ES2141174T3 - 4-arilmetiloximetil piperidinas como antagonistas de taquiquinina. - Google Patents

4-arilmetiloximetil piperidinas como antagonistas de taquiquinina.

Info

Publication number
ES2141174T3
ES2141174T3 ES93923630T ES93923630T ES2141174T3 ES 2141174 T3 ES2141174 T3 ES 2141174T3 ES 93923630 T ES93923630 T ES 93923630T ES 93923630 T ES93923630 T ES 93923630T ES 2141174 T3 ES2141174 T3 ES 2141174T3
Authority
ES
Spain
Prior art keywords
pct
antagonists
tachiquinine
arylmetiloximetil
piperidines
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Lifetime
Application number
ES93923630T
Other languages
English (en)
Inventor
Timothy Harrison
Angus Macleod
Graeme Irvine Stevenson
Brian John Williams
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Organon Pharma UK Ltd
Original Assignee
Merck Sharp and Dohme Ltd
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
Priority claimed from GB929222633A external-priority patent/GB9222633D0/en
Priority claimed from GB939308962A external-priority patent/GB9308962D0/en
Priority claimed from GB939313680A external-priority patent/GB9313680D0/en
Priority claimed from GB939316112A external-priority patent/GB9316112D0/en
Application filed by Merck Sharp and Dohme Ltd filed Critical Merck Sharp and Dohme Ltd
Application granted granted Critical
Publication of ES2141174T3 publication Critical patent/ES2141174T3/es
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

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    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/08—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
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    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/18—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D211/20—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulphur atoms
    • C07D211/22—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulphur atoms by oxygen atoms
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    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
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Abstract

