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91. 发明专利

DE602006011453D1 未知
公开(公告)号：DE602006011453D1
公开(公告)日：2010-02-11
申请号：DE602006011453
申请日：2006-04-11
申请人： BOEHRINGER INGELHEIM PHARMA
发明人： HIMMELSBACH FRANK , ECKHARDT MATTHIAS , EICKELMANN PETER , THOMAS LEO
IPC分类号： C07H7/06 , A61K31/7042 , A61P3/10
摘要： Glucopyranosyloxy-substituted (heteroaryloxy-benzyl)-benzene compounds of the general formula I where the groups R1 to R6 as well as R7a, R7b, R7c are defined according to claim 1, including the tautomers, the stereoisomers thereof, the mixtures thereof and the salts thereof. The compounds according to the invention are suitable for the treatment of metabolic disorders.

92. 发明专利

AR067969A1 COMPOSICION FARMACEUTICA QUE COMPRENDE UN INHIBIDOR DE COTRANSPORTADOR DE GLUCOSA DEPENDIENTE DE SODIO (SGLT2) 未知
公开(公告)号：AR067969A1
公开(公告)日：2009-10-28
申请号：ARP080103591
申请日：2008-08-15
申请人： BOEHRINGER INGELHEIM PHARMA
发明人： DUGI KLAUS , HIMMELSBACH FRANK , MARK MICHAEL
IPC分类号： A61K31/351 , A61K31/522 , A61P3/10 , A61P5/50
摘要： Uso. Método de tratamiento. Reivindicacion 1: Una composicion farmacéutica caracterizada porque comprende un inhibidor de cotransportador de glucosa dependiente de sodio GLT2 seleccionado entre el grupo consiste en (1) Dapagliflozina; (2) Remogliflozina o etabonato de Remogliflozina; (3) Sergliflozina o etabonato de Sergliflozina; (4) 1-Cloro-4-(beta-D-glucopiranos-1-il)-2-(4-etiI-bencil)-benceno; (5) (1S)-1,5-anhidro-1-[5-(azulen-2-ilmetil)-2-hidroxifenil]-D-glucitol; (6) (1S)-1,5-anhidra-1-[3-(1-benzotien-2-ilmetil)-4-fluorofenil]-D-glucitol; (7) Derivado d tiofeno de la formula (7-1) en la que R representa metoxi o trifluorometoxi, (8) 1-(beta-D-glucopiranosil)-4-metil-3-[5-(4-fluorofenil)-2-tienilmetil]benceno; (9) Derivado de espirocetal de la formula (9-1) en la que R representa metoxi, trifluorometoxi, etoxi etilo, isopropilo o terc. butilo; o una sal farmacéuticamente aceptable, hidrato o solvato de los mismos; combinado can un inhibidor de DPP IV (dipeptidil peptidasa IV)de formula (1), o formula (2), o formula (3) o formula (4), donde R1 denota ([1,5]naftiridin-2-il)metilo, (quinazolin-2-il)metilo, (quinoxalin-6-il)metilo, (4-metil-quinazolin-2-il)metilo, 2-ciano-bencilo, (3-ciano-quinolin-2-il)metilo, (3-ciano-piridin-2-il)metilo, (4-metil-pirimidin-2-il)metilo o (4,6-dimetil-pirimidin-2-il)metilo y R2 denota 3-(R)-amino-piperidin-1-ilo, (2-amino-2-metil-propil)-metilamino o (2-(S)-amino-propil)-metilamino o su sal farmacéuticamente aceptable. Reivindicacion 2: La composicion farmacéutica de acuerdo con la reivindicacion 1, caracterizada porque el inhibidor de dipeptidil peptidasa IV DPPIV se selecciona entre el grupo consistente en 1-[(4-metil-quinazolin-2-il)metil]-3-metil-7-(2-butin-1-il)-8-(3-( R)-amino-piperidin-1-il)-xantina, 1-[([1,5]naftiridin-2-il)metil]-3-metil-7-(2-butin-1-il)-8-(( R)-3-amino-piperidin-1-il)-xantina, 1-[(quinazolin-2-il)metil]-3-metil-7-(2-butin-1-il)-8-(( R)-3-amino-piperidin-1-il)-xantina, 2-((R)-3-amino-piperidin-1-il)-3-(but-2-iniI)-5-(4-metiI-quinazolin-2-ilmetil)-3,5-dihidro-imidazo[4,5-d]piridazin-4-ona, 1-[(4-metil-quinazolin-2-il)metil]-3-metil-7-(2-butin-1-il)-8-[(2-amino-2-metil-propil)-metilamino]-xantina.1-[(3-ciano-quinolin-2-il)metil]-3-metil-7-(2-butin-1-il)-8-(( R)-3-amino-piperidin-1-il)-xantina, 1-(2-ciano-bencil)-3-metil-7-(2-butin-1-il)-8-(( R)-3-amino-piperidin-1-il)-xantina, 1-[(4-metil-quinazolin-2-il)metil]-3-metil-7-(2-butin-1-il)-8-[(S)-(2-amino-propil)-metilamino]-xantina, 1-[(3-ciano-piridin-2-il)metil]-3-metil-7-(2-butin-1-il)-8-(( R)-3-amino-piperidin-1-il)-xantina, 1-[(4-metil-pirimidin-2-il)metil]-3-metil-7-(2-butin-1-il)-8-(( R)-3-amino-piperidin-1-il)-xantina, 1-[(4,6-dimetil-pirimidin-2-il)metil]-3-metil-7-(2-butin-1-il)-8-(( R)-3-amino-piperidin-1-il)-xantina, y 1-[(quinazolin-6-il)metil]-3-metil-7-(2-butin-1-il)-8-(( R)-3-amino-piperidin-1-il)-xantina, o una sal farmacéuticamente aceptable de los mismos.

