LTC0734381I2 - Morfolino ir tiomorfolino receptoriaus antagonistai - Google Patents

Morfolino ir tiomorfolino receptoriaus antagonistai

Info

Publication number
LTC0734381I2
LTC0734381I2 LTPA2004002C LTPA2004002C LTC0734381I2 LT C0734381 I2 LTC0734381 I2 LT C0734381I2 LT PA2004002 C LTPA2004002 C LT PA2004002C LT PA2004002 C LTPA2004002 C LT PA2004002C LT C0734381 I2 LTC0734381 I2 LT C0734381I2
Authority
LT
Lithuania
Prior art keywords
substituted
group
receptor antagonists
thiomorpholine
morpholine
Prior art date
Application number
LTPA2004002C
Other languages
English (en)
Lithuanian (lt)
Original Assignee
Merck Sharp & Dohme Corp.
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=22617632&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=LTC0734381(I2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Merck Sharp & Dohme Corp. filed Critical Merck Sharp & Dohme Corp.
Publication of LTPA2004002I1 publication Critical patent/LTPA2004002I1/lt
Publication of LTC0734381I2 publication Critical patent/LTC0734381I2/lt

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/28—1,4-Oxazines; Hydrogenated 1,4-oxazines
    • C07D265/30—1,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/06—Antimigraine agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/08—Antiepileptics; Anticonvulsants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/22—Anxiolytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/08—Vasodilators for multiple indications
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/28—1,4-Oxazines; Hydrogenated 1,4-oxazines
    • C07D265/30—1,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings
    • C07D265/32—1,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings with oxygen atoms directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D279/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one sulfur atom as the only ring hetero atoms
    • C07D279/10—1,4-Thiazines; Hydrogenated 1,4-thiazines
    • C07D279/12—1,4-Thiazines; Hydrogenated 1,4-thiazines not condensed with other rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic 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
    • C07D413/04—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic 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
    • C07D413/06—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic 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

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Pain & Pain Management (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pulmonology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Otolaryngology (AREA)
  • Vascular Medicine (AREA)
  • Rheumatology (AREA)
  • Immunology (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)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Peptides Or Proteins (AREA)
LTPA2004002C 1993-12-17 2004-05-07 Morfolino ir tiomorfolino receptoriaus antagonistai LTC0734381I2 (lt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US16988993A 1993-12-17 1993-12-17
PCT/US1994/014497 WO1995016679A1 (en) 1993-12-17 1994-12-13 Morpholine and thiomorpholine tachykinin receptor antagonists

Publications (2)

Publication Number Publication Date
LTPA2004002I1 LTPA2004002I1 (lt) 2016-11-10
LTC0734381I2 true LTC0734381I2 (lt) 2017-04-25

Family

ID=22617632

Family Applications (1)

Application Number Title Priority Date Filing Date
LTPA2004002C LTC0734381I2 (lt) 1993-12-17 2004-05-07 Morfolino ir tiomorfolino receptoriaus antagonistai

Country Status (40)

