CAS: 1672668-24-4; 3-(((1S,2S,3R)-2,3-Difluoro-1-Hydroxy-7-(Methylsulfonyl)-2,3-Dihydro-1H-Inden-4-yl)Oxy)-5-Fluorobenzonitrile

上下游产品

（s）-3-（（（2,2-二氟-1-羟基-7-（甲基磺酰基）-2,3-二氢-1H-茚满-4-基）氧基）-5-氟苄腈 Pt2385 1672665-49-4

[(1S,2S,3R)-4-(3-Cyano-5-Fluorophenoxy)-2,3-Difluoro-7-Methylsulfonylindan-1-Yl] Acetate置于lithium Hydroxide体系中,用 四氢呋喃 用作溶剂,化学反应 1.0H,反应生成3-[[(1S,2S,3R)-2,3-二氟-2,3-二氢-1-羟基-7-(甲基磺酰基)-1H-茚-4-基]氧基]-5-氟苄腈
参考文献: Methods Of Reducing Inflammation Of The Digestive System With Inhibitors Of Hif-2-Alpha[fr] Procédés De Réduction De L'Inflammation Du Système Digestif à L'Aide D'Inhibiteurs De Hif-2-Alpha
标题: Methods Of Reducing Inflammation Of The Digestive System With Inhibitors Of Hif-2-Alpha[fr] Procédés De Réduction De L'Inflammation Du Système Digestif à L'Aide D'Inhibiteurs De Hif-2-Alpha
摘要:本公开提供了一种减少消化系统炎症的方法,适用于需要的对象,包括患有炎症性肠病的对象.同时还提供了用于这些方法的组合物.

专利信息

专利号:WO-2024010785-A1
优先权日:2022-07-08
标 题:Ketoreductase enzymes for the synthesis of 1,3-diol substituted indanes
发明人：CAHN JACKSON KENAI BLENDER; CHEUNG-LEE WAI LING; CHUN STEPHANIE W; HIRAGA KAORI; KOSJEK BIRGIT; KNIGHT JOHN H; MAKAREWICZ AMANDA M; MCCANN SCOTT; MOORE JEFFREY C; VERMA DEEPTAK
权利人:MERCK SHARP & DOHME LLC
摘要:The present disclosure provides ketoreductase enzymes having improved enzymatic properties including the capability of reducing hydroxy indanones to provide diastereomerically pure 1,3-indane diols useful for the synthesis of belzutifan. Also provided are polynucleotides encoding the ketoreductase enzymes, and host cells capable of expressing the ketoreductase enzymes. A purification procedure for isolating the ketoreductase enzymes is also provided.

专利号:US-2025215464-A1
优先权日:2022-07-08
标题 :Engineered enzyme for preparing a hydroxylated indanone intermediate useful in the synthesis of belzutifan
发明人：CHEUNG-LEE WAI LING; DIROCCO DANIEL A; GIL AGNIESZKA; HIRAGA KAORI; KIM JUNGCHUL; KOLEV JOSHUA; KOSJEK BIRGIT; MALONEY KEVIN M; SALEHI MARZIJARANI NASTARAN; MCINTOSH JOHN; MCMULLEN JONATHAN P; MOORE JEFFREY C; MURPHY GRANT S; PAN WEILAN; VELASQUEZ VELEZ JUAN E; VERMA DEEPTAK; WINSTON MATTHEW S; XIAO LI; ZHANG VICTORIA
权利人:MERCK SHARP & DOHME LLC
摘要:The present disclosure provides enzymes derived from the fungi Fusarium oxysporum c8D (“FoPip4H enzymesâ€?) having improved properties as compared to a naturally occurring wild-type enzyme including the capability of hydroxylating certain substituted indanones to provide optically pure 3-hydroxyindanones. Also provided are polynucleotides encoding the FoPip4H enzymes, host cells capable of expressing the FoPip4H enzymes, and processes for using the FoPip4H enzymes to synthesize (R)-4-fluoro-3-hydroxy-7-(methylsulfonyl)-2, 3-dihydro-1H-inden-1-one, a useful intermediate in the synthesis of belzutifan.

专利号:US-2022081407-A1
优先权日:2020-09-11
标题 :Methods of preparing substituted indanes
发明人：STENGEL PETER J; XU RUI; SPENCER STACEY RENEE
权利人:PELOTON THERAPEUTICS INC
摘要:This application discloses methods for the synthesis of substituted indane analogs that modulate HIF-2α activity, as well as key intermediates produced thereby. The synthesis of 3-(((1S,2S,3R)-2,3-difluoro-1-hydroxy-7-(methylsulfonyl)-2,3-dihydro-1H-inden-4-yl)oxy)-5-fluorobenzonitrile was exemplified.

专利号:US-2021187130-A1
优先权日:2019-12-19
标题 :PET RADIOPHARMACEUTICALS FOR NON-INVASIVE EVALUATION OF HIF-2alpha
发明人：BRUGAROLAS JAMES; SUN XIANKAI; DEBNATH SASHI
权利人:UNIV TEXAS
摘要:Provided herein are hypoxia inducible factor 2-alpha (HIF-2α)-specific radioactive tracers, methods of use thereof, and methods of synthesis thereof. Specifically, provided herein are HIF-2α-specific radioactive tracers comprising an HIF-2α-specific agent developed as a therapeutic inhibitor and a positron emitting radioactive label. Embodiments provide methods of detecting an HIF-2α-expressing tumor, detecting an HIF-2α inhibitor resistant tumor, evaluating a change in HIF-2α expression in response to an anti-cancer treatment, detecting acquisition of HIF-2α inhibitor resistance, evaluating efficacy of an HIF-2α depletion therapy, detecting or monitoring an ischemic area in a subject, or detecting and monitoring pulmonary hypertension in a subject. Also provided are methods of synthesizing an HIF-2α-specific radioactive tracer.

专利号:EP-4551694-A1
优先权日:2022-07-08
标 题 :Ketoreductase enzymes for the synthesis of 1,3-diol substituted indanes

专利号:EP-4551592-A1
优先权日:2022-07-08
标 题 :Engineered enzyme for preparing a hydroxylated indanone intermediate useful in the synthesis of belzutifan