公开(公告)号：US20070015207A1

公开(公告)日：2007-01-18

申请号：US11329642

申请日：2006-01-11

申请人： Donald Ludovici ,  Richard Connors ,  Steven Coats ,  Li Liu ,  Bart De Corte ,  Dana Johnson ,  Mark Schulz

发明人： Donald Ludovici ,  Richard Connors ,  Steven Coats ,  Li Liu ,  Bart De Corte ,  Dana Johnson ,  Mark Schulz

IPC分类号： G01N33/53 ,  C07H21/04 ,  C12P21/06 ,  C12N5/06 ,  C07D487/02 ,  C07K16/40 ,  C12N9/12

CPC分类号： C07K14/4738 ,  C07D487/04 ,  C12N9/1205 ,  C12Q1/485 ,  G01N2500/02

摘要： The invention relates to the discovery of triazolopyrimidine derivatives of formula (I), which have been found to exhibit inhibitory activity against the serine-tyrosine and tyrosine kinases.

摘要翻译： 本发明涉及已发现对丝氨酸 - 酪氨酸和酪氨酸激酶具有抑制活性的式（I）三唑并嘧啶衍生物的发现。

公开(公告)号：US20060009474A1

公开(公告)日：2006-01-12

申请号：US11225839

申请日：2005-09-13

申请人： Michael Kukla ,  Donald Ludovici ,  Robert Kavash ,  Bart De Corte ,  Jan Heeres ,  Paul Janssen ,  Lucien Koymans ,  Marc de Jonge ,  Koen Van Aken ,  Alain Krief

发明人： Michael Kukla ,  Donald Ludovici ,  Robert Kavash ,  Bart De Corte ,  Jan Heeres ,  Paul Janssen ,  Lucien Koymans ,  Marc de Jonge ,  Koen Van Aken ,  Alain Krief

IPC分类号： A61K31/519 ,  C07D487/02 ,  A61K31/506 ,  C07D239/42

CPC分类号： C07D239/47 ,  C07D239/48 ,  C07D401/12

摘要： The present invention concerns compounds of formula (A1)(A2)N—R1 (I), the N-oxide forms, the pharmaceutically acceptable addition salts, the quaternary amines and stereochemically isomeric forms thereof, wherein R1 is substituted C1-6alkyl; —S(═O)—R8; —S(═O)2—R8; C7-12alkylcarbonyl; optionally substituted C1-6alkyloxycarbonylC1-6alkylcarbonyl; with R8 being C1-6alkyl, aryl1 or Het1; (A1)(A2)N— is the covalently bonded form of the corresponding intermediate of formula (A1)(A2)N—H, which is a HIV replication inhibiting pyrimidine of formula

摘要翻译： 本发明涉及式（A 1 _{1）（A 2 N）NR 1（I）的化合物，N-氧化物形式，药学上 可接受的加成盐，季胺和其立体化学异构形式，其中R 1是取代的C 1-6烷基; -S（-O）-R 8; -S（-O）2 -R 8; C 12-12烷基羰基; 任选取代的C 1-6烷氧基羰基C 1-6烷基羰基; 其中R 8是C 1-6烷基，芳基1或Het 1; （A 1 N 2）（A 2 N）N-是式（A 1 SUB）的相应中间体的共价键合形式（A 2）NH，其是具有下式的HIV复制抑制性嘧啶}

公开(公告)号：US20050288278A1

公开(公告)日：2005-12-29

申请号：US11204513

申请日：2005-08-16

申请人： Bart De Corte ,  Marc De Jonge ,  Jan Heeres ,  Chih Ho ,  Paul Janssen ,  Robert Kavash ,  Lucien Koymans ,  Michael Kukla ,  Donald Ludovici ,  Koen Van Aken

发明人： Bart De Corte ,  Marc De Jonge ,  Jan Heeres ,  Chih Ho ,  Paul Janssen ,  Robert Kavash ,  Lucien Koymans ,  Michael Kukla ,  Donald Ludovici ,  Koen Van Aken

