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1. 发明申请

WO2008030524A3 LIQUID PHARMACEUTICAL FORMULATIONS FOR ORAL ADMINISTRATION OF A CGRP ANTAGONIST 审中-公开
标题翻译：口服给予CGRP拮抗剂的液体药物制剂
公开(公告)号：WO2008030524A3
公开(公告)日：2008-10-02
申请号：PCT/US2007019461
申请日：2007-09-06
申请人： MERCK & CO INC , BRESLIN DAVID , STELLABOTT JOYCE , JAHANSOUZ HOSSAIN , ALANI LAMAN L , THOMPSON KAREN
发明人： BRESLIN DAVID , STELLABOTT JOYCE , JAHANSOUZ HOSSAIN , ALANI LAMAN L , THOMPSON KAREN
IPC分类号： A01N43/00 , A61K9/48 , A61K9/66 , A61K31/55
CPC分类号： A61K31/55 , A61K9/4858 , A61K9/4866
摘要： Liquid formulations comprising the compound 1-[1-({[(3R,6S)-6-(2,3-difluorophenyl)-2-oxo-1-(2,2,2-trifluoroethyl)azepan-3-yl]amino}carbonyl)piperidin-4-yl]-2-oxo-1,2-dihydroimidazo[4,5-b]pyridin-3-ide have surprisingly improved bioavailability and stability in comprising polyethylene glycol, Tween (polysorbate 80), Cremophor® EL (polyoxyl 35 castor oil), propylene glycol, and optionally water, and may be filled into soft or hard gelatin capsules useful for treating conditions including migraine headache and cluster headache.
摘要翻译：包含化合物1- [1 - （{[（3R，6S）-6-（2,3-二氟苯基）-2-氧代-1-（2,2,2-三氟乙基）氮杂环庚烷-3-基] 氨基}羰基）哌啶-4-基] -2-氧代-1,2-二氢咪唑并[4,5-b]吡啶-3-基令人惊讶地改善了包含聚乙二醇，吐温（聚山梨醇酯80），Cremophor EL（聚氧乙烯35蓖麻油），丙二醇和任选的水，并且可以填充到用于治疗包括偏头痛和丛集性头痛的病症的软或硬明胶胶囊中。

2. 发明专利

PE20071091A1 POLIMORFOS DE N-(3H-IMIDAZOL[4,5-B]PIRIDIN-2-ILMETIL)-2-FLUORO-4-METIL-3-OXO-4-AZA-5-ALFA-ANDROST-1-EN-17-BETA-CARBOXAMIDA 未知
公开(公告)号：PE20071091A1
公开(公告)日：2007-11-19
申请号：PE2006001552
申请日：2006-12-05
申请人： MERCK & CO INC
发明人： TAN LUSHI , MEISSNER ROBERT S , LI WENJIE , PERKINS JAMES J , COTE AARON S , STELLABOTT JOYCE , YUAN-HON KIANG
IPC分类号： A61K31/58 , A61P5/26 , C07J73/00
摘要： SE REFIERE A FORMAS CRISTALINAS DEL COMPUESTO N-(3H-IMIDAZOL[4,5-B]PIRIDIN-2-ILMETIL)-2-FLUORO-4-METIL-3-OXO-4-AZA-5-ALFA-ANDROST-1-EN-17-BETA-CARBOXAMIDA; TALES COMO LA FORMA A ANHIDRA CRISTALINA CARACTERIZADO POR PRESENTAR UN PATRON DE DIFRACCION DE POLVO DE RAYOS X CON PICOS DE DIFRACCION EN VALORES 2 TETHA DE 5,6; 7,6 Y 9,6 ±0,1; UN ESPECTRO DE RMN CPMAS DE CARBONO-13 CON VALORES DE DESPLAZAMIENTO QUIMICOS DE APROXIMADAMENTE 39,7; 118,3; 169,2; 12,6 +/- 0,1 p.p.m.; UN PUNTO DE FUSION DE 281,2ºC; ASI TAMBIEN SON IDENTIFICADAS LA FORMAS: B HIGROSCOPICA CRISTALINA; C CRISTALINA HIDRATO; D ANHIDRA CRISTALINA; E CRISTALINA TETRAHIDRATO; F CRISTALINA SESQUIHIDRATO; G CRISTALINA ETANOLATO DE DICHO COMPUESTO. TAMBIEN SE REFIERE A UN PROCEDIMIENTO DE PREPARACION DE DICHOS CRISTALES Y UNA COMPOSICION FARMACEUTICA. EL COMPUESTO ES UN MODULADOR DE RECEPTOR DE ANDROGENO SELECTIVO DE (SARM) POR LO QUE ES UTILES EN EL TRATAMIENTO POR DEFICIENCIA DE ANDROGENOS COMO OSTEOPOROSIS, POTENCIACION DEL TONO MUSCULAR DEBILITADO

