Patent classifications
A61P5/32
Selective estrogen receptor degraders and uses thereof
The present disclosure provides compounds of Formula (I) and Formula (II). The compounds described herein may be useful in treating proliferative diseases (e.g., cancer). Also provided in the present disclosure are pharmaceutical compositions, kits, methods, and uses including or using a compound described herein. ##STR00001##
Selective estrogen receptor degraders and uses thereof
The present disclosure provides compounds of Formula (I) and Formula (II). The compounds described herein may be useful in treating proliferative diseases (e.g., cancer). Also provided in the present disclosure are pharmaceutical compositions, kits, methods, and uses including or using a compound described herein. ##STR00001##
Method for manufacturing a drug delivery device and a drug delivery device manufactured according to the method
The invention relates to a method for producing a drug delivery device, which has a body comprising a siloxane-based elastomer and at least one active agent. The method comprises applying adhesive material, which comprises non-cured siloxane based elastomer, into a contact with the body and curing the said adhesive material by subjecting it to radiation energy from a laser source. The invention relates also to a drug delivery device manufactured according to the method.
ACRYLIC ACID ANALOGS
Compounds of Formula (I) are provided herein. Such compounds, as well as pharmaceutically acceptable salts and compositions thereof, are useful for treating diseases or conditions, including conditions characterized by excessive cellular proliferation, such as breast cancer.
PHARMACEUTICAL COMPOSITIONS
Novel methods for treating or reducing the likelihood of acquiring symptoms or diseases due to the menopause, in postmenopausal women, particularly osteoporosis, vaginal atrophy and dryness, hypogonadism, diminished libido, skin atrophy, connective tissue disease, urinary incontinence, breast, endometrial, ovarian and uterine cancers, hot flashes, loss of muscle mass, insulin resistance, fatigue, loss of energy, aging, physical symptoms of menopause, in susceptible warm-blooded animals including humans involving administration of a sex steroid precursor are disclosed. Said method comprising novel ways of administering and dosing dehydroepiandrosterone (DHEA) in order to take advantage of positive androgenic effects in the vaginal layers lamina propia and/or the layer muscularis, without undesirably causing systemic estrogenic effects in order to avoid the risk of breast and uterine cancer. Pharmaceutical compositions for delivery of active ingredient(s) useful to the invention are also disclosed.
A COMPOSITION FOR TREATING ONE OR MORE ESTROGEN RELATED DISEASES
The present invention relates to treating one or more estrogen related diseases while preventing or reducing the likelihood of developing estrogen deficiency related side effects, wherein said composition comprises administering a therapeutically effective amount of a Gn RH antagonist to a patient in need of said treatment, and wherein said amount of Gn RH antagonist is sufficient for providing a mean endogenous serum estradiol level of between about 20 pg/ml and 60 pg/ml, preferably between 30 pg/ml and 50 pg/m, in said patient in a treatment period of at least four weeks, without relying on add-back therapy. Said composition and method is simple, effective and will accordingly both increase patient acceptance and compliance of therapy.
A COMPOSITION FOR TREATING ONE OR MORE ESTROGEN RELATED DISEASES
The present invention relates to treating one or more estrogen related diseases while preventing or reducing the likelihood of developing estrogen deficiency related side effects, wherein said composition comprises administering a therapeutically effective amount of a Gn RH antagonist to a patient in need of said treatment, and wherein said amount of Gn RH antagonist is sufficient for providing a mean endogenous serum estradiol level of between about 20 pg/ml and 60 pg/ml, preferably between 30 pg/ml and 50 pg/m, in said patient in a treatment period of at least four weeks, without relying on add-back therapy. Said composition and method is simple, effective and will accordingly both increase patient acceptance and compliance of therapy.
COMBINATION THERAPY FOR THE TREATMENT OF CANCER
The present disclosure relates to a pharmaceutical combination comprising (1) a first agent which is a CDK inhibitor or a pharmaceutically acceptable salt thereof and (2) a second agent which is an anti-hormonal agent or a pharmaceutically acceptable salt thereof. The present disclosure also relates to a pharmaceutical combination comprising (1) a first agent which is a CDK inhibitor or a pharmaceutically acceptable salt thereof, (2) a second agent which is an anti-hormonal agent or a pharmaceutically acceptable salt thereof, and (3) a third agent which is an agent that regulates the PI3K/Akt/mTOR pathway or a pharmaceutically acceptable salt thereof.
NOVEL SUBSTITUTED N-(3-FLUOROPROPYL)-PYRROLIDINE COMPOUNDS, PROCESSES FOR THEIR PREPARATION AND THERAPEUTIC USES THEREOF
The present disclosure relates to novel substituted N-(3-fluoropropyl)-pyrrolidine compounds of formula (I-A), wherein R1 and R2 represent independently a hydrogen atom or a deuterium atom; A represents an oxygen or nitrogen atom; and SERM-F represents a selective estrogen receptor modulator fragment comprising an aryl or heteroaryl group linked to the adjacent A group. The disclosure also relates to the preparation and to the therapeutic uses of the compounds of formula (I-A) as inhibitors and degraders of estrogen receptors.
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METHOD FOR MANUFACTURING PREPARATION FOR INJECTION
A method for manufacturing a preparation for injection, including a first step of performing at least one treatment selected from the group consisting of a treatment of mixing benzyl benzoate with an antioxidant, a treatment of heating benzyl benzoate, and a treatment of purifying benzyl benzoate and a second step of mixing the benzyl benzoate treated by the first step with fulvestrant.