Nothing Special   »   [go: up one dir, main page]

PE20060748A1 - Derivados de indolcarboxamida como inhibidores de quinasa ikk2 - Google Patents

Derivados de indolcarboxamida como inhibidores de quinasa ikk2

Info

Publication number
PE20060748A1
PE20060748A1 PE2005001077A PE2005001077A PE20060748A1 PE 20060748 A1 PE20060748 A1 PE 20060748A1 PE 2005001077 A PE2005001077 A PE 2005001077A PE 2005001077 A PE2005001077 A PE 2005001077A PE 20060748 A1 PE20060748 A1 PE 20060748A1
Authority
PE
Peru
Prior art keywords
alkylene
phenyl
indolcarboxamide
ikk2
sulfonil
Prior art date
Application number
PE2005001077A
Other languages
English (en)
Inventor
Jeffrey K Kerns
Michael Lindenmuth
Hong Nie
Sonia M Thomas
Xichen Lin
Original Assignee
Smithkline Beecham Corp
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 Smithkline Beecham Corp filed Critical Smithkline Beecham Corp
Publication of PE20060748A1 publication Critical patent/PE20060748A1/es

Links

Classifications

    • 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
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • 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
    • A61P11/06—Antiasthmatics
    • 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
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • 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
    • 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
    • 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
    • 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
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • 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
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • 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
    • A61P9/10—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
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
    • 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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Diabetes (AREA)
  • Virology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Cardiology (AREA)
  • Dermatology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Urology & Nephrology (AREA)
  • Hematology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Emergency Medicine (AREA)
  • Vascular Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Transplantation (AREA)

Abstract

REFERIDA A UN COMPUESTO DERIVADO DE INDOLCARBOXAMIDA DE FORMULA I, DONDE R1 ES H, HALOGENO O UN GRUPO -YZ; R2 ES H, F O Cl; R3 ES H, F O Cl; Z ES ARILO O HETEROARILO OPCIONALMENTE SUSTITUIDOS CON HALO, CN, C(O)H, ENTRE OTROS; U ES UN ENLACE, ALQUILENO C1-C6 O ALQUENILENO C2-C6; V ES FENILO, HETEROARILO DE 5 O 6 MIEMBROS, HETEROCICLOALQUILO DE 5 A 7 MIEMBROS, ENTRE OTROS; m ES 1 O 2; R4 ES UN GRUPO -X-R5; X ES UN ENLACE, ALQUILENO C1-C6, ALQUENILENO C2-C6, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: 3-{1-[(2-AMINOETIL)SULFONIL]-4-PIPERIDINIL}-5-FENIL-1H-INDOL-7-CARBOXAMIDA, 3-(1-{[2-(DIMETILAMINO)ETIL]SULFONIL}-4-PIPERIDINIL)-5-FENIL-1H-INDOL-7-CARBOXAMIDA, 3-(1{[2-(DIMETILAMINO)ETIL]SULFONIL}-4-PIPERIDINIL)-5-FENIL-1H-INDOL-7-CARBOXAMIDA, ENTRE OTROS. TAMBIEN ESTA REFERIDA A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE LA ACTIVIDAD DE LA QUINASA, PARTICULARMENTE DE LA IKK2 Y SON UTILES PARA EL TRATAMIENTO DE TRASTORNOS INFLAMATORIOS Y DE REPARACION TISULAR TALES COMO ARTRITIS REUMATOIDE, ASMA, ENFERMEDAD OBSTRUCTIVA PULMONAR CRONICA, ENTRE OTROS
PE2005001077A 2004-09-21 2005-09-19 Derivados de indolcarboxamida como inhibidores de quinasa ikk2 PE20060748A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US61176104P 2004-09-21 2004-09-21
US69545405P 2005-06-30 2005-06-30

Publications (1)

Publication Number Publication Date
PE20060748A1 true PE20060748A1 (es) 2006-10-01

Family

ID=36090636

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2005001077A PE20060748A1 (es) 2004-09-21 2005-09-19 Derivados de indolcarboxamida como inhibidores de quinasa ikk2

Country Status (16)

