公开(公告)号：US20110319369A1

公开(公告)日：2011-12-29

申请号：US13146001

申请日：2010-02-05

Applicant: David Casebier ,  Scott Chappel

Inventor： David Casebier ,  Scott Chappel

IPC: A61K31/58 ,  A61P35/00

CPC classification number: A61K45/06 ,  A61K31/58 ,  A61K2300/00

Abstract: The invention describes methods of treating cancer in which a therapeutically-effective amount of a 17α-hydroxylase/C17,20-lyase inhibitor is administered to a subject in need thereof, including a subject with a refractory cancer and/or a subject currently undergoing another cancer treatment, wherein the 17α-hydroxylase/C17,20-lyase inhibitor is administered in combination with a therapeutically-effective amount of at least one additional therapeutic agent, including, but not limited to, another anti-cancer agent or a steroid.

Abstract translation: 本发明描述了治疗癌症的方法，其中将治疗有效量的17α-羟化酶/ C17,20-裂解酶抑制剂施用于有需要的受试者，包括患有难治性癌症的受试者和/或目前正在接受其他对象 癌症治疗，其中17α-羟化酶/ C17,20-裂解酶抑制剂与治疗有效量的至少一种另外的治疗剂组合施用，包括但不限于另一种抗癌剂或类固醇。

公开(公告)号：US20110312924A1

公开(公告)日：2011-12-22

申请号：US13145997

申请日：2010-02-05

Applicant: David Casebier

Inventor： David Casebier

IPC: A61K31/58 ,  A61P35/00 ,  C07J43/00

CPC classification number: C07J43/003 ,  A61K31/58 ,  A61K45/06

Abstract: Steroidal C-17 nitrogen-containing heterocycles of Formula I: wherein: the ABCD ring structure is the nucleus of a steroid, or an analog thereof; X is a group capable of coordinating a heme group of CYP17, and Y is an hydroxyl functionality, a suitable ester, or a prodrug group, for the treatment of urogenital and/or androgen-related cancers, such as castration-resistant prostate cancer. The invention provides methods of synthesizing new chemical entities and methods of using the same in treating urogenital and/or androgen-related cancers.

Abstract translation: 式I的甾体C-17含氮杂环：其中：ABCD环结构是类固醇或其类似物的核; X是能够协调CYP17的血红素基团，Y是羟基官能团，合适的酯或前药基团，用于治疗泌尿生殖和/或雄激素相关的癌症如去钙抗性前列腺癌。 本发明提供合成新化学物质的方法及其在治疗泌尿生殖和/或雄激素相关癌症中的应用。

公开(公告)号：US20060083681A1

公开(公告)日：2006-04-20

申请号：US11243869

申请日：2005-10-05

Applicant: Ajay Purohit ,  David Casebier

Inventor： Ajay Purohit ,  David Casebier

IPC: A61K51/00 ,  C07F15/00 ,  C07F5/00 ,  C07F13/00

CPC classification number: C07D213/68 ,  A61K51/0455 ,  C07B59/002 ,  C07D215/233 ,  C07F13/005

Abstract: The present disclosure is directed to compounds comprising imaging moieties and their use for diagnosing certain disorders.

Abstract translation: 本公开涉及包含成像部分的化合物及其用于诊断某些病症的用途。

公开(公告)号：US20050196813A1

公开(公告)日：2005-09-08

申请号：US11081784

申请日：2005-03-16

Applicant: Anthony Kreft ,  Derek Cole ,  Kevin Woller ,  Joseph Stock ,  George Diamantidis ,  Dennis Kubrak ,  Kristina Kutterer ,  William Moore ,  David Casebier

Inventor： Anthony Kreft ,  Derek Cole ,  Kevin Woller ,  Joseph Stock ,  George Diamantidis ,  Dennis Kubrak ,  Kristina Kutterer ,  William Moore ,  David Casebier

IPC: A61K31/341 ,  A61K31/381 ,  A61K31/382 ,  A61K31/4436 ,  A61K31/4535 ,  A61P25/28 ,  A61P43/00 ,  C07D233/66 ,  C07D277/32 ,  C07D307/64 ,  C07D333/34 ,  C07D333/48 ,  C07D409/12 ,  G01N33/53

CPC classification number: C07D409/12 ,  C07D307/64 ,  C07D333/34

Abstract: Compounds of Formula (I), wherein R1, R2, R3, R4, R5, R6, T, W, X, Y and Z are as defined herein are provided, together with pharmaceutically acceptable salt, hydrates and/or prodrugs thereof. Methods of using these compounds for inhibiting beta amyloid production and for treatment of Alzheimer's Disease and Down's syndrome are described

