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71. 发明专利

PH11998002606B1 Crystalline antifungal polymorph 未知
公开(公告)号：PH11998002606B1
公开(公告)日：2006-08-10
申请号：PH11998002606
申请日：1998-10-06
申请人： SCHERING CORP
发明人： ANDREWS DAVID R , LEONG WILLIAM , SUDHAKAR ANANTHA R
IPC分类号： A61K31/4196 , A61K31/496 , A61K31/4965 , A61P31/10 , C07D241/00 , C07D249/00 , C07D307/00 , C07D405/14
摘要： The crystalline polymorph Form I of (-)-4-[4- [4-[4-[ [(2R-cis)-5-(2, 4-difluorophenyl) tetrahydro-5-(1H-1, 2,4-triazol- 1-ylmethyl)furan-3-yl] methoxy]phenyl] -1-piperazinyl] phenyl-2,4-dihydro-2- [(S)-1-ethyl-2(S)- hydroxylpropyl]-3H-1, 2,4-triazol-3-one represented by formula (I), pharmaceutical compositions containing such a polymorph and methods of using such a polymorph to treat fungal infections in mammals are disclosed.

72. 发明专利

SK285190B6 Crystalline antifungal polymorph and pharmaceutical composition containing thereof 未知
公开(公告)号：SK285190B6
公开(公告)日：2006-08-03
申请号：SK5122000
申请日：1998-10-05
申请人： SCHERING CORP
发明人： ANDREWS DAVID R , LEONG WILLIAM , SUDHAKAR ANANTHA R
IPC分类号： C07D405/00 , A61K31/00 , A61K31/4196 , A61K31/496 , A61K31/4965 , A61P31/10 , C07D241/00 , C07D249/00 , C07D307/00 , C07D405/14
摘要： The crystalline polymorph Form I of compound of formula (I), pharmaceutical compositions containing such a polymorph and methods of using such a polymorph to treat fungal infections in mammals are disclosed.

73. 发明专利

AU759982B2 Crystalline antifungal polymorph 未知
公开(公告)号：AU759982B2
公开(公告)日：2003-05-01
申请号：AU9780398
申请日：1998-10-05
申请人： SCHERING CORP
发明人： ANDREWS DAVID R , LEONG WILLIAM , SUDHAKAR ANANTHA R
IPC分类号： A61K31/4196 , A61K31/496 , A61K31/4965 , A61P31/10 , C07D241/00 , C07D249/00 , C07D307/00 , C07D405/14 , A61K31/41 , A61K31/495
摘要： The crystalline polymorph Form I of (-)-4-[4- [4-[4-[ [(2R-cis)-5-(2, 4-difluorophenyl) tetrahydro-5-(1H-1, 2,4-triazol- 1-ylmethyl)furan-3-yl] methoxy]phenyl] -1-piperazinyl] phenyl-2,4-dihydro-2- [(S)-1-ethyl-2(S)- hydroxylpropyl]-3H-1, 2,4-triazol-3-one represented by formula (I), pharmaceutical compositions containing such a polymorph and methods of using such a polymorph to treat fungal infections in mammals are disclosed.

74. 发明专利

AT207881T 未知
公开(公告)号：AT207881T
公开(公告)日：2001-11-15
申请号：AT96942936
申请日：1996-12-19
申请人： SCHERING CORP
发明人： LEONG WILLIAM , SMITH LYMAN
IPC分类号： C07C241/04 , C07C243/28 , C07C337/02
摘要： A process for producing a hydrazide of formula (1.0) is disclosed. The process comprises reacting a hydrazone of formula (2.0) or (2.1), wherein said hydrazone is in toluene, with a mixture of Grignard reagents, wherein said Grignard reagents are in a suitable organic solvent; wherein: (A) Z is a suitable carbonyl protecting group; (B) R is a suitable -OH protecting group; (C) R is selected from: H, a non-enolizable alkyl, a non-enolizable substituted alkyl, aryl, substituted aryl, -S-aryl, -S-(substituted aryl), -S-alkyl, -S-(substituted alkyl), alkoxy, substituted alkoxy, aryloxy, or substituted aryloxy; (D) said mixture of Grignard reagents comprises R MgX in admixture with R MgX; (E) R is a suitable alkyl, substituted alkyl, alkenyl, alkynyl, aryl, substituted aryl, or aralkyl group capable of adding to the -C=N group of the hydrazone to produce the hydrazide; (F) R is a suitable alkyl, substituted alkyl, aryl or substituted aryl group that is more sterically hindered than said R group; (G) X is independently selected from Cl, Br or I for each Grignard reagent; (H) when said hydrazone is a compound of formula (2.0) then the reaction is conducted at a temperature of about +30 to about -40 DEG C; and (I) when said hydrazone is a compound of formula (2.1) then the reaction is conducted at a temperature of about +40 to about -20 DEG C.