LOS COMPUESTOS DE LA FORMULA (I) EN LA QUE M ES 2, 3 O 4; N ES 0, 1 O 2 CUANDO M ES 2 O 3 Y N ES 0 O 1 CUANDO M ES 4; X REPRESENTA O O S; R1 REPRESENTA FENILO OPCIONALMENTE SUSTITUIDO POR 1, 2 O 3 GRUPOS SELECCIONADOS DEL ALQUILO C1-6, ALQUENILO C2-6, ALQUINILO C26, HALO, CIANO, NITRO, TRIFUOROMETILO, TRIMETILSILILO, -ORA, SRA, SORA, SO2RA, -NRARB, -NRACORB, -NRACO2RB, -CO2RA O -CONRARB, DONDE RA Y RB REPRESENTAN CADA UNO, INDEPENDIENTEMENTE, H, ALQUILO C1-6, FENILO O TRIFUOROMETILO; R2 REPRESENTA FENILO OPCIONALMENTE SUSTITUIDO POR 1, 2 O 3 GRUPOS SELECCIONADOS DEL ALQUILO C1-6, ALQUENILO C2-6, ALQUINILO C2-6, HALO, CIANO, NITRO, TRIFUOROMETILO, TRIMETILSILILO, -ORA, SRA, SO2RA, -NRARB, -NRACORB, -NRACO2RB, -CO2RA O -CONRARB, DONDE RA Y RB REPRESENTAN LO MISMO QUE SE HA DEFINIDO PREVIAMENTE; HETEROARILO SELECCIONADO DEL INDAZOLILO, TIENILO, FURILO, PIRIDILO, TIAZOLILO, TETRAZOLILO Y QUINOLILO; BENZHIDRILO; O BENCILO; EN DONDE CADA HETEROARILO Y CADA UNIDAD DE FENILO DE BENCILO Y BENZHIDRILO SE PUEDE SUSTITUIR POR ALQUILO C1-6, ALCOXI C16, HALO O TRIFUOROMETILO; Y R3 REPRESENTA H, COR9, CO2R10, COCONR10R11, COCO2R10, SO2R15, CONR10SO2R15, ALQUILO C1-6 OPCIONALMENTE SUSTITUIDO POR UN GRUPO SELECCIONADO DEL (CO2R10, CONR10R11, HIDROXI, CIANO, COR9, NR10R11, C(NOH)NR10R11, CONHFENIL(ALQUILO C1-4), COCO2R10, COCONR10R11, SO2R15, CONR10SO2R15 Y FENILO OPCIONALMENTE SUSTITUIDO POR UNO O MAS SUSTITUYENTES SELECCIONADOS DEL ALQUILO C16, ALCOXI C1-6, HALO Y TRIFUOROMETILO), Y-R8 O CO-Z-(CH2)Q-R12; R4, R5, R6 Y R7 REPRESENTAN CADA UNO, INDEPENDIENTEMENTE, H O ALQUILO C16; R8 REPRESENTA UN HETEROCICLO AROMATICO OPCIONALMENTE SUSTITUIDO; R9 REPRESENTA H, ALQUILO C1-6 O FENILO; R10 Y R11 REPRESENTAN CADA UNO, INDEPENDIENTEMENTE, H O ALQUILO C1-6; R12 REPRESENTA NR13R14 O UN GRUPO AZACICLICO O AZABICICLICO AROMATICO O NO AROMATICO OPCIONALMENTE SUSTITUIDO; R13 Y R14 REPRESENTAN CADA UNO, INDEPENDIENTEMENTE, H, ALQUILO C1-6, FENILO OPCIONALMENTE SUSTITUIDO POR UNO O MAS DE ENTRE ALQUILO C1-6, ALCOXI C1-6, HALO O TRIFUOROMETILO O FENILALQUILO C1-4 OPCIONALMENTE SUSTITUIDO EN EL ANILLO DE FENILO POR UNO O MAS DE ENTRE ALQUILO C1-6, ALCOXI C1-6, HALO O TRIFUOROMETILO; R15 REPRESENTA ALQUILO C1-6, TRIFUOROMETILO O FENILO OPCIONALMENTE SUSTITUIDO POR UNO O MAS SUSTITUYENTES SELECCIONADOS DEL ALQUILO C1-6, ALCOXI C1-6, HALO Y TRIFUOROMETILO; Y REPRESENTA UNA CADENA DE HIDROCARBURO DE 1, 2, 3 O 4 ATOMOS DE CARBONO QUE PUEDE SER OPCIONALMENTE SUSTITUIDA POR OXO; Z REPRESENTA CH2, O, S O NR10; Y Q REPRESENTA 0, 1, 2, 3, 4, 5 O 6 Y SUS SALES SON UTILES COMO ANTAGONISTAS DE LA TAQUIQUININA.
ES93923630T 1992-10-28 1993-10-27 4-arilmetiloximetil piperidinas como antagonistas de taquiquinina. Expired - Lifetime ES2141174T3 (es)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
GB929222633A GB9222633D0 (en) 1992-10-28 1992-10-28 Therapeutic agetns
GB939308962A GB9308962D0 (en) 1993-04-30 1993-04-30 Therapeutic agetns
GB939313680A GB9313680D0 (en) 1993-07-02 1993-07-02 Therapeutic agents
GB939316112A GB9316112D0 (en) 1993-08-04 1993-08-04 Therapeutic agents

Publications (1)

Publication Number Publication Date
ES2141174T3 true ES2141174T3 (es) 2000-03-16

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Family Applications (1)

Application Number Title Priority Date Filing Date
ES93923630T Expired - Lifetime ES2141174T3 (es) 1992-10-28 1993-10-27 4-arilmetiloximetil piperidinas como antagonistas de taquiquinina.

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US (1) US5620989A (es)
EP (1) EP0666856B1 (es)
JP (1) JPH08502510A (es)
AT (1) ATE188472T1 (es)
AU (1) AU678409B2 (es)
CA (1) CA2146767A1 (es)
DE (1) DE69327541T2 (es)
ES (1) ES2141174T3 (es)
WO (1) WO1994010165A1 (es)

