CZ258896A3 - Morpholine derivatives, process of their preparation and pharmaceutical compositions containing thereof - Google Patents

Morpholine derivatives, process of their preparation and pharmaceutical compositions containing thereof

Info

Publication number
CZ258896A3
CZ258896A3 CZ962588A CZ258896A CZ258896A3 CZ 258896 A3 CZ258896 A3 CZ 258896A3 CZ 962588 A CZ962588 A CZ 962588A CZ 258896 A CZ258896 A CZ 258896A CZ 258896 A3 CZ258896 A3 CZ 258896A3
Authority
CZ
Czechia
Prior art keywords
preparation
pharmaceutical compositions
compositions containing
morpholine derivatives
morpholine
Prior art date
Application number
CZ962588A
Other languages
English (en)
Other versions
CZ288241B6 (en
Inventor
Conrad P Dorn
Jeffrey J Hale
Malcolm Maccoss
Sander G Mills
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=22767887&utm_source=***_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CZ258896(A3) "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 CZ258896A3 publication Critical patent/CZ258896A3/cs
Publication of CZ288241B6 publication Critical patent/CZ288241B6/cs

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
    • A61P11/08Bronchodilators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • 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
    • 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
    • A61P3/00Drugs for disorders of the metabolism
    • BPERFORMING OPERATIONS; TRANSPORTING
    • B60VEHICLES IN GENERAL
    • B60RVEHICLES, VEHICLE FITTINGS, OR VEHICLE PARTS, NOT OTHERWISE PROVIDED FOR
    • B60R16/00Electric or fluid circuits specially adapted for vehicles and not otherwise provided for; Arrangement of elements of electric or fluid circuits specially adapted for vehicles and not otherwise provided for
    • B60R16/02Electric or fluid circuits specially adapted for vehicles and not otherwise provided for; Arrangement of elements of electric or fluid circuits specially adapted for vehicles and not otherwise provided for electric constitutive elements
    • B60R16/037Electric or fluid circuits specially adapted for vehicles and not otherwise provided for; Arrangement of elements of electric or fluid circuits specially adapted for vehicles and not otherwise provided for electric constitutive elements for occupant comfort, e.g. for automatic adjustment of appliances according to personal settings, e.g. seats, mirrors, steering wheel
    • B60R16/0373Voice control
    • 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
    • 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
    • C07D413/02Heterocyclic 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
    • C07D413/12Heterocyclic 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 chain containing hetero atoms as chain links
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6558Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
    • C07F9/65583Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system each of the hetero rings containing nitrogen as ring hetero atom

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Pain & Pain Management (AREA)
  • Molecular Biology (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Biochemistry (AREA)
  • Otolaryngology (AREA)
  • Hospice & Palliative Care (AREA)
  • Diabetes (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Mechanical Engineering (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)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Peptides Or Proteins (AREA)
  • Cosmetics (AREA)
CZ19962588A 1994-03-04 1995-02-28 Morpholine derivatives, process of their preparation and pharmaceutical preparations in which they are comprised CZ288241B6 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US20677194A 1994-03-04 1994-03-04

Publications (2)

Publication Number Publication Date
CZ258896A3 true CZ258896A3 (en) 1997-03-12
CZ288241B6 CZ288241B6 (en) 2001-05-16

Family

ID=22767887

Family Applications (1)

Application Number Title Priority Date Filing Date
CZ19962588A CZ288241B6 (en) 1994-03-04 1995-02-28 Morpholine derivatives, process of their preparation and pharmaceutical preparations in which they are comprised

Country Status (30)

Country Link
US (4) US5716942A (cs)
EP (1) EP0748320B1 (cs)
JP (1) JP3073770B2 (cs)
KR (1) KR977001713A (cs)
CN (1) CN1075812C (cs)
AT (1) ATE227722T1 (cs)
AU (1) AU700611B2 (cs)
BG (1) BG62811B1 (cs)
BR (1) BR9507046A (cs)
CA (1) CA2183250C (cs)
CO (1) CO4340689A1 (cs)
CZ (1) CZ288241B6 (cs)
DE (2) DE69528823T2 (cs)
ES (1) ES2184794T3 (cs)
FI (1) FI963450A0 (cs)
FR (1) FR08C0019I2 (cs)
HR (1) HRP950099A2 (cs)
HU (1) HUT76324A (cs)
IL (1) IL112778A0 (cs)
LV (1) LV11688B (cs)
MX (1) MX9603845A (cs)
NO (1) NO310074B1 (cs)
NZ (1) NZ282586A (cs)
PL (1) PL180522B1 (cs)
RU (1) RU2170233C2 (cs)
SK (1) SK112396A3 (cs)
TW (1) TW385308B (cs)
WO (1) WO1995023798A1 (cs)
YU (1) YU14495A (cs)
ZA (1) ZA951780B (cs)

