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公开(公告)号：JPH0770118A
公开(公告)日：1995-03-14
申请号：JP31815193
申请日：1993-12-17
发明人： KUBO KEIJI , INADA YOSHIYUKI , NAKA TATSUHIKO
IPC分类号： A61K31/415 , A61K31/42 , A61K31/4245 , A61K31/425 , A61K31/433 , A61K31/44 , A61K31/4427 , A61K31/47 , A61K31/50 , A61K31/505 , A61P1/16 , A61P9/00 , A61P9/08 , A61P9/10 , A61P9/12 , A61P25/00 , A61P43/00 , C07D401/10 , C07D403/10 , C07D413/10 , C07D417/10 , C07D471/04 , C07D487/04
摘要： PURPOSE:To obtain a new heterocyclic compound having a strong angiotensin II antagonism and a vasodepressor activity and useful as a therapeutic agent for circulatory diseases or a medicine for improving cerebral functions. CONSTITUTION:A compound of the formula [Ring A is an aromatic heterocyclic group in which the ring is composed of 5 to 10 ring-constituting atoms and may have other substituent groups in addition to R and R ; R is a hydrocarbon residue which may be bonded through a hetero atom or may be substituted; R is a group capable of releasing protons in vivo or another group convertible thereto; R is a 5- to 7-membered heterocyclic residue having CO, CS, S, SO or SO2 as a ring-constituting group. This ring may be substituted; X shows that a ring Y is bonded directly or through a spacer having a
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公开(公告)号：JPH06239859A
公开(公告)日：1994-08-30
申请号：JP22905893
申请日：1993-09-14
发明人： KUBO KEIJI , INADA YOSHIYUKI , NAKA TATSUHIKO
IPC分类号： A61K31/41 , A61K31/415 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/505 , A61P9/00 , A61P9/12 , A61P13/02 , A61P15/00 , A61P43/00 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/12 , C07D471/04 , C07D487/04 , C07D491/048 , C07D493/04 , C07D495/04 , C07D498/04 , C07D513/04
摘要： PURPOSE:To obtain a new compound useful as a therapeutic agent for circulatory diseases such as hypertension, cardiac disease, nephritis and arteriosclerosis, a treating agent for Alzheimer's disease and geriatric dementia, an improver for cerebral function, etc. CONSTITUTION:A compound of formula I [R is (substituted)hydrocarbon group or (substituted)acyl; R is 5- to 7-membered heterocyclic residue; Q is CH or N; X is directly bonded to ring Y and ring W through
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公开(公告)号：JPH0559062A
公开(公告)日：1993-03-09
申请号：JP28182191
申请日：1991-10-29
发明人： NAKA TATSUHIKO , INADA YOSHIYUKI
IPC分类号： A61K31/415 , A61K31/4188 , A61P9/00 , A61P9/10 , A61P9/12 , A61P13/02 , A61P15/00 , A61P43/00 , C07D495/04
摘要： PURPOSE:To provide new compounds showing a strong angiotensin II antagonism and an antihypertensive action and useful as a medicine for improving circulatory system diseases such as shoulder hypertension and heart diseases. CONSTITUTION:Compounds of formula I (Ring A is group R or thiophene ring; R is H or hydrocarbon residue which may be bonded through hetero; R and R are group capable of anion formation or conversion into anion; X is bond between phenylene and phenyl; n is 1 or 2), e.g. methyl 2-ethylthio-4- methyl-1-@{9146/2[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl]thieno[3,4- d]imidazole-6-carboxylate. The compound of formula I can be obtained by reacting a compound of formula II with an alkylation agent of formula III (Z is halogen) in the presence of a base (e.g. NaH) in a solvent (e.g. DMF) at an ice-cooling temperature-room temperature.
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公开(公告)号：JP2002047203A
公开(公告)日：2002-02-12
申请号：JP2001156252
申请日：2001-05-25
IPC分类号： C12N15/09 , A61K31/7088 , A61K38/00 , A61K39/395 , A61K48/00 , A61P9/12 , A61P11/00 , C07K14/52 , C07K16/24
摘要： PROBLEM TO BE SOLVED: To obtain a new competitive inhibitory type mutein of monocyte chemoattractant protein-1(MCP-1) or its salt, a DNA having a base sequence capable of encoding the competitive inhibitory type mutein of the MCP-1 or a neutralizing antibody against the MCP-1 having hypotensive actions, etc., and useful as a prophylactic and therapeutic agent for pulmonary hypertension (especially primary pulmonary hypertension). SOLUTION: The prophylactic and therapeutic agent, etc., comprise the competitive inhibitory type mutein of MCP-1 or its salt, DNA having the base sequence capable of encoding the competitive inhibitory type mutein of the MCP-1 or the neutralizing antibody against the MCP-1.
