ZA200807767B - Nitrogenated heterocyclic derivative, and pharmaceutical agent comprising the derivative as active ingredient - Google Patents

Nitrogenated heterocyclic derivative, and pharmaceutical agent comprising the derivative as active ingredient

Info

Publication number
ZA200807767B
ZA200807767B ZA200807767A ZA200807767A ZA200807767B ZA 200807767 B ZA200807767 B ZA 200807767B ZA 200807767 A ZA200807767 A ZA 200807767A ZA 200807767 A ZA200807767 A ZA 200807767A ZA 200807767 B ZA200807767 B ZA 200807767B
Authority
ZA
South Africa
Prior art keywords
derivative
active ingredient
pharmaceutical agent
nitrogenated heterocyclic
heterocyclic derivative
Prior art date
Application number
ZA200807767A
Other languages
English (en)
Inventor
Kusuda Shinya
Nishiyama Toshihiko
Kazuya Hashimura
Ueda Junya
Shibayama Shiro
Original Assignee
Ono Pharmaceutical 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 Ono Pharmaceutical Co filed Critical Ono Pharmaceutical Co
Publication of ZA200807767B publication Critical patent/ZA200807767B/xx

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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
    • C07D401/12—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
    • 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
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • A61P11/02—Nasal agents, e.g. decongestants
    • 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
    • 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
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    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/16—Otologicals
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • 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
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D419/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms
    • C07D419/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms containing three or more hetero rings

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Oncology (AREA)
  • Diabetes (AREA)
  • Communicable Diseases (AREA)
  • Virology (AREA)
  • Rheumatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Dermatology (AREA)
  • Urology & Nephrology (AREA)
  • Cardiology (AREA)
  • Obesity (AREA)
  • Molecular Biology (AREA)
  • Transplantation (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Vascular Medicine (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Neurosurgery (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pain & Pain Management (AREA)
ZA200807767A 2006-03-10 2008-09-09 Nitrogenated heterocyclic derivative, and pharmaceutical agent comprising the derivative as active ingredient ZA200807767B (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
JP2006066451 2006-03-10

Publications (1)

Publication Number Publication Date
ZA200807767B true ZA200807767B (en) 2009-08-26

Family

ID=38509460

Family Applications (1)

Application Number Title Priority Date Filing Date
ZA200807767A ZA200807767B (en) 2006-03-10 2008-09-09 Nitrogenated heterocyclic derivative, and pharmaceutical agent comprising the derivative as active ingredient

Country Status (15)

Country Link
US (1) US8003642B2 (zh)
EP (1) EP1995246A4 (zh)
JP (1) JPWO2007105637A1 (zh)
KR (1) KR20090008217A (zh)
CN (1) CN101443322A (zh)
AU (1) AU2007225836A1 (zh)
BR (1) BRPI0708731A2 (zh)
CA (1) CA2644368A1 (zh)
EA (1) EA200870344A1 (zh)
MA (1) MA30294B1 (zh)
MX (1) MX2008011414A (zh)
NO (1) NO20083813L (zh)
RU (1) RU2008140144A (zh)
WO (1) WO2007105637A1 (zh)
ZA (1) ZA200807767B (zh)