Families Citing this family (207)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5719147A (en) * 1992-06-29 1998-02-17 Merck & Co., Inc. Morpholine and thiomorpholine tachykinin receptor antagonists
EP1462450B1 (en) * 1993-12-29 2007-06-13 MERCK SHARP & DOHME LTD. Substituted morpholine derivatives and their use as therapeutic agents
TW385308B (en) * 1994-03-04 2000-03-21 Merck & Co Inc Prodrugs of morpholine tachykinin receptor antagonists
AU690682B2 (en) * 1994-05-05 1998-04-30 Merck Sharp & Dohme Limited Morpholine derivatives and their use as antagonists of tachikinins
GB9505491D0 (en) * 1995-03-18 1995-05-03 Merck Sharp & Dohme Therapeutic agents
GB9523244D0 (en) * 1995-11-14 1996-01-17 Merck Sharp & Dohme Therapeutic agents
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
US6100256A (en) * 1996-12-02 2000-08-08 Merck Sharp & Dohme Ltd. Use of NK-1 receptors 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
ES2231902T3 (es) * 1996-12-02 2005-05-16 MERCK SHARP & DOHME LTD. Uso de antagonistas del receptor de nk-1 para el tratamiento de transtornos del movimiento.
CA2273853A1 (en) * 1996-12-02 1998-06-11 Merck Sharp & Dohme Limited Use of nk-1 receptor antagonists for treating cognitive disorders
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
CA2273351A1 (en) * 1996-12-02 1998-06-11 Merck Sharp & Dohme Limited Use of nk-1 receptor antagonists for treating sexual dysfunction
CA2273856A1 (en) * 1996-12-02 1998-06-11 Merck Sharp & Dohme Limited Use of nk-1 receptor antagonists for treating bipolar disorders
US6613765B1 (en) * 1996-12-02 2003-09-02 Merck Sharp & Dohme Limited Use of NK-1 receptor antagonists for treating major depressive disorders
AU744261B2 (en) * 1997-04-24 2002-02-21 Merck Sharp & Dohme Limited Use of NK-1 receptor antagonists for treating eating disorders
AU737019B2 (en) * 1997-08-04 2001-08-09 Merck Sharp & Dohme Limited Use of NK-1 receptor antagonists for treating aggressive behaviour disorders
AU738047B2 (en) * 1997-08-04 2001-09-06 Merck Sharp & Dohme Limited Use of NK-1 receptor antagonists for treating mania
GB9716457D0 (en) * 1997-08-04 1997-10-08 Merck Sharp & Dohme Therapeutic agents
GB9716463D0 (en) * 1997-08-04 1997-10-08 Merck Sharp & Dohme Therapeutic agents
US6087348A (en) * 1997-12-01 2000-07-11 Merck Sharp & Dohme Ltd. Use of NK-1 receptor antagonists for treating stress disorders
GB9813025D0 (en) 1998-06-16 1998-08-12 Merck Sharp & Dohme Chemical synthesis
GB9816897D0 (en) * 1998-08-04 1998-09-30 Merck Sharp & Dohme Therapeutic use
WO2000050398A2 (en) 1999-02-24 2000-08-31 F. Hoffmann-La Roche Ag Phenyl- and pyridinyl derivatives as neurokinin 1 antagonists
AU772446B2 (en) 1999-02-24 2004-04-29 F. Hoffmann-La Roche Ag 3-phenylpyridine derivatives and their use as NK-1 receptor antagonists
EP1035115B1 (en) 1999-02-24 2004-09-29 F. Hoffmann-La Roche Ag 4-Phenylpyridine derivatives and their use as NK-1 receptor antagonists
US6291465B1 (en) 1999-03-09 2001-09-18 Hoffmann-La Roche Inc. Biphenyl derivatives
FR2792835B3 (fr) * 1999-04-27 2001-05-25 Sanofi Sa Utilisation du saredutant pour la preparation de medicaments utiles dans le traitement ou la prevention de l'ensemble des troubles de l'humeur, des troubles de l'adaptation ou des troubles mixtes anxiete-depression
USRE39921E1 (en) 1999-10-07 2007-11-13 Smithkline Beecham Corporation Chemical compounds
GB9923748D0 (en) * 1999-10-07 1999-12-08 Glaxo Group Ltd Chemical compounds
US6552025B1 (en) * 1999-11-24 2003-04-22 Emory University Diimino-piperazine derivatives for use as modulators of cell regulation
DE60006340T2 (de) * 1999-11-29 2004-09-09 F. Hoffmann-La Roche Ag 2-(3,5-Bis-trifluoromethyl-phenyl)-N-methyl-N-(6-morpholin-4-yl-4-o-tolyl-pyridin-3-yl)-isobutyramid
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
US6482829B2 (en) 2000-06-08 2002-11-19 Hoffmann-La Roche Inc. Substituted heterocyclic siprodecane compound active as an antagonist of neurokinin 1 receptor
WO2002006236A1 (en) 2000-07-14 2002-01-24 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
GB0025354D0 (en) * 2000-10-17 2000-11-29 Glaxo Group Ltd Chemical compounds
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
GB0108594D0 (en) * 2001-04-05 2001-05-23 Glaxo Group Ltd Chemical compounds
US20030055026A1 (en) * 2001-04-17 2003-03-20 Dey L.P. Formoterol/steroid bronchodilating compositions and methods of use thereof
US6667344B2 (en) 2001-04-17 2003-12-23 Dey, L.P. Bronchodilating compositions and methods
