GR3036006T3 - Morpholine derivatives and their use as therapeutic agents - Google Patents

Morpholine derivatives and their use as therapeutic agents

Info

Publication number: GR3036006T3
Authority: GR; Greece
Prior art keywords: 4alkyl; pct; hydrogen; 4alkoxy; hydroxy
Prior art date: 1994-08-15

Application number

GR20010400305T

Other languages

English (en)

Inventor

Timothy Harrison

Andrew Owens

Christopher John Swain

Original Assignee

Merck Sharp & Dohme

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.)

1994-08-15

Filing date

2001-06-07

Publication date

2001-09-28

1994-08-15 Priority claimed from GB9416427A external-priority patent/GB9416427D0/en

1995-05-11 Priority claimed from GBGB9509605.3A external-priority patent/GB9509605D0/en

2001-06-07 Application filed by Merck Sharp & Dohme filed Critical Merck Sharp & Dohme

2001-09-28 Publication of GR3036006T3 publication Critical patent/GR3036006T3/el

Links

239000003814 drug Substances 0.000 title 1
150000002780 morpholines Chemical class 0.000 title 1
229940124597 therapeutic agent Drugs 0.000 title 1
229910052739 hydrogen Inorganic materials 0.000 abstract 4
239000001257 hydrogen Substances 0.000 abstract 4
125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 4
125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 3
125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 2
125000000229 (C1-C4)alkoxy group Chemical group 0.000 abstract 2
125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 2
125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 abstract 2
150000001875 compounds Chemical class 0.000 abstract 2
229910052760 oxygen Inorganic materials 0.000 abstract 2
125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
125000006413 ring segment Chemical group 0.000 abstract 2
229910052717 sulfur Inorganic materials 0.000 abstract 2
241000689227 Cora <basidiomycete fungus> Species 0.000 abstract 1
206010061218 Inflammation Diseases 0.000 abstract 1
208000019695 Migraine disease Diseases 0.000 abstract 1
208000002193 Pain Diseases 0.000 abstract 1
206010036376 Postherpetic Neuralgia Diseases 0.000 abstract 1
206010047700 Vomiting Diseases 0.000 abstract 1
125000003118 aryl group Chemical group 0.000 abstract 1
125000004432 carbon atom Chemical group C* 0.000 abstract 1
125000004122 cyclic group Chemical group 0.000 abstract 1
125000005842 heteroatom Chemical group 0.000 abstract 1
125000000623 heterocyclic group Chemical group 0.000 abstract 1
125000002883 imidazolyl group Chemical group 0.000 abstract 1
230000004054 inflammatory process Effects 0.000 abstract 1
206010027599 migraine Diseases 0.000 abstract 1
230000002265 prevention Effects 0.000 abstract 1
150000003839 salts Chemical class 0.000 abstract 1
229920006395 saturated elastomer Polymers 0.000 abstract 1

Classifications

- 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
- 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
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- 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
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/08—Bridged systems
- 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
- C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
- C07F7/02—Silicon compounds
- C07F7/08—Compounds having one or more C—Si linkages
- C07F7/18—Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
- C07F7/1804—Compounds having Si-O-C linkages

Landscapes

Chemical & Material Sciences (AREA)
Organic Chemistry (AREA)
Health & Medical Sciences (AREA)
General Health & Medical Sciences (AREA)
Veterinary Medicine (AREA)
General Chemical & Material Sciences (AREA)
Medicinal Chemistry (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Chemical Kinetics & Catalysis (AREA)
Pharmacology & Pharmacy (AREA)
Life Sciences & Earth Sciences (AREA)
Animal Behavior & Ethology (AREA)
Public Health (AREA)
Bioinformatics & Cheminformatics (AREA)
Engineering & Computer Science (AREA)
Neurosurgery (AREA)
Pain & Pain Management (AREA)
Biomedical Technology (AREA)
Neurology (AREA)
Rheumatology (AREA)
Hospice & Palliative Care (AREA)
Otolaryngology (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
Plural Heterocyclic Compounds (AREA)
Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

GR20010400305T 1994-08-15 2001-06-07 Morpholine derivatives and their use as therapeutic agents GR3036006T3 (en)

Applications Claiming Priority (3)

Application Number	Priority Date	Filing Date	Title
GB9416427A GB9416427D0 (en)	1994-08-15	1994-08-15	Therapeutic agents
GBGB9509605.3A GB9509605D0 (en)	1995-05-11	1995-05-11	Therapeutic agents
PCT/GB1995/001868 WO1996005181A1 (en)	1994-08-15	1995-08-07	Morpholine derivatives and their use as therapeutic agents

