HUP0100397A2 - Tetrahidro- vagy oktahidrobenzo-naftiridin és kinolinszármazékok, ezeket tartalmazó gyógyszerkészítmények és eljárás előállításukra - Google Patents

Tetrahidro- vagy oktahidrobenzo-naftiridin és kinolinszármazékok, ezeket tartalmazó gyógyszerkészítmények és eljárás előállításukra

Info

Publication number
HUP0100397A2
HUP0100397A2 HU0100397A HUP0100397A HUP0100397A2 HU P0100397 A2 HUP0100397 A2 HU P0100397A2 HU 0100397 A HU0100397 A HU 0100397A HU P0100397 A HUP0100397 A HU P0100397A HU P0100397 A2 HUP0100397 A2 HU P0100397A2
Authority
HU
Hungary
Prior art keywords
group
optionally substituted
general formula
optionally
aromatic
Prior art date
Application number
HU0100397A
Other languages
English (en)
Inventor
Ben C. Askew
Paul J. Coleman
Mark E. Duggan
Wasyl Halczenko
George D. Hartman
Cecilia Hunt
John H. Hutchinson
Robert S. Meissner
Michael A. Patane
Garry R. Smith
Jiabing Wang
Original Assignee
Merck & Co., 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
Priority claimed from GBGB9807382.8A external-priority patent/GB9807382D0/en
Priority claimed from GBGB9811295.6A external-priority patent/GB9811295D0/en
Application filed by Merck & Co., Inc. filed Critical Merck & Co., Inc.
Publication of HUP0100397A2 publication Critical patent/HUP0100397A2/hu
Publication of HUP0100397A3 publication Critical patent/HUP0100397A3/hu

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
    • C07D401/06—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
    • 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
    • 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
    • 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
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • 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
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/12—Drugs for disorders of the metabolism for electrolyte homeostasis
    • A61P3/14—Drugs for disorders of the metabolism for electrolyte homeostasis for calcium homeostasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic 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
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/54—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/55—Acids; Esters
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen 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
    • C07D213/62—Oxygen or sulfur atoms
    • C07D213/63—One oxygen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
    • C07D237/02—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
    • C07D237/06—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D237/08—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
    • C07D237/02—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
    • C07D237/06—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D237/10—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three 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
    • C07D237/14—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
    • C07D263/30—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D263/32—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/22—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D277/30—Radicals substituted by 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
    • 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
    • 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
    • C07D401/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • 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

Abstract

A találmány tárgyát (B) általános képletű vegyületek és sóik, ezekettartalmazó gyógyszerkészítmények és ezek előállítása képezi.Közelebbről, a találmány szerinti vegyületek az av<3, az av<5 és/vagyav<6 integrin receptorok antagonistái, és csontfelszívódás gátlásában,oszteoporózis kezelésére vagy megelőzésére, ér-újrabeszűkülés,diabéteszes retinopátia, makuladegenerálódás, angingenezis,ateroszklerózis, gyulladások, vírusfertőzések, tumornövekedés és -áttét gátlására és sebgyógyulás kezelésére alkalmazhatók. A találmányszerinti vegyületek (B) általános képletében X jelentése (1) általánosképletű csoport, 5- vagy 6-tagú monociklusos aromás vagy nem-aromás,adott esetben heteroatomot tartalmazó és adott esetben helyettesítettgyűrűrendszer, vagy 9-14-tagú policiklusos, adott esetben heteroatomottartalmazó és adott esetben helyettesített gyűrűrendszer, amelyben agyűrűk közül egy vagy több aromás; Y jelentése adott esetben egy vagytöbb oxigén, nitrogén és/vagy kén heteroatomot tartalmazó, adottesetben helyettesített telített lineáris szénhidrogénlánc; Z jelentése(3), (4) vagy (5) általános képletű csoport, vagy adott esetbenhelyettesített -CH2CH2- vagy -CH=CH- csoport; R5, R6, R7 és R8jelentése egymástól függetlenül többek között hidrogénatom, alkil-vagy arilcsoport, halogénatom, hidroxilcsoport, alkenil- vagyalkinilcsoport, adott esetben oxigén-, nitrogén- és/vagy kénatomottartalmazó, adott esetben helyettesített telített vagy telítetlenszénhidrogénlánc, és további helyettesített amino- és alkilcsoportok;R9 jelentése hidrogénatom, arilcsoport vagy adott esetbenhelyettesített alkil-csoport. Ó
HU0100397A 1997-12-17 1998-12-14 Tetrahydro- or octahydrobenzonaphtyridin and quinolin derivatives, pharmaceutical compositions thereof and process for their preparation HUP0100397A3 (en)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US6989997P 1997-12-17 1997-12-17
GBGB9807382.8A GB9807382D0 (en) 1998-04-06 1998-04-06 Vitronectin receptor antagonists
US8320998P 1998-04-27 1998-04-27
GBGB9811295.6A GB9811295D0 (en) 1998-05-26 1998-05-26 Vitronectin receptor antagonists
US9262298P 1998-07-13 1998-07-13
PCT/US1998/026484 WO1999031061A1 (en) 1997-12-17 1998-12-14 Integrin receptor antagonists

