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1. 发明申请

WO1997047599A1 SUCCINAMIDE DERIVATIVES USEFUL AS TNF- AND/OR MMP INHIBITORS 审中-公开
标题翻译： SUCCINAMIDE衍生物可用作TNF-和/或MMP抑制剂
公开(公告)号：WO1997047599A1
公开(公告)日：1997-12-18
申请号：PCT/JP1997002004
申请日：1997-06-11
申请人： FUJISAWA PHARMACEUTICAL CO., LTD. , HEMMI, Mitsue +hf , NEYA, Masahiro , URANO, Yasuharu , SHIMA, Ichiro
发明人： FUJISAWA PHARMACEUTICAL CO., LTD. , HEMMI, Mitsue +hf , HEMMI, Keiji +di
IPC分类号： C07D213/55
CPC分类号： C07D401/12 , C07D209/46 , C07D213/55 , C07D213/56 , C07D213/81 , C07D213/82 , C07D401/14 , C07D405/12 , Y02P20/55
摘要： A compound of formula (I), in which R is hydrogen or hydroxy-protective group, R is hydrogen or acyl, R is hydrogen or lower alkyl, or the formula (II) is (III), R is heterocyclic (lower) alkyl, and R is lower alkoxy or lower alkylamino, or a pharmaceutically acceptable salt thereof, which is useful as a medicament.
摘要翻译：式（I）化合物，其中R 1为氢或羟基保护基，R 2为氢或酰基，R 3为氢或低级烷基，或式（II）为（III ），R 4是杂环（低级）烷基，R 5是可用作药物的低级烷氧基或低级烷基氨基或其药学上可接受的盐。

2. 发明申请

WO1996015109A1 ENDOTHELIN ANTAGONISTS 审中-公开
标题翻译：内皮素拮抗剂
公开(公告)号：WO1996015109A1
公开(公告)日：1996-05-23
申请号：PCT/JP1995002306
申请日：1995-11-13
申请人： FUJISAWA PHARMACEUTICAL CO., LTD. , HEMMI, Mitsue +hf , NEYA, Masahiro , ZENKOH, Tatsuya , SAWADA, Hitoshi , KASAHARA, Chiyoshi , MURATA, Masayoshi
发明人： FUJISAWA PHARMACEUTICAL CO., LTD. , HEMMI, Mitsue +hf , HEMMI, Keiji +di
IPC分类号： C07D209/20
CPC分类号： C07D405/12 , C07D209/20 , C07D317/60 , C07D409/12
摘要： A compound of formula (I), in which: R is lower alkyl, cyclo(lower)alkyl, optionally substituted aryl, optionally substituted heterocyclic group, cyclo(lower)alkyl(lower)alkyl, or ar(lower)alkyl; R is hydrogen, hydroxy or protected hydroxy; R is lower alkyl, aryl, ar(lower)alkyl or optionally substituted heterocyclic(lower)alkyl; R is carboxy, protected carboxy or lower alkylsufonylcarbamoyl; R is hydrogen or lower alkyl; R is hydrogen or heterocyclic group; A is a single bond or lower alkylene, and Ar is optionally substituted aryl, or pharmaceutically acceptable salts thereof, having endothelin antagonistic activity.
摘要翻译：式（I）化合物，其中：R 1为低级烷基，环（低级）烷基，任选取代的芳基，任选取代的杂环基，环（低级）烷基（低级）烷基或芳（低级）烷基 ; R 2是氢，羟基或保护的羟基; R 3是低级烷基，芳基，芳（低级）烷基或任选取代的杂环（低级）烷基; R 4是羧基，保护的羧基或低级烷基磺酰基氨基甲酰基; R 5是氢或低级烷基; R 6是氢或杂环基; A是单键或低级亚烷基，Ar是具有内皮素拮抗活性的任选取代的芳基或其药学上可接受的盐。

