KR977001713A - 모르폴린 태키키닌 수용체 길항제의 프로드러그(Prodrugs of morpholine tachykinin receptor antagonists) - Google Patents

모르폴린 태키키닌 수용체 길항제의 프로드러그(Prodrugs of morpholine tachykinin receptor antagonists)

Info

Publication number
KR977001713A
KR977001713A KR1019960704865A KR19960704866A KR977001713A KR 977001713 A KR977001713 A KR 977001713A KR 1019960704865 A KR1019960704865 A KR 1019960704865A KR 19960704866 A KR19960704866 A KR 19960704866A KR 977001713 A KR977001713 A KR 977001713A
Authority
KR
South Korea
Prior art keywords
phenyl
morpholine
methyl
fluoro
ethoxy
Prior art date
Legal status (The legal status 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 status listed.)
Granted
Application number
KR1019960704865A
Other languages
English (en)
Korean (ko)
Inventor
콘라드 피 돈
제프리 제이 할
말콤 맥코스
산더 지 밀스
Original Assignee
폴록 도나 엘
머크 앤드 캄파니, 인코포레이티드
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=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=KR977001713(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by 폴록 도나 엘, 머크 앤드 캄파니, 인코포레이티드 filed Critical 폴록 도나 엘
Publication of KR977001713A publication Critical patent/KR977001713A/ko
Granted legal-status Critical Current

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
    • A61P11/08—Bronchodilators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • 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
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B60—VEHICLES IN GENERAL
    • B60R—VEHICLES, VEHICLE FITTINGS, OR VEHICLE PARTS, NOT OTHERWISE PROVIDED FOR
    • B60R16/00—Electric 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
    • B60R16/02—Electric 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
    • B60R16/037—Electric 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
    • B60R16/0373—Voice control
    • 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
    • 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
    • C07D413/02—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
    • C07D413/12—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 chain containing hetero atoms as chain links
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6558—Heterocyclic 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
    • C07F9/65583—Heterocyclic 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)
  • General Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pulmonology (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Diabetes (AREA)
  • Otolaryngology (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Mechanical Engineering (AREA)
  • Hospice & Palliative Care (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)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Cosmetics (AREA)
  • Peptides Or Proteins (AREA)
KR1019960704865A 1994-03-04 1995-02-28 모르폴린 태키키닌 수용체 길항제의 프로드러그(Prodrugs of morpholine tachykinin receptor antagonists) Granted KR977001713A (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US20677194A 1994-03-04 1994-03-04
US8/206,771 1994-03-04
PCT/US1995/002551 WO1995023798A1 (en) 1994-03-04 1995-02-28 Prodrugs of morpholine tachykinin receptor antagonists

Publications (1)

Publication Number Publication Date
KR977001713A true KR977001713A (ko) 1997-04-12

Family

ID=22767887

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1019960704865A Granted KR977001713A (ko) 1994-03-04 1995-02-28 모르폴린 태키키닌 수용체 길항제의 프로드러그(Prodrugs of morpholine tachykinin receptor antagonists)

Country Status (30)

Country Link
US (4) US5716942A (https=)
EP (1) EP0748320B1 (https=)
JP (1) JP3073770B2 (https=)
KR (1) KR977001713A (https=)
CN (1) CN1075812C (https=)
AT (1) ATE227722T1 (https=)
AU (1) AU700611B2 (https=)
BG (1) BG62811B1 (https=)
BR (1) BR9507046A (https=)
CA (1) CA2183250C (https=)
CO (1) CO4340689A1 (https=)
CZ (1) CZ288241B6 (https=)
DE (2) DE69528823T2 (https=)
ES (1) ES2184794T3 (https=)
FI (1) FI963450L (https=)
FR (1) FR08C0019I2 (https=)
HR (1) HRP950099A2 (https=)
HU (1) HUT76324A (https=)
IL (1) IL112778A0 (https=)
LV (1) LV11688B (https=)
MX (1) MX9603845A (https=)
NO (1) NO310074B1 (https=)
NZ (1) NZ282586A (https=)
PL (1) PL180522B1 (https=)
RU (1) RU2170233C2 (https=)
SK (1) SK112396A3 (https=)
TW (1) TW385308B (https=)
WO (1) WO1995023798A1 (https=)
YU (1) YU14495A (https=)
ZA (1) ZA951780B (https=)

