Patent classifications
C07J5/00
Sterile pharmaceutical compositions
The present invention provides a method for the sterilization of a labile glucocorticosteroid, which method comprises heat-treating by moist heat the labile glucocorticosteroid in the form of a suspension for a sterilizing-effective time. The methods and compositions according to the invention are useful as therapeutic tools to prevent, reverse, and/or reduce the symptoms of allergic and/or inflammatory conditions in a mammalian patient. The invention also provides methods and compositions, which may be manipulated and fine-tuned to fit the condition(s) to be treated while producing fewer side effects.
Chemical compounds and use thereof for improving muscular quality
Chemical compounds and the therapeutic use thereof, in particular for improving muscular quality in mammals. More particularly, a method of improving muscular quality in sarcopenic mammals and treating and/or preventing sarcopenia using the chemical compounds and, in particular, sarcopenic obesity and the associated complications and/or pathologies thereof, such as loss of strength, muscle mass, performance and of physical and movement capacity. Also, a method of improving muscle quality in obese mammals and treating and/or preventing of obesity and associated complications and/or pathologies, advantageously type 2 diabetes and metabolic syndrome, using the chemical compounds.
NEUROACTIVE STEROIDS, COMPOSITIONS, AND USES THEREOF
Described herein are steroids of Formula (I):
##STR00001##
and pharmaceutically acceptable salts thereof; wherein R.sup.1, R.sup.2a, R.sup.2b, R.sup.3, R.sup.4, R.sup.5a, R.sup.5b, R.sup.6, and Z are as defined herein. Such compounds are contemplated useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, schizophrenia spectrum disorders, convulsive disorders, disorders of memory and/or cognition, movement disorders, personality disorders, autism spectrum disorders, pain, traumatic brain injury, vascular diseases, substance abuse disorders and/or withdrawal syndromes, and tinnitus.
NON-HORMONAL STEROID MODULATORS OF NF-kB FOR TREATMENT OF DISEASE
Provided herein is a pharmaceutical composition comprising a compound having the structural formula
##STR00001##
wherein the compound is present in an amount effective to treat or reduce the symptoms of muscular dystrophy. The therapeutically effective amount may be between 10 mg to 200 mg, or may be between 0.01 mg/kg to 10.0 mg/kg. Also provided are methods of treating or reducing the symptoms of muscular dystrophy, comprising the administration, to a patient in need thereof, of a therapeutically effective of the above compound.
LYMPH DIRECTING PRODRUGS
The present invention relates to compounds and their uses, in particular, compounds in the form of prodrugs that promote transport of a pharmaceutical agent to the lymphatic system and subsequently enhance release of the parent drug.
Neuroactive steroids, compositions, and uses thereof
Described herein are steroids of Formula (I): and pharmaceutically acceptable salts thereof; wherein R.sup.1, R.sup.2a, R.sup.2b, R.sup.3, R.sup.4, R.sup.5a, R.sup.5b, R.sup.6, and Z are as defined herein. Such compounds are contemplated useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, schizophrenia spectrum disorders, convulsive disorders, disorders of memory and/or cognition, movement disorders, personality disorders, autism spectrum disorders, pain, traumatic brain injury, vascular diseases, substance abuse disorders and/or withdrawal syndromes, and tinnitus. ##STR00001##
17A-MONOESTERS AND 17A,21-DIESTERS OF CORTEXOLONE FOR USE IN THE TREATMENT OF TUMORS
The present invention relates to certain cortexolone derivatives of formula (I)
##STR00001##
and the use of the same as antitumor active ingredients for the curative or adjuvant, or neoadjuvant or palliative treatment of precancerous lesions, dysplasias, metaplasias and tumor diseases, including malignant neoplasias and metastasis. The present invention also relates to pharmaceutical compositions comprising cortexolone derivatives of formula (I) as active ingredients and at least one physiologically acceptable excipient, and to the use of the pharmaceutical compositions as antitumor medicinal products.
ENZYMATIC PROCESS FOR OBTAINING 17 ALPHA-MONOESTERS OF CORTEXOLONE AND/OR ITS 9,11-DEHYDRODERIVATIVES
The present invention refers to a new enzymatic process for obtaining 17?-monoesters of cortexolone and/or its 9,11-dehydroderivatives starting from the corresponding 17?,21-diesters which comprises an enzymatic alcoholysis reaction. Furthermore, the present invention refers to new crystalline forms of cortexolone-17?-propionate and 9,11-dehydro-cortexolone 17?-butanoate.
Process for preparation of glucocorticoid steroids
The present invention discloses a process for the preparation of 16, 17-acetals of pregnane derivatives having formula I ##STR00001##
wherein each substituent is independently selected from; R.sub.1 is H or CH.sub.3; R.sub.2 is C.sub.1-C.sub.6 linear or branched alkyl, alkynyl group or cycloalkyl group; aryl or heteroaryl group; or R.sub.1 and R.sub.2 combine to form saturated, unsaturated C.sub.3-C.sub.6 cyclic or heterocyclic ring; R.sub.3 and R.sub.4 are same or different and each independently represents H or halogen; R.sub.5 is OH or OCOR wherein R represents H or C.sub.1-C.sub.6 linear, branched or cyclic alkyl group that may be substituted.
Cortexolone 17alpha-benzoate for use in the treatment of tumours
The present invention provides certain cortexolone derivatives of formula (I), and the same for use as antitumor active ingredients for the curative or adjuvant, or neoadjuvant or palliative treatment of precancerous lesions, dysplasias, metaplasias and tumor diseases, including malignant neoplasias and metastasis. Another aspect of the invention relates to pharmaceutical compositions comprising cortexolone derivatives of formula (I) as active ingredients and at least one physiologically acceptable excipient, and to the use of said pharmaceutical compositions as antitumor medicinal products.