公开(公告)号：US11732000B2

公开(公告)日：2023-08-22

申请号：US17396034

申请日：2021-08-06

Applicant: Sage Therapeutics, Inc.

Inventor： Francesco G. Salituro ,  Albert Jean Robichaud ,  Gabriel Martinez Botella ,  Boyd L. Harrison

IPC: C07J9/00 ,  C07J7/00 ,  A61P23/00 ,  A61P25/20 ,  A61P3/00 ,  C07J17/00 ,  C07J31/00 ,  C07J13/00 ,  C07J41/00

CPC classification number: C07J9/00 ,  A61P3/00 ,  A61P23/00 ,  A61P25/20 ,  C07J17/00 ,  C07J7/002 ,  C07J9/005 ,  C07J13/005 ,  C07J13/007 ,  C07J31/006 ,  C07J41/0061

Abstract: Compounds are provided according to Formula (I) and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein R1, R2, and R3 are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of conditions.

公开(公告)号：US20190010184A1

公开(公告)日：2019-01-10

申请号：US15748716

申请日：2016-07-22

Applicant: Intercept Pharmaceuticals, Inc.

Inventor： Roberto Pellicciari ,  Antimo Gioiello

IPC: C07J9/00 ,  C07J41/00 ,  C07J7/00 ,  C07J13/00

CPC classification number: C07J9/005 ,  C07J1/0011 ,  C07J7/0035 ,  C07J13/005 ,  C07J13/007 ,  C07J41/0005 ,  C07J41/005 ,  C07J71/0005

Abstract: The present application relates to a method of preparing compounds of Formula (I) or a pharmaceutically acceptable salt, solvate, or amino acid conjugate thereof, R1 is H, α-OH, β-OH, or an oxo group.

公开(公告)号：US20170369521A1

公开(公告)日：2017-12-28

申请号：US15426209

申请日：2017-02-07

Applicant: Donesta Bioscience B.V.

Inventor： Johannes Jan PLATTEEUW ,  Herman Jan Tijmen COELINGH BENNINK ,  Franciscus Wilhelmus Petrus DAMEN ,  Michiel Christian Alexander VAN VLIET

IPC: C07J1/00 ,  C07J13/00 ,  C07J75/00

CPC classification number: C07J1/007 ,  C07J1/0059 ,  C07J13/005 ,  C07J75/00 ,  Y02P20/55

Abstract: The present invention relates to a process for the preparation of estra-1,3,5(10)-trien-3, 15a, 16a, 1713-tetraol (estetr-01), via a silyl enol ether derivative 17-B-oxy-3-A-oxy-estra-1,3,5(10), 16-tetraene, wherein A is a protecting group and B is —Si(R2)3. The invention further relates to a process for the synthesis of 3-A-oxy-estra-1,3,5(10), 15-tetraen-17-one, in which A is a protecting group, via silyl enol ether derivative 17-B-oxy-3-A-oxy-estra-1,3,5(10),16-tetraene, and B is —Si(R2)3.

公开(公告)号：US20160022701A1

公开(公告)日：2016-01-28

申请号：US14775401

申请日：2014-03-13

Applicant: SAGE THERAPEUTICS, INC.

Inventor： Kiran Reddy ,  James Doherty

IPC: A61K31/575 ,  G01N33/68 ,  G01N33/92 ,  G01N24/08 ,  A61K31/568 ,  A61K31/56

CPC classification number: A61K31/575 ,  A61K31/56 ,  A61K31/568 ,  C07J1/0011 ,  C07J1/0022 ,  C07J1/0029 ,  C07J3/00 ,  C07J7/002 ,  C07J7/007 ,  C07J9/00 ,  C07J9/005 ,  C07J13/005 ,  C07J13/007 ,  C07J17/00 ,  C07J21/00 ,  C07J21/008 ,  C07J31/006 ,  C07J41/0005 ,  C07J41/0055 ,  C07J41/0061 ,  C07J41/0088 ,  C07J43/003 ,  C07J51/00 ,  G01N24/08 ,  G01N33/5008 ,  G01N33/6896 ,  G01N33/92

Abstract: Provided are methods of evaluating or treating a patient, e.g., a patient having a disorder described herein, comprising: a) optionally, acquiring a patient sample; b) acquiring an evaluation of and/or evaluating the sample for an alteration in the level S24(S)-hydroxycholesterol compared to a reference standard.