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
MY130373A (en) * 2001-10-29 2007-06-29 Malesci Sas Linear basic compounds having nk-2 antagonist activity and formulations thereof
US6903129B2 (en) * 2001-12-14 2005-06-07 Hoffman-La Roche Inc. D-proline prodrugs
GB0203020D0 (en) * 2002-02-08 2002-03-27 Glaxo Group Ltd Chemical compounds
WO2003066589A1 (en) * 2002-02-08 2003-08-14 Glaxo Group Limited Piperidylcarboxamide derivatives and their use in the treatment of tachykinim-mediated diseases
GB0203022D0 (en) * 2002-02-08 2002-03-27 Glaxo Group Ltd Chemical compounds
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
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
US20040023935A1 (en) * 2002-08-02 2004-02-05 Dey, L.P. Inhalation compositions, methods of use thereof, and process for preparation of same
US20040109826A1 (en) * 2002-12-06 2004-06-10 Dey, L.P. Stabilized albuterol compositions and method of preparation thereof
NZ541243A (en) 2003-01-31 2008-04-30 Hoffmann La Roche New crystalline modification of 2-(3,5-bis-trifluoromethyl-phenyl)-N-[6-(1,1-dioxo-1lambda6-thiomorpholin-4-yl)-4-(4-fluoro-2-methyl-phenyl)-pyridin-3-yl]-N-methyl-isobutyramide
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
TWI359675B (en) 2003-07-10 2012-03-11 Dey L P Bronchodilating β-agonist compositions
TWI280239B (en) 2003-07-15 2007-05-01 Hoffmann La Roche Process for preparation of pyridine derivatives
JP4795022B2 (ja) * 2003-09-30 2011-10-19 エーザイ・アール・アンド・ディー・マネジメント株式会社 ヘテロ環化合物を含有する新規な抗真菌剤
US20070020299A1 (en) 2003-12-31 2007-01-25 Pipkin James D Inhalant formulation containing sulfoalkyl ether cyclodextrin and corticosteroid
KR20070007075A (ko) 2003-12-31 2007-01-12 사이덱스 인크 술포알킬 에테르 시클로덱스트린 및 코르티코스테로이드를함유한 흡입용 제형
US20070020298A1 (en) * 2003-12-31 2007-01-25 Pipkin James D Inhalant formulation containing sulfoalkyl ether gamma-cyclodextrin and corticosteroid
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.
EP1730751B1 (en) * 2004-03-12 2009-10-21 The Provost, Fellows And Scholars Of The College Of The Holy And Undivided Trinity Of Queen Elizabeth Near Dublin A magnetoresistive medium
WO2005104712A2 (en) 2004-04-23 2005-11-10 Cydex, Inc. Dpi formulation containing sulfoalkyl ether cyclodextrin
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
US20090227799A1 (en) * 2004-08-09 2009-09-10 Kazutaka Nakamoto Novel Antimalarial Agent Containing Heterocyclic Compound
US8088918B2 (en) * 2004-08-11 2012-01-03 Williamsburg Holdings Llc Noncardiotoxic pharmaceutical compounds
US7223737B1 (en) 2004-08-13 2007-05-29 Alcon, Inc. Method of treating dry eye disorders using glycosides
AR051475A1 (es) * 2004-11-05 2007-01-17 Merck & Co Inc Procedimiento para acido{3- [2 (r) -[(1r) - 1-[ 3,5- bis( trifluorometil)- fenil] etoxi] -3 (s) - (4- fluorfenil) morfolin -4- il]metil -5-oxo-4,5-dihidro- [1,2,4]-triazol-1-il} fosfonico
JP4767973B2 (ja) 2005-02-22 2011-09-07 エフ.ホフマン−ラ ロシュ アーゲー Nk1アンタゴニスト
RU2404969C2 (ru) 2005-03-23 2010-11-27 Ф. Хоффманн-Ля Рош Аг Метаболиты антагонистов nk-1 против рвоты
JP4874958B2 (ja) * 2005-03-30 2012-02-15 エーザイ・アール・アンド・ディー・マネジメント株式会社 ピリジン誘導体を含有する抗真菌剤
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
GEP20125566B (en) 2005-07-15 2012-07-10 Amr Technology Inc Aryl-and heteroaryl-substituded tetrahydro-benzazepines and use thereof to block reuptake of norepinephrine, dopamine and serotonin
CN101267808A (zh) 2005-09-23 2008-09-17 弗·哈夫曼-拉罗切有限公司 新型制剂
AU2006297443B2 (en) 2005-09-29 2010-08-12 Merck Sharp & Dohme Corp. Acylated spiropiperidine derivatives as melanocortin-4 receptor modulators
WO2007039883A2 (en) * 2005-10-05 2007-04-12 Ranbaxy Laboratories Limited Process for preparation of aprepitant
US7629331B2 (en) 2005-10-26 2009-12-08 Cydex Pharmaceuticals, Inc. Sulfoalkyl ether cyclodextrin compositions and methods of preparation thereof
TWI385169B (zh) * 2005-10-31 2013-02-11 Eisai R&D Man Co Ltd 經雜環取代之吡啶衍生物及含有彼之抗真菌劑
US20070185066A1 (en) * 2005-12-20 2007-08-09 Verus Pharmaceuticals, Inc. Systems and methods for the delivery of corticosteroids
US20070178049A1 (en) * 2005-12-20 2007-08-02 Verus Pharmaceuticals, Inc. Systems and methods for the delivery of corticosteroids having an enhanced pharmacokinetic profile
US20070160542A1 (en) * 2005-12-20 2007-07-12 Verus Pharmaceuticals, Inc. Methods and systems for the delivery of corticosteroids having an enhanced pharmacokinetic profile
US20070249572A1 (en) * 2005-12-20 2007-10-25 Verus Pharmaceuticals, Inc. Systems and methods for the delivery of corticosteroids
