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公开(公告)号:AU2306295A
公开(公告)日:1995-11-10
申请号:AU2306295
申请日:1995-04-13
Applicant: GLAXO INC
Inventor: AQUINO CHRISTOPHER JOSEPH , DEZUBE MILANA , HENKE BRAD RICHARD , BRACKEEN MARCUS , JEFFS PETER WALTER , SUH EDWARD MARTIN , HIRST GAVIN CHARLES , SUGG ELIZABETH ELLEN , WILLSON TIMOTHY MARK , MOMTAHEN TANYA
IPC: A61K31/55 , A61P1/00 , A61P1/16 , A61P3/04 , C07D243/12 , C07D401/04 , C07D401/14 , C07D403/06 , C07D405/06 , C07D409/06 , C07D409/14 , C07D413/06 , C07D471/04 , C07D498/04
Abstract: PCT No. PCT/EP95/01336 Sec. 371 Date Nov. 14, 1996 Sec. 102(e) Date Nov. 14, 1996 PCT Filed Apr. 13, 1995 PCT Pub. No. WO95/28391 PCT Pub. Date Oct. 26, 1995 (I) Benzo[b][1,4]diazepine compounds of formula (I), where R1 is selected from C1C6alkyl, C3-C6cycloalkyl, phenyl, or substituted phenyl; R2 is selected from C3-C6alkyl, C3C6cycloalkyl, C3-C6alkenyl, benzyl, phenylC1-C3alkyl of substituted phenyl; or NR1R2 together form 1,2,3,4-tetrahydroquinoline or benzazepine, mono-, di-, or trisubstituted independently with C1-6alkyl C1-6alkoxy or halogen substituents; p is an integer 0 or 1; q is an integer 0 or 1; r is an integer 0 or 1; t is an integer 0 or 1, provided that when r is 0 then t is 0; R3, R5, and R6 are independently hydrogen or C1-6alkyl; R4 is C1-6alkyl or C1-6alkenyl; R7 is selected from the group consisting of hydrogen, C1-6alkyl, C1-6cycloalkyl, C1-6alkenyl, phenyl, substituted phenyl, napthyl, heteroaryl, substituted heteroaryl, bicycloheteroaryl or substituted bicycloheteroaryl; or NR6R7 together form a saturated 5,6, or 7 membered ring optionally interrupted by 1,2,3 or 4 N, S or O heteroatoms, with the proviso that any two O or S atoms are not bonded to each other, m is an integer selected from the group of 0, 1, 2, 3 or 4; R8 and R9 are selected from a variety of substituents; Z is hydrogen or halogen; novel intermediates, a pharmaceutical composition for treating obesity, gall bladder stasis, disorders of pancreatic secretion, methods for such treatment and processes for preparing compounds of formula (I).
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公开(公告)号:ZA9503111B
公开(公告)日:1996-01-23
申请号:ZA9503111
申请日:1995-04-18
Applicant: GLAXO INC
Inventor: AQUINO CHRISTOPHER JOSEPH , DEZUBE MILANA , SUGG ELIZABETH ELLEN , SHERRILL RONALD GEORGE , WILLSON TIMOTHY MARK , SZEWCZYK JERZY RYSZARD
IPC: A61K20060101 , C07D20060101 , C07D , A61K
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公开(公告)号:PE50594A1
公开(公告)日:1995-01-06
申请号:PE24002894
申请日:1994-04-13
Applicant: GLAXO INC
Inventor: AQUINO CHRISTOPHER JOSEPH , SUGG ELIZABETH ELLEN , CARR ROBIN ARTHUR ELLIS , SZEWCZYK JERZY RYSZARD , FINCH HARRY
IPC: A61K38/00 , A61K31/55 , C07D243/12 , A61K31/551 , A61K38/02 , A61P3/00 , A61P5/00 , A61P43/00 , C07K5/02 , C07K5/06 , C07K5/078 , C07K5/08 , C07K5/097