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公开(公告)号：JP2001328988A
公开(公告)日：2001-11-27
申请号：JP2001159745
申请日：2001-05-28
发明人： NAKA TATSUHIKO , INADA YOSHIYUKI
IPC分类号： A61K31/41 , A61K31/415 , A61K31/4178 , A61K31/4184 , A61K31/4188 , A61K31/4196 , A61K31/435 , A61K31/437 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4439 , A61K31/50 , A61K31/505 , A61K31/517 , A61K31/519 , A61K31/52 , A61K31/522 , A61P9/00 , A61P9/10 , A61P9/12 , A61P13/02 , A61P13/12 , A61P15/00 , A61P43/00 , C07D401/06 , C07D401/14 , C07D403/06 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/14 , C07D471/04 , C07D473/28 , C07D473/30 , C07D487/04 , C07D495/04
摘要： PROBLEM TO BE SOLVED: To provide a heterocyclic compound having potent angiotensin II antagonism, therefore useful as a therapeutic agent for hypertension or the like. SOLUTION: This heterocyclic compound is shown by formula I [R1 is a hydrocarbon residue which may be bound via a heteroatom and substituted; R2 is an anion-forming group or a group convertible to an anion; R3 is a (substituted) aromatic hydrocarbon residue or (substituted) heterocyclic group containing a heteroatom; X indicates that R3 and W are bound to each other either directly or via a spacer with
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6.发明专利
公开(公告)号：JPH11315034A
公开(公告)日：1999-11-16
申请号：JP5504399
申请日：1999-03-03
发明人： IGARI YASUTAKA , SAIKAWA AKIRA , INADA YOSHIYUKI , KAMEI SHIGERU
IPC分类号： A61K9/52 , A61K31/00 , A61K31/415 , A61K31/4164 , A61K31/4184 , A61K45/00 , A61K47/02 , A61K47/34 , A61P9/00 , A61P43/00
摘要： PROBLEM TO BE SOLVED: To obtain the subject preparation having angiotensin II antagonism over a long period while maintaining within-day difference variation by including a compound having angiotensin II antagonism and a biodegradable polymer. SOLUTION: This sustained release preparation is obtained by including (A) a compound having angiotensin II antagonism, e.g. a compound of the formula [R and R are each an anion-forming group; X is either directly or via a spacer of is a hydrocarbon residue] (e.g. candesartan), a prodrug thereof or a salt thereof (except 2-ethyl-5,7-dimethyl-3- [2'-(1H-tetrazol-5-yl)biphenyl-4- yl]methyl}imidazo[4,5-b]pyridine) and (B) a biodegradable polymer (e.g. lactic acid-glycolic acid polymer). The single dose of this preparation is pref. 0.01-10 mg/kg per adult in terms of the effective amount of the ingredient A.
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公开(公告)号：JPH09183778A
公开(公告)日：1997-07-15
申请号：JP32017596
申请日：1996-11-29
发明人： NAKA TATSUHIKO , INADA YOSHIYUKI
IPC分类号： C07D403/10 , A61K31/40 , A61K31/41 , A61K31/415 , A61K31/4184 , A61K31/4188 , A61K31/42 , A61K31/4245 , A61K31/433 , A61K31/435 , A61K31/4365 , A61K31/495 , A61K31/505 , A61K31/513 , A61K31/517 , A61K31/53 , A61K31/535 , A61P9/00 , A61P9/08 , A61P9/10 , A61P9/12 , A61P25/28 , A61P43/00 , B29D22/00 , B32B27/42 , C07D20060101 , C07D285/08 , C07D413/10 , C07D417/10 , C07D419/10 , C07D471/04 , C07D487/04 , C07D495/04 , C07D519/00
摘要： PROBLEM TO BE SOLVED: To provide a new compound having strong angiotensin II antagonistic action, hypotensive action and central nervous action and useful for the treatment of circulatory diseases such as hypertension, cardiac diseases, cerebral apoplexy, nephritis and arteriosclerosis, Alzheimers disease, senile dementia, etc. SOLUTION: This compound is expressed by the formula I [R is a (substituted)hydrocarbon group which may be bonded through hetero-atom; R is a (substituted)heterocyclic residue having a ring-constituting group; X is bonded to rings Y and W; W and Y are each a (substituted)aromatic hydrocarbon residue which may contain hetero-atom or a heterocyclic residue; (n) is 1 or 2; (a) and (b) are each a (substituted)C or a hetero-atom; (c) is a (substituted)C, a hetero-atom, etc.], e.g. 2-ethoxy-1-[[2'-(2,5-dihydro-5-oxo-1,2,4- thiadiazol-3-yl)biphenyl-4-yl]methy]benzimidazole-7-carboxylic acid. The compound of the formula I can be produced by reacting a compound of the formula II with a compound of the formula III (L is a halogen) and, as necessary, properly subjecting the reaction product to hydrolysis, reduction, halogenation, O-, N- or S-alkylation, nucleophilic reaction, cyclization, acylation, etc.
