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PE20110819A1 - Compuestos de carbazol carboxamida utiles como inhibidores de cinasa - Google Patents

Compuestos de carbazol carboxamida utiles como inhibidores de cinasa

Info

Publication number
PE20110819A1
PE20110819A1 PE2011001234A PE2011001234A PE20110819A1 PE 20110819 A1 PE20110819 A1 PE 20110819A1 PE 2011001234 A PE2011001234 A PE 2011001234A PE 2011001234 A PE2011001234 A PE 2011001234A PE 20110819 A1 PE20110819 A1 PE 20110819A1
Authority
PE
Peru
Prior art keywords
carbazol
carboxamide
methylpiperazin
carbonyl
kinase inhibitors
Prior art date
Application number
PE2011001234A
Other languages
English (en)
Inventor
Qingjie Liu
Douglas G Batt
George V Delucca
Andrew J Tebben
Qing Shi
Original Assignee
Bristol Myers Squibb Co
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 Bristol Myers Squibb Co filed Critical Bristol Myers Squibb Co
Publication of PE20110819A1 publication Critical patent/PE20110819A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D209/56—Ring systems containing three or more rings
    • C07D209/80—[b, c]- or [b, d]-condensed
    • C07D209/82—Carbazoles; Hydrogenated carbazoles
    • C07D209/88—Carbazoles; Hydrogenated carbazoles 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 carbon atoms of the ring system
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • 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
    • 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
    • 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
    • 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
    • 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
    • C07D401/02—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
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings
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    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • 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
    • 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
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    • 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
    • C07D413/10—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 carbon chain containing aromatic rings
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    • 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
    • C07D417/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D417/10—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 carbon chain containing aromatic rings
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    • 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
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    • C07—ORGANIC CHEMISTRY
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    • 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
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Immunology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Rheumatology (AREA)
  • Transplantation (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Biomedical Technology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Indole Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

SE REFIERE A COMPUESTOS DERIVADOS DE CARBAZOL CARBOXAMIDA DE FORMULA (I) DONDE LAS LINEAS DISCONTINUAS SON UN ENLACE SIMPLE O DOBLE; A ES HALO, CARBOCICLO(C3-C10) SUSTITUIDO CON 0-3 B, ARILO(C6-C10) SUSTITUIDO CON 0-3 B, ENTRE OTROS, EN DONDE B ES HALOGENO, CN, NITRO, -C(=O)O-, ENTRE OTROS; UNO DE D1 Y D2 ES D Y EL OTRO ES H O HALO, EN DONDE D ES HALOGENO, CH=N-OH, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: 4-BROMO-7-(4-METILPIPERAZIN-1-CARBONIL)-9H-CARBAZOL-1-CARBOXAMIDA; 4-(5-AMINONAFTALEN-1-IL)-7-(4-METILPIPERAZIN-1-CARBONIL)-9H-CARBAZOL-1-CARBOXAMIDA; 4-(7-FLUORO-1H-INDOL-6-IL)-7-(4-METILPIPERAZIN-1-CARBONIL)-9H-CARBAZOL-1-CARBOXAMIDA; ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE CINASA INCLUYENDO LA MODULACION DE TIROSINA CINASA DE BRUTON (Btk) SIENDO UTILES EN EL TRATAMIENTO DE LUPUS ERITEMATOSO SISTEMICO, ARTRITIS REUMATOIDE, ESCLEROSIS MULTIPLE, RECHAZO DE TRASPLANTE
PE2011001234A 2008-12-19 2009-12-17 Compuestos de carbazol carboxamida utiles como inhibidores de cinasa PE20110819A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US13904708P 2008-12-19 2008-12-19

Publications (1)

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PE20110819A1 true PE20110819A1 (es) 2011-11-02

Family

ID=41622163

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2011001234A PE20110819A1 (es) 2008-12-19 2009-12-17 Compuestos de carbazol carboxamida utiles como inhibidores de cinasa

Country Status (22)