93. 发明专利

AU2009217435A1 Xanthine derivative, production and use thereof as a medicament 未知
公开(公告)号：AU2009217435A1
公开(公告)日：2009-10-15
申请号：AU2009217435
申请日：2009-09-22
申请人： BOEHRINGER INGELHEIM PHARMA
发明人： LANGKOPF ELKE , MAIER ROLAND , ECKHARDT MATTHIAS , LOTZ RALF , HIMMELSBACH FRANK , MARK MICHAEL
IPC分类号： C07D473/04 , A61K31/522 , A61K31/55 , A61K31/551 , A61P3/04 , A61P3/10 , A61P5/00 , A61P19/02 , A61P19/10 , A61P37/02 , C07D473/06 , C07D473/08 , C07D473/10 , C07D473/12
摘要： 8-substituted-xanthine derivatives (I), their tautomers, enantiomers, diastereomers or mixtures, and salts. 8-substituted xanthine derivatives of formula (I), their tautomers, enantiomers, diastereomers or mixtures, and salts, are new: [Image] R 1>hydrogen; 1-8C alkyl; 3-8C alkenyl or alkynyl; 3-4C alkenyl substituted by 1-2C alkoxycarbonyl, aminocarbonyl (optionally substituted by 1 or 2 1-3C alkyl) or het-CO; 1-6C alkyl substituted by Ra; phenyl(1-6C)alkyl, optionally ring-substituted by R 1> 0>-R 1> 4>; phenyl(1-4C)alkyl, optionally substituted in alkyl by Rz and in the ring by R 1> 0>-R 1> 4>; R 1> 0>-R 1> 4>-substituted phenyl; phenyl(2-3C) alkenyl, phenyl (or naphthyl)-(CH 2) m-(A or B)-(CH 2) n, naphthyl(1-3C)alkyl or phenylcarbonylmethyl (all optionally ring-substituted by R 1> 0>-R 1> 4>); [1,4-napththoquinon-2-yl; chromen-4-on-3-yl; 1-oxo- or 1,3-dioxo-indan-2-yl; 2,3-dihydro-3-oxo-benzofuran-2-yl; heteroaryl-(CH 2) m-(A or B)-(CH 2) n; 1-6C alkyl-A-(CH 2) n; 3-7C cycloalkyl-(CH 2) m-A or B)-(CH 2) n; R 2> 1>-A-(CH 2) n; phenyl- or naphthyl-(CH 2) m-D-(1-3C)alkyl; Rb-substituted 2-6C alkyl, or 3-6C cycloalkyl; amino, or arylcarbonylamino; het : pyrrolidin-1-yl, piperidin-1-yl or morpholin-4-yl; R 1> 0>-R 1> 4>, Rb and Rz : various substituents; m : 0-2; n : 1-3; A, B and D : various linking groups; R 2>hydrogen or a wide range of substituents; R 3>various substituents; R 4>a wide range of substituents. The full definitions are given in the DEFINITIONS (Full Definitions) Field. ACTIVITY : Antidiabetic; antiarthritic; antiinflammatory; immunosuppressive; osteopathic; antilipemic; antiarteriosclerosis; anabolic; cardiant; nephrotropic; antinfertility. MECHANISM OF ACTION : Inhibition of dipeptidylpeptidase-IV (DPPIV). The compound (R)-1,3-dimethyl-7-(3-methyl-2-buten-1-yl)-8-(3-aminopiperidin-1- yl)xanthine had IC50 against DDPIV expressed in Caco-2 cells of 22 nM.