Families Citing this family (220)

* 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
IL112134A (en) * 1993-12-29 1999-12-22 Merck Sharp & Dohme Substituted morpholine derivatives their preparation and pharmaceutical compositions containing them
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
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
US5977104A (en) * 1996-12-02 1999-11-02 Merck Sharp & Dohme Ltd. Use of NK-1 receptor antagonists for treating bipolar disorders
CA2273853A1 (en) * 1996-12-02 1998-06-11 Merck Sharp & Dohme Limited Use of nk-1 receptor antagonists for treating cognitive disorders
JP2001504851A (ja) * 1996-12-02 2001-04-10 メルク シヤープ エンド ドーム リミテツド 性的機能不全の治療のためのｎｋ−１受容体拮抗薬の使用
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
EP0942730A1 (en) * 1996-12-02 1999-09-22 MERCK SHARP & DOHME LTD. Use of nk-1 receptor antagonists for treating bipolar disorders
US6100256A (en) * 1996-12-02 2000-08-08 Merck Sharp & Dohme Ltd. Use of NK-1 receptors antagonists for treating schizophrenic disorders
AU734872B2 (en) * 1996-12-02 2001-06-21 Merck Sharp & Dohme Limited Use of NK-1 receptor antagonists for treating movement disorders
US6613765B1 (en) * 1996-12-02 2003-09-02 Merck Sharp & Dohme Limited Use of NK-1 receptor antagonists for treating major depressive disorders
JP2001524960A (ja) * 1997-04-24 2001-12-04 メルク シヤープ エンド ドーム リミテツド 摂食障害を治療するためのｎｋ−１受容体拮抗薬の使用
GB9716463D0 (en) * 1997-08-04 1997-10-08 Merck Sharp & Dohme Therapeutic agents
AU738047B2 (en) * 1997-08-04 2001-09-06 Merck Sharp & Dohme Limited Use of NK-1 receptor antagonists for treating mania
CA2298779A1 (en) * 1997-08-04 1999-02-18 Merck Sharp & Dohme Limited Use of nk-1 receptor antagonists for treating aggressive behaviour disorders
GB9716457D0 (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
TR200102490T2 (tr) 1999-02-24 2001-12-21 F.Hoffmann-La Roche Ag Fenil ve piridinil türevleri
PT1035115E (pt) 1999-02-24 2005-01-31 Hoffmann La Roche Derivados de 4-fenilpiridina e a sua utilizacao como antagonistas do receptor nk-1
KR100437587B1 (ko) 1999-02-24 2004-06-30 에프. 호프만-라 로슈 아게 3-페닐피리딘 유도체 및 그의 뉴로키닌-1 수용체길항제로서의 용도
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
GB9923748D0 (en) * 1999-10-07 1999-12-08 Glaxo Group Ltd Chemical compounds
USRE39921E1 (en) 1999-10-07 2007-11-13 Smithkline Beecham Corporation Chemical compounds
MXPA02004330A (es) 1999-11-03 2004-07-30 Albany Molecular Res Inc Tetrahidroisoquinolinas aril-y heteroaril-sustituidas y uso de las mismas para bloquear la recaptacion de norepinefrina, dopamina y serotonina..
US7163949B1 (en) 1999-11-03 2007-01-16 Amr Technology, Inc. 4-phenyl substituted tetrahydroisoquinolines and use thereof
US6552025B1 (en) * 1999-11-24 2003-04-22 Emory University Diimino-piperazine derivatives for use as modulators of cell regulation
SI1103545T1 (en) * 1999-11-29 2004-02-29 F. Hoffmann-La Roche Ag 2-(3,5-Bis-trifluoromethyl-phenyl)-N-methyl-N-(6-morpholin-4-yl-4-o-tolyl-pyridin-3-yl)-isobutyramide
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
KR100821410B1 (ko) 2000-07-11 2008-04-10 에이엠알 테크놀로지, 인크. 4-페닐 치환된 테트라하이드로이소퀴놀린 및 이의치료학적 용도
MXPA03000366A (es) 2000-07-14 2003-05-27 Hoffmann La Roche N-oxidos como profarmacos antagonistas del receptor nk1 de derivados de 4-fenil-piridina.
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
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
GB0203020D0 (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
KR100693367B1 (ko) * 2002-06-27 2007-03-12 아스텔라스세이야쿠 가부시키가이샤 아미노알콜 유도체
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
RU2347777C2 (ru) 2003-07-03 2009-02-27 Ф.Хоффманн-Ля Рош Аг Двойные агонисты nk1/nk3 для лечения шизофрении
TWI359675B (en) 2003-07-10 2012-03-11 Dey L P Bronchodilating β-agonist compositions
US7288658B2 (en) 2003-07-15 2007-10-30 Hoffmann-La Roche Inc. Process for preparation of pyridine derivatives
WO2005033079A1 (ja) * 2003-09-30 2005-04-14 Eisai Co., Ltd. ヘテロ環化合物を含有する新規な抗真菌剤
US20070020298A1 (en) * 2003-12-31 2007-01-25 Pipkin James D Inhalant formulation containing sulfoalkyl ether gamma-cyclodextrin and corticosteroid
AU2004311478A1 (en) 2003-12-31 2005-07-21 Cydex Pharmaceuticals, Inc. Inhalant formulation containing sulfoalkyl ether cyclodextrin and corticosteroid
US20070020299A1 (en) 2003-12-31 2007-01-25 Pipkin James D Inhalant formulation containing sulfoalkyl ether 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.
WO2005088655A1 (en) * 2004-03-12 2005-09-22 The Provost Fellows And Scholars Of The College Of The Holy And Undivided Trinity Of Queen Elizabeth Near Dublin A magnetoresistive medium