3. 发明申请

WO1997003951A1 ESTERS AND AMIDES AS PLA2 INHIBITORS 审中-公开
标题翻译：雌二醇作为PLA2抑制剂
公开(公告)号：WO1997003951A1
公开(公告)日：1997-02-06
申请号：PCT/JP1996001995
申请日：1996-07-18
申请人： FUJISAWA PHARMACEUTICAL CO., LTD. , HEMMI, Mitsue +hf , HEMMI, Keiichiro +hm , HEMMI, Yusuke +hm , FUKAMI, Naoki , YOSHIMURA, Seiji , IMAI, Keisuke
发明人： FUJISAWA PHARMACEUTICAL CO., LTD. , HEMMI, Mitsue +hf , HEMMI, Keiichiro +hm , HEMMI, Yusuke +hm , HEMMI, Keiji +di
IPC分类号： C07C271/22
CPC分类号： C07D401/06 , C07C237/22 , C07C271/22 , C07D209/42 , C07D215/48 , C07D217/26 , C07D307/80 , C07D401/12 , C07D405/12
摘要： The present invention relates to a novel fatty acid derivative of formula (I), wherein R is acyl group; R is acyl(lower)alkyl; R is hydrogen, aryl(lower)alkyl, etc.; R is acyl(lower)alkyl; and X is -O-, -NH- or formula (II) [wherein R is lower alkyl, etc.]; and a pharmaceutically acceptable salt thereof, which is useful as a medicament; the processes for the preparation of said fatty acid derivative or a salt thereof; a pharmaceutical composition comprising said fatty acid derivative or a pharmaceutically acceptable salt thereof; etc.
摘要翻译：本发明涉及式（I）的新型脂肪酸衍生物，其中R 1是酰基; R 2是酰基（低级）烷基; R 3是氢，芳基（低级）烷基等; R 4是酰基（低级）烷基; 并且X是-O - ， - NH-或式（II）[其中R 5是低级烷基等]; 和其药学上可接受的盐，其可用作药物; 所述脂肪酸衍生物或其盐的制备方法; 包含所述脂肪酸衍生物或其药学上可接受的盐的药物组合物; 等等

4. 发明申请

WO1996001825A1 HETEROBICYCLIC DERIVATIVES 审中-公开
标题翻译：杂环衍生物
公开(公告)号：WO1996001825A1
公开(公告)日：1996-01-25
申请号：PCT/JP1995001366
申请日：1995-07-10
申请人： FUJISAWA PHARMACEUTICAL CO., LTD. , HEMMI, Mitsue +hf , SHIMAZAKI, Norihiko , WATANABE, Shinya , SAWADA, Akihiko
发明人： FUJISAWA PHARMACEUTICAL CO., LTD. , HEMMI, Mitsue +hf , HEMMI, Keiji +di
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： Heterobicyclic derivatives of formula (I) wherein R is aryl which may have suitable substituent(s), ar(lower)alkyl which may have suitable substituent(s), halo(lower)alkyl, protected carboxy(lower)alkyl, acyl(lower)alkyl, heterocyclic group or heterocyclic(lower)alkyl which may have suitable substituent(s), R is aryl which may have suitable substituent(s) or heterocyclic group, and R is hydrogen, lower alkoxy or arylthio, and a pharmaceutically acceptable salt thereof which are useful as PDE IV and TNF inhibitors.
摘要翻译：式（I）的杂双环衍生物，其中R 1为可具有合适取代基的芳基，可具有合适取代基的芳基（低级）烷基，卤代（低级）烷基，被保护的羧基（低级）烷基，可以具有合适取代基的酰基（低级）烷基，杂环基或杂环（低级）烷基，R 2是可具有合适取代基或杂环基的芳基，R 3是氢，低级烷氧基或芳硫基，及其药学上可接受的盐，可用作PDE IV和TNF抑制剂。