Country Link
EP (1) EP0734381B1 (cg-RX-API-DMAC7.html)
JP (1) JP3245424B2 (cg-RX-API-DMAC7.html)
KR (1) KR100335704B1 (cg-RX-API-DMAC7.html)
CN (1) CN1057296C (cg-RX-API-DMAC7.html)
AT (1) ATE194336T1 (cg-RX-API-DMAC7.html)
AU (1) AU701862B2 (cg-RX-API-DMAC7.html)
BG (1) BG64775B1 (cg-RX-API-DMAC7.html)
BR (1) BR9408351A (cg-RX-API-DMAC7.html)
CA (1) CA2178949C (cg-RX-API-DMAC7.html)
CO (1) CO4340628A1 (cg-RX-API-DMAC7.html)
CY (2) CY2203B1 (cg-RX-API-DMAC7.html)
CZ (1) CZ295381B6 (cg-RX-API-DMAC7.html)
DE (2) DE122004000019I1 (cg-RX-API-DMAC7.html)
DK (1) DK0734381T3 (cg-RX-API-DMAC7.html)
ES (1) ES2147840T3 (cg-RX-API-DMAC7.html)
FI (1) FI109532B (cg-RX-API-DMAC7.html)
FR (1) FR04C0010I2 (cg-RX-API-DMAC7.html)
GR (1) GR3034095T3 (cg-RX-API-DMAC7.html)
HR (1) HRP941000B9 (cg-RX-API-DMAC7.html)
HU (1) HU224014B1 (cg-RX-API-DMAC7.html)
IL (1) IL111960A (cg-RX-API-DMAC7.html)
LT (1) LTC0734381I2 (cg-RX-API-DMAC7.html)
LU (1) LU91069I9 (cg-RX-API-DMAC7.html)
LV (1) LV11617B (cg-RX-API-DMAC7.html)
MY (1) MY115164A (cg-RX-API-DMAC7.html)
NL (1) NL300146I2 (cg-RX-API-DMAC7.html)
NO (3) NO308742B1 (cg-RX-API-DMAC7.html)
NZ (1) NZ278222A (cg-RX-API-DMAC7.html)
PL (1) PL182521B1 (cg-RX-API-DMAC7.html)
PT (1) PT734381E (cg-RX-API-DMAC7.html)
RO (1) RO118203B1 (cg-RX-API-DMAC7.html)
RU (1) RU2201924C2 (cg-RX-API-DMAC7.html)
SA (1) SA95150523B1 (cg-RX-API-DMAC7.html)
SI (1) SI0734381T1 (cg-RX-API-DMAC7.html)
SK (1) SK282800B6 (cg-RX-API-DMAC7.html)
TW (1) TW419471B (cg-RX-API-DMAC7.html)
UA (1) UA47397C2 (cg-RX-API-DMAC7.html)
WO (1) WO1995016679A1 (cg-RX-API-DMAC7.html)
YU (1) YU49037B (cg-RX-API-DMAC7.html)
ZA (1) ZA9410008B (cg-RX-API-DMAC7.html)

