BR0306148A - Compostos, composições farmacêuticas, e, uso de um composto - Google Patents

Compostos, composições farmacêuticas, e, uso de um composto

Info

Publication number
BR0306148A
BR0306148A BR0306148-5A BR0306148A BR0306148A BR 0306148 A BR0306148 A BR 0306148A BR 0306148 A BR0306148 A BR 0306148A BR 0306148 A BR0306148 A BR 0306148A
Authority
BR
Brazil
Prior art keywords
morpholin
compounds
pharmaceutical compositions
compound
indolyl
Prior art date
Application number
BR0306148-5A
Other languages
English (en)
Inventor
Dirk De Boer
Hein K A C Coolen
Mayke B Hesselink
Wouter I Iwema Bakker
Gijsbert D Kuil
Jan H Van Maarseveen
Andrew C Mccreary
Gustaaf J M Scharrenburg
Original Assignee
Solvay Pharm Bv
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 Solvay Pharm Bv filed Critical Solvay Pharm Bv
Publication of BR0306148A publication Critical patent/BR0306148A/pt

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • 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
    • A61P11/06—Antiasthmatics
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/16—Central respiratory analeptics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/10—Drugs for disorders of the urinary system of the bladder
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/04—Antipruritics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • 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
    • 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
    • A61P25/04—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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/16—Otologicals
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/10—Antioedematous agents; Diuretics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • 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
    • C07D487/04—Ortho-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Pulmonology (AREA)
  • Dermatology (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Cardiology (AREA)
  • Urology & Nephrology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Immunology (AREA)
  • Rheumatology (AREA)
  • Vascular Medicine (AREA)
  • Diabetes (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Hematology (AREA)
  • Otolaryngology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

"COMPOSTOS, COMPOSIçõES FARMACêUTICAS, E, USO DE UM COMPOSTO". A presente invenção refere-se a um grupo de derivados de diazabiciclo alcano únicos, tendo interessante atividade antagonística a receptor de neurocinina-NK~ 1~, representado pela Fórmula Geral (1) em que: R^ 1^ representa fenila, 2-indolila, 3-indolila, 3-indazolila ou benzo[b]tiofen-3-ila, grupos estes podendo ser substituídos por halogênio ou alquila (1 -3C), R^ 2^ e R^ 3^ representam, independentemente, halogênio, H, OCH~ 3~, CH~ 3~ e CF~ 3~, R^ 4^, R^ 5^ e R^ 6^ representam, independentemente, H, OH, O-alquila(1-4C), CH~ 2~OH, NH~ 2~, dialquila(1-3C)N, pirrolidin-1-ila, piperidin-1-ila, morfolin-4-ila ou morfolin-4-ila, substituída com um ou dois grupos metila ou metoximetila, morfolin-4-ilamino, morfolin-4-ilmetila, imidazol-1-ila, tiomorfolin-4-ila, 1-dioxotiomorfolin-4-ila ou 3-oxa-8-azabiciclo[3.2.1]oct-8-ila; R^ 4^ e R^ 5^, juntos, podem representar um grupo ceto, 1,3-dioxan-2-ila ou 1,3-dioxoloan-2-ila, X representa O ou S, n tem o valor de 1, 2 ou 3, a é o átomo de carbono assimétrico 8a, 9a ou 10a, quando n igualar 1, 2 ou 3, respectivamente. A invenção também refere-se a um método para a preparação dos novos compostos e a composições farmacêuticas contendo pelo menos um destes compostos como ingrediente ativo.
BR0306148-5A 2002-04-04 2003-04-02 Compostos, composições farmacêuticas, e, uso de um composto BR0306148A (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP02076405 2002-04-04
PCT/EP2003/050086 WO2003084955A1 (en) 2002-04-04 2003-04-02 Diazabicyclo alkane derivatives with nk1 antagonistic activity

Publications (1)

Publication Number Publication Date
BR0306148A true BR0306148A (pt) 2004-10-19

Family

ID=28685940

Family Applications (1)

Application Number Title Priority Date Filing Date
BR0306148-5A BR0306148A (pt) 2002-04-04 2003-04-02 Compostos, composições farmacêuticas, e, uso de um composto

Country Status (21)

