公开(公告)号：US20090069281A1

公开(公告)日：2009-03-12

申请号：US12229326

申请日：2008-08-20

Applicant: Brian C. Austad ,  Louis Grenier ,  Edward B. Holson ,  John J. Lee ,  Roger H. Pak ,  James R. Porter ,  James L. Wright

Inventor： Brian C. Austad ,  Louis Grenier ,  Edward B. Holson ,  John J. Lee ,  Roger H. Pak ,  James R. Porter ,  James L. Wright

IPC: A61K31/395 ,  A61P35/00 ,  A61P35/02 ,  C07D225/06

CPC classification number: A61K9/146 ,  A61K31/33 ,  C07D225/04

Abstract: Provided herein, inter alia, are solid forms of geldanamycin analogs, pharmaceutical compositions comprising a geldanamycin analog and a crystallization inhibitor, methods of making and using such compositions. Additionally, provided are methods for the treatment of cancer, a neoplastic disease state and/or a hyperproliferative disorder, and methods of inhibiting Heat Shock Protein 90 (“Hsp90”).

公开(公告)号：US20120083607A1

公开(公告)日：2012-04-05

申请号：US13175053

申请日：2011-07-01

Applicant: Brian c. Austad ,  Adilah Bahadoor ,  Jitendra D. Belani ,  Somarajannair Janardanannair ,  Charles W. Johannes ,  Gregg F. Keaney ,  Priscilla L. White ,  Sheldon L. Wallerstein

Inventor： Brian c. Austad ,  Adilah Bahadoor ,  Jitendra D. Belani ,  Somarajannair Janardanannair ,  Charles W. Johannes ,  Gregg F. Keaney ,  Priscilla L. White ,  Sheldon L. Wallerstein

IPC: C07D491/048 ,  C12P17/18

CPC classification number: C12P17/18 ,  C07D491/10 ,  C07D491/107

Abstract: Provided are processes for the synthesis of amino analogues from ketone starting materials.

Abstract translation: 提供了从酮起始原料合成氨基类似物的方法。

公开(公告)号：US20140371456A1

公开(公告)日：2014-12-18

申请号：US14257658

申请日：2014-04-21

Applicant: Brian C. Austad ,  Adilah Bahadoor ,  Jitendra D. Belani ,  Somarajannair Janardanannair ,  Sheldon L. Wallerstein ,  Gregg F. Keaney ,  Priscilla L. White ,  Charles W. Johannes

Inventor： Brian C. Austad ,  Adilah Bahadoor ,  Jitendra D. Belani ,  Somarajannair Janardanannair ,  Sheldon L. Wallerstein ,  Gregg F. Keaney ,  Priscilla L. White ,  Charles W. Johannes

IPC: C07D491/107 ,  C12P17/18

CPC classification number: C12P17/18 ,  C07D491/10 ,  C07D491/107

Abstract: Provided are processes for the synthesis of amino analogues from ketone starting materials.

Abstract translation: 提供了从酮起始原料合成氨基类似物的方法。

公开(公告)号：US08716479B2

公开(公告)日：2014-05-06

申请号：US12810600

申请日：2008-12-24

Applicant: Brian C. Austad ,  Andre Lescarbeau ,  Lin-Chen Yu

Inventor： Brian C. Austad ,  Andre Lescarbeau ,  Lin-Chen Yu

IPC: C07D471/02 ,  C07D311/96

CPC classification number: C07J7/009 ,  C07B2200/09 ,  C07D471/10 ,  C07D491/22 ,  C07J1/0011 ,  C07J5/0053 ,  C07J9/00 ,  C07J21/00 ,  C07J43/006 ,  C07J63/00 ,  C07J65/00 ,  C07J69/00 ,  C07J71/0005

Abstract: The invention is directed to a method to reduce a C—C double bond of an enone of a steroidal compound to produce a mixture of β ketone product and α ketone product, comprising treating a solution or suspension of the steroidal compound in a solvent with hydrogen gas in the presence of a catalyst and a substituted pyridine.

