CO4910148A1 - Compuestos heterociclicos de guanidinilo utiles como agonis- tas de alfa-2 adrenoceptores - Google Patents

Compuestos heterociclicos de guanidinilo utiles como agonis- tas de alfa-2 adrenoceptores

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Publication number
CO4910148A1
CO4910148A1 CO97068606A CO97068606A CO4910148A1 CO 4910148 A1 CO4910148 A1 CO 4910148A1 CO 97068606 A CO97068606 A CO 97068606A CO 97068606 A CO97068606 A CO 97068606A CO 4910148 A1 CO4910148 A1 CO 4910148A1
Authority
CO
Colombia
Prior art keywords
unsubstituted
hydrogen
alkanyl
guanidinyl
cycloalkanyl
Prior art date
Application number
CO97068606A
Other languages
English (en)
Inventor
Thomas Lee Cupps
Sophie Eva Bogdan
Raymond Todd Henry
Russell James Sheldon
William Lee Seibel
Jeffrey Joseph Ares
Original Assignee
Procter & Gamble
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 Procter & Gamble filed Critical Procter & Gamble
Publication of CO4910148A1 publication Critical patent/CO4910148A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • 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
    • A61P1/04—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
    • A61P1/12—Antidiarrhoeals
    • 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
    • A61P11/02—Nasal agents, e.g. decongestants
    • 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
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • 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
    • A61P25/06—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
    • A61P25/30—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
    • A61P25/36—Opioid-abuse
    • 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
    • A61P27/02—Ophthalmic agents
    • 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
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
    • 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
    • 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
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • 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
    • A61P9/06—Antiarrhythmics
    • 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
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D215/38—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/60—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
    • C07D277/62—Benzothiazoles

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Cardiology (AREA)
  • Biomedical Technology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Addiction (AREA)
  • Ophthalmology & Optometry (AREA)
  • Urology & Nephrology (AREA)
  • Psychiatry (AREA)
  • Vascular Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Otolaryngology (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

La presente invención se relaciona con compuestos que tienenla siguiente estructuraen donde:a) R1 es hidrógeno; o alquilo o nada; donde R1 es nada, el enlace (a) es un enlace doble; yb) D es CR2 donde R2 se selecciona de hidrógeno; alcanilo C1 -C3 insustituido; amino; hidroxi; mercapto; alquiltio o alcoxi C1 -C3 ; alquilamino C1 -C3 o dialquilamino C1 -C3 o halo; o cuando B es CR3 , D puede ser N;c) B es NR9 , CR3 =CR8 , CR3 =N, CR3 , S, O, SO o SO2 ; en donde R9 se selecciona de hidrógeno; alcanilo, alquenilo o alquinilo C1 -C3 insustituido; cicloalcanilo, cicloalquenilo y en donde R3 y R8 cada uno se seleccionan independientemente de hidrógeno; alcanilo, alquenilo o alquinilo C1 -C3 insustituido; cicloalcanilo, cicloalquenilo, alquiltio o alcoxi C1 -C3 insustituido; hidroxi; tio; nitro; ciano; amino; alquilamino C1 -C3 o dialquilamino C1 -C3 y halo;d) R4 , R5 y R6 cada uno se seleccionan independientemente de hidrógeno; alcanilo, alquenilo o alquinilo C1 -C3 insustituido; cicloalcanilo, cicloalquenilo, alquiltio o alcoxi C1 -C3 insustituido; hidroxi; tio; nitro; ciano; amino; alquilamino C1 -C3 o dialquilamino C1 -C3 y halo; y NH-C(=NR10 )NHR11 (guanidinilo); en donde R10 y R11 se seleccionan independientemente de hidrógeno; metilo y etilo; y en donde uno o solamente uno de R4 R5 y R6 es guanidinilo;e) R7 se selecciona de hidrógeno; alcanilo, alquenilo o alquinilo C1 -C3 insustituido; cicloalcanilo, cicloalquenilo, alquiltio o alcoxi C1 -C3 insustituido; hidroxi; tio; nitro; ciano; amino; alquilamino C1 -C3 o dialquilamino C1 -C3 y halo;y enantiómeros, isómeros ópticos, estereoisómeros, diastereómeros, tautómeros, sales de adición, amidasésteres biohidrolizables, y composiciones farmacéuticas que contienen tales nuevos compuestos, y el uso de tales compuestos para prevenir o tratar trastornos modulados por alfa-2 adrenoceptores.
CO97068606A 1996-11-25 1997-11-24 Compuestos heterociclicos de guanidinilo utiles como agonis- tas de alfa-2 adrenoceptores CO4910148A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US3202396P 1996-11-25 1996-11-25

Publications (1)

Publication Number Publication Date
CO4910148A1 true CO4910148A1 (es) 2000-04-24

Family

ID=21862692

Family Applications (1)

Application Number Title Priority Date Filing Date
CO97068606A CO4910148A1 (es) 1996-11-25 1997-11-24 Compuestos heterociclicos de guanidinilo utiles como agonis- tas de alfa-2 adrenoceptores

Country Status (25)

Country Link
US (3) US6225331B1 (es)
EP (1) EP0944604B1 (es)
JP (1) JP2001506600A (es)
KR (1) KR20000069131A (es)
CN (1) CN1104422C (es)
AR (1) AR009145A1 (es)
AT (1) ATE286885T1 (es)
AU (1) AU730369B2 (es)
BR (1) BR9713536A (es)
CA (1) CA2272640C (es)
CO (1) CO4910148A1 (es)
CZ (1) CZ184099A3 (es)
DE (1) DE69732244T2 (es)
ES (1) ES2236833T3 (es)
HU (1) HUP0000312A3 (es)
ID (1) ID23857A (es)
IL (1) IL130077A0 (es)
NO (1) NO313912B1 (es)
NZ (1) NZ336010A (es)
PE (1) PE16399A1 (es)
RU (1) RU2194700C2 (es)
SK (1) SK69799A3 (es)
TR (1) TR199901468T2 (es)
WO (1) WO1998023596A1 (es)
ZA (1) ZA9710578B (es)

