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1. 发明申请

US20060205750A1 Novel benzimidazole derivatives 失效
公开(公告)号：US20060205750A1
公开(公告)日：2006-09-14
申请号：US11431274
申请日：2006-05-10
申请人： Norikazu Otake , Minoru Moriya , Yoshio Ogino , Kenji Matsuda , Yoshikazu Nagae , Akio Kanatani , Takehiro Fukami
发明人： Norikazu Otake , Minoru Moriya , Yoshio Ogino , Kenji Matsuda , Yoshikazu Nagae , Akio Kanatani , Takehiro Fukami
IPC分类号： A61K31/4747 , A61K31/4184 , C07D487/10
CPC分类号： C07D473/30 , C07D405/04 , C07D471/04 , C07D471/10 , C07D473/00 , C07D491/04
摘要： The present invention relates to a compound of the formula (I): (wherein A, B, C and D are independently nitrogen or optionally substituted methine; E is nitrogen, methine or hydroxy substituted methine; n is 0 or 1; T, U, V and W are independently nitrogen or optionally substituted methine; X is —N(SO2R4)—, —N(COR5)— or —CO—; Y is —C(R6)(R7)—, —O— or —N(R8)—, provided that the compound (I) when E is nitrogen, n is 0, X is —CO—, and Y is —O— is excluded) and the like, which are useful as an agent for the treatment of various diseases related to NPY, for example cardiovascular disorders such as angina, acute or congestive heart failure, myocardial infarction, hypertension, nephropathy, electrolyte abnormality, vasospasm, arteriosclerosis, etc., central nervous system disorders such as bulimia, depression, anxiety, seizure, epilepsy, dementia, pain, alcoholism, drug withdrawal, circadian rhythm disorders, schizophrenia, memory impairment, sleep disorders, cognitive impairment, etc., metabolic diseases such as obesity, diabetes, hormone abnormality, hypercholesterolemia, hyperlipidemia, gout, fatty liver, etc., genital or reproductive disorders such as infertility, preterm labor, sexual dysfunction, etc., gastro-intestinal disorders, respiratory disorder, inflammatory diseases or glaucoma, and the like, also for example, atherosclerosis, hypogonadism, hyperandrogenism, polycystic ovary syndrome (Pickwickian syndrome), hirsutism, gastro-intestinal motility disorder, obesity-related gastro-esophageal reflux, obesity hypoventilation, sleep apnea, inflammation, systemic inflammation of the vasculature, osteoarthritis, insulin resistance, bronchoconstriction, alcohol preference, metabolic syndrome, Alzheimer's disease, cardiac hypertrophy, left ventricular hypertrophy, hypertriglyceridemia, low HDL cholesterol, cardiovascular disorders such as coronary heart disease (CHD), cerebrovascular disease, stroke, peripheral vascular disease, sudden death, gallbladder diseases, cancer (breast, endometrial, colon), breathlessness, hyperuricemia, impaired fertility, low back pain, or increased anesthetic risk, and the like.

2. 发明授权

US06388077B1 Spiro compounds 有权
标题翻译：螺环化合物
公开(公告)号：US06388077B1
公开(公告)日：2002-05-14
申请号：US09983598
申请日：2001-10-25
申请人： Takehiro Fukami , Akio Kanatani , Akane Ishihara , Yasuyuki Ishii , Toshiyuki Takahashi , Yuji Haga , Toshihiro Sakamoto , Takahiro Itoh
发明人： Takehiro Fukami , Akio Kanatani , Akane Ishihara , Yasuyuki Ishii , Toshiyuki Takahashi , Yuji Haga , Toshihiro Sakamoto , Takahiro Itoh
IPC分类号： C07D491107
CPC分类号： C07D405/12 , C07D213/61 , C07D307/94 , C07D471/10 , C07D491/10
摘要： Compounds of the general formula VI-1 and processes for their preparation: wherein t, u, v and w each independently represent a nitrogen atom or a methine group which may have a substituent selected from the group consisting of halogen, lower alkyl, lower alkoxy and optionally protected hydroxy; and wherein at least two of which represent the methine group. These compounds serve as intermediates for novel spiro compounds which exhibit neuropeptide Y receptor (NPY) antagonistic activities and are useful as agents for the treatment of various diseases related to NPY, for example, cardiovascular disorders, central nervous system disorders, metabolic diseases and the like.
摘要翻译：通式VI-1的化合物及其制备方法：其中t，u，v和w各自独立地表示氮原子或次甲基，其可以具有选自卤素，低级烷基，低级烷氧基和任选保护的羟基; 并且其中至少两个表示次甲基。这些化合物用作新的螺旋化合物的中间体，其表现出神经肽Y受体（NPY）拮抗活性，并且可用作治疗与NPY相关的各种疾病的药剂，例如心血管疾病，中枢神经系统疾病，代谢疾病等。