Families Citing this family (109)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1995018124A1 (en) * 1993-12-29 1995-07-06 Merck Sharp & Dohme Limited Substituted morpholine derivatives and their use as therapeutic agents
IL112778A0 (en) * 1994-03-04 1995-05-26 Merck & Co Inc Substituted heterocycles, their preparation and pharmaceutical compositions containing them
WO1995030674A1 (en) * 1994-05-05 1995-11-16 Merck Sharp & Dohme Limited Morpholine derivatives and their use as antagonists of tachikinins
US5824678A (en) * 1994-08-15 1998-10-20 Merck Sharp & Dohme Ltd. Morpholine derivatives and their use as therapeutic agents
GB9417956D0 (en) * 1994-09-02 1994-10-26 Merck Sharp & Dohme Therapeutic agents
GB9505491D0 (en) * 1995-03-18 1995-05-03 Merck Sharp & Dohme Therapeutic agents
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
GB9523244D0 (en) * 1995-11-14 1996-01-17 Merck Sharp & Dohme Therapeutic agents
US5750549A (en) * 1996-10-15 1998-05-12 Merck & Co., Inc. Cycloalkyl tachykinin receptor antagonists
ZA985765B (en) 1997-07-02 1999-08-04 Merck & Co Inc Polymorphic form of a tachykinin receptor antagonist.
SK285644B6 (sk) * 1997-07-02 2007-05-03 Merck & Co., Inc. Polymorfná forma zlúčeniny 2-(R)-(1-(R)-(3,5-bis(trifluórmetyl)- fenyl)etoxy)-3-(S)-(4-fluór)fenyl-4-(3-(5-oxo-1H,4H-1,2,4- triazolo)metyl)morfolínu,spôsob jej prípravy, farmaceutický prostriedok s jej obsahom a jej použitie
GB9813025D0 (en) 1998-06-16 1998-08-12 Merck Sharp & Dohme Chemical synthesis
SI1035115T1 (en) 1999-02-24 2005-02-28 F. Hoffmann-La Roche Ag 4-Phenylpyridine derivatives and their use as NK-1 receptor antagonists
CN1131212C (zh) * 1999-02-24 2003-12-17 弗·哈夫曼-拉罗切有限公司 苯基－和吡啶基衍生物
HRP20010604A2 (en) 1999-02-24 2002-08-31 Hoffmann La Roche 3-phenylpyridine derivatives and their use as nk-1 receptor antagonists
US6291465B1 (en) 1999-03-09 2001-09-18 Hoffmann-La Roche Inc. Biphenyl derivatives
CN1414953A (zh) 1999-11-03 2003-04-30 阿尔巴尼分子研究公司 芳基和杂芳基取代的四氢异喹啉及其阻断去甲肾上腺素、多巴胺和5－羟色胺重摄取的用途
US7163949B1 (en) 1999-11-03 2007-01-16 Amr Technology, Inc. 4-phenyl substituted tetrahydroisoquinolines and use thereof
EP1103545B1 (en) * 1999-11-29 2003-11-05 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
US6452001B2 (en) 2000-05-25 2002-09-17 Hoffmann-La Roche Inc. Diazapane derivatives useful as antagonists of neurokinin 1 receptor and methods for their formation
AR030284A1 (es) 2000-06-08 2003-08-20 Merck & Co Inc Proceso para la sintesis de (2r, 2-alfa-r,3a) -2-[1-(3,5-bis(trifluorometil) fenil) etoxi]-3-(4-fluorofenil)-1,4-oxazina; dicho compuesto y sus formas polimorficas
US6482829B2 (en) 2000-06-08 2002-11-19 Hoffmann-La Roche Inc. Substituted heterocyclic siprodecane compound active as an antagonist of neurokinin 1 receptor
CA2415532C (en) 2000-07-11 2010-05-11 Albany Molecular Research, Inc. Novel 4-phenyl substituted tetrahydroisoquinolines therapeutic use thereof
CZ303639B6 (cs) 2000-07-14 2013-01-23 F. Hoffmann-La Roche Ag N-Oxid derivátu 4-fenylpyridinu, zpusob jeho prípravy a lécivo s jeho obsahem
TWI287003B (en) 2000-07-24 2007-09-21 Hoffmann La Roche 4-phenyl-pyridine derivatives
TWI259180B (en) 2000-08-08 2006-08-01 Hoffmann La Roche 4-Phenyl-pyridine derivatives
YU39503A (sh) 2000-11-22 2006-05-25 F. Hoffmann-La Roche Ag. Derivati pirimidina