Abstract translation: 式（I）化合物，其中R 1，R 2，R 3，R 4，R 3， 提供了本文所定义的R 5，R 6，T，W，X，Y和Z以及其药学上可接受的盐，水合物和/或前药。 描述了使用这些化合物抑制β淀粉样蛋白生成和治疗阿尔茨海默病和唐氏综合征的方法

公开(公告)号：US5962736A

公开(公告)日：1999-10-05

申请号：US013709

申请日：1998-01-26

Applicant: Robert Zambias ,  David A. Bolten ,  Joseph C. Hogan ,  Paul Furth ,  David Casebier ,  Cheng Tu

Inventor： Robert Zambias ,  David A. Bolten ,  Joseph C. Hogan ,  Paul Furth ,  David Casebier ,  Cheng Tu

IPC: G01N33/15 ,  C07B61/00 ,  G06F17/30 ,  G06F17/50 ,  C07C233/00

CPC classification number: C40B50/08 ,  C40B30/04 ,  Y10S977/774 ,  Y10S977/779 ,  Y10S977/789 ,  Y10S977/791

Abstract: A logically ordered array of 10,240 different compounds, each compound prepared from the reaction product of an oxazolone, aldehyde and amine.

Abstract translation: 一种具有10,240种不同化合物的逻辑有序阵列，每种化合物由恶唑酮，醛和胺的反应产物制备。

公开(公告)号：US20050191238A1

公开(公告)日：2005-09-01

申请号：US11055498

申请日：2005-02-10

Applicant: David Casebier ,  Simon Robinson ,  Ajay Purohit ,  Heike Radeke ,  Michael Azure ,  Douglas Dischino

Inventor： David Casebier ,  Simon Robinson ,  Ajay Purohit ,  Heike Radeke ,  Michael Azure ,  Douglas Dischino

IPC: A61K49/00 ,  A61K51/00

CPC classification number: C07D237/16 ,  A61K49/00 ,  A61K49/0002 ,  A61K49/0052 ,  A61K49/10 ,  A61K49/22 ,  A61K51/04 ,  A61K51/0421 ,  A61K51/0453 ,  A61K51/0459 ,  C07B59/002

Abstract: The present disclosure is directed, in part, to compounds and methods for imaging myocardial perfusion, comprising administering to a patient a contrast agent which comprises a compound that binds MC-1, and an imaging moiety, and scanning the patient using diagnostic imaging.

公开(公告)号：US20050136003A1

公开(公告)日：2005-06-23

申请号：US10974238

申请日：2004-10-27

Applicant: David Casebier

Inventor： David Casebier

IPC: A61K49/00 ,  A61K51/00 ,  C07F5/00 ,  C07J17/00

CPC classification number: A61K51/0493 ,  A61K51/0427 ,  A61K51/0455 ,  A61K51/0459 ,  A61K51/0465 ,  A61K51/0491

Abstract: The present invention is directed to novel chemical agents for compounds and their use for imaging myocardial perfusion. The invention also is directed to a kit for forming such novel agents. The chemical agents for the present invention comprising (a) a cardiotonic moiety and (b) an imaging moiety.

Abstract translation: 本发明涉及用于化合物的新型化学试剂及其用于心肌灌注成像的用途。 本发明还涉及用于形成这种新型试剂的试剂盒。 本发明的化学试剂包括（a）强心部分和（b）成像部分。

公开(公告)号：US5892113A

公开(公告)日：1999-04-06

申请号：US999459

申请日：1997-12-29

Applicant: Joseph C. Hogan, Jr. ,  David Casebier ,  Paul S. Furth ,  Steve Gallion ,  Alan Kaplan

Inventor： Joseph C. Hogan, Jr. ,  David Casebier ,  Paul S. Furth ,  Steve Gallion ,  Alan Kaplan

IPC: A61K38/00 ,  A61K31/16 ,  A61K31/66 ,  A61P43/00 ,  C07C243/24 ,  C07C243/40 ,  C07C271/20 ,  C07D213/81 ,  C07D213/82 ,  C07D307/20 ,  C07D309/12 ,  C07C211/03

CPC classification number: C07D213/81 ,  C07C243/40 ,  C07C271/20 ,  C07D213/82 ,  C07D307/20 ,  C07D309/12 ,  C07C2101/02 ,  C07C2101/14