Families Citing this family (54)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI344955B (en) * 2003-03-14 2011-07-11 Ono Pharmaceutical Co Heterocyclic rinf having nitrogen atom derivatives and medicament containing the derivatives as active ingredient
TW200600086A (en) 2004-06-05 2006-01-01 Astrazeneca Ab Chemical compound
TWI400232B (zh) * 2004-09-13 2013-07-01 Ono Pharmaceutical Co 含氮雜環衍生物及以該含氮雜環衍生物為有效成分之藥劑
BRPI0622262A2 (pt) 2005-07-09 2011-08-09 Astrazeneca Ab composto, composição farmacêutica, uso de um composto ou um sal farmaceuticamente aceitável do mesmo, e, processo para a preparação de um composto
UA116187C2 (uk) 2005-12-13 2018-02-26 Інсайт Холдінгс Корпорейшн ГЕТЕРОАРИЛЗАМІЩЕНІ ПІРОЛО[2,3-b]ПІРИДИНИ Й ПІРОЛО[2,3-b]ПІРИМІДИНИ ЯК ІНГІБІТОРИ ЯНУС-КІНАЗИ
AU2007225836A1 (en) 2006-03-10 2007-09-20 Ono Pharmaceutical Co., Ltd. Nitrogenated heterocyclic derivative, and pharmaceutical agent comprising the derivative as active ingredient
SA07280576B1 (ar) * 2006-10-26 2011-06-22 استرازينيكا ايه بي مركبات بنزويل أمينو سيكليل غير متجانسة بأعتبارها عوامل منشطة للجلوكوكيناز
CA2676352A1 (en) * 2007-02-15 2008-08-21 Pfizer Limited Pharmaceutical compositions and methods for ccr5 antagonists
ES2714092T3 (es) 2007-06-13 2019-05-27 Incyte Holdings Corp Uso de sales del inhibidor de quinasas Janus (R)-3-(4-(7H-pirrolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il)-3-ciclopentilpropanonitrilo
EP2280959B1 (en) 2008-06-05 2012-04-04 Glaxo Group Limited 4-amino-indazoles
ES2445199T3 (es) 2008-06-05 2014-02-28 Glaxo Group Limited Derivados de benzpirazol como inhibidores de PI3-quinasas
WO2009147189A1 (en) 2008-06-05 2009-12-10 Glaxo Group Limited Novel compounds
EA201100097A1 (ru) * 2008-08-04 2011-10-31 Астразенека Аб Производные пиразоло[3,4]пиримидин-4-ила и их применения для лечения диабета и ожирения
CL2009001884A1 (es) * 2008-10-02 2010-05-14 Incyte Holdings Corp Uso de 3-ciclopentil-3-[4-(7h-pirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il)propanonitrilo, inhibidor de janus quinasa, y uso de una composición que lo comprende para el tratamiento del ojo seco.
GB0902406D0 (en) 2009-02-13 2009-04-01 Astrazeneca Ab Crystalline polymorphic form
GB0902434D0 (en) 2009-02-13 2009-04-01 Astrazeneca Ab Chemical process
JP5656880B2 (ja) 2009-03-09 2015-01-21 グラクソ グループ リミテッドＧｌａｘｏ Ｇｒｏｕｐ Ｌｉｍｉｔｅｄ Ｐｉ３キナーゼの阻害剤としての４−オキサジアゾール−２−イル−インダゾール
AR076221A1 (es) * 2009-04-09 2011-05-26 Astrazeneca Ab Derivado de pirazol [4,5-e] pirimidina y su uso para tratar diabetes y obesidad
WO2010116177A1 (en) 2009-04-09 2010-10-14 Astrazeneca Ab A pyrazolo [4,5-e] pyrimidine derivative and its use to treat diabetes and obesity
PL2899191T3 (pl) 2009-04-30 2018-01-31 Glaxo Group Ltd Indazole podstawione oksazolem jako inhibitory kinazy PI3
UA106078C2 (uk) 2009-05-22 2014-07-25 Інсайт Корпорейшн 3-[4-(7H-ПІРОЛО[2,3-d]ПІРИМІДИН-4-ІЛ)-1H-ПІРАЗОЛ-1-ІЛ]ОКТАН- АБО ГЕПТАННІТРИЛ ЯК JAK-ІНГІБІТОРИ
TW201100429A (en) 2009-05-22 2011-01-01 Incyte Corp N-(hetero)aryl-pyrrolidine derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines and pyrrol-3-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
WO2011028685A1 (en) * 2009-09-01 2011-03-10 Incyte Corporation Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
TWI643857B (zh) 2010-03-10 2018-12-11 英塞特公司 作為ｊａｋ１抑制劑之哌啶-４-基三亞甲亞胺衍生物
PE20130216A1 (es) 2010-05-21 2013-02-27 Incyte Corp Formulacion topica para un inhibidor de jak