Families Citing this family (21)

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WO1998023596A1 (en) 1996-11-25 1998-06-04 The Procter & Gamble Company Guanidinyl heterocycle compounds useful as alpha-2 adrenoceptor agonists
US6291514B1 (en) * 1998-02-09 2001-09-18 3-Dimensional Pharmaceuticals, Inc. Heteroaryl amidines, methylamidines and guanidines, preparation thereof, and use thereof as protease inhibitors
DZ3415A1 (fr) * 2000-08-31 2002-03-07 Chiron Corp Guanidinobenzamides comme mc4-r agonistes.
EP1317259A2 (en) * 2000-09-08 2003-06-11 Warner-Lambert Company Prevention of acute sinusitis and sinus attack
EP1767525A1 (en) * 2001-04-09 2007-03-28 Novartis Vaccines and Diagnostics, Inc. Guanidino compounds as melanocortin-4 receptor (MC4-R) agonists
US20050124652A1 (en) * 2002-02-04 2005-06-09 Rustum Boyce Guanidino compounds
US20030195187A1 (en) * 2002-02-04 2003-10-16 Chiron Corporation Guanidino compounds
US20030207814A1 (en) * 2002-02-04 2003-11-06 Chiron Corporation Novel guanidinyl derivatives
WO2003072056A2 (en) * 2002-02-25 2003-09-04 Chiron Corporation Intranasal administration of mc4-r agonists
MXPA04011557A (es) * 2002-05-23 2005-07-05 Chiron Corp Compuestos de quinazolinona sustituida.
JP2007501861A (ja) * 2003-05-23 2007-02-01 カイロン コーポレイション Ｍｃ４−ｒアゴニストとしてのグアニジノ置換キナゾリノン化合物
MXPA06005736A (es) * 2003-11-19 2006-12-14 Chiron Corp Compuestos de quinazolinona con bioacumulacion reducida.
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CA2628570A1 (en) 2005-11-09 2007-05-18 Combinatorx, Incorporated Methods, compositions, and kits for the treatment of medical conditions
CL2008000838A1 (es) * 2007-03-23 2008-10-10 Neuraxon Inc Compuestos derivados de quinolina y tetrahidroquinolina, con actividad inhibidora nos; composicion farmaceutica que comprende a dichos compuestos; y su uso para tratar un dolor de cabeza tal como migrana, dolor cronico, desordenes del sistema nervios
US20090131503A1 (en) * 2007-11-16 2009-05-21 Annedi Subhash C 3,5 - substituted indole compounds having nos and norepinephrine reuptake inhibitory activity
WO2010065547A1 (en) * 2008-12-01 2010-06-10 Map Pharmaceuticals, Inc. Inhalation delivery methods and devices
WO2010074753A1 (en) 2008-12-23 2010-07-01 Map Pharmaceuticals, Inc. Inhalation devices and related methods for administration of sedative hypnotic compounds
GB0919889D0 (en) * 2009-11-13 2009-12-30 Biocopea Ltd Drug composition and its use in therapy
EP2668177B1 (en) * 2011-01-28 2014-10-22 Boehringer Ingelheim International GmbH Substituted pyridinyl-pyrimidines and their use as medicaments
CN112047947A (zh) * 2020-10-13 2020-12-08 石药集团新诺威制药股份有限公司 一种茶碱的合成方法

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US5478858A (en) * 1993-12-17 1995-12-26 The Procter & Gamble Company 5-(2-imidazolinylamino) benzimidazole compounds useful as alpha-2 adrenoceptor agonists
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JP2001507349A (ja) * 1996-12-23 2001-06-05 セルテック セラピューティックス リミテッド 縮合多環式２−アミノピリミジン誘導体、それらの製造およびたんぱく質チロシンキナーゼ抑制因子としてのそれらの使用

Also Published As

Publication number Publication date
ATE286885T1 (de) 2005-01-15
IL130077A0 (en) 2000-02-29
KR20000069131A (ko) 2000-11-25
PE16399A1 (es) 1999-03-12
US20020128481A1 (en) 2002-09-12
AU730369B2 (en) 2001-03-08
US20010000345A1 (en) 2001-04-19
NO313912B1 (no) 2002-12-23
RU2194700C2 (ru) 2002-12-20
TR199901468T2 (xx) 1999-10-21
ES2236833T3 (es) 2005-07-16
HUP0000312A2 (hu) 2000-09-28
ID23857A (id) 2000-05-25
CA2272640A1 (en) 1998-06-04
US6225331B1 (en) 2001-05-01
ZA9710578B (en) 1998-06-25
AR009145A1 (es) 2000-03-08
NZ336010A (en) 2001-05-25
BR9713536A (pt) 2000-11-07
HUP0000312A3 (en) 2001-12-28
EP0944604A1 (en) 1999-09-29
JP2001506600A (ja) 2001-05-22
WO1998023596A1 (en) 1998-06-04
AU5438198A (en) 1998-06-22
CN1242006A (zh) 2000-01-19
CN1104422C (zh) 2003-04-02
NO992498D0 (no) 1999-05-25
CZ184099A3 (cs) 1999-11-17
US6391878B2 (en) 2002-05-21
EP0944604B1 (en) 2005-01-12
NO992498L (no) 1999-07-26
SK69799A3 (en) 2000-06-12
CA2272640C (en) 2003-07-08
DE69732244D1 (de) 2005-02-17
DE69732244T2 (de) 2006-06-29

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