CN101098678A (zh) 2004-04-23 2008-01-02 锡德克斯公司 含有磺基烷基醚环糊精的dpi制剂
NZ552397A (en) 2004-07-15 2011-04-29 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
MX2007001713A (es) * 2004-08-11 2007-07-13 Donald L Barbeau Compuestos farmaceuticos no cardiotoxicos.
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
MX2007010034A (es) 2005-02-22 2007-10-04 Hoffmann La Roche Antagonista de nk1.
ATE425144T1 (de) 2005-03-23 2009-03-15 Hoffmann La Roche Metaboliten für nk-i-antagonisten zur emesis
EP1864980A4 (en) * 2005-03-30 2010-08-18 Eisai R&D Man Co Ltd A PYRIDINE DERIVATIVE ANTIPILIC AGENT
ES2382814T3 (es) 2005-05-17 2012-06-13 Merck Sharp & Dohme Ltd. Ácido cis-4-[(4-clorofenil)sulfonil]-4-(2,5-difluorofenil)ciclohexanopropanoico para el tratamiento del cáncer
KR101594898B1 (ko) 2005-07-15 2016-02-18 알바니 몰레큘라 리써치, 인크. 아릴- 및 헤테로아릴-치환된 테트라히드로벤자제핀, 및 노르에피네프린, 도파민 및 세로토닌의 재흡수를 차단하기 위한 용도
CN103893145A (zh) 2005-09-23 2014-07-02 弗·哈夫曼-拉罗切有限公司 新型制剂
EP1940842B1 (en) 2005-09-29 2012-05-30 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
US20070197486A1 (en) * 2005-12-20 2007-08-23 Verus Pharmaceuticals, Inc. Methods and systems 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
US20070185066A1 (en) * 2005-12-20 2007-08-09 Verus Pharmaceuticals, Inc. Systems and methods for the delivery of corticosteroids
US20070249572A1 (en) * 2005-12-20 2007-10-25 Verus Pharmaceuticals, Inc. Systems and methods 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
JP2009526858A (ja) * 2006-02-15 2009-07-23 ティカ レーケメデル アーベー コルチコステロイド溶液を製造する方法
GB0603041D0 (en) 2006-02-15 2006-03-29 Angeletti P Ist Richerche Bio Therapeutic compounds
EP2065377B1 (en) * 2006-09-21 2011-11-23 Eisai R&D Management Co., Ltd. Pyridine derivative substituted by heteroaryl ring, and antifungal agent comprising the same
US8173629B2 (en) 2006-09-22 2012-05-08 Merck Sharp & Dohme Corp. Method of treatment using fatty acid synthesis inhibitors
US20110218176A1 (en) 2006-11-01 2011-09-08 Barbara Brooke Jennings-Spring Compounds, methods, and treatments for abnormal signaling pathways for prenatal and postnatal development
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
EP2117538A1 (en) 2007-01-24 2009-11-18 Glaxo Group Limited Pharmaceutical compositions comprising 2-methoxy-5- (5-trifluoromethyl-tetrazol-i-yl-benzyl) - (2s-phenyl-piperidin-3s-yl-)
JP5319518B2 (ja) 2007-04-02 2013-10-16 Ｍｓｄ株式会社 インドールジオン誘導体
AU2008240804B2 (en) 2007-04-20 2013-02-21 F. Hoffmann-La Roche Ag Pyrrolidine derivatives as dual NK1/NK3 receptor antagonists
WO2008136279A1 (ja) * 2007-04-27 2008-11-13 Eisai R & D Management Co., Ltd. ヘテロ環置換ピリジン誘導体の塩またはその結晶
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
AU2008269154B2 (en) 2007-06-27 2014-06-12 Merck Sharp & Dohme Llc 4-carboxybenzylamino derivatives as histone deacetylase inhibitors
US12370352B2 (en) 2007-06-28 2025-07-29 Cydex Pharmaceuticals, Inc. Nasal and ophthalmic delivery of aqueous corticosteroid solutions
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
US20090076007A1 (en) * 2007-09-17 2009-03-19 Protia, Llc Deuterium-enriched aprepitant
US20090076008A1 (en) * 2007-09-17 2009-03-19 Protia, Llc Deuterium-enriched fosaprepitant
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
AU2009222122A1 (en) 2008-03-03 2009-09-11 Tiger Pharmatech Tyrosine kinase inhibitors
US20100048913A1 (en) 2008-03-14 2010-02-25 Angela Brodie Novel C-17-Heteroaryl Steroidal CYP17 Inhibitors/Antiandrogens;Synthesis 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
CN102686600A (zh) 2009-02-05 2012-09-19 托凯药业股份有限公司 甾体cyp17抑制剂/抗雄激素物质的新型药物前体
BRPI1014125A2 (pt) 2009-03-17 2016-04-12 Daiichi Sankyo Co Ltd composto, composição farmacêutica, e, uso de um composto.
WO2010114780A1 (en) 2009-04-01 2010-10-07 Merck Sharp & Dohme Corp. Inhibitors of akt activity
AU2010247763B2 (en) 2009-05-12 2015-12-24 Albany Molecular Research, Inc. 7-([1,2,4,]triazolo[1,5,-a]pyridin-6-yl)-4-(3,4-dichlorophenyl)-1,2,3,4- tetrahydroisoquinoline and use thereof
AU2010247735B2 (en) 2009-05-12 2015-07-16 Albany Molecular Research, Inc. Crystalline forms of (S)-7-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-4-(3,4-dichlorophenyl)- 1,2,3,4-tetrahydroisoquinoline and use thereof
WO2010132437A1 (en) 2009-05-12 2010-11-18 Albany Molecular Research, Inc. Aryl, heteroaryl, and heterocycle substituted tetrahydroisoquinolines and use thereof
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
