HRP20210450T1 - Biciklički heterociklusni spojevi i njihova uporaba u terapiji - Google Patents

Biciklički heterociklusni spojevi i njihova uporaba u terapiji Download PDF

Info

Publication number
HRP20210450T1
HRP20210450T1 HRP20210450TT HRP20210450T HRP20210450T1 HR P20210450 T1 HRP20210450 T1 HR P20210450T1 HR P20210450T T HRP20210450T T HR P20210450TT HR P20210450 T HRP20210450 T HR P20210450T HR P20210450 T1 HRP20210450 T1 HR P20210450T1
Authority
HR
Croatia
Prior art keywords
methyl
dimethyl
pyrrolo
pyridin
methylpiperazin
Prior art date
Application number
HRP20210450TT
Other languages
English (en)
Croatian (hr)
Inventor
Alison Jo-Anne Woolford
Steven Howard
Ildiko Maria Buck
Gianni Chessari
Christopher Norbert Johnson
Emiliano TAMANINI
James Edward Harvey DAY
Elisabetta CHIARPARIN
Thomas Daniel Heightman
Martyn Frederickson
Charlotte Mary Griffiths-Jones
Original Assignee
Astex Therapeutics Limited
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 Astex Therapeutics Limited filed Critical Astex Therapeutics Limited
Publication of HRP20210450T1 publication Critical patent/HRP20210450T1/hr

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
    • 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
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • 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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic 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
    • A61K31/495—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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic 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
    • A61K31/495—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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/5025—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • 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
    • 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
    • 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
    • C07D403/12—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
    • 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
    • C07D403/14—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 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
    • 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
    • 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
    • C07D471/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • 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
    • C—CHEMISTRY; METALLURGY
    • 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
    • C07D487/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
HRP20210450TT 2011-04-21 2012-04-20 Biciklički heterociklusni spojevi i njihova uporaba u terapiji HRP20210450T1 (hr)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201161477726P 2011-04-21 2011-04-21
GBGB1106817.8A GB201106817D0 (en) 2011-04-21 2011-04-21 New compound
EP12717460.5A EP2699562B1 (en) 2011-04-21 2012-04-20 Bicyclic heterocycle compounds and their uses in therapy
PCT/GB2012/050867 WO2012143726A1 (en) 2011-04-21 2012-04-20 Bicyclic heterocycle compounds and their uses in therapy

Publications (1)

Publication Number Publication Date
HRP20210450T1 true HRP20210450T1 (hr) 2021-04-30

Family

ID=44147398

Family Applications (1)

Application Number Title Priority Date Filing Date
HRP20210450TT HRP20210450T1 (hr) 2011-04-21 2012-04-20 Biciklički heterociklusni spojevi i njihova uporaba u terapiji

Country Status (29)

Country Link
US (6) US9018214B2 (enExample)
EP (2) EP2699562B1 (enExample)
JP (1) JP6100238B2 (enExample)
KR (1) KR101896134B1 (enExample)
CN (1) CN103492376B (enExample)
AR (2) AR086468A1 (enExample)
AU (1) AU2012246081B2 (enExample)
BR (1) BR112013027121B8 (enExample)
CA (1) CA2831346C (enExample)
CY (1) CY1123991T1 (enExample)
DK (1) DK2699562T3 (enExample)
ES (1) ES2855171T3 (enExample)
GB (1) GB201106817D0 (enExample)
HR (1) HRP20210450T1 (enExample)
HU (1) HUE053688T2 (enExample)
IL (1) IL228923A (enExample)
LT (1) LT2699562T (enExample)
MX (1) MX352564B (enExample)
MY (1) MY168159A (enExample)
NZ (1) NZ615572A (enExample)
PH (1) PH12013502002A1 (enExample)
PL (1) PL2699562T3 (enExample)
PT (1) PT2699562T (enExample)
RU (1) RU2662827C2 (enExample)
SG (1) SG193542A1 (enExample)
SI (1) SI2699562T1 (enExample)
TW (1) TWI558698B (enExample)
WO (1) WO2012143726A1 (enExample)
ZA (1) ZA201307797B (enExample)