Families Citing this family (72)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1995002595A1 (en) * 1993-07-15 1995-01-26 Pfizer Inc. Benzyloxyquinuclidines as substance p antagonists
GB9315808D0 (en) * 1993-07-30 1993-09-15 Merck Sharp & Dohme Therapeutic agents
JPH09507500A (ja) * 1994-01-13 1997-07-29 メルク シヤープ エンド ドーム リミテツド ｇｅｍ二置換アザシクロ系のタキキニン拮抗薬
US7101547B1 (en) 1999-01-22 2006-09-05 The United States Of America As Represented By The Secretary Of The Department Of Health And Human Services Method for the prevention and treatment of diseases caused by an inflammatory response mediated by endogenous substance P by using anti-substance P antibodies
GB9904786D0 (en) * 1999-03-02 1999-04-28 Merck Sharp & Dohme Therapeutic agents
MXPA02006017A (es) * 1999-12-17 2002-12-05 Schering Corp Antagonistas de neuroquinina selectivos.
US6436928B1 (en) 1999-12-17 2002-08-20 Schering Corporation Selective neurokinin antagonists
WO2002046156A2 (en) 2000-12-06 2002-06-13 Sepracor, Inc. 4,4-disubstituted piperidines for use as dopamine, serotonin and norepinephrine ligands
AU2002259147A1 (en) 2001-05-08 2002-11-18 Schering Corporation Use of neurokinin receptor antagonists to treat androgen-dependent diseases
PL369108A1 (en) 2001-09-06 2005-04-18 Schering Corporation 17beta-hydroxysteroid dehydrogenase type 3 inhibitors for the treatment of androgen dependent diseases
ATE471315T1 (de) * 2001-10-17 2010-07-15 Schering Corp Piperidin- und piperazinacetamide als inhibitoren der 17beta-hydroxysteroiddehydrogenase des typs 3 zur behandlung androgenabhängiger krankheiten
TW200300347A (en) 2001-11-13 2003-06-01 Schering Corp Nk1 antagonists
PE20030762A1 (es) 2001-12-18 2003-09-05 Schering Corp Compuestos heterociclicos como antagonistas nk1
US6878732B2 (en) * 2002-03-13 2005-04-12 Schering Corporation NK1 antagonists
JP4592077B2 (ja) * 2002-07-03 2010-12-01 シェーリング コーポレイション 嘔吐、抑鬱、不安および咳の処置のためのニューロキニン−１（ｎｋ−１）アンタゴニストとしての１−アミド−４−フェニル−４−ベンジルオキシメチル−ピペリジン誘導体および関連化合物
EP1549615B1 (en) * 2002-08-29 2008-12-03 AstraZeneca AB Naphthamide derivatives and their use
WO2004022539A1 (en) * 2002-09-09 2004-03-18 Astrazeneca Ab Naphthyl ether compounds and their use
PT1799666E (pt) 2004-07-01 2016-06-17 Opko Health Inc Derivados de piperidina como antagonistas de nk1
KR101389246B1 (ko) 2004-07-15 2014-04-24 브리스톨-마이어스스퀴브컴파니 아릴- 및 헤테로아릴-치환된 테트라히드로이소퀴놀린, 및 이것의 노르에피네프린, 도파민 및 세로토닌의 재흡수를 차단하기 위한 용도
US7354922B2 (en) * 2004-12-14 2008-04-08 Schering Corporation Bridged ring NK1 antagonists
US8362075B2 (en) 2005-05-17 2013-01-29 Merck Sharp & Dohme Corp. Cyclohexyl sulphones for treatment of cancer
JP5258561B2 (ja) 2005-07-15 2013-08-07 アルバニー モレキュラー リサーチ， インコーポレイテッド アリール置換およびヘテロアリール置換テトラヒドロベンズアゼピンならびにノルエピネフリン、ドーパミンおよびセロトニンの再取り込みを遮断するためのその使用
JP4879988B2 (ja) 2005-09-29 2012-02-22 メルク・シャープ・エンド・ドーム・コーポレイション メラノコルチン−４受容体モジュレーターとしてのアシル化スピロピペリジン誘導体
GB0603041D0 (en) 2006-02-15 2006-03-29 Angeletti P Ist Richerche Bio Therapeutic compounds
AR060353A1 (es) 2006-04-05 2008-06-11 Schering Corp Sales de hidrocloruro de 8 - [( 1- (3,5 -bis- (trifluorometil) fenil) -etoxi) -metil] -8-fenil-1,7 -diaza- spiro [4.5] decan -2-ona. composiciones farmaceuticas