3. 发明授权

US06335345B1 Spiro compounds 有权
标题翻译：螺环化合物
公开(公告)号：US06335345B1
公开(公告)日：2002-01-01
申请号：US09928431
申请日：2001-08-14
申请人： Takehiro Fukami , Akio Kanatani , Akane Ishihara , Yasuyuki Ishii , Toshiyuki Takahashi , Yuji Haga , Toshihiro Sakamoto , Takahiro Itoh
发明人： Takehiro Fukami , Akio Kanatani , Akane Ishihara , Yasuyuki Ishii , Toshiyuki Takahashi , Yuji Haga , Toshihiro Sakamoto , Takahiro Itoh
IPC分类号： A61K31506
CPC分类号： C07D405/12 , C07D213/61 , C07D307/94 , C07D471/10 , C07D491/10
摘要： Spiro compounds of the general formula (I): wherein Ar1 represents an optionally substituted aryl or heteroaryl; n represents 0 or 1; T, U, V and W each represent a nitrogen atom or an optionally substituted methine group, wherein at least two of which represent said methine group; X represents methine; Y represents an optionally substituted imino or oxygen atom. These novel spiro compounds exhibit neuropeptide Y receptor (NPY) antagonistic activities and are useful as agents for the treatment of various diseases related to NPY, for example, cardiovascular disorders, central nervous system disorders, metobolic diseases and the like.
摘要翻译：通式（I）的螺环化合物：其中Ar1表示任选取代的芳基或杂芳基; n表示0或1; T，U，V和W各自表示氮原子或任选取代的次甲基，其中至少两个其表示次甲基; X表示次甲基; Y表示任选取代的亚氨基或氧原子。这些新型螺环化合物表现出神经肽Y受体（NPY）拮抗活性，可用作治疗与NPY有关的各种疾病的药剂，例如心血管疾病，中枢神经系统疾病，全身性疾病等。

4. 发明授权

US06326375B1 Spiro compounds 有权
标题翻译：螺环化合物
公开(公告)号：US06326375B1
公开(公告)日：2001-12-04
申请号：US09640784
申请日：2000-08-18
申请人： Takehiro Fukami , Akio Kanatani , Akane Ishihara , Yasuyuki Ishii , Toshiyuki Takahashi , Yuji Haga , Toshihiro Sakamoto , Takahiro Itoh
发明人： Takehiro Fukami , Akio Kanatani , Akane Ishihara , Yasuyuki Ishii , Toshiyuki Takahashi , Yuji Haga , Toshihiro Sakamoto , Takahiro Itoh
IPC分类号： A61K31438
CPC分类号： C07D405/12 , C07D213/61 , C07D307/94 , C07D471/10 , C07D491/10
摘要： Spiro compounds of the general formula (I): wherein Ar1 represents an optionally substituted aryl or heteroaryl; n represents 0 or 1; T, U, V and W each represent a nitrogen atom or an optionally substituted methine group, wherein at least two of which represent said methine group; X represents nitrogen; Y represents an optionally substituted imino or oxygen atom, which exhibit neuropeptide Y receptor (NPY) antagonistic activities and are useful as agents for the treatment of various diseases related to NPY, for example, cardiovascular disorders, central nervous system disorders, metobolic diseases and the like.
摘要翻译：通式（I）的螺环化合物：其中Ar1表示任选取代的芳基或杂芳基; n表示0或1; T，U，V和W各自表示氮原子或任选取代的次甲基，其中至少两个代表所述次甲基; X表示氮; Y表示任选取代的亚氨基或氧原子，其表现出神经肽Y受体（NPY）拮抗活性，可用作治疗与NPY相关的各种疾病的药剂，例如心血管疾病，中枢神经系统疾病，全身性疾病等。