Families Citing this family (34)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB201106817D0 (en) 2011-04-21 2011-06-01 Astex Therapeutics Ltd New compound
GB201106814D0 (en) 2011-04-21 2011-06-01 Astex Therapeutics Ltd New compounds
US9980973B2 (en) 2012-10-19 2018-05-29 Astex Therapeutics Limited Bicyclic heterocycle compounds and their uses in therapy
GB201218850D0 (en) * 2012-10-19 2012-12-05 Astex Therapeutics Ltd Bicyclic heterocycle compounds and their uses in therapy
GB201218862D0 (en) * 2012-10-19 2012-12-05 Astex Therapeutics Ltd Bicyclic heterocycle compounds and their uses in therapy
GB201218864D0 (en) * 2012-10-19 2012-12-05 Astex Therapeutics Ltd Bicyclic heterocycle compounds and their uses in therapy
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
TWI649319B (zh) * 2013-12-20 2019-02-01 英商阿斯迪克治療公司 雙環雜環化合物及其治療用途
CA2943882A1 (en) 2014-05-22 2015-11-26 F. Hoffmann-La Roche Ag Indolin-2-one and 1,3-dihydro-pyrrolo[3,2-c]pyridin-2-one derivatives
MY186124A (en) 2014-06-26 2021-06-23 Hoffmann La Roche Indolin-2-one or pyrrolo-pyridin-2-one derivatives
JOP20150179B1 (ar) 2014-08-01 2021-08-17 Janssen Pharmaceutica Nv مركبات 6 ، 7 ثاني هيدرو بيرازولو [ 1، 5 الفا ] بيرازين – 4 (5 يد) – اون واستخدامها كمنظمات الوسترية سلبية لمستقبلات ملجور 2
JOP20150177B1 (ar) 2014-08-01 2021-08-17 Janssen Pharmaceutica Nv مركبات 6 ، 7 ثاني هيدرو بيرازولو [ 1، 5 الفا ] بيرازين – 4 (5 يد) – اون واستخدامها كمنظمات الوسترية سلبية لمستقبلات ملجور 2
WO2016025637A1 (en) * 2014-08-12 2016-02-18 Loyola University Of Chicago Indoline sulfonamide inhibitors of dape and ndm-1 and use of the same
EP3227295B1 (en) 2014-12-03 2019-02-20 Janssen Pharmaceutica NV 6,7-dihydropyrazolo[1,5- ]pyrazin-4(5h)-one compounds and their use as negative allosteric modulators of mglu2 receptors
AU2015357169B2 (en) 2014-12-03 2021-03-04 Janssen Pharmaceutica Nv Radiolabelled mGluR2 PET ligands
