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1. 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。

2. 发明申请

WO1996034866A1 IMIDAZO 1,2-A PYRIDINE AND IMIDAZO 1,2-A PYRIDEZINE DERIVATIVES AND THEIR USE AS BONE RESORPTION INHIBITORS 审中-公开
标题翻译：咪唑烷1,2-A吡啶和咪唑烷1,2-A吡啶衍生物及其作为骨质还原抑制剂的用途
公开(公告)号：WO1996034866A1
公开(公告)日：1996-11-07
申请号：PCT/JP1996001103
申请日：1996-04-23
申请人： FUJISAWA PHARMACEUTICAL CO., LTD. , KAWAI, Yoshio , SATOH, Shigeki , YAMAZAKI, Hitoshi , KAYAKIRI, Natsuko , YOSHIHARA, Kousei , OKU, Teruo
发明人： FUJISAWA PHARMACEUTICAL CO., LTD.
IPC分类号： C07D471/04
CPC分类号： C07D407/04 , C07D471/04
摘要： This invention relates to a novel imidazopyridine compound represented by formula (I), wherein X is vinylene, or a group of the formula (a), Y is heterocyclic group which may have one or more suitable substituent(s), or aryl which may have one or more suitable substituent(s), Q is CH or N, and 1 is an integer of 0 or 1, which are the inhibitors of bone resorption and bone metabolism, to processes for preparation thereof, to a pharmaceutical composition comprising the same and to a method for the treatment of diseases caused by abnormal bone metabolism in human being or an animal.
摘要翻译：本发明涉及由式（I）表示的新的咪唑并吡啶化合物，其中X是亚乙烯基，或式（a）的基团，Y是可以具有一个或多个合适取代基的杂环基或可以具有一个或多个合适取代基的芳基，具有一个或多个合适的取代基，Q是CH或N，1是0或1的整数，其是骨吸收和骨代谢的抑制剂及其制备方法，包含其的药物组合物以及用于治疗由人或动物异常骨代谢引起的疾病的方法。

3. 发明申请

WO1997010219A1 BENZIMIDAZOLE DERIVATIVES AND THEIR USE IN THE PREVENTION AND/OR THE TREATMENT OF BONE DISEASES 审中-公开
标题翻译：苯并咪唑衍生物及其在预防和/或治疗骨质疏松症中的应用
公开(公告)号：WO1997010219A1
公开(公告)日：1997-03-20
申请号：PCT/JP1996002530
申请日：1996-09-05
申请人： FUJISAWA PHARMACEUTICAL CO., LTD. , OKU, Teruo , KAWAI, Yoshio , YATABE, Takumi , SATO, Shigeki , YAMAZAKI, Hitoshi , KAYAKIRI, Natsuko , YOSHIHARA, Kousei
发明人： FUJISAWA PHARMACEUTICAL CO., LTD.
IPC分类号： C07D235/06
CPC分类号： C07D235/24 , C07D231/12 , C07D233/56 , C07D235/08 , C07D235/10 , C07D235/12 , C07D235/26 , C07D235/28 , C07D235/30 , C07D249/08 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/06 , C07D405/12 , C07D409/06 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/12 , C07D471/04 , C07D487/04 , C07D513/04
摘要： The present invention relates to a new heterocyclic compound of formula (I), wherein R is acyl, lower alkenyl or lower alkyl optionally substituted with aryl, a heterocyclic group, etc., R is hydrogen, lower alkyl, hydroxy(lower)alkyl, halo(lower)alkyl, etc., R is hydrogen or halogen, R is a heterocyclic group or aryl, each of which may be substituted with suitable substituent(s), and A is (a) or (b), (wherein R and R are each hydrogen, lower alkyl or substituted lower alkyl), and pharmaceutically acceptable salts thereof which are the inhibitors of bone resorption and bone metabolism, to processes for preparation thereof, to a pharmaceutical composition comprising the same and to a method for the treatment of diseases caused by abnormal bone metabolism in human being or an animal.
摘要翻译：本发明涉及新的式（I）杂环化合物，其中R 1为酰基，低级烯基或任选被芳基，杂环基等取代的低级烷基，R 2为氢，低级烷基，羟基（低级）烷基，卤代（低级）烷基等，R 3是氢或卤素，R 4是杂环基或芳基，其各自可以被合适的取代基取代，并且A 是（a）或（b），（其中R 9和R 10各自为氢，低级烷基或取代的低级烷基）及其药学上可接受的盐，其为骨吸收和骨代谢的抑制剂，用于制备其包含该药物组合物的药物组合物和用于治疗由人或动物异常骨代谢引起的疾病的方法。