US6642226B2 (en) 2001-02-06 2003-11-04 Hoffman-La Roche Inc. Substituted phenyl-piperidine methanone compounds
CA2447329C (en) * 2001-05-14 2009-07-28 F.Hoffmann-La Roche Ag 1-oxa-3,9-diaza-spiro[5,5]undecan-2-ones derivatives and its use as antagonist of the neurikinin receptor
US6849624B2 (en) 2001-07-31 2005-02-01 Hoffmann-La Roche Inc. Aromatic and heteroaromatic substituted amides
US6638981B2 (en) 2001-08-17 2003-10-28 Epicept Corporation Topical compositions and methods for treating pain
PT1451166E (pt) * 2001-12-07 2005-11-30 Pfizer Prod Inc Sal de acido citrico de um composto terapeutico e composicoes farmaceuticas associadas
UA76810C2 (uk) * 2001-12-10 2006-09-15 Мерк Енд Ко., Інк. Фармацевтична композиція антагоніста рецептора тахікініну у формі наночастинок
AR039625A1 (es) * 2002-04-18 2005-03-02 Merck & Co Inc Proceso para la preparacion de 5-((2(r)--(1(r)- (3,5-bis (trifluormetil) fenil)etoxi-3 (s) - (4-fluorfenil) -4-morfolinil) metil) -1,2-dihidro-3h-1,2,4-triazol-3-ona
KR100700421B1 (ko) 2003-01-31 2007-03-28 에프. 호프만-라 로슈 아게 2-(3,5-비스-트라이플루오로메틸-페닐)-Ｎ-[6-(1,1-다이옥소-1λ6-티오모폴린-4-일)-4-(4-플루오로-2-메틸-페닐)-피리딘-3-일]-Ｎ-메틸-아이소부티르아미드의 새로운 결정변형체
GB0310881D0 (en) * 2003-05-12 2003-06-18 Merck Sharp & Dohme Pharmaceutical formulation
KR100744859B1 (ko) 2003-07-03 2007-08-01 에프. 호프만-라 로슈 아게 정신분열증 치료를 위한 이중 ｎｋ1/ｎｋ3 길항물질
US7288658B2 (en) 2003-07-15 2007-10-30 Hoffmann-La Roche Inc. Process for preparation of pyridine derivatives
ES2246687B2 (es) 2004-02-11 2006-11-16 Miguel Muñoz Saez Utilizacion de antagonistas no peptidicos de receptores nk1 para la produccion de apoptosis en celulas tumorales.
CN101119969B (zh) 2004-07-15 2014-04-09 阿尔巴尼分子研究公司 芳基和杂芳基取代的四氢异喹啉及其阻断去甲肾上腺素、多巴胺和血清素的重摄取的应用
EP1856052B1 (en) 2005-02-22 2009-09-02 F.Hoffmann-La Roche Ag Nk1 antagonists
PL1863767T3 (pl) 2005-03-23 2009-08-31 Helsinn Healthcare Sa Metabolity antagonistów NK-1 do leczenia wymiotów
ATE550019T1 (de) 2005-05-17 2012-04-15 Merck Sharp & Dohme Cis-4-ä(4-chlorophenyl)sulfonylü-4-(2,5- difluorophenyl)cyclohexanepropansäure zur behandlug von krebs
US7956050B2 (en) 2005-07-15 2011-06-07 Albany Molecular Research, Inc. Aryl- and heteroaryl-substituted tetrahydrobenzazepines and use thereof to block reuptake of norepinephrine, dopamine, and serotonin
SI1928427T1 (sl) 2005-09-23 2010-03-31 Hoffmann La Roche Nove formulacije za doziranje
AU2006297443B2 (en) 2005-09-29 2010-08-12 Merck Sharp & Dohme Corp. Acylated spiropiperidine derivatives as melanocortin-4 receptor modulators
EP1942734A4 (en) 2005-10-06 2010-04-07 Reddys Lab Ltd Dr PREPARATION OF THE APREPITANT
US9227958B2 (en) * 2006-02-03 2016-01-05 Glenmark Pharmaceuticals Limited Amorphous and crystalline forms of aprepitant and processes for the preparation thereof
GB0603041D0 (en) 2006-02-15 2006-03-29 Angeletti P Ist Richerche Bio Therapeutic compounds
WO2008026216A2 (en) * 2006-08-28 2008-03-06 Hetero Drugs Limited Process for purification of aprepitant
CA2770486C (en) 2006-09-22 2014-07-15 Merck Sharp & Dohme Corp. Use of platencin and platensimycin as fatty acid synthesis inhibitors to treat obesity, diabetes and cancer
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
CN101190330A (zh) 2006-11-30 2008-06-04 深圳市鼎兴生物医药技术开发有限公司 胆碱酯酶在拮抗速激肽药物中的应用
PL2805945T3 (pl) 2007-01-10 2019-09-30 Msd Italia S.R.L. Indazole podstawione grupą amidową jako inhibitory polimerazy poli(adp-rybozy) - (parp)
