[go: up one dir, main page]

CO4990963A1 - Inhibidores del dominio sh2 de la familia src - Google Patents

Inhibidores del dominio sh2 de la familia src

Info

Publication number
CO4990963A1
CO4990963A1 CO98075225A CO98075225A CO4990963A1 CO 4990963 A1 CO4990963 A1 CO 4990963A1 CO 98075225 A CO98075225 A CO 98075225A CO 98075225 A CO98075225 A CO 98075225A CO 4990963 A1 CO4990963 A1 CO 4990963A1
Authority
CO
Colombia
Prior art keywords
ring
alkyl
andgt
aryl
heterocyclyl
Prior art date
Application number
CO98075225A
Other languages
English (en)
Inventor
Betageri Rajashekhar
Mario G Cardozo
Moss Neil
R Patel Usha
John Robert Proudfoot
Louis Beaulieu Pierre
Montse Llinas-Brune
Jean Marie Ferland
Original Assignee
Boehringer Ingelheim Pharma
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 Boehringer Ingelheim Pharma filed Critical Boehringer Ingelheim Pharma
Publication of CO4990963A1 publication Critical patent/CO4990963A1/es

Links

Classifications

    • 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
    • C07D213/72—Nitrogen atoms
    • C07D213/75—Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
    • 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
    • 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
    • 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
    • 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
    • A61P3/08—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
    • A61P35/00—Antineoplastic agents
    • 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
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • 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
    • 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
    • C07D405/02—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 two hetero rings
    • C07D405/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D405/02—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 two hetero rings
    • C07D405/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen 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
    • 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
    • C07D417/02—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 two hetero rings
    • C07D417/12—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 two hetero rings linked by a chain containing hetero atoms as chain links