IPC分类号： C07D239/47 ,  A61K20060101 ,  A61K31/505 ,  A61K31/506 ,  A61K31/513 ,  A61K31/551 ,  A61K31/5513 ,  A61K31/675 ,  A61K31/715 ,  A61P31/18 ,  C07D20060101 ,  C07D239/42 ,  C07D239/46 ,  C07D239/48 ,  C07D239/50 ,  C07D239/80 ,  C07D401/12 ,  C07D403/12

CPC分类号： A61K31/505 ,  A61K31/5513

摘要： This invention concerns the use of compounds of formula the N-oxides, the pharmaceutically acceptable addition salts, quaternary amines and the stereochemically isomeric forms thereof, wherein -a1=a2-a3=a4- forms a phenyl, pyridinyl, pyrimidinyl, pyridazinyl or pyrazinyl with the attached vinyl group; n is 0 to 4; and where possible 5; R1 is hydrogen, aryl, formyl, C1-6alkylcarbonyl, C1-6alkyl, C1-6alkyloxy-carbonyl, substituted C1-6alkyl, or substituted C1-6alkyloxyC1-6alkylcarbonyl; each R2 independently is hydroxy, halo, optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl, C3-7cycloalkyl, C1-6alkyloxy, C1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalo-methylthio, —S(═O)pR6, —NH—S(═O)pR6, —C(═O)R6, —NHC(═O)H, —C(═O)NHNH2, —NHC(═O)R6, —C(═NH)R6 or a 5-membered heterocyclic ring; p is 1 or 2; L is optionally substituted C1-10alkyl, C2-10alkenyl, C2-10alkynyl or C3-7cycloalkyl; or L is —X—R3 wherein R3 is optionally substituted phenyl, pyridinyl, pyrimidinyl, pyrazinyl or pyridazinyl; X is —NR1—, —NH—NH—, —N═N—, —O—, —C(═O)—, —CHOH—, —S—, —S(═O)— or —S(═O)2—; Q is hydrogen, C1-6alkyl, halo, polyhalo-C1-6alkyl or an optionally substituted amino group; Y represents hydroxy, halo, C3-7cycloalkyl, optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl, C1-6alkyloxy, C1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, —S(═O)pR6, —NH—S(═O)pR6, —C(═O)R6, —NHC(═O)H, —C(═O)NHNH2, —NHC(═O)R6, —C(═NH)R6 or aryl; aryl is optionally substituted phenyl. Het is an optionally substituted heterocyclic radical; for the manufacture of a medicine for the treatment of subjects suffering from HIV (Human Immunodeficiency Virus) infection.

公开(公告)号：US20050277641A1

公开(公告)日：2005-12-15

申请号：US10649017

申请日：2003-08-27

申请人： Bart De Corte ,  Marc de Jonge ,  Jan Heeres ,  Paul Janssen ,  Robert Kavash ,  Lucien Koymans ,  Michael Kukla ,  Donald Ludovici ,  Koen Van Aken

发明人： Bart De Corte ,  Marc de Jonge ,  Jan Heeres ,  Paul Janssen ,  Robert Kavash ,  Lucien Koymans ,  Michael Kukla ,  Donald Ludovici ,  Koen Van Aken

