IL106142A - Morpholine and thiomorpholine tachykinin receptor antagonists, their preparation and pharmaceutical compositions containing them - Google Patents

Morpholine and thiomorpholine tachykinin receptor antagonists, their preparation and pharmaceutical compositions containing them

Info

Publication number
IL106142A
IL106142A IL106142A IL10614293A IL106142A IL 106142 A IL106142 A IL 106142A IL 106142 A IL106142 A IL 106142A IL 10614293 A IL10614293 A IL 10614293A IL 106142 A IL106142 A IL 106142A
Authority
IL
Israel
Prior art keywords
optionally substituted
phenyl
alkyl
group
substituent
Prior art date
Application number
IL106142A
Other languages
English (en)
Other versions
IL106142A0 (en
Original Assignee
Merck & Co 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 Merck & Co Inc filed Critical Merck & Co Inc
Publication of IL106142A0 publication Critical patent/IL106142A0/xx
Publication of IL106142A publication Critical patent/IL106142A/xx

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D265/00Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/281,4-Oxazines; Hydrogenated 1,4-oxazines
    • C07D265/301,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings
    • 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
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • 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
    • A61P25/06Antimigraine agents
    • 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
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D265/00Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/281,4-Oxazines; Hydrogenated 1,4-oxazines
    • C07D265/301,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings
    • C07D265/321,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings with oxygen atoms directly attached to ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D279/00Heterocyclic compounds containing six-membered rings having one nitrogen atom and one sulfur atom as the only ring hetero atoms
    • C07D279/101,4-Thiazines; Hydrogenated 1,4-thiazines
    • C07D279/121,4-Thiazines; Hydrogenated 1,4-thiazines not condensed with other rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Pain & Pain Management (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pulmonology (AREA)
  • Cardiology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Vascular Medicine (AREA)
  • Rheumatology (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
IL106142A 1992-06-29 1993-06-25 Morpholine and thiomorpholine tachykinin receptor antagonists, their preparation and pharmaceutical compositions containing them IL106142A (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US90597692A 1992-06-29 1992-06-29
US97144892A 1992-11-04 1992-11-04
US6191493A 1993-05-19 1993-05-19

Publications (2)

Publication Number Publication Date
IL106142A0 IL106142A0 (en) 1993-10-20
IL106142A true IL106142A (en) 1997-03-18

Family

ID=27370159

Family Applications (1)

Application Number Title Priority Date Filing Date
IL106142A IL106142A (en) 1992-06-29 1993-06-25 Morpholine and thiomorpholine tachykinin receptor antagonists, their preparation and pharmaceutical compositions containing them

Country Status (33)

Country Link
EP (1) EP0577394B1 (ja)
JP (1) JP2634372B2 (ja)
KR (1) KR100301212B1 (ja)
CN (1) CN1049431C (ja)
AT (1) ATE186532T1 (ja)
AU (1) AU4656193A (ja)
BG (1) BG62963B1 (ja)
BR (1) BR1100375A (ja)
CA (1) CA2099233A1 (ja)
CY (1) CY2200B1 (ja)
CZ (1) CZ288530B6 (ja)
DE (1) DE69326977T2 (ja)
DK (1) DK0577394T3 (ja)
DZ (1) DZ1700A1 (ja)
ES (1) ES2141133T3 (ja)
FI (1) FI111363B (ja)
GR (1) GR3031824T3 (ja)
HR (1) HRP931003B1 (ja)
HU (1) HU219713B (ja)
IL (1) IL106142A (ja)
LV (1) LV12568B (ja)
MX (1) MX9303888A (ja)
MY (1) MY108836A (ja)
NO (1) NO305698B1 (ja)
NZ (1) NZ254476A (ja)
RO (1) RO114448B1 (ja)
RU (1) RU2140914C1 (ja)
SI (1) SI9300346B (ja)
SK (1) SK281093B6 (ja)
TW (1) TW358808B (ja)
WO (1) WO1994000440A1 (ja)
YU (1) YU49036B (ja)
ZA (1) ZA934624B (ja)