ES2930749T3 (es) * 2015-07-02 2022-12-21 Hoffmann La Roche Lactamas bicíclicas como inhibidores de la proteína de interacción con el receptor 1 (RIP1) cinasa para tratar, por ejemplo, enfermedades inflamatorias
AU2016374571B2 (en) 2015-12-18 2021-05-06 Janssen Pharmaceutica Nv Radiolabelled mGluR2/3 PET ligands
AU2016374568B2 (en) 2015-12-18 2020-08-27 Janssen Pharmaceutica Nv Radiolabelled mGluR2/3 PET ligands
CA3020792A1 (en) * 2016-04-20 2017-10-26 Glaxosmithkline Intellectual Property Development Limited Conjugates comprising ripk2 inhibitors
JP6953435B2 (ja) * 2016-05-09 2021-10-27 エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト 二量体化合物
CN108690005B (zh) * 2018-06-26 2021-08-24 兰州大学 含硝基天然产物chrysamides B合成方法及其非对映异构体-化合物
WO2020027225A1 (ja) 2018-07-31 2020-02-06 ファイメクス株式会社 複素環化合物
CN111072549A (zh) * 2018-10-19 2020-04-28 中国科学院兰州化学物理研究所苏州研究院 一种手性氧化吲哚螺环茚酮化合物及其合成方法
KR20210125024A (ko) * 2019-02-02 2021-10-15 치아타이 티안큉 파마수티컬 그룹 주식회사 Parp 억제제로서의 인돌로 헵타밀 옥심 유사체
WO2021020585A1 (ja) 2019-07-31 2021-02-04 ファイメクス株式会社 複素環化合物
CN120247907A (zh) 2020-05-04 2025-07-04 大塚制药株式会社 Iap拮抗剂化合物和中间体及其合成方法
IL298645A (en) * 2020-06-04 2023-01-01 Beigene Ltd Pyrido[2,3-b][1,4]oxazines or tetrahydropyrido[2,3-b][1,4]oxazepines as iap antagonists
WO2022189392A1 (en) * 2021-03-10 2022-09-15 Acondicionamiento Tarrasense NEW 2,3-DIHYDRO-1H-PYRROLO[3,2-b]PYRIDINE DERIVATIVES AS SIGMA LIGANDS
WO2023169569A1 (en) * 2022-03-11 2023-09-14 Ascentage Pharma (Suzhou) Co., Ltd. Tricyclic heterocycle compounds as iap antagonists
WO2024071371A1 (ja) * 2022-09-30 2024-04-04 ユビエンス株式会社 複素環式化合物
CN118027138A (zh) * 2022-11-07 2024-05-14 南京中澳转化医学研究院有限公司 吡啶酮类化合物及其制备方法、药物组合物和应用
CN120752233A (zh) * 2023-02-28 2025-10-03 上海海雁医药科技有限公司 取代的三环衍生物及其药物组合物和用途
CN116253756B (zh) * 2023-05-11 2023-07-18 北京元延医药科技股份有限公司 克立硼罗的制备方法
WO2024258988A2 (en) * 2023-06-13 2024-12-19 Delix Therapeutics, Inc. Serotonin releasing compounds and uses thereof

