公开(公告)号：US20130079354A1

公开(公告)日：2013-03-28

申请号：US13620151

申请日：2012-09-14

Applicant: Melwyn ABREO ,  Daniel F. HARVEY ,  Mikhail A. KONDRATENKO ,  Wenbao LI ,  Rajender KAMBOJ ,  Vishnumurthy KODUMURU ,  Michael D. WINTHER ,  Heinz W. GSCHWEND ,  Nagasree CHAKKA ,  Shifeng LIU ,  Serguei SVIRIDOV ,  Shaoyi SUN

Inventor： Melwyn ABREO ,  Daniel F. HARVEY ,  Mikhail A. KONDRATENKO ,  Wenbao LI ,  Rajender KAMBOJ ,  Vishnumurthy KODUMURU ,  Michael D. WINTHER ,  Heinz W. GSCHWEND ,  Nagasree CHAKKA ,  Shifeng LIU ,  Serguei SVIRIDOV ,  Shaoyi SUN

IPC: C07D401/14 ,  C07D401/04

CPC classification number: C07D401/14 ,  A61K31/00 ,  A61K31/444 ,  A61K31/501 ,  C07D213/75 ,  C07D213/76 ,  C07D213/81 ,  C07D401/04

Abstract: Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I): wherein W, V, x, y, R1, R2, R3, R4, R5, R6, R7, R7a, R8, R8a, R9, R9a, R10 and R10a are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.

Abstract translation: 公开了在哺乳动物，优选人中治疗SCD介导的疾病或病症的方法，其中所述方法包括向有需要的哺乳动物施用式（I）化合物：其中W，V，x，y，R 1 ，R2，R3，R4，R5，R6，R7，R7a，R8，R8a，R9，R9a，R10和R10a在本文中定义。 还公开了包含式（I）化合物的药物组合物。

公开(公告)号：US07390813B1

公开(公告)日：2008-06-24

申请号：US10326210

申请日：2002-12-20

Applicant: Mark P. Gray-Keller ,  Michael D. Winther ,  Richard M. Fine ,  Boris Klebansky ,  Heinz Gschwend ,  Daniel F. Harvey

Inventor： Mark P. Gray-Keller ,  Michael D. Winther ,  Richard M. Fine ,  Boris Klebansky ,  Heinz Gschwend ,  Daniel F. Harvey

IPC: A61K31/495 ,  C07D401/04

CPC classification number: A61K31/496 ,  A61K31/551

Abstract: Novel compounds useful in the treatment of, prevention of or protection against diseases and/or conditions related to metabolic syndrome and lipid metabolism, especially diseases of fatty acid and cholesterol metabolism, such as those mediated by stearoyl-CoA desaturase, are disclosed along with methods of employing said compounds for such uses.

Abstract translation: 可用于治疗，预防或保护与代谢综合征和脂质代谢相关的疾病和/或病症的新型化合物，特别是脂肪酸和胆固醇代谢疾病，例如由硬脂酰辅酶A去饱和酶介导的那些，以及方法 使用所述化合物用于这种用途。

公开(公告)号：US07294480B2

公开(公告)日：2007-11-13

申请号：US10827668

申请日：2004-04-19

Applicant: Michael D. Winther ,  Mark P. Gray-Keller

Inventor： Michael D. Winther ,  Mark P. Gray-Keller

IPC: C12Q1/26

CPC classification number: C12Q1/26 ,  C12Q1/48 ,  G01N33/60 ,  G01N2333/90245 ,  G01N2333/91051 ,  G01N2500/04

Abstract: High throughput screening assays for the identification of potential therapeutic agents able to modulate the activity of enzymes of fatty acid biosynthesis, especially desaturases and/or elongases, are disclosed along with therapeutic uses of the agents identified by such assays for the prevention and/or treatment of diseases related to fatty acid metabolism. Substrates useful in such assays are also described.

Abstract translation: 公开了用于鉴定能够调节脂肪酸生物合成酶（特别是去饱和酶和/或延长酶）的活性的潜在治疗剂的高通量筛选分析以及通过这些测定法鉴定的药物的预防和/或治疗的治疗用途 的与脂肪酸代谢相关的疾病。 还描述了在这种测定中有用的底物。

公开(公告)号：US5276020A

公开(公告)日：1994-01-04

申请号：US990190

申请日：1992-12-14

Applicant: David F. Horrobin ,  John C. M. Stewart ,  Michael D. Winther

Inventor： David F. Horrobin ,  John C. M. Stewart ,  Michael D. Winther

IPC: C07D473/18 ,  A61K31/00 ,  A61K31/505 ,  A61K31/52 ,  A61K31/522 ,  A61K31/70 ,  A61K31/7042 ,  A61K31/7052 ,  A61K31/7064 ,  A61K31/7072 ,  A61P31/00 ,  A61P31/12 ,  C07D405/04 ,  C07D473/00 ,  C07H19/06 ,  C07H19/073 ,  C07H19/16 ,  C07H17/00

CPC classification number: C07D473/00 ,  C07H19/06 ,  C07H19/16

Abstract: Anti-virals wherein a linoleyl, gamma-linolenyl or other unsaturated long chain fatty acyl group is borne directly on a hydroxy or amino group of the sugar/sugar analogue or heterocyclic moiety of a nucleoside or nucleoside analogue.

