AR108011A1 - Moduladores receptores de estrógenos - Google Patents

Moduladores receptores de estrógenos

Info

Publication number
AR108011A1
AR108011A1 ARP170100788A ARP170100788A AR108011A1 AR 108011 A1 AR108011 A1 AR 108011A1 AR P170100788 A ARP170100788 A AR P170100788A AR P170100788 A ARP170100788 A AR P170100788A AR 108011 A1 AR108011 A1 AR 108011A1
Authority
AR
Argentina
Prior art keywords
optionally substituted
alkyl
hydrogen
group
cycloalkyl
Prior art date
Application number
ARP170100788A
Other languages
English (en)
Inventor
Rakesh Kumar Sit
Joseph Robert Pinchman
Kevin Duane Bunker
Chad Daniel Hopkins
Sayee Gajanan Hegde
Deborah Helen Slee
Peter Qinhua Huang
Original Assignee
Kalyra Pharmaceuticals Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Kalyra Pharmaceuticals Inc filed Critical Kalyra Pharmaceuticals Inc
Publication of AR108011A1 publication Critical patent/AR108011A1/es

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/438—The ring being spiro-condensed with carbocyclic or heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/30—Oestrogens
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B59/00—Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
    • C07B59/002—Heterocyclic compounds
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C69/00—Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C07C69/66—Esters of carboxylic acids having esterified carboxylic groups bound to acyclic carbon atoms and having any of the groups OH, O—metal, —CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety
    • C07C69/73—Esters of carboxylic acids having esterified carboxylic groups bound to acyclic carbon atoms and having any of the groups OH, O—metal, —CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety of unsaturated acids
    • C07C69/732—Esters of carboxylic acids having esterified carboxylic groups bound to acyclic carbon atoms and having any of the groups OH, O—metal, —CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety of unsaturated acids of unsaturated hydroxy carboxylic acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C69/00—Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C07C69/66—Esters of carboxylic acids having esterified carboxylic groups bound to acyclic carbon atoms and having any of the groups OH, O—metal, —CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety
    • C07C69/73—Esters of carboxylic acids having esterified carboxylic groups bound to acyclic carbon atoms and having any of the groups OH, O—metal, —CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety of unsaturated acids
    • C07C69/738—Esters of keto-carboxylic acids or aldehydo-carboxylic acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C69/00—Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C07C69/74—Esters of carboxylic acids having an esterified carboxyl group bound to a carbon atom of a ring other than a six-membered aromatic ring
    • C07C69/757—Esters of carboxylic acids having an esterified carboxyl group bound to a carbon atom of a ring other than a six-membered aromatic ring having any of the groups OH, O—metal, —CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/14—Radicals substituted by nitrogen atoms, not forming part of a nitro radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
    • C07D471/14—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic System
    • C07F7/02—Silicon compounds
    • C07F7/08—Compounds having one or more C—Si linkages
    • C07F7/18—Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
    • C07F7/1804—Compounds having Si-O-C linkages
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07—Optical isomers
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2602/00—Systems containing two condensed rings
    • C07C2602/36—Systems containing two condensed rings the rings having more than two atoms in common
    • C07C2602/38—Systems containing two condensed rings the rings having more than two atoms in common the bicyclo ring system containing five carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2603/00—Systems containing at least three condensed rings
    • C07C2603/56—Ring systems containing bridged rings
    • C07C2603/58—Ring systems containing bridged rings containing three rings
    • C07C2603/60—Ring systems containing bridged rings containing three rings containing at least one ring with less than six members
    • C07C2603/62—Ring systems containing bridged rings containing three rings containing at least one ring with less than six members containing three- or four-membered rings

