YU49037B - Morfolin antagonisti receptora tahikinina - Google Patents

Morfolin antagonisti receptora tahikinina

Info

Publication number
YU49037B
YU49037B YU74694A YU74694A YU49037B YU 49037 B YU49037 B YU 49037B YU 74694 A YU74694 A YU 74694A YU 74694 A YU74694 A YU 74694A YU 49037 B YU49037 B YU 49037B
Authority
YU
Yugoslavia
Prior art keywords
previously defined
phenyl
halo
alkoxy
unsubstituted
Prior art date
Application number
YU74694A
Other languages
English (en)
Serbo-Croatian (sh)
Other versions
YU74694A (sh
Inventor
Conrad P. Dorn
Paul E. Finke
Jeffrey J. Hale
Malcolm Mac Coss
Sander G. Mills
Shrenik K. Shah
Mark Stuart Chambers
Timothy Harrison
Tamara Ladduwahetty
Brian John Harlow Williams
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
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=YU49037(B) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Merck & Co. Inc. filed Critical Merck & Co. Inc.
Publication of YU74694A publication Critical patent/YU74694A/sh
Publication of YU49037B publication Critical patent/YU49037B/sh

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
    • 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
    • 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
    • A61P25/02Drugs for disorders of the nervous system for peripheral neuropathies
    • 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
    • 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
    • A61P25/22Anxiolytics
    • 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
    • A61P25/28Drugs 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
    • 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
    • A61P37/00Drugs for immunological or allergic disorders
    • 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
    • A61P9/08Vasodilators for multiple indications
    • 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

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Pain & Pain Management (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pulmonology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Immunology (AREA)
  • Urology & Nephrology (AREA)
  • Rheumatology (AREA)
  • Vascular Medicine (AREA)
  • Otolaryngology (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)
YU74694A 1993-12-17 1994-12-16 Morfolin antagonisti receptora tahikinina YU49037B (sh)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US16988993A 1993-12-17 1993-12-17

Publications (2)

Publication Number Publication Date
YU74694A YU74694A (sh) 1997-08-22
YU49037B true YU49037B (sh) 2003-07-07

Family

ID=22617632

Family Applications (1)

Application Number Title Priority Date Filing Date
YU74694A YU49037B (sh) 1993-12-17 1994-12-16 Morfolin antagonisti receptora tahikinina

Country Status (40)

Country Link
EP (1) EP0734381B1 (enExample)
JP (1) JP3245424B2 (enExample)
KR (1) KR100335704B1 (enExample)
CN (1) CN1057296C (enExample)
AT (1) ATE194336T1 (enExample)
AU (1) AU701862B2 (enExample)
BG (1) BG64775B1 (enExample)
BR (1) BR9408351A (enExample)
CA (1) CA2178949C (enExample)
CO (1) CO4340628A1 (enExample)
CY (2) CY2203B1 (enExample)
CZ (1) CZ295381B6 (enExample)
DE (2) DE69425161T2 (enExample)
DK (1) DK0734381T3 (enExample)
ES (1) ES2147840T3 (enExample)
FI (1) FI109532B (enExample)
FR (1) FR04C0010I2 (enExample)
GR (1) GR3034095T3 (enExample)
HR (1) HRP941000B9 (enExample)
HU (1) HU224014B1 (enExample)
IL (1) IL111960A (enExample)
LT (1) LTC0734381I2 (enExample)
LU (1) LU91069I9 (enExample)
LV (1) LV11617B (enExample)
MY (1) MY115164A (enExample)
NL (1) NL300146I2 (enExample)
NO (3) NO308742B1 (enExample)
NZ (1) NZ278222A (enExample)
PL (1) PL182521B1 (enExample)
PT (1) PT734381E (enExample)
RO (1) RO118203B1 (enExample)
RU (1) RU2201924C2 (enExample)
SA (1) SA95150523B1 (enExample)
SI (1) SI0734381T1 (enExample)
SK (1) SK282800B6 (enExample)
TW (1) TW419471B (enExample)
UA (1) UA47397C2 (enExample)
WO (1) WO1995016679A1 (enExample)
YU (1) YU49037B (enExample)
ZA (1) ZA9410008B (enExample)