Families Citing this family (118)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5637699A (en) * 1992-06-29 1997-06-10 Merck & Co., Inc. Process for preparing morpholine tachykinin receptor antagonists
US5719147A (en) * 1992-06-29 1998-02-17 Merck & Co., Inc. Morpholine and thiomorpholine tachykinin receptor antagonists
US6048859A (en) * 1992-06-29 2000-04-11 Merck & Co., Inc. Morpholine and thiomorpholine tachykinin receptor antagonists
IL111960A (en) * 1993-12-17 1999-12-22 Merck & Co Inc Morpholines and thiomorpholines their preparation and pharmaceutical compositions containing them
ES2164758T3 (es) * 1993-12-29 2002-03-01 Merck Sharp & Dohme Derivados de morfolina sustituidos y su uso como agentes terapeuticos.
US5610165A (en) * 1994-02-17 1997-03-11 Merck & Co., Inc. N-acylpiperidine tachykinin antagonists
TW385308B (en) * 1994-03-04 2000-03-21 Merck & Co Inc Prodrugs of morpholine tachykinin receptor antagonists
JPH10500944A (ja) * 1994-05-05 1998-01-27 メルク シヤープ エンド ドーム リミテツド モルホリン誘導体及びタキキニンのアンタゴニストとしてのそれらの使用
DK0777659T3 (da) * 1994-08-15 2001-09-03 Merck Sharp & Dohme Morpholinderivater og deres anvendelse som terapeutiske midler
GB9417956D0 (en) * 1994-09-02 1994-10-26 Merck Sharp & Dohme Therapeutic agents
US5457107A (en) * 1994-09-16 1995-10-10 Merck & Co., Inc. Polymorphic form of a tachykinin receptor antagonist
FR2728165A1 (fr) * 1994-12-19 1996-06-21 Oreal Utilisation d'un antagoniste de substance p pour le traitement des rougeurs cutanees d'origine neurogene
GB9426102D0 (en) * 1994-12-23 1995-02-22 Merck Sharp & Dohme Pharmacuetical compositions
GB9426103D0 (en) * 1994-12-23 1995-02-22 Merck Sharp & Dohme Therapeutic agents
FR2729954B1 (fr) * 1995-01-30 1997-08-01 Sanofi Sa Composes heterocycliques substitues, procede pour leur preparation et compositions pharmaceutiques les contenant
DE19504627A1 (de) * 1995-02-13 1996-08-14 Bayer Ag Verfahren und neue Zwischenprodukte zur Herstellung von Triazolinonen
GB9505492D0 (en) * 1995-03-18 1995-05-03 Merck Sharp & Dohme Therapeutic agents
GB9505491D0 (en) * 1995-03-18 1995-05-03 Merck Sharp & Dohme Therapeutic agents
DK0821671T3 (da) * 1995-04-20 2001-04-23 Pfizer Arylsulfonylhydroxamsyrederivater som MMP- og TNF-inhibitorer
GB9511031D0 (en) * 1995-06-01 1995-07-26 Merck Sharp & Dohme Chemical process
GB9513118D0 (en) * 1995-06-28 1995-08-30 Merck Sharp & Dohme Therapeutic agents
GB9513121D0 (en) * 1995-06-28 1995-08-30 Merck Sharp & Dohme Therapeutic agents
GB9513117D0 (en) * 1995-06-28 1995-08-30 Merck Sharp & Dohme Therapeutic agents
GB9523244D0 (en) * 1995-11-14 1996-01-17 Merck Sharp & Dohme Therapeutic agents
ATE194342T1 (de) * 1996-01-19 2000-07-15 Lonza Ag Verfahren zur herstellung von optisch aktivem 3- chinuclidinol
GB9603136D0 (en) * 1996-02-15 1996-04-17 Merck Sharp & Dohme Therapeutic agents
GB9603137D0 (en) * 1996-02-15 1996-04-17 Merck Sharp & Dohme Therapeutic agents