Country Link
US (1) US7858796B2 (es)
EP (1) EP1793826A4 (es)
JP (1) JP2008513500A (es)
KR (1) KR20070057969A (es)
AR (1) AR054084A1 (es)
AU (1) AU2005286795A1 (es)
BR (1) BRPI0515524A (es)
CA (1) CA2581180A1 (es)
IL (1) IL181877A0 (es)
MA (1) MA28912B1 (es)
MX (1) MX2007003283A (es)
NO (1) NO20071988L (es)
PE (1) PE20060748A1 (es)
SG (1) SG155932A1 (es)
TW (1) TW200626142A (es)
WO (1) WO2006034317A2 (es)

Families Citing this family (35)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0400895D0 (en) * 2004-01-15 2004-02-18 Smithkline Beecham Corp Chemical compounds
PE20060373A1 (es) * 2004-06-24 2006-04-29 Smithkline Beecham Corp Derivados 3-piperidinil-7-carboxamida-indazol como inhibidores de la actividad cinasa de ikk2
JP5059756B2 (ja) * 2005-06-30 2012-10-31 グラクソスミスクライン・リミテッド・ライアビリティ・カンパニー 化合物
US8063071B2 (en) * 2007-10-31 2011-11-22 GlaxoSmithKline, LLC Chemical compounds
EP1948187A4 (en) * 2005-11-18 2010-11-03 Glaxosmithkline Llc CHEMICAL COMPOUNDS
EP1959737A4 (en) * 2005-12-16 2010-12-08 Glaxosmithkline Llc CHEMICAL COMPOUNDS
TWI403320B (zh) 2005-12-16 2013-08-01 Infinity Discovery Inc 用於抑制ｂｃｌ蛋白和結合夥伴間之交互作用的化合物及方法
AR065804A1 (es) * 2007-03-23 2009-07-01 Smithkline Beecham Corp Compuesto de indol carboxamida, composicion farmaceutica que lo comprende y uso de dicho compuesto para preparar un medicamento
EP2370407B1 (en) * 2008-12-19 2014-06-18 Bristol-Myers Squibb Company Carbazole and carboline kinase inhibitors
CN102325753B (zh) 2008-12-19 2014-09-10 百时美施贵宝公司 用作激酶抑制剂的咔唑甲酰胺化合物
US8354539B2 (en) 2009-03-10 2013-01-15 Glaxo Group Limited Indole derivatives as IKK2 inhibitors
EP3246027A1 (en) 2010-05-07 2017-11-22 GlaxoSmithKline LLC Indole derivatives for the treatment of cancer
EP2582668B1 (en) 2010-06-16 2016-01-13 Bristol-Myers Squibb Company Carboline carboxamide compounds useful as kinase inhibitors
KR102273997B1 (ko) * 2013-06-26 2021-07-08 애브비 인코포레이티드 Btk 억제제로서 1급 카복스아미드
RU2677884C2 (ru) 2013-09-30 2019-01-22 Гуанчжоу Иннокэа Фарма Тек Ко., Лтд. Замещенные никотинимидные ингибиторы втк, их получение и применение в терапии раковых, воспалительных и аутоиммунных заболеваний
MX2017005259A (es) 2014-10-24 2017-07-26 Bristol Myers Squibb Co Compuestos de indol carboxamida utiles como inhibidores de cinasas.
TW201718581A (zh) 2015-10-19 2017-06-01 英塞特公司 作為免疫調節劑之雜環化合物
EP4141002A1 (en) 2015-11-19 2023-03-01 Incyte Corporation Heterocyclic compounds as immunomodulators
US20170174679A1 (en) 2015-12-22 2017-06-22 Incyte Corporation Heterocyclic compounds as immunomodulators
WO2017192961A1 (en) 2016-05-06 2017-11-09 Incyte Corporation Heterocyclic compounds as immunomodulators
WO2017205464A1 (en) 2016-05-26 2017-11-30 Incyte Corporation Heterocyclic compounds as immunomodulators
MD3472167T2 (ro) 2016-06-20 2023-02-28 Incyte Corp Compuși heterociclici ca imunomodulatori
MA45669A (fr) 2016-07-14 2019-05-22 Incyte Corp Composés hétérocycliques utilisés comme immunomodulateurs
EP3504198B1 (en) 2016-08-29 2023-01-25 Incyte Corporation Heterocyclic compounds as immunomodulators
WO2018119221A1 (en) 2016-12-22 2018-06-28 Incyte Corporation Pyridine derivatives as immunomodulators
WO2018119266A1 (en) 2016-12-22 2018-06-28 Incyte Corporation Benzooxazole derivatives as immunomodulators
WO2018119236A1 (en) 2016-12-22 2018-06-28 Incyte Corporation Triazolo[1,5-a]pyridine derivatives as immunomodulators
LT3774791T (lt) 2018-03-30 2023-04-11 Incyte Corporation Hererocikliniai junginiai kaip imunomoduliatoriai
EP3790877B1 (en) 2018-05-11 2023-03-01 Incyte Corporation Tetrahydro-imidazo[4,5-c]pyridine derivatives as pd-l1 immunomodulators
CA3150434A1 (en) 2019-08-09 2021-02-18 Incyte Corporation Salts of a pd-1/pd-l1 inhibitor
AU2020357514A1 (en) 2019-09-30 2022-04-07 Incyte Corporation Pyrido[3,2-d]pyrimidine compounds as immunomodulators
JP2023500395A (ja) 2019-11-11 2023-01-05 インサイト・コーポレイション Ｐｄ－１／ｐｄ－ｌ１阻害剤の塩及び結晶形態
CN116670114A (zh) 2020-11-06 2023-08-29 因赛特公司 用于制备pd-1/pd-l1抑制剂以及其盐和结晶形式的方法
US11780836B2 (en) 2020-11-06 2023-10-10 Incyte Corporation Process of preparing a PD-1/PD-L1 inhibitor
TW202233615A (zh) 2020-11-06 2022-09-01 美商英塞特公司 Ｐｄ—１／ｐｄ—ｌ１抑制劑之結晶形式

