ATE170174T1 - Gem-bissubstituierte azazyclische tachykinin- antagonisten - Google Patents

Gem-bissubstituierte azazyclische tachykinin- antagonisten

Info

Publication number
ATE170174T1
ATE170174T1 AT95905204T AT95905204T ATE170174T1 AT E170174 T1 ATE170174 T1 AT E170174T1 AT 95905204 T AT95905204 T AT 95905204T AT 95905204 T AT95905204 T AT 95905204T AT E170174 T1 ATE170174 T1 AT E170174T1
Authority
AT
Austria
Prior art keywords
pct
azazyclic
gem
bis
substituted
Prior art date
Application number
AT95905204T
Other languages
English (en)
Inventor
Raymond Baker
Richard Thomas Lewis
Angus Murray Macleod
Graeme Irvine Stevenson
Original Assignee
Merck Sharp & Dohme
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 GB9400542A external-priority patent/GB9400542D0/en
Priority claimed from GB9403072A external-priority patent/GB9403072D0/en
Application filed by Merck Sharp & Dohme filed Critical Merck Sharp & Dohme
Application granted granted Critical
Publication of ATE170174T1 publication Critical patent/ATE170174T1/de

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/08Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/20Hypnotics; Sedatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/26Psychostimulants, e.g. nicotine, cocaine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • A61P27/14Decongestants or antiallergics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic 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
    • C07D211/08Heterocyclic 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
    • C07D211/18Heterocyclic 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
    • C07D211/20Heterocyclic 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
    • C07D211/22Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Psychiatry (AREA)
  • Immunology (AREA)
  • Pain & Pain Management (AREA)
  • Pulmonology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Hospice & Palliative Care (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Transplantation (AREA)
  • Addiction (AREA)
  • Anesthesiology (AREA)
  • Rheumatology (AREA)
  • Otolaryngology (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
AT95905204T 1994-01-13 1995-01-12 Gem-bissubstituierte azazyclische tachykinin- antagonisten ATE170174T1 (de)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GB9400542A GB9400542D0 (en) 1994-01-13 1994-01-13 Therapeutic agents
GB9403072A GB9403072D0 (en) 1994-02-17 1994-02-17 Therapeutic agents

Publications (1)

Publication Number Publication Date
ATE170174T1 true ATE170174T1 (de) 1998-09-15

Family

ID=26304158

Family Applications (1)

Application Number Title Priority Date Filing Date
AT95905204T ATE170174T1 (de) 1994-01-13 1995-01-12 Gem-bissubstituierte azazyclische tachykinin- antagonisten

Country Status (9)

Country Link
US (1) US5760018A (de)
EP (1) EP0739336B1 (de)
JP (1) JPH09507500A (de)
AT (1) ATE170174T1 (de)
AU (1) AU685212B2 (de)
CA (1) CA2180746A1 (de)
DE (1) DE69504300T2 (de)
ES (1) ES2120170T3 (de)
WO (1) WO1995019344A1 (de)