3. 发明专利

PE10912007A1 POLIMORFOS DE N-(3H-IMIDAZOL[4,5-B]PIRIDIN-2-ILMETIL)-2-FLUORO-4-METIL-3-OXO-4-AZA-5-ALFA-ANDROST-1-EN-17-BETA-CARBOXAMIDA 未知
公开(公告)号：PE10912007A1
公开(公告)日：2007-11-19
申请号：PE0015522006
申请日：2006-12-05
申请人： MERCK & CO INC
发明人： TAN LUSHI , MEISSNER ROBERT S , LI WENJIE , PERKINS JAMES J , COTE AARON S , STELLABOTT JOYCE , YUAN-HON KIANG
IPC分类号： A61K31/58 , A61P5/26 , C07J73/00
CPC分类号： C07J73/005 , C07D471/04
摘要： SE REFIERE A FORMAS CRISTALINAS DEL COMPUESTO N-(3H-IMIDAZOL[4,5-B]PIRIDIN-2-ILMETIL)-2-FLUORO-4-METIL-3-OXO-4-AZA-5-ALFA-ANDROST-1-EN-17-BETA-CARBOXAMIDA; TALES COMO LA FORMA A ANHIDRA CRISTALINA CARACTERIZADO POR PRESENTAR UN PATRON DE DIFRACCION DE POLVO DE RAYOS X CON PICOS DE DIFRACCION EN VALORES 2 TETHA DE 5,6; 7,6 Y 9,6 ±0,1; UN ESPECTRO DE RMN CPMAS DE CARBONO-13 CON VALORES DE DESPLAZAMIENTO QUIMICOS DE APROXIMADAMENTE 39,7; 118,3; 169,2; 12,6 +/- 0,1 p.p.m.; UN PUNTO DE FUSION DE 281,2ºC; ASI TAMBIEN SON IDENTIFICADAS LA FORMAS: B HIGROSCOPICA CRISTALINA; C CRISTALINA HIDRATO; D ANHIDRA CRISTALINA; E CRISTALINA TETRAHIDRATO; F CRISTALINA SESQUIHIDRATO; G CRISTALINA ETANOLATO DE DICHO COMPUESTO. TAMBIEN SE REFIERE A UN PROCEDIMIENTO DE PREPARACION DE DICHOS CRISTALES Y UNA COMPOSICION FARMACEUTICA. EL COMPUESTO ES UN MODULADOR DE RECEPTOR DE ANDROGENO SELECTIVO DE (SARM) POR LO QUE ES UTILES EN EL TRATAMIENTO POR DEFICIENCIA DE ANDROGENOS COMO OSTEOPOROSIS, POTENCIACION DEL TONO MUSCULAR DEBILITADO

4. 发明专利

AU2006322046A1 Polymorphs of androgen receptor modulator - (N-3H-imidazo [4 , 5-B] pyridin-2-yl-methyl) -2-fluoro-4-methyl-3-oxo-4-aza-androst- l-en-17 . beta . -carboxamide 未知
公开(公告)号：AU2006322046A1
公开(公告)日：2007-06-14
申请号：AU2006322046
申请日：2006-12-04
申请人： MERCK & CO INC
发明人： MEISSNER ROBERT S , COTE AARON S , PERKINS JAMES J , TAN LUSHI , KIANG YUAN-HON , LI WENJIE , STELLABOTT JOYCE
IPC分类号： C07J73/00 , A61K31/58 , A61P5/26
摘要： Compounds of structural formula I are modulators of the androgen receptor (AR) in a tissue selective manner. These compounds are useful in the enhancement of weakened muscle tone and the treatment of conditions caused by androgen deficiency or which can be ameliorated by androgen administration, including osteoporosis, osteopenia, glucocorticoid-induced osteoporosis, periodontal disease, bone fracture, bone damage following bone reconstructive surgery, sarcopenia, frailty, aging skin, male hypogonadism, postmenopausal symptoms in women, atherosclerosis, hypercholesterolemia, hyperlipidemia, obesity, aplastic anemia and other hematopoietic disorders, inflammatory arthritis and joint repair, HIV-wasting, prostate cancer, benign prostatic hyperplasia (BPH), abdominal adiposity, metabolic syndrome, type II diabetes, cancer cachexia, Alzheimer's disease, muscular dystrophies, cognitive decline, sexual dysfunction, sleep apnea, depression, premature ovarian failure, and autoimmune disease, alone or in combination with other active agents.

