BR0215080A - Composto inibidores de lipase pancreática, sua sìntese e uso - Google Patents

Composto inibidores de lipase pancreática, sua sìntese e uso

Info

Publication number
BR0215080A
BR0215080A BR0215080-8A BR0215080A BR0215080A BR 0215080 A BR0215080 A BR 0215080A BR 0215080 A BR0215080 A BR 0215080A BR 0215080 A BR0215080 A BR 0215080A
Authority
BR
Brazil
Prior art keywords
alkyl
substituted
unsubstituted
cycloalkyl
aryl
Prior art date
Application number
BR0215080-8A
Other languages
English (en)
Inventor
David Witter
Arlindo L Castelhano
Original Assignee
Osi Pharm Inc
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 Osi Pharm Inc filed Critical Osi Pharm Inc
Publication of BR0215080A publication Critical patent/BR0215080A/pt

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5365—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/542—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/26—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur 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
    • C07D333/38—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Diabetes (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Heterocyclic Compounds Containing Sulfur Atoms (AREA)

Abstract

"COMPOSTOS INIBIDORES DE LIPASE PANCREáTICA, SUA SìNTESE E USO". A presente invenção se refere aos compostos que possuem a estrutura: onde X é O, S, CH~ 2~ ou NR~ 5~; Y é O ou S; R~ 1~ é H, alquila C~ 1~-C~ 15~ substituída ou não substituída, alquilarila C~ 1~- C~ 8~, -C(O) OR~ 4~, -C(O)NR~ 4~R~ 5~, -CR~ 6~R~ 6~,OR~ 4~, - CR~ 6~R~ 6~,OC(O)R~ 4~, -CR~ 6~R~ 6~, OC(O)NHR~ 7~, -C(O)NR~ 10~R~ 11~, -C(O)NR~ 8~R~ 9~NR~ 8~R~ 9~, -N(R~ 5~)C(O)NHR~ 5~, ou CH~ 2~R~ 4~; R~ 2~ é uma alquila C~ 1~-C~ 30~ de cadeia linear substituída ou não substituída ou alquila C~ 3~-C~ 30~ ramificada, arila, alquilarila, arilalquila, heteroarilalquila ou cicloalquila; R~ 3~ é H ou alquila C~ 1~-C~ 6~ substituída ou não substituída ou cicloalquila C~ 3~-C~ 10~, R~ 4~ é H ou uma cadeia linear ou ramificada, substituída ou não substituída, C~ 6~-C~ 30~ alquila, arila, -CH~ 2~-arila, aril-alquila C~ 1~-C~ 15~, heteroaril-alquila C~ 1~-C~ 15~ ou cicloalquila C~ 3~-C~ 10~; R~ 5~ é H ou uma cadeia linear ou ramificada, substituída ou não substituída, C~ 6~-C~ 30~ alquila, aril-alquila C~ 1~-C~ 30~, heteroarilalquila ou cicloalquila; R~ 6~ e R~ 6~, são cada um independentemente H, alquila C~ 1~-C~ 6~ substituída ou não substituída, dialquila ou cicloalquila C~ 3~-C~ 10~ ou em conjunto formam um sistema de anel de 3-7 elementos; R~ 7~ é H ou alquila C~ 1~-C~ 12~ substituída ou não substituída ou cicloalquila C~ 3~-C~ 10~; e R~ 8~ e R~ 9~ são cada um independentemente H, alquila C~ 1~-C~ 6~ substituída ou não substituída, alcóxi C~ 1~-C~ 6~, alquilarila C~ 1~-C~ 6~, ou NR~ 8~R~ 9~ em conjunto formam um anel piperazina ou piperidina substituído ou um sistema de anel diidro-1H-isoquinolina, ou um enantiómero específico do mesmo, ou um tautêmero específico, ou um sal farmaceuticamente aceitável do mesmo e um processo para tratar diabetes ou obesidade por administração de uma quantidade terapeuticamente eficaz dos compostos da invenção.
BR0215080-8A 2001-12-20 2002-12-20 Composto inibidores de lipase pancreática, sua sìntese e uso BR0215080A (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US34261701P 2001-12-20 2001-12-20
US35701502P 2002-02-13 2002-02-13
PCT/US2002/041272 WO2003053944A1 (en) 2001-12-20 2002-12-20 Pancreatic lipase inhibitor compounds, their synthesis and use

Publications (1)

Publication Number Publication Date
BR0215080A true BR0215080A (pt) 2004-10-05

Family

ID=26993102

Family Applications (1)

Application Number Title Priority Date Filing Date
BR0215080-8A BR0215080A (pt) 2001-12-20 2002-12-20 Composto inibidores de lipase pancreática, sua sìntese e uso

Country Status (11)

