公开(公告)号：US09212174B2

公开(公告)日：2015-12-15

申请号：US13579004

申请日：2011-02-07

申请人： Yusuke Iriyama ,  Tsutomu Higashiyama

发明人： Yusuke Iriyama ,  Tsutomu Higashiyama

IPC分类号： C07D307/32 ,  C07D405/04

CPC分类号： C07D405/04 ,  C07D307/32 ,  Y02P20/582

摘要： The invention provides a process for producing a β-dihydrofuran derivative represented by formula (1) or a β-tetrahydrofuran derivative represented by formula (4), characterized in that the process includes causing a dialkyl dicarbonate, a diaralkyl dicarbonate, or a halide to act on a diol compound represented by formula (2) or (3). The invention also provides a process for producing 4′-ethynyl-2′,3′-didehydro-3′-deoxythymidine or an analog thereof, the process including glycosylation and deprotection.

摘要翻译： 本发明提供一种制备由式（1）表示的二氢呋喃衍生物或由式（4）表示的四氢呋喃衍生物的方法，其特征在于该方法包括使二碳酸二烷基酯，二碳酸二烷基酯或 卤化物作用于由式（2）或（3）表示的二醇化合物。 本发明还提供了一种生产4'-乙炔基-2'，3'-二脱氢-3'-脱氧胸苷或其类似物的方法，该方法包括糖基化和脱保护。

公开(公告)号：US20120322995A1

公开(公告)日：2012-12-20

申请号：US13579004

申请日：2011-02-07

申请人： Yusuke Iriyama ,  Tsutomu Higashiyama

发明人： Yusuke Iriyama ,  Tsutomu Higashiyama

IPC分类号： C07D307/32 ,  C07H19/06 ,  C07H1/00 ,  C07F7/08 ,  C07H23/00

CPC分类号： C07D405/04 ,  C07D307/32 ,  Y02P20/582

摘要： The invention provides a process for producing a β-dihydrofuran derivative represented by formula (1) or a β-tetrahydrofuran derivative represented by formula (4), characterized in that the process includes causing a dialkyl dicarbonate, a diaralkyl dicarbonate, or a halide to act on a diol compound represented by formula (2) or (3). The invention also provides a process for producing 4′-ethynyl-2′,3′-didehydro-3′-deoxythymidine or an analog thereof, the process including glycosylation and deprotection.

摘要翻译： 本发明提供一种制备由式（1）表示的二氢呋喃衍生物或由式（4）表示的四氢呋喃衍生物的方法，其特征在于该方法包括使二碳酸二烷基酯，二碳酸二烷基酯或 卤化物作用于由式（2）或（3）表示的二醇化合物。 本发明还提供了一种生产4'-乙炔基-2'，3'-二脱氢-3'-脱氧胸苷或其类似物的方法，该方法包括糖基化和脱保护。

公开(公告)号：US5840909A

公开(公告)日：1998-11-24

申请号：US998669

申请日：1997-12-29

申请人： Keizo Tanikawa ,  Yoshimasa Kamikawaji ,  Keisuke Odoi ,  Tsutomu Higashiyama ,  Masayuki Sato ,  Yukinori Masuda

发明人： Keizo Tanikawa ,  Yoshimasa Kamikawaji ,  Keisuke Odoi ,  Tsutomu Higashiyama ,  Masayuki Sato ,  Yukinori Masuda

IPC分类号： C07D231/38 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07F9/6558 ,  A61K31/415

CPC分类号： C07D231/38 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07F9/65583

摘要： Pyrazole compounds of formula �1! and their tautomers and salts: ##STR1## (wherein R.sup.1 is an alkyl group, etc.; R.sup.2 is a carboxyl group, etc.; R.sup.3 is a halogen atom, an alkyl group, a phenyl group, etc.; R.sup.4, R.sup.5 and R.sup.6 each are a hydrogen atom, a halogen atom, etc.; R.sup.7 is a carboxyl group, a 5-tetrazolyl group, etc.; X is a nitrogen atom, etc.; Y and Z each are CH, a nitrogen atom, etc.; A and E each are a methylene group, etc.; D is a phenyl group, etc.; G is a covalent bond, etc.). The compounds of the invention have an antagonistic effect against angiotensin II and are useful for prevention and remedy of hypertension, congestive cardiac insufficiency, chronic renal insufficiency, aldosteronism, hyper-intraocular pressure, etc.

摘要翻译： 式[1]的吡唑化合物及其互变异构体和盐：其中R1是烷基等; R2是羧基等; R3是卤素原子，烷基， 苯基等; R4，R5和R6分别是氢原子，卤素原子等; R7是羧基，5-四唑基等; X是氮原子等; Y和 Z各自为CH，氮原子等; A和E各自为亚甲基等; D为苯基等; G为共价键等）。 本发明化合物对血管紧张素II具有拮抗作用，可用于预防和治疗高血压，充血性心功能不全，慢性肾功能不全，醛固酮增多症，超眼压等。

公开(公告)号：US5846991A

公开(公告)日：1998-12-08

申请号：US998671

申请日：1997-12-29

申请人： Keizo Tanikawa ,  Yoshimasa Kamikawaji ,  Keisuke Odoi ,  Tsutomu Higashiyama ,  Masayuki Sato ,  Yukinori Masuda