Publications (2)

Publication Number Publication Date
HUP0100397A2 true HUP0100397A2 (hu) 2001-09-28
HUP0100397A3 HUP0100397A3 (en) 2002-10-28

Family

ID=27517453

Family Applications (1)

Application Number Title Priority Date Filing Date
HU0100397A HUP0100397A3 (en) 1997-12-17 1998-12-14 Tetrahydro- or octahydrobenzonaphtyridin and quinolin derivatives, pharmaceutical compositions thereof and process for their preparation

Country Status (25)

Country Link
EP (1) EP1040098B1 (hu)
JP (1) JP3585839B2 (hu)
KR (1) KR20010033248A (hu)
CN (1) CN1284944A (hu)
AT (1) ATE294163T1 (hu)
AU (1) AU739811B2 (hu)
BG (1) BG104605A (hu)
BR (1) BR9813769A (hu)
CA (1) CA2315220C (hu)
DE (1) DE69829996T2 (hu)
EA (1) EA002822B1 (hu)
EE (1) EE200000362A (hu)
ES (1) ES2241192T3 (hu)
GE (1) GEP20032921B (hu)
HR (1) HRP20000401A2 (hu)
HU (1) HUP0100397A3 (hu)
ID (1) ID24955A (hu)
IL (1) IL136495A0 (hu)
IS (1) IS5521A (hu)
NO (1) NO20003114L (hu)
NZ (1) NZ504893A (hu)
PL (1) PL341215A1 (hu)
SK (1) SK9192000A3 (hu)
TR (1) TR200002557T2 (hu)
WO (1) WO1999031061A1 (hu)

