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1. 发明申请

WO1991015487A1 NOVEL 4H-3,1-BENZOXAZIN-4-ONE DERIVATIVE 审中-公开
标题翻译：新的4H-3,1-苯并恶嗪-4-酮衍生物
公开(公告)号：WO1991015487A1
公开(公告)日：1991-10-17
申请号：PCT/JP1991000386
申请日：1991-03-26
申请人： JAPAN TOBACCO INC. , KOBAYASHI, Koji; , OZAWA, Koichi; , SASABUCHI, Masashi; , UCHIDA, Itsuo;
发明人： JAPAN TOBACCO INC.
IPC分类号： C07D413/12
CPC分类号： C07D413/10 , A61K38/00 , C07D207/16 , C07K5/06052 , C07K5/06078 , C07K5/06165 , C07K5/0806 , C07K5/0812
摘要： A 4H-3,1-benzoxazin-4-one derivative of general formula (I), which has a potent serine protease inhibitory action and is useful as the active ingredient of drugs for preventing and treating pneumonia, pulmonary emphysema, pulmonary fibrosis, bronchitis, arthritis, pancreatitis, nephritis, shock, sepsis, arteriosclerosis, etc.; wherein R1 represents lower alkyl; R2 represents lower alkyl, lower alkylthioalkyl or lower alkanesulfinylalkyl; R3 represents hydrogen, hydroxyl, lower alkoxy or lower acyloxy; X represents a residue of an amino acid selected from the group consisting of alanine, valine and phenyl-alanine; n is an integer of 0, 1 or 2; and Y represents a substituent selected from the group consisting of C¿2? to C6 alkanoyl optionally substituted with phenyl, benzyloxycarbonyl, lower alkoxycarbonyl, cinnamoyl and methoxysuccinoyl.

2. 发明申请

WO1993011121A1 BENZOXAZINONE DERIVATIVE 审中-公开
标题翻译：苯并咪唑衍生物
公开(公告)号：WO1993011121A1
公开(公告)日：1993-06-10
申请号：PCT/JP1992001550
申请日：1992-11-27
申请人： JAPAN TOBACCO INC. , KOBAYASHI, Koji; , MANABE, Shunichi; , WATANABE, Yoshihiro; , HAYAKAWA, Kazuhide; , UCHIDA, Itsuo;
发明人： JAPAN TOBACCO INC.
IPC分类号： C07D265/22
CPC分类号： C07D265/22 , C07D413/10 , C07D413/14
摘要： A benzoxazinone derivative represented by general formula (I) or a pharmaceutically acceptable acid addition salt thereof, and an anti-inflammatory, a neutrophil infiltration inhibitor and a serine protease inhibitor each containing the derivative as an active ingredient, wherein R, R?1, R2 and R3¿ may be the same or different from one another and each represents hydrogen or lower alkyl; A represents optionally halogenated phenyl, heterocycle or adamantyl; B represents hydrogen or optionally halogenated phenyl or heterocycle; U represents =CH-, =C= or =N-; V represents -O-, -CH¿2?-, =N-, -NH-, -CH= or a single bond; X represents -O-, =CH-, -CH2- or a single bond; Y represents -CH2-, -NH-, -O- or a single bond; Z represents -CO- or -CH2-; and l represents an integer of 0 to 3. This compound has excellent activities of inhibiting serine protease, neutrotaxis, and infiltration of neutrophils into carragheenin-induced pneumocephalus.