Families Citing this family (109)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE69428913T2 (de) * 1993-12-29 2002-05-29 Merck Sharp & Dohme Ltd., Hoddesdon Substituierte morpholinderivate und ihre verwendung als arzneimittel
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
WO1996005181A1 (en) * 1994-08-15 1996-02-22 Merck Sharp & Dohme Limited 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
DE69838421D1 (en) * 1997-07-02 2007-10-25 Merck & Co Inc Polymorphe form des tachykininrezeptorantagonisten 2-(r)-(1-(r)-(3,5-bis(trifluormethyl)phenyl)ethoxy)-3-(s)-(4-fluor)phenyl-4-(3-5-oxo-1h,4h-1,2,4-triazolo)methylmorpholin
ZA985765B (en) 1997-07-02 1999-08-04 Merck & Co Inc Polymorphic form of a tachykinin receptor antagonist.
GB9813025D0 (en) * 1998-06-16 1998-08-12 Merck Sharp & Dohme Chemical synthesis
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
CN1134417C (zh) 1999-02-24 2004-01-14 弗·哈夫曼-拉罗切有限公司 3-苯基吡啶衍生物及其作为nk-1受体拮抗剂的应用
DE60045564D1 (de) 1999-02-24 2011-03-03 Hoffmann La Roche 4-Phenylpyridinderivate und deren Verwendung als NK-1 Rezeptorantagonisten
US6291465B1 (en) 1999-03-09 2001-09-18 Hoffmann-La Roche Inc. Biphenyl derivatives
US7163949B1 (en) 1999-11-03 2007-01-16 Amr Technology, Inc. 4-phenyl substituted tetrahydroisoquinolines and use thereof
KR100885986B1 (ko) 1999-11-03 2009-03-03 에이엠알 테크놀로지, 인크. 노르에피네프린, 도파민 및 세로토닌의 재흡수를 방지하기위한 아릴 및 헤테로아릴 치환된테트라하이드로이소퀴놀린 및 이들의 용도
ES2208205T3 (es) * 1999-11-29 2004-06-16 F. Hoffmann-La Roche Ag 2-(3,5-bis-trifluorometil-fenil)-n-metil-n-(6-morfolin-4-il-4-otolil-piridin-3-il)-isobutiramida.
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
CA2415890C (en) 2000-07-14 2009-04-07 F. Hoffmann-La Roche Ag N-oxides as nk1 receptor antagonist prodrugs of 4-phenyl-pyridine derivatives
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
DE60227657D1 (de) * 2001-05-14 2008-08-28 Hoffmann La Roche 1-OXA-3,9-DIAZASPIROc5.5ÜUNDECAN-2-ONDERIVATE UND ZEPTORS
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
JP4165882B2 (ja) * 2001-12-07 2008-10-15 ファイザー・プロダクツ・インク 治療用化合物のクエン酸塩及びその医薬組成物
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
CN100562320C (zh) 2003-01-31 2009-11-25 弗·哈夫曼-拉罗切有限公司 2-(3,5-二-三氟甲基-苯基)-N-[6-(1,1-二氧代-1λ6-硫代吗啉-4-基)-4-(4-氟-2-甲基-苯基)-吡啶-3-基]-N-甲基-异丁酰胺的新晶体变体
GB0310881D0 (en) * 2003-05-12 2003-06-18 Merck Sharp & Dohme Pharmaceutical formulation
JP4490421B2 (ja) 2003-07-03 2010-06-23 エフ.ホフマン−ラ ロシュ アーゲー 統合失調症を処置するデュアルnk1/nk3アンタゴニスト
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.
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
CA2601935C (en) 2005-02-22 2013-04-09 F. Hoffmann-La Roche Ag Nk1 antagonists
RU2404969C2 (ru) 2005-03-23 2010-11-27 Ф. Хоффманн-Ля Рош Аг Метаболиты антагонистов nk-1 против рвоты