Families Citing this family (62)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9805655D0 (en) 1998-03-16 1998-05-13 Celltech Therapeutics Ltd Chemical compounds
US6521626B1 (en) 1998-03-24 2003-02-18 Celltech R&D Limited Thiocarboxamide derivatives
KR20010087125A (ko) * 1998-04-16 2001-09-15 데이비드 비. 맥윌리암스 인테그린 수용체에 대한 인테그린의 결합을 억제하는 화합물
GB9814414D0 (en) 1998-07-03 1998-09-02 Celltech Therapeutics Ltd Chemical compounds
AU748621B2 (en) * 1998-08-13 2002-06-06 Merck & Co., Inc. Integrin receptor antagonists
GB9821061D0 (en) 1998-09-28 1998-11-18 Celltech Therapeutics Ltd Chemical compounds
GB9826174D0 (en) 1998-11-30 1999-01-20 Celltech Therapeutics Ltd Chemical compounds
US6518283B1 (en) 1999-05-28 2003-02-11 Celltech R&D Limited Squaric acid derivatives
BR0011108A (pt) 1999-06-02 2002-03-19 Merck & Co Inc Composto, composição farmacêutica, e, processos de eliciar um efeito antagonizante do receptor da integrina, de tratamento ou prevenção da osteoporose, de tratamento ou prevenção de uma condição mediada por antagonismo de um receptor de integrina, de inibição da reabsorção óssea em um mamìfero em necessidade do mesmo, e de tratamento do desenvolvimento tumoral
US6534513B1 (en) 1999-09-29 2003-03-18 Celltech R&D Limited Phenylalkanoic acid derivatives
JP2003510360A (ja) * 1999-10-04 2003-03-18 メルク エンド カムパニー インコーポレーテッド インテグリン受容体拮抗薬
WO2001024828A2 (en) * 1999-10-06 2001-04-12 Basf Aktiengesellschaft MODULATORS OF CYTOKINE MEDIATED SIGNALLING PATHWAYS AND INTEGRIN αVβ3 RECEPTOR ANTAGONISTS FOR COMBINATION THERAPY
US6407241B1 (en) 1999-11-08 2002-06-18 Merck & Co., Inc. Process and intermediates for the preparation of imidazolidinone αv integrin antagonists
GB2356630A (en) 1999-11-10 2001-05-30 Merck & Co Inc Intermediates used in the preparation of tetrahydronaphthyridine
ATE258177T1 (de) 1999-11-23 2004-02-15 Merck & Co Inc Verfahren für die herstellung und zwischenprodukte von tetrahydro-(1,8)- naphthyridin
US6455539B2 (en) 1999-12-23 2002-09-24 Celltech R&D Limited Squaric acid derivates
AU780988B2 (en) 2000-01-24 2005-04-28 Merck & Co., Inc. Alpha V integrin receptor antagonists
JP2003531141A (ja) 2000-04-17 2003-10-21 セルテック アール アンド ディ リミテッド エナミン誘導体
US6403608B1 (en) 2000-05-30 2002-06-11 Celltech R&D, Ltd. 3-Substituted isoquinolin-1-yl derivatives
US6545013B2 (en) 2000-05-30 2003-04-08 Celltech R&D Limited 2,7-naphthyridine derivatives
WO2002004426A1 (en) 2000-07-07 2002-01-17 Celltech R & D Limited Squaric acid derivatives containing a bicyclic heteroaromatic ring as integrin antagonists
WO2002010136A1 (en) 2000-08-02 2002-02-07 Celltech R & D Limited 3-substituted isoquinolin-1-yl derivatives
AU2001290772A1 (en) * 2000-09-14 2002-03-26 Merck And Co., Inc. Alpha v integrin receptor antagonists
US6444680B1 (en) 2000-11-30 2002-09-03 Merck & Co., Inc. Amine salts of an integrin receptor antagonist
US6764842B2 (en) 2001-03-28 2004-07-20 Merck & Co., Inc. Enantioselective bioreduction for the preparation of integrin receptor antagonist intermediates
KR100861466B1 (ko) 2001-04-24 2008-10-02 메르크 파텐트 게엠베하 항혈관형성제 및 ＴＮＦα를 이용한 병용 요법
PE20030120A1 (es) * 2001-06-19 2003-02-12 Merck & Co Inc Sal amina de un antagonista de receptor de integrin
US20040224986A1 (en) 2002-08-16 2004-11-11 Bart De Corte Piperidinyl targeting compounds that selectively bind integrins
GB0420424D0 (en) * 2004-09-14 2004-10-20 Ionix Pharmaceuticals Ltd Therapeutic compounds
JP2009523813A (ja) 2006-01-18 2009-06-25 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツング 癌を治療するためにインテグリンのリガンドを使用する特異的な治療法
KR20090108713A (ko) 2007-01-18 2009-10-16 메르크 파텐트 게엠베하 인테그린 리간드를 사용하는 암치료용 특이적 요법 및 의약
WO2009114776A2 (en) 2008-03-14 2009-09-17 Visen Medical, Inc. Integrin targeting agents and methods of using same
NZ597339A (en) 2009-05-25 2013-10-25 Merck Patent Gmbh Continuous administration of cilengitide in cancer treatments
MX2012005994A (es) * 2009-12-04 2012-08-08 Taisho Pharmaceutical Co Ltd Compuestos de 2-piridona.
US8901144B2 (en) 2013-02-07 2014-12-02 Scifluor Life Sciences, Llc Fluorinated 3-(2-oxo-3-(3-arylpropyl)imidazolidin-1-yl)-3-arylpropanoic acid derivatives
CA2899321C (en) * 2013-02-07 2021-03-09 Ben C. Askew Fluorinated .alpha..nu.integrin antagonists
GB201305668D0 (en) 2013-03-28 2013-05-15 Glaxosmithkline Ip Dev Ltd Avs6 Integrin Antagonists
PT3050878T (pt) 2013-09-24 2021-12-02 Fujifilm Corp Novo composto contendo azoto ou seu sal, ou seu complexo de metal
WO2015059668A1 (en) 2013-10-25 2015-04-30 Novartis Ag Ring-fused bicyclic pyridyl derivatives as fgfr4 inhibitors
GB201417002D0 (en) 2014-09-26 2014-11-12 Glaxosmithkline Ip Dev Ltd Novel compound
GB201417094D0 (en) 2014-09-26 2014-11-12 Glaxosmithkline Ip Dev Ltd Novel compounds
GB201417018D0 (en) 2014-09-26 2014-11-12 Glaxosmithkline Ip Dev Ltd Novel compounds
GB201417011D0 (en) 2014-09-26 2014-11-12 Glaxosmithkline Ip Dev Ltd Novel compounds
CA2976634C (en) 2015-02-19 2023-10-17 Scifluor Life Sciences, Inc Fluorinated tetrahydronaphthyridinyl nonanoic acid derivatives and uses thereof
US9802917B2 (en) 2015-03-25 2017-10-31 Novartis Ag Particles of N-(5-cyano-4-((2-methoxyethyl)amino)pyridin-2-yl)-7-formyl-6-((4-methyl-2-oxopiperazin-1-yl)methyl)-3,4-dihydro-1,8-naphthyridine-1(2H)-carboxamide
RU2720989C2 (ru) * 2015-03-25 2020-05-15 Фуджифилм Корпорэйшн Способ получения нового азотсодержащего соединения или его соли и получение его промежуточного соединения
GB201604680D0 (en) 2016-03-21 2016-05-04 Glaxosmithkline Ip Dev Ltd Chemical Compounds
JP2019524702A (ja) * 2016-07-05 2019-09-05 ザ ロックフェラー ユニバーシティー テトラヒドロナフチルリジンペンタンアミドインテグリンアンタゴニスト
WO2018049068A1 (en) 2016-09-07 2018-03-15 Pliant Therapeutics, Inc. N-acyl amino acid compounds and methods of use
PL3660004T3 (pl) 2016-10-11 2023-10-02 Arvinas Operations, Inc. Związki i sposoby do ukierunkowanej degradacji receptora androgenowego
MA47692A (fr) 2017-02-28 2020-01-08 Morphic Therapeutic Inc Inhibiteurs de l'intégrine (alpha-v) (bêta-6)
CA3054604A1 (en) 2017-02-28 2018-09-07 Morphic Therapeutic, Inc. Inhibitors of .alpha.v.beta.6 integrin
CR20200452A (es) * 2018-03-07 2020-11-19 Pliant Therapeutics Inc Compuestos de aminoacidos y métodos de uso
SG11202009734VA (en) * 2018-04-27 2020-11-27 Arrowhead Pharmaceuticals Inc Integrin targeting ligands and uses thereof
TW202010492A (zh) 2018-06-27 2020-03-16 美商普萊恩醫療公司 具有未分支連接子之胺基酸化合物及使用方法
AU2019327475A1 (en) 2018-08-29 2021-03-11 Morphic Therapeutic, Inc. INHIBITING αV β6 INTEGRIN
AR116036A1 (es) * 2018-08-29 2021-03-25 Morphic Therapeutic Inc DERIVADOS DE NAFTIRIDINA COMO INHIBIDORES DE INTEGRINA avb6
WO2020047207A1 (en) * 2018-08-29 2020-03-05 Morphic Therapeutics, Inc. Inhibitors of (alpha-v)(beta-6) integrin
CA3136745A1 (en) 2019-04-08 2020-10-15 Pliant Therapeutics, Inc. Dosage forms and regimens for amino acid compounds
EP4077309A1 (en) 2019-12-19 2022-10-26 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of androgen receptor
CN114507202B (zh) * 2022-01-26 2023-10-03 海南大学 一种桑辛素类化合物及其制备方法与应用
GB202209228D0 (en) 2022-06-23 2022-08-10 Univ Strathclyde Modified amino acids and uses thereof

