公开(公告)号：WO2009094528A1

公开(公告)日：2009-07-30

申请号：PCT/US2009/031819

申请日：2009-01-23

Applicant: HIGH POINT PHARMACEUTICALS, LLC ,  MJALLI, Adnan M M ,  GADDAM, Bapu ,  POLISETTI, Dharma Rao ,  KOSTURA, Matthew ,  GUZEL, Mustafa

Inventor： MJALLI, Adnan M M ,  GADDAM, Bapu ,  POLISETTI, Dharma Rao ,  KOSTURA, Matthew ,  GUZEL, Mustafa

IPC: A01N43/54 ,  A61K31/505 ,  C07D239/42

CPC classification number: A61K31/519 ,  C07D471/04 ,  Y02A50/411

Abstract: The present invention relates to chemical compounds of Formula (I) are as herein defined, pharmaceutical compositions, and methods of use in the treatment of conditions or disorders mediated by TNF-alpha or by PDE4, including but not limited to rheumatoid arthritis.

Abstract translation: 本发明涉及式（I）的化合物如本文所定义，药物组合物和用于治疗由TNF-α或PDE4介导的病症或病症的方法，包括但不限于类风湿性关节炎。

公开(公告)号：WO2004014844A3

公开(公告)日：2005-04-28

申请号：PCT/US0325045

申请日：2003-08-08

Applicant: TRANSTECH PHARMA INC ,  MJALLI ADNAN M M ,  ANDREWS ROB ,  GUO XIAO-CHUAN ,  CHRISTEN DANIEL PETER ,  GOHIMMUKKULA DEVI REDDY ,  HUANG GUOXIANG ,  ROTHLEIN ROBERT ,  TYAGI SAMEER ,  YARAMASU TRIPURA ,  BEHME CHRISTOPHER

Inventor： MJALLI ADNAN M M ,  ANDREWS ROB ,  GUO XIAO-CHUAN ,  CHRISTEN DANIEL PETER ,  GOHIMMUKKULA DEVI REDDY ,  HUANG GUOXIANG ,  ROTHLEIN ROBERT ,  TYAGI SAMEER ,  YARAMASU TRIPURA ,  BEHME CHRISTOPHER

IPC: A61K31/166 ,  A61K31/167 ,  A61K31/198 ,  A61K31/341 ,  A61K31/343 ,  A61K31/381 ,  A61K31/402 ,  A61K31/4025 ,  A61K31/4155 ,  A61K31/4164 ,  A61K31/421 ,  A61K31/422 ,  A61K31/4245 ,  A61K31/433 ,  A61K31/44 ,  A61K31/4409 ,  A61K31/4418 ,  A61K31/4453 ,  A61K31/4465 ,  A61K31/472 ,  A61K31/501 ,  A61K31/506 ,  A61K31/517 ,  A61K31/5377 ,  A61K31/55 ,  A61K31/609 ,  A61K31/625 ,  A61K31/63 ,  A61P7/02 ,  A61P9/06 ,  A61P9/10 ,  A61P9/14 ,  A61P13/12 ,  A61P15/06 ,  A61P29/00 ,  A61P37/00 ,  A61P41/00 ,  A61P43/00 ,  C07C233/29 ,  C07C233/87 ,  C07C235/42 ,  C07C235/52 ,  C07C235/60 ,  C07C235/66 ,  C07C237/20 ,  C07C237/36 ,  C07C237/42 ,  C07C237/44 ,  C07C255/58 ,  C07C255/60 ,  C07C257/18 ,  C07C271/20 ,  C07C271/44 ,  C07C311/18 ,  C07C311/19 ,  C07C311/29 ,  C07C311/44 ,  C07C317/14 ,  C07C317/28 ,  C07C317/36 ,  C07C317/46 ,  C07C323/36 ,  C07D207/09 ,  C07D207/26 ,  C07D207/267 ,  C07D207/27 ,  C07D207/48 ,  C07D211/14 ,  C07D211/26 ,  C07D213/30 ,  C07D213/38 ,  C07D213/55 ,  C07D213/56 ,  C07D213/70 ,  C07D213/71 ,  C07D213/74 ,  C07D213/75 ,  C07D213/81 ,  C07D213/82 ,  C07D215/36 ,  C07D217/02 ,  C07D217/04 ,  C07D217/16 ,  C07D217/22 ,  C07D217/26 ,  C07D231/12 ,  C07D231/14 ,  C07D231/18 ,  C07D233/84 ,  C07D239/94 ,  C07D249/08 ,  C07D261/10 ,  C07D263/32 ,  C07D271/10 ,  C07D277/20 ,  C07D277/44 ,  C07D277/46 ,  C07D277/54 ,  C07D285/06 ,  C07D285/08 ,  C07D295/08 ,  C07D295/092 ,  C07D295/14 ,  C07D295/155 ,  C07D307/52 ,  C07D307/66 ,  C07D307/79 ,  C07D307/85 ,  C07D317/60 ,  C07D317/66 ,  C07D333/20 ,  C07D333/24 ,  C07D333/38 ,  C07D333/70 ,  C07D401/04 ,  C07D403/04 ,  C07D409/04 ,  C07D409/06 ,  C07D413/04 ,  A61K31/33