Abstract translation: 其中亚油酰基，γ-亚麻醇基或其它不饱和长链脂肪酰基直接承载在核苷或核苷类似物的糖/糖类似物或杂环部分的羟基或氨基上的抗病毒剂。

公开(公告)号：US20110021530A1

公开(公告)日：2011-01-27

申请号：US12919232

申请日：2009-02-19

Applicant: Andreas Billich ,  Michael D. Winther ,  Yigal Paul Goldberg ,  Gesine Winzenburg ,  Karin Rapp ,  Andreas Fritze

Inventor： Andreas Billich ,  Michael D. Winther ,  Yigal Paul Goldberg ,  Gesine Winzenburg ,  Karin Rapp ,  Andreas Fritze

IPC: A61K31/53 ,  A61K31/501 ,  A61K31/506 ,  A61P17/00 ,  A61P17/10 ,  A61P17/08 ,  A61P17/18

CPC classification number: A61K31/00 ,  A61K31/501 ,  A61K31/551 ,  C07D237/20 ,  C07D237/24 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  C07D473/00

Abstract: Methods of treating an SCD-mediated skin disorder or condition in a mammal, preferably a human, including administering to a mammal in need thereof a compound of formula (I): where x, y, W, V, R2, R3, R4, R5, R6, R6a, R7, R7a, R8, R8a, R9 and R9a are defined herein, and compositions including a compound of formula (I).

Abstract translation: 包括向有需要的哺乳动物施用式（I）化合物：其中x，y，W，V，R 2，R 3，R 4， R5，R6，R6a，R7，R7a，R8，R8a，R9和R9a在本文中定义，组合物包括式（I）化合物。

公开(公告)号：US07456180B2

公开(公告)日：2008-11-25

申请号：US10567009

申请日：2004-07-29

Applicant: Serguei Sviridov ,  Vishnumurthy Kodumuru ,  Shifeng Liu ,  Melwyn Abreo ,  Michael D. Winther ,  Heinz W. Gschwend ,  Rajender Kamboj ,  Shaoyi Sun ,  Mark W. Holladay ,  Wenbao Li ,  Chi Tu

Inventor： Serguei Sviridov ,  Vishnumurthy Kodumuru ,  Shifeng Liu ,  Melwyn Abreo ,  Michael D. Winther ,  Heinz W. Gschwend ,  Rajender Kamboj ,  Shaoyi Sun ,  Mark W. Holladay ,  Wenbao Li ,  Chi Tu

IPC: A61K31/497 ,  C07D241/02

CPC classification number: A61K31/551 ,  A61K31/00 ,  A61K31/501 ,  C07D237/20 ,  C07D403/08 ,  C07D405/08 ,  C07D409/12 ,  C07D413/08

Abstract: Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I): where G, J, L, M, x, y, W, V, R2, R3, R4, R5, R6, R7, R8, R8a, R9, R9a, R10, R10a, R11 and R11a are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.

Abstract translation: 公开了在哺乳动物，优选人中治疗SCD介导的疾病或病症的方法，其中所述方法包括向有需要的哺乳动物施用式（I）化合物：其中G，J，L，M，x ，y，W，V，R 2，R 3，R 4，R 5，R SUP > 6，R 7，R 8，R 8a，R 9，R SUP， > 9a，R 10，R 10a，R 11和R 11是本文定义的 。 还公开了包含式（I）化合物的药物组合物。

公开(公告)号：US20080280916A1

公开(公告)日：2008-11-13

申请号：US12036685

申请日：2008-02-25

Applicant: Andreas Bilich ,  Michael D. Winther ,  Yigal Paul Goldberg

Inventor： Andreas Bilich ,  Michael D. Winther ,  Yigal Paul Goldberg

IPC: A61K31/501 ,  A61P17/00

CPC classification number: A61K31/00 ,  A61K31/501 ,  A61K31/551 ,  C07D237/20 ,  C07D237/24 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  C07D473/00

Abstract: Methods of treating an SCD-mediated skin disorder or condition in a mammal, preferably a human include administering to a mammal in need thereof a compound of formula (I): where x, y, W, V, R2, R3, R4, R5, R6, R6a, R7, R7a, R8, R8a, R9 and R9a are defined herein.