PE20121172A1 (es) 2009-10-14 2012-09-05 Merck Sharp & Dohme Piperidinas sustituidas con actividad en la hdm2
WO2011045817A2 (en) * 2009-10-15 2011-04-21 Sandoz Private Limited Process for the preparation of fosaprepitant, intermediate and pharmaceutical acceptable salt thereof
US20130245253A1 (en) * 2010-03-26 2013-09-19 Department Of Veterans Affairs 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
WO2011163330A1 (en) 2010-06-24 2011-12-29 Merck Sharp & Dohme Corp. Novel heterocyclic compounds as erk inhibitors
DK2483255T3 (da) * 2010-07-13 2014-01-20 Novartis Ag Oxazinderivater samt deres anvendelse ved behandling af neurologiske lidelser
US9446029B2 (en) 2010-07-27 2016-09-20 Colorado State University Research Foundation Use of NK-1 receptor antagonists in management of visceral pain
EP3330377A1 (en) 2010-08-02 2018-06-06 Sirna Therapeutics, Inc. 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.
US9029341B2 (en) 2010-08-17 2015-05-12 Sirna Therapeutics, Inc. RNA interference mediated inhibition of hepatitis B virus (HBV) gene expression using short interfering nucleic acid (siNA)
US8883801B2 (en) 2010-08-23 2014-11-11 Merck Sharp & Dohme Corp. Substituted pyrazolo[1,5-a]pyrimidines as mTOR inhibitors
EP2613782B1 (en) 2010-09-01 2016-11-02 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
WO2012058210A1 (en) 2010-10-29 2012-05-03 Merck Sharp & Dohme Corp. RNA INTERFERENCE MEDIATED INHIBITION OF GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACIDS (siNA)
WO2012087772A1 (en) 2010-12-21 2012-06-28 Schering Corporation Indazole derivatives useful as erk inhibitors
US8524897B2 (en) 2011-01-12 2013-09-03 Novartis Ag Crystalline oxazine derivative
MY162413A (en) 2011-01-13 2017-06-15 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
US11072632B2 (en) * 2011-03-25 2021-07-27 UNIVERSITé LAVAL Inhibitors of 17β-HSD1, 17β-HSD3 and 17β-HSD10
AU2012245971A1 (en) 2011-04-21 2013-10-17 Piramal Enterprises Limited A crystalline form of a salt of a morpholino sulfonyl indole derivative and a process for its preparation
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
WO2013004766A1 (en) 2011-07-04 2013-01-10 Ferrari Giulio 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
CA2848212C (en) 2011-09-08 2022-03-29 Sage Therapeutics, Inc. Neuroactive steroids, compositions, and uses thereof
EP2770987B1 (en) 2011-10-27 2018-04-04 Merck Sharp & Dohme Corp. Novel compounds that are erk inhibitors
US20150297613A1 (en) 2011-12-13 2015-10-22 Servicio Andaluz De Salud Use of agents that alter 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
US20150299696A1 (en) 2012-05-02 2015-10-22 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]‑三唑‑1‑基]膦酸一苄酯的新方法
CA2872644A1 (en) * 2012-05-31 2013-12-05 Allergan Pharmaceuticals International Limited Formulations and methods for vaginal delivery of antiprogestins
PL2866797T3 (pl) 2012-07-06 2020-11-02 Pharmathen S.A. Stabilna, nadająca się do wstrzykiwania kompozycja farmaceutyczna antagonisty receptora neurokininy-1 i sposób jej wytwarzania
RU2660429C2 (ru) 2012-09-28 2018-07-06 Мерк Шарп И Доум Корп. Новые соединения, которые являются ингибиторами erk
EP2912046A1 (en) * 2012-10-29 2015-09-02 Allergan, Inc. Phosphate esters of bimatoprost and the prostamides
US8778964B2 (en) 2012-11-05 2014-07-15 Bayer Pharma Aktiengesellschaft Hydroxy-substituted imidazo[1,2-a]-pyridinecarboxamides and their use
US9126998B2 (en) 2012-11-05 2015-09-08 Bayer Pharma AG Amino-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
US8796305B2 (en) 2012-11-05 2014-08-05 Bayer Pharma Aktiengesellschaft Carboxy-substituted imidazo[1,2-a]pyridinecarboxamides and their use
RS56680B1 (sr) 2012-11-28 2018-03-30 Merck Sharp & Dohme Kompozicije i postupci za lečenje kancera
KR102196882B1 (ko) 2012-12-20 2020-12-30 머크 샤프 앤드 돔 코포레이션 Hdm2 억제제로서의 치환된 이미다조피리딘
WO2014120748A1 (en) 2013-01-30 2014-08-07 Merck Sharp & Dohme Corp. 2,6,7,8 substituted purines as hdm2 inhibitors
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
WO2014134413A2 (en) * 2013-03-01 2014-09-04 Revlon Consumer Products Corporation Cyrrhetinic alkyl esters and protected derivatives thereof
PT2968369T (pt) 2013-03-13 2018-12-05 Sage Therapeutics Inc Esteroides neuroativos e métodos para o seu uso
RU2015137617A (ru) 2013-03-14 2017-04-18 Юниверсити Оф Мэриленд, Балтимор Офис Оф Текнолоджи Трансфер Агенты, подавляющие андрогенные рецепторы, и их применение
US20160060288A1 (en) * 2013-04-18 2016-03-03 Xi'anlibang Pharmaceutical Technology Co., Ltd. Ester derivatives of 7-alpha-[9-(4,4,5,5,5-pentafluoropentylsulfinyl)nonyl)-estra-1,3,5(10)-triene-3,17beta-diol having anticancer activity and preparation method thereof