Publications (1)

Publication Number	Publication Date
GR3036006T3 true GR3036006T3 (en)	2001-09-28

Family

ID=26305450

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
GR20010400305T GR3036006T3 (en)	1994-08-15	2001-06-07	Morpholine derivatives and their use as therapeutic agents

Country Status (13)

Country	Link
US (1)	US5824678A (el)
EP (1)	EP0777659B1 (el)
JP (1)	JP2002502351A (el)
AT (1)	ATE201866T1 (el)
AU (1)	AU691327B2 (el)
CA (1)	CA2195972A1 (el)
DE (1)	DE69521208T2 (el)
DK (1)	DK0777659T3 (el)
ES (1)	ES2157337T3 (el)
GR (1)	GR3036006T3 (el)
IL (1)	IL114865A (el)
PT (1)	PT777659E (el)
WO (1)	WO1996005181A1 (el)

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WO1998024446A1 (en) *	1996-12-02	1998-06-11	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
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
EP0942735A1 (en) *	1996-12-02	1999-09-22	MERCK SHARP & DOHME LTD.	Use of nk-1 receptor antagonists for treating schizophrenic disorders
WO1998024444A1 (en) *	1996-12-02	1998-06-11	Merck Sharp & Dohme Limited	Use of nk-1 receptor antagonists for treating substance use disorders
EP0942728A1 (en) *	1996-12-02	1999-09-22	MERCK SHARP & DOHME LTD.	Use of nk-1 receptor antagonists for treating sexual dysfunction
US6100256A (en) *	1996-12-02	2000-08-08	Merck Sharp & Dohme Ltd.	Use of NK-1 receptors antagonists for treating schizophrenic disorders
WO1998024443A1 (en) *	1996-12-02	1998-06-11	Merck Sharp & Dohme Limited	Use of nk-1 receptor antagonists for treating bipolar disorders
US5977104A (en) *	1996-12-02	1999-11-02	Merck Sharp & Dohme Ltd.	Use of NK-1 receptor antagonists for treating bipolar disorders
PT942729E (pt) *	1996-12-02	2004-12-31	Merck Sharp & Dohme	Utilizacao de antagonistas de receptores nk-1 para tratamento de doencas do stresse
CA2287487A1 (en) *	1997-04-24	1998-10-29	Merck Sharp & Dohme Limited	Use of nk-1 receptor antagonists for treating eating disorders
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
CA2298779A1 (en) *	1997-08-04	1999-02-18	Merck Sharp & Dohme Limited	Use of nk-1 receptor antagonists for treating aggressive behaviour disorders
CA2298777A1 (en) *	1997-08-04	1999-02-18	Merck Sharp & Dohme Limited	Use of nk-1 receptor antagonists for treating mania
US6087348A (en) *	1997-12-01	2000-07-11	Merck Sharp & Dohme Ltd.	Use of NK-1 receptor antagonists for treating stress disorders
US6156749A (en) *	1997-12-01	2000-12-05	Merck Sharp & Dohme Limited	Use of NK-1 receptor antagonists for treating movement disorders
US6271230B1 (en)	1997-12-01	2001-08-07	Merck Sharp & Dohme Limited	Use of NK-1 receptor antagonists for treating cognitive disorders
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GB9907571D0 (en)	1999-04-06	1999-05-26	Zeneca Ltd	Compounds
DK1246806T3 (da)	1999-11-03	2008-06-16	Amr Technology Inc	Aryl- og heteroarylsubstituerede tetrahydroisoquinoliner og anvendelse deraf til blokering af genoptagelse af norepinefrin, dopsmin og serotonin
US7163949B1 (en)	1999-11-03	2007-01-16	Amr Technology, Inc.	4-phenyl substituted tetrahydroisoquinolines and use thereof
US7279547B2 (en) *	2000-02-10	2007-10-09	University Of Connecticut	Insecticidal compounds and methods for selection thereof
WO2001068622A1 (en)	2000-03-13	2001-09-20	Ortho-Mcneil Pharmaceutical, Inc.	Novel cyclobutene derivatives useful as antagonists of the motilin receptor
WO2001068621A1 (en)	2000-03-13	2001-09-20	Ortho-Mcneil Pharmaceutical, Inc.	Novel cyclohexene derivatives useful as antagonists of the motilin receptor
WO2001068620A1 (en)	2000-03-13	2001-09-20	Ortho-Mcneil Pharmaceutical, Inc.	Novel cyclopentene derivatives useful as antagonists of the motilin receptor
MXPA03000275A (es)	2000-07-11	2004-12-13	Albany Molecular Res Inc	Nuevas tetrahidroisoquinolinas substituidas con 4-fenilo y su uso terapeutico.