Abstract

Compuestos derivados de indolpirimidina utilizables en el tratamiento del cáncer de mama. Se proveen además, intermediarios para su síntesis. Reivindicación 1: Un compuesto de la fórmula (1), o una sal farmacéuticamente aceptable del mismo, en donde: X¹, Y¹ y Z¹ son cada uno independientemente C o N; con la primera salvedad de que por lo menos uno de X¹, Y¹ y Z¹ es N; con la segunda salvedad de que cada uno de X¹, Y¹ y Z¹ es neutro; con la tercera salvedad de que dos de las líneas de puntos indican uniones doble; con la cuarta salvedad de que las valencias de X¹, Y¹ y Z¹ puede ser satisfechas cada una independientemente mediante acople a un sustituyente seleccionado de H y R¹²; X² es O, NH o S; A¹ se selecciona del grupo que consiste de un cicloalquilo opcionalmente sustituido, un arilo opcionalmente sustituido, un heteroarilo opcionalmente sustituido y un heterociclilo opcionalmente sustituido; R¹ se selecciona del grupo que consiste de un alquilo C₁₋₆ opcionalmente sustituido, un cicloalquilo opcionalmente sustituido, un cicloalquenilo opcionalmente sustituido, un arilo opcionalmente sustituido, un heteroarilo opcionalmente sustituido, un heterociclilo opcionalmente sustituido, un cicloalquil(C₁₋₆ alquilo) opcionalmente sustituido, un cicloalquenil(C₁₋₆ alquilo) opcionalmente sustituido, un aril(C₁₋₆ alquilo) opcionalmente sustituido, un heteroaril(C₁₋₆ alquilo) opcionalmente sustituido y un heterociclil(C₁₋₆ alquilo) opcionalmente sustituido; R² y R³ cada uno independientemente se selecciona del grupo que consiste de hidrógeno, halógeno, un C₁₋₆ alquilo opcionalmente sustituido y un C₁₋₆ haloalquilo opcionalmente sustituido; o R² y R³ junto con el carbono al cual R² y R³ se acoplan forman un cicloalquilo opcionalmente sustituido, un cicloalquenilo opcionalmente sustituido o un heterociclilo opcionalmente sustituido; R⁴ y R⁵ cada uno se selecciona independientemente del grupo que consiste de hidrógeno, halógeno, un C₁₋₆ alquilo opcionalmente sustituido y un C₁₋₆ haloalquilo opcionalmente sustituido; o R⁴ y R⁵ junto con el carbono al cual R⁴ y R⁵ se acoplan forman un cicloalquilo opcionalmente sustituido, un cicloalquenilo opcionalmente sustituido o un heterociclilo opcionalmente sustituido; R⁶, R⁷, R⁸ y R⁹ cada uno independientemente se selecciona del grupo que consiste de hidrógeno, halógeno, hidroxi, un alquilo opcionalmente sustituido, un alcoxi opcionalmente sustituido, un haloalquilo opcionalmente sustituido, una amina mono-sustituida opcionalmente sustituida y una amina di-sustituida opcionalmente sustituida; R¹⁰ es hidrógeno, halógeno, un alquilo opcionalmente sustituido o un cicloalquilo opcionalmente sustituido; R¹¹ es hidrógeno o un C₁₋₆ alquilo opcionalmente sustituido; y R¹² es hidrógeno, halógeno, un C₁₋₃ alquilo opcionalmente sustituido, un C₁₋₃ haloalquilo opcionalmente sustituido o un C₁₋₃ alcoxi opcionalmente sustituido; siempre que cuando R¹¹ sea hidrógeno o metilo, X¹ es NH, Y¹ y Z¹ cada uno es C, X² es O, A¹ es un fenilo, 2-fluorofenilo, o 2,6-difluorofenilo, tanto R² como R³ son metilo o uno de R² y R³ es hidrógeno y el otro de R² y R³ es metilo, y R⁴, R⁵, R⁶, R⁷, R⁸, R⁹ y R¹⁰ cada uno es hidrógeno, entonces R¹ no podrá ser 2-hidroxietilo, 2-metilpropilo, 2-fluoro-2-metilpropilo, 3-fluoro-2-metilpropilo, 3-hidroxi-2-metilpropilo o 2-fluoro-3-hidroxi-2-metilpropilo. Reivindicación 43: Un compuesto seleccionado del grupo que consiste de los restos del grupo de fórmulas (2). Reivindicación 44: Un compuesto seleccionado del grupo que consiste de los compuesto de fórmula (3) y (4). Reivindicación 45: Un compuesto de la fórmula (5). Reivindicación 46: Un compuesto de la fórmula (6).
ARP170100788A 2016-04-01 2017-03-30 Moduladores receptores de estrógenos AR108011A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201662317254P 2016-04-01 2016-04-01