3. 发明申请

WO1993013065A1 PROLINE DERIVATIVE 审中-公开
公开(公告)号：WO1993013065A1
公开(公告)日：1993-07-08
申请号：PCT/JP1992001711
申请日：1992-12-25
申请人： JAPAN TOBACCO INC. , KOBAYASHI, Koji; , ABE, Hiroyuki; , TOIDE, Katsuo; , UCHIDA, Itsuo;
发明人： JAPAN TOBACCO INC.
IPC分类号： C07D207/08
CPC分类号： C07D207/08 , C07D207/16 , C07D401/14 , C07D403/12 , C07D403/14 , C07D407/14 , C07D417/06 , C07D417/14 , Y02P20/55
摘要： A proline derivative represented by general formula (I), wherein A represents -O-, -CHR - or -NR - wherein R represents hydrogen or heterocycle and R represents lower alkoxycarbonyl-lower alkyl; W represents phenyl which may be substituted by halogen, lower alkyl or lower alkoxy, adamantyl, lower alkyl or heterocycle; U represents -O-, -S-, -NH- or -CHR - wherein R represents hydrogen or lower alkoxycarbonyl; X represents -S-, -SO-, -SO2-, -O- or -NH-; D represents benzene or heterocycle; and Y and Z may be the same or different from each other and represent each hydrogen, halogen, optionally fluorinated lower alkyl, amino, nitro, hydroxy or lower alkoxy. This derivative has a specifically potent inhibitory activity against prolyl endopeptidase and inhibits the decomposition and inactivation of TRH, substance P, neurotensin, vasopressin, etc. Therefore, it can be used for preventing and/or treating dementia including Alzheimer's disease and amnesia.
摘要翻译：由通式（I）表示的脯氨酸衍生物，其中A表示-O-，-CHR 1 - 或-NR 2 - ，其中R 1表示氢或杂环，R 2表示低级烷氧基羰基 - 低级烷基; W表示可被卤素，低级烷基或低级烷氧基，金刚烷基，低级烷基或杂环取代的苯基; U表示-O - ， - S - ， - NH-或-CHR 5 - ，其中R 5表示氢或低级烷氧基羰基; X表示-S - ， - SO - ， - SO 2 - ， - O-或-NH-; D表示苯或杂环; Y和Z可以相同或不同，表示各个氢，卤素，任选氟化的低级烷基，氨基，硝基，羟基或低级烷氧基。该衍生物对脯氨酰内肽酶具有特异性的抑制活性，抑制TRH，物质P，神经丝氨酸，加压素等的分解和失活。因此，它可用于预防和/或治疗痴呆，包括阿尔茨海默病和遗忘症。

4. 发明申请

WO1994012474A1 COMPOUND WITH PROLYL ENDOPEPTIDASE INHIBITOR ACTIVITY AND PHARMACEUTICAL USE THEREOF 审中-公开
标题翻译：具有内切肽酶抑制剂活性的化合物及其药物用途
公开(公告)号：WO1994012474A1
公开(公告)日：1994-06-09
申请号：PCT/JP1993001687
申请日：1993-11-17
申请人： JAPAN TOBACCO INC. , YOSHITOMI PHARMACEUTICAL INDUSTRIES, LTD. , KOBAYASHI, Koji; , AKAMATSU, Minoru; , YATA, Shinji; , ABE, Hiroyuki; , TOIDE, Katsuo; , KOGAYU, Motohiro; , UCHIDA, Itsuo;
发明人： JAPAN TOBACCO INC. , YOSHITOMI PHARMACEUTICAL INDUSTRIES, LTD.
IPC分类号： C07D207/16
CPC分类号： C07D417/06 , C07D207/16 , C07D277/06
摘要： A compound represented by general formula (I) or a pharmaceutically acceptable salt thereof, wherein: R represents hydrogen or acyl; U represents -O-, -CHR - or -NR -, wherein R represents hydrogen or heterocycle, and R represents hydrogen or lower alkyl substituted by lower alkoxycarbonyl; V represents -O-, -S-, -CHR - or -NR -, wherein R represents hydrogen or lower alkoxycarbonyl, and R represents hydrogen, lower alkyl or acyl; W represents methyl, heterocycle or optionally substituted phenyl; X and Y, which may be the same or different from each other, represent each -CH2- or -S-; m represents an integer of 0 to 6; and n represents an integer of 1 to 4. The compound has a specifically potent inhibitory activity against prolyl endopeptidase and suppresses the decomposition and deactivation of TRH, substance P, neurotensin, vasopressin, and so forth. Hence it can be used for preventing and/or treating dementia and amnesia including Alzheimer's disease.
摘要翻译：由通式（I）表示的化合物或其药学上可接受的盐，其中：R表示氢或酰基; U表示-O-，-CHR 1 - 或-NR 2 - ，其中R 1表示氢或杂环，R 2表示氢或被低级烷氧基羰基取代的低级烷基; V表示-O - ， - S - ， - CH 3 - 或-NR 4 - ，其中R 3表示氢或低级烷氧基羰基，R 4表示氢，低级烷基或酰基。 W代表甲基，杂环或任选取代的苯基; X和Y可以相同或不同，表示每个-CH 2 - 或-S-; m表示0〜6的整数， n表示1〜4的整数。该化合物对脯氨酰内肽酶具有特异的抑制活性，抑制TRH，物质P，神经降压素，加压素等的分解和失活。因此，它可用于预防和/或治疗包括阿尔茨海默氏病在内的痴呆和遗忘。