GB201018124D0 (en) 2010-10-27 2010-12-08 Glaxo Group Ltd Polymorphs and salts
JP5917545B2 (ja) 2010-11-19 2016-05-18 インサイト・ホールディングス・コーポレイションＩｎｃｙｔｅ Ｈｏｌｄｉｎｇｓ Ｃｏｒｐｏｒａｔｉｏｎ Ｊａｋ阻害剤としてのシクロブチル置換ピロロピリジンおよびピロロピリミジン誘導体
WO2012068440A1 (en) 2010-11-19 2012-05-24 Incyte Corporation Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as jak inhibitors
MX2013010330A (es) 2011-03-09 2014-11-26 Richard G Pestell Líneas de célula cancerosa de próstata, signaturas de gen, y usos de las mismas.
AR086983A1 (es) 2011-06-20 2014-02-05 Incyte Corp Derivados de azetidinil fenil, piridil o pirazinil carboxamida como inhibidores de jak
WO2013025733A1 (en) 2011-08-15 2013-02-21 Intermune, Inc. Lysophosphatidic acid receptor antagonists
TW201313721A (zh) 2011-08-18 2013-04-01 Incyte Corp 作為ｊａｋ抑制劑之環己基氮雜環丁烷衍生物
UA111854C2 (uk) 2011-09-07 2016-06-24 Інсайт Холдінгс Корпорейшн Способи і проміжні сполуки для отримання інгібіторів jak
CN104853806A (zh) * 2012-05-14 2015-08-19 理查德·G·佩斯泰尔 使用ccr5调节剂治疗癌症
US9193733B2 (en) 2012-05-18 2015-11-24 Incyte Holdings Corporation Piperidinylcyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as JAK inhibitors
NZ748448A (en) 2012-11-15 2019-12-20 Incyte Holdings Corp Sustained-release dosage forms of ruxolitinib
TWI634121B (zh) 2013-03-06 2018-09-01 英塞特控股公司 用於製備ｊａｋ抑制劑之方法及中間物
CA2916653C (en) 2013-06-27 2017-07-18 Pfizer Inc. Heteroaromatic compounds and their use as dopamine d1 ligands
KR20220103810A (ko) 2013-08-07 2022-07-22 인사이트 코포레이션 Jak1 억제제용 지속 방출 복용 형태
AU2014338549B2 (en) 2013-10-25 2017-05-25 Novartis Ag Ring-fused bicyclic pyridyl derivatives as FGFR4 inhibitors
WO2015184305A1 (en) 2014-05-30 2015-12-03 Incyte Corporation TREATMENT OF CHRONIC NEUTROPHILIC LEUKEMIA (CNL) AND ATYPICAL CHRONIC MYELOID LEUKEMIA (aCML) BY INHIBITORS OF JAK1
WO2016054483A1 (en) 2014-10-03 2016-04-07 Novartis Ag Use of ring-fused bicyclic pyridyl derivatives as fgfr4 inhibitors
MD3259253T2 (ro) * 2015-02-16 2020-06-30 Univ Queensland Sulfoniluree și compuși înrudiți și utilizări ale acestora
US9802917B2 (en) 2015-03-25 2017-10-31 Novartis Ag Particles of N-(5-cyano-4-((2-methoxyethyl)amino)pyridin-2-yl)-7-formyl-6-((4-methyl-2-oxopiperazin-1-yl)methyl)-3,4-dihydro-1,8-naphthyridine-1(2H)-carboxamide
TW202246215A (zh) 2015-12-18 2022-12-01 美商亞德利克斯公司 作為非全身ｔｇｒ５促效劑之經取代之４－苯基吡啶化合物
US12084472B2 (en) 2015-12-18 2024-09-10 Ardelyx, Inc. Substituted 4-phenyl pyridine compounds as non-systemic TGR5 agonists
US10316021B2 (en) 2016-11-28 2019-06-11 Pfizer Inc. Heteroarylphenoxy benzamide kappa opioid ligands
AR113922A1 (es) 2017-12-08 2020-07-01 Incyte Corp Terapia de combinación de dosis baja para el tratamiento de neoplasias mieloproliferativas
AU2019213665B2 (en) 2018-01-30 2024-06-13 Incyte Corporation Processes for preparing (1 -(3-fluoro-2-(trifluoromethyl)isonicotinyl)piperidine-4-one)
SI3773593T1 (sl) 2018-03-30 2024-08-30 Incyte Corporation Zdravljenje hidradenitisa suppurative z zaviralci jak
US20220185815A1 (en) 2019-03-06 2022-06-16 Daiichi Sankyo Company, Limited Pyrrolopyrazole derivative
CN110590748A (zh) * 2019-10-03 2019-12-20 黄泳华 芳香基氨基苄基哌嗪氮氧化物及其组合物与用途
US11629196B2 (en) 2020-04-27 2023-04-18 Incelldx, Inc. Method of treating SARS-CoV-2-associated hypercytokinemia by administering a human monoclonal antibody (PRO-140) that inhibits CCR5/CCL5 binding interactions
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms

Family Cites Families (118)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1063744A (en) 1964-05-25 1967-03-30 American Cyanamid Co 4-substituted-4'-tertiary aminoalkoxy biphenyls
US5169855A (en) 1990-03-28 1992-12-08 Du Pont Merck Pharmaceutical Company Piperidine ether derivatives as psychotropic drugs or plant fungicides
US5486534A (en) 1994-07-21 1996-01-23 G. D. Searle & Co. 3,4-substituted pyrazoles for the treatment of inflammation
US5593994A (en) 1994-09-29 1997-01-14 The Dupont Merck Pharmaceutical Company Prostaglandin synthase inhibitors
IL118469A (en) 1995-06-15 2000-08-13 Tanabe Seiyaku Co Naphthalene derivatives their preparation and intermediates thereof
ES2217404T3 (es) 1996-03-28 2004-11-01 Glaxo Group Limited Derivados de pirrolopirrolona como inhibidores de la elastasa de neutrofilos.
AU5803398A (en) 1996-12-13 1998-07-03 Merck & Co., Inc. Spiro-substituted azacycles as modulators of chemokine receptor activity
PL189777B1 (pl) 1996-12-19 2005-09-30 Aventis Pharma Inc Karboksy-podstawione cykliczne pochodne karboksyamidowe, kompozycja farmaceutyczna zawierająca te związki, zastosowania i sposób wytwarzania tych związków
ZA985542B (en) 1997-07-03 1999-04-07 Smithkline Beecham Corp Substituted benzanilides as CCR5 receptor ligands antiinflammatory agents and antiviral agents
AU8576098A (en) 1997-07-25 1999-02-16 Merck & Co., Inc. Cyclic amine modulators of chemokine receptor activity
GB9716657D0 (en) 1997-08-07 1997-10-15 Zeneca Ltd Chemical compounds
IL125658A0 (en) 1997-08-18 1999-04-11 Hoffmann La Roche Ccr-3 receptor antagonists
US6340759B1 (en) 1997-10-02 2002-01-22 Eisai Co., Ltd. Fused pyridine derivatives
AR013669A1 (es) 1997-10-07 2001-01-10 Smithkline Beecham Corp Compuestos y metodos
AU1504599A (en) 1997-12-17 1999-07-05 Shionogi & Co., Ltd. Novel pyridine compounds
CA2304959A1 (en) 1997-12-19 1999-07-01 Takeda Chemical Industries, Ltd. Pharmaceutical composition for antagonizing ccr5 comprising anilide derivative
AU2654399A (en) 1998-02-02 1999-08-16 Merck & Co., Inc. Cyclic amine modulators of chemokine receptor activity
GB9803226D0 (en) 1998-02-17 1998-04-08 Zeneca Ltd Chemical compounds
CA2329821A1 (en) 1998-04-27 1999-11-04 Dashyant Dhanak Ccr-3 receptor antagonists
EP1076557A1 (en) 1998-04-27 2001-02-21 Smithkline Beecham Corporation Ccr-3 receptor antagonists
WO2000004003A1 (en) 1998-07-14 2000-01-27 Smithkline Beecham Corporation Ccr-3 receptor antagonists
KR20010074779A (ko) 1998-07-28 2001-08-09 스튜어트 알. 수터, 스티븐 베네티아너, 피터 존 기딩스 치환된 아닐리드 화합물 및 제조방법
CA2338697A1 (en) 1998-07-28 2000-02-10 Smithkline Beecham Corporation Compounds and methods