5. 发明授权

US5614498A Endothelin antagonistic substance 失效
标题翻译：内皮素拮抗物质
公开(公告)号：US5614498A
公开(公告)日：1997-03-25
申请号：US945414
申请日：1992-09-16
申请人： Kiyofumi Ishikawa , Takehiro Fukami , Takeshi Hayama , Kenji Niiyama , Toshio Nagase , Toshiaki Mase , Kagari Fujita , Masaki Ihara , Fumihiko Ikemoto , Mitsuo Yano , Masaru Nishikibe
发明人： Kiyofumi Ishikawa , Takehiro Fukami , Takeshi Hayama , Kenji Niiyama , Toshio Nagase , Toshiaki Mase , Kagari Fujita , Masaki Ihara , Fumihiko Ikemoto , Mitsuo Yano , Masaru Nishikibe
IPC分类号： A61K38/00 , C07K5/02 , C07K5/06 , C07K5/083 , C07K5/087 , C07K5/103 , C07K5/00 , C07K5/08 , C07K5/10
CPC分类号： C07K5/1008 , C07K5/0202 , C07K5/0205 , C07K5/06034 , C07K5/06043 , C07K5/0808 , C07K5/0812 , A61K38/00
摘要： Peptides having the formula: ##STR1## inhibit the binding of endothelin to its ET.sub.B receptor and are useful in treating diseases associated with excess production or secretion of endothelin.
摘要翻译：具有下式的肽：（I）抑制内皮素与其ETB受体的结合，并且可用于治疗与内皮素过量产生或分泌相关的疾病。

6. 发明授权

US5494897A Endothelin antagonistic peptide 失效
标题翻译：内皮素拮抗肽
公开(公告)号：US5494897A
公开(公告)日：1996-02-27
申请号：US253775
申请日：1994-06-03
申请人： Kiyofumi Ishikawa , Takehiro Fukami , Masaki Ihara , Mitsuo Yano
发明人： Kiyofumi Ishikawa , Takehiro Fukami , Masaki Ihara , Mitsuo Yano
IPC分类号： A61K38/00 , C07D209/42 , C07K5/083 , C07K5/087 , C07K14/575 , A61K38/04 , C07K5/00
CPC分类号： C07K14/57536 , C07D209/42 , C07K5/0808 , C07K5/0812 , A61K38/00
摘要： A peptide derivative of the formula: ##STR1## is a novel compound having antagonism against three endothelin isopeptides. A 2-cyanotryptophan or a protected compound thereof, is an intermediate for the preparation of the endothelin antagonist.
摘要翻译：式（I）的肽衍生物是对三种内皮素多肽具有拮抗作用的新化合物。 2-氰基色氨酸或其保护的化合物是制备内皮素拮抗剂的中间体。