CN101641099A (zh) 2007-01-24 2010-02-03 葛兰素集团有限公司 包含3,5-二氨基-6-(2,3-二氯苯基)-1,2,4-三嗪或r(-)-2,4-二氨基-5-(2,3-二氯苯基)-6-氟甲基嘧啶和nk1的药物组合物
JP5319518B2 (ja) 2007-04-02 2013-10-16 Ｍｓｄ株式会社 インドールジオン誘導体
BRPI0810402A2 (pt) 2007-04-20 2014-11-04 Hoffmann La Roche Derivados de pirrolidina como antagonistas duais dos receptores nk1/nk3
WO2009002495A1 (en) 2007-06-27 2008-12-31 Merck & Co., Inc. 4-carboxybenzylamino derivatives as histone deacetylase inhibitors
WO2009019163A1 (en) 2007-08-07 2009-02-12 F. Hoffmann-La Roche Ag Pyrrolidine aryl-ether as nk3 receptor antagonists
WO2009104080A2 (en) 2008-02-20 2009-08-27 Targia Pharmaceuticals Cns pharmaceutical compositions and methods of use
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
BRPI0923815A2 (pt) 2008-12-23 2015-07-14 Pharmasset Inc Síntese de nucleosídeos de purina
EA019341B1 (ru) 2008-12-23 2014-02-28 Джилид Фармассет, Ллс. Фосфорамидаты нуклеозидов
EP2376514A2 (en) 2008-12-23 2011-10-19 Pharmasset, Inc. Nucleoside analogs
EP2413932A4 (en) 2009-04-01 2012-09-19 Merck Sharp & Dohme HAMMER OF ACT ACTIVITY
JP5764553B2 (ja) 2009-05-12 2015-08-19 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 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およびその使用
JP2012526823A (ja) 2009-05-12 2012-11-01 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、ヘテロアリール、および複素環置換テトラヒドロイソキノリンならびにそれらの使用
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
EP2488028B1 (en) 2009-10-14 2020-08-19 Merck Sharp & Dohme Corp. Substituted piperidines that increase p53 activity and the uses thereof
LT2609923T (lt) 2010-03-31 2017-09-11 Gilead Pharmasset Llc (s)-izopropilo 2-(((s)-(perfluorfenoksi)(fenoksi)fosforil)amino)-propanoato kristalinimo būdas
US8487102B2 (en) 2010-04-20 2013-07-16 Hoffmann-La Roche Inc. Pyrrazolopyridine compounds as dual NK1/NK3 receptor antagonists
EP2584903B1 (en) 2010-06-24 2018-10-24 Merck Sharp & Dohme Corp. Novel heterocyclic compounds as erk inhibitors
WO2012018754A2 (en) 2010-08-02 2012-02-09 Merck Sharp & Dohme Corp. RNA INTERFERENCE MEDIATED INHIBITION OF CATENIN (CADHERIN-ASSOCIATED PROTEIN), BETA 1 (CTNNB1) GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACID (siNA)
ES2376564B1 (es) 2010-08-12 2013-01-24 Manuel Vicente Salinas Martín Utilización de anticuerpos contra los receptores nk1, nk2 y/o nk3, para producir apoptosis en las células tumorales y modificar el estroma, la inmunidad y la vascularización intra y peritumorales, como tratamiento del cáncer.
HUE044815T2 (hu) 2010-08-17 2019-11-28 Sirna Therapeutics Inc Hepatitisz B vírus (HBV) génexpressziójának RNS-interferencia közvetített gátlása, rövid interferáló nukleinsav (SINS) alkalmazásával
US8883801B2 (en) 2010-08-23 2014-11-11 Merck Sharp & Dohme Corp. Substituted pyrazolo[1,5-a]pyrimidines as mTOR inhibitors
US8946216B2 (en) 2010-09-01 2015-02-03 Merck Sharp & Dohme Corp. 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
KR101833578B1 (ko) 2010-09-23 2018-02-28 누포믹스 리미티드 아프레피탄트 l-프롤린 조성물 및 공결정
US9260471B2 (en) 2010-10-29 2016-02-16 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
EP2699568A1 (en) 2011-04-21 2014-02-26 Piramal Enterprises Limited A crystalline form of a salt of a morpholino sulfonyl indole derivative and a process for its preparation
WO2012146692A1 (en) 2011-04-29 2012-11-01 Sandoz Ag Novel intermediates for the preparation of highly pure aprepitant or fosaprepitant