CPC classification number: C07D207/267 ,  C07C233/29 ,  C07C233/87 ,  C07C235/42 ,  C07C235/52 ,  C07C235/60 ,  C07C235/66 ,  C07C237/36 ,  C07C237/42 ,  C07C237/44 ,  C07C255/60 ,  C07C257/18 ,  C07C271/20 ,  C07C271/44 ,  C07C311/18 ,  C07C311/19 ,  C07C311/44 ,  C07C317/14 ,  C07C317/28 ,  C07C317/36 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2603/74 ,  C07D207/09 ,  C07D211/26 ,  C07D213/30 ,  C07D213/70 ,  C07D213/71 ,  C07D213/74 ,  C07D213/81 ,  C07D217/02 ,  C07D217/16 ,  C07D217/22 ,  C07D231/12 ,  C07D231/14 ,  C07D231/18 ,  C07D233/84 ,  C07D239/94 ,  C07D249/08 ,  C07D261/10 ,  C07D263/32 ,  C07D271/10 ,  C07D277/46 ,  C07D285/08 ,  C07D295/088 ,  C07D295/155 ,  C07D307/66 ,  C07D307/79 ,  C07D307/85 ,  C07D317/60 ,  C07D333/24 ,  C07D333/38 ,  C07D333/70 ,  C07D401/04 ,  C07D409/04 ,  C07D409/06 ,  C07D413/04

Abstract: This invention provides certain compounds, methods of their preparation, pharmaceutical compositions comprising the compounds, and their use in treating human or animal disorders. The compounds of the invention are useful as antagonists, or more preferably, partial antagonist of factor IX and thus, may be used to inhibit the intrinsic pathway of blood coagulation. The compounds are useful in a variety of applications including the management, treatment and/or control of diseases caused in part by the intrinsic clotting pathway utilizing factor IX. Such diseases or disease states include stroke, myocardial infarction, aneurysm surgery, and deep vein thrombosis associated with surgical procedures, long periods of confinement, and acquired or inherited pro-coagulant states.

Abstract translation: 本发明提供某些化合物，其制备方法，包含该化合物的药物组合物及其在治疗人或动物疾病中的用途。 本发明的化合物可用作拮抗剂，或更优选为因子IX的部分拮抗剂，因此可用于抑制血液凝固的内在途径。 该化合物可用于各种应用，包括通过利用因子IX的内在凝血途径部分引起的疾病的管理，治疗和/或控制。 这些疾病或疾病状态包括中风，心肌梗死，动脉瘤手术以及与外科手术相关的深部静脉血栓形成，长时间的约束，以及获得性或遗传的促凝血状态。

公开(公告)号：WO2005000295A1

公开(公告)日：2005-01-06

申请号：PCT/US2004/016104

申请日：2004-05-20

Applicant: TRANSTECH PHARMA, INC. ,  MJALLI, Adnan, M., M. ,  ANDREWS, Robert, C. ,  SHEN, Jane, M. ,  ROTHLEIN, Robert

Inventor： MJALLI, Adnan, M., M. ,  ANDREWS, Robert, C. ,  SHEN, Jane, M. ,  ROTHLEIN, Robert

IPC: A61K31/4184

CPC classification number: A61K31/4164 ,  A61K31/4184 ,  A61K31/425

Abstract: Disclosed are RAGE antagonist compounds that have the ability to reverse pre-existing amyloidosis. Treatment with the RAGE antagonist compounds described herein may be used to reduce plaque size and improve cognition for subjects in the later stages of Alzheimer's disease. Additionally, the RAGE antagonists described herein may be used to reduce the onset of plaque formation and thereby prevent loss of cognition and other symptoms associated with Alzheimer's Disease and other diseases of amyloid deposition.