5. 发明申请

WO1992018488A1 NOVEL OXAZINONE DERIVATIVE 审中-公开
标题翻译：新奥西汀酮衍生物
公开(公告)号：WO1992018488A1
公开(公告)日：1992-10-29
申请号：PCT/JP1992000444
申请日：1992-04-09
申请人： JAPAN TOBACCO INC. , KOBAYASHI, Koji; , MANABE, Shunichi; , WATANABE, Yoshihiro; , HAYAKAWA, Kazuhide; , UCHIDA, Itsuo;
发明人： JAPAN TOBACCO INC.
IPC分类号： C07D265/22
CPC分类号： C07D265/22 , C07D413/10 , C07D417/12 , C07D471/04
摘要： A novel oxazinone derivative represented by general formula (I), which is useful as an antiinflammatory agent, a neutrophile infiltration inhibitor and a serine protease inhibitor, and a pharmaceutically acceptable acid addition salt thereof. In formula (I) A represents the group (a) (wherein W represents a single bond, -O-, -S-, -CH=CH- or -NR -; V represents =CR - or =N-; and D represents a 5-to 7-membered carbocyclic or heterocyclic ring); X represents a single bond, -O-, -S-, -CO- or -NR -; Y represents a single bond, -O-, -CH=CH- or -NR -; Z represents -CH2- or -CO-; I represents an integer of 0 to 4; and R, R to R represent each hydrogen, lower alkyl, etc.
摘要翻译：由通式（I）表示的可用作抗炎剂，嗜中性粒细胞浸润抑制剂和丝氨酸蛋白酶抑制剂的恶嗪酮衍生物及其药学上可接受的酸加成盐。在式（I）中，A表示基团（a）（其中W表示单键，-O - ， - S-，-CH = CH-或-NR 9 - ; V 2表示= CR 12 > - 或= N-; D表示5至7元碳环或杂环）; X表示单键，-O - ， - S-，-CO-或-NR 15 - 。 Y表示单键，-O - ， - CH = CH-或-NR 16 - 。 Z表示-CH 2 - 或-CO-; I表示0〜4的整数， R 1，R 1〜R 16各自表示氢，低级烷基等。

6. 发明申请

WO1995020598A1 METHOD OF SEPARATING AND PURIFYING TRH ANALOGS AND PROCESS FOR PRODUCING SOLVATES OF TRH ANALOGS 审中-公开
标题翻译：分离和纯化TRH类似物的方法和生产TRH类似物溶剂的方法
公开(公告)号：WO1995020598A1
公开(公告)日：1995-08-03
申请号：PCT/JP1995000107
申请日：1995-01-27
申请人： JAPAN TOBACCO INC. , SAKUMA, Kazuhiko , HARA, Katsuyoshi , HARUTA, Junichi , SAITOH, Akira , UCHIDA, Itsuo
发明人： JAPAN TOBACCO INC.
IPC分类号： C07K05/078
CPC分类号： C07K5/06147 , Y02P20/55
摘要： A method of separating and purifying a TRH derivative by introducing an imino protective group into the histidine portion of a TRH analog represented by formula (I) and separating and purifying the resultant protected imino compound represented by general formula (II) (wherein Y represents an imino protective group). Thus, the compound (I) can be separated from the reaction mixture and purified efficiently in a simplified manner. As the obtained compound (I) can readily be recrystallized from water or other solvent in the form of a solvate, a high-purity solvate represented by general formula (III) can be obtained in a high yield.
摘要翻译：通过将亚氨基保护基引入由式（I）表示的TRH类似物的组氨酸部分中分离和纯化由通式（II）表示的所得保护的亚氨基化合物（其中Y表示亚氨基保护基）。因此，化合物（I）可以与反应混合物分离，并以简化的方式有效地纯化。由于所得到的化合物（I）可以容易地从溶剂合物形式的水或其它溶剂中重结晶，所以可以高产率获得由通式（III）表示的高纯度溶剂化物。