US9776997B2 (en) 2013-06-04 2017-10-03 Bayer Pharma Aktiengesellschaft 3-aryl-substituted imidazo[1,2-A]pyridines and their use
CN105636594A (zh) 2013-08-12 2016-06-01 托凯药业股份有限公司 使用雄激素靶向疗法用于治疗肿瘤性疾病的生物标记物
WO2015034925A1 (en) 2013-09-03 2015-03-12 Moderna Therapeutics, Inc. Circular polynucleotides
WO2015065919A1 (en) 2013-10-28 2015-05-07 The Regents Of The University Of California Treatment of metastatic prostate cancer
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
EP3091977A2 (en) 2013-12-30 2016-11-16 Oncoprevent GmbH Neurokinin-1 receptor antagonists for use in a method of prevention of cancer
US9688699B2 (en) 2014-02-19 2017-06-27 Bayer Pharma Aktiengesellschaft 3-(pyrimidine-2-yl)imidazo[1,2-a]pyridines
CN106715426A (zh) 2014-03-21 2017-05-24 拜耳医药股份有限公司 氰基取代的咪唑并[1,2‑a]吡啶甲酰胺及其用途
US10259840B2 (en) 2014-06-18 2019-04-16 Sage Therapeutics, Inc. Oxysterols and methods of use thereof
TW201613888A (en) 2014-09-26 2016-04-16 Helsinn Healthcare Sa Crystalline forms of an NK-1 antagonist
EP3227287B1 (de) 2014-12-02 2019-08-07 Bayer Pharma Aktiengesellschaft Heteroaryl-substituierte imidazo[1,2-a]pyridine und ihre verwendung
EP3828194B1 (en) 2015-07-06 2025-04-16 Sage Therapeutics, Inc. Oxysterols and methods of use thereof
HUE071964T2 (hu) 2015-07-06 2025-10-28 Sage Therapeutics Inc Oxiszterolok és alkalmazási eljárásaik
WO2017021880A1 (en) 2015-08-03 2017-02-09 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
WO2017093899A1 (en) 2015-12-01 2017-06-08 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
SMT202200300T1 (it) 2016-04-01 2022-09-14 Sage Therapeutics Inc Ossisteroli e relativi metodi d'uso
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
CA3025837C (en) 2016-06-06 2024-02-13 Helsinn Healthcare Sa Physiologically balanced injectable formulations of fosnetupitant
ES2884071T3 (es) 2016-07-07 2021-12-10 Sage Therapeutics Inc 24-hidroxiesteroles sustituidos en 11 para el tratamiento de afecciones relacionadas con NMDA
ES2935057T3 (es) 2016-09-30 2023-03-01 Sage Therapeutics Inc C7 oxisteroles sustituidos y estos compuestos para su uso como moduladores de la NMDA
EP3525785B1 (en) 2016-10-12 2025-08-27 Merck Sharp & Dohme LLC Kdm5 inhibitors
RU2019115113A (ru) 2016-10-18 2020-11-24 Сейдж Терапьютикс, Инк. Оксистеролы и способы их применения
KR20230051723A (ko) 2016-10-18 2023-04-18 세이지 테라퓨틱스, 인크. 옥시스테롤 및 그의 사용 방법
IL312486B2 (en) 2017-04-10 2025-05-01 Chase Therapeutics Corp NK1 antagonist combination and method for treating synucleinopathies
CA3104811C (en) 2017-06-30 2024-05-28 Chase Therapeutics Corporation Composition comprising pramipexole and nk1-antagonists for treating depression
EP3672964A4 (en) 2017-08-21 2021-05-26 Leiutis Pharmaceuticals Pvt. Ltd. Novel 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
US10947234B2 (en) 2017-11-08 2021-03-16 Merck Sharp & Dohme Corp. PRMT5 inhibitors
EP3706747B1 (en) 2017-11-08 2025-09-03 Merck Sharp & Dohme LLC Prmt5 inhibitors
US20210015834A1 (en) * 2018-02-26 2021-01-21 Ospedale San Raffaele S.R.L. Nk-1 antagonists for use in the treatment of ocular pain
US12173026B2 (en) 2018-08-07 2024-12-24 Merck Sharp & Dohme Llc PRMT5 inhibitors
US11981701B2 (en) 2018-08-07 2024-05-14 Merck Sharp & Dohme Llc PRMT5 inhibitors
EP3833668B1 (en) 2018-08-07 2025-03-19 Merck Sharp & Dohme LLC Prmt5 inhibitors
WO2021180885A1 (en) 2020-03-11 2021-09-16 Ospedale San Raffaele S.R.L. Treatment of stem cell deficiency
CA3173697A1 (en) 2020-04-03 2021-10-07 Mike TROWER An nk-1 receptor antagonist for treating a disease selecting from sepsis, septic shock, acute respiratory distress syndrome (ards) or multiple organ dysfunction syndrome (mods)
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
US20240024339A1 (en) 2020-11-19 2024-01-25 Nippon Kayaku Kabushiki Kaisha Composition containing water-soluble drug causing vascular disorder, solution for use in preparation of administration solution containing water-soluble drug causing vascular disorder, kit, agent for suppressing vascular disorder, and solution containing nonionic surfactant
US11541066B2 (en) 2021-03-04 2023-01-03 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
WO2025008409A2 (en) 2023-07-03 2025-01-09 Preeti Jha Substituted 2-phenylpiperidine compounds for use in the diagnosis, treatment and/or prevention of cancer
WO2025085662A1 (en) 2023-10-17 2025-04-24 Vanderbilt University Compounds for tocolytic use