AU5301599A (en) 1998-08-20 2000-03-14 Takeda Chemical Industries Ltd. Quaternary ammonium salts and their use
WO2000010653A1 (en) 1998-08-24 2000-03-02 Orlimar Golf Equipment Company, Llc Iron golf club head and club
WO2000021916A1 (fr) 1998-10-15 2000-04-20 Takeda Chemical Industries, Ltd. Procede de preparation de derives d'amine
WO2000027800A1 (en) 1998-11-09 2000-05-18 Smithkline Beecham Corporation Ccr-3 receptor antagonists
WO2000027843A1 (en) 1998-11-09 2000-05-18 Smithkline Beecham Corporation Ccr-3 receptor antagonists
WO2000027835A1 (en) 1998-11-09 2000-05-18 Smithkline Beecham Corporation Ccr-3 receptor antagonists
CN1163484C (zh) 1998-11-17 2004-08-25 霍夫曼-拉罗奇有限公司 4-芳酰基-哌啶-ccr-3受体拮抗剂ⅲ
CA2350903A1 (en) 1998-11-20 2000-06-02 F. Hoffmann-La Roche Ag Pyrrolidine derivatives-ccr-3 receptor antagonists
KR20010081034A (ko) 1998-11-20 2001-08-25 프리돌린 클라우스너, 롤란드 비. 보레르 피페리딘 씨씨알-3 수용체 길항제
WO2000034278A1 (fr) 1998-12-04 2000-06-15 Toray Industries, Inc. Derives triazolo, et inhibiteurs de chimiokines contenant ces derives comme ingredient actif
EP1140086A4 (en) 1998-12-18 2002-04-03 Du Pont Pharm Co N-UREIDOALKYL-PIPERIDINES FOR USE AS MODULATORS OF THE ACTIVITY OF CHIMIOKIN RECEPTORS
WO2000035449A1 (en) 1998-12-18 2000-06-22 Du Pont Pharmaceuticals Company N-ureidoalkyl-piperidines as modulators of chemokine receptor activity
ATE302606T1 (de) 1998-12-18 2005-09-15 Bristol Myers Squibb Pharma Co N-ureidoalkylpiperidine als modulatoren der aktivität der chemokinrezeptoren
CA2348923A1 (en) 1998-12-18 2000-06-22 Dean A. Wacker N-ureidoalkyl-piperidines as modulators of chemokine receptor activity
CA2347912A1 (en) 1998-12-18 2000-06-22 Soo S. Ko Heterocyclic piperidines as modulators of chemokine receptor activity
AU770042B2 (en) 1998-12-18 2004-02-12 Bristol-Myers Squibb Pharma Company N-ureidoalkyl-piperidines as modulators of chemokine receptor activity
WO2000035876A1 (en) 1998-12-18 2000-06-22 Du Pont Pharmaceuticals Company 2-substituted-4-nitrogen heterocycles as modulators of chemokine receptor activity
WO2000037455A1 (en) 1998-12-21 2000-06-29 Takeda Chemical Industries, Ltd. Benzothiepin-anilide derivatives, their production and their use for antagonizing ccr-5
US7217714B1 (en) 1998-12-23 2007-05-15 Agouron Pharmaceuticals, Inc. CCR5 modulators
EP1013276A1 (en) 1998-12-23 2000-06-28 Pfizer Inc. Aminoazacycloalkanes as CCR5 modulators
PE20001420A1 (es) 1998-12-23 2000-12-18 Pfizer Moduladores de ccr5
WO2000040239A1 (en) 1998-12-30 2000-07-13 Smithkline Beecham Corporation Compounds and methods
KR20010086166A (ko) 1999-01-13 2001-09-08 로즈 암스트롱, 크리스틴 에이. 트러트웨인 케모카인 수용체 조절제로서의 관능화된 헤테로시클