Country Link
US (1) US7064122B2 (pt)
EP (1) EP1467978A4 (pt)
JP (1) JP4668536B2 (pt)
KR (1) KR20040068316A (pt)
CN (1) CN1620439A (pt)
AU (1) AU2002366810B2 (pt)
BR (1) BR0215080A (pt)
CA (1) CA2471098A1 (pt)
EA (1) EA009368B1 (pt)
MX (1) MXPA04005863A (pt)
WO (1) WO2003053944A1 (pt)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NZ531272A (en) 2001-08-30 2006-01-27 Alizyme Therapeutics Ltd Thieno-(1,3)-oxazin-4-ones with lipase inhibiting activity
US20090082435A1 (en) * 2005-04-28 2009-03-26 The Regents Of The University Of California Methods, Compositions, And Compounds For Modulation Of Monoacylglycerol Lipase, Pain, And Stress-Related Disorders
WO2010112569A1 (en) 2009-03-31 2010-10-07 Robert Zimmermann Modulation of adipose triglyceride lipase for prevention and treatment of cachexia, loss of weight and muscle atrophy and methods of screening therefor
EP2414830A2 (en) 2009-03-31 2012-02-08 Robert Zimmermann Modulation of adipose triglyceride lipase for prevention and treatment of cachexia, loss of weight and muscle atrophy and methods of screening therefor
US9278958B2 (en) * 2012-06-22 2016-03-08 Katholieke Universiteit Leuven K.U. Leuven R&D Anti-cancer compounds
WO2016095205A1 (en) * 2014-12-19 2016-06-23 Merck Sharp & Dohme Corp. Heteroaryl orexin receptor antagonists
CN107216339B (zh) * 2016-03-22 2021-05-04 中国科学院上海药物研究所 一种dppiv抑制剂马来酸盐的多晶型及其制备方法
CN107216340B (zh) * 2016-03-22 2021-05-04 中国科学院上海药物研究所 一种dppiv抑制剂的盐型及其制备方法

Family Cites Families (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE2447477A1 (de) * 1974-10-03 1976-04-15 Schering Ag Thieno-pyridoncarbonsaeurederivate, verfahren zur herstellung dieser verbindungen und ihre therapeutische verwendung
US4054656A (en) * 1975-09-10 1977-10-18 Mead Johnson & Company Thieno[2,3-d]pyrimidine antiallergic agents
JPS5772979A (en) * 1980-08-27 1982-05-07 Eastman Kodak Co Manufacture of thiophenes
GB8311426D0 (en) * 1983-04-27 1983-06-02 Beecham Group Plc Compounds
CA1247547A (en) 1983-06-22 1988-12-28 Paul Hadvary Leucine derivatives
DE3540377A1 (de) * 1985-11-14 1987-05-21 Bayer Ag Thienooxazinone, verfahren zu ihrer herstellung und ihre verwendung als leistungsfoerderer
JPS62132884A (ja) * 1985-12-05 1987-06-16 Mitsubishi Chem Ind Ltd ２−ベンジルチエノ〔２，３−ｄ〕ピリミジン−４（３Ｈ）−オン誘導体
DE4039734A1 (de) 1990-12-13 1992-06-17 Basf Ag Substituierte 2-aminothiophene enthaltende herbizide mittel
GB9426021D0 (en) 1994-12-22 1995-02-22 Smithkline Beecham Plc Pharmaceuticals
WO1997027200A1 (en) 1996-01-26 1997-07-31 Smithkline Beecham Plc Thienoxazinone derivatives useful as antiviral agents
WO1997048707A1 (en) * 1996-06-20 1997-12-24 Smithkline Beecham Plc 4h-3,1-benzoxazin-4-one derivatives and analogs as antiviral agents
WO1998045298A1 (en) * 1997-04-10 1998-10-15 Smithkline Beecham Plc Antiviral agents
US6037340A (en) 1997-05-28 2000-03-14 Cadus Pharmaceutical Corporation Synthesis and use of thiophene- and pyrrole-based heteroaromatic compounds
GB9710928D0 (en) 1997-05-29 1997-07-23 Smithkline Beecham Plc Pharmaceuticals
WO2000030646A1 (en) 1998-11-26 2000-06-02 Novo Nordisk A/S Heterocyclic compounds regulating clotting
GB9900416D0 (en) * 1999-01-08 1999-02-24 Alizyme Therapeutics Ltd Inhibitors
AR022204A1 (es) * 1999-01-08 2002-09-04 Norgine Bv Compuesto, proceso para su preparacion, composicion farmaceutica y producto comestible que lo comprende.
ES2184705T3 (es) * 1999-03-09 2003-04-16 Upjohn Co 4-oxo-4,7-dihidro-tieno(2,3-b)piridina-5-carboxamidas como agentes antivirales.
PE20010588A1 (es) * 1999-09-10 2001-06-23 Procter & Gamble Conjugados polimericos inhibidores de enzimas proteoliticas y lipoliticas
GB0001572D0 (en) * 2000-01-24 2000-03-15 Alizyme Therapeutics Ltd Inhibitors
NZ531272A (en) * 2001-08-30 2006-01-27 Alizyme Therapeutics Ltd Thieno-(1,3)-oxazin-4-ones with lipase inhibiting activity