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Rheumatology (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Transplantation (AREA)
  • Pain & Pain Management (AREA)
  • Emergency Medicine (AREA)
  • Dermatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Un compuesto de la fórmula (I): en donde: el anillo se selecciona del grupo que consiste en cicloalquilo C1 a C10 ; Arilo- Con el arilo seleccionado de fenilo, naftilo; fenilo y/o naftilo que son parcial o completamente halogenados, fenilo y/o naftilo sustituido con flúor, cloro, bromo, yodo, alquilo C1 a C10 , hidroxilo; nitro; -COOH; -COOH; -CO(alcoxi C1 a C6 ), - CO(alquilo C1 a C6 ); amino; alquilamino C1 a C10 ; dialquilamino C1 a C10 , Alcoxi C1 -C10 ; -NCOH; -NCI(alquilo C1 a C6 ); -NSO2 -Ph(halo)0-3 , Ph; -O-Ph; naftilo; -O-naftilo; pirrolilo; pirrolilo sustituido con alquilo C1 a C6 , piridilo; piridinilo; pirazinilo; pirimidinilo y piridazinilo; heterociclilo- con el heterociclilo seleccionado de heterociclos monocíclicos de 5-8 miembros con 1 a 4 heteroátomos seleccionados de nitrógeno, oxígeno, azufre o un heterociclilo bicíclico con 8-11 miembros con 1 a 4 heteroátomos seleccionados de nitrógeno, oxígeno, azufre. A se selecciona del grupo que consiste en alquilo C1 a C10 ; alquenilo C2 a C12 ; alquinilo C2 a C12 ; alcoxi C1 a C10 ; cicloalquilo C1 a C10 ; cicloalquenilo C2 a C12 ; heterocíclilo como en la definición del anillo a; arilo como se definió anteriormente para el anillo a; en donde dicho cicloalquilo, heterociclilo o arilo está opcionalmente enlazado a Q o N a través de un enlazador alcoxi C1 a C10 , -O-amino, alquilo C1 a C6 , alquil amino C1 a C6 , carbonilo, amido amido alquilo C1 a C10 , alcoxicarbonilo C1 a C10 , carbonil alquiloxi C1 a C10 , con el heterociclilo como en la definición para el anillo a, Q se selecciona del grupo que consiste en un enlace, ANDgt;C=O, ANDgt;S(O)2 y ANDgt;C=S; - 2 -B se selecciona de un grupo que consiste en H; alquilo C1 a C6 y un grupo protector de nitrógeno; R es un enlace o un enlazador alquilo C1 a C10 ; arilo como se definió para el anillo a; heterocíclilo con el heterociclilo como se definió para el anillo a o un enlazador cicloalquilo C1 a C10 ; C es una funcionalidad de cáracter ácido que lleva una o dos cargas negativas a pH fisiológico; D es ANDgt;CH2 ; ANDgt;C=O o ANDgt;C=S; E es un heterociclo insaturado de 6 miembros que tiene dos dobles enlaces dentro del anillo y los siguientes miembros del anillo:(a) uno o dos miembros del anillo de nitrógeno, opcionalmente sustituidos con Rb , (b) un miembro del anillo seleccionado del grupo que consiste en ANDgt;C=O; C=S; ANDgt;C=NH; ANDgt;C=N-alquilo C1 a C6 y un grupo protector de ANDgt;C=N-nitrógeno ANDgt;C=N; (c) un miembro del anillo ANDgt;C-Ra o ANDgt;N-Ra situado en posición meta con el punto de unión del heterociclo E al nitrógeno adyacente; y (d) dos o tres miembros del anillo de carbono adicionales, en donde dichos miembros del anillo de carbono adicionales están opcionalmente sustituidos con alquilo C1 a C10 ; alcoxi C1 a C10 ; flúor, cloro, bromo, o yodo, el arilo como se definió anteriormente para el anillo a; alquiloxi carbonilo C1 a C10 o alquilamino C1 a C10 . y si dos miembros del anillo opcionalmente sustituidos están presentes en posiciones adyacentes en el heterociclo E, muchos miembros del anillo adyacente pueden estar enlazados uno con otro para formar un anillo heterocíclico o carbocíclico de 5AND#8209;8 miembros condensado, que puede ser aromático, parcialmente insaturado o totalmente saturado, Ra se selecciona del grupo que consiste en alquilo C1 a C10 ; alquenilo C2 a C12 ; alquinilo C2 a C12 ; heterociclilo en la definicion como para el anillo a; cicloalquilo C1 a C10 , arilo como se definió anteriormente para el anillo a; en donde dicho cicloalquilo o arilo puede estar opcionalmente estar enlazados al carbono o nitrógeno adyacente a través de un enlazador alquilo C1 a C6 ; alcoxi C1 a C6 , alquilamino C1 a C6 , alquilurea C1 a C6 , o alquil carboxiloxi C1 a C6 ; cada Rb se selecciona del grupo que consiste en H; alquilo C1 a C10 ; alcoxi C1 a C10 , flúor, cloro, bromo o yodo; arilo como se definió anteriormente para el anillo a; alquiloxi carboxilo C1 a C10 ; y alquilamino C1 a C10 .Y los tautómeros, sales y ésteres farmacéuticamente aceptables de estos.
CO98075225A 1997-12-18 1998-12-17 Inhibidores del dominio sh2 de la familia src CO4990963A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US6997197P 1997-12-18 1997-12-18

Publications (1)

Publication Number Publication Date
CO4990963A1 true CO4990963A1 (es) 2000-12-26

Family

ID=22092332

Family Applications (1)

Application Number Title Priority Date Filing Date
CO98075225A CO4990963A1 (es) 1997-12-18 1998-12-17 Inhibidores del dominio sh2 de la familia src

Country Status (13)

Country Link
US (3) US6054470A (es)
EP (1) EP1045836B1 (es)
JP (1) JP4524039B2 (es)
AR (1) AR017895A1 (es)
AT (1) ATE388139T1 (es)
AU (1) AU1719499A (es)
CA (1) CA2315113C (es)
CO (1) CO4990963A1 (es)
DE (1) DE69839221T2 (es)
ES (1) ES2302363T3 (es)
UY (1) UY25313A1 (es)
WO (1) WO1999031066A1 (es)
ZA (1) ZA9811570B (es)

