PE20010741A1 - Derivados de piperazina como antagonistas de taquicininas - Google Patents

Derivados de piperazina como antagonistas de taquicininas

Info

Publication number
PE20010741A1
PE20010741A1 PE2000001068A PE0010682000A PE20010741A1 PE 20010741 A1 PE20010741 A1 PE 20010741A1 PE 2000001068 A PE2000001068 A PE 2000001068A PE 0010682000 A PE0010682000 A PE 0010682000A PE 20010741 A1 PE20010741 A1 PE 20010741A1
Authority
PE
Peru
Prior art keywords
alkyl
members
tachycinins
antagonists
methyl
Prior art date
Application number
PE2000001068A
Other languages
English (en)
Inventor
Giuseppe Alvaro
Giuseppe Guercio
Yves St-Denis
Fabio Romano Di
Antonella Ursini
Riccardo Giovannini
Original Assignee
Glaxo Group Ltd
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
Application filed by Glaxo Group Ltd filed Critical Glaxo Group Ltd
Publication of PE20010741A1 publication Critical patent/PE20010741A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/13—Amines
    • A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/196—Carboxylic acids, e.g. valproic acid having an amino group the amino group being directly attached to a ring, e.g. anthranilic acid, mefenamic acid, diclofenac, chlorambucil
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
    • 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
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/06—Antimigraine agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/22—Anxiolytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • 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
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/32—Alcohol-abuse
    • 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
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/34—Tobacco-abuse
    • 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
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36—Opioid-abuse
    • 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]
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/04—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms

Abstract

SE REFIERE A DERIVADOS DE PIPERAZINA DE FORMULA I, DONDE R ES HALOGENO, ALQUILO C1-C4; R1 ES H, ALQUILO C1-C4; R2 ES H, ALQUILO C1-C4, ALQUENILO C2-C6, CICLOALQUILO C3-C7; R1 Y R2 JUNTO CON N FORMAN UN HETEROCICLO DE 5-6 MIEMBROS; R3 ES TRIFLUOROMETILO, ALQUILO C1-C4, ALCOXILO C1-C4, TRIFLUOROMETOXI, HALOGENO; R4 ES H, (CH2)qR7, (CH2)rCO(CH2)pR7; R5 ES H, ALQUILO C1-C4, COR6; R6 ES H, OH, AMINO, METILAMINO, DIMETILAMINO, HETEROARILO DE 5 MIEMBROS CON 1-3 O, S, N; HETEROARILO DE 6 MIEMBROS CON 1-3 N; R7 ES H, OH, NR8R9; R8 Y R9 SON H, ALQUILO C1-C4 OPCIONALMENTE SUSTITUIDO POR OH, AMINO; R10 ES H, ALQUILO C1-C4; R10 Y R2 SON CICLOALQUILO C3-C7; m Y n SON 0-3; p Y r SON 0-4; q ES 1-4; CUANDO R1 Y R2 JUNTO CON N Y C FORMAN UN HETEROCICLO DE 5-6 MIEMBROS; i)m ES 1-2; ii)CUANDO m ES 1; R NO ES F; iii)CUANDO m ES 2, LOS DOS R NO SON F. SON COMPUESTOS PREFERIDOS (3,5-BIS-TRIFLUOROMETIL-BENCIL)METIL-AMIDA DEL ACIDO 2-(4-FLUORO-2-METIL-FENIL)-PIPERAZIN-1-CARBOXILICO, CLORHIDRATO DE (3,5-BIS-TRIFLUORO-BENCIL)-METIL-AMIDA DEL ACIDO 2-(S)-(4-FLUORO-2-METIL-FENIL)-4-(PIPERIN-4-CARBONIL)-PIPERAZINA-1-CARBOXILICO. TAMBIEN SE REFIERE A UN PROCEDIMIENTO PARA LA PREPARACION. LOS COMPUESTOS SON ANTAGONISTAS DE TAQUICININAS (SUSTANCIA P, NEUROCININAS) Y PUEDEN SER UTIL PARA EL TRATAMIENTO DE LA DEPRESION, ANSIEDAD, PANICO
PE2000001068A 1999-10-07 2000-10-06 Derivados de piperazina como antagonistas de taquicininas PE20010741A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
GBGB9923748.9A GB9923748D0 (en) 1999-10-07 1999-10-07 Chemical compounds