Country Link
US (2) US8084620B2 (es)
EP (1) EP2391602B1 (es)
JP (1) JP5487214B2 (es)
KR (1) KR20110098827A (es)
CN (1) CN102325753B (es)
AR (1) AR074812A1 (es)
AU (1) AU2009335821A1 (es)
BR (1) BRPI0922565A2 (es)
CA (1) CA2747670A1 (es)
CL (1) CL2011001516A1 (es)
CO (1) CO6390055A2 (es)
EA (1) EA019041B1 (es)
ES (1) ES2443948T3 (es)
IL (1) IL213185A0 (es)
MX (1) MX2011006171A (es)
NZ (1) NZ593096A (es)
PE (1) PE20110819A1 (es)
SG (1) SG171815A1 (es)
TN (1) TN2011000274A1 (es)
TW (1) TW201028401A (es)
WO (1) WO2010080481A1 (es)
ZA (1) ZA201104469B (es)

Families Citing this family (90)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX2008014450A (es) * 2006-05-18 2009-03-09 Mannkind Corp Inhibidores de cinasa intracelular.
JP5487214B2 (ja) * 2008-12-19 2014-05-07 ブリストル−マイヤーズ スクイブ カンパニー キナーゼ阻害剤として有用なカルバゾールカルボキシアミド化合物
US8785440B2 (en) 2009-09-04 2014-07-22 Biogen Idec Ma, Inc. Bruton's tyrosine kinase inhibitors
US8685969B2 (en) 2010-06-16 2014-04-01 Bristol-Myers Squibb Company Carboline carboxamide compounds useful as kinase inhibitors
WO2012102239A1 (ja) * 2011-01-25 2012-08-02 三井化学アグロ株式会社 芳香族アミドカルボン酸誘導体の製造方法
KR101585753B1 (ko) * 2011-05-17 2016-01-14 에프. 호프만-라 로슈 아게 브루톤 티로신 키나아제의 억제제
WO2013156431A1 (en) 2012-04-17 2013-10-24 Syngenta Participations Ag Pesticidally active pyridyl- and pyrimidyl- substituted thiazole and thiadiazole derivatives
WO2013157021A1 (en) 2012-04-20 2013-10-24 Advinus Therapeutics Limited Bicyclic compounds, compositions and medicinal applications thereof
WO2013157022A1 (en) 2012-04-20 2013-10-24 Advinus Therapeutics Limited Substituted hetero-bicyclic compounds, compositions and medicinal applications thereof
AR091273A1 (es) * 2012-06-08 2015-01-21 Biogen Idec Inc Inhibidores de pirimidinil tirosina quinasa
EP2858500A4 (en) 2012-06-08 2016-04-06 Biogen Ma Inc BRUTON TYROSINE KINASE HEMMER
BR112015001690A2 (pt) 2012-07-24 2017-11-07 Pharmacyclics Inc mutações associadas com a resistência a inibidores da tirosina quinase de bruton (btk)
ES2660210T3 (es) * 2012-09-07 2018-03-21 Novartis Ag Derivados de indolcarboxamida y usos de los mismos
EA028756B1 (ru) 2013-04-25 2017-12-29 Бэйджин, Лтд. Конденсированные гетероциклические соединения в качестве ингибиторов протеинкиназы
TWI648272B (zh) * 2013-06-25 2019-01-21 美商必治妥美雅史谷比公司 經取代之四氫咔唑及咔唑甲醯胺化合物
CN105473573B (zh) * 2013-06-25 2018-03-16 百时美施贵宝公司 用作激酶抑制剂的咔唑甲酰胺化合物
WO2014210255A1 (en) * 2013-06-26 2014-12-31 Abbvie Inc. Primary carboxamides as btk inhibitors
PL3702373T3 (pl) 2013-09-13 2022-12-05 Beigene Switzerland Gmbh Przeciwciała anty-PD1 i ich zastosowanie jako środki terapeutyczne i diagnostyczne
