RU95113434A - Диметилбензофураны и диметилбензопираны, их применение в качестве 5-нт*003-антагонистов, способы их получения, фармацевтическая композиция - Google Patents

Диметилбензофураны и диметилбензопираны, их применение в качестве 5-нт*003-антагонистов, способы их получения, фармацевтическая композиция

Info

Publication number
RU95113434A
RU95113434A RU95113434/04A RU95113434A RU95113434A RU 95113434 A RU95113434 A RU 95113434A RU 95113434/04 A RU95113434/04 A RU 95113434/04A RU 95113434 A RU95113434 A RU 95113434A RU 95113434 A RU95113434 A RU 95113434A
Authority
RU
Russia
Prior art keywords
hydrogen
synthesis
group
compound
new compounds
Prior art date
Application number
RU95113434/04A
Other languages
English (en)
Other versions
RU2116072C1 (ru
Inventor
Анри Поль Ван Даель Жорж
Be]
Рене Мари Андре Босман Жан-Поль
Джоунс Каролус Ван Лаерован Уилли
Original Assignee
Жансен Фармасетика Н.В. (BE)
Жансен Фармасетика Н.В.
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 Жансен Фармасетика Н.В. (BE), Жансен Фармасетика Н.В. filed Critical Жансен Фармасетика Н.В. (BE)
Publication of RU95113434A publication Critical patent/RU95113434A/ru
Application granted granted Critical
Publication of RU2116072C1 publication Critical patent/RU2116072C1/ru

Links

Classifications

    • 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
    • C07D401/12—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 chain containing hetero atoms as chain links
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic 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
    • 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
    • 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
    • A61P25/18—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
    • A61P25/24—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
    • A61P25/26—Psychostimulants, e.g. nicotine, cocaine
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D211/56—Nitrogen atoms
    • C07D211/58—Nitrogen atoms attached in position 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Psychiatry (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Addiction (AREA)
  • Otolaryngology (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Furan Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Steroid Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pyrane Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Dental Preparations (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)

Abstract

Предложены способы лечения 5-НТ-медиированных нарушений, который предусматривает системное введение эффективного количества соединения общей формулыгде Rи R- водород или вместе образуют двухвалентный радикал формулы (а) - СН=СН-СН=СН-, (b) - CH=C(Cl)-CH=CH- или (c) -CH=CH-C(Cl)=CH-;n=2,3 или 4; Rводород или метоксигруппа; m= 1 или 2; R- водород, аминогруппа или C- C- алкилкарбониламиногруппа и R- водород или галоген; или фармацевтически пригодной аддитивной кислой соли, или стереохимического изомера этого соединения, а также новые соединения, препараты, способы получения новых соединений и промежуточных продуктов синтеза.

Claims (1)

  1. Предложены способы лечения 5-НТ3-медиированных нарушений, который предусматривает системное введение эффективного количества соединения общей формулы
    Figure 00000001

    где R1 и R2 - водород или вместе образуют двухвалентный радикал формулы (а) - СН=СН-СН=СН-, (b) - CH=C(Cl)-CH=CH- или (c) -CH=CH-C(Cl)=CH-;n=2,3 или 4; R3 водород или метоксигруппа; m= 1 или 2; R4- водород, аминогруппа или C1 - C3- алкилкарбониламиногруппа и R5- водород или галоген; или фармацевтически пригодной аддитивной кислой соли, или стереохимического изомера этого соединения, а также новые соединения, препараты, способы получения новых соединений и промежуточных продуктов синтеза.
RU95113434A 1992-11-20 1993-11-15 Диметилбензофураны и диметилбензопираны, их применение в качестве 5-нт3-антагонистов, способы их получения и фармацевтическая композиция RU2116072C1 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US97901392A 1992-11-20 1992-11-20
US979,013 1992-11-20
US979013 1992-11-20

Publications (2)

Publication Number Publication Date
RU95113434A true RU95113434A (ru) 1997-03-10
RU2116072C1 RU2116072C1 (ru) 1998-07-27

Family

ID=25526607

Family Applications (1)

Application Number Title Priority Date Filing Date
RU95113434A RU2116072C1 (ru) 1992-11-20 1993-11-15 Диметилбензофураны и диметилбензопираны, их применение в качестве 5-нт3-антагонистов, способы их получения и фармацевтическая композиция

Country Status (31)