IPC分类号： C07D251/46 ,  A61K9/14 ,  A61K31/53 ,  A61P31/18 ,  C07D251/16 ,  C07D251/18 ,  C07D251/48 ,  C07D43/02

CPC分类号： A61K9/146 ,  Y10S977/775 ,  Y10S977/915

摘要： This invention concerns the use of the compounds of formula the N-oxides, the pharmaceutically acceptable addition salts, quaternary amines and the stereochemically isomeric forms thereof, wherein −a1=a2−a3=a4—forms a phenyl, pyridinyl, pyrimidinyl, pyridazinyl or pyrazinyl with the attached vinyl group; n is 0 to 4; and where possible 5; R1 is hydrogen, aryl, formyl, C1-6alkylcarbonyl, C1-6alkyl, C1-6alkyloxycarbonyl or substituted C1-6alkyl; each R2 independently is hydroxy, halo, optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl, C3-7cycloalkyl, C1-6alkyloxy, C1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, —S(═O)pR4, —NH—S(═O)pR4, —C(═O)R4, —NHC(═O)H, —C(═O)NHNH2, —NHC(═O)R4, —C(═NH)R4 or a 5-membered heterocyclic ring; p is 1 or 2; L is optionally substituted C1-10alkyl, C2-10alkenyl, C2-10alkynyl or C3-7cycloalkyl; or L is —X—R3 wherein R3 is optionally substituted phenyl, pyridinyl, pyrimidinyl, pyrazinyl or pyridazinyl; X is —NR1—, —NH—NH—, —N═N—, —O—, —C(═O)—, —CHOH—, —S—, —S(═O)— or —S(═O)2—; aryl is optionally substituted phenyl; for the manufacture of a medicine for the treatment of subjects suffering from HIV (Human Immunodeficiency Virus) infection.

公开(公告)号：US20050192305A1

公开(公告)日：2005-09-01

申请号：US11111400

申请日：2005-04-21

申请人： Koenraad Jozef Andries ,  Bart De Corte ,  Marc De Jonge ,  Jan Heeres ,  Chih Ho ,  Marcel Janssen ,  Paul Janssen ,  Lucien Koymans ,  Michael Kukla ,  Donald Ludovici ,  Koen Van Aken

发明人： Koenraad Jozef Andries ,  Bart De Corte ,  Marc De Jonge ,  Jan Heeres ,  Chih Ho ,  Marcel Janssen ,  Paul Janssen ,  Lucien Koymans ,  Michael Kukla ,  Donald Ludovici ,  Koen Van Aken

IPC分类号： C07D239/42 ,  C07D239/46 ,  C07D239/48 ,  C07D239/50 ,  C07D401/12 ,  A61K31/506 ,  C07D43/14

CPC分类号： C07D239/42 ,  C07D239/47 ,  C07D239/48 ,  C07D239/49 ,  C07D239/50 ,  C07D401/12

摘要： This invention concerns the use of the compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein A is CH, CR4 or N; n is 0 to 4; Q is hydrogen or —NR1R2; R1 and R2 are selected from hydrogen, hydroxy, C1-12alkyl, C1-12alkyloxy, C1-12alkylcarbonyl, C1-12alkyloxycarbonyl, aryl, amino, mono- or di(C1-12alkyl)-amino, mono- or di(C1-12alkyl)aminocarbonyl wherein each C1-12alkyl may optionally be substituted: or R1 and R2 taken together may form pyrrolidinyl, piperidinyl, morpholinyl, azido or mono- or di(C1-12alkyl)aminoC1-4alkylidene; R3 is hydrogen, aryl, C1-6alkylcarbonyl, optionally substituted C1-6alkyl, C1-6alkyloxy-carbonyl,; and R4 is hydroxy, halo, optionally substituted C1-6alkyl, C1-6alkyloxy, cyano, aminocarbonyl, nitro, amino, trihalomethyl, trihalomethyloxy; R5 is hydrogen or C1-4alkyl; L is optionally substituted C1-10alkyl, C3-10alkenyl, C3-10alkynyl, C3-7cycloalkyl: or L is —X1—R6 or —X2-Alk-R7 wherein R6 and R7 are optionally substituted phenyl; X1 and X2 are —NR3—, —NH—NH—, —N═N—, —O—, —S—, —S(═O)— or —S(═O)2—; Alk is C1-4alkanediyl; aryl is potionally substituted phenyl; Het is an optionally substituted aliphatic or aromatic heterocyclic radical: for the manufacture of a medicine for the treatment of subjects suffering from HIV (Human Immunodeficiency Virus) infection. It further relates to new compounds being a subgroup of the compounds of formula (I), their preparation and compositions comprising them.