Abstract translation: 在哺乳动物，优选人中治疗SCD介导的皮肤病症或病症的方法包括向有需要的哺乳动物施用式（I）化合物：其中x，y，W，V，R 2， R 3，R 3，R 4，R 5，R 6，R 6a， R S，R 7，R 7a，R 8，R 8a，R 9， SUP＆gt;和R 9a在本文中定义。

公开(公告)号：US5216142A

公开(公告)日：1993-06-01

申请号：US521075

申请日：1990-04-10

Applicant: David F. Horrobin ,  John C. M. Stewart ,  Michael D. Winther

Inventor： David F. Horrobin ,  John C. M. Stewart ,  Michael D. Winther

IPC: C07D473/18 ,  A61K31/00 ,  A61K31/505 ,  A61K31/52 ,  A61K31/522 ,  A61K31/70 ,  A61K31/7042 ,  A61K31/7052 ,  A61K31/7064 ,  A61K31/7072 ,  A61P31/00 ,  A61P31/12 ,  C07D405/04 ,  C07D473/00 ,  C07H19/06 ,  C07H19/073 ,  C07H19/16

CPC classification number: C07D473/00 ,  C07H19/06 ,  C07H19/16

Abstract: Anti-virals wherein a linoleyl, gamma-linolenyl or other unsaturated long chain fatty acyl group is borne directly on a hydroxy or amino group of the sugar/sugar analogue or heterocyclic moiety of a nucleoside or nucleoside analogue.

公开(公告)号：US08153636B2

公开(公告)日：2012-04-10

申请号：US12552868

申请日：2009-09-02

Applicant: Melwyn Abreo ,  Daniel F. Harvey ,  Heinz W. Gschwend ,  Wenbao Li ,  Chi Tu ,  Rajender Kamboj ,  Michael D. Winther ,  Vishnumurthy Kodumuru ,  Cindy J. Hudson ,  Mikhail A. Kondratenko ,  Shifeng Liu ,  Vandna Raina ,  Serguei Sviridov ,  Zaihui Zhang ,  Mehran Seid Bagherzadeh ,  Shaoyi Sun

Inventor： Melwyn Abreo ,  Daniel F. Harvey ,  Heinz W. Gschwend ,  Wenbao Li ,  Chi Tu ,  Rajender Kamboj ,  Michael D. Winther ,  Vishnumurthy Kodumuru ,  Cindy J. Hudson ,  Mikhail A. Kondratenko ,  Shifeng Liu ,  Vandna Raina ,  Serguei Sviridov ,  Zaihui Zhang ,  Mehran Seid Bagherzadeh ,  Shaoyi Sun

IPC: A61K31/497 ,  C07D401/00

CPC classification number: C07D213/71 ,  A61K31/00 ,  A61K31/501 ,  C07D213/75 ,  C07D213/76

Abstract: Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I): wherein x, y, W, V, R1, R2, R3, R4, R5, R6, R7, R7a, R8, R8a, R9, R9a, R10 and R10a are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.

Abstract translation: 公开了在哺乳动物，优选人中治疗SCD介导的疾病或病症的方法，其中所述方法包括向有需要的哺乳动物施用式（I）化合物：其中x，y，W，V，R 1 ，R2，R3，R4，R5，R6，R7，R7a，R8，R8a，R9，R9a，R10和R10a在本文中定义。 还公开了包含式（I）化合物的药物组合物。

公开(公告)号：US07964591B2

公开(公告)日：2011-06-21

申请号：US12794575

申请日：2010-06-04

Applicant: Andreas Billich ,  Michael D. Winther ,  Yigal Paul Goldberg

Inventor： Andreas Billich ,  Michael D. Winther ,  Yigal Paul Goldberg

IPC: A61K31/497

CPC classification number: A61K31/00 ,  A61K31/501 ,  A61K31/551 ,  C07D237/20 ,  C07D237/24 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  C07D473/00

Abstract: Methods of treating an SCD-mediated skin disorder or condition in a mammal, preferably a human include administering to a mammal in need thereof a compound of formula (I): where x, y, W, V, R2, R3, R4, R5, R6, R6a, R7, R7a, R8, R8a, R9 and R9a are defined herein.

Abstract translation: 在哺乳动物，优选人中治疗SCD介导的皮肤病症或病症的方法包括向有需要的哺乳动物施用式（I）化合物：其中x，y，W，V，R 2，R 3，R 4，R 5 ，R6，R6a，R7，R7a，R8，R8a，R9和R9a如本文所定义。