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1. 发明申请

WO9507279A3 PROCESS FOR THE PREPARATION OF INDOLIZINE DERIVATIVES 审中-公开
标题翻译：制备衍生物衍生物的方法
公开(公告)号：WO9507279A3
公开(公告)日：1995-04-27
申请号：PCT/JP9401465
申请日：1994-09-06
申请人： FUJISAWA PHARMACEUTICAL CO , OKADA SATOSHI , SAWADA KOZO , KURODA AKIO , WATANABE SHINYA , TANAKA HIROKAZU
发明人： OKADA SATOSHI , SAWADA KOZO , KURODA AKIO , WATANABE SHINYA , TANAKA HIROKAZU
IPC分类号： A61K31/435 , A61P43/00 , C07D213/50 , C07D213/61 , C07D471/04
CPC分类号： C07D471/04 , C07D213/50
摘要： A new process for preparing a compound of formula (I).

2. 发明专利

JPH08119936A HETEROCYCLIC DERIVATIVE 失效
公开(公告)号：JPH08119936A
公开(公告)日：1996-05-14
申请号：JP25215894
申请日：1994-10-18
申请人： FUJISAWA PHARMACEUTICAL CO
发明人： SHIMAZAKI NORIHIKO , WATANABE SHINYA , SAWADA AKIHIKO , HENMI KEIJI
IPC分类号： C07D333/24 , A61K31/38 , A61K31/381 , A61K31/40 , A61K31/44 , A61K31/4427 , A61K31/4433 , A61P1/04 , A61P1/16 , A61P7/02 , A61P9/10 , A61P9/12 , A61P27/02 , A61P27/14 , A61P35/00 , A61P37/08 , A61P43/00 , C07D207/337 , C07D333/38 , C07D401/06 , C07D409/06 , C07D409/14
摘要： PURPOSE: To obtain the subject compound represented by a specific formula, having a thromboxane A2 -antagonizing action and a thromboxane A2 synthesis- inhibiting action, and useful for preventing and treating thrombotic diseases, etc. CONSTITUTION: This compound is expressed by formula I [R is (protected) carboxy, (protected)carboxy (lower)alkyl, (protected)carboxy (lower)alkenyl; R is H, lower alkyl, heterocyclic (lower)alkyl, heterocyclic (lower) alkenyl, heterocyclic carbonyl; R is H, lower alkyl; R is acyl, R is H; A is lower alkylene; Z is S, NH], e.g. 2-(2-carboxyethyl)-4-[3-(4-chlorophenylsulfonylamino) propyl]thiophene. For example, a compound of formula II, its reactive derivative at the amino group or its salt is preferably reacted with a compound of formula: R -X (X is halogen) or its salt in the presence of a base such as an alkali metal in a solvent such as methanol at room temperature, under cooling or under heating to obtain the objective compound.

3. 发明专利

JPH04279570A AMINO ACID DERIVATIVE AND ITS PRODUCTION 失效
公开(公告)号：JPH04279570A
公开(公告)日：1992-10-05
申请号：JP31027991
申请日：1991-09-13
申请人： FUJISAWA PHARMACEUTICAL CO
发明人： HENMI KEIJI , KEI MASAHIRO , MARUSAWA HIROSHI , WATANABE SHINYA , HASHIMOTO SHINJI
IPC分类号： C07D217/02 , A61K31/415 , A61K31/445 , A61K31/535 , A61K31/54 , A61K31/55 , A61K38/00 , A61K38/55 , A61P9/00 , A61P9/12 , A61P13/02 , A61P15/00 , A61P27/02 , A61P27/06 , C07C237/22 , C07D233/54 , C07D233/64 , C07D401/12 , C07D403/12 , C07K5/065 , C07K5/078 , C07K14/81
摘要： PURPOSE:To obtain a new compound usable as an antihypertensive, agent for cardiac failure, etc., and having renin inhibiting activity. CONSTITUTION:A compound expressed by formula I (R is morpholinocarbonyl, etc.; R , R , R , are lower alkyl; X is lower alkylene; Y is single bond, etc.; Y is NH or O), e.g. (2S, 3S)-2-[N -[N-methyl-N-{2-(N-morpholinocarbonyl-N- methylamino)ethyl} aminocarbonyl]-L-phenylalanyl]-N -methyl-L-histidyl]amino-1- cyclohexyl-3-hydroxy-5-methylhexane. The compound is obtained by eliminating an N-protecting group from a compound expressed by formula IV obtained by reacting a compound expressed by formula II (R is N-protecting group; R is H, etc.) with a compound expressed by formula III to afford a compound expressed by formula V, and then reacting the compound expressed by formula V with a compound expressed by formula VI.