公开(公告)号：US20050197354A1

公开(公告)日：2005-09-08

申请号：US11111358

申请日：2005-04-21

申请人： Koenraad Jozef Andries ,  Bart De Corte ,  Marc De Jonge ,  Jan Heeres ,  Chih Ho ,  Marcel Janssen ,  Paul Janssen ,  Lucien Koymans ,  Michael Kukla ,  Donald Ludovici ,  Koen Van Aken

发明人： Koenraad Jozef Andries ,  Bart De Corte ,  Marc De Jonge ,  Jan Heeres ,  Chih Ho ,  Marcel Janssen ,  Paul Janssen ,  Lucien Koymans ,  Michael Kukla ,  Donald Ludovici ,  Koen Van Aken

IPC分类号： C07D239/42 ,  C07D239/46 ,  C07D239/48 ,  C07D239/50 ,  C07D401/12 ,  A61K31/506 ,  C07D43/02

CPC分类号： C07D239/42 ,  C07D239/47 ,  C07D239/48 ,  C07D239/49 ,  C07D239/50 ,  C07D401/12

摘要： This invention concerns the use of the compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein A is CH, CR4 or N; n is 0 to 4; Q is hydrogen or —NR1R2; R1 and R2 are selected from hydrogen, hydroxy, C1-12alkyl, C1-12alkyloxy, C1-12alkylcarbonyl, C1-12alkyloxycarbonyl, aryl, amino, mono- or di(C1-12alkyl)-amino, mono- or di(C1-12alkyl)aminocarbonyl wherein each C1-12alkyl may optionally be substituted; or R1 and R2 taken together may form pyrrolidinyl, piperidinyl, morpholinyl, azido or mono- or di(C1-12alkyl)aminoC1-4alkylidene; R3 is hydrogen, aryl. C1-6alkylcarbonyl, optionally substituted C1-6alkyl, C1-6alkyloxy-carbonyl; and R4 is hydroxy, halo, optionally substituted C1-6alkyl, C1-6alkyloxy, cyano, aminocarbonyl, nitro, amino, trihalomethyl, trihalomethyloxy; R5 is hydrogen or C1-4alkyl; L is optionally substituted C1-10alkyl, C3-10alkenyl, C3-10alkynyl, C3-7cycloalkyl; or L is —X1—R6 or —X2-Alk-R7 wherein R6 and R7 are optionally substituted phenyl; X1 and X2 are —NR3—, —NH—NH—, —N═N—, —O—, —S—, —S(═O)— or —S(═O)2—; Alk is C1-4alkanediyl; aryl is potionally substituted phenyl; Het is an optionally substituted aliphatic or aromatic heterocyclic radical; for the manufacture of a medicine for the treatment of subjects suffering from HIV (Human Immunodeficiency Virus) infection. It further relates to new compounds being a subgroup of the compounds of formula (I), their preparation and compositions comprising them.

公开(公告)号：US20070142305A1

公开(公告)日：2007-06-21

申请号：US11657912

申请日：2007-01-25

申请人： Chih Ho ,  Bengt Brunmark ,  Stuart Emanuel ,  Robert Galemmo ,  Dana Johnson ,  Donald Ludovici ,  Umar Maharoof ,  Jay Mei ,  Jan Sechler ,  Eric Strobel ,  Robert Tuman ,  Hwa Yen

发明人： Chih Ho ,  Bengt Brunmark ,  Stuart Emanuel ,  Robert Galemmo ,  Dana Johnson ,  Donald Ludovici ,  Umar Maharoof ,  Jay Mei ,  Jan Sechler ,  Eric Strobel ,  Robert Tuman ,  Hwa Yen

IPC分类号： A61K31/7052 ,  A61K31/5377 ,  A61K31/496 ,  A61K31/454 ,  A61K31/4439 ,  A61K31/4162 ,  C07D413/02 ,  C07D403/02

CPC分类号： C07F9/65038 ,  C07D231/54 ,  C07D231/56 ,  C07D233/64 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D405/04 ,  C07D405/12 ,  C07D413/12 ,  C07D491/04 ,  C07D495/04

摘要： The invention is directed to N-substituted tricyclic 3-AMINOPYRAZOLE derivatives, which are useful as inhibitors of platelet-derived growth factor receptor (PDGF-R) kinase, and methods for the preparation of said derivatives. The present invention is further directed to pharmaceutical compositions comprising the compounds of the present invention and to methods for treating conditions such as tumors and other cell. proliferative disorders.