US20070197486A1 (en) * 2005-12-20 2007-08-23 Verus Pharmaceuticals, Inc. Methods and systems for the delivery of corticosteroids
EP1984359A1 (en) * 2006-02-03 2008-10-29 Glenmark Pharmaceuticals Limited Amorphous and crystalline forms of aprepitant and processes for the preparation thereof
JP2009526860A (ja) * 2006-02-15 2009-07-23 ティカ レーケメデル アーベー 安定したコルチコステロイド混合物
GB0603041D0 (en) 2006-02-15 2006-03-29 Angeletti P Ist Richerche Bio Therapeutic compounds
US8183264B2 (en) * 2006-09-21 2012-05-22 Eisai R&D Managment Co., Ltd. Pyridine derivative substituted by heteroaryl ring, and antifungal agent comprising the same
CA2664113C (en) 2006-09-22 2013-05-28 Merck & Co., Inc. 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
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
WO2008090114A1 (en) 2007-01-24 2008-07-31 Glaxo Group Limited Pharmaceutical compositions comprising 2-methoxy-5- (5-trifluoromethyl-tetrazol-i-yl-benzyl) - (2s-phenyl-piperidin-3s-yl-)
CA2682727C (en) 2007-04-02 2016-03-22 Banyu Pharmaceutical Co., Ltd. Indoledione derivative
JP5203449B2 (ja) 2007-04-20 2013-06-05 エフ.ホフマン−ラ ロシュ アーゲー 二重nk1/nk3受容体アンタゴニストとしてのピロリジン誘導体
CN102702185A (zh) * 2007-04-27 2012-10-03 卫材R&D管理有限公司 杂环取代吡啶衍生物的盐的结晶
TW200841879A (en) * 2007-04-27 2008-11-01 Eisai R&D Man Co Ltd Pyridine derivatives substituted by heterocyclic ring and phosphonoamino group, and anti-fungal agent containing same
EP1994930A1 (en) * 2007-05-22 2008-11-26 Novartis AG Triazol compounds for treating biofilm formation
EP3103791B1 (en) 2007-06-27 2018-01-31 Merck Sharp & Dohme Corp. 4-carboxybenzylamino derivatives as histone deacetylase inhibitors
RU2010106974A (ru) 2007-08-07 2011-09-20 Ф.Хоффманн-Ля Рош Аг (Ch) Ариловые эфиры пирролидина в качестве антагонистов рецепторов nk3
US20090076008A1 (en) * 2007-09-17 2009-03-19 Protia, Llc Deuterium-enriched fosaprepitant
US20090076007A1 (en) * 2007-09-17 2009-03-19 Protia, Llc Deuterium-enriched aprepitant
US8513287B2 (en) 2007-12-27 2013-08-20 Eisai R&D Management Co., Ltd. Heterocyclic ring and phosphonoxymethyl group substituted pyridine derivatives and antifungal agent containing same
CA2716080C (en) 2008-02-20 2016-12-13 Targia Pharmaceuticals Cns pharmaceutical compositions and methods of use
US8598184B2 (en) 2008-03-03 2013-12-03 Tiger Pharmatech Protein kinase inhibitors
US20100048912A1 (en) 2008-03-14 2010-02-25 Angela Brodie Novel C-17-Heteroaryl Steroidal CYP17 Inhibitors/Antiandrogens, In Vitro Biological Activities, Pharmacokinetics and Antitumor Activity
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
CA2730681C (en) * 2008-07-17 2017-03-07 Glenmark Generics Limited Fosaprepitant dimeglumine intermediate, neutral fosaprepitant, and amorphous fosaprepitant dimeglumine and processes for their preparations
US8188119B2 (en) * 2008-10-24 2012-05-29 Eisai R&D Management Co., Ltd Pyridine derivatives substituted with heterocyclic ring and γ-glutamylamino group, and antifungal agents containing same
EP2393827B1 (en) 2009-02-05 2015-10-07 Tokai Pharmaceuticals, Inc. Novel prodrugs of steroidal cyp17 inhibitors/antiandrogens
WO2010106988A1 (ja) 2009-03-17 2010-09-23 第一三共株式会社 アミド誘導体
WO2010114780A1 (en) 2009-04-01 2010-10-07 Merck Sharp & Dohme Corp. Inhibitors of akt activity
WO2010132487A1 (en) 2009-05-12 2010-11-18 Bristol-Myers Squibb Company CRYSTALLINE FORMS OF (S)-7-([1,2,4]TRIAZOLO[1,5-a]PYRIDIN-6-YL)-4-(3,4-DICHLOROHPHENYL)-1,2,3,4-TETRAHYDROISOQUINOLINE AND USE THEREOF
PE20120373A1 (es) 2009-05-12 2012-05-17 Albany Molecular Res Inc 7-([1,2,4]triazolo[1,5-a]piridin-6-il)-4-(3,4-diclorofenil)-1,2,3,4-tetrahidroisoquinolina
CN102458123A (zh) 2009-05-12 2012-05-16 阿尔巴尼分子研究公司 芳基、杂芳基和杂环取代的四氢异喹啉及其用途
UY32799A (es) * 2009-07-24 2011-02-28 Novartis Ag Derivados de oxazina y su uso en el tratamiento de trastornos neurológicos
US8188079B2 (en) * 2009-08-19 2012-05-29 Hoffman-La Roche Inc. 3-amino-5-phenyl-5,6-dihydro-2H-[1,4]oxazines
JP5099731B1 (ja) 2009-10-14 2012-12-19 メルク・シャープ・アンド・ドーム・コーポレーション p53活性を増大する置換ピペリジン及びその使用
WO2011045817A2 (en) * 2009-10-15 2011-04-21 Sandoz Private Limited Process for the preparation of fosaprepitant, intermediate and pharmaceutical acceptable salt thereof
WO2011120044A1 (en) * 2010-03-26 2011-09-29 Duke University Conjugated neuroactive steroid compositions and methods of use
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
US20120302558A1 (en) * 2010-07-13 2012-11-29 Sangamesh Badiger Oxazine derivatives and their use in the treatment of neurological disorders