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3843798A (en) * 1973-03-12 1974-10-22 Stanley Drug Products Inc Methods and compositions for inducing resistance to bacterial infections
FR2466252A2 (fr) * 1979-10-03 1981-04-10 Clin Midy Nouveaux produits ayant notamment des proprietes anticancereuses a base de chaine a de la ricine et d'une proteine
US5025025A (en) * 1989-06-28 1991-06-18 Ciba-Geigy Corporation (Arylsulfonamido- and pyridyl-)-substituted carboxylic acids and derivatives thereof and use for suppressing thromboxane activity
FR2658511B1 (fr) * 1990-02-16 1992-06-19 Union Pharma Scient Appl Nouveaux derives de benzimidazole et d'azabenzimidazole, antagonistes des recepteurs au thromboxane; leurs procedes de preparation, compositions pharmaceutiques les contenant.
AU1748792A (en) * 1991-04-04 1992-11-02 Upjohn Company, The Phosphorus containing compounds as inhibitors of retroviruses
US5352667A (en) * 1991-11-22 1994-10-04 Ofer Lider Non-peptidic surrogates of the Arg-Gly-Asp sequence and pharmaceutical compositions comprising them
US5252591A (en) * 1992-08-14 1993-10-12 G. D. Searle & Company Pyridinyl-terminated alkylamino ethynyl alanine amino diol compounds for treatment of hypertension
AU674553B2 (en) * 1992-10-14 1997-01-02 Merck & Co., Inc. Fibrinogen receptor antagonists
NZ277206A (en) * 1993-12-06 1997-11-24 Cytel Corp Peptide inhibiting binding of vlh-4 receptor expressed in inflammatory leukocytes and fibronectin cs-1 peptide expressed on endothelial cells involved in inflammatory disease states
EP0760658B1 (en) * 1994-05-27 2002-11-13 Merck & Co. Inc. Compounds for inhibiting osteoclast-mediated bone resorption
US5650386A (en) * 1995-03-31 1997-07-22 Emisphere Technologies, Inc. Compositions for oral delivery of active agents
PT910563E (pt) * 1995-06-29 2003-09-30 Smithkline Beecham Corp Antagonistas de receptores de integrina
EP0880511A4 (en) * 1996-01-16 1999-06-16 Merck & Co Inc INTEGRIN RECEPTOR ANTAGONISTS