4. 发明专利

JPH10147587A 2-AMINO-1,3 PROPANEDIOL DERIVATIVE AND ITS PHARMACEUTICAL USE 失效
公开(公告)号：JPH10147587A
公开(公告)日：1998-06-02
申请号：JP31553497
申请日：1997-11-17
申请人： FUJISAWA PHARMACEUTICAL CO
发明人： SHIMAZAKI NORIHIKO , KAYAKIRI HIROSHI , FUKAMI NAOKI , WATANABE SHINYA , YOSHIMURA SEIJI , ABE YOSHITO , MIZUTANI TAKESHI
IPC分类号： A61K31/695 , A61P17/00 , A61P37/06 , C07F7/08 , C07F7/10
摘要： PROBLEM TO BE SOLVED: To obtain the subject new compound, comprising a specific 2-amino-1,3- propanediol derivative, having immunological activities and useful for treatment, prevention, etc., of rejection due to transplantation, a graft versus host reaction due to bone marrow transplantation, autoimmune diseases, psoriasis, etc. SOLUTION: This new 2-amino-1,3-propanediol derivative (salt) is represented by formula I [R is H or an acyl; R is H, a lower alkyl or an aryl; R is H, a lower alkyl, a higher alkyl, etc.; R is H, a (halo)lower alkyl, a higher alkyl, a (substituted)aryl, etc.; A is an alkylene; E is a bond, 0 or imino; G is a bond or an arylene; J is a bond or O; L is a bond or a lower alkylene] and is useful for treatment, prevention, etc., of a rejection due to transplantation, a graft versus host reaction due to bone marrow transplantation, autoimmune diseases, psoriasis, etc. The compound is obtained by carrying out the hydrosilylating reaction of an unsaturated compound represented by formula II (A is same as A; Y is a lower alkyl; X is a halogen atom) with silanes represented by formula III and reducing the resultant compound represented by formula IV.

5. 发明专利

JPH05178856A HETEROCYCLIC DERIVATIVE 失效
公开(公告)号：JPH05178856A
公开(公告)日：1993-07-20
申请号：JP15707492
申请日：1992-06-16
申请人： FUJISAWA PHARMACEUTICAL CO
发明人： OKADA TATSU , SAWADA KOZO , KURODA AKIO , WATANABE SHINYA , TANAKA HIROKAZU
IPC分类号： A61K31/435 , A61P13/02 , A61P15/00 , A61P17/00 , A61P43/00 , C07D20060101 , C07D471/04
摘要： PURPOSE:To provide the subject new compound useful as a testoterone5alpha- reductase inhibitor for prostatism, alopecia, hirsutism, etc. CONSTITUTION:A compound of formula I {R is (protected) carboxy; R H, lower alkyl, halogen; R is (substituted) aryl, (substituted) ar(lower)alkyl, [substituted carbamoyl] (lower) alkyl, etc.; R are H, lower alkyl; A is (oxo- substituted) lower alkylene, etc.; Q is carbonyl, lower alkylene; X is group of formula II or III (R is H, lower alkyl; R is H, lower alkyl, Y-Z-R ); Z is lower alkylene,-O-, etc.}. For example, 4-[3-[3-[bis(4-isobutylphenyl) methylamino] benzoyl]indolidin-1-yl]butyric acid. The compound of formula I is obtained by reacting a compound (salt) of formula IV (Z is-O-, etc.) with a compound (salt) of formula W -R a [R a is (substituted) ar(lower) alkyl, etc.; W is releasable group].