US9446029B2 (en) 2010-07-27 2016-09-20 Colorado State University Research Foundation Use of NK-1 receptor antagonists in management of visceral pain
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)
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.
DK2606134T3 (da) 2010-08-17 2019-07-22 Sirna Therapeutics Inc RNA-Interferens-formidlet inhibering af hepatitis-B-virus (HBV)-genekspression ved hjælp af kort interfererende nukleinsyre (siNA)
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
DK2632472T3 (en) 2010-10-29 2018-03-19 Sirna Therapeutics Inc RNA INTERFERENCE-MEDIATED INHIBITION OF GENE EXPRESSION USING SHORT INTERFERRING NUCLEIC ACIDS (SINA)
EP2654748B1 (en) 2010-12-21 2016-07-27 Merck Sharp & Dohme Corp. Indazole derivatives useful as erk inhibitors
US8524897B2 (en) 2011-01-12 2013-09-03 Novartis Ag Crystalline oxazine derivative
AP3807A (en) 2011-01-13 2016-09-30 Novartis Ag Novel heterocyclic derivatives and their use in the treatment of neurological disorders
CN102127031B (zh) * 2011-01-17 2012-10-17 江苏江神药物化学有限公司 一种麻黄碱类化合物季胺盐及其合成方法和应用
US9067924B2 (en) * 2011-03-04 2015-06-30 Hoffmann-La Roche Inc. 1,4 thiazepines/sulfones as BACE1 and/or BACE2 inhibitors
FR2973031B1 (fr) * 2011-03-23 2013-11-29 Univ Strasbourg Derives de l'allopregnanolone et de l'epiallopregnanolone et leurs utilisations pour traiter un etat neuropathologique
EP2688901B1 (en) * 2011-03-25 2019-05-08 Université Laval INHIBITORS OF 17ß-HSD1, 17ß-HSD3 AND 17ß-HSD10
US20140045847A1 (en) 2011-04-21 2014-02-13 Piramal Enterprises Limited 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
CA2837797A1 (en) * 2011-06-07 2012-12-13 F. Hoffmann-La Roche Ag [1,3]oxazines
EP2729147B1 (en) 2011-07-04 2017-09-06 IRBM - Science Park S.p.A. Nk-1 receptor antagonists for treating corneal neovascularisation
CN102977142B (zh) * 2011-09-02 2017-03-29 江苏豪森药业集团有限公司 福沙匹坦二甲葡胺的制备方法
WO2013063214A1 (en) 2011-10-27 2013-05-02 Merck Sharp & Dohme Corp. Novel compounds that are erk inhibitors
EP2837381A4 (en) 2011-12-13 2015-12-09 Servicio Andaluz De Salud USE OF AGENTS MODIFYING THE PERITUMORAL ENVIRONMENT FOR THE TREATMENT OF CANCER
US8338413B1 (en) 2012-03-07 2012-12-25 Novartis Ag Oxazine derivatives and their use in the treatment of neurological disorders
WO2013168176A2 (en) * 2012-03-30 2013-11-14 Glenmark Generics Limited Process for preparation of fosaprepitant and salt thereof
CZ304982B6 (cs) * 2012-04-30 2015-03-11 Zentiva, K.S. Způsob přípravy a čištění nových polymorfů intermediátu fosaprepitantu
EP3358013B1 (en) 2012-05-02 2020-06-24 Sirna Therapeutics, Inc. Short interfering nucleic acid (sina) compositions
CN102675369B (zh) * 2012-05-16 2017-07-11 北京华众思康医药技术有限公司 一种制备[3‑[(2r)‑[(1r)‑1‑[3,5‑二(三氟甲基)苯基]乙氧基]‑3(s)‑(4‑氟苯基)吗啉‑4‑基]甲基]‑5‑氧代‑4,5‑二氢‑[1,2,4]‑***‑1‑基]膦酸一苄酯的新方法
US10328022B2 (en) * 2012-05-31 2019-06-25 Repros Therapeutics Inc. Formulations and methods for vaginal delivery of antiprogestins
SI2866797T1 (sl) 2012-07-06 2020-08-31 Pharmathen S.A. Stabilni injekcijski farmacevtski sestavek antagonista neurokinin 1 receptorja in postopek za njegovo pripravo
RU2660429C2 (ru) 2012-09-28 2018-07-06 Мерк Шарп И Доум Корп. Новые соединения, которые являются ингибиторами erk
CA2889977A1 (en) * 2012-10-29 2014-05-08 Allergan, Inc. Phosphate esters of bimatoprost and the prostamides
US9126998B2 (en) 2012-11-05 2015-09-08 Bayer Pharma AG Amino-substituted imidazo[1,2-a]pyridinecarboxamides and their use
US8778964B2 (en) 2012-11-05 2014-07-15 Bayer Pharma Aktiengesellschaft Hydroxy-substituted imidazo[1,2-a]-pyridinecarboxamides and their use
US8796305B2 (en) 2012-11-05 2014-08-05 Bayer Pharma Aktiengesellschaft Carboxy-substituted imidazo[1,2-a]pyridinecarboxamides and their use
US9624214B2 (en) 2012-11-05 2017-04-18 Bayer Pharma Aktiengesellschaft Amino-substituted imidazo[1,2-a]pyridinecarboxamides and their use
AU2013352568B2 (en) 2012-11-28 2019-09-19 Merck Sharp & Dohme Llc Compositions and methods for treating cancer
ES2707305T3 (es) 2012-12-20 2019-04-03 Merck Sharp & Dohme Imidazopiridinas sustituidas como inhibidores de HDM2
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
US20160009755A1 (en) * 2013-03-01 2016-01-14 Revlon Consumer Products Corporation Cyrrhetinic alkyl esters and protected derivatives thereof
PT3461834T (pt) 2013-03-13 2021-09-10 Sage Therapeutics Inc Esteroides neuroativos
KR20150127720A (ko) 2013-03-14 2015-11-17 유니버시티 오브 매릴랜드, 발티모어 안드로겐 수용체 하향 조절제 및 그의 용도