Abstract translation: 公开了具有逆转预先存在的淀粉样变性的能力的RAGE拮抗剂化合物。 本文所述的RAGE拮抗剂化合物的治疗可用于减少斑块大小并改善阿尔茨海默氏病后期受试者的认知。 此外，本文所述的RAGE拮抗剂可用于减少斑块形成的发作，从而防止与阿尔茨海默病和其他淀粉样蛋白沉积疾病相关的认知和其它症状的丧失。

公开(公告)号：WO02070473A3

公开(公告)日：2002-12-27

申请号：PCT/US0206707

申请日：2002-03-05

Applicant: TRANSTECH PHARMA INC ,  MJALLI ADNAN M M ,  ANDREWS ROB ,  WYSONG CHRISTOPHER

Inventor： MJALLI ADNAN M M ,  ANDREWS ROB ,  WYSONG CHRISTOPHER

IPC: C07D233/60 ,  A61K31/167 ,  A61K31/27 ,  A61K31/351 ,  A61K31/401 ,  A61K31/4164 ,  A61K31/445 ,  A61K31/4462 ,  A61K31/4465 ,  A61K31/472 ,  A61P3/10 ,  A61P7/00 ,  A61P9/10 ,  A61P13/12 ,  A61P15/10 ,  A61P25/28 ,  A61P27/02 ,  A61P29/00 ,  A61P35/00 ,  A61P35/04 ,  A61P43/00 ,  C07C235/38 ,  C07C237/20 ,  C07C271/18 ,  C07C271/22 ,  C07D207/16 ,  C07D211/34 ,  C07D217/26 ,  C07D233/90 ,  C07D309/04 ,  C07D521/00 ,  A61K31/47 ,  A61K31/165 ,  A61K31/35 ,  A61K31/40 ,  A61K31/415 ,  A61K31/44 ,  C07C235/56 ,  C07C271/36 ,  C07D211/20 ,  C07D217/12 ,  C07D309/14

CPC classification number: C07D231/12 ,  C07C235/38 ,  C07C237/20 ,  C07C271/22 ,  C07C2601/08 ,  C07C2603/18 ,  C07D207/16 ,  C07D211/34 ,  C07D217/26 ,  C07D233/56 ,  C07D249/08 ,  C07D309/04

Abstract: This invention provides certain compounds, methods of their preparation, pharmaceutical compositions comprising the compounds, and their use in treating human or animal disorders. The compounds of the invention are useful as modulators of the interaction between the receptor for advanced glycated end products (RAGE) and its ligands, such as advanced glycated end products (AGEs), S100/calgranulin/EN-RAGE, beta -amyloid and amphoterin, and for the management, treatment, control, or as an adjunct treatment for diseases in humans caused by RAGE. Such diseases or disease states include acute and chronic inflammation, the development of diabetic late complications such as increased vascular permeability, nephropathy, atherosclerosis, and retinopathy, the development of Alzheimer's disease, erectile dysfunction, and tumor invasion and metastasis.