Country Link
US (2) US5674868A (ru)
EP (1) EP0669919B1 (ru)
JP (1) JP2830952B2 (ru)
KR (1) KR0166661B1 (ru)
AT (1) ATE176232T1 (ru)
AU (1) AU680640B2 (ru)
BG (1) BG62489B1 (ru)
BR (1) BR9307477A (ru)
CA (1) CA2149044C (ru)
CZ (1) CZ287262B6 (ru)
DE (1) DE69323322T2 (ru)
DK (1) DK0669919T3 (ru)
ES (1) ES2129615T3 (ru)
FI (1) FI952458A0 (ru)
GR (1) GR3029831T3 (ru)
HU (2) HUT72740A (ru)
IL (3) IL119273A0 (ru)
LV (1) LV10956B (ru)
MX (1) MX9307257A (ru)
NO (2) NO307690B1 (ru)
NZ (1) NZ257854A (ru)
OA (1) OA10158A (ru)
PL (1) PL176051B1 (ru)
RO (1) RO115160B1 (ru)
RU (1) RU2116072C1 (ru)
SG (1) SG47488A1 (ru)
SK (1) SK282378B6 (ru)
TW (1) TW294595B (ru)
UA (1) UA49792C2 (ru)
WO (1) WO1994012494A1 (ru)
ZA (1) ZA938676B (ru)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5374637A (en) * 1989-03-22 1994-12-20 Janssen Pharmaceutica N.V. N-(3-hydroxy-4-piperidinyl)(dihydrobenzofuran, dihydro-2H-benzopyran or dihydrobenzodioxin)carboxamide derivatives
ES2202855T3 (es) * 1997-04-18 2004-04-01 Janssen Pharmaceutica Nv Uso de antagonistas 5ht3 para promover el lavado intestinal.
BR9811676A (pt) * 1997-07-11 2000-09-19 Janssen Pharmaceutica Nv (+) norcisaprida útil para distúrbios mediados por 5-ht3 e 5-ht4
US6239122B1 (en) * 2000-01-05 2001-05-29 Joy Ann Steele Method of treatment of nausea, vomiting, and other disorders using estrogens
ATE440825T1 (de) * 2003-06-06 2009-09-15 Vertex Pharma Pyrimidin-derivate zur verwendung als modulatoren von atp-bindende kassette transportern
JP4864717B2 (ja) 2003-11-20 2012-02-01 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ ポリ（ａｄｐ−リボース）ポリメラーゼインヒビターとしての７−フェニルアルキル置換２−キノリノンおよび２−キノキサリノン
BRPI0416206A (pt) 2003-11-20 2006-12-26 Janssen Pharmaceutica Nv 2-quinolinonas e 2-quinoxalinonas substituìdas por 6-alquenila e 6-fenilalquila como inibidores de polimerase de poli(adp-ribose)
ES2563954T3 (es) 2004-06-30 2016-03-16 Janssen Pharmaceutica Nv Derivados de ftalazina como inhibidores de PARP
AU2005259190B2 (en) 2004-06-30 2011-05-12 Janssen Pharmaceutica N.V. Quinazolinedione derivatives as PARP inhibitors
EA012416B1 (ru) * 2004-06-30 2009-10-30 Янссен Фармацевтика Н.В. Производные замещенного 2-алкилхиназолинона как ингибиторы parp
AU2008223793B2 (en) 2007-03-08 2012-08-23 Janssen Pharmaceutica Nv Quinolinone derivatives as PARP and TANK inhibitors
ES2448870T3 (es) 2007-10-26 2014-03-17 Janssen Pharmaceutica, N.V. Derivados de quinolina como inhibidores de PARP
ATE513818T1 (de) 2008-03-27 2011-07-15 Janssen Pharmaceutica Nv Chinazolinonderivate als tubulinpolymerisationshemmer
RU2490260C2 (ru) 2008-03-27 2013-08-20 Янссен Фармацевтика Нв Тетрагидрофенантридиноны и тетрагидроциклопентахинолиноны в качестве ингибиторов parp и ингибиторов полимеризации тубулина

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA1183847A (en) * 1981-10-01 1985-03-12 Georges Van Daele N-(3-hydroxy-4-piperidinyl)benzamide derivatives
ZW12187A1 (en) * 1986-07-03 1989-02-01 Janssen Pharmaceutica Nv 4-(aroylamino)piperidinebutanamide derivatives
CA1317940C (en) * 1987-09-25 1993-05-18 Georges H. P. Van Daele Substituted n-(1-alkyl-3-hydroxy-4-piperidinyl)benzamides
US5374637A (en) * 1989-03-22 1994-12-20 Janssen Pharmaceutica N.V. N-(3-hydroxy-4-piperidinyl)(dihydrobenzofuran, dihydro-2H-benzopyran or dihydrobenzodioxin)carboxamide derivatives
GB9005014D0 (en) * 1990-03-06 1990-05-02 Janssen Pharmaceutica Nv N.(4.piperidinyl)(dihydrobenzofuran or dihydro.2h.benzopyran)carboxamide derivatives

