公开(公告)号：US08293909B2

公开(公告)日：2012-10-23

申请号：US12720182

申请日：2010-03-09

申请人： Richard Pracitto ,  John F. Kadow ,  John A. Bender ,  Brett R. Beno ,  Katharine A. Grant-Young ,  Ying Han ,  Piyasena Hewawasam ,  Andrew Nickel ,  Kyle E. Parcella ,  Kap-Sun Yeung ,  Louis S. Chupak

发明人： Richard Pracitto ,  John F. Kadow ,  John A. Bender ,  Brett R. Beno ,  Katharine A. Grant-Young ,  Ying Han ,  Piyasena Hewawasam ,  Andrew Nickel ,  Kyle E. Parcella ,  Kap-Sun Yeung ,  Louis S. Chupak

IPC分类号： C07D471/04 ,  A61K31/437

CPC分类号： C07D209/42 ,  C07D333/68 ,  C07D471/04 ,  C07D491/048

摘要： The disclosure provides compounds of formula I, II, III, IV, and V, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.

公开(公告)号：US20110207749A1

公开(公告)日：2011-08-25

申请号：US13025384

申请日：2011-02-11

申请人： Louis S. Chupak ,  Xiaofan Zheng ,  Min Ding ,  Shuanghua Hu ,  Yazhong Huang ,  Robert G. Gentles

发明人： Louis S. Chupak ,  Xiaofan Zheng ,  Min Ding ,  Shuanghua Hu ,  Yazhong Huang ,  Robert G. Gentles

IPC分类号： A61K31/198 ,  C07C311/29 ,  C07D239/26 ,  A61K31/505 ,  C07D277/30 ,  A61K31/426 ,  C07D311/58 ,  A61K31/352 ,  A61K31/277 ,  A61P3/10 ,  A61P3/06 ,  A61P25/24 ,  A61P25/22 ,  A61P25/18

CPC分类号： C07D311/70 ,  C07D239/26 ,  C07D277/28 ,  C07D407/12

摘要： The present disclosure is generally directed to compounds that can inhibit DAGLα and/or β activity, compositions comprising such compounds, and methods for inhibiting DAGLα and/or β activity.

公开(公告)号：US06903128B2

公开(公告)日：2005-06-07

申请号：US10702539

申请日：2003-11-05

申请人： Allen J. Duplantier ,  Louis S. Chupak ,  Anthony J. Milici ,  Wan F. Lau

发明人： Allen J. Duplantier ,  Louis S. Chupak ,  Anthony J. Milici ,  Wan F. Lau

IPC分类号： A61K31/135 ,  A61K31/137 ,  A61K31/198 ,  A61K31/275 ,  A61K31/4184 ,  A61K31/42 ,  A61K31/421 ,  A61K31/422 ,  A61K31/436 ,  A61K31/519 ,  A61K31/522 ,  A61K31/56 ,  A61K31/58 ,  A61K31/606 ,  A61K31/635 ,  A61K31/675 ,  A61K38/00 ,  A61K38/21 ,  A61P1/00 ,  A61P3/00 ,  A61P3/10 ,  A61P9/10 ,  A61P11/06 ,  A61P11/08 ,  A61P17/06 ,  A61P19/02 ,  A61P19/10 ,  A61P25/00 ,  A61P29/00 ,  A61P37/00 ,  A61P37/04 ,  A61P37/06 ,  C07C229/34 ,  C07C233/47 ,  C07C275/42 ,  C07C311/06 ,  C07D233/64 ,  C07D235/10 ,  C07D235/14 ,  C07D261/08 ,  C07D277/22 ,  C07D277/38 ,  C07D413/04 ,  C07D235/04 ,  C07D263/54