Family Cites Families (69)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4775761A (en) * 1983-08-22 1988-10-04 Hoechst-Roussel Pharmaceuticals, Inc. 3-(piperidinyl)- and 3-(pyrrolidinyl)-1H-indazoles
US5256673A (en) * 1983-11-25 1993-10-26 Merck Patent Gesellschaft Mit Beschrankter Haftung Indole-3-yl-A-tetrahydropyridyl or piperidyl compounds
DE3342632A1 (de) 1983-11-25 1985-06-05 Merck Patent Gmbh, 6100 Darmstadt Indolderivate
EP0279263B1 (en) 1987-02-10 1993-08-04 Abbott Laboratories Indole, benzofuran, benzothiophene containing lipoxygenase inhibiting compounds
IL95584A (en) 1989-09-07 1995-03-15 Abbott Lab Indole-, benzoporene- and benzothiophene compounds including lipoxygenase-inhibiting compounds and pharmaceutical compounds containing them
US5330986A (en) * 1992-11-24 1994-07-19 Hoechst-Roussel Pharmaceuticals Inc. Indole-7-carboxamide derivatives
FR2701026B1 (fr) 1993-02-02 1995-03-31 Adir Nouveaux dérivés de l'indole, de l'indazole et du benzisoxazole, leur procédé de préparation et les compositions pharmaceutiques qui les contiennent.
DE19500689A1 (de) 1995-01-12 1996-07-18 Merck Patent Gmbh Indolpiperidin-Derivate
EP1077213A3 (en) 1996-06-14 2001-06-13 Eli Lilly And Company Inhibition of serotonin reuptake
US5846982A (en) 1996-06-14 1998-12-08 Eli Lilly And Company Inhibition of serotonin reuptake
AR013669A1 (es) 1997-10-07 2001-01-10 Smithkline Beecham Corp Compuestos y metodos
DE19807993A1 (de) 1998-02-26 1999-09-02 Bayer Ag Verwendung von ß-Carbolinderivaten zur Bekämpfung von TNF-alpha-abhängigen Krankheiten
CZ2001960A3 (cs) * 1998-09-18 2001-10-17 Basf Aktiengesellschaft Pyrrolopyrimidiny jako inhibitory protein kinasy
DE19928424A1 (de) 1999-06-23 2000-12-28 Aventis Pharma Gmbh Substituierte Benzimidazole
DE19951360A1 (de) 1999-10-26 2001-05-03 Aventis Pharma Gmbh Substituierte Indole
US6245799B1 (en) * 1999-11-08 2001-06-12 American Home Products Corp [(Indol-3-yl)-cycloalkyl]-3-substituted azetidines for the treatment of central nervous system disorders
WO2001034598A1 (en) 1999-11-08 2001-05-17 Wyeth [(indol-3-yl)-cycloalkyl]-3-substituted azetidines for the treatment of central nervous system disorders
GB0003154D0 (en) 2000-02-12 2000-04-05 Astrazeneca Uk Ltd Novel compounds
WO2001068648A1 (en) 2000-03-15 2001-09-20 Aventis Pharma Deutschland Gmbh Substituted beta-carbolines with ikb-kinase inhibiting activity
EP1209158A1 (en) 2000-11-18 2002-05-29 Aventis Pharma Deutschland GmbH Substituted beta-carbolines
EP1134221A1 (en) 2000-03-15 2001-09-19 Aventis Pharma Deutschland GmbH Substituted beta-carbolines as lkB kinase inhibitors
CN1814596A (zh) 2000-04-28 2006-08-09 阿卡蒂亚药品公司 毒蕈碱性激动剂
AU2001256714A1 (en) 2000-05-15 2001-11-26 Kissei Pharmaceutical Co. Ltd. Water-based liquid preparation