Family Cites Families (85)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR901228A (fr) 1943-01-16 1945-07-20 Deutsche Edelstahlwerke Ag Système d'aimant à entrefer annulaire
US4080330A (en) 1975-06-23 1978-03-21 Delmar Chemicals Limited Phenylindolines and process for their production
US4666828A (en) 1984-08-15 1987-05-19 The General Hospital Corporation Test for Huntington's disease
US4683202A (en) 1985-03-28 1987-07-28 Cetus Corporation Process for amplifying nucleic acid sequences
US4801531A (en) 1985-04-17 1989-01-31 Biotechnology Research Partners, Ltd. Apo AI/CIII genomic polymorphisms predictive of atherosclerosis
DE3822792C2 (de) 1987-07-11 1997-11-27 Sandoz Ag Neue Verwendung von 5HT¶3¶-Antagonisten
US5272057A (en) 1988-10-14 1993-12-21 Georgetown University Method of detecting a predisposition to cancer by the use of restriction fragment length polymorphism of the gene for human poly (ADP-ribose) polymerase
US5192659A (en) 1989-08-25 1993-03-09 Genetype Ag Intron sequence analysis method for detection of adjacent and remote locus alleles as haplotypes
TW218875B (enExample) 1992-03-09 1994-01-11 Takeda Pharm Industry Co Ltd
WO1998004689A1 (en) 1995-07-31 1998-02-05 Urocor, Inc. Biomarkers and targets for diagnosis, prognosis and management of prostate disease
US6218529B1 (en) 1995-07-31 2001-04-17 Urocor, Inc. Biomarkers and targets for diagnosis, prognosis and management of prostate, breast and bladder cancer
NZ321575A (en) 1995-10-30 1999-05-28 Janssen Pharmaceutica Nv 1-(1,2-disubstituted piperidinyl)-4- substituted piperazine derivatives
PT778277E (pt) 1995-12-08 2003-11-28 Pfizer Derivados heterociclicos substituidos como antagonistas do crf
AU2056197A (en) 1996-02-22 1997-09-10 Du Pont Merck Pharmaceutical Company, The M-amidino phenyl analogs as factor xa inhibitors
WO1997038665A2 (en) 1996-04-03 1997-10-23 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
CA2257950A1 (en) 1996-06-28 1998-01-08 Merck & Co., Inc. Fibrinogen receptor antagonist prodrugs
US5977134A (en) 1996-12-05 1999-11-02 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
TR199902590T2 (xx) 1997-04-18 2000-06-21 Smithkline Beecham P.L.C. Birle�ik 5HT1A 5HT1B ve 5HT1D resept�r antagonist aktivitesi olan indol t�revleri.
WO1998050346A2 (en) 1997-04-18 1998-11-12 Smithkline Beecham Plc Acetamide and urea derivatives, process for their preparation and their use in the treatment of cns disorders
US6557977B1 (en) 1997-07-15 2003-05-06 Silverbrook Research Pty Ltd Shape memory alloy ink jet printing mechanism
WO1999043670A1 (en) 1998-02-26 1999-09-02 Neurogen Corporation Benzylpiperazinyl- and benzylpiperidinyl ethanone derivatives, their preparation and their use as dopamine d4 receptor antagonists
US6084098A (en) 1999-02-26 2000-07-04 Neurogen Corporation Benzylpiperazinyl and piperidinyl ethanone derivatives: dopamine receptor subtype specific ligands
NZ507204A (en) 1998-03-31 2003-12-19 Acadia Pharm Inc Substituted piperidine and piperazine derivatives having activity on muscarinic receptors
US6528529B1 (en) 1998-03-31 2003-03-04 Acadia Pharmaceuticals Inc. Compounds with activity on muscarinic receptors
SK2612001A3 (en) 1998-08-26 2001-11-06 Aventis Pharma Ltd Aza-bicycles which modulate the inhibition of cell adhesion
GB9905010D0 (en) 1999-03-04 1999-04-28 Merck Sharp & Dohme Therapeutic agents