EP2987799B1 (en) * 2013-04-18 2020-04-08 Xi'an Libang Pharmaceutical Technology Co.,ltd. Ester derivative of 7-alpha-[9-(4,4,5,5,5-pentafluoropentylsulphinyl)nonyl]oestra-1,3,5(10)-triene-3,17beta-diol having antitumour activity and preparation method thereof
EP3004094B1 (de) 2013-06-04 2017-03-01 Bayer Pharma Aktiengesellschaft 3-aryl-substituierte imidazo[1,2-a]pyridine und ihre verwendung
BR112016002970A2 (pt) 2013-08-12 2017-09-12 Tokai Pharmaceuticals Inc biomarcadores para o tratamento de distúrbios neoplásicos que usa terapias direcionadas ao androgênio
WO2015034925A1 (en) 2013-09-03 2015-03-12 Moderna Therapeutics, Inc. Circular polynucleotides
CN105899223A (zh) 2013-10-28 2016-08-24 加利福尼亚大学董事会 转移性***癌的治疗
CN104650142B (zh) * 2013-11-25 2018-06-22 山东新时代药业有限公司 一种福沙匹坦二甲葡胺的制备方法
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
US20160324881A1 (en) 2013-12-30 2016-11-10 Oncoprevent Gmbh Neurokinin-1 Receptor Antagonists For Use In A Method Of Prevention Of Cancer
JP2017507140A (ja) 2014-02-19 2017-03-16 バイエル・ファルマ・アクティエンゲゼルシャフト 3−(ピリミジン−2−イル)イミダゾ[1,2−a]ピリジン
WO2015140199A1 (de) 2014-03-21 2015-09-24 Bayer Pharma Aktiengesellschaft Cyano-substituierte imidazo[1,2-a]pyridincarboxamide und ihre verwendung
TW201613888A (en) 2014-09-26 2016-04-16 Helsinn Healthcare Sa Crystalline forms of an NK-1 antagonist
CA2969268A1 (en) 2014-12-02 2016-06-09 Bayer Pharma Aktiengesellschaft Heteroaryl-substituted imidazo[1,2-a]pyridines and their use
CN108135911B (zh) 2015-07-06 2021-06-25 萨奇治疗股份有限公司 氧甾醇及其使用方法
US10610532B2 (en) 2015-08-03 2020-04-07 Leiutis Pharmaceuticals Pvt. Ltd. Liquid formulations of fosaprepitant
US10005803B2 (en) 2015-10-06 2018-06-26 Helsinn Healthcare Sa Crystalline forms of fosnetupitant
US9913853B2 (en) 2015-11-03 2018-03-13 Cipla Limited Stabilized liquid fosaprepitant formulations
EP3383829B1 (en) 2015-12-01 2020-10-21 Piramal Enterprises Limited A process for preparation of fosaprepitant dimeglumine and an intermediate thereof
CN105837526B (zh) * 2016-01-22 2018-02-27 浙江工业大学 一种阿瑞吡坦重要合成中间体(2s,3r)‑4‑苄基‑3‑(4‑氟苯基)吗啉‑2‑醇的制备方法
ES2921010T3 (es) 2016-04-01 2022-08-16 Sage Therapeutics Inc Oxisteroles y procedimientos de uso de los mismos
WO2017193046A1 (en) 2016-05-06 2017-11-09 Sage Therapeutics, Inc. Oxysterols and methods of use thereof
CN107353303B (zh) 2016-05-09 2020-09-01 上海奥博生物医药技术有限公司 一种福沙匹坦磷酸酯中间体的制备方法
BR112018074655B1 (pt) 2016-06-06 2024-02-15 Helsinn Healthcare Sa Formulação injetável de fosnetupitanto, método de fabricação de uma formulação e uso de uma formulação injetável
PL3481846T3 (pl) 2016-07-07 2021-12-20 Sage Therapeutics, Inc. 11-podstawione 24-hydroksysterole do stosowania w leczeniu stanów związanych z NMDA
US11149056B2 (en) 2016-09-30 2021-10-19 Sage Therapeutics, Inc. C7 substituted oxysterols and methods of use thereof
JP2019532079A (ja) 2016-10-18 2019-11-07 セージ セラピューティクス, インコーポレイテッド オキシステロールおよびその使用方法
US11149054B2 (en) 2016-10-18 2021-10-19 Sage Therapeutics, Inc. Oxysterols and methods of use thereof
KR20200002899A (ko) 2017-04-10 2020-01-08 체이스 테라퓨틱스 코포레이션 시누클레인병변을 치료하기 위한 nk1-길항제 배합물 및 방법
JP7158425B2 (ja) 2017-06-30 2022-10-21 チェイス セラピューティクス コーポレイション Nk-1アンタゴニスト組成物およびうつ病の処置における使用法
EP3672964A4 (en) 2017-08-21 2021-05-26 Leiutis Pharmaceuticals Pvt. Ltd. NEW TRIPLE COMBINATION FORMULATIONS FOR ANTIEMETIC THERAPY
CN109694390A (zh) * 2017-10-24 2019-04-30 齐鲁制药有限公司 一种福沙匹坦氮氧化物
EP3706742B1 (en) 2017-11-08 2023-03-15 Merck Sharp & Dohme LLC Prmt5 inhibitors
WO2019162519A1 (en) 2018-02-26 2019-08-29 Ospedale San Raffaele S.R.L. Nk-1 antagonists for use in the treatment of ocular pain
WO2020033282A1 (en) 2018-08-07 2020-02-13 Merck Sharp & Dohme Corp. Prmt5 inhibitors
EP3833667B1 (en) 2018-08-07 2024-03-13 Merck Sharp & Dohme LLC Prmt5 inhibitors
EP4117673A1 (en) 2020-03-11 2023-01-18 Ospedale San Raffaele S.r.l. Treatment of stem cell deficiency
BR112022018876A2 (pt) 2020-04-03 2022-11-22 Nerre Therapeutics Ltd Antagonista de receptor de nk-1 para tratar uma doença selecionada a partir de sepse, choque séptico, síndrome de desconforto respiratório agudo (ards) ou síndrome de disfunção múltipla dos órgãos
WO2021245512A1 (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
KR20230110283A (ko) 2020-11-19 2023-07-21 니폰 카야쿠 가부시키가이샤 혈관 장애를 유발하는 수용성 의약 함유 조성물, 혈관 장애를 유발하는 수용성 의약 함유 투여액 조제용 용액, 키트, 혈관 장애 억제제 및 비이온계 계면활성제 함유 용액
EP4052696A1 (en) 2021-03-04 2022-09-07 Extrovis AG Stable ready-to-use parenteral compositions of fosaprepitant
CN113582982B (zh) * 2021-06-15 2023-06-16 山东罗欣药业集团股份有限公司 一种nk1受体拮抗剂的制备方法