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
FI892468A7 (fi) * 1988-05-23 1989-11-24 Glaxo Group Ltd Piperazinderivat.
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
JPH072740B2 (ja) * 1990-06-01 1995-01-18 フアイザー・インコーポレイテツド ３―アミノ―２―アリールキヌクリジン
DK178590D0 (da) * 1990-07-26 1990-07-26 Novo Nordisk As 1,4-disubstituerede piperaziner
HUT68667A (en) * 1990-09-28 1995-07-28 Pfizer Fused ring analogs of nitrogen containing nonaromatic heterocycles
US5138060A (en) * 1991-01-03 1992-08-11 Pfizer Inc. Process and intermediates for preparing azabicyclo(2.2.2)octan-3-imines
EP0566589A1 (en) * 1991-01-10 1993-10-27 Pfizer Inc. N-alkyl quinuclidinium salts as substance p antagonists
US5254569A (en) * 1991-01-14 1993-10-19 The Du Pont Merck Pharmaceutical Company (Amidomethyl)nitrogen heterocyclic analgesics
EP0499313B1 (en) * 1991-02-11 1997-06-11 MERCK SHARP & DOHME LTD. Azabicyclic compounds, pharmaceutical compositions containing them and their use in therapy
EP0600952B1 (en) * 1991-08-20 1996-04-17 MERCK SHARP & DOHME LTD. Azacyclic compounds, processes for their preparation and pharmaceutical compositions containing them
DE69231395T3 (de) * 1991-09-20 2005-07-21 Glaxo Group Ltd., Greenford Neue medizinische Indikation für Tachykinin-Antagonisten
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
IL112778A0 (en) * 1994-03-04 1995-05-26 Merck & Co Inc Substituted heterocycles, their preparation and pharmaceutical compositions containing them