WO2000055143A1 (en) 1999-03-17 2000-09-21 F. Hoffmann-La Roche Ag Oxazolone derivatives and their use as alpha-1 adrenoreceptor modulators
GB9929552D0 (en) 1999-12-14 2000-02-09 Proteus Molecular Design Compounds
US6534535B1 (en) 1999-08-12 2003-03-18 Millennium Pharmaceuticals, Inc. Inhibitors of factor Xa
ES2307528T3 (es) 1999-09-04 2008-12-01 Astrazeneca Ab Amidas como inhibidores para la piruvato deshidrogenasa.
GB0031088D0 (en) 2000-12-20 2001-01-31 Smithkline Beecham Plc Medicaments
US20040180925A1 (en) 2000-12-27 2004-09-16 Kenji Matsuno Dipeptidylpeptidase-IV inhibitor
US6790845B2 (en) 2001-04-09 2004-09-14 Bristol-Myers Squibb Pharma Company Fused heterocyclic inhibitors of factor Xa
US20030095958A1 (en) 2001-04-27 2003-05-22 Bhisetti Govinda R. Inhibitors of bace
US20050245537A1 (en) 2002-04-24 2005-11-03 Noboru Tsuchimori Use of compounds having ccr antagonism
TW200402417A (en) * 2002-06-21 2004-02-16 Akzo Nobel Nv 1-[(Indol-3-yl)carbonyl]piperazine derivatives
MXPA05009290A (es) 2003-03-07 2006-05-31 Astellas Pharma Inc Derivados heterociclicos que contienen nitrogeno que tienen estirilo 2,6-disustituido.
GB0307891D0 (en) * 2003-04-04 2003-05-14 Angeletti P Ist Richerche Bio Chemical compounds,compositions and uses
TWI372050B (en) * 2003-07-03 2012-09-11 Astex Therapeutics Ltd (morpholin-4-ylmethyl-1h-benzimidazol-2-yl)-1h-pyrazoles
AU2004266233A1 (en) 2003-08-13 2005-03-03 Amgen, Inc. Melanin concentrating hormone receptor antagonist
TW200524887A (en) 2003-10-27 2005-08-01 Lundbeck & Co As H N-thiazol-2-yl-benzamide derivatives
PE20110102A1 (es) 2004-04-07 2011-02-07 Novartis Ag Derivados de n-(2-oxo-2-pirrolidinil-1-il)etil-2-amino-acetamida como inhibidores de proteinas de apoptosis (iap)
KR100984459B1 (ko) 2004-07-02 2010-09-29 제넨테크, 인크. Ｉａｐ의 억제제
WO2006010118A2 (en) 2004-07-09 2006-01-26 The Regents Of The University Of Michigan Conformationally constrained smac mimetics and the uses thereof
WO2006032987A1 (en) 2004-09-23 2006-03-30 Pfizer Products Inc. Indoline compounds and their use in the treatment of arteriosclerosis
KR20120127754A (ko) 2004-12-20 2012-11-23 제넨테크, 인크. Ｉａｐ의 피롤리딘 억제제
AU2006216450C1 (en) 2005-02-25 2013-01-10 Medivir Ab Dimeric IAP inhibitors
CA2627426A1 (en) 2005-11-11 2007-05-18 Markus Boehringer Carbocyclic fused cyclic amines as inhibitors of the coagulation factor xa
US8247557B2 (en) 2005-12-19 2012-08-21 Genentech, Inc. IAP inhibitors
CA2634699A1 (en) 2005-12-21 2007-06-28 Decode Genetics Ehf N-linked aryl heteroaryl inhibitors of lta4h for treating inflammation
FR2896504B1 (fr) 2006-01-23 2012-07-13 Aventis Pharma Sa Nouveaux derives d'uree cyclique, leur preparation et leur utilisation pharmaceutique comme inhibiteurs de kinases
GB0602335D0 (en) 2006-02-07 2006-03-15 Remynd Nv Thiadiazole Derivatives For The Treatment Of Neurodegenerative Diseases
GB0608184D0 (en) * 2006-04-25 2006-06-07 Astex Therapeutics Ltd Pharmaceutical compounds
EP2029592A1 (en) 2006-04-25 2009-03-04 Astex Therapeutics Limited Pharmaceutical compounds
EA017279B1 (ru) * 2006-05-05 2012-11-30 Дзе Риджентс Оф Дзе Юниверсити Оф Мичиган БИВАЛЕНТНЫЕ МИМЕТИКИ Smac И ИХ ПРИМЕНЕНИЯ
EP2049524A2 (en) * 2006-07-24 2009-04-22 Tetralogic Pharmaceuticals Corporation Iap inhibitors
CN101595121A (zh) 2006-10-12 2009-12-02 诺瓦提斯公司 作为iap抑制剂的吡咯烷衍生物