4. 发明申请

WO1995029907A1 BENZOFURAN DERIVATIVES USEFUL AS INHIBITORS OF BONE RESORPTION 审中-公开
标题翻译： BENZOFURAN衍生物作为骨质疏松症的抑制剂有用
公开(公告)号：WO1995029907A1
公开(公告)日：1995-11-09
申请号：PCT/JP1995000787
申请日：1995-04-21
申请人： FUJISAWA PHARMACEUTICAL CO., LTD. , KAWAI, Yoshio , YAMAZAKI, Hitoshi , KAYAKIRI, Natsuko , YOSHIHARA, Kousei , YATABE, Takumi , OKU, Teruo
发明人： FUJISAWA PHARMACEUTICAL CO., LTD.
IPC分类号： C07D307/79
CPC分类号： C07D307/79 , C07C233/76 , C07C2603/30 , C07D209/94 , C07D223/32 , C07D231/12 , C07D233/56 , C07D249/08 , C07D307/80 , C07D307/81 , C07D307/82 , C07D307/91 , C07D405/04 , C07D405/12 , C07D407/12 , C07D409/12 , C07D413/12 , C07D417/04 , C07D417/12 , C07D495/04 , C07F7/1804 , C07F9/65517
摘要： This invention relates to a novel heterocyclic compound represented by formula (I), wherein X is O or S, Y is vinylene, or a group of formula: -NHCO-, -NHSO2-, -OCO-, -OCH2-, -NHCOCO-, -NHCOCH=CH-, -NHCOCH2-, -NHCONH- or (a) (wherein R is lower alkyl), Z is heterocyclic group which may have one or more suitable substituent(s), or aryl which may have one or more suitable substituent(s), 1 = 0, 1 and the other symbols are as defined in the specification and a pharmaceutically acceptable salt thereof which are the inhibitors of bone resorption and bone metabolism, to processes for preparation thereof, to a pharmaceutical composition comprising the same and to a method for the treatment of diseases caused by abnormal bone metabolism in human being or an animal.
摘要翻译：本发明涉及由式（I）表示的新型杂环化合物，其中X为O或S，Y为亚乙烯基，或下列基团：-NHCO-，-NHSO 2 - ， - OCO - ， - OCH 2 - ， - NHCOCO - ， - NHCOCH = CH - ， - NHCOCH 2 - ， - NHCONH-或（a）（其中R 6为低级烷基），Z为可具有一个或多个合适取代基的杂环基或可以具有一个或多个合适的取代基，1 = 0,1，其它符号如本说明书中所定义，以及其药学上可接受的盐，其是骨吸收和骨代谢的抑制剂，其制备方法，包含其的药物组合物和用于治疗由人或动物中的异常骨代谢引起的疾病的方法。