Abstract translation: 提供评估或治疗患者，例如患有本文所述障碍的患者的方法，包括：a）任选地获取患者样品; b）与参考标准相比，获得对S24（S） - 羟基胆固醇水平的改变的评估和/或评估样品。

公开(公告)号：US09198921B2

公开(公告)日：2015-12-01

申请号：US13639650

申请日：2011-04-05

Applicant: John M. McCall ,  Eric Hoffman ,  Kanneboyina Nagaraju

Inventor： John M. McCall ,  Eric Hoffman ,  Kanneboyina Nagaraju

IPC: A61K31/56 ,  C07J5/00 ,  A61K31/573 ,  A61K31/575 ,  A61K45/06 ,  C07J7/00 ,  C07J13/00 ,  C07J21/00 ,  C07J51/00

CPC classification number: C07J9/005 ,  A61K31/573 ,  A61K31/575 ,  A61K45/06 ,  C07J5/003 ,  C07J5/0038 ,  C07J5/0053 ,  C07J5/0069 ,  C07J5/0076 ,  C07J7/008 ,  C07J9/00 ,  C07J13/005 ,  C07J21/00 ,  C07J51/00 ,  Y02A50/479

Abstract: The present invention relates to compounds and methods which may be useful as treatments of neuromuscular diseases such as muscular dystrophy, and as inhibitors of NF-κB for the treatment or prevention of muscular wasting disease, including muscular dystrophy.

Abstract translation: 本发明涉及可用作治疗神经肌肉疾病如肌营养不良的化合物和方法，以及作为NF-κB抑制剂用于治疗或预防肌肉萎缩性疾病，包括肌营养不良症的化合物和方法。

公开(公告)号：US20130261317A1

公开(公告)日：2013-10-03

申请号：US13876069

申请日：2011-09-19

Applicant: Robert M. Moriarty ,  Photon Rao

Inventor： Robert M. Moriarty ,  Photon Rao

IPC: C07J41/00 ,  C07J9/00 ,  C07J21/00

CPC classification number: C07J41/0061 ,  A61K31/56 ,  A61K45/06 ,  C07J1/0011 ,  C07J5/0053 ,  C07J9/005 ,  C07J13/005 ,  C07J13/007 ,  C07J21/006 ,  C07J43/003 ,  A61K2300/00

Abstract: This invention relates generally to methods for preparing certain bile acids from non-mammalian sourced starting materials as well as to synthetic bile acids and compositions comprising such acids wherein the acids are characterized by a different C14 population than naturally occurring bile acids as well as being free from any mammalian pathogens. This invention is also directed to the synthesis of intermediates useful in the synthesis of such bile acids. Accordingly, the C ring of the steroidal scaffold is oxidized to provide a synthetic route and intermediates to DCA. This invention also provides synthetic methods for preparing deoxycholic acid or a salt thereof starting from aromatic steroids such as estrogen, equilenin, and derivatives thereof. This invention is also directed to intermediates such as 12-oxo or delta-9,11-ene steroids as well as novel processes for their preparation. In preferred embodiments, bile acids are provided herein which have substituents on the B-ring and/or D-ring side chain and optionally on the hydroxy group of the A-ring.

Abstract translation: 本发明一般涉及从非哺乳动物源起始原料以及合成胆汁酸制备某些胆汁酸的方法以及包含这些酸的组合物，其中酸的特征在于不同于天然存在的胆汁酸的C14种群以及游离的酸 来自任何哺乳动物病原体。 本发明还涉及可用于合成这种胆汁酸的中间体的合成。 因此，甾体支架的C环被氧化以提供DCA的合成途径和中间体。 本发明还提供从芳族类固醇如雌激素，平衡物及其衍生物制备脱氧胆酸或其盐的合成方法。 本发明还涉及中间体，例如12-氧代或δ-9,11-烯类固醇，以及它们制备的新方法。 在优选的实施方案中，本文提供了在B-环和/或D-环侧链和任选地在A环的羟基上具有取代基的胆汁酸。