EP2099769B1 (en) 2006-12-07 2011-07-27 Novartis AG 6-oxo.-1, 6-dihydropyrimidin-2-yls in the treatment of proliferative diseases
MX2009009540A (es) 2007-03-07 2009-09-16 Alantos Pharm Holding Inhibidores de metaloproteasa que contienen una porcion heterociclica.
US8173645B2 (en) 2007-03-21 2012-05-08 Takeda San Diego, Inc. Glucokinase activators
WO2008128171A2 (en) * 2007-04-13 2008-10-23 The Regents Of The University Of Michigan Diazo bicyclic smac mimetics and the uses thereof
WO2009020990A1 (en) 2007-08-08 2009-02-12 Smithkline Beecham Corporation 2- [ (2-{phenylamino}-1h-pyrrolo [2, 3-d] pyrimidin-4-yl) amino] benzamide derivatives as igf-1r inhibitors for the treatment of cancer
WO2009067233A1 (en) 2007-11-20 2009-05-28 Millennium Pharmaceuticals, Inc. Beta carbolines and uses thereof
BRPI0906785A2 (pt) 2008-01-24 2015-07-14 Tetralogic Pharm Corp Composto, composição farmacêutica, e, métodos para induzir a apoptose em uma célula, para tratar câncer e uma doença autoimune
WO2009147476A1 (en) 2008-06-02 2009-12-10 Matrix Laboratories Ltd. Novel pde inhibitors, pharmaceutical compositions containing them and processes for their preparation
WO2010011666A2 (en) 2008-07-21 2010-01-28 University Of South Florida Indoline scaffold shp-2 inhibitors and cancer treatment method
WO2010048149A2 (en) 2008-10-20 2010-04-29 Kalypsys, Inc. Heterocyclic modulators of gpr119 for treatment of disease
DE102008059578A1 (de) 2008-11-28 2010-06-10 Merck Patent Gmbh Benzo-Naphtyridin Verbindungen
JP5628841B2 (ja) 2009-02-27 2014-11-19 エナンタ ファーマシューティカルズ インコーポレイテッド Ｃ型肝炎ウイルスインヒビター
WO2010121212A2 (en) 2009-04-17 2010-10-21 H. Lee Moffit Cancer Center And Research Institute, Inc. Indoline scaffold shp-2 inhibitors and method of treating cancer
WO2010129467A1 (en) 2009-05-04 2010-11-11 Plexxikon, Inc. Compounds and methods for inhibition of renin, and indications therefor
NZ596675A (en) * 2009-05-28 2013-11-29 Tetralogic Pharm Corp Iap inhibitors
UY33794A (es) 2010-12-13 2012-07-31 Novartis Ag Inhibidores diméricos de las iap
GB201106817D0 (en) 2011-04-21 2011-06-01 Astex Therapeutics Ltd New compound
GB201106814D0 (en) 2011-04-21 2011-06-01 Astex Therapeutics Ltd New compounds
US9499479B2 (en) 2011-10-03 2016-11-22 The Trustees Of Columbia University In The City Of New York Molecules that selectively inhibit histone deacetylase 6 relative to histone deacetylase 1
ES2802251T3 (es) 2012-01-06 2021-01-18 Novartis Ag Compuestos heterocíclicos y métodos para su uso
GB201218850D0 (en) 2012-10-19 2012-12-05 Astex Therapeutics Ltd Bicyclic heterocycle compounds and their uses in therapy
US9980973B2 (en) 2012-10-19 2018-05-29 Astex Therapeutics Limited Bicyclic heterocycle compounds and their uses in therapy
GB201218862D0 (en) 2012-10-19 2012-12-05 Astex Therapeutics Ltd Bicyclic heterocycle compounds and their uses in therapy
GB201218864D0 (en) 2012-10-19 2012-12-05 Astex Therapeutics Ltd Bicyclic heterocycle compounds and their uses in therapy
TWI649319B (zh) 2013-12-20 2019-02-01 英商阿斯迪克治療公司 雙環雜環化合物及其治療用途
WO2015106025A1 (en) 2014-01-09 2015-07-16 The J. David Gladstone Institutes, A Testamentary Trust Established Under The Will Of J. David Gladstone Substituted benzoxazine and related compounds
CN120247907A (zh) 2020-05-04 2025-07-04 大塚制药株式会社 Iap拮抗剂化合物和中间体及其合成方法
DK4146617T3 (da) 2020-05-04 2025-10-27 Taiho Pharmaceutical Co Ltd Fremgangsmåder til syntetisering af vandfri mælkesyre