Family Cites Families (35)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA676161A (en) * 1963-12-17 Hoffmann Karl Benzimidazolyl-acetic acid derivatives and process for their manufacture
US2943022A (en) * 1958-02-25 1960-06-28 Ravensberg G M B H Substituted 1-phenyl-2, 3-dimethyl-4-morpholino methyl pyrazolone-(5) compounds and process of making same
DE1138057B (de) * 1958-04-03 1962-10-18 Ravensberg G M B H Chem Fab Verfahren zur Herstellung von 1-Phenyl-2, 3-dimethyl-4-morpholino-methyl-pyrazolon-(5)-derivaten
GB852727A (en) * 1959-06-24 1960-11-02 Ravensberg G M B H Analgesic compounds
US3458509A (en) * 1966-10-24 1969-07-29 Dow Chemical Co 4-allyltetrahydro-dimethyl-2h-1,4-thiazines
DE1670840A1 (de) * 1967-03-31 1971-03-11 Bayer Ag Verfahren zur Herstellung von Tetra-hydro-1,4-thiazin-1,1-dioxiden
US3506673A (en) * 1968-03-29 1970-04-14 Aldrich Chem Co Inc 2-(4'halo)-benzhydryl-3-quinuclidinols
GB1452701A (en) * 1974-05-07 1976-10-13 Ici Ltd Morpholine derivatives
IE50355B1 (en) * 1979-10-20 1986-04-02 Wyeth John & Brother Ltd Morpholine derivatives
US4476311A (en) * 1980-03-12 1984-10-09 The Purdue Frederick Company Analgesic 4-carboxy-pyrrolidin-2-one compound
DE3134842A1 (de) * 1981-09-03 1983-03-17 Boehringer Ingelheim KG, 6507 Ingelheim Neue anilino-1,2,3-triazol-derivate, diese enthaltende arzneimittel sowie verfahren zu deren herstellung und deren verwendung
FR2534915B1 (fr) * 1982-10-26 1985-10-25 Lafon Labor Nouveaux derives de 2-(phenoxymethyl)-morpholine, utilisation en therapeutique et procede de preparation
US4435395A (en) * 1983-03-03 1984-03-06 Usv Pharmaceutical Corporation N-Substituted 1,4-dihydropyridazines and pharmaceutical compositions
DE3421810A1 (de) * 1984-06-12 1985-12-12 Basf Ag, 6700 Ludwigshafen Phenylalkylamine - bioregulatoren
FR2612926B1 (fr) * 1987-03-24 1989-06-09 Adir Nouveaux derives de la morpholine, leur procede de preparation et les compositions pharmaceutiques les renfermant
DE3800977A1 (de) * 1988-01-15 1989-07-27 Ant Nachrichtentech Digitalsignal-uebertragungssystem mit linienersatzbetrieb
US5064838A (en) * 1988-01-21 1991-11-12 Merrell Dow Pharmaceuticals 1,4-disubstituted-piperidinyl compounds as pain relievers
KR900018073A (ko) * 1988-05-23 1990-12-20 추후보충 피페라진 화합물
EP0360390A1 (en) * 1988-07-25 1990-03-28 Glaxo Group Limited Spirolactam derivatives
MX18467A (es) * 1988-11-23 1993-07-01 Pfizer Agentes terapeuticos de quinuclidinas
DE3901244A1 (de) * 1989-01-18 1990-07-19 Basf Ag Phenylalkylamine und diese enthaltende fungizide
US5070090A (en) * 1989-05-15 1991-12-03 Janssen Pharmaceutica N.V. Antipicorpaviral herterocyclic-substituted morpholinyl alkylphenol ethers
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
EP0532527B1 (en) * 1990-06-01 1994-11-09 Pfizer Inc. 3-amino-2-aryl quinuclidines, process for their preparation and pharmaceutical compositions containing them
DK178590D0 (da) * 1990-07-26 1990-07-26 Novo Nordisk As 1,4-disubstituerede piperaziner
DK0550635T3 (da) * 1990-09-28 1995-09-04 Pfizer Cykliske forbindelser med kondeserede ringe, som er analoger til nitrogenholdige ikke-aromatiske het erocykliske forbindelser
US5138060A (en) * 1991-01-03 1992-08-11 Pfizer Inc. Process and intermediates for preparing azabicyclo(2.2.2)octan-3-imines
HUT65612A (en) * 1991-01-10 1994-07-28 Pfizer Process n-alcyl-quinuclidinium salts of p-antagonistic activity
US5254569A (en) * 1991-01-14 1993-10-19 The Du Pont Merck Pharmaceutical Company (Amidomethyl)nitrogen heterocyclic analgesics
US5242930A (en) * 1991-02-11 1993-09-07 Merck Sharp & Dohme Ltd. Azabicyclic compounds, pharmaceutical compositions containing them and their use in therapy
EP0528495A1 (en) * 1991-08-20 1993-02-24 Merck Sharp & Dohme Ltd. Azacyclic compounds, processes for their preparation and pharmaceutical compositions containing them
PT533280E (pt) * 1991-09-20 2001-01-31 Glaxo Group Ltd Novas utilizacoes medicas para antagonistas de taquiquinina
IL106142A (en) * 1992-06-29 1997-03-18 Merck & Co Inc Morpholine and thiomorpholine tachykinin receptor antagonists, their preparation and pharmaceutical compositions containing them
IL111960A (en) * 1993-12-17 1999-12-22 Merck & Co Inc Morpholines and thiomorpholines their preparation and pharmaceutical compositions containing them
TW385308B (en) * 1994-03-04 2000-03-21 Merck & Co Inc Prodrugs of morpholine tachykinin receptor antagonists