Also Published As

Publication number Publication date
DE69829996D1 (de) 2005-06-02
ATE294163T1 (de) 2005-05-15
ID24955A (id) 2000-08-31
JP2002508355A (ja) 2002-03-19
HUP0100397A3 (en) 2002-10-28
IL136495A0 (en) 2001-06-14
HRP20000401A2 (en) 2001-12-31
EA200000660A1 (ru) 2001-02-26
EP1040098A4 (en) 2002-10-30
IS5521A (is) 2000-05-31
AU1822099A (en) 1999-07-05
EA002822B1 (ru) 2002-10-31
DE69829996T2 (de) 2006-02-23
CA2315220C (en) 2006-03-21
WO1999031061A1 (en) 1999-06-24
NZ504893A (en) 2002-10-25
SK9192000A3 (en) 2001-03-12
GEP20032921B (en) 2003-03-25
EP1040098A1 (en) 2000-10-04
CA2315220A1 (en) 1999-06-24
NO20003114L (no) 2000-08-16
EP1040098B1 (en) 2005-04-27
BG104605A (bg) 2001-05-31
NO20003114D0 (no) 2000-06-16
KR20010033248A (ko) 2001-04-25
JP3585839B2 (ja) 2004-11-04
CN1284944A (zh) 2001-02-21
TR200002557T2 (tr) 2000-12-21
BR9813769A (pt) 2000-10-10
AU739811B2 (en) 2001-10-18
EE200000362A (et) 2001-12-17
ES2241192T3 (es) 2005-10-16
PL341215A1 (en) 2001-03-26