Families Citing this family (76)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW458774B (en) 1995-10-20 2001-10-11 Pfizer Antiemetic pharmaceutical compositions
GB9600235D0 (en) * 1996-01-05 1996-03-06 Pfizer Ltd Therapeutic agents
WO2000035876A1 (en) 1998-12-18 2000-06-22 Du Pont Pharmaceuticals Company 2-substituted-4-nitrogen heterocycles as modulators of chemokine receptor activity
US6525069B1 (en) 1998-12-18 2003-02-25 Bristol-Myers Squibb Pharma Co. N-ureidoalkyl-piperidines as modulators of chemokine receptor activity
US6331541B1 (en) 1998-12-18 2001-12-18 Soo S. Ko N-ureidoalkyl-piperidines as modulators of chemokine receptor activity
DE69926806D1 (de) 1998-12-18 2005-09-22 Bristol Myers Squibb Pharma Co N-ureidoalkylpiperidine als modulatoren der aktivität der chemokinrezeptoren
US6486180B1 (en) 1998-12-18 2002-11-26 Bristol-Myers Squibb Pharma Company N-ureidoalkyl-piperidines as modulators of chemokine receptor activity
US6331545B1 (en) 1998-12-18 2001-12-18 Soo S. Ko Heterocycyclic piperidines as modulators of chemokine receptor activity
US6492400B1 (en) 1998-12-18 2002-12-10 Bristol-Myers Squibb Pharma Company N-ureidoalkyl-piperidines as modulators of chemokine receptor activity
US6828460B2 (en) 1999-03-22 2004-12-07 Pfizer Inc. Resorcinol derivatives
US6897234B2 (en) 1999-12-17 2005-05-24 Bristol-Myers Squibb Pharma Company N-ureidoalkyl-piperidines as modulators of chemokine receptor activity
US6436928B1 (en) * 1999-12-17 2002-08-20 Schering Corporation Selective neurokinin antagonists
CA2412355A1 (en) * 2000-06-12 2001-12-20 University Of Rochester Method of treating symptoms of hormonal variation, including hot flashes, using tachykinin receptor antagonist
JP2004517805A (ja) 2000-06-30 2004-06-17 ブリストル−マイヤーズ・スクイブ・ファーマ・カンパニー ケモカイン受容体活性調節剤としてのn−ウレイドヘテロシクロアルキル−ピペリジン
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
PE20030703A1 (es) * 2001-09-06 2003-08-21 Schering Corp Inhibidores de la 17b-hidroxiesteroide deshidrogenasa tipo 3
EP1436281B1 (de) 2001-10-17 2010-06-16 Schering Corporation Piperidin- und piperazinacetamide als inhibitoren der 17beta-hydroxysteroiddehydrogenase des typs 3 zur behandlung androgenabhängiger krankheiten
DE60222693T2 (de) * 2001-11-13 2008-07-17 Schering Corp. Nk1-antagonisten
PE20030762A1 (es) 2001-12-18 2003-09-05 Schering Corp Compuestos heterociclicos como antagonistas nk1
US20060205724A1 (en) * 2002-05-29 2006-09-14 The Regents Of The University Of California Antagonizing nk-1 receptors inhibits consumption of substances of abuse
CN1678317B (zh) * 2002-07-03 2010-10-27 先灵公司 用作治疗呕吐、抑郁症、焦虑症和咳嗽的神经激肽-1(nk-1)拮抗剂的1-酰氨基-4-苯基-4-苄氧基甲基-哌啶衍生物和相关化合物
JP2006502157A (ja) * 2002-09-09 2006-01-19 アストラゼネカ・アクチエボラーグ ナフチルエーテル化合物及びそれらの使用
EP3269713A1 (de) 2004-07-01 2018-01-17 OPKO Health, Inc. Piperidinderivate als nk1 antagonisten
US7354922B2 (en) * 2004-12-14 2008-04-08 Schering Corporation Bridged ring NK1 antagonists
ES2382814T3 (es) 2005-05-17 2012-06-13 Merck Sharp & Dohme Ltd. Ácido cis-4-[(4-clorofenil)sulfonil]-4-(2,5-difluorofenil)ciclohexanopropanoico para el tratamiento del cáncer
KR101594898B1 (ko) 2005-07-15 2016-02-18 알바니 몰레큘라 리써치, 인크. 아릴- 및 헤테로아릴-치환된 테트라히드로벤자제핀, 및 노르에피네프린, 도파민 및 세로토닌의 재흡수를 차단하기 위한 용도
EP1940842B1 (de) 2005-09-29 2012-05-30 Merck Sharp & Dohme Corp. Acylierte spiropiperidinderivate als modulatoren des melanocortin-4-rezeptors
GB0519879D0 (en) * 2005-09-30 2005-11-09 Astrazeneca Ab Chemical process
GB0603041D0 (en) 2006-02-15 2006-03-29 Angeletti P Ist Richerche Bio Therapeutic compounds
HUE028908T2 (en) 2006-04-05 2017-01-30 Opko Health Inc The hydrochloride salt of 8 - [{1- (3,5-bis (trifluoromethyl) phenyl) ethoxy} methyl] -8-phenyl-1,7-diazaspiro [4.5] decan-2-one, and process
CN103751186B (zh) 2006-04-05 2016-08-24 欧科生医股份有限公司 药物制剂:8-[{1-(3,5-双-(三氟甲基)苯基)-乙氧基}-甲基]-8-苯基-1,7-二氮杂-螺[4.5]癸-2-酮的盐及用其治疗的方法
US20070249607A1 (en) * 2006-04-17 2007-10-25 Bristol-Myers Squibb Company Nk-1 and serotonin transporter inhibitors
US8071778B2 (en) * 2006-07-27 2011-12-06 Bristol-Myers Squibb Company Substituted heterocyclic ethers and their use in CNS disorders
US8173629B2 (en) 2006-09-22 2012-05-08 Merck Sharp & Dohme Corp. 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