公开(公告)号：US20110212935A1

公开(公告)日：2011-09-01

申请号：US13095528

申请日：2011-04-27

Applicant: James M. Frincke

Inventor： James M. Frincke

IPC: A61K31/58 ,  C07J43/00 ,  C07J41/00 ,  A61P37/00 ,  A61K31/565

CPC classification number: C07J43/003 ,  C07J13/005 ,  C07J41/0011

Abstract: The invention relates to the use of compounds to ameliorate or treat an condition such as a cystic fibrosis, neutropenia or other exemplified conditions. Exemplary compounds that can be used include 3β-hydroxy-17β-aminoandrost-5-ene, 3β-hydroxy-16α-fluoro-17β-aminoandrost-5-ene, 3α-hydroxy-16α-fluoro-17β-aminoandrost-5-ene, 3β-hydroxy-16β-fluoro-17β-aminoandrost-5-ene, 1α,3β-dihydroxy-4α-fluoroandrost-5-ene-17-one, 1α,3β,17β-trihydroxy-4α-fluoroandrost-5-ene, 1β,3β-dihydroxy-6α-bromoandrost-5-ene, 1α-fluoro-3β,12α-dihydroxyandrost-5-ene-17-one, 1α-fluoro-3β,4α-dihydroxyandrost-5-ene and 4α-fluoro-3β,6α,17β-trihydroxyandrostane.

Abstract translation: 本发明涉及化合物用于改善或治疗诸如囊性纤维化，中性白细胞减少症或其他示例性病症的病症的用途。 可以使用的示例性化合物包括3'-二羟基-17和bgr-氨基雄甾-5-烯，3β-羟基-16α-氟-17β-氨基雄甾-5-烯，3α-羟基-16α-氟-17β- 氨基雄甾-5-烯，3'-二羟基-16b-双-gr-17＆bgr-氨基雄甾-5-烯，1α，3'-二羟基-4α-氟雄甾-5-烯-17-酮，1α，3＆bgr，17＆bgr ; 3'-二羟基-4α-氟雄甾-5-烯，1α-氟，1α-氟，1α-氟代雄甾-5-烯，1α-氟-3β，12α-二羟基雄甾-5-烯-17-酮，1α-氟 -3α，bα，4α-二羟基雄甾-5-烯和4α-氟-3β，6α，17β-三羟基雄甾烷。

公开(公告)号：US06875758B2

公开(公告)日：2005-04-05

申请号：US10385936

申请日：2003-03-14

Applicant: Ram Pratap ,  Ram Chandra Gupta ,  Ramesh Chander ,  Ashok Kumar Khanna ,  Arvind Kumar Srivastava ,  Deepak Raina ,  Satyavan Singh ,  Savita Srivastava ,  Anil Kumar Rastogi ,  Omkar Prasad Asthana ,  Swarn Nityanand ,  Nitya Anand ,  Ashim Ghatak ,  Narinder Kumar Kapoor ,  Sukh Dev

Inventor： Ram Pratap ,  Ram Chandra Gupta ,  Ramesh Chander ,  Ashok Kumar Khanna ,  Arvind Kumar Srivastava ,  Deepak Raina ,  Satyavan Singh ,  Savita Srivastava ,  Anil Kumar Rastogi ,  Omkar Prasad Asthana ,  Swarn Nityanand ,  Nitya Anand ,  Ashim Ghatak ,  Narinder Kumar Kapoor ,  Sukh Dev

IPC: C07J13/00 ,  A61K31/56 ,  A61K31/59

CPC classification number: A61K31/573 ,  C07J13/005 ,  C07J13/007

Abstract: The invention provides a method of using pregnadienones and pregnadienols represented by the structural formula (I) as shown herein below Wherein X═OH or O or combination thereof and positioning of olefinic bonds are at 4(5); 5(6); 16(17); 17(20) or various combinations and said compounds containing at least one olefinic bond in or on their D-ring for the treatment of hyperlipidemic and hyperglycemic conditions in mammals, said method comprising administering an effective amount of the said compounds to the recipient mammals.