7. 发明申请

WO1992019582A1 NOVEL CYCLOHEXENE DERIVATIVE AND PRODUCTION THEREOF 审中-公开
标题翻译：新的环烯醇衍生物及其生产方法
公开(公告)号：WO1992019582A1
公开(公告)日：1992-11-12
申请号：PCT/JP1992000537
申请日：1992-04-24
申请人： JAPAN TOBACCO INC. , HARUTA, Junichi; , SAKUMA, Kazuhiko; , YASUDA, Akihiro; , HARA, Katsuyoshi; , UCHIDA, Itsuo;
发明人： JAPAN TOBACCO INC.
IPC分类号： C07C62/24
CPC分类号： C07D307/88 , C07C61/22 , C07C62/24 , C07C62/34 , C07C62/36 , C07C62/38 , C07C67/317 , C07C67/333 , C07C69/757 , C07C69/75
摘要： A novel (1R, 2S)-1-acyl-2-carboxycyclohex-4-ene derivative represented by general formula (I), and a process for producing the same. In the said formula, R1 represents hydrogen, lower alkyl or (un)substituted aryl; and R2 represents hydrogen or lower alkyl. A process for producing a (3S, 4R)-4-substituted-3-carboxycyclopentanone derivative represented by general formula (A), wherein R?1 and R2¿ are each as defined above.

8. 发明申请

WO1992016497A1 AMINO ACID DERIVATIVE HAVING RENIN INHIBITORY ACTIVITY 审中-公开
标题翻译：具有雷宁抑制活性的氨基酸衍生物
公开(公告)号：WO1992016497A1
公开(公告)日：1992-10-01
申请号：PCT/JP1992000329
申请日：1992-03-18
申请人： JAPAN TOBACCO INC. , YOSHITOMI PHARMACEUTICAL INDUSTRIES, LTD. , SHIBATA, Saizo; , YAMADA, Yasuki; , TADA, Hiroki; , TSUJI, Hiroyuki; , UCHIDA, Itsuo; , NAKAMURA, Ikuro , HAYASHI, Yoshiharu , IKEGAMI, Kiyoteru
发明人： JAPAN TOBACCO INC. , YOSHITOMI PHARMACEUTICAL INDUSTRIES, LTD.
IPC分类号： C07C237/22
CPC分类号： C07D233/64 , C07C271/16 , C07C323/60 , C07C2601/14 , C07D209/30 , C07D209/34 , C07D217/26 , C07D235/24 , C07D263/06 , C07D295/15 , C07D319/06 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/12 , C07D471/04 , C07D487/04
摘要： Compounds represented by general formulae (I), (II) and (III), wherein compound (I) is useful as a renin inhibitor, while compounds (II) and (III) are intermediates for the production thereof.
摘要翻译：由通式（I），（II）和（III）表示的化合物，其中化合物（I）可用作肾素抑制剂，而化合物（II）和（III）是其制备的中间体。