EP1888050B1 (en) 2005-05-17 2012-03-21 Merck Sharp & Dohme Ltd. cis-4-[(4-chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexanepropanoic acid for the treatment of cancer
ZA200800440B (en) 2005-07-15 2009-12-30 Amr Technology 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
US8293900B2 (en) 2005-09-29 2012-10-23 Merck Sharp & Dohme Corp Acylated spiropiperidine derivatives as melanocortin-4 receptor modulators
WO2007044829A2 (en) 2005-10-06 2007-04-19 Dr. Reddy's Laboratories Ltd. Preparation of 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
EP2057151A4 (en) * 2006-08-28 2010-07-21 Hetero Drugs Ltd PROCESS FOR PURIFYING APREPITANT
EP2698157B1 (en) 2006-09-22 2015-05-20 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
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
EP2805945B1 (en) 2007-01-10 2019-04-03 MSD Italia S.r.l. Amide substituted indazoles as poly(ADP-ribose)polymerase (PARP) inhibitors
JP2010516734A (ja) 2007-01-24 2010-05-20 グラクソ グループ リミテッド 3,5−ジアミノ−6−(2,3−ジクロロフェニル)−1,2,4−トリアジンまたはr(−)−2,4−ジアミノ−5−(2,3−ジクロロフェニル)−6−フルオロメチルピリミジンを含む医薬組成物
US8106086B2 (en) 2007-04-02 2012-01-31 Msd K.K. Indoledione derivative
CN101657418B (zh) 2007-04-20 2012-05-30 弗·哈夫曼-拉罗切有限公司 作为nk1/nk3受体双重拮抗剂的吡咯烷衍生物
US8389553B2 (en) 2007-06-27 2013-03-05 Merck Sharp & Dohme Corp. 4-carboxybenzylamino derivatives as histone deacetylase inhibitors
CN101778837A (zh) 2007-08-07 2010-07-14 弗·哈夫曼-拉罗切有限公司 作为nk3受体拮抗剂的吡咯烷芳基-醚
CA2716080C (en) 2008-02-20 2016-12-13 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
EP2376515A1 (en) 2008-12-23 2011-10-19 Pharmasset, Inc. Synthesis of purine nucleosides
CA2748057C (en) 2008-12-23 2018-07-03 Pharmasset, Inc. Nucleoside phosphoramidates
US8551973B2 (en) 2008-12-23 2013-10-08 Gilead Pharmasset Llc Nucleoside analogs
US8691825B2 (en) 2009-04-01 2014-04-08 Merck Sharp & Dohme Corp. Inhibitors of AKT activity
KR101830447B1 (ko) 2009-05-12 2018-02-20 알바니 몰레큘라 리써치, 인크. 7-([1,2,4]트리아졸로[1,5-α]피리딘-6-일)-4-(3,4-디클로로페닐)-1,2,3,4-테트라하이드로이소퀴놀린 및 이의 용도
CN102638982B (zh) 2009-05-12 2015-07-08 百时美施贵宝公司 (S)-7-([1,2,4]三唑并[1,5-a]吡啶-6-基)-4-(3,4-二氯苯基)-1,2,3,4-四氢异喹啉的晶型及其用途
EP2429295B1 (en) 2009-05-12 2013-12-25 Albany Molecular Research, Inc. Aryl, heteroaryl, and heterocycle substituted tetrahydroisoquinolines and use thereof
EP2488028B1 (en) 2009-10-14 2020-08-19 Merck Sharp & Dohme Corp. Substituted piperidines that increase p53 activity and the uses thereof
CL2011000718A1 (es) 2010-03-31 2012-04-09 Gilead Pharmasset Llc Proceso para la preparacion de compuestos fosforados enantiomericos.
US8487102B2 (en) 2010-04-20 2013-07-16 Hoffmann-La Roche Inc. Pyrrazolopyridine compounds as dual NK1/NK3 receptor antagonists
WO2011163330A1 (en) 2010-06-24 2011-12-29 Merck Sharp & Dohme Corp. Novel heterocyclic compounds as erk inhibitors