Abstract: This invention relates to a class of aminimides structurally characterized as an acyl nitrogen-nitrogen ylide such that the acyl moiety possess the structural diversity element G, the quaternary nitrogen possess structural diversity elements E and F, and the quaternary nitrogen is bonded to a hydroxyethyl substituent, which in turn is bonded to an aminomethylene moiety that possess structural diversity elements A and B from the amino group and diversity element c from the methylene substituent, as shown below, ##STR1## wherein structural diversity element A, B, C, D, E, F and G are chosen from the set of elements consisting of substituted and unsubstituted as well as branched and straight chain alkyl, aryl, alkaryl, aralkyl, carbocyclic, heterocyclic, hydrogen, amino acid, peptide, polypeptide, protein, depsipeptide, carbohydrate derivatives, nucleotide derivatives, oligonucleotide derivatives, naturally occurring or synthetic organic structural motifs, reporter elements, organic moieties containing at least one polymerizable group, macromolecular component, resin, silicate, other surface and particle support, the diversity elements can be the same, can be different, and can also be connected to form a ringed to several ringed species.

Abstract translation: 本发明涉及一类结构特征为酰基氮 - 氮内鎓盐的氨基酰亚胺，使得酰基部分具有结构多样性元素G，季氮具有结构多样性元素E和F，并且季氮键合到羟乙基取代基 ，其又结合到具有来自亚甲基取代基的氨基和多样性元件c的结构多样性元件A和B的氨基亚甲基部分，如下所示，其中结构分集元件A，B，C，D 芳基，烷芳基，芳烷基，碳环，杂环，氢，氨基酸，肽，多肽，蛋白质，前肽，前列腺素， 碳水化合物衍生物，核苷酸衍生物，寡核苷酸衍生物，天然存在或合成的有机结构基序，报道元件，有机物 含有至少一个可聚合基团，大分子组分，树脂，硅酸盐，其他表面和颗粒载体的结合物，多样性元素可以相同，可以不同，并且还可以连接形成环状至几个环状物质。

公开(公告)号：US5736412A

公开(公告)日：1998-04-07

申请号：US649371

申请日：1996-05-17

Applicant: Robert Zambias ,  David A. Bolten ,  Joseph C. Hogan ,  Paul Furth ,  David Casebier ,  Cheng Tu

Inventor： Robert Zambias ,  David A. Bolten ,  Joseph C. Hogan ,  Paul Furth ,  David Casebier ,  Cheng Tu

IPC: G01N33/15 ,  C07B61/00 ,  G06F17/30 ,  G06F17/50 ,  G01N33/543

CPC classification number: C40B50/08 ,  C40B30/04 ,  Y10S977/774 ,  Y10S977/779 ,  Y10S977/789 ,  Y10S977/791

Abstract: This invention is directed to an m.times.n array of different chemical compounds wherein each of said compounds has at least one structural diversity element selected from a group of amines and ketones and wherein the scaffold structure is selected from a group consisting of aminimide, imidazolone, sulfonylaminimide and phosphonylaminimide.

Abstract translation: 本发明涉及不同化合物的mxn阵列，其中每个所述化合物具有至少一种选自一组胺和酮的结构多样性元件，其中所述支架结构选自氨基酰亚胺，咪唑啉酮，磺酰氨基酰亚胺和 膦酰氨基酰亚胺。

公开(公告)号：US20110312916A1

公开(公告)日：2011-12-22

申请号：US13146004

申请日：2010-02-05

Applicant: David Casebier

Inventor： David Casebier

IPC: A61K31/675 ,  A61P15/00 ,  A61P35/00 ,  C07J43/00 ,  A61K31/58

Abstract: Prodrugs of C-17-heterocyclic-steroidal drugs providing improved oral bioavailability and pharmacokinetics are described. The drugs are inhibitors of human CYP 17 enzyme, as well as potent antagonists of both wild type and mutant androgen receptors (AR), and are useful for the treatment of urogenital and/or androgen-related cancers, diseases and/or conditions, such as human prostate cancer, breast cancer, and prostate hyperplasia. The disclosure describes methods of synthesizing and using the prodrugs in cancer therapy.

Abstract translation: 描述了提供改善的口服生物利用度和药代动力学的C-17-杂环类甾体药物的前药。 这些药物是人CYP17酶的抑制剂，以及野生型和突变体雄激素受体（AR）的有效拮抗剂，可用于治疗泌尿生殖和/或雄激素相关的癌症，疾病和/或病症，例如 作为人前列腺癌，乳腺癌和前列腺增生。 本公开描述了在癌症治疗中合成和使用前药的方法。