Publications (1)

Publication Number Publication Date
PE20010741A1 true PE20010741A1 (es) 2001-07-18

Family

ID=10862304

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2000001068A PE20010741A1 (es) 1999-10-07 2000-10-06 Derivados de piperazina como antagonistas de taquicininas

Country Status (33)

Country Link
US (6) US6951861B1 (es)
EP (3) EP1218359B1 (es)
JP (1) JP4776844B2 (es)
KR (2) KR100817373B1 (es)
CN (1) CN100413850C (es)
AR (2) AR025975A1 (es)
AT (3) ATE407125T1 (es)
AU (1) AU768780B2 (es)
BR (1) BR0014541A (es)
CA (1) CA2386515C (es)
CO (1) CO5251467A1 (es)
CY (2) CY1110172T1 (es)
CZ (1) CZ302340B6 (es)
DE (3) DE60042501D1 (es)
DK (3) DK1218359T3 (es)
ES (3) ES2312917T3 (es)
GB (1) GB9923748D0 (es)
HK (3) HK1052506B (es)
HU (1) HUP0203136A3 (es)
IL (2) IL148964A0 (es)
MX (1) MXPA02003515A (es)
MY (1) MY130907A (es)
NO (1) NO323776B1 (es)
NZ (2) NZ518144A (es)
PE (1) PE20010741A1 (es)
PL (1) PL201191B1 (es)
PT (3) PT1218359E (es)
SI (3) SI1454901T1 (es)
TN (1) TNSN00194A1 (es)
TR (1) TR200200936T2 (es)
TW (1) TWI225485B (es)
WO (1) WO2001025219A2 (es)
ZA (1) ZA200202589B (es)