7. 发明授权

US07205417B2 Spiro compounds 失效
标题翻译：螺环化合物
公开(公告)号：US07205417B2
公开(公告)日：2007-04-17
申请号：US10485955
申请日：2002-08-02
申请人： Takehiro Fukami , Katsumasa Nonoshita , Takeshi Sagara , Hiroyuki Kishino
发明人： Takehiro Fukami , Katsumasa Nonoshita , Takeshi Sagara , Hiroyuki Kishino
IPC分类号： C07D307/94 , C07D407/12 , A61K31/4525
CPC分类号： C07D401/12 , A61K31/4747 , C07D209/96 , C07D307/94 , C07D403/12 , C07D405/12 , C07D471/10 , C07D491/10
摘要： Compounds of the formula (I): (wherein A is an optionally substituted straight-chain hydrocarbon having 1 to 6 carbon atoms, which is optionally intervened by oxygen or nitrogen atom; Ar1 is aryl or heteroaryl, any of which is optionally substituted; n is 0 or 1; R0 is hydrogen, or lower alkylene attached to an arbitrary, bondable position of A; T, U, V and W are independently nitrogen atom or optionally substituted methine, and at least two of T, U, V and W are said methine group; X is —N(SO2R1)—, —N(COR2)— or —CO—; Y is —C(R3)(R4)—, —O— or —N(R5)—; Z is methine or nitrogen atom) exhibit NPY antagonistic activities and are useful as agents for the treatment of various diseases related to NPY, for example, cardiovascular disorders such as hypertension, nephropathy, heart disease, vasospasm, arteriosclerosis, etc., central nervous system disorders such as bulimia, depression, anxiety, seizure, epilepsy, dementia, pain, alcoholism, drug withdrawal, circadian rhythm disorders, schizophrenia, etc., metabolic diseases such as obesity, diabetes, hormone abnormality, hypercholesterolemia, hyperlipidemia, etc., sexual and reproductive dysfunctions, and gastro-intestinal motility disorder.
摘要翻译：式（I）的化合物：

8. 发明授权

US06649624B2 Spiro compounds 有权
标题翻译：螺环化合物
公开(公告)号：US06649624B2
公开(公告)日：2003-11-18
申请号：US10226225
申请日：2002-08-23
申请人： Takehiro Fukami , Akio Kanatani , Akane Ishihara , Yasuyuki Ishii , Toshiyuki Takahashi , Yuji Haga , Toshihiro Sakamoto , Takahiro Itoh
发明人： Takehiro Fukami , Akio Kanatani , Akane Ishihara , Yasuyuki Ishii , Toshiyuki Takahashi , Yuji Haga , Toshihiro Sakamoto , Takahiro Itoh
IPC分类号： A61K31438
CPC分类号： C07D405/12 , C07D213/61 , C07D307/94 , C07D471/10 , C07D491/10
摘要： A method for treating a central nervous system disorder, which involves administering to a patient in need a therapeutically effective amount of a compound of formula (I): wherein Ar1 represents an aryl or heteroaryl which may be substituted, the substituent being selected from the group consisting of halogen, nitro, lower alkyl, halo(lower) alkyl, hydroxy(lower) alkyl, cyclo(lower) alkyl, lower alkenyl, lower alkoxy, halo(lower) alkoxy, lower alkylthio, carboxyl, lower alkanoyl, lower alkoxycarbonyl, lower alkylene optionally substituted with oxo, and a group represented by the formula —Q—Ar2; Ar2 represents an aryl or heteroaryl which may be substituted, the substituent being selected from the group consisting of halogen, cyano, lower alkyl, halo(lower) alkyl, hydroxy(lower) alkyl, hydroxy, lower alkoxy, halo(lower) alkoxy, lower alkylamino, di-lower alkylamino, lower alkanoyl and aryl: n represents 0 or 1; Q represents a single bond or carbonyl; T, U, V and W each independently represent a nitrogen atom or a methine group which may have a substituent selected from the group consisting of halogen, lower alkyl, hydroxy and lower alkoxy, wherein at least two of which represent said methine group; X represents methine; Y represents an imino which may be substituted with lower alkyl, or oxygen; or a salt or ester thereof
摘要翻译：一种治疗中枢神经系统疾病的方法，其涉及向需要的患者施用治疗有效量的式（I）化合物：其中Ar 1表示可被取代的芳基或杂芳基，所选择的取代基卤代低级烷基，羟基（低级）烷基，环（低级）烷基，低级烯基，低级烷氧基，卤代（低级）烷氧基，低级烷硫基，羧基，低级烷酰基，低级烷氧基羰基，任选被氧代取代的低级亚烷基和由式-Q-Ar 2表示的基团; Ar 2表示可被取代的芳基或杂芳基，该取代基选自卤素，氰基，低级烷基，卤代（低级）烷基，羟基（低级）烷基，羟基，低级烷氧基，卤代（低级）烷氧基，低级烷基氨基，二低级烷基氨基，低级烷酰基和芳基：n表示0或1; Q表示单键或羰基; T，U，V和W各自独立地表示反应可以具有选自卤素，低级烷基，羟基和低级烷氧基的取代基的氮原子或次甲基，其中至少两个表示所述次甲基; X表示次甲基; Y表示亚氨基，被低级烷基或氧取代; 或其盐或酯

