- PROCESS AND INTERMEDIATES FOR PREPARING ARZOXIFENE
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The present invention provides for novel compounds of formula I wherein X is S or S(O); R1 and R2 are each independently selected from the group consisting of -CH2CH3 and phenyl; or R1 and R2/su
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Page/Page column 11-12
(2008/12/07)
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- Benzothiophene selective estrogen receptor modulators with modulated oxidative activity and receptor affinity
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The regulation of estrogenic and antiestrogenic effects of selective estrogen receptor modulators (SERMs) is thought to underlie their clinical use. Most SERMs are polyaromatic phenols susceptible to oxidative metabolism to quinoids, which are proposed to
- Qin, Zhihui,Kastrati, Irida,Chandrasena, R. Esala P.,Liu, Hong,Yao, Ping,Petukhov, Pavel A.,Bolton, Judy L.,Thatcher, Gregory R. J.
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p. 2682 - 2692
(2008/02/07)
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- Crystalline form of 6-hydroxy-3-(4-[2-(piperidin-1-yl)ethoxy]phenoxy)-2-(4-methoxyphenyl)benzo[b] thiophene hydrochloride
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The present invention is directed to a novel crystalline hydrate of 6-hydroxy-3-(4-[2-(piperidin-1-yl)ethoxy]phenoxy)-2-(4-methoxyphenyl)benzo[b]thiophene hydrochloride and uses for same, including inhibition of disease states associated with estrogen dep
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Page/Page column 7-8
(2008/06/13)
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- Treatment of skeletal disorders
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This invention relates to methods for treating bone loss in a mammal by administering to the mammal a therapeutically effective amount of leptin or a leptin mimetic. This invention also relates to methods for treating bone fracture, enhancing bone healing following facial reconstruction, maxillary reconstruction or madibular reconstruction, enhancing long bone extension, enhancing the healing rate of a bone graft, enhancing prosthetic growth and inducing vertebral synostosis by administering a therapeutically effective amount of leptin or a leptin mimetic. This invention further relates to methods and compositions comprising leptin or a leptin mimetic and estrogen, a selective estrogen receptor modulator or a bisphonate for treating the above-recited diseases and conditions.
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- Treatment of central nervous system disorders with selective estrogen receptor modulators
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The present invention provides a method of treating depression, mood swings, or Alzheimer's disease in a patient in need of such treatment by administering a selective estrogen receptor modulating compound of the formula in which R1 and R2 are independently hydroxy and alkoxy of one to four carbon atoms; and R3 and R4 are independently methyl or ethyl, or R3 and R4, taken together with the nitrogen atom to which they are attached, form a pyrrolidino, methyl-pyrrolidino, dimethylpyrrolidino, piperidino, morpholino, or hexamethyleneimino ring.
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- Osteoporosis compounds
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This invention relates to prostaglandin agonists, methods of using such prostaglandin agonists, pharmaceutical compositions containing such prostaglandin agonists and kits containing such prostaglandin agonists. The prostaglandin agonists are useful for the treatment of bone disorders including osteoporosis.
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- Benzothiophene compounds, intermediates, compositions, and methods
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The present invention provides intermediate compounds and processes for the preparation of compounds of formula I STR1 wherein R1a is --H or --OR7a in which R7a is --H or a hydroxy protecting group; R2a is --H, halo, or --OR8a in which R8a is --H or a hydroxy protecting group; R3 is 1-piperidinyl, 1-pyrrolidino, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidino, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino; n is 2 or 3; and Z is --O-- or --S--; or a pharmaceutically acceptable salt thereof.
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- Method of treating estrogen dependent cancers
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A method for alleviating the symptoms of post-menopausal syndrome comprising administering to a woman in need thereof an effective amount of a compound of formula I STR1 wherein R1a is --H or --OR7a in which R7a is --H or a hydroxy protecting group; R2a is --H, halo, or --OR8a in which R8a is --H or a hydroxy protecting group; R3 is 1-piperidinyl, 1-pyrrolidino, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidino, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino; n is 2 or 3; and Z is --O-- or --S--; or a pharmaceutically acceptable salt thereof.
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- Benzothiophene compounds, intermediates, compositions, and methods
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The present invention provides a method for inhibiting endometriosis comprising administering to a woman an effective amount of a compound of formula I STR1 wherein R1a is --H or --OR7a in which R7a is --H or a hydroxy protecting group; R2a is --H, halo, or --OR8a in which R8a is --H or a hydroxy protecting group; R3 is 1-piperidinyl, 1-pyrrolidino, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidino, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino; n is 2 or 3; and Z is --O-- or --S--; or a pharmaceutically acceptable salt thereof.
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- Benzothiophene compounds, intermediates, compositions, and methods
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A method for alleviating the symptoms of post-menopausal syndrome comprising administering to a woman in need thereof an effective amount of a compound of formula I wherein R1a is --H or --OR7a in which R7a is --H or a hydroxy protecting group; R2a is --H, halo, or --OR8a in which R8a is --H or a hydroxy protecting group; R3 is 1-piperidinyl, 1-pyrrolidino, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidino, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino; n is 2 or 3; and Z is --O-- or --S--; or a pharmaceutically acceptable salt thereof, and further comprising administering to said woman an effective amount of progestin.
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- Benzothiophene compounds, intermediates, compositions, and methods
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A method for alleviating the symptoms of post-menopausal syndrome comprising administering to a woman in need thereof an effective amount of a compound of formula I wherein R1a is -H or -OR7a in which R7a is -H or a hydroxy protecting group; R2a is -H, halo, or -OR8a in which R8a is -H or a hydroxy protecting group; R3 is 1-piperidinyl, 1-pyrrolidino, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidino, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino; n is 2 or 3; and Z is -O-or -S-; or a pharmaceutically acceptable salt thereof, and further comprising administering to said woman an effective amount of estrogen.
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- Treatment of skeletal disorders
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This invention relates to methods for treating bone loss in a mammal by administering to the mammal a therapeutically effective amount of leptin or a leptin mimetic. This invention also relates to methods for treating bone fracture, enhancing bone healing following facial reconstruction, maxillary reconstruction or madibular reconstruction, enhancing long bone extension, enhancing the healing rate of a bone graft, enhancing prosthetic growth and inducing vertebral synostosis by administering a therapeutically effective amount of leptin or a leptin mimetic. This invention further relates to methods and compositions comprising leptin or a leptin mimetic and estrogen, a selective estrogen receptor modulator or a bisphonate for treating the above-recited diseases and conditions.
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- Benzothiophene compounds, intermediates, compositions, and methods
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The present invention provides pharmaceutically active compounds of formula I STR1 wherein R1 is --H, --OH, --O(C1 -C4 alkyl), --OCOC6 H5, --OCO(C1 -C6 alkyl), or --OSO2/su
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