专利号:US-7022730-B2 优先权日:2001-10-19 标题:Bis-heteroaryl alkanes as therapeutic agents 发明人:MJALLI ADNAN M M; SHAHBAZ KATHY G J 权利人:TRANSTECH PHARMA INC 摘要:This invention provides compounds which are useful as inhibitors of protein tyrosine phosphatases (PTPases). As inhibitors of PTPases the compounds of the invention are useful for the management, treatment, control and adjunct treatment of diseases in mammals mediated by PTPase activity. Such diseases include type I diabetes, type II diabetes, immune dysfunction, AIDS, autoimmunity, glucose intolerance, obesity, cancer, psoriasis, allergic diseases, infectious diseases, inflammatory diseases, diseases involving the modulated synthesis of growth hormone or the modulated synthesis of growth factors or cytokines which affect the production of growth hormone, or Alzheimer's disease.
专利号:US-8916705-B2 优先权日:2011-10-14 标 题:Procaspase-activating compounds and compositions 发明人:HERGENROTHER PAUL J 权利人:UNIV ILLINOIS; TRUSTEES OF THE UNIVERSITY OF ILLILNOIS BOARD OF 摘要:The invention provides compounds and compositions useful for the modulation of certain enzymes. The compounds and compositions can induce of cell death, particularly cancer cell death. The invention also provides methods for the synthesis and use of the compounds and compositions, including the use of compounds and compositions in therapy for the treatment of cancer and selective induction of apoptosis in cells.
专利号:EP-4058432-A1 优先权日:2019-11-14 标 题:Improved synthesis of kras g12c inhibitor compound
专利号:US-9663482-B2 优先权日:2012-08-03 标 题:Substituted piperazinyl acetohydrazide procaspase-activating compounds 发明人:HERGENROTHER PAUL J; ROTH HOWARD S 权利人:UNIV ILLINOIS 摘要:The invention provides compounds and compositions useful for the modulation of certain enzymes. The compounds are of Formula I n nThe compounds and compositions can induce of cell death, particularly cancer cell death. The invention also provides methods for the synthesis and use of the compounds and compositions, including the use of compounds and compositions in therapy for the treatment of cancer and selective induction of apoptosis in cells.
专利号:US-2014315915-A1 优先权日:2009-02-09 标题:Design, synthesis and evaluation of procaspase activating compounds as personalized anti-cancer drugs
专利号:US-9522901-B2 优先权日:2005-05-26 标题:Compositions and methods including cell death inducers and procaspase activation 发明人:HERGENROTHER PAUL J; PUTT KARSON S; PETERSON QUINN P; FAKO VALERIE 权利人:UNIV ILLINOIS 摘要:Compositions and methods are disclosed in embodiments relating to induction of cell death such as in cancer cells. Compounds and related methods for synthesis and use thereof, including the use of compounds in therapy for the treatment of cancer and selective induction of apoptosis in cells are disclosed. Compounds are disclosed in connection with modification of procaspases such as procaspase-3. In embodiments, compositions are capable of activation of procaspase-3.
1: Inglott MA, Lerner EA, Pilowsky PM, Farnham MM. Activation of PAC(1) and VPAC receptor subtypes elicits differential physiological responses from sympathetic preganglionic neurons in the anaesthetized rat. Br J Pharmacol. 2012 Nov;167(5):1089-98. doi: 10.1111/j.1476-5381.2012.02045.x. 2: Hsu DC, Roth HS, West DC, Botham RC, Novotny CJ, Schmid SC, Hergenrother PJ. Parallel synthesis and biological evaluation of 837 analogues of procaspase-activating compound 1 (PAC-1). ACS Comb Sci. 2012 Jan 9;14(1):44-50. doi: 10.1021/co2001372. Epub 2011 Oct 28. 3: Zhang X, Tan F, Duan CZ. [Effect of electro-needling at acupoints of the yangming meridian on the expression of PAC-1 and lower limb functions in acute cerebral infarction patients]. Zhongguo Zhong Xi Yi Jie He Za Zhi. 2011 Apr;31(4):483-6. Chinese. doi: 10.1016/j.jpba.2010.07.042. Epub 2010 Aug 6. Chinese. doi: 10.1007/s10637-010-9445-z. Epub 2010 May 25.
合成参考文献
摘要:Li M, Cong Y, Deng X, Hu J, Qin X. [Impact of shear stress on expression of platelet membrane glycoproteins]. Zhonghua Yi Xue Za Zhi. 2002 Feb 25;82(4):267–70. 参考文献:10.1158/0008-5472.can-03-3424 摘要:Givant-Horwitz V, Davidson B, Reich R. Laminin-induced signaling in tumor cells: the role of the M(r) 67,000 laminin receptor. Cancer Res. 2004 May 15;64(10):3572–9. doi: 10.1158/0008-5472.can-03-3424. 摘要:Angiolillo DJ, Fernandez-Ortiz A, Bernardo E, Ramírez C, Sabaté M, Hernández-Antolín R, Moreno R, Escaned J, Alfonso F, Bañuelos C, Macaya C. Is a 300 mg clopidogrel loading dose sufficient to inhibit platelet function early after coronary stenting A platelet function profile study. J Invasive Cardiol. 2004 Jun;16(6):325–9. 参考文献:10.1136/pgmj.2006.047696 摘要:Serebruany VL, Midei MG, Meilman H, Malinin AI, Lowry DR. Platelet inhibition with prasugrel (CS-747) compared with clopidogrel in patients undergoing coronary stenting: the subset from the JUMBO study. Postgrad Med J. 2006 Jun;82(968):404–10. 参考文献:10.1111/j.1538-7836.2009.03716.x 摘要:PENNINGS GJ, YONG ASC, KRITHARIDES L. Expression of EMMPRIN (CD147) on circulating platelets in vivo. Journal of Thrombosis and Haemostasis. 2010 Mar;8(3):472–81. doi: 10.1111/j.1538-7836.2009.03716.x.