6. 发明专利

JPH02243674A AMINO ACID DERIVATIVE, PRODUCTION THEREOF AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME 失效
公开(公告)号：JPH02243674A
公开(公告)日：1990-09-27
申请号：JP3457290
申请日：1990-02-15
申请人： FUJISAWA PHARMACEUTICAL CO
发明人： HENMI KEIJI , NEYA MASAHIRO , MARUSAWA HIROSHI , WATANABE SHINYA , HASHIMOTO SHINJI
IPC分类号： C07D295/10 , A61K31/415 , A61P9/00 , C07C237/22 , C07C311/46 , C07D233/64 , C07D295/20 , C07D521/00 , C07K5/06 , C07K14/81
摘要： NEW MATERIAL:An amino acid derivative expressed by formula I [R is H or alkyl; R is aryl; R is N-containing heterocyclic ring, (i) R is alkyl substituted with acyl, etc.; R is formula II (R and R are H or alkyl or both, together with the adjacent N, form a ring; X is single bond, O, etc.; X is NH, O or CH2; (ii) R is heterocyclic ring; R is formula II; X is single bond; X is O or CH2; (iii) R is alkyl substituted with acyl, etc.; R is alkyl; X is NR (R is H or alkyl); X is NH or CH2 or (iv) R is alkyl substituted with acyl, etc.; R is alkyl; X is O; X is NH, O or CH2] and salts thereof. EXAMPLE:(3S)-N,N-Dimethyl-3-tritylamino-4-cyclohexyl-2-hydroxybu- tanesulfonamide. USE:A medicine capable of exhibiting renin inhibitory activity. PREPARATION:For example, a compound expressed by formula III (Ra is N-containing heterocyclic ring; R is N-protecting group) is reacted with a compound expressed by formula IV to provide a compound expressed by formula V. The N-protecting group is then eliminated to afford a compound expressed by formula VI, which is subsequently reacted with a compound expressed by formula VII to provide the compound expressed by formula I.

7. 发明专利

JPH08283244A AMINO ACID DERIVATIVE AND ITS PRODUCTION 失效
公开(公告)号：JPH08283244A
公开(公告)日：1996-10-29
申请号：JP1000096
申请日：1996-01-24
申请人： FUJISAWA PHARMACEUTICAL CO
发明人： HENMI KEIJI , NEYA MASAHIRO , MARUSAWA HIROSHI , WATANABE SHINYA , HASHIMOTO SHINJI
IPC分类号： C07D217/02 , A61K31/415 , A61K31/445 , A61K31/535 , A61K31/54 , A61K31/55 , A61K38/00 , A61K38/55 , A61P9/00 , A61P9/12 , A61P13/02 , A61P15/00 , A61P27/02 , A61P27/06 , C07C237/22 , C07D233/54 , C07D233/64 , C07D401/12 , C07D403/12 , C07K5/065 , C07K5/078 , C07K14/81
摘要： PURPOSE: To produce the subject derivative, having a specific structure and storing inhibiting activities against resin and useful for treating and preventing hypertension, cardiac insufficiency, renopathy, etc., especially a therapeutic agent for dementia. CONSTITUTION: A compound of formula I [R is (thio)morpholinocarbonyl, hexahydro-1H-azepin-1-y1-carbonyl, octahydroazocin-1-ylcarbonyl, etc.; R and R are each a lower alkyl, R is a (substituted) lower alkyl; X is a lower alkylene; Y is a single bond or NR (R is a lower alkyl); Y is NH or O], e.g. (2S, 3S)-2-[Nα-[N-[N-methyl-N- 2-(N-morpholinocarbonyl-N-methylamino) ethyl}aminocarbonyl]-L-phenylalanyl]-Nα-methyl-L-histidyl]amino-1-chclohexyl-3- hydroxy-5-methylhexane. This compound is obtained by reacting a compound of formula II (R is H or an N-protecting group) with a compound of formula III.

8. 发明专利

DE69529614T2 未知
公开(公告)号：DE69529614T2
公开(公告)日：2003-07-03
申请号：DE69529614
申请日：1995-07-10
申请人： FUJISAWA PHARMACEUTICAL CO
发明人： HEMMI KEIJI , SHIMAZAKI NORIHIKO , WATANABE SHINYA , SAWADA AKIHIKO
IPC分类号： A61K31/495 , A61K31/4985 , A61P11/06 , A61P19/10 , A61P29/00 , A61P31/04 , A61P31/14 , A61P35/00 , A61P37/00 , A61P37/06 , A61P43/00 , 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 for the treatment of hepatitis in human beings and animals.