US8420622B2 (en) * 2006-12-20 2013-04-16 Merck, Sharp & Dohme, Corp. Silylated piperidine derivatives
JP4611444B2 (ja) 2007-01-10 2011-01-12 イステイチユート・デイ・リチエルケ・デイ・ビオロジア・モレコラーレ・ピ・アンジエレツテイ・エツセ・ピー・アー ポリ(adp−リボース)ポリメラーゼ(parp)阻害剤としてのアミド置換インダゾール
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
JP5319518B2 (ja) 2007-04-02 2013-10-16 Msd株式会社 インドールジオン誘導体
AU2008269154B2 (en) 2007-06-27 2014-06-12 Merck Sharp & Dohme Llc 4-carboxybenzylamino derivatives as histone deacetylase inhibitors
US20090018163A1 (en) * 2007-07-11 2009-01-15 Bristol-Myers Squibb Company Substituted Heterocyclic Ethers and Their Use in CNS Disorders
US8026257B2 (en) * 2007-07-11 2011-09-27 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
AU2009222122A1 (en) 2008-03-03 2009-09-11 Tiger Pharmatech Tyrosine kinase inhibitors
EP3034493A1 (de) 2008-09-05 2016-06-22 OPKO Health, Inc. Synthese von 8-[{1-(3,5-bis-(trifluormethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diaza-spiro[4.5]decan-2-on-verbindungen
WO2010114780A1 (en) 2009-04-01 2010-10-07 Merck Sharp & Dohme Corp. Inhibitors of akt activity
AU2010247763B2 (en) 2009-05-12 2015-12-24 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
AU2010247735B2 (en) 2009-05-12 2015-07-16 Albany Molecular Research, Inc. Crystalline forms of (S)-7-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-4-(3,4-dichlorophenyl)- 1,2,3,4-tetrahydroisoquinoline and use thereof
CN102573475B (zh) 2009-08-14 2016-01-20 欧科生医股份有限公司 神经激肽-1拮抗剂的静脉内制剂
PE20121172A1 (es) 2009-10-14 2012-09-05 Merck Sharp & Dohme Piperidinas sustituidas con actividad en la hdm2
WO2011163330A1 (en) 2010-06-24 2011-12-29 Merck Sharp & Dohme Corp. Novel heterocyclic compounds as erk inhibitors
EP3330377A1 (de) 2010-08-02 2018-06-06 Sirna Therapeutics, Inc. Durch rna-interferenz vermittelte hemmung der catenin (cadherin-assoziiertes protein)-beta-1 (ctnnb1)- genexpression mittels kurzer interferierender nukleinsäuren (sina)
US9029341B2 (en) 2010-08-17 2015-05-12 Sirna Therapeutics, Inc. 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 (de) 2010-09-01 2016-11-02 Merck Sharp & Dohme Corp. Indazolderivate als erk-hemmer
US9242981B2 (en) 2010-09-16 2016-01-26 Merck Sharp & Dohme Corp. Fused pyrazole derivatives as novel ERK inhibitors
WO2012058210A1 (en) 2010-10-29 2012-05-03 Merck Sharp & Dohme Corp. RNA INTERFERENCE MEDIATED INHIBITION OF GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACIDS (siNA)
WO2012087772A1 (en) 2010-12-21 2012-06-28 Schering Corporation Indazole derivatives useful as erk inhibitors
AU2012245971A1 (en) 2011-04-21 2013-10-17 Piramal Enterprises Limited A crystalline form of a salt of a morpholino sulfonyl indole derivative and a process for its preparation
EP2770987B1 (de) 2011-10-27 2018-04-04 Merck Sharp & Dohme Corp. Neue verbindungen als erk-hemmer
US20150299696A1 (en) 2012-05-02 2015-10-22 Sirna Therapeutics, Inc. SHORT INTERFERING NUCLEIC ACID (siNA) COMPOSITIONS
RU2660429C2 (ru) 2012-09-28 2018-07-06 Мерк Шарп И Доум Корп. Новые соединения, которые являются ингибиторами erk
RS56680B1 (sr) 2012-11-28 2018-03-30 Merck Sharp & Dohme Kompozicije i postupci za lečenje kancera
KR102196882B1 (ko) 2012-12-20 2020-12-30 머크 샤프 앤드 돔 코포레이션 Hdm2 억제제로서의 치환된 이미다조피리딘
WO2014120748A1 (en) 2013-01-30 2014-08-07 Merck Sharp & Dohme Corp. 2,6,7,8 substituted purines as hdm2 inhibitors
WO2015034925A1 (en) 2013-09-03 2015-03-12 Moderna Therapeutics, Inc. Circular polynucleotides
EP3525785B1 (de) 2016-10-12 2025-08-27 Merck Sharp & Dohme LLC Kdm5-inhibitoren
US10947234B2 (en) 2017-11-08 2021-03-16 Merck Sharp & Dohme Corp. PRMT5 inhibitors
EP3706747B1 (de) 2017-11-08 2025-09-03 Merck Sharp & Dohme LLC Prmt5-inhibitoren
US11981701B2 (en) 2018-08-07 2024-05-14 Merck Sharp & Dohme Llc PRMT5 inhibitors
US12173026B2 (en) 2018-08-07 2024-12-24 Merck Sharp & Dohme Llc PRMT5 inhibitors
EP3833668B1 (de) 2018-08-07 2025-03-19 Merck Sharp & Dohme LLC Prmt5-inhibitoren
JP7702887B2 (ja) 2019-06-28 2025-07-04 上海盛迪医薬有限公司 ニューロキニン-1アンタゴニスト
AU2021407138A1 (en) 2020-12-25 2023-06-29 Jiangsu Hengrui Pharmaceuticals Co., Ltd. Use of nk1 antagonist prodrug compound in combination with 5-ht3 receptor antagonist
CN119528985A (zh) 2023-08-28 2025-02-28 科睿迪(南京)医药科技有限公司 神经激肽-1受体拮抗剂化合物