94. 发明专利

AU2002234640B2 Xanthine derivative, production and use thereof as a medicament 未知
公开(公告)号：AU2002234640B2
公开(公告)日：2009-10-08
申请号：AU2002234640
申请日：2002-02-21
申请人： BOEHRINGER INGELHEIM PHARMA
发明人： HIMMELSBACH FRANK , MAIER ROLAND , ECKJARDT MATTHIAS , LOTZ RALF , MARK MICHAEL , LANGKOPF ELKE
IPC分类号： C07D473/04 , A61K31/522 , A61K31/55 , A61K31/551 , A61P3/04 , A61P3/10 , A61P5/00 , A61P19/02 , A61P19/10 , A61P37/02 , C07D473/06 , C07D473/08 , C07D473/10 , C07D473/12
摘要： 8-substituted-xanthine derivatives (I), their tautomers, enantiomers, diastereomers or mixtures, and salts. 8-substituted xanthine derivatives of formula (I), their tautomers, enantiomers, diastereomers or mixtures, and salts, are new: [Image] R 1>hydrogen; 1-8C alkyl; 3-8C alkenyl or alkynyl; 3-4C alkenyl substituted by 1-2C alkoxycarbonyl, aminocarbonyl (optionally substituted by 1 or 2 1-3C alkyl) or het-CO; 1-6C alkyl substituted by Ra; phenyl(1-6C)alkyl, optionally ring-substituted by R 1> 0>-R 1> 4>; phenyl(1-4C)alkyl, optionally substituted in alkyl by Rz and in the ring by R 1> 0>-R 1> 4>; R 1> 0>-R 1> 4>-substituted phenyl; phenyl(2-3C) alkenyl, phenyl (or naphthyl)-(CH 2) m-(A or B)-(CH 2) n, naphthyl(1-3C)alkyl or phenylcarbonylmethyl (all optionally ring-substituted by R 1> 0>-R 1> 4>); [1,4-napththoquinon-2-yl; chromen-4-on-3-yl; 1-oxo- or 1,3-dioxo-indan-2-yl; 2,3-dihydro-3-oxo-benzofuran-2-yl; heteroaryl-(CH 2) m-(A or B)-(CH 2) n; 1-6C alkyl-A-(CH 2) n; 3-7C cycloalkyl-(CH 2) m-A or B)-(CH 2) n; R 2> 1>-A-(CH 2) n; phenyl- or naphthyl-(CH 2) m-D-(1-3C)alkyl; Rb-substituted 2-6C alkyl, or 3-6C cycloalkyl; amino, or arylcarbonylamino; het : pyrrolidin-1-yl, piperidin-1-yl or morpholin-4-yl; R 1> 0>-R 1> 4>, Rb and Rz : various substituents; m : 0-2; n : 1-3; A, B and D : various linking groups; R 2>hydrogen or a wide range of substituents; R 3>various substituents; R 4>a wide range of substituents. The full definitions are given in the DEFINITIONS (Full Definitions) Field. ACTIVITY : Antidiabetic; antiarthritic; antiinflammatory; immunosuppressive; osteopathic; antilipemic; antiarteriosclerosis; anabolic; cardiant; nephrotropic; antinfertility. MECHANISM OF ACTION : Inhibition of dipeptidylpeptidase-IV (DPPIV). The compound (R)-1,3-dimethyl-7-(3-methyl-2-buten-1-yl)-8-(3-aminopiperidin-1- yl)xanthine had IC50 against DDPIV expressed in Caco-2 cells of 22 nM.