Publications (1)

Publication Number Publication Date
AR108011A1 true AR108011A1 (es) 2018-07-04

Family

ID=59966438

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP170100788A AR108011A1 (es) 2016-04-01 2017-03-30 Moduladores receptores de estrógenos

Country Status (15)

Country Link
US (5) US20190142811A1 (es)
EP (1) EP3442971A4 (es)
JP (2) JP6926189B2 (es)
KR (2) KR20220071293A (es)
CN (4) CN113717170A (es)
AR (1) AR108011A1 (es)
AU (3) AU2017242027B2 (es)
BR (1) BR112018070161A2 (es)
CA (1) CA3017388C (es)
IL (3) IL295050A (es)
MX (2) MX2018011419A (es)
RU (1) RU2738646C2 (es)
SG (1) SG11201807708SA (es)
TW (2) TW202235418A (es)
WO (1) WO2017172957A1 (es)

Families Citing this family (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP6905539B2 (ja) 2016-02-05 2021-07-21 インベンティスバイオ リミテッド ライアビリティ カンパニー 選択的エストロゲン受容体分解剤およびその使用
CN113717170A (zh) 2016-04-01 2021-11-30 里科瑞尔姆Ip控股有限责任公司 雌激素受体调节剂
CN107814798B (zh) * 2016-09-14 2020-11-03 四川科伦博泰生物医药股份有限公司 3-取代丙烯酸类化合物及其制备方法和用途
WO2018130124A1 (zh) * 2017-01-11 2018-07-19 南京圣和药业股份有限公司 作为选择性雌激素受体下调剂的三环类化合物及其应用
CN111164063A (zh) 2017-09-11 2020-05-15 里科瑞尔姆Ip控股有限责任公司 用于制备双环化合物的连续流动方法
JP2021503448A (ja) * 2017-11-16 2021-02-12 ノバルティス アーゲー Ｌｓｚ１０２及びリボシクリブを含む医薬組合せ
US20220220107A1 (en) * 2019-05-24 2022-07-14 Zhejiang Hisun Pharmaceutical Co., Ltd. Crystal forms of acrylic acid derivatives, preparation method therefor and use thereof
EP3993787A4 (en) * 2019-08-06 2023-07-12 Recurium IP Holdings, LLC ESTROGEN RECEPTOR MODULATORS FOR THE TREATMENT OF MUTANTS
JP2022553833A (ja) * 2019-11-04 2022-12-26 リキュリウム アイピー ホールディングス リミテッド ライアビリティー カンパニー エストロゲン受容体調節薬の塩及び形態
US20230042653A1 (en) * 2019-12-20 2023-02-09 Recurium Ip Holdings, Llc Combinations
MX2022007627A (es) * 2019-12-20 2022-08-16 Recurium Ip Holdings Llc Combinaciones.
US20230087941A1 (en) * 2019-12-20 2023-03-23 Recurium Ip Holdings, Llc Combinations
EP4069236A4 (en) * 2019-12-20 2023-12-27 Recurium IP Holdings, LLC COMBINATIONS
WO2021127042A1 (en) * 2019-12-20 2021-06-24 Recurium Ip Holdings, Llc Combinations
IL297448A (en) * 2020-04-22 2022-12-01 Recurium Ip Holdings Llc Preparation of a selective estrogen receptor complex
WO2021253380A1 (en) * 2020-06-19 2021-12-23 InventisBio Co., Ltd. Oral formulations and uses thereof
WO2022061242A1 (en) * 2020-09-20 2022-03-24 Tactogen Inc Advantageous tryptamine compositions for mental disorders or enhancement
WO2022133446A1 (en) * 2020-12-16 2022-06-23 Recurium Ip Holdings, Llc Combinations
JP2024502270A (ja) 2020-12-23 2024-01-18 リキュリウム アイピー ホールディングス リミテッド ライアビリティー カンパニー エストロゲン受容体調節薬
AU2022305957A1 (en) * 2021-07-08 2024-01-25 Olema Pharmaceuticals, Inc. Methods of treating estrogen receptor-associated diseases