US10662193B2 (en) 2014-01-21 2020-05-26 Ac Immune Sa Carbazole and carboline compounds for use in the diagnosis, treatment, alleviation or prevention of disorders associated with amyloid or amyloid-like proteins
MX2016015005A (es) 2014-05-15 2017-09-28 Iteos Therapeutics Derivados de pirrolidina-2,5-diona, composiciones farmaceuticas y metodos para usar como inhibidores ido1.
CN110156892B (zh) 2014-07-03 2023-05-16 百济神州有限公司 抗pd-l1抗体及其作为治疗剂及诊断剂的用途
ES2807785T3 (es) 2014-10-22 2021-02-24 Bristol Myers Squibb Co Compuestos de heteroarilamina bicíclicos como inhibidores de pi3k
US10023576B2 (en) 2014-10-22 2018-07-17 Bristol-Myers Squibb Company Heteroaryl substituted pyrrolotriazine amine compounds as PI3K inhibitors
SG11201703187PA (en) 2014-10-24 2017-05-30 Bristol Myers Squibb Co Carbazole derivatives
KR102030305B1 (ko) 2014-10-24 2019-10-08 브리스톨-마이어스 스큅 컴퍼니 키나제 억제제로서 유용한 인돌 카르복스아미드 화합물
US10023534B2 (en) * 2014-10-24 2018-07-17 Bristol-Myers Squibb Company Carbazole and tetrahydrocarbazole compounds useful as inhibitors of BTK
BR112017013767A2 (pt) * 2014-12-30 2018-03-13 Dow Agrosciences Llc uso de picolinamidas como fungicidas
EP3042903B1 (en) 2015-01-06 2019-08-14 Impetis Biosciences Ltd. Substituted hetero-bicyclic compounds, compositions and medicinal applications thereof
BR112017019699A2 (pt) 2015-03-17 2018-09-04 Pfizer Inc. derivados substituídos por 3-indol, composições farmacêuticas e métodos para uso
US10189840B2 (en) * 2015-03-18 2019-01-29 Bristol-Myers Squibb Company Substituted tricyclic heterocyclic compounds
US20170107216A1 (en) 2015-10-19 2017-04-20 Incyte Corporation Heterocyclic compounds as immunomodulators
IL291017B2 (en) * 2015-10-21 2023-11-01 Otsuka Pharma Co Ltd Benzolactam compounds as protein kinase inhibitors
CN105272903B (zh) * 2015-11-17 2018-07-10 江苏师范大学 系列含氟咔唑类化合物及其制备方法和应用
SG11201804152RA (en) 2015-11-19 2018-06-28 Incyte Corp Heterocyclic compounds as immunomodulators
JP2017101020A (ja) * 2015-11-25 2017-06-08 宇部興産株式会社 高純度フェノール化合物の製造方法
MA44075A (fr) 2015-12-17 2021-05-19 Incyte Corp Dérivés de n-phényl-pyridine-2-carboxamide et leur utilisation en tant que modulateurs des interactions protéine/protéine pd-1/pd-l1
EP3828171A1 (en) 2015-12-22 2021-06-02 Incyte Corporation Heterocyclic compounds as immunomodulators
AR108396A1 (es) 2016-05-06 2018-08-15 Incyte Corp Compuestos heterocíclicos como inmunomoduladores
TW201808902A (zh) 2016-05-26 2018-03-16 美商英塞特公司 作為免疫調節劑之雜環化合物
AU2017281285C1 (en) 2016-06-20 2022-05-12 Incyte Corporation Heterocyclic compounds as immunomodulators
WO2018007885A1 (en) 2016-07-05 2018-01-11 Beigene, Ltd. COMBINATION OF A PD-l ANTAGONIST AND A RAF INHIBITOR FOR TREATING CANCER
EP3484866B1 (en) 2016-07-14 2022-09-07 Incyte Corporation Heterocyclic compounds as immunomodulators
KR20190035769A (ko) 2016-07-21 2019-04-03 바이오젠 엠에이 인코포레이티드 브루톤 타이로신 카이나제 저해제의 석신에이트 형태 및 조성물