95. 发明专利

ES2324294T3 NUEVAS IMIDAZO-PIRIDINONAS E IMIDAZO-PIRIDAZINONAS SUSTITUIDAS, SU PREPARACION Y SU USO COMO MEDICAMENTOS. 未知
公开(公告)号：ES2324294T3
公开(公告)日：2009-08-04
申请号：ES03789123
申请日：2003-12-03
申请人： BOEHRINGER INGELHEIM PHARMA
发明人： HAUEL NORBERT , HIMMELSBACH FRANK , LANGKOPF ELKE , ECKHARDT MATTHIAS , MAIER ROLAND , MARK MICHAEL
IPC分类号： C07D487/04 , A61P5/48 , C07D471/04 , C07D519/00
摘要： Compuestos de la fórmula general ** ver fórmula** en la que significa X un átomo de nitrógeno o un grupo de la fórmula C-R 5 , significando R 5 un átomo de hidrógeno o un grupo metilo, R 1 un grupo cicloalquilenimino de 5 a 7 miembros que está sustituido en el esqueleto de carbonos con un grupo amino y que puede estar sustituido con un grupo alquilo C1-3, o un grupo amino sustituido con un grupo cicloalquilo C 5-7, estando el grupo cicloalquilo C5-7 sustituido con un grupo amino, o un átomo de carbono en la posición 3 del grupo cicloalquilo C5-7 está reemplazado por un grupo -NH, R 2 un grupo bencilo, en el que el radical fenilo puede estar sustituido con uno o dos átomos de flúor, cloro o bromo o con un grupo ciano, un grupo alquenilo C 3-8 lineal o ramificado, un grupo alquinilo C3-5, un grupo cicloalquil C3-7-metilo, un grupo cicloalquenil C5-7-metilo, o un grupo furilmetilo, tienilmetilo, pirrolilmetilo, tiazolilmetilo, imidazolilmetilo, piridinilmetilo, pirimidinilmetilo, piridazinilmetilo o pirazinilmetilo, R 3 un grupo alquilo C1-6 lineal o ramificado, un grupo fenil-alquilo C1-3 o naftil-alquilo C1-3, eventualmente sustituido en la parte de arilo con un átomo de halógeno, un grupo ciano, un grupo alquilo C 1-3 o un grupo metoxi, un grupo 2-fenil-2-hidroxi-etilo, un grupo fenilcarbonilmetilo, en el que el grupo fenilo puede estar sustituido con un grupo hidroxi, alquiloxi C1-3, aminocarbonil-alcoxi C1-3, (alquil C1-3-amino)-carbonil-alcoxi C1-3, [di-(alquil C1-3)-amino]-carbonil-alcoxi C1-3, amino, alquil C1-3-carbonilamino, cicloalquil C3-6-carbonilamino, alcoxi C1-3-carbonilamino, alquil C1-3-sulfonilamino o aminocarbonilo, un grupo (3-metil-2-oxo-2,3-dihidro-benzoxazolil)-carbonilmetilo, un grupo tienilcarbonilmetilo, un grupo heteroaril-alquilo C1-3, debiéndose entender por la expresión "grupo heteroarilo" un grupo heteroarilo monocíclico, de 5 o 6 miembros, eventualmente sustituido con uno o dos grupos alquilo C 1-3 o con un grupo morfolin-4-ilo, piridilo o fenilo, en donde el grupo heteroarilo de 6 miembros contiene uno, dos o tres átomos de nitrógeno, y el grupo heteroarilo de 5 miembros contiene un grupo imino, eventualmente sustituido con un grupo alquilo C 1-3 o fenil-alquilo C 1-3, un átomo de oxígeno o azufre, o un grupo imino, eventualmente sustituido con un grupo alquilo C1-3 o fenil-alquilo C1-3, o un átomo de oxígeno o azufre y, adicionalmente, un átomo de nitrógeno, o un grupo imino, eventualmente sustituido con un grupo alquilo C 1-3 o fenil-alquilo C 1-3, o un átomo de oxígeno o azufre y, adicionalmente, dos o tres átomos de nitrógeno, y, en donde, adicionalmente, a los grupos heteroarilo monocíclicos precedentemente mencionados puede estar condensado un anillo de fenilo a través de dos átomos de carbono contiguos, el cual puede estar eventualmente sustituido con un átomo de halógeno, con uno o dos grupos alquilo C1-3 o con un grupo trifluorometilo o metoxi, y el enlace puede realizarse a través de un átomo de la parte heterocíclica o del anillo de fenilo condensado, un grupo heteroarilmetilo bicíclico conforme a una de las fórmulas un grupo de la fórmula o un grupo de las fórmulas en las que R 6 significa en cada caso un átomo de hidrógeno o un grupo metilo, y R 4 un átomo de hidrógeno o un grupo alquilo C1-3, pudiendo los grupos alquilo y alcoxi contenidos en las definiciones, que presentan más de dos átomos de carbono, si no se mencionó de otro modo, ser de cadena lineal o ramificados, y en donde los átomos de hidrógeno de los grupos metilo o etilo contenidos en las definiciones estar reemplazados, en su totalidad o en parte, por átomos de flúor, con la condición de que estén excluidos los siguientes dos compuestos: 2-(2-amino-ciclohexilamino)-3-(but-2-inil)-5-metil-3,5-dihidro-imidazo[4,5-d]piridazin-4-ona y 2-(3-amino-piperidin-1-il)-3-(but-2-inil)-5-metil-3,5-dihidro-imidazo[4,5-d]piridazin-4-ona, sus tautómeros, sus enantiómeros, sus diastereoisómeros, sus mezclas y sus sales.