CN107090456B (zh) 2010-08-02 2022-01-18 瑟纳治疗公司 使用短干扰核酸的RNA干扰介导的联蛋白(钙粘蛋白关联蛋白质),β1基因表达的抑制
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.
JP2013537423A (ja) 2010-08-17 2013-10-03 メルク・シャープ・エンド・ドーム・コーポレイション 低分子干渉核酸(siNA)を用いたB型肝炎ウイルス(HBV)遺伝子発現のRNA干渉媒介性阻害
US8883801B2 (en) 2010-08-23 2014-11-11 Merck Sharp & Dohme Corp. Substituted pyrazolo[1,5-a]pyrimidines as mTOR inhibitors
WO2012030685A2 (en) 2010-09-01 2012-03-08 Schering Corporation Indazole derivatives useful as erk inhibitors
EP2615916B1 (en) 2010-09-16 2017-01-04 Merck Sharp & Dohme Corp. Fused pyrazole derivatives as novel erk inhibitors
ES2616752T3 (es) 2010-09-23 2017-06-14 Nuformix Limited Composición y cocristal de aprepitant L-prolina
DK2632472T3 (en) 2010-10-29 2018-03-19 Sirna Therapeutics Inc RNA INTERFERENCE-MEDIATED INHIBITION OF GENE EXPRESSION USING SHORT INTERFERRING NUCLEIC ACIDS (SINA)
WO2012087772A1 (en) 2010-12-21 2012-06-28 Schering Corporation 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
WO2013063214A1 (en) 2011-10-27 2013-05-02 Merck Sharp & Dohme Corp. Novel compounds that are erk inhibitors
WO2013076659A1 (en) 2011-11-25 2013-05-30 Nuformix Limited Aprepitant l-proline solvates - compositions and cocrystals
WO2013087964A1 (es) 2011-12-13 2013-06-20 Servicio Andaluz De Salud Uso de agentes modificadores del ambiente peritumoral para el tratamiento del cáncer
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
EP2844261B1 (en) 2012-05-02 2018-10-17 Sirna Therapeutics, Inc. SHORT INTERFERING NUCLEIC ACID (siNA) COMPOSITIONS
CN105050598B (zh) 2012-09-28 2018-04-27 默沙东公司 作为erk抑制剂的新型化合物
RS56680B1 (sr) 2012-11-28 2018-03-30 Merck Sharp & Dohme Kompozicije i postupci za lečenje kancera
US8846657B2 (en) 2012-12-20 2014-09-30 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
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
MX376118B (es) 2016-06-06 2025-03-07 Helsinn Healthcare Sa Formulaciones inyectables fisiológicamente balanceadas de fosnetupitant.
US10975084B2 (en) 2016-10-12 2021-04-13 Merck Sharp & Dohme Corp. KDM5 inhibitors
US11098059B2 (en) 2017-11-08 2021-08-24 Merck Sharp & Dohme Corp. PRMT5 inhibitors
EP3706742B1 (en) 2017-11-08 2023-03-15 Merck Sharp & Dohme LLC Prmt5 inhibitors
CA3108388A1 (en) 2018-08-07 2020-02-13 Merck Sharp & Dohme Corp. Prmt5 inhibitors
EP3833668B1 (en) 2018-08-07 2025-03-19 Merck Sharp & Dohme LLC Prmt5 inhibitors
EP3833667B1 (en) 2018-08-07 2024-03-13 Merck Sharp & Dohme LLC 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
MX2022014901A (es) 2020-06-02 2023-01-18 Nerre Therapeutics Ltd Antagonistas del receptor de neuroquinina (nk)-1 para su uso en el tratamiento de condiciones de fibrosis pulmonar promovidas por lesion mecanica a los pulmones.