9. 发明申请

WO1992013827A1 PROCESS FOR PRODUCING 'alpha'-AMINO-'beta','delta'-DIOL DERIVATIVE 审中-公开
标题翻译：生产α-氨基-β，δ-衍生物的方法
公开(公告)号：WO1992013827A1
公开(公告)日：1992-08-20
申请号：PCT/JP1992000106
申请日：1992-02-04
申请人： JAPAN TOBACCO INC. , SHIBATA, Saizo; , SHIRAKAWA, Eiji; , YAMADA, Yasuki; , ANDO, Koji; , UCHIDA, Itsuo;
发明人： JAPAN TOBACCO INC.
IPC分类号： C07C233/31
CPC分类号： C07C271/18 , B01J27/12 , B01J31/2208 , B01J2231/341 , C07C223/02 , C07C225/10 , C07C225/16 , C07C269/06 , C07C271/16 , C07C2601/14 , Y02P20/55
摘要： A process for producing compounds represented by general formulae (III) and (IV), which are useful as intermediates for the production of amino acid derivatives which have a renin inhibitory activity and are useful as a hypotensive, stereo-selectively in high yields, which comprises reacting an α-amino aldehyde derivative (I) with a compound (II) in the presence of BF3 OEt2 to give an α-amino-β-hydroxy-δ-keto derivative (III) and, if necessary, reducing it into a compound (IV), wherein R1 represents an amino blocking group; R2 represents lower alkyl which may be branched; and R3 represents cyclohexyl or phenyl.

10. 发明申请

WO1994004523A1 DIOXACYCLOALKANE COMPOUND WITH RENIN-INHIBITING ACTIVITY 审中-公开
标题翻译：二烯酮化合物与仁宁抑制活性
公开(公告)号：WO1994004523A1
公开(公告)日：1994-03-03
申请号：PCT/JP1993001156
申请日：1993-08-18
申请人： JAPAN TOBACCO INC. , YOSHITOMI PHARMACEUTICAL INDUSTRIES, LTD. , SHIBATA, Saizo; , YAMADA, Yasuki; , ANDO, Koji; , FUKUI, Kiyoshi; , NAKAMURA, Ikuro , UCHIDA, Itsuo;
发明人： JAPAN TOBACCO INC. , YOSHITOMI PHARMACEUTICAL INDUSTRIES, LTD.
IPC分类号： C07D317/28
CPC分类号： C07D295/205 , A61K38/00 , C07C233/63 , C07C271/16 , C07C271/18 , C07C275/24 , C07C2601/14 , C07D295/20 , C07D295/215 , C07D317/28 , C07D405/12 , C07D405/14 , C07D417/12 , C07D491/10 , C07F7/1804 , C07K5/06078 , C07K5/06139
摘要： A dioxacycloalkane compound represented by general formula [1], a pharmaceutically acceptable salt thereof, an intermediate for producing the compound, and a process for producing the intermediate. The compound [1] has a potent activity of inhibiting renin and a persistent hypotensive effect by peroral administration, thus being useful as a hypotensive and a remedy for cardiac insufficiency. General formula [1] wherein A represents [a] or [b]; W represents [c], [d] or [e], X represents -CO- or -SO2-; Y represents -CH2, -O- or -NR -; R represents aralkyl which may be substituted by lower alkoxy; R represents hydrogen or lower alkyl; R represents -(CH2)d-SR or [f]; R and R represent each hydrogen or lower alkyl; and E represents -C(R )(R )- or -CH2CH2-.
摘要翻译：由通式[1]表示的二氧杂环烷烃化合物，其药学上可接受的盐，制备该化合物的中间体及其制备方法。化合物[1]具有抑制肾素的有效活性和通过口服给药持续的降压作用，因此可用作心脏功能不全的低血压和补救措施。通式[1]其中A代表[a]或[b]; W表示[c]，[d]或[e]，X表示-CO-或-SO 2 - ; Y表示-CH 2，-O-或-NR 25 - ; R 1表示可被低级烷氧基取代的芳烷基; R 2表示氢或低级烷基; R 3表示 - （CH 2）d -R SR 26或[f]; R 4和R 5各自代表氢或低级烷基; 且E表示-C（R 29）（R 30） - 或-CH 2 CH 2 - 。

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