Novel Substituted Steroid Hormones

该研究项目的目标是开发新型男性避孕药。候选药物已经开发出来，并通过员工发明报告提交了专利申请。这类类固醇核心分子可能是一种一流的男性避孕药，具有血清睾酮负责的所有必要的激素特性。衍生的候选先导药物可用于制备口服或透皮凝胶、贴剂或气雾剂制剂的促雄激素活性24小时，或可在注射、植入、微针阵列或其他给药方法用于男性避孕或潜在内分泌治疗时提供持续数月的活性。 作为一种男性避孕药，本发明利用了具有雄激素活性、口服生物利用度的分子，并结合了在持续时间内保持药物水平的修饰，从而将口服剂量限制在每天一剂。因此，一个分子包含多个激素活动，以满足所有必要的激素活动，这是血清睾酮所必需的，但不支持导致精子生成的睾丸功能。正在对几个候选的主要受体结合和激活特性进行评估，这些特性展示了该药物所需的功能活性。由于这些产品如果成功实现了预期的功能，将具有商业用途，因此只有在通过适当渠道提交专利申请后才能发行出版物。

The research project has a goal to develop novel male contraceptive agents. Candidate drugs have been developed and have been submitted for patents through an employee invention report. This class of steroid core molecules could be a first-in-class male contraceptive agent that possesses all necessary hormonal properties for which serum testosterone is responsible. Lead candidates are derivitized to prepare pro-drugs that can sustain the androgenic activity for 24 hours for oral or transdermal gel, patch or aerosol formulations or could provide extended activity over several months when administered as an injection, implant, microneedle array or other delivery method for the purpose of male contraception or potential endocrine therapies. As a male contraceptive agent, this invention takes advantage of molecules with demonstrated androgenic activity, oral bioavailability and combines modifications that maintain drug levels over a sustained period so that oral dosing is limited to one dose per day. Thus, one molecule contains multiple hormonal activities that fulfill all necessary hormonal activities for which serum testosterone is required but does not support testicular function that would lead to spermatogenesis. Several lead candidates are being evaluated for receptor binding and transactivation properties that demonstrate the desired functional activities of the drug. Since the products, if successful in achieving the desired functions, would have commercial utility, publications cannot be issued until after patent applications have been filed through appropriate channels.