75. 发明专利

NO20001779L 未知
公开(公告)号：NO20001779L
公开(公告)日：2000-06-06
申请号：NO20001779
申请日：2000-04-06
申请人： SCHERING CORP
发明人： ANDREWS DAVID R , LEONG WILLIAM , SUDHAKAR ANANTHA R
IPC分类号： A61K31/4196 , A61K31/496 , A61K31/4965 , A61P31/10 , C07D241/00 , C07D249/00 , C07D307/00 , C07D405/14
摘要： The crystalline polymorph Form I of (-)-4-[4- [4-[4-[ [(2R-cis)-5-(2, 4-difluorophenyl) tetrahydro-5-(1H-1, 2,4-triazol- 1-ylmethyl)furan-3-yl] methoxy]phenyl] -1-piperazinyl] phenyl-2,4-dihydro-2- [(S)-1-ethyl-2(S)- hydroxylpropyl]-3H-1, 2,4-triazol-3-one represented by formula (I), pharmaceutical compositions containing such a polymorph and methods of using such a polymorph to treat fungal infections in mammals are disclosed.

76. 发明专利

BR9612046A 未知
公开(公告)号：BR9612046A
公开(公告)日：1999-02-09
申请号：BR9612046
申请日：1996-12-19
申请人： SCHERING CORP
发明人： LEONG WILLIAM , SMITH LYMAN
IPC分类号： C07C241/04 , C07C243/28 , C07C337/02
摘要： A process for producing a hydrazide of formula (1.0) is disclosed. The process comprises reacting a hydrazone of formula (2.0) or (2.1), wherein said hydrazone is in toluene, with a mixture of Grignard reagents, wherein said Grignard reagents are in a suitable organic solvent; wherein: (A) Z is a suitable carbonyl protecting group; (B) R is a suitable -OH protecting group; (C) R is selected from: H, a non-enolizable alkyl, a non-enolizable substituted alkyl, aryl, substituted aryl, -S-aryl, -S-(substituted aryl), -S-alkyl, -S-(substituted alkyl), alkoxy, substituted alkoxy, aryloxy, or substituted aryloxy; (D) said mixture of Grignard reagents comprises R MgX in admixture with R MgX; (E) R is a suitable alkyl, substituted alkyl, alkenyl, alkynyl, aryl, substituted aryl, or aralkyl group capable of adding to the -C=N group of the hydrazone to produce the hydrazide; (F) R is a suitable alkyl, substituted alkyl, aryl or substituted aryl group that is more sterically hindered than said R group; (G) X is independently selected from Cl, Br or I for each Grignard reagent; (H) when said hydrazone is a compound of formula (2.0) then the reaction is conducted at a temperature of about +30 to about -40 DEG C; and (I) when said hydrazone is a compound of formula (2.1) then the reaction is conducted at a temperature of about +40 to about -20 DEG C.