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公开(公告)号：JPH0753373A
公开(公告)日：1995-02-28
申请号：JP12483894
申请日：1994-06-07
发明人： INADA YOSHIYUKI , KUBO KEIJI
IPC分类号： A61K31/135 , A61K31/18 , A61K31/19 , A61K31/192 , A61K31/195 , A61K31/275 , A61K31/34 , A61K31/341 , A61K31/343 , A61K31/38 , A61K31/40 , A61K31/402 , A61K31/4035 , A61K31/404 , A61K31/41 , A61K31/415 , A61K31/4184 , A61K31/42 , A61K31/4245 , A61K31/425 , A61K31/433 , A61K31/4422 , A61K31/465 , A61K31/495 , A61K31/496 , A61K31/505 , A61K31/517 , A61K31/519 , A61K31/52 , A61K31/54 , A61K31/541 , A61K31/549 , A61K31/55 , A61K31/554 , A61K31/575 , A61K31/585 , A61K45/00 , A61P7/10 , A61P9/00 , A61P9/04 , A61P9/08 , A61P9/10 , A61P9/12 , A61P13/02 , A61P13/12 , A61P15/00 , A61P17/00 , A61P25/20 , A61P25/24 , A61P25/28 , A61P27/06 , A61P43/00 , C07D235/26 , C07D235/28 , C07D235/30
摘要： PURPOSE:To provide an agent for the prevention or treatment of angiotensin II-mediated diseases, having suppressed side actions of drug and composed of a combination of a compound (salt) having angiotensin II antagonistic action consisting of a specific benzimidazole with a compound having diuretic action or Ca antagonistic action. CONSTITUTION:This agent for the prevention or treatment of various angiotensin II-mediated diseases can be prepared by combining (A) a compound (salt) expressed by the formula [R is a (substituted)hydrocarbon group; R is an (esterified)carboxyl; R is a group capable of forming anion or group convertible to the anion-forming group; X is a group to bond a phenylene group to a phenyl group directly or through a spacer containing (R is H or an alkyl) ; (n) is 1 or 2; ring A is benzene ring which may have substituent in addition to R ] with (B) a compound having diuretic action or a compound having calcium antagonistic action.
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公开(公告)号：JPH05163267A
公开(公告)日：1993-06-29
申请号：JP13748592
申请日：1992-04-15
发明人： NAKA TATSUHIKO , INADA YOSHIYUKI
IPC分类号： A61K31/41 , A61K31/415 , A61K31/4178 , A61K31/4184 , A61K31/4188 , A61K31/4196 , A61K31/435 , A61K31/437 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4439 , A61K31/50 , A61K31/505 , A61K31/517 , A61K31/519 , A61K31/52 , A61K31/522 , A61P9/00 , A61P9/10 , A61P9/12 , A61P13/02 , A61P13/12 , A61P15/00 , A61P43/00 , C07D401/06 , C07D401/14 , C07D403/06 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/14 , C07D471/04 , C07D473/28 , C07D473/30 , C07D487/04 , C07D495/04
摘要： PURPOSE:To provide a new compound having strong angiotensin II antagonistic action and useful as an agent for the treatment of circulatory diseases such as hypertensive heart diseases, cerebral apoplexy and nephritis. CONSTITUTION:The compound of formula I (R is hydrocarbon residue which may be bonded through a hetero atom; R is group capable of forming anion, etc.; R is aromatic hydrocarbon residue or heterocyclic residue; X is direct bond or bond interposing a spacer composed of a chain having
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