WO2000041685A1 (en) 1999-01-19 2000-07-20 Smithkline Beecham Corporation Ccr-3 receptor antagonists
EP1146790A4 (en) 1999-01-25 2004-03-17 Smithkline Beecham Corp COMPOUNDS AND METHODS
GB9902452D0 (en) 1999-02-05 1999-03-24 Zeneca Ltd Chemical compounds
GB9902459D0 (en) 1999-02-05 1999-03-24 Zeneca Ltd Chemical compounds
GB9902455D0 (en) 1999-02-05 1999-03-24 Zeneca Ltd Chemical compounds
GB9902453D0 (en) 1999-02-05 1999-03-24 Zeneca Ltd Chemical compounds
GB9902461D0 (en) 1999-02-05 1999-03-24 Zeneca Ltd Chemical compounds
JP2000309598A (ja) 1999-02-25 2000-11-07 Takeda Chem Ind Ltd 多剤結合型新規化合物、その製造法および用途
US6362201B1 (en) 1999-03-02 2002-03-26 Merck & Co., Inc. 3-cyclopropyl and 3-cyclobutyl pyrrolidine modulators of chemokine receptor activity
AU3389300A (en) 1999-03-02 2000-09-21 Merck & Co., Inc. Pyrrolidine modulators of chemokine receptor activity
AU3386400A (en) 1999-03-02 2000-09-21 Merck & Co., Inc. 3-alkyl substituted pyrrolidine modulators of chemokine receptor activity
US6303593B1 (en) 1999-03-02 2001-10-16 Merck & Co., Inc. 3-thienyl and 3-furanyl pyrrolidine modulators of chemokine receptor activity
WO2000053172A1 (en) 1999-03-08 2000-09-14 Smithkline Beecham Corporation Ccr-3 receptor antagonists
ES2223481T3 (es) 1999-03-10 2005-03-01 Smithkline Beecham Corporation Benzo(1,2-b:5,4-b')dipiran-4-aminas sustituidas como moduladores de ccr5.
WO2000053600A1 (fr) 1999-03-11 2000-09-14 Banyu Pharmaceutical Co., Ltd. Derives piperidiniques
CN1219780C (zh) 1999-03-24 2005-09-21 阿诺麦德股份有限公司 结合趋化因子受体的杂环化合物
CA2361366A1 (en) 1999-03-26 2000-10-05 Nicholas Kindon Novel compounds
US6399619B1 (en) 1999-04-06 2002-06-04 Merck & Co., Inc. Pyrrolidine modulators of chemokine receptor activity
US6498161B1 (en) 1999-04-06 2002-12-24 Merck & Co., Inc. Pyrrolidine modulators of chemokine receptor activity
US6248755B1 (en) 1999-04-06 2001-06-19 Merck & Co., Inc. Pyrrolidine modulators of chemokine receptor activity
US6265434B1 (en) 1999-04-06 2001-07-24 Merck & Co., Inc. Pyrrolidine modulators of chemokine receptor activity
US6358697B2 (en) 1999-04-21 2002-03-19 Children's Hospital Medical Center Intracellular pharmaceutical targeting
WO2000066551A1 (fr) 1999-04-28 2000-11-09 Takeda Chemical Industries, Ltd. Composes d'amides cycliques, leurs procedes de preparation et d'utilisation
JP2002543126A (ja) 1999-05-03 2002-12-17 スミスクライン・ビーチャム・コーポレイション Ｃｘｃｒ−４受容体アンタゴニスト−トロンボポエチン模倣物
HUP0202734A3 (en) 1999-05-04 2003-11-28 Schering Corp Use of pegylated interfron alfa-ccr5 antagonist combination for hiv therapy