Abstract translation: 本发明提供了某些化合物，它们的制备方法，包含这些化合物的药物组合物，以及它们在治疗人或动物疾病中的用途。 本发明化合物可用作晚期糖基化终产物（RAGE）受体与其配体如高级糖基化终产物（AGEs），S100 /钙粒蛋白/ EN-RAGE，β-淀粉样蛋白和两性蛋白之间相互作用的调节剂 ，以及用于RAGE引起的人类疾病的管理，治疗，控制或辅助治疗。 这些疾病或疾病状态包括急性和慢性炎症，糖尿病晚期并发症如血管通透性增加，肾病，动脉粥样硬化和视网膜病的发展，阿尔茨海默氏病的发展，勃起功能障碍以及肿瘤浸润和转移。

公开(公告)号：WO2002069965A1

公开(公告)日：2002-09-12

申请号：PCT/US2002/006706

申请日：2002-03-05

Applicant: TRANSTECH PHARMA, INC. ,  MJALLI, Adnan, M., M. ,  GOPALASWAMY, Ramesh

Inventor： MJALLI, Adnan, M., M. ,  GOPALASWAMY, Ramesh

IPC: A61K31/4184

CPC classification number: A61K31/4188 ,  C07D235/14 ,  C07D235/16

Abstract: This invention provides certain compounds, methods of their preparation, pharmaceutical compositions comprising the compounds, and their use in treating human or animal disorders. The compounds of the invention are useful as modulators of the interaction between the receptor for advanced glycated end products (RAGE) and its ligands, such as advanced glycated end products (AGEs), S100/calgranulin/EN-RAGE, ß-amyloid and amphoterin, and for the management, treatment, control, or as an adjunct treatment for diseases in humans caused by RAGE. Such diseases or disease states include acute and chronic inflammation, the development of diabetic late complications such as increased vascular permeability, nephropathy, atherosclerosis, and retinopathy, the development of Alzheimer's disease, erectile dysfunction, and tumor invasion and metastasis.

Abstract translation: 本发明提供某些化合物，其制备方法，包含该化合物的药物组合物及其在治疗人或动物疾病中的用途。 本发明的化合物可用作晚期糖基化终产物（RAGE）的受体与其配体如晚期糖基化终产物（AGE），S100 /钙粒蛋白/ EN-RAGE，β-淀粉样蛋白和两性蛋白之间相互作用的调节剂 ，以及由RAGE引起的人类疾病的管理，治疗，控制或辅助治疗。 这些疾病或疾病状态包括急性和慢性炎症，糖尿病晚期并发症的发展，例如血管通透性增加，肾病，动脉粥样硬化和视网膜病变，阿尔茨海默病的发展，勃起功能障碍和肿瘤侵袭和转移。

公开(公告)号：WO2011103018A1

公开(公告)日：2011-08-25

申请号：PCT/US2011/024311

申请日：2011-02-10

Applicant: HIGH POINT PHARMACEUTICALS, LLC ,  MJALLI, Adnan, M., M. ,  POLISETTI, Dharma, Rao ,  KASSIS, Jareer, Nabeel ,  KOSTURA, Matthew, J. ,  GUZZEL, Mustafa ,  ATTUCKS, Otis, Clinton ,  ANDREWS, Robert, Carl ,  VICTORY, Samuel ,  GUPTA, Suparna

Inventor： MJALLI, Adnan, M., M. ,  POLISETTI, Dharma, Rao ,  KASSIS, Jareer, Nabeel ,  KOSTURA, Matthew, J. ,  GUZZEL, Mustafa ,  ATTUCKS, Otis, Clinton ,  ANDREWS, Robert, Carl ,  VICTORY, Samuel ,  GUPTA, Suparna

IPC: A01N43/78 ,  A61K31/425

CPC classification number: C07D417/12 ,  C07D471/04

Abstract: Substituted fused imidazole derivatives, methods of their preparation, pharmaceutical compositions comprising a substituted fused imidazole derivative, and methods of use in treating inflammation are provided. The substituted fused imidazole derivatives may control of the activity or the amount or both the activity and the amount of heme-oxygenase.

Abstract translation: 提供了取代的稠合咪唑衍生物，其制备方法，包含取代的稠合咪唑衍生物的药物组合物，以及用于治疗炎症的方法。 取代的稠合咪唑衍生物可以控制血红素加氧酶的活性或量或两者的活性和量。