EP2770987B1 (en) 2011-10-27 2018-04-04 Merck Sharp & Dohme Corp. Novel compounds that are erk inhibitors
US9532993B2 (en) 2011-11-25 2017-01-03 Nuformix Limited Aprepitant L-proline solvates—compositions and cocrystals
EP2837381A4 (en) 2011-12-13 2015-12-09 Servicio Andaluz De Salud USE OF MEDICAMENTS FOR THE TREATMENT OF CANCER THAT CHANGE THE PERITUMORAL ENVIRONMENT
CZ304770B6 (cs) 2012-03-13 2014-10-08 Zentiva, K.S. Způsob výroby 3-(((2R,3S)-2-((R)-1-(3,5-bis(trifluormethyl)fenyl)ethoxy)-3-(4-fluorfenyl)morfolino)methyl)-1H-1,2,4-triazol-5(4H)-onu (Aprepitantu) v polymorfní formě II
WO2013165816A2 (en) 2012-05-02 2013-11-07 Merck Sharp & Dohme Corp. 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
PL2925888T3 (pl) 2012-11-28 2018-03-30 Merck Sharp & Dohme Corp. Kompozycje i sposoby do stosowania w leczeniu nowotworów
RU2690663C2 (ru) 2012-12-20 2019-06-05 Мерк Шарп И Доум Корп. Замещенные имидазопиридины в качестве ингибиторов hdm2
US9540377B2 (en) 2013-01-30 2017-01-10 Merck Sharp & Dohme Corp. 2,6,7,8 substituted purines as HDM2 inhibitors
ES2493693B1 (es) 2013-02-11 2015-07-07 Servicio Andaluz De Salud Método para predecir o pronosticar la respuesta de un sujeto humano que padece un cáncer al tratamiento con un antagonista del receptor NK1
EP3041938A1 (en) 2013-09-03 2016-07-13 Moderna Therapeutics, Inc. Circular polynucleotides
CN103694146B (zh) * 2013-12-04 2015-10-28 深圳万乐药业有限公司 2-(2-氯-1-亚乙基)酰肼甲酸甲酯的制备方法
ES2541870B1 (es) 2013-12-27 2016-05-12 Servicio Andaluz De Salud Uso de antagonistas no peptídicos de NK1 en una determinada dosis para el tratamiento del cáncer
TW201613888A (en) 2014-09-26 2016-04-16 Helsinn Healthcare Sa Crystalline forms of an NK-1 antagonist
US10005803B2 (en) 2015-10-06 2018-06-26 Helsinn Healthcare Sa Crystalline forms of fosnetupitant
EA036605B1 (ru) 2016-06-06 2020-11-27 Хелсинн Хелскеа Са Физиологически сбалансированный состав для инъекций, включающий фоснетупитант
WO2018071283A1 (en) 2016-10-12 2018-04-19 Merck Sharp & Dohme Corp. Kdm5 inhibitors
WO2019094312A1 (en) 2017-11-08 2019-05-16 Merck Sharp & Dohme Corp. Prmt5 inhibitors
US10947234B2 (en) 2017-11-08 2021-03-16 Merck Sharp & Dohme Corp. PRMT5 inhibitors
AU2019317549A1 (en) 2018-08-07 2021-02-25 Msd International Gmbh PRMT5 inhibitors
EP3833667B1 (en) 2018-08-07 2024-03-13 Merck Sharp & Dohme LLC Prmt5 inhibitors
WO2020033282A1 (en) 2018-08-07 2020-02-13 Merck Sharp & Dohme Corp. Prmt5 inhibitors
KR20220165251A (ko) 2020-04-03 2022-12-14 네르 쎄라퓨틱스 리미티드 패혈증, 패혈성 쇼크, 급성 호흡 곤란 증후군 (ards) 또는 다발성 기관 기능장애 증후군 (mods)으로부터 선택된 질환을 치료하기 위한 nk-1 수용체 길항제
CA3177477A1 (en) 2020-06-02 2021-12-09 Nerre Therapeutics Limited Neurokinin (nk)-1 receptor antagonists for use in the treatment of pulmonary fibrosis conditions promoted by mechanical injury to the lungs

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2534915B1 (fr) * 1982-10-26 1985-10-25 Lafon Labor Nouveaux derives de 2-(phenoxymethyl)-morpholine, utilisation en therapeutique et procede de preparation
JPH06510034A (ja) * 1991-08-20 1994-11-10 メルク　シヤープ　エンド　ドーム　リミテツド アザ環式化合物、それらの製造方法、及びそれらを含む医薬組成物
CA2099233A1 (en) * 1992-06-29 1993-12-30 Conrad P. Dorn Morpholine and thiomorpholine 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

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