US6391865B1 (en) 1999-05-04 2002-05-21 Schering Corporation Piperazine derivatives useful as CCR5 antagonists
IL145742A0 (en) 1999-05-04 2002-07-25 Schering Corp Piperidine derivatives useful as ccr5 antagonists
EP1632479B1 (en) 1999-05-04 2011-01-12 Schering Corporation Pharmaceutical compositions comprising CCR5 antagonizing piperazine derivatives
CA2373073A1 (en) 1999-05-07 2000-11-16 Takeda Chemical Industries, Ltd. Cyclic compounds and uses thereof
AU4796700A (en) 1999-05-13 2000-12-05 Dupont Pharmaceuticals Research Laboratories, Inc. Ureido-substituted cyclic amine derivatives and their use as drug
DK1179341T3 (da) 1999-05-18 2006-03-27 Teijin Ltd Lægemidler eller forebyggende midler mod sygdomme der er associeret med chemokiner
AU781780B2 (en) 1999-05-27 2005-06-09 Celltek Biotechnologies Inc. Chemokine receptor CCR3 antagonists
US6165261A (en) 1999-06-10 2000-12-26 Ergon, Inc. Water-resistant gypsum composition
ATE321751T1 (de) 1999-07-28 2006-04-15 Kirin Brewery Harnstoffderivate als ccr-3 rezeptor-inhibitoren
SE9902987D0 (sv) 1999-08-24 1999-08-24 Astra Pharma Prod Novel compounds
AU7080500A (en) 1999-08-27 2001-03-26 Chemocentryx, Inc. Compounds and methods for modulating cxcr3 function
ATE283854T1 (de) 1999-12-03 2004-12-15 Ono Pharmaceutical Co Triazaspiro(5.5)undecan-derivate und drogen, die dasselbe als aktiven inhaltsstoff enthalten
GB0011838D0 (en) 2000-05-17 2000-07-05 Astrazeneca Ab Chemical compounds
US6894063B2 (en) 2000-09-14 2005-05-17 Schering Corporation Substituted urea neuropeptide Y Y5 Receptor antagonists
AU2001294547A1 (en) 2000-09-14 2002-03-26 Schering Corporation Substituted urea neuropeptide y y5 receptor antagonists
AR031130A1 (es) 2000-09-20 2003-09-10 Abbott Lab N-acilsulfonamidas promotoras de la apoptosis
CZ20031910A3 (cs) 2000-12-11 2003-12-17 Tularik Inc. Sloučenina s antagonistickými účinky na CXCR3 a farmaceutický postředek
GB0100102D0 (en) 2001-01-03 2001-02-14 Syngenta Participations Ag Organic compounds
EP1370546A2 (en) 2001-03-16 2003-12-17 Abbott Laboratories Novel amines as histamine-3 receptor ligands and their therapeutic applications
CA2440264A1 (en) 2001-03-19 2002-09-26 Ono Pharmaceutical Co., Ltd. Triazaspiro[5.5]undecane derivative and pharmaceutical composition comprising the same as active ingredient
GB0108099D0 (en) 2001-03-30 2001-05-23 Hoffmann La Roche Aminopiperidine derivatives
EP1381592A1 (en) 2001-04-13 2004-01-21 Boehringer Ingelheim Pharmaceuticals Inc. 1,4-disubstituted benzo-fused compounds
US6495569B1 (en) 2001-04-19 2002-12-17 Millennium Pharmaceuticals, Inc. Imidazolidine compounds
US6469002B1 (en) 2001-04-19 2002-10-22 Millennium Pharmaceuticals, Inc. Imidazolidine compounds