Similar Documents

Publication Publication Date Title
HUP0100397A2 (hu) Tetrahidro- vagy oktahidrobenzo-naftiridin és kinolinszármazékok, ezeket tartalmazó gyógyszerkészítmények és eljárás előállításukra
HUP0105409A2 (hu) Csípőbél-epesav transzport és taurokolát felvétel inhibitor aktivitású 1,2-benzotiazepin-származékok, alkalmazásuk és az ezeket tartalmazó gyógyszerkészítmények
SE9902987D0 (sv) Novel compounds
SE9904738D0 (sv) Novel compounds
HUP0104188A2 (hu) Antranilsav- és tioantranilsav-N-aril-amidok, előállításuk és alkalmazásuk VEGF receptor tirozinkináz inhibítorokként
HUP9903671A2 (hu) Gonadotropint leadó hormonok antagonistái,e vegyületeket tartalmazó gyógyászati készítmények,valamint azok előállítása
HUT67434A (en) Fluoroalkoxy-benzylamino derivatives of nitrogen containing heterocycles and pharmaceutical compositions containing them and process for their production
HUP9902121A2 (hu) Gonadotropin-leadó hormon antagonista hatású indolszármazékok és ezeket a vegyületeket tartalmazó gyógyszerkészítmények
DK0790986T3 (da) Anilinderivater
NO20053827L (no) Nye forbindelser.
HUP9901960A2 (hu) Kristályos ziprasidont tartalmazó gyógyszerkészítmények és eljárás ilyen kristályok előállítására
FI941987A (fi) Uudet aminohappojohdannaiset, menetelmät niiden valmistamiseksi ja näitä yhdisteitä sisältävät farmaseuttiset koostumukset
DE60214179D1 (de) IMIDAZOi1,2-AöPYRIDIN-DERIVATE ZUR PROPHYLAXE UND BEHANDLUNG VON HERPES-INFEKTIONEN
HUP0401009A2 (hu) 5-Hidroxitriptamin-6-ligandumokként alkalmazható 1-aril- vagy 1- alkil-szulfonilbenzazol-származékok, eljárás az előállításukra és ezeket tartalmazó gyógyszerkészítmények
FI875229A (fi) Menetelmä uusien farmakologisesti aktiivisten katekolijohdoksien valmistamiseksi
HUP0401333A2 (hu) Spiropirazol vegyületek és ezeket tartalmazó gyógyszerkészítmények
HUP0402227A2 (hu) Fenil-szubsztituált triazolok és az AKL5 kináz szelektív inhibitoraiként történő felhasználásuk és a vegyületeket tartalmazó gyógyszerkészítmények
DZ1694A1 (fr) &#34;n-(2-Aminoethyl)-benzothialozones&#34;.
HU911301D0 (en) Process for producing 2,9-disubstituted 4h-pyrido(1,2a)-pyrimidine derivatives and pharmaceutical preparatives containing these compounds as active substance
DE69911935D1 (de) Granulatimide-derivate zur behandlung von krebs
DE69330282D1 (de) Chinolon und acridinon derivate zur behandlung der harninkontinenz
HUP0400156A2 (hu) Pirrolidinszármazékok, mint Xa faktor inhibítorok, előállításuk és ezeket tartalmazó gyógyszerkészítmények
GR1001597B (el) Νέα βιολογικώς δραστικά παράγωγα εμπουρναμενίνης, φαρμακευτικές συν?έσεις οι οποίες περιέχουν αυτά και μέ?οδος δια την παρασκευή αυτών.
KR950014103A (ko) 1-[2H-1-벤조피란-2-온-8-일]-피페라진 유도체(1-[2H-1-benzopyran-2-one-8-yl]-piperazine derivatives)
NO179974C (no) Analogifremgangsmåte for fremstilling av terapeutisk aktive piperidinforbindelser