5. 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。

6. 发明申请

WO1995003053A1 OXOPHTHALAZINES FOR TREATING CACHEXIA 审中-公开
标题翻译：用于治疗CACHEXIA的OXOPHTHALAZINES
公开(公告)号：WO1995003053A1
公开(公告)日：1995-02-02
申请号：PCT/JP1994001179
申请日：1994-07-18
申请人： FUJISAWA PHARMACEUTICAL CO., LTD. , SAKAI, Fumihiko , YAMAMOTO, Nobuchika , NAKAHARA, Kunio , YAMAZAKI, Harumi , NOTSU, Yoshitada , KAWAI, Yoshio , YAMAZAKI, Hitoshi , ABE, Yoshito , OKU, Teruo
发明人： FUJISAWA PHARMACEUTICAL CO., LTD.
IPC分类号： A61K31/495
CPC分类号： A61K31/50
摘要： This invention relates to a new use of the oxophthalazine compounds or pharmaceutically acceptable salts thereof as the prophylactic and/or therapeutic treatment of cachexia and the like, wherein oxophthalazine compounds can be represented by general formula (I), wherein R is ar(lower)alkyl which may have one or more suitable substituent(s), and R is carboxy(lower)alkyl or protected carboxy(lower)alkyl.
摘要翻译：本发明涉及氧酞嗪化合物或其药学上可接受的盐作为恶病质等的预防和/或治疗性治疗的新用途，其中氧酞嗪化合物可以由通式（I）表示，其中R 1为芳（低级）烷基，其可以具有一个或多个合适的取代基，R 2是羧基（低级）烷基或保护的羧基（低级）烷基。

7. 发明申请

WO1994019350A1 PYRAZOLITRIAZINES WITH INTERLEUKIN-1 AND TUMOUR NECROSIS FACTOR INHIBITORY ACTIVITY 审中-公开
标题翻译：具有白细胞介素-1和肿瘤坏死因子抑制活性的吡格列酮
公开(公告)号：WO1994019350A1
公开(公告)日：1994-09-01
申请号：PCT/JP1994000213
申请日：1994-02-09
申请人： FUJISAWA PHARMACEUTICAL CO., LTD. , KAWAI, Yoshio , YAMAZAKI, Hitoshi , TANAKA, Hirokazu , OKU, Teruo
发明人： FUJISAWA PHARMACEUTICAL CO., LTD.
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： New heterocyclic derivatives of formula (I) wherein R is aryl which may have suitable substituent(s) or heterocyclic group which may have suitable substituent(s), R is aryl which may have suitable substituent(s) or heterocyclic group which may have suitable substituent(s), R is hydrogen or acyl, R is hydrogen, lower alkyl, cyclo(lower)alkyl, cyclo(lower)alkyl-(lower)alkyl, carboxy(lower)alkyl, protected carboxy(lower)alkyl, ar(lower)alkyl which may have suitable substituent(s), ar(lower)alkenyl, bridged tricyclicalkyl, heterocyclic group which may have suitable substituent(s), acyl, or a group of formula (b) (in which A is lower alkylene), and R is hydrogen or lower alkyl, and a pharmaceutically acceptable salt thereof which are useful as interleukin-1 and tumor necrosis inhibitors.
摘要翻译：式（I）的新杂环衍生物，其中R 1为可具有合适取代基的芳基或可具有合适取代基的杂环基，R 2为可具有合适取代基的芳基或可以具有合适取代基的杂环基，R 3是氢或酰基，R 4是氢，低级烷基，环（低级）烷基，环（低级）烷基 - （低级）烷基，羧基）烷基，被保护的羧基（低级）烷基，可具有合适取代基的芳（低级）烷基，芳（低级）烯基，桥连三环烷基，可具有合适取代基的杂环基，酰基或一式（b）（其中A为低级亚烷基），R 5为氢或低级烷基，及其药学上可接受的盐，其可用作白介素-1和肿瘤坏死抑制剂。