UA56185C2 (uk) * 1996-09-30 2003-05-15 Пфайзер Інк. Аралкіл- та аралкіліденгетероциклічні лактами та іміди, фармацевтична композиція та спосіб лікування
US6423708B1 (en) 1996-09-30 2002-07-23 Pfizer Inc Aralkyl and aralkylidene heterocyclic lactams and imides
JP2001502311A (ja) * 1996-10-07 2001-02-20 メルク シヤープ エンド ドーム リミテツド 抗鬱及び/又は抗不安薬としてのcns浸透性nk―1受容体拮抗薬
US6117855A (en) * 1996-10-07 2000-09-12 Merck Sharp & Dohme Ltd. Use of a NK-1 receptor antagonist and an antidepressant and/or an anti-anxiety agent
US5750549A (en) * 1996-10-15 1998-05-12 Merck & Co., Inc. Cycloalkyl tachykinin receptor antagonists
US6613765B1 (en) 1996-12-02 2003-09-02 Merck Sharp & Dohme Limited Use of NK-1 receptor antagonists for treating major depressive disorders
ES2231901T3 (es) * 1996-12-02 2005-05-16 MERCK SHARP & DOHME LTD. Uso de antagonistas del receptor de nk-1 para tratar transtornos por el uso de sustancias.
JP2001504851A (ja) * 1996-12-02 2001-04-10 メルク シヤープ エンド ドーム リミテツド 性的機能不全の治療のためのnk−1受容体拮抗薬の使用
AU734860B2 (en) * 1996-12-02 2001-06-21 Merck Sharp & Dohme Limited Use of NK-1 receptor antagonists for treating cognitive disorders
CA2273807A1 (en) * 1996-12-02 1998-06-11 Merck Sharp & Dohme Limited Use of nk-1 receptor antagonists for treating schizophrenic disorders
US5977104A (en) * 1996-12-02 1999-11-02 Merck Sharp & Dohme Ltd. Use of NK-1 receptor antagonists for treating bipolar disorders
WO1998024439A1 (en) * 1996-12-02 1998-06-11 Merck Sharp & Dohme Limited Use of nk-1 receptor antagonists for treating severe anxiety disorders
ES2234039T3 (es) * 1996-12-02 2005-06-16 MERCK SHARP & DOHME LTD. Uso de antagonistas del receptor nk-1 para tratar trastornos de depresion mayor.
US6114315A (en) * 1996-12-02 2000-09-05 Merck Sharp & Dohme Ltd. Use of NK-1 receptor antagonists for treating major depressive disorders with anxiety
WO1998024443A1 (en) * 1996-12-02 1998-06-11 Merck Sharp & Dohme Limited Use of nk-1 receptor antagonists for treating bipolar disorders
DE69730515T2 (de) * 1996-12-02 2005-09-01 Merck Sharp & Dohme Ltd., Hoddesdon Die verwendung von nk-1 rezeptor antagonisten für die behandlungen von stress störungen
CA2273809A1 (en) * 1996-12-02 1998-06-11 Merck Sharp & Dohme Limited Use of nk-1 receptor antagonists for treating movement disorders
JP2001504850A (ja) * 1996-12-02 2001-04-10 メルク シヤープ エンド ドーム リミテツド 不安を伴う重抑鬱性障害を治療するためのnk−1受容体拮抗薬の使用
US6100256A (en) * 1996-12-02 2000-08-08 Merck Sharp & Dohme Ltd. Use of NK-1 receptors antagonists for treating schizophrenic disorders
NZ336600A (en) * 1997-01-09 2000-07-28 Bifodan As Use of dichlorobenzyl alcohol for preparing a preparation for topical treatment of inflammation
CA2287487A1 (en) * 1997-04-24 1998-10-29 Merck Sharp & Dohme Limited Use of nk-1 receptor antagonists for treating eating disorders
ZA985765B (en) 1997-07-02 1999-08-04 Merck & Co Inc Polymorphic form of a tachykinin receptor antagonist.
GB9716457D0 (en) * 1997-08-04 1997-10-08 Merck Sharp & Dohme Therapeutic agents