96. 发明专利

CA2368059C BICYCLIC HETEROCYCLES, PHARMACEUTICAL COMPOSITIONS CONTAINING THESE COMPOUNDS, THEIR USE AND PROCESSES FOR PREPARING THEM 未知
公开(公告)号：CA2368059C
公开(公告)日：2009-05-19
申请号：CA2368059
申请日：2000-03-14
申请人： BOEHRINGER INGELHEIM PHARMA
发明人： JUNG BIRGIT , HIMMELSBACH FRANK , BLECH STEFAN , LANGKOPF ELKE , SOLCA FLAVIO , METZ THOMAS
IPC分类号： C07D403/12 , A61K31/517 , A61K31/5355 , A61K31/5377 , A61K31/662 , A61P1/00 , A61P11/00 , A61P13/12 , A61P17/00 , A61P35/00 , C07D215/54 , C07D239/94 , C07D401/12 , C07D401/14 , C07D403/14 , C07D405/12 , C07D413/12
摘要： The present invention relates to bicyclic heterocyclic compounds of general formula (I), wherein R a to R d, A to D and X are defined as in claims 1 to 8, the tautomers, stereoisomers and salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases which have valuable pharmacological properties, particularly an inhibitory effect on signal transduction mediated by tyrosine kinases, their use in treating diseases, particularly tumour diseases, diseases of the lung and airways and the preparation thereof.

97. 发明专利

AT425979T 未知
公开(公告)号：AT425979T
公开(公告)日：2009-04-15
申请号：AT03789123
申请日：2003-12-03
申请人： BOEHRINGER INGELHEIM PHARMA
发明人： HAUEL NORBERT , HIMMELSBACH FRANK , LANGKOPF ELKE , ECKHARDT MATTHIAS , MAIER ROLAND , MARK MICHAEL , TADAYYON MOHAMMAD , KAUFFMANN-HEFNER IRIS
IPC分类号： C07D487/04 , A61P5/48 , C07D471/04 , C07D519/00

98. 发明专利

DE602005009745D1 未知
公开(公告)号：DE602005009745D1
公开(公告)日：2008-10-23
申请号：DE602005009745
申请日：2005-12-15
申请人： BOEHRINGER INGELHEIM PHARMA
发明人： ECKHARDT MATTHIAS , HIMMELSBACH FRANK , EICKELMANN PETER , BARSOUMIAN EDWARD LEON , THOMAS LEO
IPC分类号： C07H7/04 , A61K31/7042
摘要： Glucopyranosyl-substituted benzene derivatives defined according to claim 1, including the tautomers, the stereoisomers thereof, the mixtures thereof and the salts thereof. The compounds according to the invention are suitable for the treatment of metabolic disorders.

