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1. 发明申请

US20120136006A1 COLD MENTHOL RECEPTOR ANTAGONISTS 有权
标题翻译：冷门痛受体拮抗剂
公开(公告)号：US20120136006A1
公开(公告)日：2012-05-31
申请号：US13366555
申请日：2012-02-06
申请人： Raymond W. Colburn , Scott L. Dax , Christopher M. Flores , Donald W. Ludovici , Jay M. Matthews , Mingde Xia , Xiaoqing Xu , Mark A. Youngman , Bin Zhu
发明人： Raymond W. Colburn , Scott L. Dax , Christopher M. Flores , Donald W. Ludovici , Jay M. Matthews , Mingde Xia , Xiaoqing Xu , Mark A. Youngman , Bin Zhu
IPC分类号： A61K31/40 , A61K31/4709 , A61K31/4545 , A61K31/4025 , A61K31/4439 , A61K31/495 , A61K31/41 , A61P25/00 , A61P25/22 , A61P25/24 , A61P25/06 , A61P13/00 , A61P13/08 , A61P11/14 , A61P11/06 , A61P11/02 , A61P17/00 , A61P37/08 , A61P11/00 , A61P9/00 , A61P9/12 , A61K31/404
CPC分类号： C07D207/08 , C07D209/08 , C07D209/44 , C07D217/06 , C07D241/04 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/10 , C07D405/04 , C07D405/06 , C07D405/10 , C07D409/04 , C07D409/06 , C07D417/06
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, L, Q, R1, R2, and R3 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，L，Q，R 1，R 2和R 3在本文中定义。

2. 发明授权

US07795440B2 N-substituted tricyclic 1-aminopyrazoles as inhibitors for the treatment of cell proliferative disorders 有权
标题翻译： N-取代的三环1-氨基吡唑作为治疗细胞增殖性疾病的抑制剂
公开(公告)号：US07795440B2
公开(公告)日：2010-09-14
申请号：US11657912
申请日：2007-01-25
申请人： Chih Yung Ho , Bengt Anders Brunmark , Stuart Emanuel , Robert A. Galemmo, Jr. , Dana L. Johnson , Donald W. Ludovici , Umar Maharoof , Jay M. Mei , Jan L. Sechler , Eric D. Strobel , Robert W. Tuman , Hwa Kwo Yen
发明人： Chih Yung Ho , Bengt Anders Brunmark , Stuart Emanuel , Robert A. Galemmo, Jr. , Dana L. Johnson , Donald W. Ludovici , Umar Maharoof , Jay M. Mei , Jan L. Sechler , Eric D. Strobel , Robert W. Tuman , Hwa Kwo Yen
IPC分类号： A61K31/416 , A61K31/4439 , C07D401/12
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。本发明进一步涉及包含本发明化合物的药物组合物和治疗诸如肿瘤和其它细胞增殖性疾病的病症的方法。

3. 发明申请

US20100048619A1 Cold Menthol Receptor Antagonists 有权
标题翻译：冷薄荷醇受体拮抗剂
公开(公告)号：US20100048619A1
公开(公告)日：2010-02-25
申请号：US12539277
申请日：2009-08-11
申请人： Raymond W. Colburn , Scott L. Dax , Christopher M. Flores , Donald W. Ludovici , Mingde Xia , Xiaoqing Xu , Mark A. Youngman , Bin Zhu
发明人： Raymond W. Colburn , Scott L. Dax , Christopher M. Flores , Donald W. Ludovici , Mingde Xia , Xiaoqing Xu , Mark A. Youngman , Bin Zhu
IPC分类号： A61K31/472 , C07D217/22 , A61P25/00 , A61P29/00
CPC分类号： C07D217/04 , C07C237/20 , C07C2102/08 , C07C2602/08 , C07D215/38 , C07D217/02 , C07D401/12
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, L, R1, R2, R4 and R5 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，L，R 1，R 2，R 4和R 5在本文中定义。

4. 发明授权

US07563781B2 Triazolopyrimidine derivatives 有权
标题翻译：三唑并嘧啶衍生物
公开(公告)号：US07563781B2
公开(公告)日：2009-07-21
申请号：US11329642
申请日：2006-01-11
申请人： Donald W. Ludovici , Richard W. Connors , Steven J. Coats , Li Liu , Bart L. De Corte , Dana L. Johnson , Mark J. Schulz
发明人： Donald W. Ludovici , Richard W. Connors , Steven J. Coats , Li Liu , Bart L. De Corte , Dana L. Johnson , Mark J. Schulz
IPC分类号： C07D487/04 , C07F9/40 , A61K31/5355 , A61K31/519 , C07D239/30 , A61P35/00 , G01N33/53 , C07H21/04 , C12P21/06 , C12N5/06 , 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。