公开(公告)号：WO2006093823A9

公开(公告)日：2006-11-02

申请号：PCT/US2006006571

申请日：2006-02-23

Applicant: TRANSTECH PHARMA INC ,  MJALLI ADNAN M M ,  GOHIMMUKKULA DEVI REDDY ,  TYAGI SAMEER

Inventor： MJALLI ADNAN M M ,  GOHIMMUKKULA DEVI REDDY ,  TYAGI SAMEER

IPC: C07D409/12 ,  A61K31/4725 ,  A61P7/02 ,  A61P9/00 ,  C07C233/87 ,  C07C235/42 ,  C07C235/52 ,  C07C235/60 ,  C07C235/66 ,  C07C237/36 ,  C07C237/42 ,  C07C271/20 ,  C07C311/08 ,  C07C311/09 ,  C07C311/21 ,  C07C311/44 ,  C07C317/32 ,  C07C323/36 ,  C07D217/26 ,  C07D295/155 ,  C07D407/12

CPC classification number: A61K31/47 ,  C07D217/26 ,  C07D405/04 ,  C07D405/12 ,  C07D409/12

Abstract: This invention provides aryl and heteroaryl compounds of formula (X). The compounds of the invention may be useful as antagonists, or partial antagonist of factor IX and/or factor Xl and thus, may be used to inhibit the intrinsic pathway of blood coagulation. Formula (X) wherein R 102 is selected from the group consisting of -C(O)OH, -C(O)OCH 3 , -C(O)O-t-butyl, -C(O)NH-OCH 2 -phenyl, C(O)NHOH, and -C(O)NHSO 2 CH 3 ; and wherein R 101 .R 103 ,R 104 and Y are as defined herein.

Abstract translation: 本发明提供式（X）的芳基和杂芳基化合物。 本发明的化合物可用作拮抗剂或因子IX和/或因子XI的部分拮抗剂，因此可用于抑制凝血的内在途径。 式（X）其中R 102选自-C（O）OH，-C（O）OCH 3，-C（O）O 2 - 丁基，-C（O）NH-OCH 2 - 苯基，C（O）NHOH和-C（O）NHSO 2 CH 3 >; 并且其中R 101 101 R 103，R 104和Y如本文所定义。

公开(公告)号：WO2004071447A2

公开(公告)日：2004-08-26

申请号：PCT/US2004004074

申请日：2004-02-12

Applicant: TRANSTECH PHARMA INC ,  MJALLI ADNAN M M ,  ANDREWS ROBERT C ,  YARRAGUNTA RAVINDRA R ,  XIE RONGYUAN ,  SUBRAMANIAN GOVINDAN ,  QUADA JR JAMES C ,  ARIMILLI MURTY N ,  POLISETTI DHARMA R

Inventor： MJALLI ADNAN M M ,  ANDREWS ROBERT C ,  YARRAGUNTA RAVINDRA R ,  XIE RONGYUAN ,  SUBRAMANIAN GOVINDAN ,  QUADA JR JAMES C ,  ARIMILLI MURTY N ,  POLISETTI DHARMA R

IPC: A61K20060101 ,  A61K31/40 ,  A61K31/4178 ,  A61K31/422 ,  A61K31/426 ,  C07D233/54 ,  C07D263/32 ,  C07D401/10 ,  C07D401/12 ,  C07D403/04 ,  C07D403/10 ,  C07D403/12 ,  C07D405/10 ,  C07D405/12 ,  C07D407/12 ,  C07D413/04 ,  C07D417/12 ,  A61K

CPC classification number: C07D417/12 ,  C07D233/54 ,  C07D263/32 ,  C07D401/10 ,  C07D401/12 ,  C07D403/04 ,  C07D403/10 ,  C07D403/12 ,  C07D405/10 ,  C07D405/12 ,  C07D413/04

Abstract: This invention provides azoles which may be useful as inhibitors of protein tyrosine phosphatases (PTPases). The present invention provides compounds of Formula (I), methods of their preparation, pharmaceutical compositions comprising the compounds and their use in treating human or animal disorders. The compounds of the invention may be useful as inhibitors of protein tyrosine phosphatases and thus can be useful for the management, treatment, control and adjunct treatment of diseases mediated by PTPase activity. Such diseases include Type I diabetes, Type II diabetes.