99. 发明专利

DE50309979D1 未知
公开(公告)号：DE50309979D1
公开(公告)日：2008-07-24
申请号：DE50309979
申请日：2003-08-16
申请人： BOEHRINGER INGELHEIM PHARMA
发明人： HIMMELSBACH FRANK , ECKHARDT MATTHIAS , LANGKOPF ELKE , LOTZ RALF R , MAIER ROLAND , MARK MICHAEL
IPC分类号： C07D473/30 , A61K31/52 , A61K31/522 , A61P3/10 , A61P19/10 , A61P29/00 , C07D473/38

100. 发明专利

NO325672B1 未知
公开(公告)号：NO325672B1
公开(公告)日：2008-07-07
申请号：NO20032726
申请日：2003-06-16
申请人： BOEHRINGER INGELHEIM PHARMA
发明人： HIMMELSBACH FRANK , LANGKOPF ELKE , SOLCA FLAVIO , BLECH STEFAN , BAUM ELKE , JUNG BIRGIT
IPC分类号： C07D239/94 , A61K31/517 , A61K31/5377 , A61P1/00 , A61P1/04 , A61P1/16 , A61P11/00 , A61P11/06 , A61P11/08 , A61P17/06 , A61P27/16 , A61P29/00 , A61P35/00 , A61P35/04 , A61P37/02 , A61P37/08 , A61P43/00 , C07D405/12
摘要： 4-Amino-6-(4-amino-1-oxo-but-2-enylamino)-quinazoline derivatives (I) are new. 4-Amino-6-(4-amino-1-oxo-but-2-enylamino)-quinazoline derivatives of formula (I) and their tautomers, stereoisomers and salts are new. [Image] R abenzyl, 1-phenylethyl or 3-chloro-4-fluorophenyl; R bdimethylamino, N-methyl-N-ethylamino, Diethylamino, N-methyl-N-isopropylamino, N-methyl-N-cyclopropylamino, N-methyl-N-(2-methoxyethyl)-amino, N-ethyl-N-(2-methoxyethyl)-amino, bis-(2-methoxyethyl)-amino, morpholino, N-methyl-N-(tetrahydrofuran-3-yl)-amino, N-methyl-N-(tetrahydrofuran-2-yl-methyl)-amino, N-methyl-N-(tetrahydrofuran-3-yl-methyl)-amino, N-methyl-N-(tetrahydropyran-4-yl)-amino or N-methyl-N-(tetrahydropyran-4-ylmethyl)-amino; R ccyclopropylmethoxy, cyclobutyloxy, cyclopentyloxy, tetrahydrofuran-3-yloxy, tetrahydrofuran-2-yl-methoxy, tetrahydrofuran-3-yl-methoxy, tetrahydropyran-4-yloxy or tetrahydropyran-4-ylmethoxy; and provided the following compounds are excluded: (1) 4-((3-chloro-4-fluorophenyl)-amino)-6-((4-(N,N-diethylamino)-1-oxo-2-buten-1-yl)-amino)-7-cyclopropylmethoxy-quinazoline; (2) 4-((3-chloro-4-fluorophenyl)-amino)-6-((4-(morpholin-4-yl)-1-oxo-2-buten-1-yl)-amino)-7-cyclopropylmethoxy-quinazoline; (3) 4-((3-chloro-4-fluorophenyl)-amino)-6-((4-(dimethylamino)-1-oxo-2-buten-1-yl)-amino)-7-cyclopropylmethoxy-quinazoline; (4) 4-((3-chloro-4-fluorophenyl)-amino)-6-((4-(morpholin-4-yl)-1-oxo-2-buten-1-yl)-amino)-7-cyclobutyloxy-quinazoline; (5) 4-((3-chloro-4-fluorophenyl)-amino)-6-((4-(morpholin-4-yl)-1-oxo-2-buten-1-yl)-amino)-7-cyclopentyloxy-quinazoline; (6) 4-((3-chloro-4-fluorophenyl)-amino)-6-((4-(diethylamino)-1-oxo-2-buten-1-yl)-amino)-7-cyclobutyloxy-quinazoline; (7) 