CPC分类号： C07D413/04 ,  C07C229/34 ,  C07C233/47 ,  C07C311/06 ,  C07D235/14 ,  C07D261/08

摘要： There is disclosed a genus of non-peptidyl compounds, wherein said compounds are VLA-4 inhibitors useful in treating inflammatory, autoimmune, and respiratory diseases, and wherein said compounds comprise a compound of Formula (1.0.0): and pharmaceutically acceptable salts and other prodrug derivatives thereof, wherein: A is (C1-C6) alkyl, cycloalkyl, aryl, heteroaryl or heterocyclyl optionally substituted with 0 to 3 R9; or is a member selected from the group consisiting of the following radicals: A1-NHC(═O)NH-A2-, A1-NHC(═O)O-A2-, A1-OC(═O)NH-A2-, A1-NHSO2NH-A2-, A1-NHC(═O)-A2-, A1-C(═O)NH-A2-, A1-NHSO2-A2-, A1-SO2NH-A2-, A1-(CH2)rO-A2-, A1-O(CH2)r-A2, A1-(CH2)r-A2-, where A1 and A2 are each independently selected from the group consisting of hydrogen, aryl, (C1-C6) alkyl, (C2-C6) alkenyl, (C2-C6) alkynyl, cycloalkyl, heteroaryl, and heterocyclyl substituted with 0 to 3 R9; B is a member independently selected from the group consisting of the following: E is a single bond; —O—; —NR10—; —CH═CH—; —CC—; S(═O)q; —CR11R12NR10—; or —CR11R12—; X is —O—; —C(═O)—; —S(═O)q—; or —NR10—; X1, X2 and X3 are each independently selected from the group consisting of CH, CR9 or N; Y is a single bond; —C(═O)—; —C(═S)—; or —S(═O)2—; R7 is (C1-C6) alkyl; (CH2)kOR5; (CH2)kNR6C(═O)R5; (CH2)kNR6C(═O)OR5; (CH2)kNR6SO2R5; (CH2)kNR6R5; F; CF3; OCF3; aryl, substituted with 0 to 3 R9; heterocyclyl, substituted with 0 to 3 R9; heteroaryl, substituted with 0 to 3 R9; cycloalkyl, substituted with 0 to 3 R9; or R7 may be taken together with R8 to form a cycloalkyl or heterocyclyl ring; or R7 may be taken together with R11 to form a cycloalkyl or heterocyclyl ring; and R8 is hydrogen; F; (C1-C6) alkyl or (C1-C6) alkoxy.

公开(公告)号：US20120232099A1

公开(公告)日：2012-09-13

申请号：US13470727

申请日：2012-05-14

申请人： Richard Pracitto ,  John F. Kadow ,  John A. Bender ,  Brett R. Beno ,  Katherine A. Grant-Young ,  Ying Han ,  Piyasena Hewawasam ,  Andrew Nickel ,  Kyle E. Parcella ,  Kap-Sun Yeung ,  Louis S. Chupak

发明人： Richard Pracitto ,  John F. Kadow ,  John A. Bender ,  Brett R. Beno ,  Katherine A. Grant-Young ,  Ying Han ,  Piyasena Hewawasam ,  Andrew Nickel ,  Kyle E. Parcella ,  Kap-Sun Yeung ,  Louis S. Chupak

IPC分类号： A61K31/4355 ,  A61K31/506 ,  A61P31/04 ,  C07D491/048

CPC分类号： C07D471/04 ,  C07D209/42 ,  C07D333/68 ,  C07D491/048

摘要： The disclosure provides compounds of formula I, II, III, IV, and V, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.

摘要翻译： 本公开提供式I，II，III，IV和V的化合物，包括它们的盐，以及使用该化合物的组合物和方法。 该化合物具有抗丙型肝炎病毒（HCV）的活性，可用于治疗HCV感染者。

公开(公告)号：US06387901B1

公开(公告)日：2002-05-14

申请号：US09608259

申请日：2000-06-30

申请人： Louis S. Chupak

发明人： Louis S. Chupak

IPC分类号： A61K315375

CPC分类号： C07D265/30

摘要： The present invention relates to alkyne containing metalloproteinase inhibitors of the formula wherein n, X, and R1-R9 are as defined in the specification, and to pharmaceutical compositions and methods of treatment thereof.

摘要翻译： 本发明涉及制剂中含有炔烃的金属蛋白酶抑制剂，X和R 1 -R 9如说明书中所定义，以及药物组合物及其治疗方法。

公开(公告)号：US06329397B1

公开(公告)日：2001-12-11

申请号：US09372946

申请日：1999-08-12

申请人： Kim F. McClure ,  Mark C. Noe ,  Michael A. Letavic ,  Louis S. Chupak

发明人： Kim F. McClure ,  Mark C. Noe ,  Michael A. Letavic ,  Louis S. Chupak

IPC分类号： A61K31445

CPC分类号： C07D401/12 ,  C07D211/96 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12

摘要： A compound of the formula wherein R1, R2 R3, R4 R5, R6, R7, R8, R9 and Ar are as defined above, useful in the treatment of a condition selected from the group consisting of arthritis, cancer, and other diseases characterized by matrix metalloproteinase or mammalian reprolysin activity. In addition, the compounds of the present invention may be used in combination therapy with standard non-steroidal anti-inflammatory drugs (NSAID'S), COX-2 inhibitors and analgesics, and in combination with cytotoxic drugs such as adriamycin, daunomycin, cis-platinum, etoposide, taxol, taxotere and other alkaloids, such as vincristine, in the treatment of cancer.