US6414013B1 (en) 2000-06-19 2002-07-02 Pharmacia & Upjohn S.P.A. Thiophene compounds, process for preparing the same, and pharmaceutical compositions containing the same background of the invention
CA2419550A1 (en) 2000-08-14 2002-02-21 Ortho-Mcneil Pharmaceutical, Inc. Substituted pyrazoles
WO2002016353A1 (en) 2000-08-17 2002-02-28 Celltech R & D Limited Bicyclic heteroaromatic derivatives for the treatment of immune and inflammatory disorders
US6369032B1 (en) * 2000-09-06 2002-04-09 Ortho-Mcneil Pharmaceutical, Inc. Method for treating allergies
JP4272338B2 (ja) 2000-09-22 2009-06-03 バイエル アクチェンゲゼルシャフト ピリジン誘導体
AU1182702A (en) 2000-10-03 2002-04-15 Bristol Myers Squibb Co Amino-substituted tetracyclic compounds useful as anti-inflammatory agents and pharmaceutical compositions comprising same
US6869956B2 (en) * 2000-10-03 2005-03-22 Bristol-Myers Squibb Company Methods of treating inflammatory and immune diseases using inhibitors of IκB kinase (IKK)
AU2002211663A1 (en) * 2000-10-12 2002-04-22 Smith Kline Beecham Corporation Nf-$g(k)b inhibitors
JP2004532797A (ja) 2000-10-12 2004-10-28 スミスクライン・ビーチャム・コーポレイション ＮＦ−κＢ阻害剤
AU3980602A (en) * 2000-10-26 2002-06-03 Tularik Inc Antiinflammation agents
JP2002193938A (ja) 2000-12-01 2002-07-10 Bayer Ag ４−アリールピリジン誘導体
US7122544B2 (en) 2000-12-06 2006-10-17 Signal Pharmaceuticals, Llc Anilinopyrimidine derivatives as IKK inhibitors and compositions and methods related thereto
DK1355904T3 (da) 2000-12-22 2007-10-15 Wyeth Corp Heterocyclindazol- og -azaindazolforbindelser som 5-hydroxytryptamin-6-ligander
JP2004529088A (ja) 2001-02-01 2004-09-24 ブリストル−マイヤーズ　スクイブ　カンパニー ＩｋＢキナーゼ（ＩＫＫ）のインヒビターを用いる炎症性および免疫疾患の処置法
DE10112151A1 (de) 2001-03-14 2002-09-19 Merck Patent Gmbh Substituierte Benzofuran-2-carbonsäureamide
WO2002094265A1 (en) 2001-05-24 2002-11-28 Leo Pharma A/S A method of modulating nf-$g(k)b activity
US20030045515A1 (en) 2001-05-24 2003-03-06 Lise Binderup Combination medicament for treatment of neoplastic diseases
CA2447021C (en) 2001-05-24 2010-08-10 Leo Pharma A/S Pyridyl cyanoguanidine compounds
SE0102616D0 (sv) 2001-07-25 2001-07-25 Astrazeneca Ab Novel compounds
SE0102617D0 (sv) 2001-07-25 2001-07-25 Astrazeneca Ab Novel compounds
US20030127204A1 (en) 2001-09-06 2003-07-10 Varnell Daniel F. Amphoteric polymer resins that increase the rate of sizing development
BR0212617A (pt) 2001-09-19 2005-02-09 Pharmacia Corp Compostos de pirazolila substituìdo para o tratamento de inflamação
WO2003027075A2 (en) 2001-09-19 2003-04-03 Pharmacia Corporation Substituted pyrazolyl benzenesulfamide compounds for the treatment of inflammation
WO2003035625A1 (en) * 2001-09-19 2003-05-01 Pharmacia Corporation Substituted indazole compounds for the treatment of inflammation
BR0212611A (pt) 2001-09-19 2004-08-17 Pharmacia Corp Compostos de pirazolila substituìdos para o tratamento da inflamação