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PL180522B1 (pl) 2001-02-28
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MX9603845A (es) 1997-07-31
BG100798A (bg) 1997-03-31
CO4340689A1 (es) 1996-07-30
US5691336A (en) 1997-11-25
CA2183250A1 (en) 1995-09-08
US5512570A (en) 1996-04-30
NO310074B1 (no) 2001-05-14
FI963450A0 (fi) 1996-09-03
IL112778A0 (en) 1995-05-26
TW385308B (en) 2000-03-21
DE69528823T2 (de) 2003-07-03
DE69528823D1 (en) 2002-12-19
FI963450A7 (fi) 1996-09-03
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AU700611B2 (en) 1999-01-07
US5780467A (en) 1998-07-14
YU14495A (sh) 1999-07-28
ES2184794T3 (es) 2003-04-16
HU9602409D0 (en) 1996-11-28
BR9507046A (pt) 1997-09-09
HUT76324A (en) 1997-08-28
CZ258896A3 (en) 1997-03-12
FR08C0019I2 (fr) 2009-10-30
JP3073770B2 (ja) 2000-08-07
NO963675D0 (no) 1996-09-03
EP0748320B1 (en) 2002-11-13
LV11688A (lv) 1997-02-20
NO963675L (no) 1996-11-04
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US5716942A (en) 1998-02-10
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ATE227722T1 (de) 2002-11-15
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EP0748320A1 (en) 1996-12-18
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