Family Cites Families (46)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0749313A4 (en) 1994-03-11 2001-10-24 Lilly Co Eli METHOD OF TREATING CONDITIONS ASSOCIATED WITH THE 5HT 2B RECEPTOR
GB9604996D0 (en) 1996-03-08 1996-05-08 Black James Foundation Benzodiazonine derivatives
EP1113007A1 (en) * 1999-12-24 2001-07-04 Pfizer Inc. Tetrahydroisoquinoline compounds as estrogen agonists/antagonists
EP1438310B1 (en) 2001-10-19 2006-12-20 TransTech Pharma Inc. Beta-carbolin derivatives as ptp-inhibitors
US8076352B2 (en) * 2004-03-15 2011-12-13 Ptc Therapeutics, Inc. Administration of carboline derivatives useful in the treatment of cancer and other diseases
WO2006015035A1 (en) 2004-08-02 2006-02-09 Smithkline Beecham Corporation Useful compounds for hpv infection
WO2007002051A1 (en) 2005-06-22 2007-01-04 Smithkline Beecham Corporation Carboline derivatives and their use as inhibitors of flaviviridae infections
CA2656067C (en) 2006-06-23 2014-08-12 Radius Health, Inc. Treatment of vasomotor symptoms with selective estrogen receptor modulators
EP2139476A1 (en) 2007-04-13 2010-01-06 PTC Therapeutics, Inc. Administration of carboline derivatives useful in the treatment of cancer and other diseases
DE102007028515A1 (de) 2007-06-21 2008-12-24 Merck Patent Gmbh 6-(Pyrrolopyridinyl)-pyrimidinyl-2-amin-derivate
TW201028414A (en) * 2009-01-16 2010-08-01 Merck Sharp & Dohme Oxadiazole beta carboline derivatives as antidiabetic compounds
WO2010107485A1 (en) 2009-03-17 2010-09-23 The Trustees Of Columbia University In The City Of New York E3 ligase inhibitors
CA3184380A1 (en) * 2009-05-27 2010-12-02 Ptc Therapeutics, Inc. Methods for treating cancer and non-neoplastic conditions
WO2010138706A1 (en) * 2009-05-27 2010-12-02 Ptc Therapeutics, Inc. Methods for treating breast cancer
EP2653468B1 (en) * 2009-07-28 2016-02-24 Ono Pharmaceutical Co., Ltd. Bicyclic Compound and Use Thereof for Medical Purposes
JP2013517272A (ja) 2010-01-15 2013-05-16 メルク・シャープ・エンド・ドーム・コーポレイション 抗糖尿病化合物としてのオキサジアゾール・ベータ・カルボリン誘導体
EA020528B1 (ru) * 2010-02-11 2014-11-28 Бристол-Майерс Сквибб Компани Макроциклы в качестве ингибиторов фактора xia
US20130172320A1 (en) 2010-02-18 2013-07-04 Sarvajit Chakravarty Pyrido [4,3-b] indole and pyrido [3,4-b] indole derivatives and methods of use
JP2013528223A (ja) 2010-06-10 2013-07-08 アラゴン ファーマシューティカルズ，インク． エストロゲン受容体モジュレーターおよびその用途
EP2669279B1 (en) * 2011-01-27 2017-01-11 ONO Pharmaceutical Co., Ltd. Bicyclic compound and use thereof for medical purposes
CN102432608B (zh) 2011-11-01 2013-04-17 浙江大学 手性螺环磷酸催化合成光学活性四氢-β-咔啉衍生物的方法
EA029559B1 (ru) 2011-12-14 2018-04-30 Серагон Фармасьютикалс, Инк. Фторированные модуляторы рецепторов эстрогенов и их применение
NO2797921T3 (es) * 2011-12-31 2018-02-03