AU2003243353A1 (en) *	2002-05-29	2003-12-19	The Regents Of The University Of California	Antagonizing nk1 receptors inhibits consumption of substances of abuse
UA91341C2 (ru)	2004-07-15	2010-07-26	Амр Текнолоджи, Інк.	Арил- и гетероарилзамещенные тетрагидроизохинолины и их применение для блокирования обратного захвата норэпинефрина, допамина и серотонина
ATE550019T1 (de)	2005-05-17	2012-04-15	Merck Sharp & Dohme	Cis-4-ä(4-chlorophenyl)sulfonylü-4-(2,5- difluorophenyl)cyclohexanepropansäure zur behandlug von krebs
US7956050B2 (en)	2005-07-15	2011-06-07	Albany Molecular Research, Inc.	Aryl- and heteroaryl-substituted tetrahydrobenzazepines and use thereof to block reuptake of norepinephrine, dopamine, and serotonin
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GB0603041D0 (en)	2006-02-15	2006-03-29	Angeletti P Ist Richerche Bio	Therapeutic compounds
AU2007300627B2 (en)	2006-09-22	2012-02-16	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
BRPI0806245B1 (pt)	2007-01-10	2022-01-25	Msd Italia S.R.L.	Compostos de fórmula i e seus usos
US8093268B2 (en)	2007-01-24	2012-01-10	Glaxo Group Limited	Pharmaceutical compositions comprising 2-methoxy-5-(5-trifluoromethyl-tetrazol-1-yl-benzyl)-(2S-phenylpiperidin-3S-yl-)
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WO2009002495A1 (en)	2007-06-27	2008-12-31	Merck & Co., Inc.	4-carboxybenzylamino derivatives as histone deacetylase inhibitors
US8598184B2 (en)	2008-03-03	2013-12-03	Tiger Pharmatech	Protein kinase inhibitors
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
EP2413932A4 (en)	2009-04-01	2012-09-19	Merck Sharp & Dohme	HAMMER OF ACT ACTIVITY
JP5739415B2 (ja)	2009-05-12	2015-06-24	ブリストル−マイヤーズスクウィブカンパニー	（Ｓ）−７−（［１，２，４］トリアゾロ［１，５−ａ］ピリジン−６−イル）−４−（３，４−ジクロロフェニル）−１，２，３，４−テトラヒドロイソキノリンの結晶形態およびその使用
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CN102595902B (zh)	2009-05-12	2015-04-29	阿尔巴尼分子研究公司	7-([1,2,4]三唑并[1,5-a]吡啶-6-基)-4-(3,4-二氯苯基)-1,2,3,4-四氢异喹啉及其用途
CA2777043C (en)	2009-10-14	2015-12-15	Schering Corporation	Substituted piperidines that increase p53 activity and the uses thereof
EP2584903B1 (en)	2010-06-24	2018-10-24	Merck Sharp & Dohme Corp.	Novel heterocyclic compounds as erk inhibitors
CN103068980B (zh)	2010-08-02	2017-04-05	瑟纳治疗公司	使用短干扰核酸（siNA）的RNA干扰介导的联蛋白（钙粘蛋白关联蛋白质），β1（CTNNB1）基因表达的抑制
RU2745848C2 (ru)	2010-08-17	2021-04-01	Сирна Терапьютикс, Инк.	ОПОСРЕДУЕМОЕ РНК-ИНТЕРФЕРЕНЦИЕЙ ИНГИБИРОВАНИЕ ЭКСПРЕССИИ ГЕНОВ ВИРУСА ГЕПАТИТА B (HBV) С ПРИМЕНЕНИЕМ МАЛОЙ ИНТЕРФЕРИРУЮЩЕЙ НУКЛЕИНОВОЙ КИСЛОТЫ (миНК)
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)
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WO2012143879A1 (en)	2011-04-21	2012-10-26	Piramal Healthcare Limited	A crystalline form of a salt of a morpholino sulfonyl indole derivative and a process for its preparation
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SMT201700595T1 (it)	2012-11-28	2018-03-08	Merck Sharp & Dohme	Composizioni e metodi per trattare il cancro
WO2014100065A1 (en)	2012-12-20	2014-06-26	Merck Sharp & Dohme Corp.	Substituted imidazopyridines as hdm2 inhibitors
WO2014120748A1 (en)	2013-01-30	2014-08-07	Merck Sharp & Dohme Corp.	2,6,7,8 substituted purines as hdm2 inhibitors
WO2015034925A1 (en)	2013-09-03	2015-03-12	Moderna Therapeutics, Inc.	Circular polynucleotides
US10975084B2 (en)	2016-10-12	2021-04-13	Merck Sharp & Dohme Corp.	KDM5 inhibitors
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EP3706742B1 (en)	2017-11-08	2023-03-15	Merck Sharp & Dohme LLC	Prmt5 inhibitors
CA3108388A1 (en)	2018-08-07	2020-02-13	Merck Sharp & Dohme Corp.	Prmt5 inhibitors
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EP3833667B1 (en)	2018-08-07	2024-03-13	Merck Sharp & Dohme LLC	Prmt5 inhibitors
CN111004190A (zh) *	2019-11-08	2020-04-14	广州曼翔医药有限公司	一种阿瑞匹坦中间体的制备方法