AU738047B2 (en) * 1997-08-04 2001-09-06 Merck Sharp & Dohme Limited Use of NK-1 receptor antagonists for treating mania
GB9716463D0 (en) * 1997-08-04 1997-10-08 Merck Sharp & Dohme Therapeutic agents
AU737019B2 (en) * 1997-08-04 2001-08-09 Merck Sharp & Dohme Limited Use of NK-1 receptor antagonists for treating aggressive behaviour disorders
US6087348A (en) * 1997-12-01 2000-07-11 Merck Sharp & Dohme Ltd. Use of NK-1 receptor antagonists for treating stress disorders
US6271230B1 (en) 1997-12-01 2001-08-07 Merck Sharp & Dohme Limited Use of NK-1 receptor antagonists for treating cognitive disorders
US6156749A (en) * 1997-12-01 2000-12-05 Merck Sharp & Dohme Limited Use of NK-1 receptor antagonists for treating movement disorders
GB9810920D0 (en) * 1998-05-21 1998-07-22 Merck Sharp & Dohme Therapeutic use
GB9816897D0 (en) * 1998-08-04 1998-09-30 Merck Sharp & Dohme Therapeutic use
GB9819888D0 (en) * 1998-09-11 1998-11-04 Merck Sharp & Dohme Chemical synthesis
US6218390B1 (en) * 1998-12-17 2001-04-17 Synaptic Pharmaceutical Corporation Morpholinone and morpholine derivatives and uses thereof
DE60013942T2 (de) * 1999-03-30 2006-02-23 Pfizer Products Inc., Groton Verfahren zur Herstellung von cyclischen Thioamiden
US7163949B1 (en) 1999-11-03 2007-01-16 Amr Technology, Inc. 4-phenyl substituted tetrahydroisoquinolines and use thereof
PT1246806E (pt) 1999-11-03 2008-04-03 Amr Technology Inc Tetra-hidroisoquinolinas aril- e heteroaril-substituídas e sua utilização no bloqueio da recaptação de norepinefrina, dopamina e serotonina.
SI1103545T1 (en) * 1999-11-29 2004-02-29 F. Hoffmann-La Roche Ag 2-(3,5-Bis-trifluoromethyl-phenyl)-N-methyl-N-(6-morpholin-4-yl-4-o-tolyl-pyridin-3-yl)-isobutyramide
CN100430401C (zh) 2000-07-11 2008-11-05 Amr科技公司 新的4-苯基取代的四氢异喹啉类化合物及其治疗用途
GB0022988D0 (en) * 2000-09-19 2000-11-01 Merck Sharp & Dohme Therapeutic agents
DE10116978A1 (de) * 2001-04-05 2002-10-10 Merck Patent Gmbh Kappa-Opiatagonisten für die Behandlung von Erkrankungen der Blase
US20030083345A1 (en) * 2001-07-10 2003-05-01 Torsten Hoffmann Method of treatment and/or prevention of brain, spinal or nerve injury
US6638981B2 (en) 2001-08-17 2003-10-28 Epicept Corporation Topical compositions and methods for treating pain
CA2501938A1 (en) * 2002-10-11 2004-04-22 Cytokinetics, Inc. Compounds, compositions, and methods
ATE533745T1 (de) 2004-03-17 2011-12-15 Pfizer Prod Inc Neue benzyl(iden)-lactam-derivate
US7541357B2 (en) 2004-07-15 2009-06-02 Amr Technology, Inc. Aryl- and heteroaryl-substituted tetrahydroisoquinolines and use thereof to block reuptake of norepinephrine, dopamine, and serotonin
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
EP1904069B1 (en) 2005-07-15 2018-06-13 Albany Molecular Research, Inc. Aryl-and heteroaryl-substituted tetrahydrobenzazepines and use thereof to block reuptake of norepinephrine, dopamine, and serotonin