Also Published As

Publication number Publication date
SK282378B6 (sk) 2002-01-07
RU2116072C1 (ru) 1998-07-27
EP0669919B1 (en) 1999-01-27
WO1994012494A1 (en) 1994-06-09
DK0669919T3 (da) 1999-09-13
AU5465994A (en) 1994-06-22
NO995762D0 (no) 1999-11-24
MX9307257A (es) 1994-05-31
NO307690B1 (no) 2000-05-15
IL119273A0 (en) 1996-12-05
RO115160B1 (ro) 1999-11-30
TW294595B (ru) 1997-01-01
IL107654A0 (en) 1994-02-27
DE69323322D1 (de) 1999-03-11
ATE176232T1 (de) 1999-02-15
US5674868A (en) 1997-10-07
PL176051B1 (pl) 1999-03-31
PL309045A1 (en) 1995-09-18
NO995762L (no) 1995-05-19
JP2830952B2 (ja) 1998-12-02
CA2149044A1 (en) 1994-06-09
NO308530B1 (no) 2000-09-25
KR0166661B1 (ko) 1999-01-15
US5863923A (en) 1999-01-26
UA49792C2 (ru) 2002-10-15
GR3029831T3 (en) 1999-06-30
BR9307477A (pt) 1999-06-29
EP0669919A1 (en) 1995-09-06
IL107654A (en) 1998-01-04
NO951980L (no) 1995-05-19
IL119273A (en) 2000-07-16
NZ257854A (en) 1997-04-24
CZ125895A3 (en) 1995-10-18
BG62489B1 (bg) 1999-12-30
ZA938676B (en) 1995-05-19
DE69323322T2 (de) 1999-09-09
HUT72740A (en) 1996-05-28
BG99593A (en) 1995-12-29
AU680640B2 (en) 1997-08-07
LV10956A (lv) 1995-12-20
CA2149044C (en) 2007-04-03
NO951980D0 (no) 1995-05-19
ES2129615T3 (es) 1999-06-16
OA10158A (en) 1996-12-18
CZ287262B6 (en) 2000-10-11
SK67595A3 (en) 1995-11-08
FI952458A (fi) 1995-05-19
SG47488A1 (en) 1998-04-17
HU9501476D0 (en) 1995-07-28
HU211546A9 (en) 1995-12-28
LV10956B (en) 1996-10-20
FI952458A0 (fi) 1995-05-19
JPH08505840A (ja) 1996-06-25

Similar Documents

Publication Publication Date Title
US5032617A (en) Substituted benzamide radiosensitizers
RU95113434A (ru) Диметилбензофураны и диметилбензопираны, их применение в качестве 5-нт*003-антагонистов, способы их получения, фармацевтическая композиция
RU94044671A (ru) Применение непептидных антагонистов рецептора тахикинина
RU94019334A (ru) Ингибиторы стероид-сульфатазы
DE69616749D1 (de) Arylsubstituierte 5,5 verknüpfte aromatische nitroverbindungen als entzündungshemmende wirkstoffe
RU94040390A (ru) Производные виниленазаиндола, способ их получения, фармацевтическая композиция
LU91145I2 (fr) FIROCOXIB facultativement sous forme d'un sel pharmaceutiquement acceptable (PREVICOX).
EA200500088A1 (ru) Трициклические модуляторы ядерного рецептора стероидного гормона
RU94045915A (ru) Производные индола, способ их получения, фармкомпозиция
RU93050199A (ru) Дезокситаксолы, способы их получения, промежуточные соединения, фармацевтический препарат
ATE219363T1 (de) Lösliche prodrugs von paclitaxel
EP0395328A3 (en) Penylpyrimidone derivates and their use as therapeutic agents
EA200000723A1 (ru) Производные 2-(пурин-9-ил)-тетрагидрофуран-3,4-диола
RU94036758A (ru) Применение 2-фенил-3-ароилбензотиофенов для лечения пери-менопаузного синдрома
JPS62240619A (ja) 制癌剤
RU95106675A (ru) 3-индолилпиперидины, способ их получения, фармацевтическая композиция и способ ее получения
RU99127433A (ru) Эрголиновые производные и их применение в качестве антагонистов рецепторов соматостатина
JP2004532185A5 (ru)
RU94044454A (ru) Ингибитор аутоимунных заболеваний
RU94036771A (ru) Ингибиторы ангиогенеза и ангиогенных заболеваний
EA200000847A1 (ru) Противоопухолевые средства
RU94037246A (ru) Применение 2-фенил-3-ароилбензотиофенов для ингибирования разрушения хряща
ATE269865T1 (de) Pyrazolo(3,4-g)chinoxaline als pdgf-rezeptor protein tyrosin-kinase inhibitoren
RU94039545A (ru) Новые производные аденозина, способы их получения, фармацевтические композиции на их основе, способы получения фармацевтических композиций и их применение
RU94030470A (ru) Производные 1-(арилалкиламиноалкил)имидазола, способ их получения, фармацевтическая композиция и способ лечения

Legal Events

Date Code Title Description
MM4A The patent is invalid due to non-payment of fees

Effective date: 20041116