BR0213734A (pt) 2001-10-30 2004-10-19 Pharmacia Corp Derivados de carboxamida heteroaromático para o tratamento de inflamação
MXPA04008130A (es) 2002-02-19 2004-11-26 Pharmacia Corp Derivados triciclicos de pirazol para el tratamiento de la inflamacion.
US6933294B2 (en) 2002-04-03 2005-08-23 Bristol-Myers Squibb Company Thiophene-based tricyclic compounds and pharmaceutical compositions comprising same
EP1501805A1 (en) 2002-05-09 2005-02-02 Pharmacia Corporation Substituted pyrazolyl compounds for the treatment of inflammation
DK1513516T3 (da) 2002-06-06 2009-10-19 Boehringer Ingelheim Pharma Substitueret 3-amino-thieno(2,3-b)-pyridin-2-carboxylsyreamid-forbindelser og fremgangsmåder til fremstilling og deres anvendelser
US6900206B2 (en) * 2002-06-20 2005-05-31 Bristol-Myers Squibb Company Indole, azaindole and related heterocyclic sulfonylureido piperazine derivatives
DE10237722A1 (de) 2002-08-17 2004-08-19 Aventis Pharma Deutschland Gmbh Indol- oder Benzimidazolderivate zur Modulation der IKappaB-Kinase
ES2349164T3 (es) 2002-08-29 2010-12-28 Boehringer Ingelheim Pharmaceuticals Inc. Derivados de 3-(sulfonamidoetil)-indol para uso como compuestos miméticos de glucocorticoides en el tratamiento de enfermedades inflamatorias, alérgicas y proliferativas.
SE0202693D0 (sv) * 2002-09-11 2002-09-11 Astrazeneca Ab Compounds
US6919334B2 (en) 2002-09-12 2005-07-19 Wyeth Antidepressant azaheterocyclymethyl derivatives of 4,5-dihydroimidazo[1,4,5-de][1,4]benzoxazine
US7135479B2 (en) 2002-09-12 2006-11-14 Wyeth Antidepressant azaheterocyclylmethyl derivatives of heterocycle-fused benzodioxans
US6911445B2 (en) 2002-09-12 2005-06-28 Wyeth Antidepressant cycloalkylamine derivatives of heterocycle-fused benzodioxans
DE10259244A1 (de) 2002-12-17 2004-07-01 Merck Patent Gmbh N-(Indolethyl-)cycloamin-Verbindungen
US7329668B2 (en) 2003-02-25 2008-02-12 Bristol-Myers Squibb Company Pyrazolopurine-based tricyclic compounds and pharmaceutical compositions comprising same
GB0308466D0 (en) 2003-04-11 2003-05-21 Novartis Ag Organic compounds
US7176214B2 (en) 2003-05-21 2007-02-13 Bristol-Myers Squibb Company Imidazo-fused oxazolo[4,5-β]pyridine and imidazo-fused thiazolo[4,5-β]pyridine based tricyclic compounds and pharmaceutical compositions comprising same
WO2005012283A1 (en) 2003-07-31 2005-02-10 Boehringer Ingelheim Pharmaceuticals, Inc. Substituted benzothiophene compounds and uses thereof
US7291733B2 (en) 2003-10-10 2007-11-06 Boehringer Ingelheim Pharmaceuticals, Inc. Substituted tricyclic heterocycles and their uses
GB0400895D0 (en) * 2004-01-15 2004-02-18 Smithkline Beecham Corp Chemical compounds
PE20060373A1 (es) * 2004-06-24 2006-04-29 Smithkline Beecham Corp Derivados 3-piperidinil-7-carboxamida-indazol como inhibidores de la actividad cinasa de ikk2
JP5059756B2 (ja) 2005-06-30 2012-10-31 グラクソスミスクライン・リミテッド・ライアビリティ・カンパニー 化合物