摘要翻译： 本发明涉及可用作血小板衍生生长因子受体（PDGF-R）激酶抑制剂的N-取代三环3-氨基吡唑衍生物，以及制备所述衍生物的方法。 本发明还涉及包含本发明化合物的药物组合物和用于治疗诸如肿瘤和其它细胞的病症的方法。 增生性疾病

公开(公告)号：US20120190674A1

公开(公告)日：2012-07-26

申请号：US13407251

申请日：2012-02-28

申请人： Shawn T. Branum ,  Raymond W. Colburn ,  Scott L. Dax ,  Christopher M. Flores ,  Michele C. Jetter ,  Yi Liu ,  Donald Ludovici ,  Mark J. Macielag ,  Jay M. Matthews ,  James J. McNally ,  Laura M. Reaney ,  Ronald K. Russell ,  Ning Qin ,  Christopher Teleha ,  Kenneth M. Wells ,  Scott C. Youells ,  Mark A. Youngman

发明人： Shawn T. Branum ,  Raymond W. Colburn ,  Scott L. Dax ,  Christopher M. Flores ,  Michele C. Jetter ,  Yi Liu ,  Donald Ludovici ,  Mark J. Macielag ,  Jay M. Matthews ,  James J. McNally ,  Laura M. Reaney ,  Ronald K. Russell ,  Ning Qin ,  Christopher Teleha ,  Kenneth M. Wells ,  Scott C. Youells ,  Mark A. Youngman

IPC分类号： A61K31/381 ,  A61K31/4436 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/5377 ,  A61P9/12 ,  A61P25/00 ,  A61P29/00 ,  A61P25/22 ,  A61P25/24 ,  A61P9/00 ,  C07D333/66 ,  A61K31/541

CPC分类号： C07D333/66 ,  C07D333/36 ,  C07D409/12 ,  C07D409/14 ,  C07D417/12 ,  C07D495/04

摘要： Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein A, B, G, Y, R1, R2, R3, and R4 are defined herein.

摘要翻译： 公开了用于治疗各种疾病，综合征，病症和障碍（包括疼痛）的化合物，组合物和方法。 这样的化合物由式I表示如下：其中A，B，G，Y，R 1，R 2，R 3和R 4在本文中定义。

公开(公告)号：US20090264474A1

公开(公告)日：2009-10-22

申请号：US12175740

申请日：2008-07-18

申请人： Shawn T. Branum ,  Raymond W. Colburn ,  Scott L. Dax ,  Christopher M. Flores ,  Michele C. Jetter ,  Yi Liu ,  Donald Ludovici ,  Mark J. Macielag ,  Jay M. Matthews ,  James J. McNally ,  Laura M. Reaney ,  Ronald K. Russell ,  Ning Qin ,  Christopher Teleha ,  Kenneth M. Wells ,  Scott C. Youells ,  Mark A. Youngman

发明人： Shawn T. Branum ,  Raymond W. Colburn ,  Scott L. Dax ,  Christopher M. Flores ,  Michele C. Jetter ,  Yi Liu ,  Donald Ludovici ,  Mark J. Macielag ,  Jay M. Matthews ,  James J. McNally ,  Laura M. Reaney ,  Ronald K. Russell ,  Ning Qin ,  Christopher Teleha ,  Kenneth M. Wells ,  Scott C. Youells ,  Mark A. Youngman

IPC分类号： A61K31/4439 ,  C07D333/66 ,  A61K31/381 ,  C07D417/12 ,  C07D409/12 ,  A61K31/4196 ,  A61K31/427 ,  C07D401/14

CPC分类号： C07D333/66 ,  C07D333/36 ,  C07D409/12 ,  C07D409/14 ,  C07D417/12 ,  C07D495/04

摘要： Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein A, B, G, Y, R1, R2, R3, and R4 are defined herein.