EP2004148B1 (en) 2006-04-05 2015-07-15 OPKO Health, Inc. Pharmaceutical formulations comprising salts of (5S,8S)-8-[{(1 R)-1-(3,5-Bis-trifluoromethyl)phenyl]- ethoxy}-methyl]-8-phenyl-1 ,7-diazaspiro[4.5]decan-2-one and their medical use
US20070249607A1 (en) * 2006-04-17 2007-10-25 Bristol-Myers Squibb Company Nk-1 and serotonin transporter inhibitors
JP2009544726A (ja) * 2006-07-27 2009-12-17 ブリストル−マイヤーズ スクイブ カンパニー 置換ヘテロサイクリックエーテルおよびｃｎｓ疾患におけるその使用
US8071778B2 (en) * 2006-07-27 2011-12-06 Bristol-Myers Squibb Company Substituted heterocyclic ethers and their use in CNS disorders
WO2008039327A2 (en) 2006-09-22 2008-04-03 Merck & Co., Inc. Method of treatment using fatty acid synthesis inhibitors
US20110218176A1 (en) 2006-11-01 2011-09-08 Barbara Brooke Jennings-Spring Compounds, methods, and treatments for abnormal signaling pathways for prenatal and postnatal development
CA2674436C (en) 2007-01-10 2012-07-17 Istituto Di Ricerche Di Biologia Molecolare P. Angeletti S.P.A. Amide substituted indazoles as poly(adp-ribose)polymerase (parp) inhibitors
AR066191A1 (es) 2007-03-22 2009-08-05 Schering Corp Proceso e intermediarios para la sintesis de compuestos 8- [ ( 1- (3,5- bis- ( trifluorometil) fenil) - etoxi ) - metil]- 8 fenil - 1,7- diaza - espiro (4, 5) decan -2 ona
EP2145884B1 (en) 2007-04-02 2014-08-06 Msd K.K. Indoledione derivative
CA2690191C (en) 2007-06-27 2015-07-28 Merck Sharp & Dohme Corp. 4-carboxybenzylamino derivatives as histone deacetylase inhibitors
US8026257B2 (en) * 2007-07-11 2011-09-27 Bristol-Myers Squibb Company Substituted heterocyclic ethers and their use in CNS disorders
US20090018163A1 (en) * 2007-07-11 2009-01-15 Bristol-Myers Squibb Company Substituted Heterocyclic Ethers and Their Use in CNS Disorders
US7632861B2 (en) * 2007-11-13 2009-12-15 Bristol-Myers Squibb Company Substituted heterocyclic ethers and their use in CNS disorders
CA2711399C (en) 2008-02-06 2016-10-11 Banyu Pharmaceutical Co., Ltd. 3-substituted sulfonylpiperidine derivative
KR20100126467A (ko) 2008-03-03 2010-12-01 타이거 파마테크 티로신 키나아제 억제제
US9156812B2 (en) 2008-06-04 2015-10-13 Bristol-Myers Squibb Company Crystalline form of 6-[(4S)-2-methyl-4-(2-naphthyl)-1,2,3,4-tetrahydroisoquinolin-7-yl]pyridazin-3-amine
PT2346823E (pt) 2008-09-05 2015-11-26 Opko Health Inc Intermediários para a síntese de compostos 8-[{1-(3,5-bis(trifluorometil)fenil)-etóxi}-metil]-8-fenil-1,7-diazaspiro[ 4.5]decan-2-ona
US8691825B2 (en) 2009-04-01 2014-04-08 Merck Sharp & Dohme Corp. Inhibitors of AKT activity
EP2429296B1 (en) 2009-05-12 2017-12-27 Albany Molecular Research, Inc. 7-([1,2,4,]triazolo[1,5,-a]pyridin-6-yl)-4-(3,4-dichlorophenyl)-1,2,3,4- tetrahydroisoquinoline and use thereof
JP5739415B2 (ja) 2009-05-12 2015-06-24 ブリストル−マイヤーズ スクウィブ カンパニー （Ｓ）−７−（［１，２，４］トリアゾロ［１，５−ａ］ピリジン−６−イル）−４−（３，４−ジクロロフェニル）−１，２，３，４−テトラヒドロイソキノリンの結晶形態およびその使用
MX2011011901A (es) 2009-05-12 2012-01-20 Albany Molecular Res Inc Tetrahidroisoquinolinas aril, heteroaril, y heterociclo sustituidas y uso de las mismas.
RU2017145628A (ru) 2009-08-14 2019-02-19 ОПКО Хельс, Инк. Композиции антагонистов нейрокинина-1 для внутривенного введения