Families Citing this family (43)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2002537245A (ja) * 1999-02-18 2002-11-05 ノバルティス アクチエンゲゼルシャフト ５−ｈｔ３レセプターアンタゴニストの使用
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
AUPQ514600A0 (en) * 2000-01-18 2000-02-10 James Cook University Brain injury treatment
GB0003232D0 (en) * 2000-02-11 2000-04-05 Smithkline Beecham Plc Novel composition
GB0025354D0 (en) 2000-10-17 2000-11-29 Glaxo Group Ltd Chemical compounds
GB0108595D0 (en) 2001-04-05 2001-05-23 Glaxo Group Ltd Chemical compounds
GB0108594D0 (en) * 2001-04-05 2001-05-23 Glaxo Group Ltd Chemical compounds
US20030083345A1 (en) * 2001-07-10 2003-05-01 Torsten Hoffmann Method of treatment and/or prevention of brain, spinal or nerve injury
GB0119797D0 (en) * 2001-08-14 2001-10-03 Glaxo Group Ltd Chemical compounds
GB0124463D0 (en) 2001-10-11 2001-12-05 Smithkline Beecham Plc Compounds
GB0203020D0 (en) 2002-02-08 2002-03-27 Glaxo Group Ltd Chemical compounds
GB0203022D0 (en) * 2002-02-08 2002-03-27 Glaxo Group Ltd Chemical compounds
US7482365B2 (en) 2002-02-08 2009-01-27 Glaxo Group Limited Piperidylcarboxamide derivatives and their use in the treatment of tachykinin-mediated diseases
DE10209145A1 (de) * 2002-03-01 2003-09-04 Bayer Cropscience Ag Halogenbenzole
AU2003243353A1 (en) * 2002-05-29 2003-12-19 The Regents Of The University Of California Antagonizing nk1 receptors inhibits consumption of substances of abuse
JP4079727B2 (ja) * 2002-09-06 2008-04-23 セントラル硝子株式会社 光学活性１−（フルオロ、トリフルオロメチルまたはトリフルオロメトキシ置換フェニル）アルキルアミンｎ−モノアルキル誘導体とその製造方法
WO2004067093A2 (en) * 2003-01-27 2004-08-12 Glaxo Group Limited Nk1 receptor antagonists for the treatment of functional dyspepsia
GB0308968D0 (en) * 2003-04-17 2003-05-28 Glaxo Group Ltd Medicaments
MXPA05013770A (es) * 2003-06-19 2006-03-08 Pfizer Prod Inc Antagonista de neuroquinina 1.
US20070142367A1 (en) * 2003-11-10 2007-06-21 Lundeen James E Method and medicine for treating gastrointestinal disorder including fecal incontinence
US20060148783A1 (en) * 2003-11-10 2006-07-06 Lundeen James E Method and medicine for treating gastrointestinal disorder including fecal incontinence
US20060148781A1 (en) * 2003-11-10 2006-07-06 Lundeen James E Method and medicine for treating gastrointestinal disorder in a non-human mammal
US20050113365A1 (en) * 2003-11-10 2005-05-26 Sir Isaac Newton Enterprises Llc Method and medicine for treating gastrointestinal disorder including irritable bowel syndrome
US20060148782A1 (en) * 2003-11-10 2006-07-06 Lundeen James E Method and medicine for treating a mammal presenting urinary incontinence, urinary urgency, or both
JPWO2005051912A1 (ja) * 2003-11-28 2007-12-06 田辺三菱製薬株式会社 ピペリジン化合物およびその製法
EP1705176A4 (en) * 2004-01-14 2009-06-03 Takeda Pharmaceutical CARBOXYLAMIDE DERIVATIVE AND ITS USE
TW200730494A (en) * 2005-10-10 2007-08-16 Glaxo Group Ltd Novel compounds
US7855218B2 (en) * 2005-10-10 2010-12-21 Convergence Pharmaceuticals Limited Compounds
US20100009983A1 (en) * 2006-05-09 2010-01-14 Braincells, Inc. 5 ht receptor mediated neurogenesis
JP4904945B2 (ja) 2006-06-30 2012-03-28 セントラル硝子株式会社 光学活性１−（フルオロ、トリフルオロメチルまたはトリフルオロメトキシ置換フェニル）アルキルアミンｎ−モノアルキル誘導体の製造方法
GB0621229D0 (en) * 2006-10-20 2006-12-06 Glaxo Group Ltd Novel use
EP2129381A1 (en) 2007-01-24 2009-12-09 Glaxo Group Limited Pharmaceutical compositions comprising 3, 5-diamin0-6- (2, 3-dichl0phenyl) -l, 2, 4-triazine or r (-) -2, 4-diamino-5- (2, 3-dichlorophenyl) -6-fluoromethyl pyrimidine and an nk1
JP5510040B2 (ja) * 2010-04-28 2014-06-04 セントラル硝子株式会社 光学活性（ｒ）−１−（４−フルオロフェニル）エチルアミンを得る光学分割
WO2012175434A1 (en) 2011-06-20 2012-12-27 Glaxo Group Limited Pharmaceutical formulations comprising vestipitant
ES2672099T3 (es) 2011-07-04 2018-06-12 Irbm - Science Park S.P.A. Antagonistas del receptor NK-1 para el tratamiento de la neovascularización corneal
KR20140122764A (ko) * 2012-02-22 2014-10-20 레오 파마 에이/에스 신규한 뉴로키닌 1 수용체 길항제 화합물
WO2015024203A1 (en) * 2013-08-20 2015-02-26 Leo Pharma A/S Novel neurokinin 1 receptor antagonist compounds ii
ES2912881T3 (es) 2014-12-23 2022-05-30 Convergence Pharmaceuticals Procedimiento para preparar derivados de alfa-carboxamida pirrolidina
US10399949B2 (en) 2015-12-07 2019-09-03 Kissei Pharmaceutical Co., Ltd. NK1 receptor antagonist
AU2018251604B2 (en) 2017-04-10 2022-04-14 Chase Therapeutics Corporation NK1-antagonist combination and method for treating synucleinopathies
EP3645120A4 (en) 2017-06-30 2021-03-24 Chase Pharmaceuticals Corporation NK-1 ANTAGONIST COMPOSITIONS AND METHODS OF USE IN THE TREATMENT OF DEPRESSION
KR20200061381A (ko) 2017-10-05 2020-06-02 바이오젠 인크. 알파-카르복스아미드 피롤리딘 유도체를 제조하기 위한 공정