77. 发明专利

PL327142A1 METHOD OF OBTAINING HYDRAZIDES 未知
公开(公告)号：PL327142A1
公开(公告)日：1998-11-23
申请号：PL32714296
申请日：1996-12-19
申请人： SCHERING CORP
发明人： LEONG WILLIAM , SMITH LYMAN
IPC分类号： C07C241/04 , C07C243/28 , C07C337/02
摘要： A process for producing a hydrazide of formula (1.0) is disclosed. The process comprises reacting a hydrazone of formula (2.0) or (2.1), wherein said hydrazone is in toluene, with a mixture of Grignard reagents, wherein said Grignard reagents are in a suitable organic solvent; wherein: (A) Z is a suitable carbonyl protecting group; (B) R is a suitable -OH protecting group; (C) R is selected from: H, a non-enolizable alkyl, a non-enolizable substituted alkyl, aryl, substituted aryl, -S-aryl, -S-(substituted aryl), -S-alkyl, -S-(substituted alkyl), alkoxy, substituted alkoxy, aryloxy, or substituted aryloxy; (D) said mixture of Grignard reagents comprises R MgX in admixture with R MgX; (E) R is a suitable alkyl, substituted alkyl, alkenyl, alkynyl, aryl, substituted aryl, or aralkyl group capable of adding to the -C=N group of the hydrazone to produce the hydrazide; (F) R is a suitable alkyl, substituted alkyl, aryl or substituted aryl group that is more sterically hindered than said R group; (G) X is independently selected from Cl, Br or I for each Grignard reagent; (H) when said hydrazone is a compound of formula (2.0) then the reaction is conducted at a temperature of about +30 to about -40 DEG C; and (I) when said hydrazone is a compound of formula (2.1) then the reaction is conducted at a temperature of about +40 to about -20 DEG C.

78. 发明专利

CZ187798A3 PROCESS FOR PREPARING HYDRAZIDES 未知
公开(公告)号：CZ187798A3
公开(公告)日：1998-09-16
申请号：CZ187798
申请日：1996-12-19
申请人： SCHERING CORP
发明人： LEONG WILLIAM , SMITH LYMAN
IPC分类号： C07C241/04 , C07C243/28 , C07C337/02
摘要： A process for producing a hydrazide of formula (1.0) is disclosed. The process comprises reacting a hydrazone of formula (2.0) or (2.1), wherein said hydrazone is in toluene, with a mixture of Grignard reagents, wherein said Grignard reagents are in a suitable organic solvent; wherein: (A) Z is a suitable carbonyl protecting group; (B) R is a suitable -OH protecting group; (C) R is selected from: H, a non-enolizable alkyl, a non-enolizable substituted alkyl, aryl, substituted aryl, -S-aryl, -S-(substituted aryl), -S-alkyl, -S-(substituted alkyl), alkoxy, substituted alkoxy, aryloxy, or substituted aryloxy; (D) said mixture of Grignard reagents comprises R MgX in admixture with R MgX; (E) R is a suitable alkyl, substituted alkyl, alkenyl, alkynyl, aryl, substituted aryl, or aralkyl group capable of adding to the -C=N group of the hydrazone to produce the hydrazide; (F) R is a suitable alkyl, substituted alkyl, aryl or substituted aryl group that is more sterically hindered than said R group; (G) X is independently selected from Cl, Br or I for each Grignard reagent; (H) when said hydrazone is a compound of formula (2.0) then the reaction is conducted at a temperature of about +30 to about -40 DEG C; and (I) when said hydrazone is a compound of formula (2.1) then the reaction is conducted at a temperature of about +40 to about -20 DEG C.

79. 发明专利

NO982876A 未知
公开(公告)号：NO982876A
公开(公告)日：1998-08-19
申请号：NO982876
申请日：1998-06-19
申请人： SCHERING CORP
发明人： LEONG WILLIAM , SMITH LYMAN
IPC分类号： C07C241/04 , C07C243/28 , C07C337/02
CPC分类号： C07C241/04 , Y02P20/55 , C07C243/28

80. 发明专利

MX9700143A PROCESO PARA LA PREPARACION DE INTERMEDIOS QUIRALES UTILES PARA LA SINTESIS DE AGENTES ANTIFUNGOSOS. 未知
公开(公告)号：MX9700143A
公开(公告)日：1998-01-31
申请号：MX9700143
申请日：1995-07-05
申请人： SCHERING CORP
发明人： LEONG WILLIAM , SMITH LYMAN
IPC分类号： C07D405/06 , C07D407/04
摘要： Se describe un proceso para preparar compuestos quirales de la formula (II), en donde X1 y X2 son independientemente F o Cl, e Y es Cl, Br o I, que comprende hacer reaccionar un triol de la formula (VIII), en donde X1 y X2 son como se define anteriormente, con acetona en presencia de un catalizador, y luego con un halogeno que se selecciona de Cl2, Br2 o I2, o N-bromosuccinimida o N-yodosuccinimida.

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