9. 发明专利

AT214067T 未知
公开(公告)号：AT214067T
公开(公告)日：2002-03-15
申请号：AT96941882
申请日：1996-12-13
申请人： FUJISAWA PHARMACEUTICAL CO
发明人： SHIMAZAKI NORIHIKO , SAWADA AKIHIKO , WATANABE SHINYA
IPC分类号： A61K31/00 , A61K31/495 , A61K31/4985 , A61P43/00 , C07D471/04 , C07D241/00 , C07D221/00
摘要： PCT No. PCT/JP96/03666 Sec. 371 Date Jun. 19, 1998 Sec. 102(e) Date Jun. 19, 1998 PCT Filed Dec. 13, 1996 PCT Pub. No. WO97/24355 PCT Pub. Date Jul. 10, 1997A compound of the formula: wherein R1 is pyridyl(lower)alkyl, N-oxidopyridyl(lower)alkyl or imidazolyl(lower)alkyl, R2 is aminophenyl, [protected amino]phenyl, [[[halophenyl](lower)alkenoyl]amino]phenyl, [[pyridyl(lower)alkenoyl]amino]phenyl, [[[N-oxidopyridyl](lower)alkenoyl]amino]phenyl, [[[protected aminopyridyl](lower)alkenoyl]amino]phenyl, [thiazolylcarbonylamino]phenyl which may have pyridyl, naphthyl having lower alkoxy and halogen, [dihalophenyl](lower)alkenyl, [N-oxidopyridyl](lower)alkenyl, [aminopyridyl](lower)alkenyl, [protected aminopyridyl](lower)alkenyl, [carboxypyridyl](lower)alkenyl, [protected carboxypyridyl](lower)alkenyl, [[pyridyl(lower)alkenyl]pyridyl](lower)alkenyl, [[carboxy(lower)alkenyl]pyridyl](lower)alkenyl, [[protected carboxy(lower)alkenyl]pyridyl](lower)alkenyl, [pyridyl(lower)alkenyl]pyridyl, lower alkylbenzothiazolyl or [halopyridylcarbonyl]amino, with proviso that when R2 is [[4-pyridyl(lower)alkenoyl]amino]phenyl, aminophenyl, [lower alkanoylamino]phenyl or [dihalophenyl](lower)alkenyl, then R1 is N-oxidopyridyl(lower)alkyl or imidazolyl(lower)alkyl, and a pharmaceutically acceptable salt thereof, which is useful as a medicament.

10. 发明专利

IE921805A1 HETEROCYCLIC DERIVATIVES 未知
公开(公告)号：IE921805A1
公开(公告)日：1992-12-30
申请号：IE921805
申请日：1992-07-01
申请人： FUJISAWA PHARMACEUTICAL CO
发明人： OKADA SATOSHI , SAWADA KOZO , KURODA AKIO , WATANABE SHINYA , TANAKA HIROKAZU
IPC分类号： A61P13/02 , A61K31/435 , A61P15/00 , A61P17/00 , A61P43/00 , C07D20060101 , C07D471/04 , C07D471/00
摘要： A compound of the formula : wherein R is carboxy or protected carboxy, R is hydrogen, lower alkyl or halogen, R is aryl or ar(lower)alkyl, each of which may have suitable substituent(s), [substituted carbamoyl](lower)alkyl, or a group of the formula : in which is heterocyclic group containing nitrogen atom, and n is 0 or 1, R is hydrogen or lower alkyl, A is lower alkylene which may be substituted by oxo, or lower alkenylene, Q is carbonyl or lower alkylene, X is in which R is hydrogen or lower alkyl, and R is hydrogen, lower alkyl or Y-Z-R , Y is bond or lower alkylene, Z is lower alkylene, lower alkenylene, -O-or in which R is hydrogen, lower alkyl, ar(lower)alkyl which may have suitable substituent(s) or amino protective group, and pharmaceutically acceptable salts thereof, processes for their preparation and pharmaceutical compositions comprising them.

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