Family Cites Families (55)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4110327A (en) 1974-05-09 1978-08-29 Toyama Chemical Co., Ltd. 2,3 Diketo-piperazinocarbonylamino alkanoic acids and derivatives
US4112090A (en) 1974-05-09 1978-09-05 Toyama Chemical Co., Ltd. Novel penicillins and cephalosporins and process for producing the same
US4219554A (en) 1974-05-09 1980-08-26 Toyama Chemical Company, Limited Novel penicillins and cephalosporins and process for producing same
US4379152A (en) 1974-05-09 1983-04-05 Toyama Chemical Co., Ltd. Cephalosporins
US4087424A (en) 1974-05-09 1978-05-02 Toyama Chemical Co., Ltd. Novel penicillins and cephalosporins and process for producing the same
US4410522A (en) 1974-05-09 1983-10-18 Toyama Chemical Co., Ltd. Cephalosporins
US4327097A (en) 1974-05-09 1982-04-27 Toyama Chemical Co., Ltd. Novel penicillins
IL47168A (en) 1974-05-09 1979-07-25 Toyama Chemical Co Ltd Mono or dioxo piperazino(thio)carbonylamino derivatives ofpenicillins and cephalosporins and process for producing the same
NO154582C (no) * 1978-10-20 1986-11-05 Ferrosan Ab Analogifremgangsmaate for fremstilling av terapeutisk aktive difenyl-dibutylpiperazinkarboksamider.
JPS57118587A (en) 1981-11-26 1982-07-23 Toyama Chem Co Ltd Novel penicillin
US5028610A (en) 1987-03-18 1991-07-02 Sankyo Company Limited N-benzhydryl-substituted heterocyclic derivatives, their preparation and their use
GB8709666D0 (en) 1987-04-23 1987-05-28 Beecham Group Plc Compounds
GB8713061D0 (en) 1987-06-04 1987-07-08 Beecham Group Plc Compounds
US5109014A (en) 1990-12-10 1992-04-28 Jacobson Richard M N-aryl-3-aryl-4-substituted-2,3,4,5-tetrahydro-1H-pyrazole-1-carboxamides
SE9100860D0 (sv) 1991-03-22 1991-03-22 Kabi Pharmacia Ab New use
ES2149767T5 (es) 1991-09-20 2005-06-16 Glaxo Group Limited Nuevo uso medico para antagonistas de taquiquininas.
EP0545478A1 (en) 1991-12-03 1993-06-09 MERCK SHARP & DOHME LTD. Heterocyclic compounds as tachykinin antagonists
US5563127A (en) 1993-03-24 1996-10-08 The Dupont Merck Pharmaceutical Company Boronic acid and ester inhibitors of thrombin
US5348955A (en) 1993-06-22 1994-09-20 Merck & Co., Inc. N,N-diacylpiperazines
IL111730A (en) 1993-11-29 1998-12-06 Fujisawa Pharmaceutical Co Piperazine derivatives, processes for their preparation and pharmaceutical preparations containing them
TW385308B (en) 1994-03-04 2000-03-21 Merck & Co Inc Prodrugs of morpholine tachykinin receptor antagonists
US5464788A (en) 1994-03-24 1995-11-07 Merck & Co., Inc. Tocolytic oxytocin receptor antagonists
DE4425146A1 (de) 1994-07-15 1996-01-18 Basf Ag Verwendung heterocyclischer Verbindungen
AU3085895A (en) 1994-07-26 1996-02-22 Sankyo Company Limited N-phenylated amide and urea derivatives
DE19520499C2 (de) 1994-09-17 2003-06-18 Boehringer Ingelheim Kg Neurokinin-Antagonisten, Verfahren zu ihrer Herstellung, diese Verbindungen enthaltende pharmazeutische Zusammensetzungen sowie ihre Verwendung
US5696123A (en) 1994-09-17 1997-12-09 Boehringer Ingelheim Kg Neurokinin antagonists
US5998444A (en) 1995-10-24 1999-12-07 Zeneca Ltd. Piperidinyl compounds as NK1 or NK2 antagonists