WO2007041052A2 (en) 2005-09-29 2007-04-12 Merck & Co., Inc. Acylated spiropiperidine derivatives as melanocortin-4 receptor modulators
GB0603041D0 (en) 2006-02-15 2006-03-29 Angeletti P Ist Richerche Bio Therapeutic compounds
EP2083831B1 (en) 2006-09-22 2013-12-25 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
DK2805945T3 (da) 2007-01-10 2019-07-15 Msd Italia Srl Amid-substituerede indazoler som poly(adp-ribose)polymerase- (parp) hæmmere
EP2117538A1 (en) 2007-01-24 2009-11-18 Glaxo Group Limited Pharmaceutical compositions comprising 2-methoxy-5- (5-trifluoromethyl-tetrazol-i-yl-benzyl) - (2s-phenyl-piperidin-3s-yl-)
JP5319518B2 (ja) 2007-04-02 2013-10-16 Msd株式会社 インドールジオン誘導体
WO2008130616A2 (en) * 2007-04-19 2008-10-30 Schering Corporation Diaryl morpholines as cb1 modulators
EP3103791B1 (en) 2007-06-27 2018-01-31 Merck Sharp & Dohme Corp. 4-carboxybenzylamino derivatives as histone deacetylase inhibitors
EP2254420A4 (en) 2008-02-20 2012-02-15 Targia Pharmaceuticals CNS PHARMACEUTICALS AND METHOD FOR THEIR USE
CA2717509A1 (en) 2008-03-03 2009-09-11 Tiger Pharmatech Tyrosine kinase inhibitors
WO2009124756A1 (en) * 2008-04-08 2009-10-15 European Molecular Biology Laboratory (Embl) Use of aprepitant and derivatives thereof for the treatment of cancer
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
AR071997A1 (es) 2008-06-04 2010-07-28 Bristol Myers Squibb Co Forma cristalina de 6-((4s)-2-metil-4-(2-naftil)-1,2,3,4-tetrahidroisoquinolin-7-il)piridazin-3-amina
WO2010114780A1 (en) 2009-04-01 2010-10-07 Merck Sharp & Dohme Corp. Inhibitors of akt activity
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
CA2760837C (en) 2009-05-12 2018-04-03 Albany Molecular Research, Inc. 7-([1,2,4]triazolo[1,5-.alpha.]pyridin-6-yl)-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydroisoquinoline and use thereof
ES2446971T3 (es) 2009-05-12 2014-03-11 Albany Molecular Research, Inc. Tetrahidroisoquinolinas sustituidas con arilo, heteroarilo, y heterociclo y su uso
PH12012500713A1 (en) 2009-10-14 2012-11-26 Merck Sharp & Dohme Substituted piperidines that increase p53 activity and the uses thereof
EP2584903B1 (en) 2010-06-24 2018-10-24 Merck Sharp & Dohme Corp. Novel heterocyclic compounds as erk inhibitors
US8518907B2 (en) 2010-08-02 2013-08-27 Merck Sharp & Dohme Corp. RNA interference mediated inhibition of catenin (cadherin-associated protein), beta 1 (CTNNB1) gene expression using short interfering nucleic acid (siNA)
RU2624045C2 (ru) 2010-08-17 2017-06-30 Сирна Терапьютикс,Инк ОПОСРЕДУЕМОЕ РНК-ИНТЕРФЕРЕНЦИЕЙ ИНГИБИРОВАНИЕ ЭКСПРЕССИИ ГЕНОВ ВИРУСА ГЕПАТИТА B (HBV) С ПРИМЕНЕНИЕМ МАЛОЙ ИНТЕРФЕРИРУЮЩЕЙ НУКЛЕИНОВОЙ КИСЛОТЫ (миНК)
EP2608669B1 (en) 2010-08-23 2016-06-22 Merck Sharp & Dohme Corp. NOVEL PYRAZOLO[1,5-a]PYRIMIDINE DERIVATIVES AS mTOR INHIBITORS
WO2012030685A2 (en) 2010-09-01 2012-03-08 Schering Corporation Indazole derivatives useful as erk inhibitors
US9242981B2 (en) 2010-09-16 2016-01-26 Merck Sharp & Dohme Corp. Fused pyrazole derivatives as novel ERK inhibitors