8. 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。

9. 发明申请

WO1996013485A1 PYRIDOPYRIMIDONES, QUINOLINES AND FUSED N-HERETOCYCLES AS BRADYKININ ANTAGONISTS 审中-公开
标题翻译：吡咯烷酮，喹啉和熔融N-酰基转移酶作为BRADYKININ拮抗剂
公开(公告)号：WO1996013485A1
公开(公告)日：1996-05-09
申请号：PCT/JP1995002192
申请日：1995-10-25
申请人： FUJISAWA PHARMACEUTICAL CO., LTD. , OKU, Teruo , KAYAKIRI, Hiroshi , SATOH, Shigeki , ABE, Yoshito , SAWADA, Yuki , INOUE, Takayuki , TANAKA, Hirokazu
发明人： FUJISAWA PHARMACEUTICAL CO., LTD.
IPC分类号： C07D215/16
CPC分类号： C07D401/12 , C07D215/26 , C07D215/40 , C07D215/42 , C07D215/48 , C07D241/40 , C07D401/14 , C07D403/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04
摘要： The invention relates to Pyridopyrimidones, Quinolines and fused N-heterocyclic compounds of formula (I) wherein Z is a group of the formula (a) or (b) in which X is N or C-R , X is N or C-R , X is N or C-R , R is lower alkyl, R is hydrogen, lower alkyl, etc., R is hydrogen or lower alkyl, R is halogen, etc., R is halogen, etc., R is a group of formula (c), etc., A is lower alkylene, and Y is O, etc., and pharmaceutically acceptable salts thereof, to processes for preparation thereof, to a pharmaceutical composition comprising the same, and to methods of using the same therapeutically in the prevention and/or the treatment of bradykinin or its analogues mediated diseases in human being or animals.
摘要翻译：本发明涉及式（I）的吡啶并嘧啶酮，喹啉和稠合的N-杂环化合物，其中Z是式（a）或（b）的基团，其中X 1是N或CR 1，X 2 >为N或CR 9，X 3为N或CR 2，R 1为低级烷基，R 2为氢，低级烷基等，R 9为氢或低级烷基，R 3为卤素等，R 4为卤素等，R 5为式（c）等基团，A为低级亚烷基，Y为O等。及其药学上可接受的盐，其制备方法，涉及含有该组合物的药物组合物，以及在预防和/或治疗缓激肽或其类似物介导的人或动物疾病中的治疗方法。

10. 发明申请

WO1993016071A1 HETEROCYCLIC DERIVATIVES AS ANGIOTENSIN II ANTAGONISTS 审中-公开
标题翻译：杂环衍生物作为ANGIOTENSIN II拮抗剂
公开(公告)号：WO1993016071A1
公开(公告)日：1993-08-19
申请号：PCT/JP1993000133
申请日：1993-02-03
申请人： FUJISAWA PHARMACEUTICAL CO., LTD. , OKU, Teruo , SETOI, Hiroyuki , KAYAKIRI, Hiroshi , SATOH, Shigeki , INOUE, Takayuki , SAWADA, Yuki , KURODA, Akio , TANAKA, Hirokazu
发明人： FUJISAWA PHARMACEUTICAL CO., LTD.
IPC分类号： C07D401/14
CPC分类号： C07D401/14 , C07D471/04 , Y02P20/55
摘要： The object compound of formula (I) wherein R is quinolyl or naphthyridinyl which may have suitable substituent(s), R is hydrogen, halogen, nitro, lower alkyl, lower alkoxy, amino or acylamino, R , R and R are each hydrogen, halogen, nitro, cyano, lower alkyl, lower alkenyl, lower alkylthio, mono or di or trihalo(lower)alkyl, oxo(lower)alkyl, hydroxy(lower)alkyl or optionally esterified carboxy; or R and R are linked together to form 1,3-butadienylene; R is hydrogen or imino-protective group; A is lower alkylene; Q is CH or N; X is N or CH; Y is NH, O or S; and n is 0 or 1; and pharmaceutically acceptable salts thereof which are useful as a medicament.
摘要翻译：式（I）的目标化合物，其中R是可具有合适取代基的喹啉基或萘啶基，R 1是氢，卤素，硝基，低级烷基，低级烷氧基，氨基或酰氨基，R 2，R 低级烷基，低级烷基，低级烷硫基，一或二或三卤代（低级）烷基，氧代（低级）烷基，羟基（低级）烷基或任选地酯化羧基; 或R 2和R 3连接在一起形成1,3-丁二烯; R 5是氢或亚氨基保护基; A是低级亚烷基; Q是CH或N; X为N或CH; Y是NH，O或S; 并且n为0或1; 和其药学上可接受的盐，其可用作药物。

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