DE69534213T2 (de) 1994-10-25 2006-01-12 Astrazeneca Ab Therapeutisch wirksame Heterocyclen
US5629322A (en) 1994-11-15 1997-05-13 Merck & Co., Inc. Cyclic amidine analogs as inhibitors of nitric oxide synthase
US5576317A (en) 1994-12-09 1996-11-19 Pfizer Inc. NK-1 receptor antagonists and 5HT3 receptor antagonists for the treatment of emesis
EE9700141A (et) 1994-12-23 1997-12-15 Dr. Karl Thomae Gmbh Piperasiinderivaadid, neid sisaldavad ravimid, nende kasutamine ja valmistamise meetod
US5700801A (en) 1994-12-23 1997-12-23 Karl Thomae, Gmbh Piperazine derivatives, pharmaceutical compositions containing these compounds, their use and processes for preparing them
NZ321575A (en) 1995-10-30 1999-05-28 Janssen Pharmaceutica Nv 1-(1,2-disubstituted piperidinyl)-4- substituted piperazine derivatives
DE19608665A1 (de) 1996-03-06 1997-09-11 Boehringer Ingelheim Kg Neue Arylglycinamidderivate, Verfahren zu ihrer Herstellung und diese Verbindungen enthaltende pharmazeutische Zusammensetzungen
US6057323A (en) 1996-03-08 2000-05-02 Adolor Corporation Kappa agonist compounds pharmaceutical formulations and method of prevention and treatment of pruritus therewith
US5859012A (en) 1996-04-03 1999-01-12 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
WO1997036593A1 (en) * 1996-04-03 1997-10-09 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
WO1997036888A1 (en) 1996-04-03 1997-10-09 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
AU707139B2 (en) 1996-04-03 1999-07-01 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
AU3359697A (en) 1996-07-08 1998-02-02 Yamanouchi Pharmaceutical Co., Ltd. Bone resorption inhibitors
AU3716997A (en) * 1996-07-17 1998-02-09 Merck & Co., Inc. Alteration of circadian rhythmicity with a tachykinin antagonist
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
US5929077A (en) 1996-11-08 1999-07-27 Leftheris; Katerina Thioproline-containing inhibitors of farnesyl protein transferase
US5977104A (en) 1996-12-02 1999-11-02 Merck Sharp & Dohme Ltd. Use of NK-1 receptor antagonists for treating bipolar disorders
JP2001504852A (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 双極性障害の治療のための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
AUPO735997A0 (en) 1997-06-17 1997-07-10 Fujisawa Pharmaceutical Co., Ltd. Piperazine derivatives
EP1014984A1 (en) 1997-08-27 2000-07-05 Merck & Co., Inc. Inhibitors of prenyl-protein transferase
EP1034164B1 (en) 1997-11-24 2004-05-19 Merck & Co., Inc. Substituted beta-alanine derivatives as cell adhesion inhibitors
KR20010086104A (ko) * 1998-12-14 2001-09-07 후지야마 아키라 피페라진 유도체
GB9923748D0 (en) * 1999-10-07 1999-12-08 Glaxo Group Ltd Chemical compounds
AU7788500A (en) * 1999-10-25 2001-05-08 Janssen Pharmaceutica N.V. Use of substance p antagonists for influencing the circadian timing system
GB0025354D0 (en) 2000-10-17 2000-11-29 Glaxo Group Ltd Chemical compounds
US20030022891A1 (en) 2000-12-01 2003-01-30 Anandan Palani MCH antagonists and their use in the treatment of obesity
MY141736A (en) 2002-10-08 2010-06-15 Elanco Animal Health Ireland Substituted 1,4-di-piperidin-4-yi-piperazine derivatives and their use as neurokinin antagonists

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