Also Published As

Publication number Publication date
AU2012246081A1 (en) 2013-10-03
SG193542A1 (en) 2013-10-30
US9676768B2 (en) 2017-06-13
IL228923A (en) 2017-12-31
CA2831346A1 (en) 2012-10-26
JP2014514317A (ja) 2014-06-19
TWI558698B (zh) 2016-11-21
BR112013027121A2 (enExample) 2017-01-03
KR101896134B1 (ko) 2018-09-07
US20140179666A1 (en) 2014-06-26
CN103492376B (zh) 2015-07-22
US20150291586A1 (en) 2015-10-15
EP2699562A1 (en) 2014-02-26
US20190375748A1 (en) 2019-12-12
ZA201307797B (en) 2019-02-27
MX2013012243A (es) 2014-01-23
SI2699562T1 (sl) 2021-07-30
EP2699562B1 (en) 2020-12-23
US11866428B2 (en) 2024-01-09
DK2699562T3 (da) 2021-03-01
BR112013027121B8 (pt) 2023-01-31
PT2699562T (pt) 2021-03-25
RU2662827C2 (ru) 2018-07-31
CY1123991T1 (el) 2022-05-27
US9018214B2 (en) 2015-04-28
TW201309673A (zh) 2013-03-01
BR112013027121B1 (pt) 2022-03-03
KR20140032405A (ko) 2014-03-14
PL2699562T3 (pl) 2021-06-14
MY168159A (en) 2018-10-11
NZ615572A (en) 2015-02-27
IL228923A0 (en) 2013-12-31
US20170334907A1 (en) 2017-11-23
GB201106817D0 (en) 2011-06-01
HUE053688T2 (hu) 2021-07-28
MX352564B (es) 2017-11-28
AR116993A2 (es) 2021-06-30
CA2831346C (en) 2021-04-13
US20240199607A1 (en) 2024-06-20
AR086468A1 (es) 2013-12-18
EP3868747A1 (en) 2021-08-25
JP6100238B2 (ja) 2017-03-22
WO2012143726A1 (en) 2012-10-26
LT2699562T (lt) 2021-04-26
US20210122749A1 (en) 2021-04-29
RU2013151803A (ru) 2015-05-27
CN103492376A (zh) 2014-01-01
PH12013502002A1 (en) 2013-12-02
ES2855171T3 (es) 2021-09-23
AU2012246081B2 (en) 2017-01-05

Similar Documents

Publication Publication Date Title
HRP20210450T1 (hr) Biciklički heterociklusni spojevi i njihova uporaba u terapiji
JP7041198B2 (ja) Ｊａｋ阻害剤である５－クロロ－２－ジフルオロメトキシフェニルピラゾロピリミジン化合物
JP7284830B2 (ja) タンパク質チロシンホスファターゼ阻害剤
EP3414247B1 (en) Spiroindolinones as ddr1 inhibitors
TWI476198B (zh) 新穎之吲嗪化合物、其製備方法及含彼之醫藥組合物
ES2834462T3 (es) Compuestos heterocíclicos bicíclicos y sus usos en terapia
JP5876596B2 (ja) カゼインキナーゼ阻害剤としての新規縮合ピリジン化合物
JP6914933B2 (ja) ヤヌスキナーゼ、並びにその組成物及びその使用
WO2020210828A1 (en) (aza)indazolyl-aryl sulfonamide and related compounds and their use in treating medical conditions
MX2012014549A (es) [1, 8]-naftiridinas sustituidas con 2, 4-diarilo como inhibidores de cinasa que se usan contra el cancer.
JP6900491B2 (ja) ピラゾロピリミジン化合物及びその使用方法
KR20240149429A (ko) 약학적 화합물
CN108473501A (zh) 治疗化合物、其组合物及使用方法
CA3160988A1 (en) Allosteric egfr inhibitors and methods of use thereof
JP2010519226A (ja) ５−ｈｔ６受容体親和性を有する６’位置換インドール及びインダゾール誘導体
EP3596072A2 (en) Pyrazolochlorophenyl compounds, compositions and methods of use thereof
JP5219150B2 (ja) キナーゼ阻害薬として活性な置換ピラゾロ［４，３−ｃ］ピリジン誘導体