摘要翻译： 式R 1，R 2，R 3，R 4，R 5，R 6，R 7，R 8，R 9和Ar的化合物如上所定义，可用于治疗选自以下的病症：关节炎，癌症和其它以基质为特征的疾病 金属蛋白酶或哺乳动物生殖毒素活性。 此外，本发明的化合物可以与标准非甾体抗炎药（NSAID'S），COX-2抑制剂和镇痛药组合使用，并与细胞毒性药物如阿霉素，道诺霉素，顺式铂 ，依托泊苷，紫杉醇，泰索帝等生物碱，如长春新碱，用于治疗癌症。

公开(公告)号：US08198449B2

公开(公告)日：2012-06-12

申请号：US12549983

申请日：2009-08-28

申请人： Richard Pracitto ,  John F. Kadow ,  John A. Bender ,  Brett R. Beno ,  Katharine A. Grant-Young ,  Ying Han ,  Piyasena Hewawasam ,  Andrew Nickel ,  Kyle E. Parcella ,  Kap-Sun Yeung ,  Louis S. Chupak

发明人： Richard Pracitto ,  John F. Kadow ,  John A. Bender ,  Brett R. Beno ,  Katharine A. Grant-Young ,  Ying Han ,  Piyasena Hewawasam ,  Andrew Nickel ,  Kyle E. Parcella ,  Kap-Sun Yeung ,  Louis S. Chupak

IPC分类号： A61K31/437 ,  C07D471/04

CPC分类号： C07D471/04 ,  C07D209/42 ,  C07D333/68 ,  C07D491/048

摘要： The disclosure provides compounds of formula I, II, III, IV, and V, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.

摘要翻译： 本公开提供式I，II，III，IV和V的化合物，包括它们的盐，以及使用该化合物的组合物和方法。 该化合物具有抗丙型肝炎病毒（HCV）的活性，可用于治疗HCV感染者。

公开(公告)号：US20100184800A1

公开(公告)日：2010-07-22

申请号：US12720182

申请日：2010-03-09

申请人： Richard Pracitto ,  John F. Kadow ,  John A. Bender ,  Brett R. Beno ,  Katharine A. Grant-Young ,  Ying Han ,  Piyasena Hewawasam ,  Andrew Nickel ,  Kyle E. Parcella ,  Kap-Sun Yeung ,  Louis S. Chupak

发明人： Richard Pracitto ,  John F. Kadow ,  John A. Bender ,  Brett R. Beno ,  Katharine A. Grant-Young ,  Ying Han ,  Piyasena Hewawasam ,  Andrew Nickel ,  Kyle E. Parcella ,  Kap-Sun Yeung ,  Louis S. Chupak

IPC分类号： A61K31/437 ,  C07D471/04 ,  A61P31/14

CPC分类号： C07D209/42 ,  C07D333/68 ,  C07D471/04 ,  C07D491/048

摘要： The disclosure provides compounds of formula I, II, III, IV, and V, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.

公开(公告)号：US07462600B2

公开(公告)日：2008-12-09

申请号：US11313523

申请日：2005-12-21

申请人： Louis S. Chupak ,  Mark E. Flanagan ,  Takushi Kaneko ,  Thomas V. Magee ,  Mark C. Noe ,  Usa Reilly

发明人： Louis S. Chupak ,  Mark E. Flanagan ,  Takushi Kaneko ,  Thomas V. Magee ,  Mark C. Noe ,  Usa Reilly

IPC分类号： A61K31/70 ,  C07H17/08

CPC分类号： C07H17/08

摘要： Macrolide compounds per se, as shown below and defined herein, and their use, e.g., as antibacterial and antiprotozoal agents in animals, including humans: Also disclosed are methods of preparing the compounds, intermediates, and pharmaceutical compositions thereof, and methods of treating or preventing disease by administering the compounds to subjects in need. This abstract is only an excerpt and is not limiting of the invention.

摘要翻译： 大环内酯类化合物本身，如下文所示和定义，以及它们在动物（包括人）中作为抗细菌剂和抗原虫药的用途：还公开了制备化合物，中间体及其药物组合物的方法，以及治疗或 通过将化合物给予需要的受试者来预防疾病。 该摘要仅是摘录而不是本发明的限制。

公开(公告)号：US08404741B2

公开(公告)日：2013-03-26

申请号：US13025384

申请日：2011-02-11

申请人： Louis S. Chupak ,  Xiaofan Zheng ,  Min Ding ,  Shuanghua Hu ,  Yazhong Huang ,  Robert G. Gentles

发明人： Louis S. Chupak ,  Xiaofan Zheng ,  Min Ding ,  Shuanghua Hu ,  Yazhong Huang ,  Robert G. Gentles

IPC分类号： A01N43/16 ,  A01N37/12 ,  A01N37/44 ,  A61K31/35 ,  A61K31/195 ,  C07D317/70 ,  C07C51/16 ,  C07C229/00

CPC分类号： C07D311/70 ,  C07D239/26 ,  C07D277/28 ,  C07D407/12

摘要： The present disclosure is generally directed to compounds that can inhibit DAGLα and/or β activity, compositions comprising such compounds, and methods for inhibiting DAGLα and/or β activity.

摘要翻译： 本公开一般涉及可抑制DAGLα和/或bgr的化合物; 活性，包含这些化合物的组合物和抑制DAGLα和/或bgr的方法; 活动。