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CA2112397A1 (en) *	1991-08-20	1993-03-04	Raymond Baker	Azacyclic compounds, processes for their preparation and pharmaceutical compositions containing them
CA2099233A1 (en) *	1992-06-29	1993-12-30	Conrad P. Dorn	Morpholine and thiomorpholine tachykinin receptor antagonists
IL111960A (en) *	1993-12-17	1999-12-22	Merck & Co Inc	Morpholines and thiomorpholines their preparation and pharmaceutical compositions containing them
IL112134A (en) *	1993-12-29	1999-12-22	Merck Sharp & Dohme	Substituted morpholine derivatives their preparation and pharmaceutical compositions containing them

1995
- 1995-08-07 ES ES95927862T patent/ES2157337T3/es not_active Expired - Lifetime
- 1995-08-07 CA CA002195972A patent/CA2195972A1/en not_active Abandoned
- 1995-08-07 WO PCT/GB1995/001868 patent/WO1996005181A1/en not_active Ceased
- 1995-08-07 PT PT95927862T patent/PT777659E/pt unknown
- 1995-08-07 DK DK95927862T patent/DK0777659T3/da active
- 1995-08-07 JP JP50710696A patent/JP2002502351A/ja not_active Withdrawn
- 1995-08-07 EP EP95927862A patent/EP0777659B1/en not_active Expired - Lifetime
- 1995-08-07 AT AT95927862T patent/ATE201866T1/de not_active IP Right Cessation
- 1995-08-07 AU AU31855/95A patent/AU691327B2/en not_active Ceased
- 1995-08-07 US US08/793,186 patent/US5824678A/en not_active Expired - Fee Related
- 1995-08-07 DE DE69521208T patent/DE69521208T2/de not_active Expired - Fee Related
- 1995-08-08 IL IL11486595A patent/IL114865A/xx active IP Right Grant
2001
- 2001-06-07 GR GR20010400305T patent/GR3036006T3/el not_active IP Right Cessation

Also Published As

Publication number	Publication date
ES2157337T3 (es)	2001-08-16
EP0777659B1 (en)	2001-06-06
DE69521208D1 (de)	2001-07-12
WO1996005181A1 (en)	1996-02-22
AU3185595A (en)	1996-03-07
JP2002502351A (ja)	2002-01-22
IL114865A0 (en)	1995-12-08
DE69521208T2 (de)	2001-11-08
ATE201866T1 (de)	2001-06-15
US5824678A (en)	1998-10-20
EP0777659A1 (en)	1997-06-11
PT777659E (pt)	2001-09-28
DK0777659T3 (da)	2001-09-03
AU691327B2 (en)	1998-05-14
IL114865A (en)	1999-06-20
CA2195972A1 (en)	1996-02-22

Legal Events

Date	Code	Title	Description
2003-03-05	ML	Lapse due to non-payment of fees

Publication	Publication Date	Title
AU3185595A (en)	1996-03-07	Morpholine derivatives and their use as therapeutic agents
GB9426103D0 (en)	1995-02-22	Therapeutic agents
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