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK162087D0 (da) * 1987-03-31 1987-03-31 Ferrosan As Piperidinforbindelser, deres fremstilling og anvendelse
IL99320A (en) * 1990-09-05 1995-07-31 Sanofi Sa Arylalkylamines, their preparation and pharmaceutical compositions containing them
EP0636130A1 (de) * 1992-04-15 1995-02-01 Merck Sharp & Dohme Ltd. Azaclyclische Verbindungen
AU678409B2 (en) * 1992-10-28 1997-05-29 Merck Sharp & Dohme Limited 4-arylmethyloxymethyl piperidines as tachykinin antagonists
US5661162A (en) * 1992-12-14 1997-08-26 Merck Sharp & Dohme Limited 4-aminomethyl/thiomethyl/sulfonylmethyl-4-phenylpiperdines as tachykinin receptor antagonists
ATE166867T1 (de) * 1993-02-18 1998-06-15 Merck Sharp & Dohme Azacyclische verbindungen, sie enthaltende zusammensetzungen und ihre verwendung als tachykinin antagoniste

Also Published As

Publication number Publication date
ES2120170T3 (es) 1998-10-16
AU1390295A (en) 1995-08-01
EP0739336A1 (de) 1996-10-30
DE69504300T2 (de) 1999-04-29
WO1995019344A1 (en) 1995-07-20
EP0739336B1 (de) 1998-08-26
CA2180746A1 (en) 1995-07-20
AU685212B2 (en) 1998-01-15
US5760018A (en) 1998-06-02
JPH09507500A (ja) 1997-07-29
DE69504300D1 (de) 1998-10-01

Similar Documents

Publication Publication Date Title
ATE170174T1 (de) Gem-bissubstituierte azazyclische tachykinin- antagonisten
ATE169001T1 (de) Substituierte spiro-azaringen als tachykinine rezeptor antagonisten
DE69327541D1 (en) 4-arylmethyloxymethyl piperidine als tachykinin antagonisten
ATE227722T1 (de) Morpholinwirkstoffvorläufer als tachykininreceptorantagonisten
DE69318854D1 (de) Spiroazacyclischderivate als substanz p antagonisten
DE69416869D1 (de) Diazabicyclische neurokinin antagonisten
AR008384A1 (es) Composicion topica para el tratamiento de condiciones de la piel, uso del compuesto para la preparacion de un medicamento y metodo no-terapeuticos para el pulido de la piel y de suavizante capilar .
NZ325449A (en) Naphthyl-substituted benzimidazole derivatives as anticoagulants
DE69523169D1 (de) Verwendung von Mangiferin oder seinen Derivaten zur kosmetischen Anwendung
DE69616480D1 (de) Piperidinderivate als neurokininantagonisten
ATE247096T1 (de) Tetrahydropyranderivate und deren verwendung als therapeutische mittel
ATE279406T1 (de) Piperidinderivate mit tachykinin-antagonistischer wirkung
ATE413382T1 (de) Verbindungen, die als liganden des melanocortin- rezeptors fungieren
DE59409312D1 (de) Imidazopyridine und ihre anwendung zur behandlung von magen-darm krankheiten
DE69614847D1 (de) Spirocyclische und bicyclische diazinyl- und carbazinyloxazolidinone
NO985977L (no) Spiro-piperidinderivater og deres anvendelse som terapeutiske midler
PE34297A1 (es) Ligandos especificos del neuropeptido y1
TR199900318T2 (xx) IL-8 resept�r antagonistleri.
ES2160103T3 (es) Peptidos que tienen actividad antagonista de taquiquinina.
GB9603137D0 (en) Therapeutic agents
NO942775L (no) 3-fenylureido-azepin-2-oner og -benzazepin-2-oner anvendelige som cholecystokinin-antagonister
ATE198887T1 (de) Substituierte arylthioalkylthiopyridine