EP3327125B1 (en) 2010-10-29 2020-08-05 Sirna Therapeutics, Inc. Rna interference mediated inhibition of gene expression using short interfering nucleic acids (sina)
EP2654748B1 (en) 2010-12-21 2016-07-27 Merck Sharp & Dohme Corp. Indazole derivatives useful as erk inhibitors
JP2014514321A (ja) 2011-04-21 2014-06-19 メルク・シャープ・アンド・ドーム・コーポレーション インスリン様増殖因子1受容体阻害剤
WO2013063214A1 (en) 2011-10-27 2013-05-02 Merck Sharp & Dohme Corp. Novel compounds that are erk inhibitors
EP3358013B1 (en) 2012-05-02 2020-06-24 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
ME02925B (me) 2012-11-28 2018-04-20 Merck Sharp & Dohme Kompozicije i postupci za liječenje kancera
CA2895504A1 (en) 2012-12-20 2014-06-26 Merck Sharp & Dohme Corp. Substituted imidazopyridines as hdm2 inhibitors
WO2014120748A1 (en) 2013-01-30 2014-08-07 Merck Sharp & Dohme Corp. 2,6,7,8 substituted purines as hdm2 inhibitors
US20160194368A1 (en) 2013-09-03 2016-07-07 Moderna Therapeutics, Inc. Circular polynucleotides
WO2018071283A1 (en) 2016-10-12 2018-04-19 Merck Sharp & Dohme Corp. Kdm5 inhibitors
WO2019094311A1 (en) 2017-11-08 2019-05-16 Merck Sharp & Dohme Corp. Prmt5 inhibitors
US11098059B2 (en) 2017-11-08 2021-08-24 Merck Sharp & Dohme Corp. PRMT5 inhibitors
EP3833667B1 (en) 2018-08-07 2024-03-13 Merck Sharp & Dohme LLC Prmt5 inhibitors
AU2019317549A1 (en) 2018-08-07 2021-02-25 Msd International Gmbh PRMT5 inhibitors
EP3833668B1 (en) 2018-08-07 2025-03-19 Merck Sharp & Dohme LLC Prmt5 inhibitors
CA3173697A1 (en) 2020-04-03 2021-10-07 Mike TROWER An nk-1 receptor antagonist for treating a disease selecting from sepsis, septic shock, acute respiratory distress syndrome (ards) or multiple organ dysfunction syndrome (mods)
AU2021285503A1 (en) 2020-06-02 2022-12-08 Nerre Therapeutics Limited Neurokinin (NK)-1 receptor antagonists for use in the treatment of pulmonary fibrosis conditions promoted by mechanical injury to the lungs
CN115650969B (zh) * 2022-10-29 2024-10-01 河南师范大学 一种α-取代-β-胺氧基取代吗啉类化合物的合成方法

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4476311A (en) * 1980-03-12 1984-10-09 The Purdue Frederick Company Analgesic 4-carboxy-pyrrolidin-2-one compound
JPS5739599A (en) * 1980-08-20 1982-03-04 Fuji Machine Mfg Method and device for automatically mounting leadless electronic part on printed board or like
FR2534915B1 (fr) * 1982-10-26 1985-10-25 Lafon Labor Nouveaux derives de 2-(phenoxymethyl)-morpholine, utilisation en therapeutique et procede de preparation
UA41251C2 (uk) * 1990-01-04 2001-09-17 Пфайзер, Інк. Гідровані азотвмісні гетероциклічні сполуки, похідні піперидину, фармацевтична композиція та спосіб пригнічення активності речовини р в організмі
EP0528495A1 (en) * 1991-08-20 1993-02-24 Merck Sharp & Dohme Ltd. Azacyclic compounds, processes for their preparation and pharmaceutical compositions containing them

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