Also Published As

Publication number Publication date
FI963450A (fi) 1996-09-03
BG62811B1 (bg) 2000-08-31
PL180522B1 (pl) 2001-02-28
CO4340689A1 (es) 1996-07-30
NO310074B1 (no) 2001-05-14
MX9603845A (es) 1997-07-31
ATE227722T1 (de) 2002-11-15
CA2183250A1 (en) 1995-09-08
CA2183250C (en) 2006-03-21
JP3073770B2 (ja) 2000-08-07
NO963675D0 (no) 1996-09-03
FR08C0019I2 (fr) 2009-10-30
DE69528823D1 (en) 2002-12-19
SK112396A3 (en) 1997-03-05
JPH09509935A (ja) 1997-10-07
FR08C0019I1 (cs) 2008-07-18
ZA951780B (en) 1995-11-15
NO963675L (no) 1996-11-04
LV11688B (en) 1997-06-20
AU700611B2 (en) 1999-01-07
EP0748320B1 (en) 2002-11-13
HRP950099A2 (en) 1998-04-30
DE69528823T2 (de) 2003-07-03
EP0748320A1 (en) 1996-12-18
WO1995023798A1 (en) 1995-09-08
US5716942A (en) 1998-02-10
TW385308B (en) 2000-03-21
AU1975095A (en) 1995-09-18
RU2170233C2 (ru) 2001-07-10
NZ282586A (en) 1998-07-28
BG100798A (bg) 1997-03-31
YU14495A (sh) 1999-07-28
CN1075812C (zh) 2001-12-05
BR9507046A (pt) 1997-09-09
CZ288241B6 (en) 2001-05-16
FI963450A0 (fi) 1996-09-03
HUT76324A (en) 1997-08-28
KR977001713A (ko) 1997-04-12
PL316143A1 (en) 1996-12-23
ES2184794T3 (es) 2003-04-16
US5780467A (en) 1998-07-14
US5512570A (en) 1996-04-30
DE122008000037I1 (de) 2008-11-06
US5691336A (en) 1997-11-25
CN1147254A (zh) 1997-04-09
IL112778A0 (en) 1995-05-26
LV11688A (lv) 1997-02-20
HU9602409D0 (en) 1996-11-28

Similar Documents

Publication Publication Date Title
CZ258896A3 (en) Morpholine derivatives, process of their preparation and pharmaceutical compositions containing thereof
MY112102A (en) Therapeutic heterocycles.
MY107157A (en) Quinuclidine derivatives.
MY119181A (en) Aryl pyrimidine derivatives
UA39168C2 (uk) Фторалкоксифенільні похідні піперидину або хінуклідину, що є антагоністами речовини p і фармацевтична композиція на їх основі
GB9322643D0 (en) Lactam derivatives
GB9523526D0 (en) Therapeutic compounds
ZA961069B (en) Heterocyclic derivatives
AU3563695A (en) Novel piperidine derivatives with paf antagonist activity
MX9403088A (es) Composiciones farmaceuticas que contienen deriva- dos de indol y metodos de uso.
AU2001290480A1 (en) Cyclized benzamide neurokinin antagonists for use in therapy
UA42731C2 (uk) Арилалкілтіадіазинони, спосіб їх отримання, фармацевтична композиція, спосіб її отримання, спосіб лікування
BG105204A (en) Salts of paroxetine
DE69730137D1 (de) Naphthyridine die den rezeptor il-4 und den faktor g-csf beeinflussen
IL114185A (en) Substituted alkyldiamine derivatives pharmaceutical compositions containing them and process for their preparation
NO974687L (no) Kondenserte <beta>-carboliner

Legal Events

Date Code Title Description
PD00 Pending as of 2000-06-30 in czech republic