EA023838B1 (ru) 2009-10-14 2016-07-29 Мерк Шарп Энд Домэ Корп. ЗАМЕЩЕННЫЕ ПИПЕРИДИНЫ, КОТОРЫЕ ПОВЫШАЮТ АКТИВНОСТЬ p53, И ИХ ПРИМЕНЕНИЕ
WO2011163330A1 (en) 2010-06-24 2011-12-29 Merck Sharp & Dohme Corp. Novel heterocyclic compounds as erk inhibitors
EP3330377A1 (en) 2010-08-02 2018-06-06 Sirna Therapeutics, Inc. Rna interference mediated inhibition of catenin (cadherin-associated protein), beta 1 (ctnnb1) gene expression using short interfering nucleic acid (sina)
CA2807307C (en) 2010-08-17 2021-02-09 Merck Sharp & Dohme Corp. Rna interference mediated inhibition of hepatitis b virus (hbv) gene expression using short interfering nucleic acid (sina)
US8883801B2 (en) 2010-08-23 2014-11-11 Merck Sharp & Dohme Corp. Substituted pyrazolo[1,5-a]pyrimidines as mTOR inhibitors
EP2613782B1 (en) 2010-09-01 2016-11-02 Merck Sharp & Dohme Corp. Indazole derivatives useful as erk inhibitors
WO2012036997A1 (en) 2010-09-16 2012-03-22 Schering Corporation Fused pyrazole derivatives as novel erk inhibitors
EP3766975A1 (en) 2010-10-29 2021-01-20 Sirna Therapeutics, Inc. Rna interference mediated inhibition of gene expression using short interfering nucleic acid (sina)
US9351965B2 (en) 2010-12-21 2016-05-31 Merck Sharp & Dohme Corp. Indazole derivatives useful as ERK inhibitors
CN103732592A (zh) 2011-04-21 2014-04-16 默沙东公司 胰岛素样生长因子-1受体抑制剂
US9023865B2 (en) 2011-10-27 2015-05-05 Merck Sharp & Dohme Corp. Compounds that are ERK inhibitors
EP2844261B1 (en) 2012-05-02 2018-10-17 Sirna Therapeutics, Inc. SHORT INTERFERING NUCLEIC ACID (siNA) COMPOSITIONS
US9233979B2 (en) 2012-09-28 2016-01-12 Merck Sharp & Dohme Corp. Compounds that are ERK inhibitors
SI2925888T1 (en) 2012-11-28 2018-02-28 Merck Sharp & Dohme Corp. Compounds and methods for the treatment of cancer
AU2013361694B2 (en) 2012-12-20 2017-10-26 Merck Sharp & Dohme Corp. Substituted imidazopyridines as HDM2 inhibitors
EP2951180B1 (en) 2013-01-30 2018-05-02 Merck Sharp & Dohme Corp. 2,6,7,8 substituted purines as hdm2 inhibitors
WO2014124212A1 (en) 2013-02-08 2014-08-14 General Mills, Inc. Reduced sodium food products
US20160194368A1 (en) 2013-09-03 2016-07-07 Moderna Therapeutics, Inc. Circular polynucleotides
CN104557868A (zh) * 2015-01-22 2015-04-29 湖南华腾制药有限公司 一种喹啉衍生物的制备方法
WO2018169818A1 (en) * 2017-03-12 2018-09-20 Xiaodong Wang Polycyclic amines as opioid receptor modulators
WO2019094311A1 (en) 2017-11-08 2019-05-16 Merck Sharp & Dohme Corp. Prmt5 inhibitors
WO2020033282A1 (en) 2018-08-07 2020-02-13 Merck Sharp & Dohme Corp. Prmt5 inhibitors
WO2020033284A1 (en) 2018-08-07 2020-02-13 Merck Sharp & Dohme Corp. Prmt5 inhibitors
US20220380393A1 (en) 2019-06-28 2022-12-01 Shanghai Shengdi Pharmaceutical Co., Ltd Neurokinin-1 antagonist
WO2022135549A1 (zh) 2020-12-25 2022-06-30 上海盛迪医药有限公司 Nk1拮抗剂前药化合物与5-ht3受体拮抗剂的联用用途

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA1337418C (en) * 1988-03-28 1995-10-24 Engelbert Ciganek 4-aryl-4-piperiding (or pyrrolidine or hexahydroazepine) carbinols and heterocyclic analogs thereof
EP0593557B1 (en) * 1991-07-05 1996-01-31 MERCK SHARP & DOHME LTD. Aromatic compounds, pharmaceutical compositions containing them and their use in therapy

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