公开(公告)号：US06756385B2

公开(公告)日：2004-06-29

申请号：US09919630

申请日：2001-07-31

申请人： Mark A. Sanner ,  Chris J. Helal ,  Christoper B. Cooper ,  Frank S. Menniti ,  Michael K. Ahlijanian ,  Annabella Villalobos ,  Lit-Fui Lau ,  Patricia A. Seymour

发明人： Mark A. Sanner ,  Chris J. Helal ,  Christoper B. Cooper ,  Frank S. Menniti ,  Michael K. Ahlijanian ,  Annabella Villalobos ,  Lit-Fui Lau ,  Patricia A. Seymour

IPC分类号： A61K314709

CPC分类号： C07D401/12 ,  C07D233/88 ,  C07D233/90 ,  C07D401/14 ,  C07D403/12 ,  C07D417/14

摘要： The invention provides compounds of formula 1 wherein R1, R2, R3, and R4 are as defined, and their pharmaceutically acceptable salts. Compounds of formula 1 are indicated to have activity inhibiting cdk5, cdk2, and GSK-3. Pharmaceutical compositions and methods comprising compounds of formula 1 for treating and preventing diseases and conditions comprising abnormal cell growth, such as cancer, and neurodegenerative diseases and conditions and those affected by dopamine neurotransmission. Also described are pharmaceutical compositions and methods comprising compounds of formula 1 for treating male fertility and sperm motility; diabetes mellitus; impaired glucose tolerance; metabolic syndrome or syndrome X; polycystic ovary syndrome; adipogenesis and obesity; myogenesis and frailty, for example age-related decline in physical performance; acute sarcopenia, for example muscle atrophy and/or cachexia associated with burns, bed rest, limb immobilization, or major thoracic, abdominal, and/or orthopedic surgery; sepsis; hair loss, hair thinning, and balding; and immunodeficiency.

摘要翻译： 本发明提供了式1化合物，其中R 1，R 2，R 3和R 4如上定义，及其药学上可接受的盐。 式1的化合物表示具有抑制cdk5，cdk2和GSK-3的活性。 包含式1化合物的药物组合物和方法，用于治疗和预防包括异常细胞生长（例如癌症）和神经变性疾病和病症以及受多巴胺神经传递影响的疾病和病症。 还描述了包含用于治疗雄性生育力和精子活力的式1化合物的药物组合物和方法; 糖尿病 葡萄糖耐量降低; 代谢综合征或综合征X; 多囊卵巢综合征; 脂肪生成和肥胖; 造血和虚弱，例如年龄相关的身体表现下降; 急性肌肉减少症，例如与烧伤，卧床休息，肢体固定或主要胸部，腹部和/或整形外科手术相关的肌肉萎缩和/或恶病质; 败血症 脱发，脱发，秃头; 和免疫缺陷。

公开(公告)号：US07078529B2

公开(公告)日：2006-07-18

申请号：US10818855

申请日：2004-04-05

申请人： Mark A. Sanner ,  Chris J. Helal ,  Christoper B. Cooper ,  Frank S. Menniti ,  Patricia A. Seymour ,  Michael K. Ahlijanian ,  Anabella Villalobos ,  Lit-Fui Lau

发明人： Mark A. Sanner ,  Chris J. Helal ,  Christoper B. Cooper ,  Frank S. Menniti ,  Patricia A. Seymour ,  Michael K. Ahlijanian ,  Anabella Villalobos ,  Lit-Fui Lau

IPC分类号： C07D233/88

CPC分类号： C07D401/12 ,  C07D233/88 ,  C07D233/90 ,  C07D401/14 ,  C07D403/12 ,  C07D417/14

摘要： The invention provides compounds of formula 1 wherein R1, R2, R3, and R4 are as defined, and their pharmaceutically acceptable salts. Compounds of formula 1 are indicated to have activity inhibiting cdk5, cdk2, and GSK-3. Pharmaceutical compositions and methods comprising compounds of formula 1 for treating and preventing diseases and conditions comprising abnormal cell growth, such as cancer, and neurodegenerative diseases and conditions and those affected by dopamine neurotransmission. Also described are pharmaceutical compositions and methods comprising compounds of formula 1 for treating male fertility and sperm motility; diabetes mellitus; impaired glucose tolerance; metabolic syndrome or syndrome X; polycystic ovary syndrome; adipogenesis and obesity; myogenesis and frailty, for example age-related decline in physical performance; acute sarcopenia, for example muscle atrophy and/or cachexia associated with burns, bed rest, limb immobilization, or major thoracic, abdominal, and/or orthopedic surgery; sepsis; hair loss, hair thinning, and balding; and immunodeficiency.

摘要翻译： 本发明提供式1化合物，其中R 1，R 2，R 3，R 4和R 4均为 并且其药学上可接受的盐。 式1的化合物表示具有抑制cdk5，cdk2和GSK-3的活性。 包含式1化合物的药物组合物和方法，用于治疗和预防包括异常细胞生长（例如癌症）和神经变性疾病和病症以及受多巴胺神经传递影响的疾病和病症。 还描述了包含用于治疗雄性生育力和精子活力的式1化合物的药物组合物和方法; 糖尿病 葡萄糖耐量降低; 代谢综合征或综合征X; 多囊卵巢综合征; 脂肪生成和肥胖; 造血和虚弱，例如年龄相关的身体表现下降; 急性肌肉减少症，例如与烧伤，卧床休息，肢体固定或主要胸部，腹部和/或整形外科手术相关的肌肉萎缩和/或恶病质; 败血症 脱发，脱发，秃头; 和免疫缺陷。