JP4424983B2 (ja) 2001-06-05 2010-03-03 ベーリンガー インゲルハイム ファーマシューティカルズ インコーポレイテッド １，４−ジ置換ベンゾ−縮合シクロアルキルウレア化合物
CN1529699A (zh) 2001-06-20 2004-09-15 �Ʒ� 新的磺酸衍生物
US6867221B2 (en) 2001-08-30 2005-03-15 Kowa Co., Ltd. Cyclic amine compounds and pharmaceutical composition containing the same
WO2003037271A2 (en) * 2001-10-30 2003-05-08 Millennium Pharmaceuticals,Inc. Compounds, pharmaceutical compositions and methods of use therefor
MXPA04004674A (es) 2001-11-14 2004-08-12 Schering Corp Ligados de los receptors de los canabinodies.
TW200302717A (en) 2002-02-06 2003-08-16 Schering Corp Novel gamma secretase inhibitors
US20030195192A1 (en) 2002-04-05 2003-10-16 Fortuna Haviv Nicotinamides having antiangiogenic activity
EP1554253A4 (en) 2002-06-03 2006-09-20 Smithkline Beecham Corp IMIDAZOLIUM COMPOUNDS INHIBITORS OF CXCR3
EP1552842A1 (en) 2002-06-07 2005-07-13 Kyowa Hakko Kogyo Co., Ltd. Bicyclic pyrimidine derivatives
CN1688577A (zh) 2002-09-18 2005-10-26 小野药品工业株式会社 三氮杂螺[5.5]十一烷衍生物及以它为活性成分的药物
JP2006511500A (ja) 2002-10-30 2006-04-06 メルク　エンド　カムパニー　インコーポレーテッド γ−アミノアミド系のケモカイン受容体活性調節剤
ATE552253T1 (de) * 2002-11-08 2012-04-15 Novartis Int Pharm Ltd 3-substituierte-6-aryl- pyridin derivate als liganden für c5a-rezeptoren
AU2003284402A1 (en) 2002-11-15 2004-06-15 Yamanouchi Pharmaceutical Co., Ltd. Antagonist to melanin-concentrating hormone receptor
WO2004052862A1 (ja) 2002-12-10 2004-06-24 Ono Pharmaceutical Co., Ltd. 含窒素複素環化合物およびその医薬用途
JP2004256531A (ja) 2003-02-07 2004-09-16 Takeda Chem Ind Ltd 三環性化合物、その製造法および用途
GB0305426D0 (en) 2003-03-08 2003-04-16 Glaxo Group Ltd Novel compounds
TWI344955B (en) 2003-03-14 2011-07-11 Ono Pharmaceutical Co Heterocyclic rinf having nitrogen atom derivatives and medicament containing the derivatives as active ingredient
AU2004233828B2 (en) 2003-04-24 2009-05-28 Merck Sharp & Dohme Corp. Inhibitors of Akt activity
EP1661889A4 (en) 2003-09-05 2009-08-05 Ono Pharmaceutical Co ANTAGONIST OF THE CHEMOKINE RECEPTOR AND ITS USE FOR MEDICAL PURPOSES
TWI400232B (zh) 2004-09-13 2013-07-01 Ono Pharmaceutical Co 含氮雜環衍生物及以該含氮雜環衍生物為有效成分之藥劑
JP2007063268A (ja) 2005-08-05 2007-03-15 Tanabe Seiyaku Co Ltd 医薬組成物
BRPI0614801A2 (pt) 2005-08-16 2009-05-19 Genzyme Corp compostos de ligação a receptor de quimiocina
AU2007225836A1 (en) 2006-03-10 2007-09-20 Ono Pharmaceutical Co., Ltd. Nitrogenated heterocyclic derivative, and pharmaceutical agent comprising the derivative as active ingredient

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CA2644368A1 (en) 2007-09-20
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