Method of using 3-cyano-4-arylpyridine derivatives as modulators of androgen receptor function
First Claim
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1. A method for treating androgen receptor-associated conditions, which comprises administering to a mammalian patient in need of treatment a therapeutically effective amount of a compound having the structure
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Abstract
A method is provided for treating androgen receptor-associated conditions such as age-related diseases, for example sarcopenia, employing a compound of the structure
- R1 is CN or H; X is O or S;
- R2 is alkyl or substituted alkyl, cycloalkyl or substituted cycloalkyl, arylalkyl or substituted arylalkyl, aryl or substituted aryl, or heteroaryl or substituted heteroaryl;
- R3 and R4 are the same or different and are independently selected from H, C(O)R2a, alkyl or substituted alkyl, cycloalkyl or substituted cycloalkyl, arylalkyl or substituted arylalkyl, aryl or substituted aryl, or heteroaryl or substituted heteroaryl;
- R2a is alkyl or substituted alkyl, cycloalkyl or substituted cycloalkyl, arylalkyl or substituted arylalkyl, aryl or substituted aryl, or heteroaryl or substituted heteroaryl;
- G is aryl or heteroaryl, or aryl or heteroaryl substituted with one, two, three, four or five, where possible, of the substituents selected from the group consisting of hydrogen (H), halo, NO2, CN, OR2b, OH, CF3, NR3aR4a;
- wherein R3a and R4a, and R2b are the same or different and are independently selected from alkyl or substituted alkyl, cycloalkyl or substituted cycloalkyl, arylalkyl or substituted arylalkyl, aryl or substituted aryl, or heteroaryl and substituted heteroaryl; or a pharmaceutically acceptable salt thereof and a prodrug ester thereof.
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18 Claims
- 1. A method for treating androgen receptor-associated conditions, which comprises administering to a mammalian patient in need of treatment a therapeutically effective amount of a compound having the structure
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7. A method for preventing, inhibiting or treating the progression or onset of diseases or disorders associated with nuclear hormone receptors, wherein a therapeutically effective amount of a compound of formula I is administered to a mammalian patient in need of treatment.
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17. A method for the maintenance of muscle strength and function;
- reversal or prevention of frailty or age-related functional decline;
treatment of catabolic side effects of glucocorticoids;
prevention and/or treatment of reduced bone mass, density or growth;
osteoporosis and osteopenia;
treatment of chronic fatigue syndrome (CFS);
chronic myalgia;
treatment of acute fatigue syndrome and muscle loss following elective surgery;
accelerating of wound healing;
accelerating bone fracture repair;
accelerating healing of complicated fractures, distraction osteogenesis;
in joint replacement;
prevention of post-surgical adhesion formation;
accelerating tooth repair or growth;
maintenance of sensory function;
treatment of periodontal disease;
treatment of wasting secondary to fractures and wasting in connection with chronic obstructive pulmonary disease (COPD), chronic liver disease, AIDS, weightlessness, cancer cachexia, burn and trauma recovery, chronic catabolic state;
eating disorders;
treatment of cardiomyopathy;
treatment of thrombocytopenia;
treatment of growth retardation in connection with Crohn'"'"'s disease;
treatment of short bowel syndrome;
treatment of irritable bowel syndrome;
treatment of inflammatory bowel disease;
treatment of Crohn'"'"'s disease and ulcerative colits;
treatment of complications associated with transplantation;
treatment of physiological short stature including growth hormone deficient children and short stature associated with chronic illness;
treatment of obesity and growth retardation associated with obesity;
treatment of anorexia;
treatment of hypercortisolism and Cushing'"'"'s syndrome;
Paget'"'"'s disease;
treatment of osteoarthritis;
induction of pulsatile growth hormone release;
treatment of osteochondrodysplasias;
treatment of depression, nervousness, irritability and stress;
treatment of reduced mental energy and low self-esteem;
improvement of cognitive function, the treatment of dementia, Alzheimer'"'"'s disease and short term memory loss;
treatment of catabolism in connection with pulmonary dysfunction and ventilator dependency;
treatment of cardiac dysfunction associated with valvular disease, myocardial infarction, cardiac hypertrophy or congestive heart failure;
lowering blood pressure;
protection against ventricular dysfunction or prevention of reperfusion events;
treatment of adults in chronic dialysis;
reversal or slowing of the catabolic state of aging;
attenuation or reversal of protein catabolic responses following trauma, reversal of the catabolic state associated with surgery, congestive heart failure, cardiac myopathy, bums, cancer, COPD;
reducing cachexia and protein loss due to chronic illness such as cancer or AIDS;
treatment of hyperinsulinemia including nesidioblastosis;
treatment of immunosuppressed patients;
treatment of wasting in connection with multiple sclerosis or other neurodegenerative disorders;
promotion of myelin repair;
maintenance of skin thickness;
treatment of metabolic homeostasis and renal homeostasis;
stimulation of osteoblasts, bone remodeling and cartilage growth;
regulation of food intake;
treatment of insulin resistance, treatment of NIDDM, in mammals;
treatment of insulin resistance in the heart;
improvement of sleep quality and correction of the relative hyposomatotropism of senescence due to high increase in REM sleep and a decrease in REM latency;
treatment of hypothermia;
treatment of congestive heart failure;
treatment of lipodystrophy;
treatment of muscular atrophy;
treatment of musculoskeletal impairment;
improvement of the overall pulmonary function;
treatment of sleep disorders; and
the treatment of the catabolic state of prolonged critical illness;
treatment of hirsutism, acne, seborrhea, androgenic alopecia, anemia, hyperpilosity, benign prostate hypertrophy, adenomas and neoplasies of the prostate and malignant tumor cells containing the androgen receptor, as is the case for breast, brain, skin, ovarian, bladder, lymphatic, liver and kidney cancers;
cancers of the skin, pancreas, endometrium, lung and colon;
osteosarcoma;
hypercalcemia of malignancy;
metastatic bone disease;
treatment of spermatogenesis, endometriosis and polycystic ovary syndrome;
conteracting preeclampsia, eclampsia of pregnancy and preterm labor;
treatment of premenstrual syndrome;
treatment of vaginal dryness;
age related decreased testosterone levels in men, male menopause, hypogonadism, male hormone replacement, male and female sexual dysfunction, erectile dysfunction, decreased sex drive, sexual well-being, decreased libido, urinary incontinence, male and female contraception, hair loss, Reaven'"'"'s Syndrome and the enhancement of bone and muscle performance/strength, and “
Syndrome X”
or Metabolic Syndrome, which comprises treating a human patient in need of treatment with a therapeutic amount of a compound having the structure - View Dependent Claims (18)
- reversal or prevention of frailty or age-related functional decline;
Specification