MX384627B (es) 2016-08-16 2025-03-14 Beigene Ltd Forma cristalina de (s)-7-(1-acriloilpiperidin-4-il)-2-(4-fenoxifenil)-4,5,6,7-tetra-hidropirazolo[1,5-a]pirimidin-3-carboxamida, preparacion y usos de la misma
AU2017313085B2 (en) 2016-08-19 2024-06-20 Beone Medicines I Gmbh Use of a combination comprising a Btk inhibitor for treating cancers
EP3504198B1 (en) 2016-08-29 2023-01-25 Incyte Corporation Heterocyclic compounds as immunomodulators
BR112019005337A2 (pt) 2016-09-19 2019-08-27 Mei Pharma Inc terapia combinada
PL3689868T3 (pl) 2016-12-01 2024-03-11 Arvinas Operations, Inc. Pochodne tetrahydronaftalenu i tetrahydroizochinoliny jako degradery receptorów estrogenowych
CN110312713B (zh) * 2016-12-20 2022-08-12 百时美施贵宝公司 用于制备四氢咔唑甲酰胺化合物的方法
US20180179179A1 (en) 2016-12-22 2018-06-28 Incyte Corporation Heterocyclic compounds as immunomodulators
EP3558989B1 (en) 2016-12-22 2021-04-14 Incyte Corporation Triazolo[1,5-a]pyridine derivatives as immunomodulators
WO2018119286A1 (en) 2016-12-22 2018-06-28 Incyte Corporation Bicyclic heteroaromatic compounds as immunomodulators
IL295660A (en) 2016-12-22 2022-10-01 Incyte Corp Benzooxazole derivatives as immunomodulators
PE20200005A1 (es) 2016-12-22 2020-01-06 Incyte Corp Derivados de tetrahidro imidazo[4,5-c]piridina como inductores de internalizacion pd-l1
EP3573989A4 (en) 2017-01-25 2020-11-18 Beigene, Ltd. CRYSTALLINE FORMS OF (S) -7- (1- (BUT-2-YNOYL) PIPERIDIN-4-YL) -2- (4-PHENOXYPHENYL) -4, 5, 6, 7-TETRAHY DROPYRAZOLO [1, 5-A ] PYRIMIDINE-3-CARBOXAMIDE, PREPARATION AND ASSOCIATED USES
GB201706327D0 (en) 2017-04-20 2017-06-07 Otsuka Pharma Co Ltd A pharmaceutical compound
AU2018290532A1 (en) 2017-06-26 2019-11-21 Beigene, Ltd. Immunotherapy for hepatocellular carcinoma
CN110997677A (zh) 2017-08-12 2020-04-10 百济神州有限公司 具有改进的双重选择性的Btk抑制剂
WO2019108795A1 (en) 2017-11-29 2019-06-06 Beigene Switzerland Gmbh Treatment of indolent or aggressive b-cell lymphomas using a combination comprising btk inhibitors
KR20250067967A (ko) 2018-03-30 2025-05-15 인사이트 코포레이션 면역조절제로서 복소환형 화합물
HUE061503T2 (hu) 2018-05-11 2023-07-28 Incyte Corp Tetrahidro-imidazo[4,5-C]piridin-származékok mint PD-L1 immunmodulátorok
WO2020030754A1 (en) 2018-08-10 2020-02-13 Syngenta Crop Protection Ag Pesticidally-active mesoionic bicyclic heteroaromatic compounds
WO2020035565A1 (en) 2018-08-17 2020-02-20 Syngenta Crop Protection Ag Pesticidally-active mesoionic bicyclic heteroaromatic compounds
TW202045011A (zh) 2019-02-28 2020-12-16 瑞士商先正達農作物保護公司 具有含硫取代基之殺有害生物活性雜環衍生物
CN113939289A (zh) 2019-06-10 2022-01-14 百济神州瑞士有限责任公司 一种含有布鲁顿氏酪氨酸激酶抑制剂的口服固体片剂及其制备方法
EP4010342A1 (en) 2019-08-09 2022-06-15 Incyte Corporation Salts of a pd-1/pd-l1 inhibitor