Families Citing this family (48)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2222753T3 (es) * 1999-04-15 2005-02-01 Boehringer Ingelheim Pharmaceuticals, Inc. Compuestos utiles como mimeticos de fosfotirosina.
EP1244677A1 (en) 1999-12-22 2002-10-02 Merck Frosst Canada Inc. Phosphonic acid biaryl derivatives as inhibitors of protein tyrosine phosphatase 1b (ptp-1b)
US6583126B2 (en) 1999-12-22 2003-06-24 Merck Erosst Canada & Co. Phosphonic acid derivatives as inhibitors of protein tyrosine phosphatase 1B (PTP-1B)
US6486142B2 (en) 1999-12-22 2002-11-26 Merck Frosst Canada & Co. Phosphonic acid derivatives as inhibitors of protein tyrosine phosphatase 1B (PTP-1B)
US6777433B2 (en) 1999-12-22 2004-08-17 Merck Frosst Canada & Co. Protein tyrosine phosphatase 1B (PTP-1B) inhibitors containing two ortho-substituted aromatic phosphonates
AU2001243601A1 (en) * 2000-03-10 2001-09-24 Ariad Pharmaceuticals, Inc. Caprolactam derivatives and uses thereof
WO2001070754A1 (en) 2000-03-22 2001-09-27 Merck Frosst Canada & Co. Sulfur substituted aryldifluoromethylphosphonic acids as ptp-1b inhibitors
PE20011350A1 (es) 2000-05-19 2002-01-15 Vertex Pharma PROFARMACO DE UN INHIBIDOR DE ENZIMA CONVERTIDORA DE INTERLEUCINA-1ß (ICE)
CN100575345C (zh) 2000-12-28 2009-12-30 盐野义制药株式会社 对2型大麻素受体具有结合活性的吡啶酮衍生物
IL141647A0 (en) 2001-02-26 2002-03-10 Yeda Res & Dev Synthetic human peptides and pharmaceutical compositions comprising them for the treatment of systemic lupus erythematosus
US7482366B2 (en) 2001-12-21 2009-01-27 X-Ceptor Therapeutics, Inc. Modulators of LXR
WO2003059884A1 (en) * 2001-12-21 2003-07-24 X-Ceptor Therapeutics, Inc. Modulators of lxr
AU2004206844A1 (en) 2003-01-14 2004-08-05 Teva Pharmaceutical Industries, Ltd. Parenteral formulations of a peptide for the treatment of systemic lupus erythematosus
US20050119163A1 (en) 2003-09-18 2005-06-02 The Government Of The United States Of America, As Represented By The Secretary, SH2 domain binding inhibitors
HUE024556T2 (hu) 2004-03-12 2016-02-29 Vertex Pharma Eljárások és intermedierek aszparagin acetál kapszáz inhibitorok elõállítására
EP1768662A2 (en) 2004-06-24 2007-04-04 Novartis Vaccines and Diagnostics, Inc. Small molecule immunopotentiators and assays for their detection
TWI417095B (zh) 2006-03-15 2013-12-01 Janssen Pharmaceuticals Inc １，４-二取代之３-氰基-吡啶酮衍生物及其作為ｍＧｌｕＲ２-受體之正向異位性調節劑之用途
TW200845978A (en) 2007-03-07 2008-12-01 Janssen Pharmaceutica Nv 3-cyano-4-(4-tetrahydropyran-phenyl)-pyridin-2-one derivatives
TW200900065A (en) 2007-03-07 2009-01-01 Janssen Pharmaceutica Nv 3-cyano-4-(4-pyridinyloxy-phenyl)-pyridin-2-one derivatives
TWI448284B (zh) * 2007-04-24 2014-08-11 Theravance Inc 雙效抗高血壓劑
MY152078A (en) 2007-09-14 2014-08-15 Ortho Mcneil Janssen Pharm 1',3'-disubstituted-4-phenyl-3,4,5,6-tetrahydro-2h,1'h-[1,4']bipyridinyl-2'-ones
AU2009289784B2 (en) 2008-09-02 2012-03-22 Addex Pharma S.A. 3-azabicyclo[3.1.0]hexyl derivatives as modulators of metabotropic glutamate receptors
WO2010060589A1 (en) 2008-11-28 2010-06-03 Ortho-Mcneil-Janssen Pharmaceuticals, Inc. Indole and benzoxazine derivatives as modulators of metabotropic glutamate receptors
