter, which takes the expression of laminin 511 as an indicator. Also provided is an agent for improving skin barrier function, elasticity, hydration and inflammation. This agent includes at least one extract selected from among a group consisting of brown algae, red algae and green algae.
SUBSTITUTED HYDANTOINAMIDES AS ADAMTS7 ANTAGONISTS
The application relates to substituted hydantoinamides of formula (I) as ADAMTS7 antagonists, to processes for their preparation, their use alone or in combination for the treatment or prophylaxis of diseases, in particular of cardiovascular diseases, including atherosclerosis, coronary artery disease (CAD), peripheral vascular disease (PAD), arterial occlusive disease or restenosis after angioplasty. R.sup.1 is hydrogen, alkyl, cycloalkyl, heterocycloalkyl, heteroaryl or phenyl; R.sup.2 is hydrogen, cyano, halogen, alkylsulfonyl, alkyl, cycloalkyl or alkoxy; R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7 and R.sup.8 are independently hydrogen, halogen, alkyl or alkoxy; most groups being optionally substituted; with the proviso that at least one of R.sup.2, R.sup.3, R.sup.4 is H; X.sup.1, X.sup.2, X.sup.3, X.sup.4, X.sup.5 and X.sup.6 are independently N or C; with the proviso that in each ring maximal one X is N.
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SUBSTITUTED HYDANTOINAMIDES AS ADAMTS7 ANTAGONISTS
The application relates to substituted hydantoinamides of formula (I) as ADAMTS7 antagonists, to processes for their preparation, their use alone or in combination for the treatment or prophylaxis of diseases, in particular of cardiovascular diseases, including atherosclerosis, coronary artery disease (CAD), peripheral vascular disease (PAD), arterial occlusive disease or restenosis after angioplasty. R.sup.1 is hydrogen, alkyl, cycloalkyl, heterocycloalkyl, heteroaryl or phenyl; R.sup.2 is hydrogen, cyano, halogen, alkylsulfonyl, alkyl, cycloalkyl or alkoxy; R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7 and R.sup.8 are independently hydrogen, halogen, alkyl or alkoxy; most groups being optionally substituted; with the proviso that at least one of R.sup.2, R.sup.3, R.sup.4 is H; X.sup.1, X.sup.2, X.sup.3, X.sup.4, X.sup.5 and X.sup.6 are independently N or C; with the proviso that in each ring maximal one X is N.
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Artemisinin Derivatives
The present invention generally relates to artemisinin/dihydroartemisinin (DHA) derivatives, and their use for therapy, in particular cancer therapy. These tumor-homing artemisinin derivatives (THAD) comprise three moieties: an artemisinin/DHA or a derivative thereof, a heptamethine carbocyanine dye (HMCD) residue, and a linker that conjugates the HMCD dye residue to the artemisinin residue. The THAD include compounds wherein the linker is linked to one or two DHA residue(s) via one or more ether bonds, and wherein the linker is linked to two DHA residues via two bonds independently selected from ester, carbamate and thiocarbamate. The THAD of the invention provide improved growth inhibition of cancer cells. The present invention also relates to improved methods of cancer therapy wherein a THAD is administered to a cancer patient. In embodiments, one or more THAD may be co-administered in a coordinated administration schedule. Advantages of the THAD and their use include, among others, improved dose-response and/or efficacy. The invention also relates to new dyes, their drug conjugates, and processes of making them.
Use of cannabinoids in the treatment of epilepsy
The present disclosure relates to the use of cannabidiol (CBD) for the reduction of total convulsive seizure frequency in the treatment of “treatment-resistant epilepsy” (TRE). In particular, the disclosure relates to the use of CBD of treating TRE when the TRE is Dravet syndrome; myoclonic absence seizures or febrile infection related epilepsy syndrome (FIRES). The disclosure further relates to the use of CBD in combination with one or more anti-epileptic drugs (AEDs).
Use of cannabinoids in the treatment of epilepsy
The present disclosure relates to the use of cannabidiol (CBD) for the reduction of total convulsive seizure frequency in the treatment of “treatment-resistant epilepsy” (TRE). In particular, the disclosure relates to the use of CBD of treating TRE when the TRE is Dravet syndrome; myoclonic absence seizures or febrile infection related epilepsy syndrome (FIRES). The disclosure further relates to the use of CBD in combination with one or more anti-epileptic drugs (AEDs).
Use of cannabinoids in the treatment of epilepsy
The present disclosure relates to the use of cannabidiol (CBD) for the reduction of total convulsive seizure frequency in the treatment of “treatment-resistant epilepsy” (TRE). In particular, the disclosure relates to the use of CBD of treating TRE when the TRE is Dravet syndrome; myoclonic absence seizures or febrile infection related epilepsy syndrome (FIRES). The disclosure further relates to the use of CBD in combination with one or more anti-epileptic drugs (AEDs).
METHODS OF TREATING CASTRATION-RESISTANT PROSTATE CANCER WITH GLUCOCORTICOID RECEPTOR ANTAGONISTS AND ANTI-ANDROGEN RECEPTOR THERAPY AND ANTI-ANDROGEN RECEPTOR THERAPY
Embodiments of the invention are directed to the treatment of subjects with prostate cancer, in particular those with castration resistant prostate cancer, with glucocorticoid receptor antagonists. The prostate cancer may be one that has become resistant to androgen deprivation therapy, for example, by increase in glucocorticoid receptor expression and/or activity.
METHODS OF TREATING CASTRATION-RESISTANT PROSTATE CANCER WITH GLUCOCORTICOID RECEPTOR ANTAGONISTS AND ANTI-ANDROGEN RECEPTOR THERAPY AND ANTI-ANDROGEN RECEPTOR THERAPY
Embodiments of the invention are directed to the treatment of subjects with prostate cancer, in particular those with castration resistant prostate cancer, with glucocorticoid receptor antagonists. The prostate cancer may be one that has become resistant to androgen deprivation therapy, for example, by increase in glucocorticoid receptor expression and/or activity.
METHODS OF TREATING CASTRATION-RESISTANT PROSTATE CANCER WITH GLUCOCORTICOID RECEPTOR ANTAGONISTS AND ANTI-ANDROGEN RECEPTOR THERAPY AND ANTI-ANDROGEN RECEPTOR THERAPY
Embodiments of the invention are directed to the treatment of subjects with prostate cancer, in particular those with castration resistant prostate cancer, with glucocorticoid receptor antagonists. The prostate cancer may be one that has become resistant to androgen deprivation therapy, for example, by increase in glucocorticoid receptor expression and/or activity.