5. 发明申请

WO1997014681A1 HETEROCYCLIC COMPOUNDS AS H+-ATPASES 审中-公开
标题翻译：杂环化合物作为H + -ATPASES
公开(公告)号：WO1997014681A1
公开(公告)日：1997-04-24
申请号：PCT/JP1996002981
申请日：1996-10-15
申请人： FUJISAWA PHARMACEUTICAL CO., LTD. , OKU, Teruo , KAWAI, Yoshio , SATOH, Shigeki , YAMAZAKI, Hitoshi , KAYAKIRI, Natsuko , URANO, Yasuharu , YOSHIHARA, Kousei , YOSHIDA, Noriko
发明人： FUJISAWA PHARMACEUTICAL CO., LTD.
IPC分类号： C07D215/40
CPC分类号： C07D231/12 , C07D215/40 , C07D215/42 , C07D215/44 , C07D215/46 , C07D215/48 , C07D215/54 , C07D215/56 , C07D215/60 , C07D221/12 , C07D233/56 , C07D237/28 , C07D239/74 , C07D239/88 , C07D241/42 , C07D249/08 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D471/04 , C07D495/04 , C07D513/14 , C07F7/0812 , C07F7/1804
摘要： This invention relates to a compound of formula (I), wherein R is a heterocyclic group or aryl, each of which may be substituted with suitable substituent(s), A is -CONH- or -NHCO-, n is an integer of 0 or 1, and (II) is a group of formula (III), in which R , R and R are each hydrogen, halogen, etc., R is hydrogen or lower alkyl, R is hydrogen, halogen, lower alkyl, etc., and R is hydrogen, substituted lower alkyl, a heterocyclic group, etc., and pharmaceutically acceptable salt thereof, to processes for preparation thereof, to a pharmaceutical composition comprising the same, and to a method for the prevention and/or the treatment of bone diseases caused by abnormal bone metabolism in human beings or animals.
摘要翻译：本发明涉及式（I）化合物，其中R 1是杂环基或芳基，其各自可被合适的取代基取代，A是-CONH-或-NHCO-，n是 0或1的整数，和（II）是式（III）的基团，其中R 2，R 3和R 4各自为氢，卤素等，R 5为氢或低级烷基，R 6是氢，卤素，低级烷基等，R 7是氢，取代的低级烷基，杂环基等及其药学上可接受的盐，其制备方法，涉及包含其的药物组合物，以及用于预防和/或治疗由人或动物异常骨代谢引起的骨疾病的方法。

6. 发明申请

WO1992017456A1 AMINO ACID DERIVATIVE AND SALT THEREOF 审中-公开
标题翻译：氨基酸衍生物及其盐
公开(公告)号：WO1992017456A1
公开(公告)日：1992-10-15
申请号：PCT/JP1992000349
申请日：1992-03-21
申请人： FUJISAWA PHARMACEUTICAL CO., LTD. , HEMMI, Keiji , NEYA, Masahiro , WATANABE, Shinya , HASHIMOTO, Masashi
发明人： FUJISAWA PHARMACEUTICAL CO., LTD.
IPC分类号： C07D233/64
CPC分类号： C07D233/64 , A61K38/00 , C07K5/06078
摘要： A novel amino acid derivative having a renin inhibitory activity, represented by general formula (A), a salt thereof, and a process for producing the same.
摘要翻译：具有由通式（A）表示的肾素抑制活性的新型氨基酸衍生物及其盐及其制备方法。

7. 发明申请

WO1993010144A1 NEW ENDOTHELIN ANTAGONISTS AND THEIR PREPARATION 审中-公开
标题翻译：新的内皮素拮抗剂及其制备
公开(公告)号：WO1993010144A1
公开(公告)日：1993-05-27
申请号：PCT/JP1992001405
申请日：1992-10-30
申请人： FUJISAWA PHARMACEUTICAL CO., LTD. , HEMMI, Keiji , NEYA, Masahiro , FUKAMI, Naoki , HASHIMOTO, Masashi , TANAKA, Hirokazu , KAYAKIRI, Natsuko
发明人： FUJISAWA PHARMACEUTICAL CO., LTD.
IPC分类号： C07K05/06
CPC分类号： C07K5/06156 , A61K38/00 , C07K5/0808 , C07K5/1005 , C07K5/1024
摘要： A compound of the formula (I), where R -R and A have the meanings disclosed in the description; or a pharmaceutically acceptable salt thereof; display endothelm antagonistic activity.
摘要翻译：式（I）的化合物，其中R 1 -R 5和A具有说明书中公开的含义; 或其药学上可接受的盐; 显示内皮拮抗活性。

