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1. 发明专利

JPH10182639A NEW FORM I OF DOXAZOSIN MESYLATE 失效
公开(公告)号：JPH10182639A
公开(公告)日：1998-07-07
申请号：JP36406997
申请日：1997-12-17
申请人： HEUMANN PHARMA GMBH & CO
发明人： GRAFE INGOMAR , MOERSDORF JOHANN PETER
IPC分类号： A61K31/505 , A61P9/12 , A61P13/02 , A61P15/00 , C07D405/12
摘要： PROBLEM TO BE SOLVED: To obtain a crystalline anhydride of the subject compound useful for treating hypertension and benign prostatomegaly, by taking a specific crystal form so as to be easily synthesizable, capable of realizing its high purity and water solubility, and also capable of advantageously producing solid preparations such as tablets or capsules. SOLUTION: This crystalline anhydride of doxazosin mesylate is in a form giving such powder X-ray pattern as to have peaks of high or medium intensity at diffraction angles of 15.40 deg., 16.85 deg., 18.06 deg., 24.15 deg. and 25.81 deg., being obtained, for example, by the following process, that is, basic doxazosin A1 is suspended in the mixture of an alcohol and water followed by addition of a weak acid to form a water-soluble salt of A1 with the weak acid, methanesulfonic acid and a base are then added to the system to adjust to pH2-4 to effect precipitation of doxazosin mesylate, and the precipitate is then collected through filtration, washed with an organic solvent, and then dried.

2. 发明专利

JPH06312988A PREPARATION OF 1,2,3,4,10,14B-HEXAHYDRO-2-METHYLBENZO- (C,F)PYRAZINO(1,2-A)AZEPINE AND ITS SALT 失效
公开(公告)号：JPH06312988A
公开(公告)日：1994-11-08
申请号：JP1745794
申请日：1994-02-14
申请人： HEUMANN PHARMA GMBH & CO
发明人： ROOTAA KISHIEROFUSUKII-RUPAATO , YOOHAN PEETAA MORUSHIYUDORUFU , INGOMAA GURAAFUE , KURUTOOHENINGU AARENZU
IPC分类号： C07C213/04 , C07C215/30 , C07D241/04 , C07D487/04

3. 发明专利

JPH0753490A NEW STABLE CRYSTAL FORM OF BEZAFIBRATE 失效
公开(公告)号：JPH0753490A
公开(公告)日：1995-02-28
申请号：JP9415394
申请日：1994-05-06
申请人： HEUMANN PHARMA GMBH & CO
发明人： PEETAA MORUSHIYUDORUFU , PEETAA MAIYAA , JIYOSEFU SHIYUMITSUTO , KAATOOHENINGU AARENZU
IPC分类号： C07C231/24 , C07C231/22 , C07C233/73

4. 发明专利

JPH01313475A 6-OXOPYRIDAZINE DERIVATIVE, ITS PRODUCTION AND DRUG PREPARATION 失效
公开(公告)号：JPH01313475A
公开(公告)日：1989-12-18
申请号：JP10438089
申请日：1989-04-24
申请人： HEUMANN PHARMA GMBH & CO
发明人： PEETA MERUSUDORUFU , RORUFU HAATAA , HAIDORUN ENGURAA , FUORUKAA FUAARERUTO , RAINHOORUTO BUAITONAA , KURUTO HENINGU AARENSU
IPC分类号： C07D403/00 , A61K31/50 , A61P9/00 , A61P9/04 , C07D401/14 , C07D403/12

5. 发明专利

JPS6383072A NOVEL IMIDAZOLYLGUANIDINE DERIVATIVE, MANUFACTURE AND MEDICINE 失效
公开(公告)号：JPS6383072A
公开(公告)日：1988-04-13
申请号：JP23087587
申请日：1987-09-14
申请人： HEUMANN PHARMA GMBH & CO
发明人： BUSCHAUER ARMIN , SCHICKANEDER HELMUT , MORSDORF PETER , SCHUNACK WALTER , BAUMANN GERT , AHRENS KURT-HENNING
IPC分类号： A61K31/415 , A61K31/38 , A61K31/44 , A61K31/4427 , A61K31/4433 , A61P7/02 , A61P9/00 , A61P9/12 , C07D233/54 , C07D233/64 , C07D401/12 , C07D409/12 , C07D409/14