EP2811997B1 (en) * 2012-02-07 2018-04-11 Eolas Therapeutics Inc. Substituted prolines/piperidines as orexin receptor antagonists
MX2014011217A (es) 2012-03-20 2015-03-10 Seragon Pharmaceuticals Inc Moduladores del receptor de estrogeno y sus usos.
LT2872482T (lt) 2012-07-13 2020-12-28 Oncternal Therapeutics, Inc. Krūties vėžių gydymo būdas selektyviu androgeno receptoriaus moduliatoriumi
EP2958907B1 (en) 2013-02-19 2018-02-28 Novartis AG Benzothiophene derivatives and compositions thereof as selective estrogen receptor degraders
MX2015011132A (es) 2013-03-14 2015-11-30 Seragon Pharmaceuticals Inc Moduladores policiclicos del receptor de estrogenos y sus usos.
US9155727B2 (en) * 2013-05-28 2015-10-13 Astrazeneca Ab Chemical compounds
CA2932106A1 (en) 2013-12-06 2015-06-11 F. Hoffmann-La Roche Ag Estrogen receptor modulator for the treatment of locally advanced or metastatic estrogen receptor positive breast cancer
CN104693211A (zh) 2013-12-10 2015-06-10 南京明德新药研发股份有限公司 作为抗病毒剂的咪唑衍生物及其制药用途
UY35993A (es) * 2014-02-12 2015-08-31 Eolas Therapeutics Inc Prolinas / piperidinas sustituidas como antagonistas del receptor de orexina
US9695166B2 (en) * 2014-05-05 2017-07-04 Global Blood Therapeutics, Inc. Pyrazolopyridine pyrazolopyrimidine and related compounds
WO2015173329A1 (en) 2014-05-16 2015-11-19 Actelion Pharmaceuticals Ltd Antibacterial quinazoline-4(3h)-one derivatives
KR20230035446A (ko) 2014-06-27 2023-03-13 노그라 파마 리미티드 아릴 수용체 조정제, 및 그의 제조 및 사용 방법
NZ731344A (en) 2014-10-09 2018-08-31 Guangdong Raynovent Biotech Co Ltd Hydroxyl purine compounds and applications thereof
US10654809B2 (en) 2016-06-10 2020-05-19 University Of Tennessee Research Foundation Selective androgen receptor degrader (SARD) ligands and methods of use thereof
EP3286164A4 (en) 2015-04-21 2018-12-05 Gtx, Inc. Selective androgen receptor degrader (sard) ligands and methods of use thereof
EP3312184A4 (en) * 2015-06-16 2019-02-27 Jiangsu Hengrui Medicine Co., Ltd. PIPERIDINE DERIVATIVE AND ITS PREPARATION METHOD AND PHARMACEUTICAL USE THEREOF
JP6592197B2 (ja) * 2015-11-12 2019-10-16 浙江海正薬業股▲ふん▼有限公司Ｚｈｅｊｉａｎｇ Ｈｉｓｕｎ Ｐｈａｒｍａｃｅｕｔｉｃａｌ ＣＯ．，ＬＴＤ． アクリル酸誘導体、製造方法、および医薬としてのその使用
JP6905539B2 (ja) * 2016-02-05 2021-07-21 インベンティスバイオ リミテッド ライアビリティ カンパニー 選択的エストロゲン受容体分解剤およびその使用
CN113717170A (zh) 2016-04-01 2021-11-30 里科瑞尔姆Ip控股有限责任公司 雌激素受体调节剂
MX2018015179A (es) 2016-06-10 2019-10-14 Univ Tennessee Res Found Ligandos degradadores selectivos del receptor de androgenos (sard) y metodos de uso de los mismos.
WO2018001232A1 (zh) * 2016-06-29 2018-01-04 浙江海正药业股份有限公司 丙烯酸类衍生物及其制备方法和其在医药上的用途
JP7050770B2 (ja) * 2016-10-05 2022-04-08 エフ・ホフマン－ラ・ロシュ・アクチェンゲゼルシャフト 抗体薬物コンジュゲートの調製方法
WO2018130124A1 (zh) * 2017-01-11 2018-07-19 南京圣和药业股份有限公司 作为选择性雌激素受体下调剂的三环类化合物及其应用