5. 发明授权

US07449575B2 Substituted diamino-1,3,5-triazine derivatives 失效
公开(公告)号：US07449575B2
公开(公告)日：2008-11-11
申请号：US11203325
申请日：2005-08-12
申请人： Paul A. J. Janssen , Jan Heeres , Henri E. L. Moereels , Michael Joseph Kukla , Donald W. Ludovici
发明人： Paul A. J. Janssen , Jan Heeres , Henri E. L. Moereels , Michael Joseph Kukla , Donald W. Ludovici
IPC分类号： C07D251/48 , C07D403/04
CPC分类号： C07D403/06 , C07D251/18 , C07D251/48 , C07D405/06 , C07D405/12 , C07D409/12
摘要： This invention concerns the compounds of formula the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein R1 and R2 are each independently selected from hydrogen; hydroxy; amino; optionally substituted C1-6alkyl; C1-6alkyloxy; C1-6alkylcarbonyl; C1-6alkyloxycarbonyl; Ar1; mono- or di(C1-6alkyl)amino; mono- or di(C1-6alkyl)-aminocarbonyl; dihydro-2(3H)-furanone; or R1 and R2 taken together may form pyrrolidinyl, piperidinyl, morpholinyl, azido or mono- or di(C1-6alkyl)amino-C1-4alkylidene; R3 is hydrogen, Ar1, C1-6alkylcarbonyl, C1-6alkyl, C1-6alkyloxy-carbonyl, C1-6alkyl substituted with C1-6alkyloxycarbonyl; and R4, R5, R6, R7 and R8 are each independently selected from hydrogen, halo, C1-6alkyl, C1-6alkyloxy, cyano, aminocarbonyl, nitro, amino, trihalomethyl or trihalomethyloxy; L is optionally substituted C1-10alkyl; C3-10alkenyl; C3-10alkynyl; C3-7cycloalkyl; Ar1 is optionally substituted phenyl; 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.

6. 发明授权

US08143259B2 Cold menthol receptor antagonists 有权
公开(公告)号：US08143259B2
公开(公告)日：2012-03-27
申请号：US12539267
申请日：2009-08-11
申请人： Raymond W. Colburn , Scott L. Dax , Christopher M. Flores , Donald W. Ludovici , Jay M. Matthews , Mingde Xia , Xiaoqing Xu , Mark A. Youngman , Bin Zhu
发明人： Raymond W. Colburn , Scott L. Dax , Christopher M. Flores , Donald W. Ludovici , Jay M. Matthews , Mingde Xia , Xiaoqing Xu , Mark A. Youngman , Bin Zhu
IPC分类号： A61K31/495 , A61K31/47 , A61K31/404 , A61K31/40 , C07D241/04 , C07D215/02 , C07D209/04 , C07D207/08
CPC分类号： C07D207/08 , C07D209/08 , C07D209/44 , C07D217/06 , C07D241/04 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/10 , C07D405/04 , C07D405/06 , C07D405/10 , C07D409/04 , C07D409/06 , C07D417/06
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, L, Q, R1, R2, and R3 are defined herein.

7. 发明授权

US06380194B1 Substituted diamino-1,3,5-triazine derivatives 失效
标题翻译：取代的二氨基-1,3,5-三嗪衍生物
公开(公告)号：US06380194B1
公开(公告)日：2002-04-30
申请号：US08938602
申请日：1997-09-26
申请人： Paul A. J. Janssen , Jan Heeres , Henri E. L. Moereels , Michael Joseph Kukla , Donald W. Ludovici
发明人： Paul A. J. Janssen , Jan Heeres , Henri E. L. Moereels , Michael Joseph Kukla , Donald W. Ludovici
IPC分类号： C07D25150
CPC分类号： C07D403/06 , C07D251/18 , C07D251/48 , C07D405/06 , C07D405/12 , C07D409/12
摘要： This invention concerns the compounds of formula the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein R1 and R2 are each independently selected from hydrogen; hydroxy; amino; optionally substituted C1-6alkyl; C1-6alkyloxy; C1-6alkylcarbonyl; C1-6alkyloxycarbonyl; Ar1; mono- or di(C1-6alkyl)amino; mono- or di(C1-6alkyl)-aminocarbonyl; dihydro-2(3H)-furanone; or R1and R2 taken together may form pyrrolidinyl, piperidinyl, morpholinyl, azido or mono- or di(C1-6alkyl)amino-C1-4alkylidene; R3 is hydrogen, Ar1, C1-6alkylcarbonyl, C1-6alkyl, C1-6alkyloxycarbonyl, C1-6alkyl substituted with C1-6alkyloxycarbonyl; and R4, R5, R6, R7 and R8 are each independently selected from hydrogen, halo, C1-6alkyl, C1-6alkyloxy, cyano, aminocarbonyl, nitro, amino, trihalomethyl or trihalomethyloxy; L is optionally substituted C1-10alkyl; C3-10alkenyl; C3-10alkynyl; C3-7cycloalkyl; Ar1is optionally substituted phenyl; 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.
摘要翻译：本发明涉及配制药学上可接受的酸加成盐及其立体化学异构形式的化合物，其中R 1和R 2各自独立地选自氢; 羟基; 氨基; 任选取代的C 1-6烷基; C 1-6烷氧基; C 1-6烷基羰基; C 1-6烷氧基羰基; Ar1; 单或二（C 1-6烷基）氨基; 单或二（C 1-6烷基） - 氨基羰基; 二氢-2（3H） - 呋喃酮; 或R 1和R 2一起可以形成吡咯烷基，哌啶基，吗啉基，叠氮基或单或二（C 1-6烷基）氨基-C 1-4亚烷基; R3是氢，Ar1，C1-6烷基羰基，C1-6烷基，C1-6烷氧基羰基，被C1-6烷氧基羰基取代的C1-6烷基; 并且R 4，R 5，R 6，R 7和R 8各自独立地选自氢，卤素，C 1-6烷基，C 1-6烷氧基，氰基，氨基羰基，硝基，氨基，三卤甲基或三卤代甲氧基。 L是任选取代的C 1-10烷基; C3-10烯基; C3-10炔基; C 3-7环烷基; 任选取代的苯基; 用于制造用于治疗患有HIV（人类免疫缺陷病毒）感染的受试者的药物。它还涉及作为式（I）化合物的亚组的新化合物，其制备方法和包含它们的组合物。