Abstract: SE REFIERE A UN COMPUESTO DE FORMULA I DONDE: 1) X ES H, -CF3, ALQUILO, ALQUILTIO C1-C4, -O(ALQUILO(C1-C4)), HALOGENO; 2) R1 ES LA FORMULA II o -NR4R5 DONDE R4 ES PROPILO, ISOPROPILO, R5 ES FENILO, FENILO SUSTITUIDO EN LA POSICION PARA POR OH, OCH3, F; 3) R2 ES UN HETEROCICLO COMO PIRROL, TETRAHIDROPIRROL, INDOL, BENZOFURANO, FENILO, PIRIDINA, -NHR11 DONDE R11 ES 7-INDAZOLILO, FENILO Y OTROS; 4) R3 ES H, ALQUILO C1-C6, CICLOALQUILO C3-C6, FENILO O FENILO MONO O DISUSTITUIDO CON HALOGENOS; 5) R6 ES H, CH3; 6) R7 ES H, OH, F, DIMETILAMINO, -O(ALQUILO C1-C4), -O(CH2-C6H5); EL CUAL ES AGONISTA PARA EL RECEPTOR CCK-A, MODULANDO LAS HORMONAS GASTRINA Y COLECISTOCININA (CCK), PUDIENDO USARSE EN LA REGULACION DEL APETITO, TRATAR LA OBESIDAD Y MANTENER LA PERDIDA DE PESO
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公开(公告)号:ZA9503056B
公开(公告)日:1996-01-30
申请号:ZA9503056
申请日:1995-04-13
Applicant: GLAXO INC
Inventor: AQUINO CHRISTOPHER JOSEPH , DEZUBE MILANA , HENKE BRAD RICHARD , BRACKEEN MARCUS , JEFFS PETER WALTER , SUH EDWARD MARTIN , HIRST GAVIN CHARLES , SUGG ELIZABETH ELLEN , WILLSON TIMOTHY MARK , MOMTAHEN TANYA
IPC: A61K20060101 , C07D20060101 , C07D , A61K
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公开(公告)号:ZA953111B
公开(公告)日:1996-01-23
申请号:ZA953111
申请日:1995-04-18
Applicant: GLAXO INC
Inventor: AQUINO CHRISTOPHER JOSEPH , DEZUBE MILANA , SUGG ELIZABETH ELLEN , SHERRILL RONALD GEORGE , WILLSON TIMOTHY MARK , SZEWCZYK JERZY RYSZARD
IPC: A61K20060101 , C07D20060101 , C07D , A61K
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公开(公告)号:AU2446295A
公开(公告)日:1995-11-10
申请号:AU2446295
申请日:1995-04-13
Applicant: GLAXO INC
Inventor: AQUINO CHRISTOPHER JOSEPH , DEZUBE MILANA , SUGG ELIZABETH ELLEN , SHERRILL RONALD GEORGE , WILLSON TIMOTHY MARK , SZEWCZYK JERZY RYSZARD
IPC: C07D243/14 , A61K31/55 , A61K31/551 , A61K31/5513 , A61P1/00 , A61P1/16 , A61P3/04 , A61P25/00 , A61P43/00 , C07D243/24 , C07D401/04 , C07D403/06 , C07D403/12 , C07D487/04
Abstract: PCT No. PCT/EP95/01335 Sec. 371 Date Oct. 11, 1996 Sec. 102(e) Date Oct. 11, 1996 PCT Filed Apr. 13, 1995 PCT Pub. No. WO95/28399 PCT Pub. Date Oct. 26, 1995A method of inducing a Cholescystokinin-A receptor agonist response in a mammal by administering a compound of formula (I), (I) where R1 is C1-C6alkyl, C3-6cycloalkyl, phenyl, or substituted phenyl; R2 is C3-6alkyl, C3-6cycloalkyl, C3-6alkenyl, benzyl, phenylC1-3alkyl or substituted phenyl; or NR1R2 together form 1,2,3,4-tetrahydroquinoline or benzazepine mono-, di-, or trisubstituted independently with C1-6alkyl, C1-6alkoxy or halogen substituents; n is an integer selected from the grouping consisting of 0,1,2 or 3; p is the integer 0 or 1; q is the integer 0 or 1; r is the integer 0 or 1, provided that when q is 0 then r is 0; R3, R4, R5 and R8 are selected from a variety of substituents; X is nitrogen, nitroso or R8; m is an integer selected from the group consisting of 0, 1, 2 or 3; Y and Z are hydrogen or halogen, novel intermediates, a pharmaceutical composition for treating obesity, gall bladder stasis, disorders of pancreatic secretion, methods for such treatment and processes for preparing compounds of formula (I).