Country Link
US (1) US7202238B2 (pt)
EP (1) EP1495022B1 (pt)
JP (1) JP2005525395A (pt)
KR (1) KR20040095361A (pt)
CN (1) CN1279041C (pt)
AR (1) AR039192A1 (pt)
AT (1) ATE435863T1 (pt)
AU (1) AU2003224162B2 (pt)
BR (1) BR0306148A (pt)
CA (1) CA2462708A1 (pt)
DE (1) DE60328272D1 (pt)
HK (1) HK1070356A1 (pt)
HR (1) HRP20040273A2 (pt)
IL (2) IL160943A0 (pt)
MX (1) MXPA04004812A (pt)
NO (1) NO20044775L (pt)
PL (1) PL371378A1 (pt)
RU (1) RU2310656C2 (pt)
UA (1) UA77515C2 (pt)
WO (1) WO2003084955A1 (pt)
ZA (1) ZA200404744B (pt)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
SA04250304B1 (ar) * 2003-09-26 2009-03-11 سولفاي فارماسوتيكالز بي . في مشتقات هكسا - واوكتاهيدرو - بيريدو {1،2-a} بيرازين ذات نشاط مضاد لـ nk1
WO2006013205A1 (en) * 2004-08-04 2006-02-09 Solvay Pharmaceuticals B.V. Neurokinin-1 receptor antagonists for the treatment of conditions responsive to testosterone elevation
DE102006049452A1 (de) * 2006-10-17 2008-05-08 Grünenthal GmbH Substituierte Tetrahydropyrolopiperazin-Verbindungen und deren Verwendung in Arzneimitteln
WO2010011912A1 (en) * 2008-07-25 2010-01-28 Smithkline Beecham Corporation Trpv4 antagonists
EP2312947B1 (en) * 2008-07-25 2014-01-01 GlaxoSmithKline LLC Trpv4 antagonists
WO2013049174A1 (en) 2011-09-29 2013-04-04 Abbvie Inc. Substituted octahydropyrrolo[1,2-a]pyrazine sulfonamides as calcium channel blockers
WO2013049164A1 (en) * 2011-09-29 2013-04-04 Abbvie Inc. SUBSTITUTED OCTAHYDROPYRROLO[1,2-a]PYRAZINES AS CALCIUM CHANNEL BLOCKERS
US9181259B2 (en) * 2012-02-22 2015-11-10 Leo Pharma A/S Substituted pyrrolo[1,2-a]piperazines and pyrrolo[1,2-a][1,4]diazepines as neurokinin 1 receptor antagonists
BR112015013948A2 (pt) 2012-12-12 2017-07-11 Abbvie Inc derivados diazepínicos úteis como bloqueadores do canal de cálcio no tratamento de dor
WO2015013397A2 (en) * 2013-07-25 2015-01-29 Neuren Pharmaceuticals Limited Neuroprotective bicyclic compounds and methods for their use in treating autism spectrum disorders and neurodevelopmental disorders
WO2015024203A1 (en) * 2013-08-20 2015-02-26 Leo Pharma A/S Novel neurokinin 1 receptor antagonist compounds ii
ES2966369T3 (es) 2017-03-20 2024-04-22 Broad Inst Inc Compuestos y métodos para el tratamiento de enfermedades parasitarias

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1125112A (en) * 1966-01-07 1968-08-28 Science Union & Cie New derivatives of diazabicyclo-decane and process for preparing them
IL111730A (en) 1993-11-29 1998-12-06 Fujisawa Pharmaceutical Co Piperazine derivatives, processes for their preparation and pharmaceutical preparations containing them
ATE208766T1 (de) * 1995-05-23 2001-11-15 Janssen Pharmaceutica Nv (2-morpholinylmethyl)benzamid-derivate
CN1072220C (zh) 1995-05-25 2001-10-03 藤泽药品工业株式会社 作为神经激肽受体拮抗剂的1－苯甲酰基－2－(吲哚基－3－烷基)－哌嗪衍生物
GB9510600D0 (en) 1995-05-25 1995-07-19 Fujisawa Pharmaceutical Co Piperazine derivatives
JP2000502100A (ja) 1995-12-18 2000-02-22 藤沢薬品工業株式会社 タキキニン拮抗薬としてのピペラジン誘導体
AUPO735997A0 (en) * 1997-06-17 1997-07-10 Fujisawa Pharmaceutical Co., Ltd. Piperazine derivatives
DE59814233D1 (de) 1997-08-27 2008-07-03 Solvay Pharm Gmbh Indolmethyl-N,N'-bisacylpiperazine als Neurokininrezeptorantagonisten
EP0982030A3 (en) * 1998-08-17 2000-05-10 Pfizer Products Inc. 2,7-substituted octahydro-pyrrolo 1,2-a]pyrazine derivatives as 5ht 1a ligands
CA2354875A1 (en) 1998-12-14 2000-06-22 Fujisawa Pharmaceutical Co., Ltd. Piperazine derivatives
DE10036818A1 (de) 2000-07-28 2002-02-07 Solvay Pharm Gmbh Neue N-Triazolylmethyl-Piperazinderivate als Neurokininrezeptor-Antagonisten

Also Published As

Publication number Publication date
UA77515C2 (en) 2006-12-15
EP1495022A1 (en) 2005-01-12
WO2003084955A1 (en) 2003-10-16
US7202238B2 (en) 2007-04-10
CA2462708A1 (en) 2003-10-16
DE60328272D1 (de) 2009-08-20
CN1279041C (zh) 2006-10-11
NO20044775L (no) 2004-12-16
CN1592747A (zh) 2005-03-09
EP1495022B1 (en) 2009-07-08
ATE435863T1 (de) 2009-07-15
KR20040095361A (ko) 2004-11-12
RU2004112415A (ru) 2005-03-27
AU2003224162A1 (en) 2003-10-20
PL371378A1 (en) 2005-06-13
JP2005525395A (ja) 2005-08-25
IL160943A0 (en) 2004-08-31
MXPA04004812A (es) 2004-08-11
AU2003224162B2 (en) 2008-06-12
HK1070356A1 (en) 2005-06-17
HRP20040273A2 (en) 2005-02-28
IL160943A (en) 2008-11-03
RU2310656C2 (ru) 2007-11-20
US20050119267A1 (en) 2005-06-02
AR039192A1 (es) 2005-02-09
ZA200404744B (en) 2005-09-21

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