WO2010091164A1 (en) * 2009-02-06 2010-08-12 Exelixis, Inc. Inhibitors of glucosylceramide synthase
AU2010246609B2 (en) 2009-05-12 2013-09-05 Addex Pharma S.A. 1,2,4-triazolo [4,3-a] pyridine derivatives and their use for the treatment or prevention of neurological and psychiatric disorders
NZ596053A (en) 2009-05-12 2013-05-31 Janssen Pharmaceuticals Inc 1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of mglur2 receptors
MY153913A (en) 2009-05-12 2015-04-15 Janssen Pharmaceuticals Inc 7-aryl-1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of mglur2 receptors
EP2661435B1 (en) 2010-11-08 2015-08-19 Janssen Pharmaceuticals, Inc. 1,2,4-TRIAZOLO[4,3-a]PYRIDINE DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS
EP2643320B1 (en) 2010-11-08 2015-03-04 Janssen Pharmaceuticals, Inc. 1,2,4-TRIAZOLO[4,3-a]PYRIDINE DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS
CN103298810B (zh) 2010-11-08 2016-03-16 杨森制药公司 1,2,4-三唑并[4,3-a]吡啶衍生物及其作为MGLUR2受体的正变构调节剂的用途
JP6450323B2 (ja) 2013-01-07 2019-01-09 ユニバーシティ オブ サザン カリフォルニア デオキシウリジントリホスファターゼ阻害剤
JO3368B1 (ar) 2013-06-04 2019-03-13 Janssen Pharmaceutica Nv مركبات 6، 7- ثاني هيدرو بيرازولو [5،1-a] بيرازين- 4 (5 يد)- اون واستخدامها بصفة منظمات تفارغية سلبية لمستقبلات ميجلور 2
JO3367B1 (ar) 2013-09-06 2019-03-13 Janssen Pharmaceutica Nv مركبات 2،1، 4- ثلاثي زولو [3،4-a] بيريدين واستخدامها بصفة منظمات تفارغية موجبة لمستقبلات ميجلور 2
JP6513095B2 (ja) 2014-01-03 2019-05-15 ユニバーシティ オブ サザン カリフォルニア ヘテロ原子含有デオキシウリジントリホスファターゼ阻害剤
DK3096790T3 (da) 2014-01-21 2019-10-07 Janssen Pharmaceutica Nv Kombinationer omfattende positive allosteriske modulatorer eller orthosteriske agonister af metabotrop glutamaterg subtype 2-receptor og anvendelse af disse
KR20220038826A (ko) 2014-01-21 2022-03-29 얀센 파마슈티카 엔.브이. 대사 조절형 글루탐산 작동성 수용체 제2아형의 양성 알로스테릭 조절제 또는 오르토스테릭 작동제를 포함하는 조합 및 그 용도
US10544105B2 (en) 2015-07-08 2020-01-28 Cv6 Therapeutics (Ni) Limited Deoxyuridine triphosphatase inhibitors containing cyclopropano linkage
US10577321B2 (en) 2015-07-08 2020-03-03 University Of Southern California Deoxyuridine triphosphatase inhibitors
DK3319939T3 (da) 2015-07-08 2025-02-24 Cv6 Therapeutics Ni Ltd Hydantoin indeholdende deoxyuridintriphosphatase-inhibitorer
US10570100B2 (en) 2015-07-08 2020-02-25 University Of Southern California Deoxyuridine triphosphatase inhibitors containing amino sulfonyl linkage
WO2017156350A1 (en) 2016-03-09 2017-09-14 K-Gen, Inc. Methods of cancer treatment
US11014924B2 (en) 2016-11-23 2021-05-25 Cv6 Therapeutics (Ni) Limited Hydantoin containing deoxyuridine triphosphatase inhibitors
US10858344B2 (en) 2016-11-23 2020-12-08 Cv6 Therapeutics (Ni) Limited Hydantoin containing deoxyuridine triphosphatase inhibitors
US11174271B2 (en) 2016-11-23 2021-11-16 Cv6 Therapeutics (Ni) Limited 6-membered uracil isosteres
US10829457B2 (en) 2016-11-23 2020-11-10 Cv6 Therapeutics (Ni) Limited Nitrogen ring linked deoxyuridine triphosphatase inhibitors
WO2018098209A1 (en) 2016-11-23 2018-05-31 Cv6 Therapeutics (Ni) Limited Amino sulfonyl compounds
WO2018128720A1 (en) 2017-01-05 2018-07-12 Cv6 Therapeutics (Ni) Limited Uracil containing compounds
CN119954663A (zh) * 2025-02-06 2025-05-09 山东师范大学 一种针对氨基/叠氮/羧基化合物的稳定同位素标记试剂及其制备方法与应用