IL320609A (en) 2019-08-26 2025-07-01 Arvinas Operations Inc Methods for treating breast cancer with a history of tetrahydronaphthalene as estrogen receptor-disrupting agents
TWI879811B (zh) 2019-09-30 2025-04-11 美商英塞特公司 作為免疫調節劑之吡啶并[3,2-d]嘧啶化合物
PH12022551136A1 (en) 2019-11-11 2023-10-09 Incyte Corp Salts and crystalline forms of a pd-1/pd-l1 inhibitor
TW202132300A (zh) 2020-01-06 2021-09-01 瑞士商先正達農作物保護公司 具有含硫取代基的殺有害生物活性雜環衍生物
KR20220136395A (ko) 2020-02-03 2022-10-07 브리스톨-마이어스 스큅 컴퍼니 Irak4 억제제로서 유용한 트리시클릭 헤테로아릴 화합물
WO2021207549A1 (en) * 2020-04-10 2021-10-14 Gb005, Inc. Kinase inhibitors
WO2022013417A1 (en) 2020-07-17 2022-01-20 Syngenta Crop Protection Ag Pesticidally active heterocyclic derivatives with sulfur containing substituents
WO2022017975A1 (en) 2020-07-18 2022-01-27 Syngenta Crop Protection Ag Pesticidally active heterocyclic derivatives with sulfur containing substituents
CA3189161A1 (en) 2020-08-31 2022-03-03 Syngenta Crop Protection Ag Pesticidally active heterocyclic derivatives with sulfur containing substituents
JP2023540274A (ja) 2020-09-01 2023-09-22 シンジェンタ クロップ プロテクション アクチェンゲゼルシャフト 硫黄含有置換基を有する殺有害生物的に活性な複素環式誘導体
JP2023540311A (ja) 2020-09-02 2023-09-22 シンジェンタ クロップ プロテクション アクチェンゲゼルシャフト 殺有害生物的に活性である硫黄含有置換基を有する複素環式誘導体
US20230303565A1 (en) 2020-09-02 2023-09-28 Syngenta Crop Protection Ag Pesticidally active heterocyclic derivatives with sulfur containing substituents
PE20231555A1 (es) 2020-09-14 2023-10-03 Arvinas Operations Inc Formas cristalinas y amorfas de un compuesto para la degradacion dirigida del receptor de estrogenos
US20240158375A1 (en) * 2020-10-21 2024-05-16 Azura Ophthalmics Ltd. Compounds and methods for the treatment of ocular disorders
US11780836B2 (en) 2020-11-06 2023-10-10 Incyte Corporation Process of preparing a PD-1/PD-L1 inhibitor
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
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
EP4384523A1 (en) 2021-08-10 2024-06-19 Syngenta Crop Protection AG 2,2-difluoro-5h-[1,3]dioxolo[4,5-f]isoindol-7-one derivatives as pesticides
WO2023187191A1 (en) 2022-04-01 2023-10-05 Syngenta Crop Protection Ag Pesticidally active heterocyclic derivatives with sulfur containing substituents
US11786531B1 (en) 2022-06-08 2023-10-17 Beigene Switzerland Gmbh Methods of treating B-cell proliferative disorder
WO2024033374A1 (en) 2022-08-11 2024-02-15 Syngenta Crop Protection Ag Novel arylcarboxamide or arylthioamide compounds
WO2024089216A1 (en) 2022-10-27 2024-05-02 Syngenta Crop Protection Ag Novel sulfur-containing heteroaryl carboxamide compounds
CN120476107A (zh) 2022-12-15 2025-08-12 先正达农作物保护股份公司 可用作杀有害生物剂的新型的二环-甲酰胺化合物
CN118993985A (zh) * 2023-05-17 2024-11-22 中国医学科学院药物研究所 一种具有抗肿瘤活性的化合物，其制备方法及制药用途