Abstract translation: 本发明提供了一种使用由下式结构式（I）表示的孕ad酮和孕二烯醇的方法，其中X = OH或O或其组合，烯键的定位为4（5）; 5（6）; 16（17）; 17（20）或各种组合，并且所述化合物在其D环上或其D环上含有至少一个烯键，用于治疗哺乳动物中的高脂血症和高血糖病症，所述方法包括向受体哺乳动物施用有效量的所述化合物。

公开(公告)号：US20040157814A1

公开(公告)日：2004-08-12

申请号：US10703153

申请日：2003-11-06

Applicant: Inflazyme Pharmaceuticals Ltd. ,  The University of British Columbia ,  The University of Alberta

Inventor： David L. Burgoyne ,  Yaping Shen ,  John M. Langlands ,  Christine Rogers ,  Joseph H.L. Chau ,  Edward Piers ,  Hassan Salari

IPC: C07J017/00 ,  A61K031/585 ,  A61K031/56 ,  C07J003/00

CPC classification number: C07J9/00 ,  C07J1/0007 ,  C07J1/0011 ,  C07J1/0022 ,  C07J3/00 ,  C07J7/002 ,  C07J13/005 ,  C07J13/007 ,  C07J17/00 ,  C07J21/008 ,  C07J31/006 ,  C07J41/0016 ,  C07J51/00 ,  C07J71/001 ,  C07J71/0026 ,  Y02P20/55 ,  Y10S514/825 ,  Y10S514/826

Abstract: Steroid compounds having various oxygen substitution on the steroid nucleus are disclosed. A specific functionality present on many of the steroid compounds is oxygen substitution at both of positions 6 and 7. Thus, certain steroids have oxygen substitution at C6 and C7, and some have specific stereochemistries such as 6null and 7null oxygen substitution, and an alpha hydrogen at the 5 position in addition to having 6null and 7null oxygen substitution. Steroids having 3,4-epoxy functionality are also disclosed. In addition, steroids having C17 pyran and null-lactone functionality, with oxygen substitution at C6 and C7, or at C15, of the steroid nucleus, are disclosed.

Abstract translation: 公开了在类固醇核上具有各种氧取代的类固醇化合物。 存在于许多类固醇化合物上的具体功能是在6和7位都是氧取代。因此，某些类固醇在C6和C7具有氧取代，并且一些具有特异性立体化学例如6α和7beta氧取代，以及α氢 在5位，除了具有6alpha和7beta氧替代。 还公开了具有3,4-环氧官能团的类固醇。 此外，公开了具有C17吡喃和δ-内酯官能团的类固醇，其具有类固醇核的C6和C7或C15的氧取代。

公开(公告)号：US20030216363A1

公开(公告)日：2003-11-20

申请号：US10385936

申请日：2003-03-14

Applicant: Council of Scientific & Industrial Research

Inventor： Ram Pratap ,  Ram Chandra Gupta ,  Ramesh Chander ,  Ashok Kumar Khanna ,  Arvind Kumar Srivastava ,  Deepak Raina ,  Satyavan Singh ,  Savita Srivastava ,  Anil Kumar Rastogi ,  Omkar Prasad Asthana ,  Swarn Nityanand ,  Nitya Anand ,  Ashim Ghatak ,  Narinder Kumar Kapoor ,  Sukh Dev

IPC: A61K031/56

CPC classification number: A61K31/573 ,  C07J13/005 ,  C07J13/007

Abstract: The invention provides a method of using pregnadienones and pregnadienols represented by the structural formula (I) as shown herein below 1 Wherein XnullOH or O or combination thereof and positioning of olefinic bonds are at 4(5); 5(6); 6(17); 17(20) or various combinations and said compounds containing at least one olefinic bond in or on their D-ring for the treatment of hypolipidemic and hypoglycemic conditions in mammals, said method comprising administering an effective amount of the said compounds to the recipient mammals.

Abstract translation: 本发明提供了一种使用由下式结构式（I）表示的孕ad酮和孕二烯醇的方法：其中X = OH或O或其组合，烯键的定位为4（5）; 5（6）; 6（17）; 17（20）或各种组合，并且所述化合物在其D环上或其D环上含有至少一个烯键，用于治疗哺乳动物的降血脂和降血糖病症，所述方法包括向受体哺乳动物施用有效量的所述化合物。