摘要翻译： 公开了用于治疗各种疾病，综合征，病症和障碍（包括疼痛）的化合物，组合物和方法。 这样的化合物由式I表示如下：其中A，B，G，Y，R 1，R 2，R 3和R 4在本文中定义。

公开(公告)号：US20060063789A1

公开(公告)日：2006-03-23

申请号：US10493446

申请日：2002-10-29

申请人： Eddy Jean Freyne ,  Peter Antonius ,  Marc Willems ,  Werner Johan ,  Paul Janssen ,  Paulus Joannes ,  Jan Heeres ,  Marc de Jonge ,  Lucien Koymans ,  Frederik Daeyaert ,  Michael Kukla ,  Hugo Gabriel ,  Bony Nuydens ,  Marc Mercken ,  Donald Ludovici ,  Herwig Janssen ,  Paul Maria ,  Graziella Janssen ,  Jasmine Werner ,  Maroussia Janssen ,  Theodora Arts

发明人： Eddy Jean Freyne ,  Peter Antonius ,  Marc Willems ,  Werner Johan ,  Paul Janssen ,  Paulus Joannes ,  Jan Heeres ,  Marc de Jonge ,  Lucien Koymans ,  Frederik Daeyaert ,  Michael Kukla ,  Hugo Gabriel ,  Bony Nuydens ,  Marc Mercken ,  Donald Ludovici ,  Herwig Janssen ,  Paul Maria ,  Graziella Janssen ,  Jasmine Werner ,  Maroussia Janssen ,  Theodora Arts

IPC分类号： A61K31/655 ,  A61K31/50 ,  A61K31/4965 ,  A61K31/513 ,  C07D241/18 ,  C07D239/47

CPC分类号： C07D239/42 ,  A61K31/506 ,  C07D239/47 ,  C07D239/48 ,  C07D239/50 ,  C07D403/12

摘要： This invention concerns a compound of formula a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein ring A represents a 6-membered heterocycle; R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; optionally substituted C1-6alkyl; C1-6alkyloxycarbonyl; optionally substituted C1-6alkyloxyC1-6alkylcarbonyl; X is a direct bond or a linker atom or group; Z is O or S; R2 is hydrogen, C1-10alkyl, C2-10alkenyl, C2-10alkynyl, a carbocycle or a heterocycle, each of said groups may optionally be substituted; R3 is hydrogen; hydroxy; halo; optionally substituted C1-6alkyl or C2-6alkenyl or C2-6alkynyl; C1-6alkyloxy; C1-6alkylthio; C1-6alkyloxycarbonyl; C1-6alkylcarbonyloxy; carboxyl; cyano; nitro; amino; mono- or di(C1-6alkyl)amino; polyhaloC1-6alkyl; polyhaloC1-6alkyloxy; polyhaloC1-6alkylthio; R21; R21—C1-6alkyl; R21—O—; R21—S—; R21—C(═O)—; R21—S(═O)p—; R7—S(═O)p—; R7—S(═O)p—NH—; R21—S(═O)p—NH—; R7—C(═O)—; —NHC(═O)H; —C(═O)NHNH2; R7—C(═O)—NH—; R21—C(═O)—NH—; —C(═NH)R7; —C(═NH)R21; R4a or R4b each independently represent hydrogen, R8, —Y1—NR9—Y2—NR10R11, —Y1—NR9—Y1—R8, —Y1—NR9R10; provided that —X—R2 and/or R3 is other than hydrogen; their use, pharmaceutical compositions comprising them and processes for their preparation.

摘要翻译： 本发明涉及式的化合物