8. 发明申请

US20140128428A1 COLD MENTHOL RECEPTOR ANTAGONISTS 审中-公开
标题翻译：冷门痛受体拮抗剂
公开(公告)号：US20140128428A1
公开(公告)日：2014-05-08
申请号：US14152006
申请日：2014-01-10
申请人： Raymond W. Colburn , Scott L. Dax , Christopher M. Flores , Donald W. Ludovici , Mingde Xia , Xiaoqing Xu , Mark A. Youngman , Bin Zhu
发明人： Raymond W. Colburn , Scott L. Dax , Christopher M. Flores , Donald W. Ludovici , Mingde Xia , Xiaoqing Xu , Mark A. Youngman , Bin Zhu
IPC分类号： C07D217/04
CPC分类号： C07D217/04 , C07C237/20 , C07C2102/08 , C07C2602/08 , C07D215/38 , C07D217/02 , C07D401/12
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, L, R1, R2, R4, and R5 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，L，R 1，R 2，R 4和R 5在本文中定义。

9. 发明授权

US06201025B1 N-aralkylaminotetralins as ligands for the neuropeptide Y Y5 receptor 有权
标题翻译： N-芳烷基氨基螺环素作为神经肽Y Y5受体的配体
公开(公告)号：US06201025B1
公开(公告)日：2001-03-13
申请号：US09413292
申请日：1999-10-06
申请人： Scott L. Dax , Timothy W. Lovenberg , Ellen W. Baxter , John R. Carson , Donald W. Ludovici , Mark A. Youngman
发明人： Scott L. Dax , Timothy W. Lovenberg , Ellen W. Baxter , John R. Carson , Donald W. Ludovici , Mark A. Youngman
IPC分类号： A61K31135
CPC分类号： C07C217/74 , C07B2200/07 , C07C217/58 , C07C2602/10 , C07D209/16 , C07D213/38
摘要： &bgr;-Aminotetralin derivatives of the formula: which are ligands for the neuropeptide Y Y5 (NPY5) receptor, methods of preparation and pharmaceutical compositions containing a &bgr;-aminotetralin derivative as the active ingredient are described. The 62 -aminotetralins are useful in the treatment of disorders and diseases associated with NPY receptor subtype Y5.
摘要翻译：描述了作为神经肽Y Y5（NPY5）受体的配体的制备方法和含有β-氨基四氢卟吩衍生物作为活性成分的药物组合物的下式的β-氨基四氢萘衍生物。 62-氨基四氢叶酸可用于治疗与NPY受体亚型Y5相关的疾病和疾病。

10. 发明授权

US08653099B2 Cold menthol receptor antagonists 有权
标题翻译：冷薄荷醇受体拮抗剂
公开(公告)号：US08653099B2
公开(公告)日：2014-02-18
申请号：US12539277
申请日：2009-08-11
申请人： Raymond W. Colburn , Scott L. Dax , Christopher M. Flores , Donald W. Ludovici , Mingde Xia , Xiaoqing Xu , Mark A. Youngman , Bin Zhu
发明人： Raymond W. Colburn , Scott L. Dax , Christopher M. Flores , Donald W. Ludovici , Mingde Xia , Xiaoqing Xu , Mark A. Youngman , Bin Zhu
IPC分类号： C07D217/22 , C07D215/16 , A61K31/47
CPC分类号： C07D217/04 , C07C237/20 , C07C2102/08 , C07C2602/08 , C07D215/38 , C07D217/02 , C07D401/12
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, L, R1, R2, R4 and R5 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，L，R 1，R 2，R 4和R 5在本文中定义。

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