9. 发明授权

US5691315A Endothelin antagonistic peptide derivatives 失效
标题翻译：内皮素拮抗肽衍生物
公开(公告)号：US5691315A
公开(公告)日：1997-11-25
申请号：US494818
申请日：1995-06-26
申请人： Kiyofumi Ishikawa , Takehiro Fukami , Takashi Hayama , Kenji Niiyama , Toshio Nagase , Toshiaki Mase , Kagari Fujita , Masaki Ihara , Fumihiko Ikemoto , Mitsuo Yano
发明人： Kiyofumi Ishikawa , Takehiro Fukami , Takashi Hayama , Kenji Niiyama , Toshio Nagase , Toshiaki Mase , Kagari Fujita , Masaki Ihara , Fumihiko Ikemoto , Mitsuo Yano
IPC分类号： A61K38/00 , C07K5/02 , C07K5/06 , C07K5/083 , C07K5/103 , C07K5/08 , C07K7/06
CPC分类号： C07K5/06156 , C07K5/0202 , C07K5/0205 , C07K5/06043 , C07K5/0808 , C07K5/1008 , A61K38/00
摘要： The invention relates to compounds which are antagonists of endothelin, to processes for their preparation, and to their use as pharmaceuticals. The compounds of the invention are Useful in the treatment of hypertension, pulmonary hypertension, Reynaud's disease, myocardial infarction, angina pectoris, acute renal failure, cerebral infarction, cerebral vasospasm, arteriosclerosis, asthma, endotoxin shock, endotoxin-induced multiple organ failure or disseminated intravascular coagulation, and/or cyclosporin-induced renal failure or hypertension.
摘要翻译：本发明涉及作为内皮素拮抗剂的化合物，其制备方法及其作为药物的用途。本发明化合物可用于治疗高血压，肺动脉高压，雷诺氏病，心肌梗塞，心绞痛，急性肾衰竭，脑梗塞，脑血管痉挛，动脉硬化，哮喘，内毒素休克，内毒素诱导的多器官功能衰竭或弥散性血管内凝血和/或环孢菌素诱导的肾衰竭或高血压。

10. 发明授权

US5496928A Endothelin antagonistic substance 失效
标题翻译：内皮素拮抗物质
公开(公告)号：US5496928A
公开(公告)日：1996-03-05
申请号：US230534
申请日：1994-04-20
申请人： Kiyofumi Ishikawa , Takehiro Fukami , Takashi Hayama , Kenji Niiyama , Toshio Nagase , Toshiaki Mase , Kagari Fujita , Masaki Ihara , Fumihiko Ikemoto , Mitsuo Yano , Masaru Nishikibe
发明人： Kiyofumi Ishikawa , Takehiro Fukami , Takashi Hayama , Kenji Niiyama , Toshio Nagase , Toshiaki Mase , Kagari Fujita , Masaki Ihara , Fumihiko Ikemoto , Mitsuo Yano , Masaru Nishikibe
IPC分类号： A61K38/00 , C07K5/02 , C07K5/06 , C07K5/083 , C07K5/087 , C07K5/103 , A61K38/06
CPC分类号： C07K5/1008 , C07K5/0202 , C07K5/0205 , C07K5/06034 , C07K5/06043 , C07K5/0808 , C07K5/0812 , A61K38/00
摘要： Peptides having the formula: ##STR1## inhibit the binding of endothelin and are useful in treating diseases associated with excess production or secretion of endothelin.
摘要翻译：具有下式的肽：（I）抑制内皮素的结合，并且可用于治疗与内皮素过量产生或分泌相关的疾病。

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