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
CA2112397A1 (en) * 1991-08-20 1993-03-04 Raymond Baker Azacyclic compounds, processes for their preparation and pharmaceutical compositions containing them
CA2099233A1 (en) * 1992-06-29 1993-12-30 Conrad P. Dorn Morpholine and thiomorpholine tachykinin receptor antagonists
DE69410784T2 (de) * 1993-02-18 1999-01-14 Merck Sharp & Dohme Ltd., Hoddesdon, Hertfordshire Azacyclische verbindungen, sie enthaltende zusammensetzungen und ihre verwendung als tachykinin antagoniste

Also Published As

Publication number Publication date
PL315153A1 (en) 1996-10-14
FI962489A0 (fi) 1996-06-14
FR04C0010I2 (fr) 2004-12-17
LTC0734381I2 (lt) 2017-04-25
NO2004003I2 (no) 2006-10-04
CZ177296A3 (en) 1996-12-11
DK0734381T3 (da) 2000-09-18
NO2018011I2 (no) 2018-12-14
FI109532B (fi) 2002-08-30
DE122004000019I1 (de) 2004-09-30
CA2178949A1 (en) 1995-06-22
SA95150523B1 (ar) 2006-03-15
GR3034095T3 (en) 2000-11-30
ES2147840T3 (es) 2000-10-01
RO118203B1 (ro) 2003-03-28
PL182521B1 (pl) 2002-01-31
LTPA2004002I1 (lt) 2016-11-10
HU224014B1 (hu) 2005-04-28
CN1057296C (zh) 2000-10-11
KR960706483A (ko) 1996-12-09
HK1009046A1 (en) 1999-05-21
RU2201924C2 (ru) 2003-04-10
EP0734381B1 (en) 2000-07-05
NO2018011I1 (no) 2018-04-04
TW419471B (en) 2001-01-21
EP0734381A1 (en) 1996-10-02
LU91069I9 (en) 2018-07-24
FR04C0010I1 (enExample) 2004-05-21
UA47397C2 (uk) 2002-07-15
NZ278222A (en) 1998-05-27
DE69425161T2 (de) 2001-02-15
JP3245424B2 (ja) 2002-01-15
FI962489A7 (fi) 1996-08-13
ATE194336T1 (de) 2000-07-15
AU1437595A (en) 1995-07-03
NO308742B1 (no) 2000-10-23
HRP941000A2 (en) 1997-06-30
NL300146I1 (nl) 2004-06-01
IL111960A0 (en) 1995-03-15
CN1142819A (zh) 1997-02-12
CY2004012I2 (el) 2017-04-05
PT734381E (pt) 2000-12-29
CA2178949C (en) 2006-03-21
HRP941000B1 (en) 2001-04-30
HUT76476A (en) 1997-09-29
HRP941000B9 (hr) 2014-11-07
KR100335704B1 (ko) 2002-11-18
YU74694A (sh) 1997-08-22
JPH09506628A (ja) 1997-06-30
HU9601634D0 (en) 1996-08-28
SI0734381T1 (en) 2000-10-31
BG64775B1 (bg) 2006-03-31
DE69425161D1 (de) 2000-08-10
AU701862B2 (en) 1999-02-04
MY115164A (en) 2003-04-30
IL111960A (en) 1999-12-22
SK75396A3 (en) 1996-12-04
WO1995016679A1 (en) 1995-06-22
BR9408351A (pt) 1997-08-26
CO4340628A1 (es) 1996-07-30
NO962523L (no) 1996-08-16
NO2004003I1 (no) 2004-06-28
NO962523D0 (no) 1996-06-14
BG100715A (bg) 1997-01-31
LU91069I2 (fr) 2004-04-07
ZA9410008B (en) 1996-07-15
CY2004012I1 (el) 2010-07-28
SK282800B6 (sk) 2002-12-03
CZ295381B6 (cs) 2005-07-13
CY2203B1 (en) 2002-11-08
NL300146I2 (nl) 2004-07-01
LV11617A (lv) 1996-12-20
LV11617B (en) 1997-04-20

Similar Documents

Publication Publication Date Title
YU49037B (sh) Morfolin antagonisti receptora tahikinina
YU49036B (sh) Morfolin i tiomorfolin antagonisti tahikinin receptora
HRP950482B1 (en) SYNTHESIS OF 3-(4-(2-AMINOETOXY)BENZOYL)-ARYL-6-HYDROXYBENZO(b)THIOPHENE
HRP20020751B1 (hr) Pirolom supstituirani 2-indolinoni kao inhibitori protein kinaze
MEP22008A (en) Derivatives of n-[heteroaryl(piperidine-2-yl)methyl]benzamide, preparation method thereof and application of same in therapeutics
YU35296A (sh) Novi terapeutski amidi i njihove farmaceutske kompozicije
GB0113233D0 (en) Chemical compounds
YU34896A (sh) Supstituisani n-(indol-2-karbonil)-glicinamidi, njihovi intermedijeri i farmaceutske kompozicije
AR046625A1 (es) Derivados de pirazol y composiciones farmaceuticas.
EA200401381A1 (ru) 3-гетероарилзамещённые изоксазолины
ES8104233A1 (es) Procedimiento para preparar derivados de acidos quinolina- carboxilicos
SE8000920L (sv) 4-(naftylmetyl)piperidinderivat
GB1105522A (en) N-phenylpiperazine compounds
YU48949B (sh) Benzopiran i srodni ltb-antagonisti
AR039122A1 (es) Derivados de ftalimido como inhibidores de monoamino oxidasa b
MXPA03011032A (es) Activadores de derivados de oxazol/tiazol del receptor hppar-alfa.
YU48079B (sh) Heterociklična jedinjenja
TR200100660T2 (tr) Piperidin türevleri.
GB971043A (en) New phenylpiperazine compounds
GB1035918A (en) 1,4-benzodiazepin-2-ones
GB1000686A (en) Phenothiazine derivatives and their preparation
ATE80835T1 (de) Fluoran-farbbildnerverbindungen.
IE801382L (en) Piperidines.
DK0555481T3 (da) Tri(C1-C6-alkoxy)benzenderivat.
GB1080880A (en) New thioamides