Abstract translation: 本发明提供可用作蛋白酪氨酸磷酸酶（PTPases）的抑制剂的唑类。 本发明提供式（I）化合物，其制备方法，包含该化合物的药物组合物及其在治疗人或动物疾病中的用途。 本发明的化合物可用作蛋白质酪氨酸磷酸酶的抑制剂，因此可用于由PTPase活性介导的疾病的管理，治疗，控制和辅助治疗。 这些疾病包括I型糖尿病，II型糖尿病。

公开(公告)号：WO2011103018A8

公开(公告)日：2011-10-27

申请号：PCT/US2011024311

申请日：2011-02-10

Applicant: HIGH POINT PHARMACEUTICALS LLC ,  MJALLI ADNAN M M ,  POLISETTI DHARMA RAO ,  KASSIS JAREER NABEEL ,  KOSTURA MATTHEW J ,  GUZEL MUSTAFA ,  ATTUCKS OTIS CLINTON ,  ANDREWS ROBERT CARL ,  VICTORY SAMUEL ,  GUPTA SUPARNA

Inventor： MJALLI ADNAN M M ,  POLISETTI DHARMA RAO ,  KASSIS JAREER NABEEL ,  KOSTURA MATTHEW J ,  GUZEL MUSTAFA ,  ATTUCKS OTIS CLINTON ,  ANDREWS ROBERT CARL ,  VICTORY SAMUEL ,  GUPTA SUPARNA

IPC: A01N43/78 ,  A61K31/425

CPC classification number: C07D417/12 ,  C07D471/04

Abstract: Substituted fused imidazole derivatives, methods of their preparation, pharmaceutical compositions comprising a substituted fused imidazole derivative, and methods of use in treating inflammation are provided. The substituted fused imidazole derivatives may control of the activity or the amount or both the activity and the amount of heme-oxygenase.

Abstract translation: 提供取代的稠合咪唑衍生物，其制备方法，包含取代的稠合咪唑衍生物的药物组合物和用于治疗炎症的方法。 取代的稠合咪唑衍生物可以控制血红素加氧酶的活性或活性和量的量。

公开(公告)号：WO2010114824A8

公开(公告)日：2011-10-06

申请号：PCT/US2010029172

申请日：2010-03-30

Applicant: TRANSTECH PHARMA INC ,  MJALLI ADNAN M M ,  BEHME CHRISTOPHER ,  CHRISTEN DANIEL P ,  POLISETTI DHARMA RAO ,  QUADA JAMES ,  SANTHOSH KALPATHY ,  BONDLELA MURALIDHAR ,  GUZEL MUSTAFA ,  YARRAGUNTA RAVINDRA REDDY ,  GOHIMUKKULA DEVI REDDY ,  ANDREWS ROBERT CARL ,  DAVIS STEPHEN THOMAS ,  YOKUM THOMAS SCOTT ,  FREEMAN JENNIFER L R

Inventor： MJALLI ADNAN M M ,  BEHME CHRISTOPHER ,  CHRISTEN DANIEL P ,  POLISETTI DHARMA RAO ,  QUADA JAMES ,  SANTHOSH KALPATHY ,  BONDLELA MURALIDHAR ,  GUZEL MUSTAFA ,  YARRAGUNTA RAVINDRA REDDY ,  GOHIMUKKULA DEVI REDDY ,  ANDREWS ROBERT CARL ,  DAVIS STEPHEN THOMAS ,  YOKUM THOMAS SCOTT ,  FREEMAN JENNIFER L R

IPC: A01N35/00 ,  A61K31/12

CPC classification number: C07D491/056 ,  C07D319/20 ,  C07D491/06

Abstract: The present invention is directed to substituted azoanthracene derivatives or pharmaceutically acceptable salts thereof that modulate the human GLP-1 receptor and that may be useful in the treatment of diseases, disorders, or conditions in which modulation of the human GLP-1 receptor is beneficial, such as diabetes mellitus type 2. The invention is also directed to pharmaceutical compositions comprising these compounds and to the use of these compounds and compositions in the treatment of such diseases, disorders, or conditions in which modulation of the human GLP-1 receptor is beneficial.

Abstract translation: 本发明涉及调节人GLP-1受体并且可用于治疗人GLP-1受体调节有益的疾病，病症或病症的取代的偶氮蒽衍生物或其药学上可接受的盐， 例如2型糖尿病。本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在治疗人GLP-1受体调节有益的疾病，病症或病症中的用途 。