8. 发明申请

WO1998027069A1 PIPERAZINE COMPOUNDS AS INHIBITORS OF MMP OR TNF 审中-公开
标题翻译：作为MMP或TNF的抑制剂的哌嗪化合物
公开(公告)号：WO1998027069A1
公开(公告)日：1998-06-25
申请号：PCT/JP1997004613
申请日：1997-12-15
申请人： FUJISAWA PHARMACEUTICAL CO., LTD. , NEYA, Masahiro , YAMAZAKI, Hitoshi , KAYAKIRI, Natsuko , SATO, Kentaro , OKU, Teruo
发明人： FUJISAWA PHARMACEUTICAL CO., LTD.
IPC分类号： C07D241/04
CPC分类号： C07D405/12 , C07D241/04 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/14 , C07D417/12 , C07D417/14
摘要： A compound of formula (I) wherein A is a sulfonyl or a carbonyl; R is an optionally substituted aryl, an optionally substituted heterocyclic group, an optionally substituted lower alkyl or an optionally substituted lower alkenyl; R is a hydrogen, an optionally substituted lower alkyl, an optionally substituted aryl or an optionally substituted heterocyclic group; R is an optionally substituted lower alkyl, an optionally substituted lower alkoxy, an optionally substituted aryloxy, an optionally substitued lower alkenyl, an optionally substituted aryl, an optionally substituted heterocyclic group or an optionally substitued amino; R is a hydrogen, an optionally substituted lower alkyl, an optionally substituted aryl or an optionally substituted heterocyclic group; R is a hydrogen, an optionally substituted lower alkyl, an optionally substituted aryl or an optionally substituted heterocyclic group; and R is a hydroxy or a protected hydroxy, and a pharmaceutically acceptable salt thereof. The compound of the present invention is useful as a medicament for prophylactic and therapeutic treatment of MMP- or TNF alpha -mediated diseases.
摘要翻译：式（I）的化合物，其中A是磺酰基或羰基; R 1是任选取代的芳基，任选取代的杂环基，任选取代的低级烷基或任选取代的低级烯基; R 2是氢，任选取代的低级烷基，任选取代的芳基或任选取代的杂环基; R 3是任选取代的低级烷基，任选取代的低级烷氧基，任选取代的芳氧基，任选取代的低级烯基，任选取代的芳基，任选取代的杂环基或任选取代的氨基; R 4是氢，任选取代的低级烷基，任选取代的芳基或任选取代的杂环基; R 5是氢，任选取代的低级烷基，任选取代的芳基或任选取代的杂环基; R 10为羟基或保护的羟基及其药学上可接受的盐。本发明的化合物可用作用于预防和治疗MMP或TNFα介导的疾病的药物。

9. 发明申请

WO1995000537A1 NEW COMPOUND AND ITS PREPARATION 审中-公开
标题翻译：新化合物及其制备
公开(公告)号：WO1995000537A1
公开(公告)日：1995-01-05
申请号：PCT/JP1994001042
申请日：1994-06-28
申请人： FUJISAWA PHARMACEUTICAL CO., LTD. , HEMMI, Keiji , NEYA, Masahiro , FUKAMI, Naoki , KAYAKIRI, Natsuko , TANAKA, Hirokazu
发明人： FUJISAWA PHARMACEUTICAL CO., LTD.
IPC分类号： C07K05/08
CPC分类号： C07K5/0808 , A61K38/00 , C07K5/0207 , C07K5/0827 , Y02P20/55
摘要： A compound of formula (1) in which R is acyl, R is lower alkyl, R is optionally substituted ar(lower)alkyl or optionally substituted heterocyclic-(lower)alkyl, R is lower alkyl or lower alkylthio(lower)alkyl, R is carboxy or protected carboxy, A is lower alkylene, Z is a group of formula (2) wherein R is hydrogen, lower alkyl, common amino-protective group or optionally substituted ar(lower)alkyl, R is hydrogen, lower alkyl, optionally substituted ar(lower)alkyl, optionally substituted heterocyclic-(lower)alkyl, optionally substituted cyclo(lower)alkyl(lower)alkyl, common amino-protective group, amino(or protected amino)(lower)alkyl, optionally substituted heterocyclic-carbonyl or cyclo(lower)alkyl, and R is optionally substituted heterocyclic(lower)alkyl, and m is an integer of 0 to 2, or pharmaceutically acceptable salts thereof, useful as endothelin antagonist.
摘要翻译：式（1）的化合物，其中R 4是酰基，R 5是低级烷基，R 6是任选取代的芳（低级）烷基或任选取代的杂环 - （低级）烷基，R 7是是低级烷基或低级烷硫基（低级）烷基，R 8是羧基或保护的羧基，A是低级亚烷基，Z是式（2）的基团，其中R 1是氢，低级烷基，常见的氨基保护基基团或任选取代的芳（低级）烷基，R 2是氢，低级烷基，任选取代的芳（低级）烷基，任选取代的杂环 - （低级）烷基，任选取代的环（低级）烷基氨基（或保护的氨基）（低级）烷基，任选取代的杂环 - 羰基或环（低级）烷基，R 3是任选取代的杂环（低级）烷基，m是0至 2或其药学上可接受的盐，其可用作内皮素拮抗剂。