Family Cites Families (35)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001007409A1 (en) 1999-07-23 2001-02-01 Astrazeneca Uk Limited Carbazole derivatives and their use as neuropeptide y5 receptor ligands
EP1434578A1 (en) 2001-10-09 2004-07-07 PHARMACIA & UPJOHN COMPANY Arylsulphonyl-substituted tetrahydro- and hexahydro-carbazoles as 5-ht-6 receptor ligands
KR20060017494A (ko) 2003-04-11 2006-02-23 그렌마크 파머수티칼스 에스. 아. 염증 및 알레르기성 질환 치료용으로 유용한 신규 헤테로사이클릭 화합물, 이의 제조방법 및 이를 함유하는 약학 조성물
US20060183746A1 (en) 2003-06-04 2006-08-17 Currie Kevin S Certain imidazo[1,2-a]pyrazin-8-ylamines and method of inhibition of Bruton's tyrosine kinase by such compounds
WO2005014599A1 (en) 2003-06-04 2005-02-17 Cellular Genomics, Inc. Imidazo[1,2-a]pyrazin-8-ylamines and method of inhibition of bruton’s tyrosine kinase by such compounds
US7393848B2 (en) 2003-06-30 2008-07-01 Cgi Pharmaceuticals, Inc. Certain heterocyclic substituted imidazo[1,2-A]pyrazin-8-ylamines and methods of inhibition of Bruton's tyrosine kinase by such compounds
WO2005047290A2 (en) 2003-11-11 2005-05-26 Cellular Genomics Inc. Imidazo[1,2-a] pyrazin-8-ylamines as kinase inhibitors
CN1937994A (zh) 2004-04-06 2007-03-28 宝洁公司 角蛋白染色化合物、包含它们的角蛋白染色组合物以及它们的应用
PE20060748A1 (es) 2004-09-21 2006-10-01 Smithkline Beecham Corp Derivados de indolcarboxamida como inhibidores de quinasa ikk2
WO2006034337A2 (en) 2004-09-23 2006-03-30 Wyeth Carbazole and cyclopentaindole derivatives to treat infection with hepatitis c virus
EP1812439B2 (en) 2004-10-15 2017-12-06 Takeda Pharmaceutical Company Limited Kinase inhibitors
JP2008519843A (ja) 2004-11-10 2008-06-12 シージーアイ ファーマスーティカル インコーポレーテッド 特定のイミダゾ［１，２−ａ］ビラジン−８−イラミンズ、その生成方法及びそれに関する使用方法
US20060173183A1 (en) 2004-12-31 2006-08-03 Alantos Pharmaceuticals, Inc., Multicyclic bis-amide MMP inhibitors
EP1863766B1 (en) 2005-03-10 2015-05-20 Gilead Connecticut, Inc. Certain substituted amides, method of making, and method of use thereof
US20070078136A1 (en) 2005-09-22 2007-04-05 Bristol-Myers Squibb Company Fused heterocyclic compounds useful as kinase modulators
US7723336B2 (en) 2005-09-22 2010-05-25 Bristol-Myers Squibb Company Fused heterocyclic compounds useful as kinase modulators
RS51843B (sr) 2005-11-17 2012-02-29 Osi Pharmaceuticals Llc. KONDENZOVANI BICIKLIČNI m TOR INHIBITORI
AU2006316322B2 (en) 2005-11-22 2011-08-25 Merck Canada Inc. Tricyclic compounds useful as inhibitors of kinases
US20100222345A1 (en) 2006-08-09 2010-09-02 Caroline Jean Diaz Novel compounds as antagonists or inverse agonists for opioid receptors
WO2008021745A2 (en) 2006-08-16 2008-02-21 Itherx Pharmaceuticals, Inc. Hepatitis c virus entry inhibitors
AU2007297221B2 (en) 2006-09-11 2012-11-08 Mylan Laboratories Limited Dibenzofuran derivatives as inhibitors of PDE-4 and PDE-10
EP2068849A2 (en) 2006-09-11 2009-06-17 CGI Pharmaceuticals, Inc. Kinase inhibitors, and methods of using and identifying kinase inhibitors
US7492329B2 (en) 2006-10-12 2009-02-17 Hewlett-Packard Development Company, L.P. Composite material with chirped resonant cells
CA2667644A1 (en) 2006-10-27 2008-05-15 Wyeth Tricyclic compounds as matrix metalloproteinase inhibitors
WO2008064318A2 (en) 2006-11-22 2008-05-29 University Of Medicine And Dentistry Of New Jersey Peripheral opioid receptor active compounds
WO2008064317A1 (en) 2006-11-22 2008-05-29 University Of Medicine And Dentistry Of New Jersey Lipophilic opioid receptor active compounds
EP2121692B1 (en) 2006-12-22 2013-04-10 Incyte Corporation Substituted heterocycles as janus kinase inhibitors
SE530889C2 (sv) 2007-02-27 2008-10-07 Scania Cv Abp Bränsletankarrangemang för ett fordon
DE102007056922A1 (de) 2007-11-27 2009-05-28 BSH Bosch und Siemens Hausgeräte GmbH Wasserführendes Hausgerät mit einer Wasserweiche
AU2008335761B2 (en) 2007-12-13 2014-04-24 Merck Sharp & Dohme Corp. Inhibitors of janus kinases
WO2009086303A2 (en) 2007-12-21 2009-07-09 University Of Rochester Method for altering the lifespan of eukaryotic organisms
JP5381718B2 (ja) 2008-01-31 2014-01-08 コニカミノルタ株式会社 ハロ多環芳香族化合物及びその製造方法
EP2095818A1 (en) 2008-02-29 2009-09-02 AEterna Zentaris GmbH Use of LHRH antagonists at non-castrating doses
JP5487214B2 (ja) * 2008-12-19 2014-05-07 ブリストル−マイヤーズ スクイブ カンパニー キナーゼ阻害剤として有用なカルバゾールカルボキシアミド化合物
ES2490867T3 (es) 2008-12-19 2014-09-04 Bristol-Myers Squibb Company Inhibidores de carbazol y carbolina quinasas

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