Also Published As

Publication number Publication date
US20190142811A1 (en) 2019-05-16
IL261654A (en) 2018-10-31
JP2019515026A (ja) 2019-06-06
KR102401841B1 (ko) 2022-05-25
AU2020294196A1 (en) 2021-01-28
KR20220071293A (ko) 2022-05-31
CN112679495A (zh) 2021-04-20
CN109311870B (zh) 2021-09-21
RU2738646C2 (ru) 2020-12-15
AU2020294196B2 (en) 2022-06-16
TW202235418A (zh) 2022-09-16
RU2018132037A3 (es) 2020-05-15
US20200261430A1 (en) 2020-08-20
IL285318A (en) 2021-09-30
SG11201807708SA (en) 2018-10-30
US11065233B2 (en) 2021-07-20
KR20190002478A (ko) 2019-01-08
TWI746535B (zh) 2021-11-21
JP6926189B2 (ja) 2021-08-25
CA3017388A1 (en) 2017-10-05
TW201736334A (zh) 2017-10-16
CN112745316A (zh) 2021-05-04
IL285318B (en) 2022-09-01
US20200261429A1 (en) 2020-08-20
JP2021176911A (ja) 2021-11-11
AU2017242027A1 (en) 2018-10-11
CN112679495B (zh) 2023-03-28
AU2022204025A1 (en) 2022-06-30
CA3017388C (en) 2024-03-12
EP3442971A1 (en) 2019-02-20
US11065234B2 (en) 2021-07-20
CN113717170A (zh) 2021-11-30
US20200261428A1 (en) 2020-08-20
AU2017242027B2 (en) 2020-10-08
RU2018132037A (ru) 2020-05-12
US10959989B2 (en) 2021-03-30
US20210330651A1 (en) 2021-10-28
CN109311870A (zh) 2019-02-05
WO2017172957A1 (en) 2017-10-05
BR112018070161A2 (pt) 2019-02-12
MX2022005780A (es) 2022-06-09
IL261654B (en) 2021-08-31
IL295050A (en) 2022-09-01
MX2018011419A (es) 2019-06-06
EP3442971A4 (en) 2020-01-01

Similar Documents

Publication Publication Date Title
AR108011A1 (es) Moduladores receptores de estrógenos
AR103252A1 (es) Compuestos de quinazolina
AR119651A1 (es) Compuestos heterocíclicos y de heteroarilo para tratar la enfermedad de huntington
AR103064A1 (es) Compuestos moduladores de fxr (nr1h4)
AR089143A1 (es) Triazolopiridinas sustituidas con actividad inhibidora de ttk
AR104025A1 (es) Carbamatos de piperazina como moduladores de magl y/o abhd6, procesos para su preparación y composiciones farmacéuticas
AR100702A1 (es) Compuestos inhibidores de quinasa de unión tank
AR096979A1 (es) Derivados de pirrol, su procedimiento de preparación y las composiciones farmacéuticas que los contienen
AR085958A1 (es) 8-etil-6-(aril)pirido[2,3-d]pirimidin-7(8h)-onas para el tratamiento de trastornos del cns y cancer
AR088029A1 (es) Compuestos de pirimidina sustituidos, composiciones farmaceuticas que los contienen y uso de los mismos para el tratamiento del dolor, accidentes cerebrovasculares, epilepsia y otras enfermedades del sistema nervioso central
AR094557A1 (es) Tiadiazol, análogos del mismo, y métodos para el tratamiento de condiciones relacionadas con deficiencia de smn
AR089550A1 (es) Compuestos quimicos
AR106301A1 (es) Composiciones de pirrolpirimidina como inhibidores de quinasas
AR100775A1 (es) Compuestos pesticidas y procedimientos relacionados con los mismos
AR094496A1 (es) Compuestos tetracíclicos sustituidos con heterociclo y métodos de uso de los mismos para el tratamiento de enfermedades víricas
AR107321A1 (es) Compuestos antiproliferativos, y sus composiciones farmacéuticas y usos
AR101528A1 (es) Inhibidores de cdk9 quinasa de pirrolo[2,3-b]piridina
AR102544A1 (es) Compuestos derivados de dihidrohidantoína como herbicidas
AR098818A1 (es) Derivados de oxindol, preparación de los mismos y uso terapéutico de los mismos
AR104512A1 (es) Compuestos de pirazol inhibidores de proteína activadora de 5-lipoxigenasa (flap)
AR102258A1 (es) Compuestos de quinolina y quinazolina
AR099867A1 (es) Compuestos imidazobenzotiazolo fusionados
AR098436A1 (es) Compuestos tricíclicos de piperidina
AR095436A1 (es) Procedimiento para preparar inhibidores de la glucosilceramida sintasa
AR110514A1 (es) Péptidos antimicrobianos