6. 发明专利

JPS635089A 1,4-DIHYDROPYRIDINE DERIVATIVE, MANUFACTURE AND MEDICINE 失效
公开(公告)号：JPS635089A
公开(公告)日：1988-01-11
申请号：JP13762887
申请日：1987-05-29
申请人： HEUMANN PHARMA GMBH & CO
发明人： HERUMUUTO SHITSUKANEEDAA , PIITAA MUUSHIYUDORUFU , ARUMIN BUSHIYAA , BARUTAA SHIYUNATSUKU , HAIDORUN INGURAA , HARUTOMUUTO BERUGIN , KURUTO HENNINGU AARENSU
IPC分类号： A61K31/44 , A61K31/4427 , A61K31/455 , A61P9/10 , A61P9/12 , C07D211/90 , C07D401/12 , C07D413/14

7. 发明专利

JPH10182641A NEW FORM III OF DOXAZOSIN MESYLATE 失效
公开(公告)号：JPH10182641A
公开(公告)日：1998-07-07
申请号：JP36407197
申请日：1997-12-17
申请人： HEUMANN PHARMA GMBH & CO
发明人： GRAFE INGOMAR , MOERSDORF JOHANN PETER
IPC分类号： A61K31/505 , A61P9/12 , A61P13/02 , A61P15/00 , C07D405/12
摘要： PROBLEM TO BE SOLVED: To obtain a crystalline anhydride of the subject compound useful for treating hypertension and benign prostomegaly, by taking a specific crystal form so as to be easily synthesizable, capable of realizing its high purity and water solubility, and also capable of advantageously producing solid preparations such as tablets or capsules. SOLUTION: This crystalline anhydride of doxazosin mesylate is in a form giving such power X-ray pattern as to have peaks of high or medium intensity at diffraction angles of 8.49 deg., 11.72 deg., 16.03 deg., 18.29 deg., 21.03 deg., 22.87 deg. and 25.02 deg., being obtained, for example, by the following process, that is, basic doxazosin is converted to doxazosin acetate by acetic acid in an organic solvent, the resultant solution is clarified in a hot state and then mixed with methanesulfonic acid followed by agitating the solution at a temperature ranging from 30 deg.C to the boiling point of the solvent; the resultant solvent adduct is collected through filtration, and, in a wet state, put into a lower alcohol, heated at the boiling point for 10min to 12hr, and then cooled to room temperature; and the resulting precipitated crystal is collected through filtration.

8. 发明专利

JPH10182640A NEW FORM II OF DOXAZOSIN MESYLATE 失效
公开(公告)号：JPH10182640A
公开(公告)日：1998-07-07
申请号：JP36407097
申请日：1997-12-17
申请人： HEUMANN PHARMA GMBH & CO
发明人： GRAFE INGOMAR , MOERSDORF JOHANN PETER
IPC分类号： A61K31/505 , A61P13/02 , A61P15/00 , C07D405/12
摘要： PROBLEM TO BE SOLVED: To obtain a crystalline anhydride of the subject compound useful for treating hypertension and benign prostomegaly, by taking a specific crystal form so as to be easily synthesizable, capable of realizing its high purity and water solubility, and also capable of advantageously producing solid preparations such as tablets or capsules. SOLUTION: This crystalline anhydrous doxazosin mesylate is in a form giving such power X-ray pattern as to have peaks of high or medium intensity at diffraction angles of 10.68 deg., 14.45 deg., 17.37 deg., 23.45 deg., 23.82 deg., and 24.30 deg., being obtained, for example, by the following process, that is, basic doxazosin A1 is suspended in a lower ketone followed by addition of a weak acid and, optionally, methanesulfonic acid A2 in an amount below equimolar level to form a water-soluble salt of A1 with the weak acid and/or a salt of part of A1 with A2 followed by adding A2 and a base to the system to adjust pH2-4 to effect precipitation of doxazosin mesylate, and the precipitate is collected through filtration, washed with an organic solvent, and then dried.

10. 发明专利

JPS63258861A PRODUCTION OF NITROETHENE DERIVATIVE 失效
公开(公告)号：JPS63258861A
公开(公告)日：1988-10-26
申请号：JP8113288
申请日：1988-03-31
申请人： HEUMANN PHARMA GMBH & CO
发明人： PEETAA MERUSUDORUFU , HERUMUUTO SHITSUKANEEDERU , KURUTO HENINGU AARENSU
IPC分类号： C07D277/28 , C07D307/52

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