4-((3-chloro-4-fluorophenyl)-amino)-6-((4-(diethylamino)-1-oxo-2-buten-1-yl)-amino)-7-cyclopentyloxy-quinazoline; (8) 4-((R)-(1-phenyl-ethyl)-amino)-6-((4-(morpholin-4-yl)-1-oxo-2-buten-1-yl)-amino)-7-cyclobutyloxy-quinazoline; (9) 4-((R)-(1-phenyl-ethyl)-amino)-6-((4-(morpholin-4-yl)-1-oxo-2-buten-1-yl)-amino)-7-cyclopropylmethoxy-quinazoline; (10) 4-((R)-(1-phenyl-ethyl)-amino)-6-((4-(morpholin-4-yl)-1-oxo-2-buten-1-yl)-amino)-7-cyclopentyloxy-quinazoline; (11) 4-((R)-(1-phenyl-ethyl)-amino)-6-((4-(diethylamino)-1-oxo-2-buten-1-yl)-amino)-7-cyclobutyloxy-quinazoline; (12) 4-((R)-(1-phenyl-ethyl)-amino)-6-((4-(diethylamino)-1-oxo-2-buten-1-yl)-amino)-7-cyclopentyloxy-quinazoline; (13) 4-((R)-(1-phenyl-ethyl)-amino)-6-((4-(diethylamino)-1-oxo-2-buten-1-yl)-amino)-7-cyclopropylmethoxy-quinazoline; (14) 4-((3-chloro-4-fluorophenyl)-amino)-6-((4-(bis-(2-methoxyethyl)-amino)-1-oxo-2-buten-1-yl)-amino)-7-cyclopropylmethoxy-quinazoline; (15) 4-((3-chloro-4-fluorophenyl)-amino)-6-((4-(N-ethyl-N-(2-methoxyethyl)-amino)-1-oxo-2-buten-1-yl)-amino)-7-cyclopropylmethoxy-quinazoline; (16) 4-((3-chloro-4-fluorophenyl)-amino)-6-((4-(N-methyl-N-(tetrahydropyran-4-yl)-amino)-1-oxo-2-buten-1-yl)-amino)-7-cyclopropylmethoxy-quinazoline; (17) 4-((3-chloro-4-fluorophenyl)-amino)-6-((4-(diethylamino)-1-oxo-2-buten-1-yl)-amino)-7-(tetrahydrofuran-2-yl)-methoxy)-quinazoline; (18) 4-((3-chloro-4-fluorophenyl)-amino)-6-((4-(diethylamino)-1-oxo-2-buten-1-yl)-amino)-7-(tetrahydrofuran-3-yl)-oxy)-quinazoline; (19) 4-((3-chloro-4-fluorophenyl)-amino)-6-((4-(diethylamino)-1-oxo-2-buten-1-yl)-amino)-7-(tetrahydropyran-4-yl)-oxy)-quinazoline; (20) 4-((3-chloro-4-fluorophenyl)-amino)-6-((4-(N-methyl-N-(tetrahydrofuran-2-yl-methyl)-amino)-1-oxo-2-buten-1-yl)-amino)-7-cyclopropylmethoxy-quinazoline; and (21) 4-((3-chloro-4-fluorophenyl)-amino)-6-((4-(N-methyl-N-(tetrahydrofuran-3-yl)-amino)-1-oxo-2-buten-1-yl)-amino)-7-cyclopropylmethoxy-quinazoline. An independent claim is included for the preparation of (I). ACTIVITY : Cytostatic; Respiratory; Gastrointestinal; Antiinflammatory; Antiasthmatic; Antiallergic; Antitussive; Antiulcer; Immunosuppressive; Antipsoriatic. MECHANISM OF ACTION : Tyrosine kinase-mediated signal transduction inhibitor. In a test, 4-((3-Chloro-4-fluorophenyl)-amino)-6-((4-(N,N-dimethylamino)-1-oxo-2-buten-1-yl)-amino)-7-((S)-(tetrahydrofuran-2-yl)-methoxy)-quinazoline (Ia) had IC 5 0 value 0.3 MicroM for inhibition of human EGF-receptor kinase.

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