Also Published As

Publication number Publication date
AU2005286795A1 (en) 2006-03-30
KR20070057969A (ko) 2007-06-07
BRPI0515524A (pt) 2008-07-29
WO2006034317A3 (en) 2007-04-19
EP1793826A4 (en) 2010-04-21
IL181877A0 (en) 2007-07-04
NO20071988L (no) 2007-04-18
MX2007003283A (es) 2007-05-18
WO2006034317A2 (en) 2006-03-30
US20070254873A1 (en) 2007-11-01
TW200626142A (en) 2006-08-01
SG155932A1 (en) 2009-10-29
JP2008513500A (ja) 2008-05-01
US7858796B2 (en) 2010-12-28
CA2581180A1 (en) 2006-03-30
EP1793826A2 (en) 2007-06-13
AR054084A1 (es) 2007-06-06
MA28912B1 (fr) 2007-10-01

Similar Documents

Publication Publication Date Title
PE20060748A1 (es) Derivados de indolcarboxamida como inhibidores de quinasa ikk2
PE20060373A1 (es) Derivados 3-piperidinil-7-carboxamida-indazol como inhibidores de la actividad cinasa de ikk2
PE20081889A1 (es) Indol carboxamidas como inhibidores de ikk2
NO341591B1 (no) 3-Z-[1-(4-(N-((4-metyl-piperazin-1-yl)-metylkarbonyl)-N-metyl-amino)-anilino)-1-fenyl-metylen]-6-metoksykarbonyl-2-indolinon, tautomerene, diastereomerene, enantiomerene, blandinger derav og saltene derav, og i kombinasjon med en ytterligere farmakologisk aktiv substans, for anvendelse i forebygging eller behandling av fibrose ved revmatoid artritt
PE20100138A1 (es) Derivados de morfolino pirimidina usados en enfermedades relacionadas en mtor quinasa y/o pi3k
NO20063470L (no) Tetrazolforbindelser og deres anvendelse av metabotrofe glutamatreseptorantagonister
NO20063599L (no) Ytterligere heterosykliske forbindelser og deres anvendelse som metabotrofiske glutamatreseptorantagonister
NO20084418L (no) Azolopyridin-3-on derivater som inhibitorer av endoteliallipase
PE20091100A1 (es) Nuevos compuestos 010
NO20064282L (no) Morfolinforbindelser
NO20076502L (no) Pyrrolopyridiner nyttige som inhibitorer av proteinkinase
PE20091623A1 (es) DERIVADOS DE 1H-PIRAZOLO[3,4-b]PIRIDINA COMO INHIBIDORES DE RAF QUINASA
NO20091590L (no) Heterocykliske amidforbindelser anvendbare som kinaseinhibitorer
NO20063468L (no) Triazolforbindelser og deres anvendelse som metabotrofe glutamatreseptorantagonister
NO20063928L (no) Substituerte kinolinforbindelser
DE602006010540D1 (de) (3,4-dihydro-chinazolin-2-yl)-(2-aryloxy-ethyl)-amine mit aktivität am 5-ht-rezeptor
NO20084674L (no) 1- [ (4-(benzoyl (metyl) amino] -3- (fenyl) butyl] azetidinderivater for behandling av gastrointestinale lidelser
PE20070359A1 (es) Inhibidores de pirimidinilpirazol de aurora quinasas
NO20080445L (no) Nye azetidinderivater som neurokininreseptorantagonister for behandling av gastrointestinale sykdommer
PE20080205A1 (es) DERIVADOS DE PIRAZOLOPIRIDINAS SUSTITUIDAS COMO INHIBIDORES DE LA TIROSIN QUINASA Tie2
EA200601880A1 (ru) Замещенные производные 4-алкил- и 4-алканоилпиперидина и их применение в качестве антагонистов нейрокининов
NO20082112L (no) 3-Amino-2-arylpropylazaindoler og deres anvendelse
EA200701879A1 (ru) Замещённые производные оксадиазаспиро [5.5] ундеканона и их применение в качестве антагонистов нейрокинина
MX2010003849A (es) Antagonistas de cgrp.
PE20060881A1 (es) Sulfonamido-macrociclos y sus sales como inhibidores de tie2 y composiciones farmaceuticas que comprenden estos compuestos

Legal Events

Date Code Title Description
FG Grant, registration
FD Application declared void or lapsed