10. 发明申请

WO1998027108A2 NEW AMIDE COMPOUNDS 审中-公开
标题翻译：新型化合物
公开(公告)号：WO1998027108A2
公开(公告)日：1998-06-25
申请号：PCT/JP1997004243
申请日：1997-11-20
申请人： FUJISAWA PHARMACEUTICAL CO., LTD. , YATABE, Yoshiko +hf , ITOH, Yoshikuni , INOUE, Takayuki , HAMASHIMA, Hitoshi , SHIMA, Ichiro , OHNE, Kazuhiko , YOSHIHARA, Kousei , OKU, Teruo
发明人： FUJISAWA PHARMACEUTICAL CO., LTD. , YATABE, Yoshiko +hf , YATABE, Takumi +di
IPC分类号： C07K05/00
CPC分类号： C07D233/64 , C07D231/12 , C07D233/56 , C07D233/90 , C07D249/08 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D417/12
摘要： A compound of formula (I) wherein each symbol is as defined in the specification, and pharmaceutically acceptable salts thereof. The compound (I) of the present invention and pharmaceutically acceptable salts thereof possess a strong inhibitory activity on the production of nitric oxide (NO), and are useful for prevention and/or treatment of NO-mediated diseases such as adult respiratory distress syndrome, cardiovascular ischemia, myocarditis, heart failure, synovitis, shock, diabetes, diabetic nephropathy, diabetic retinopathy, diabetic neuropathy, glomerulonephritis, peptic ulcer, inflammatory bowel disease, cerebral infarction, cerebral ischemia, cerebral hemorrhage, migraine, rheumatoid arthritis, gout, neuritis, postherpetic neuralgia, osteoarthritis, osteoporosis, systemic lupus erythematosus, rejection by organ transplantation, asthma, metastasis, Alzheimer's disease, arthritis, CNS disorders, dermatitis, hepatitis, liver cirrhosis, multiple sclerosis, pancreatitis, atherosclerosis, and the like in human being and animals.
摘要翻译：式（I）的化合物，其中每个符号如说明书中所定义，及其药学上可接受的盐。本发明的化合物（I）及其药学上可接受的盐对一氧化氮（NO）的产生具有很强的抑制活性，可用于预防和/或治疗NO介导的疾病如成人呼吸窘迫综合征，心血管缺血，心肌炎，心力衰竭，滑膜炎，休克，糖尿病，糖尿病肾病，糖尿病性视网膜病变，糖尿病性神经病，肾小球性肾炎，消化性溃疡，炎性肠病，脑梗塞，脑缺血，脑出血，偏头痛，类风湿性关节炎，痛风，神经炎，带状疱疹神经痛，骨关节炎，骨质疏松症，系统性红斑狼疮，器官移植排斥反应，哮喘，转移，阿尔茨海默氏病，关节炎，中枢神经系统疾病，皮炎，肝炎，肝硬化，多发性硬化，胰腺炎，动脉粥样硬化等。

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