5. 发明专利

NO20083046L 未知
公开(公告)号：NO20083046L
公开(公告)日：2008-09-05
申请号：NO20083046
申请日：2008-07-04
申请人： MERCK & CO INC
发明人： MEISSNER ROBERT S , PERKINS JAMES J , COTE AARON S , TAN LUSHI , LI WENJIE , STELLABOTT JOYCE
IPC分类号： C07J3/00
摘要： Compounds of structural formula I are modulators of the androgen receptor (AR) in a tissue selective manner. These compounds are useful in the enhancement of weakened muscle tone and the treatment of conditions caused by androgen deficiency or which can be ameliorated by androgen administration, including osteoporosis, osteopenia, glucocorticoid-induced osteoporosis, periodontal disease, bone fracture, bone damage following bone reconstructive surgery, sarcopenia, frailty, aging skin, male hypogonadism, postmenopausal symptoms in women, atherosclerosis, hypercholesterolemia, hyperlipidemia, obesity, aplastic anemia and other hematopoietic disorders, inflammatory arthritis and joint repair, HIV-wasting, prostate cancer, benign prostatic hyperplasia (BPH), abdominal adiposity, metabolic syndrome, type II diabetes, cancer cachexia, Alzheimer's disease, muscular dystrophies, cognitive decline, sexual dysfunction, sleep apnea, depression, premature ovarian failure, and autoimmune disease, alone or in combination with other active agents.

6. 发明专利

NO20083046A 未知
公开(公告)号：NO20083046A
公开(公告)日：2008-09-05
申请号：NO20083046
申请日：2008-07-04
申请人： MERCK & CO INC
发明人： MEISSNER ROBERT S , PERKINS JAMES J , COTE AARON S , TAN LUSHI , LI WENJIE , STELLABOTT JOYCE
IPC分类号： C07J3/00
CPC分类号： C07J73/005 , C07D471/04

7. 发明专利

CA2662748A1 LIQUID PHARMACEUTICAL FORMULATIONS FOR ORAL ADMINISTRATION OF A CGRP ANTAGONIST 未知
公开(公告)号：CA2662748A1
公开(公告)日：2008-03-13
申请号：CA2662748
申请日：2007-09-06
申请人： MERCK & CO INC
发明人： ALANI LAMAN L , BRESLIN DAVID , STELLABOTT JOYCE , JAHANSOUZ HOSSAIN , THOMPSON KAREN
IPC分类号： A01N43/00 , A61K9/48 , A61K9/66 , A61K31/55
摘要： Liquid formulations comprising the compound 1-[1-({[(3R,6S)-6-(2,3-difluo rophenyl)-2-oxo-1-(2,2,2-trifluoroethyl)azepan-3-yl]amino}carbonyl)piperidin -4-yl]-2-oxo-1,2-dihydroimidazo[4,5-b]pyridin-3-ide have surprisingly improv ed bioavailability and stability in comprising polyethylene glycol, Tween (p olysorbate 80), Cremophor® EL (polyoxyl 35 castor oil), propylene glycol, an d optionally water, and may be filled into soft or hard gelatin capsules use ful for treating conditions including migraine headache and cluster headache .

8. 发明专利

DOP2006000276A POLIMORFOS DE UN MODULADOR DE RECEPTOR DE ANDRÓGENO 未知
公开(公告)号：DOP2006000276A
公开(公告)日：2007-07-31
申请号：DO2006000276
申请日：2006-12-06
申请人： MERCK & CO INC
发明人： COTE AARON S , TAN LUSHI , MEISSNER ROBERT S , LI WENJIE , PERKINS JAMES J , STELLABOTT JOYCE , KIANG YUAN-HON

9. 发明专利

CA2631936A1 POLYMORPHS OF ANDROGEN RECEPTOR MODULATOR - (N-3H-IMIDAZO [4 , 5-B] PYRIDIN-2-YL-METHYL) -2-FLUORO-4-METHYL-3-OXO-4-AZA-ANDROST- 1-EN-17 . BETA . -CARBOXAMIDE 未知
公开(公告)号：CA2631936A1
公开(公告)日：2007-06-14
申请号：CA2631936
申请日：2006-12-04
申请人： MERCK & CO INC
发明人： MEISSNER ROBERT S , PERKINS JAMES J , STELLABOTT JOYCE , COTE AARON S , LI WENJIE , KIANG YUAN-HON , TAN LUSHI
IPC分类号： C07J73/00 , A61K31/58 , A61P5/26
摘要： Compounds of structural formula I are modulators of the androgen receptor (AR) in a tissue selective manner. These compounds are useful in the enhancement of weakened muscle tone and the treatment of conditions caused by androgen deficiency or which can be ameliorated by androgen administration, including osteoporosis, osteopenia, glucocorticoid-induced osteoporosis, periodontal disease, bone fracture, bone damage following bone reconstructive surgery, sarcopenia, frailty, aging skin, male hypogonadism, postmenopausal symptoms in women, atherosclerosis, hypercholesterolemia, hyperlipidemia, obesity, aplastic anemia and other hematopoietic disorders, inflammatory arthritis and joint repair, HIV-wasting, prostate cancer, benign prostatic hyperplasia (BPH), abdominal adiposity, metabolic syndrome, type II diabetes, cancer cachexia, Alzheimer~s disease, muscular dystrophies, cognitive decline, sexual dysfunction, sleep apnea, depression, premature ovarian failure, and autoimmune disease, alone or in combination with other active agents.

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