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公开(公告)号:ZA953005B
公开(公告)日:1996-03-20
申请号:ZA953005
申请日:1995-04-12
Applicant: GLAXO INC
IPC: A61K20060101 , C07K20060101 , C07K , A61K
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公开(公告)号:ZA9503005B
公开(公告)日:1996-03-20
申请号:ZA9503005
申请日:1995-04-12
Applicant: GLAXO INC
IPC: A61K20060101 , C07K20060101 , C07K , A61K
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公开(公告)号:ECSP941065A
公开(公告)日:1994-12-15
申请号:ECSP941065
申请日:1994-04-12
Applicant: GLAXO INC
Inventor: SUGG ELIZABETH E , AQUINO CHRISTOPHER JOSEPH , DEZUBE MILANA , HENKE BRAD RICHARD , BRACKEEN MARCUS , JEFFS PETER WALTER , SUH EDWARD MARTIN , HIRST GAVIN CHARLES , WILLSON TIMOTHY MARK , MOMTAHEN TANYA
IPC: A61K20060101 , A61K38/00 , C07D20060101
Abstract: Novedosos como el proceso para su preparación, con las composiciones farmacéuticas que los contienen y con su uso en medicina, más particularmente, se relaciona con compuestos que exhiben actividad egonista para los receptores de CCK-A permitiéndoles por tanto modular las hormonas gastrina y colecistocinina en mamíferos.
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公开(公告)号:ZA942570B
公开(公告)日:1994-11-11
申请号:ZA942570
申请日:1994-04-14
Applicant: GLAXO INC
Inventor: SUGG ELIZABETH ELLEN , AQUINO CHRISTOPHER JOSEPH , SZEWCZYK JERZY RYSZARD , FINCH HARRY , CARR ROBIN ARTHUR ELLIS
IPC: A61K31/551 , A61K38/02 , A61K38/00 , A61P3/00 , A61P5/00 , A61P43/00 , C07D243/12 , C07K5/02 , C07K5/06 , C07K5/078 , C07K5/08 , C07K5/097 , C07K , A61K
Abstract: PCT No. PCT/EP94/01130 Sec. 371 Date Oct. 30, 1995 Sec. 102(e) Date Oct. 30, 1995 PCT Filed Apr. 13, 1994 PCT Pub. No. WO94/24151 PCT Pub. Date Oct. 27, 1994The present invention relates to compounds of general formula (I) (I) and physiologically acceptable salts thereof wherein the group NR1R2 represents a 5-7 membered saturated heterocyclic ring which may be substituted by one or two methyl groups; R3 is C1-6alkyl, C3-6cycloalkyl or phenyl optionally substituted by 1 or 2 halogen atoms; R4 is phenyl or phenyl substituted by one or two groups selected from the group consisting of halogen, C1-4alkyl, trifluoromethyl, trifluoromethoxy or (CH2)nR5 wherein n is zero or 1 and R5 represents C1-4alkoxy, hydroxy, nitro, cyano, CO2R6, S(O)pCH3, NR7R8, CONR7R8, SO2NR7CO(C1-4)alkyl, tetrazolyl, carboxamidotetrazolyl, or a 3-trifluoromethyl 1,2,4-triazolyl; R6 is hydrogen, C1-4alkyl or benzyl; R7 is hydrogen or C1-4alkyl, R8 is hydrogen, C1-4alkyl, SO2CH3 or SO2CF3, X represent hydrogen, C1-4alkyl or halogen; m is zero, 1 or 2, and p is zero, 1 or 2. The invention also relates to processes for preparation of these compounds and to their use in medicine as antagonists of gastrin and CCK.
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