Abstract translation: 本发明涉及一种降低甾族化合物的烯酮的C-C双键以产生“bgr”的混合物的方法。 酮产物和α-酮产物，包括在催化剂和取代的吡啶的存在下，用氢气处理溶剂中的甾族化合物的溶液或悬浮液。

公开(公告)号：US08283343B2

公开(公告)日：2012-10-09

申请号：US12229277

申请日：2008-08-20

Applicant: Brian C. Austad ,  Louis Grenier ,  Edward B. Holson ,  John J. Lee ,  Roger H. Pak ,  James R. Porter ,  James L. Wright

Inventor： Brian C. Austad ,  Louis Grenier ,  Edward B. Holson ,  John J. Lee ,  Roger H. Pak ,  James R. Porter ,  James L. Wright

IPC: A61K31/27 ,  A61K31/33

CPC classification number: A61K9/146 ,  A61K31/33 ,  C07D225/04

Abstract: Amorphous, polymorphic, and solvated forms of 17-amino geldanamycin are disclosed. These compounds are particularly useful for the treatment of cancer, a neoplastic disease state and/or a hyperproliferative disorder, and inhibiting Heat Shock Protein 90 (“Hsp90”).

Abstract translation: 公开了17-氨基格尔德霉素的无定形，多晶型和溶剂化形式。 这些化合物特别可用于治疗癌症，肿瘤疾病状态和/或过度增殖性疾病，并且抑制热休克蛋白90（Hsp90）。

公开(公告)号：US20120065399A1

公开(公告)日：2012-03-15

申请号：US13232851

申请日：2011-09-14

Applicant: Daniel G. Genov ,  Brian C. Austad ,  Brian H. White

Inventor： Daniel G. Genov ,  Brian C. Austad ,  Brian H. White

IPC: C07D491/048 ,  C07F17/02

CPC classification number: C07D491/107 ,  B01J31/181 ,  B01J31/2428 ,  B01J2231/643 ,  B01J2531/821 ,  C07D491/048 ,  C07F17/02

Abstract: Provided herein is a process for the transfer-hydrogenation of ketone analogs of members of the jervine type of Veratrum alkaloids, such as cyclopamine. Also provided herein are novel ruthenium transfer-hydrogenation catalysts.

Abstract translation: 本文提供了一种用于转化氢化Ver藜类生物碱成员的酮类似物的方法，例如环巴胺。 本文还提供了新的钌转移氢化催化剂。

公开(公告)号：US20080221077A1

公开(公告)日：2008-09-11

申请号：US12001239

申请日：2007-12-11

Applicant: Brian C. Austad ,  Louis Grenier ,  Edward B. Holson ,  John J. Lee ,  Roger H. Pak ,  James R. Porter ,  James L. Wright

Inventor： Brian C. Austad ,  Louis Grenier ,  Edward B. Holson ,  John J. Lee ,  Roger H. Pak ,  James R. Porter ,  James L. Wright

IPC: A61K31/397 ,  A61K31/395 ,  C07D225/06 ,  A61P35/00 ,  A61K31/40

CPC classification number: A61K9/146 ,  A61K31/33 ,  C07D225/04

Abstract: Provided herein, inter alia, are solid forms of geldanamycin analogs, pharmaceutical compositions comprising a geldanamycin analog and a crystallization inhibitor, methods of making and using such compositions. Additionally, provided are methods for the treatment of cancer, a neoplastic disease state and/or a hyperproliferative disorder, and methods of inhibiting Heat Shock Protein 90 (“Hsp90”).

Abstract translation: 特别地，本文提供了固体形式的格尔德霉素类似物，包含格尔德霉素类似物和结晶抑制剂的药物组合物，制备和使用这些组合物的方法。 另外，提供了用于治疗癌症，肿瘤疾病状态和/或过度增殖性疾病的方法，以及抑制热休克蛋白90（“Hsp90”）的方法。