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH0662529B2 (ja) * 1984-07-13 1994-08-17 三共株式会社 アミノ酸誘導体
AU598750B2 (en) * 1985-09-27 1990-07-05 Mitsubishi Chemical Corporation Phenylalanine derivative and proteinase inhibitor
US5580979A (en) * 1994-03-15 1996-12-03 Trustees Of Tufts University Phosphotyrosine peptidomimetics for inhibiting SH2 domain interactions
US5716929A (en) * 1994-06-17 1998-02-10 Vertex Pharmaceuticals, Inc. Inhibitors of interleukin-1β converting enzyme
WO1996023813A1 (en) * 1995-02-01 1996-08-08 Affymax Technologies N.V. Peptides and compounds that bind to sh2 domains
AU4440496A (en) * 1995-02-10 1996-08-22 Smithkline Beecham Corporation Use of src SH2 specific compounds to treat a bone resorption disease
AU7392696A (en) * 1995-10-04 1997-04-28 Warner-Lambert Company Compounds, compositions and methods for inhibiting the binding of proteins containing an sh2 domain to cognate phosphorylated proteins
AU2277597A (en) * 1996-02-23 1997-09-10 Ariad Pharmaceuticals, Inc. New inhibitors of sh2-mediated processes

Also Published As

Publication number Publication date
EP1045836A1 (en) 2000-10-25
AU1719499A (en) 1999-07-05
DE69839221D1 (de) 2008-04-17
UY25313A1 (es) 2000-12-29
ATE388139T1 (de) 2008-03-15
CA2315113C (en) 2009-12-08
EP1045836B1 (en) 2008-03-05
JP2003514762A (ja) 2003-04-22
AR017895A1 (es) 2001-10-24
DE69839221T2 (de) 2009-04-30
ZA9811570B (en) 1999-09-16
US6284768B1 (en) 2001-09-04
US6268365B1 (en) 2001-07-31
US6054470A (en) 2000-04-25
JP4524039B2 (ja) 2010-08-11
CA2315113A1 (en) 1999-06-24
WO1999031066A1 (en) 1999-06-24
ES2302363T3 (es) 2008-07-01

Similar Documents

Publication Publication Date Title
CO4990963A1 (es) Inhibidores del dominio sh2 de la familia src
BR0108816A (pt) Derivados de quinolina como antagonistas alfa-2
BRPI0014526C1 (pt) compostos cíclicos de seis elementos contendo nitrogênio aromático, composição farmacêutica e uso do mesmo
TR200201505T2 (tr) Terapötik maddeler olarak pirazolopirimidinler
EA200300919A1 (ru) N-замещенные неарильные гетероциклические антагонисты nmda/nr2b
BRPI0616574A2 (pt) derivado de sulfonamida tendo atividade antagonìstica de receptor de pgd2
AR030959A1 (es) Derivados de aminoalcoholes, procedimiento para prepararlos, el uso de los mismos para preparar medicamentos y las composiciones farmaceuticas que las contienen
KR927003052A (ko) 2-아릴티아졸 유도체 및 그의 약제학적 조성물
ES2182535T3 (es) Derivados de benzo(b)tiepina-1,-dioxido, procedimiento para su preparacion, medicamentos que contienen estos compuestos y su utilizacion.
ATE194335T1 (de) 4,5-diaryloxazol-derivate
ATE402174T1 (de) Imidazopyridinderivate als kinaseinhibitoren
MX9603506A (es) Compuestos oxazol aromaticos, heterociclicos y sus usos.
ES2053609T3 (es) Derivados de urea inhibidores de lipoxigenasa.
EP1310488A4 (en) CONCENTRATED BICYCLIC AMID COMPOUNDS AND THEIR MEDICAL USE
FI932518A0 (fi) Antagonister av angiotensin II
FI950309A0 (fi) Proliiniamidijohdannaisia
DE69835430D1 (de) Sulfonamidderivate, ihre herstellung und verwendung
ES2065182T3 (es) Derivados de fenilamidinas utiles como inhibidores de la agregacion de plaquetas.
AR016868A1 (es) Derivados de 3-amidinoanilina, composicion farmaceutica, un inhibidor del factor x de coagulacion de la sangre activado, usos y procedimiento en lafabricacion de una composicion farmaceutica y de un inhibidor de la prevencion y tratamiento de enfermedades tromboembolicas e intermediarios en la prepa
BR0012697A (pt) Inibidores da diferenciação de th2
AR040626A1 (es) Derivados de quinolina utiles como ligandos del receptor del neuropeptido y (npy)
BG100016A (bg) Нiv протеазни инхибитори във фармацевтични комбинации за лечение на спин
ATE377602T1 (de) Morphinanderivate und ihre medizinische anwendung
ATE271868T1 (de) Neue cathechole als antimikrobielle mittel
ES2191659T3 (es) Derivados heterociclicos substituidos utiles como inhibidores de la agregacion plaquetaria.