发明人： Keizo Tanikawa ,  Yoshimasa Kamikawaji ,  Keisuke Odoi ,  Tsutomu Higashiyama ,  Masayuki Sato ,  Yukinori Masuda

IPC分类号： C07D231/38 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07F9/6558 ,  A61K31/415 ,  A61K31/44

CPC分类号： C07D231/38 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07F9/65583

摘要： Pyrazole compounds of formula �1! and their tautomers and salts: ##STR1## (wherein R.sup.1 is an alkyl group, etc.; R.sup.2 is a carboxyl group, etc.; R.sup.3 is a halogen atom, an alkyl group, a phenyl group, etc.; R.sup.4, R.sup.5 and R.sup.6 each are a hydrogen atom, a halogen atom, etc.; R.sup.7 is a carboxyl group, a 5-tetrazolyl group, etc.; X is a nitrogen atom, etc.; Y and Z each are CH, a nitrogen atom, etc.; A and E each are a methylene group, etc.; D is a phenyl group, etc.; G is a covalent bond, etc.). The compounds of the invention have an antagonistic effect against angiotensin II and are useful for prevention and remedy of hypertension, congestive cardiac insufficiency, chronic renal insufficiency, aldosteronism, hyper-intraocular pressure, etc.

公开(公告)号：US5721264A

公开(公告)日：1998-02-24

申请号：US525555

申请日：1995-09-29

申请人： Keizo Tanikawa ,  Yoshimasa Kamikawaji ,  Keisuke Odoi ,  Tsutomu Higashiyama ,  Masayuki Sato ,  Yukinori Masuda

发明人： Keizo Tanikawa ,  Yoshimasa Kamikawaji ,  Keisuke Odoi ,  Tsutomu Higashiyama ,  Masayuki Sato ,  Yukinori Masuda

IPC分类号： C07D231/38 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07F9/6558 ,  A61K31/415

CPC分类号： C07D231/38 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07F9/65583

摘要： Pyrazole compounds of formula �1! and their tautomers and salts: ##STR1## (wherein R.sup.1 is an alkyl group, etc.; R.sup.2 is a carboxyl group, etc.; R.sup.3 is a halogen atom, an alkyl group, a phenyl group, etc.; R.sup.4, R.sup.5 and R.sup.6 each are a hydrogen atom, a halogen atom, etc.; R.sup.7 is a carboxyl group, a 5-tetrazolyl group, etc.; X is a nitrogen atom, etc.; Y and Z each are CH, a nitrogen atom, etc.; A and E each are a methylene group, etc.; D is a phenyl group, etc.; G is a covalent bond, etc.). The compounds of the invention have an antagonistic effect against angiotensin II and are useful for prevention and remedy of hypertension, congestive cardiac insufficiency, chronic renal insufficiency, aldosteronism, hyper-intraocular pressure, etc.

摘要翻译： PCT No.PCT / JP94 / 00587第 371 1995年9月29日第 102（e）1995年9月29日PCT PCT 1994年4月7日PCT公布。 公开号WO94 / 22838 日期：1994年10月13日式[1]吡唑化合物及其互变异构体和盐：其中R1是烷基等; R2是羧基等; R3是卤素原子， 烷基，苯基等; R4，R5和R6各自为氢原子，卤素原子等; R7为羧基，5-四唑基等; X为氮原子， Y和Z各自为CH，氮原子等; A和E各自为亚甲基等; D为苯基等; G为共价键等）。 本发明化合物对血管紧张素II具有拮抗作用，可用于预防和治疗高血压，充血性心功能不全，慢性肾功能不全，醛固酮增多症，超眼压等。

公开(公告)号：US5817828A

公开(公告)日：1998-10-06

申请号：US999493

申请日：1997-12-29

申请人： Keizo Tanikawa ,  Yoshimasa Kamikawaji ,  Keisuke Odoi ,  Tsutomu Higashiyama ,  Masayuki Sato ,  Yukinori Masuda

发明人： Keizo Tanikawa ,  Yoshimasa Kamikawaji ,  Keisuke Odoi ,  Tsutomu Higashiyama ,  Masayuki Sato ,  Yukinori Masuda

IPC分类号： C07D231/38 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07F9/6558 ,  A61K31/415

CPC分类号： C07D231/38 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07F9/65583

摘要： Pyrazole compounds of formula �1! and their tautomers and salts: ##STR1## (wherein R.sup.1 is an alkyl group, etc.; R.sup.2 is a carboxyl group, etc.; R.sup.3 is a halogen atom, an alkyl group, a phenyl group, etc.; R.sup.4, R.sup.5 and R.sup.6 each are a hydrogen atom, a halogen atom, etc.; R.sup.7 is a carboxyl group, a 5-tetrazolyl group, etc.; X is a nitrogen atom, etc.; Y and Z each are CH, a nitrogen atom, etc.; A and E each are a methylene group, etc.; D is a phenyl group, etc.; G is a covalent bond, etc.). The compounds of the invention have an antagonistic effect against angiotensin II and are useful for prevention and remedy of hypertension, congestive cardiac insufficiency, chronic renal insufficiency, aldosteronism, hyper-intraocular pressure, etc.