Also Published As

Publication number Publication date
EA200400831A1 (ru) 2005-08-25
EA009368B1 (ru) 2007-12-28
MXPA04005863A (es) 2004-10-29
EP1467978A1 (en) 2004-10-20
US20030195199A1 (en) 2003-10-16
KR20040068316A (ko) 2004-07-30
CN1620439A (zh) 2005-05-25
US7064122B2 (en) 2006-06-20
EP1467978A4 (en) 2005-11-02
CA2471098A1 (en) 2003-07-03
JP2005518383A (ja) 2005-06-23
JP4668536B2 (ja) 2011-04-13
AU2002366810B2 (en) 2009-06-11
WO2003053944A1 (en) 2003-07-03
AU2002366810A1 (en) 2003-07-09

Similar Documents

Publication Publication Date Title
HUP0100142A2 (hu) Szubsztituált ciklopentán- és ciklopenténszármazékok és alkalmazásuk neuraminidáz-inhibitorokként
BRPI0409227C1 (pt) composto, composição farmacêutica, uso de um composto e processo para a preparação de um composto de fórmula (i)
TN2010000026A1 (fr) Nouveaux derives de 6-triazolopyridazine-sulfanyl benzothiazole et benzimidazole, leur procede de preparation, leur application a titre de medicaments, compositions pharmaceutiques et nouvelle utilisation notamment comme inhibiteurs de met
BR0010555A (pt) Inibidores de neuraminidases
BR9907300A (pt) Inibidores do fator xa oxoaza-heterociclila substituìdos
BRPI0516905A (pt) processo para a preparação de um derivado n-[2-(2-piridinil)etil]carboxamida e compostos
NO20050741L (no) Ny fremgangsmate for syntesen og ny krystallinsk form av agomelatin og farmasoytiske sammensetninger inneholdende den
CO5140119A1 (es) 3-substituido-n-(hetero)arilalquil-pirrolidinas
BR0102607A (pt) Compostos de difeniluréia, um processo para sua preparação e composições farmacêuticas contendo os mesmos
EA200301310A1 (ru) Триамид-замещённые индолы, бензофураны и бензотиофены в качестве ингибиторов микросомального белка, переносящего триглицериды, (мтр) и/или ингибиторов секреции аполипопротеина в (аро в)
BRPI0507052A (pt) inibidores de quìnase
BRPI0906495B8 (pt) compostos derivados de indolil-piridona e composição farmacêutica
DK1140918T3 (da) Thrombininhibitorer
BRPI0407695A (pt) compostos, processo para a preparação de um composto, composições farmacêuticas que compreendem o composto, utilização dos compostos e processo de tratamento para diabetes do tipo 2
AR054045A1 (es) Compuestos benzoimidazol sustituidos con actividad dual no inhibitoria y mu opioide agonista
AR064307A1 (es) Monofosfatos utiles para el tratamiento de la inflamacion pulmonar y broncoconstriccion, formulaciones aerosolicas que los contienen, y metodo de preparacion.
EA200401053A1 (ru) Оксо-азабициклические соединения
BRPI0416287A (pt) compostos, processo para a manufatura dos mesmos, composições farmacêuticas que os compreendem, método para o tratamento e/ou prevenção de enfermidades que são moduladas por inibidores de accß e sua utilização
BRPI0519057A2 (pt) derivados de hidantoÍna éteis como inibidores de metaloproteinase
BR0215080A (pt) Composto inibidores de lipase pancreática, sua sìntese e uso
EA200600760A1 (ru) Новые соединения фенилпиридилпиперазина, способ их получения и фармацевтические композиции, содержащие их
BR0100234A (pt) Compostos de piperidina-4-sulfonamida, processo para a sua preparação e composições farmacêuticas contendo os mesmos
BR0109328A (pt) Inibidores de metaloprotease n-substituìdos, contendo cadeia lateral heterocìclica
BR0313734A (pt) Derivados do tiofeno, o seu processo de preparação e as composições farmacêuticas que os contêm
EA200701476A1 (ru) Новые гетероциклические соединения оксима, способ их получения и фармацевтические композиции, которые их содержат

Legal Events

Date Code Title Description
B06F Objections, documents and/or translations needed after an examination request according [chapter 6.6 patent gazette]
B08F Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette]

Free format text: REFERENTE A(S) 8A ANUIDADE(S).

B08K Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette]

Free format text: REFERENTE AO DESPACHO 8.6 PUBLICADO NA RPI 2108 DE 31/05/2011.