PL2486041T3 - Pochodne hydroksylowe, keto i glukuronidowe 3-(4-(7H-pirolo[2,3-d]pirymidyn-4-ylo)-1H-pirazol-1-ilo)-3-cyklopentylopropanonitrylu - Google Patents

Pochodne hydroksylowe, keto i glukuronidowe 3-(4-(7H-pirolo[2,3-d]pirymidyn-4-ylo)-1H-pirazol-1-ilo)-3-cyklopentylopropanonitrylu

Info

Publication number
PL2486041T3
PL2486041T3 PL10765557T PL10765557T PL2486041T3 PL 2486041 T3 PL2486041 T3 PL 2486041T3 PL 10765557 T PL10765557 T PL 10765557T PL 10765557 T PL10765557 T PL 10765557T PL 2486041 T3 PL2486041 T3 PL 2486041T3
Authority
PL
Poland
Prior art keywords
cyclopentylpropanenitrile
pyrrolo
pyrazol
pyrimidin
keto
Prior art date
Application number
PL10765557T
Other languages
English (en)
Polish (pl)
Inventor
James D Rodgers
Adam Shilling
Argyrios G Arvanitis
Stacey Shepard
Laurine G Galya
Mei Li
Frank M Nedza
Original Assignee
Incyte Holdings Corp
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Incyte Holdings Corp filed Critical Incyte Holdings Corp
Publication of PL2486041T3 publication Critical patent/PL2486041T3/pl

Links

Classifications

    • 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
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/4155—1,2-Diazoles non 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • 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
    • 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
    • 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
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • 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
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/04—Drugs for skeletal disorders for non-specific disorders of the connective tissue
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • 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
    • A61P5/00—Drugs for disorders of the endocrine 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
    • 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
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H15/00—Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
    • C07H15/26—Acyclic or carbocyclic radicals, substituted by hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H17/00—Compounds containing heterocyclic radicals directly attached to hetero atoms of saccharide radicals
    • C07H17/02—Heterocyclic radicals containing only nitrogen as ring hetero atoms

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Biotechnology (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Diabetes (AREA)
  • Neurosurgery (AREA)
  • Endocrinology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Transplantation (AREA)
  • Psychiatry (AREA)
  • Reproductive Health (AREA)
  • Hospice & Palliative Care (AREA)
  • Pain & Pain Management (AREA)
  • Obesity (AREA)
  • Urology & Nephrology (AREA)
  • Emergency Medicine (AREA)
PL10765557T 2009-10-09 2010-10-08 Pochodne hydroksylowe, keto i glukuronidowe 3-(4-(7H-pirolo[2,3-d]pirymidyn-4-ylo)-1H-pirazol-1-ilo)-3-cyklopentylopropanonitrylu PL2486041T3 (pl)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US25038709P 2009-10-09 2009-10-09
US31621810P 2010-03-22 2010-03-22
EP10765557.3A EP2486041B1 (en) 2009-10-09 2010-10-08 Hydroxyl, keto, and glucuronide derivatives of 3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl)-3-cyclopentylpropanenitrile
PCT/US2010/052011 WO2011044481A1 (en) 2009-10-09 2010-10-08 Hydroxyl, keto, and glucuronide derivatives of 3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl)-3-cyclopentylpropanenitrile

Publications (1)

Publication Number Publication Date
PL2486041T3 true PL2486041T3 (pl) 2014-01-31

Family

ID=43037845

Family Applications (1)

Application Number Title Priority Date Filing Date
PL10765557T PL2486041T3 (pl) 2009-10-09 2010-10-08 Pochodne hydroksylowe, keto i glukuronidowe 3-(4-(7H-pirolo[2,3-d]pirymidyn-4-ylo)-1H-pirazol-1-ilo)-3-cyklopentylopropanonitrylu

Country Status (13)

Country Link
US (3) US8486902B2 (2)
EP (1) EP2486041B1 (2)
JP (3) JP5946768B2 (2)
KR (3) KR20180126619A (2)
CN (2) CN102596960B (2)
BR (1) BR112012008267B1 (2)
CA (1) CA2777114C (2)
EA (1) EA021478B1 (2)
ES (1) ES2435491T3 (2)
MX (1) MX2012004180A (2)
PL (1) PL2486041T3 (2)
PT (1) PT2486041E (2)
WO (1) WO2011044481A1 (2)

Families Citing this family (69)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SG10202003901UA (en) 2005-12-13 2020-05-28 Incyte Holdings Corp Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as janus kinase inhibitors
CL2008001709A1 (es) 2007-06-13 2008-11-03 Incyte Corp Compuestos derivados de pirrolo [2,3-b]pirimidina, moduladores de quinasas jak; composicion farmaceutica; y uso en el tratamiento de enfermedades tales como cancer, psoriasis, artritis reumatoide, entre otras.
KR20150036210A (ko) 2007-06-13 2015-04-07 인사이트 코포레이션 야누스 키나제 억제제（Ｒ）―３―（４―（７Ｈ―피롤로［２，３－ｄ］피리미딘―4―일）―1Ｈ―피라졸―1―일）―３―사이클로펜틸프로판니트릴의 염
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.
TWI720517B (zh) 2009-01-15 2021-03-01 美商英塞特公司 製造ｊａｋ抑制劑之方法及相關中間化合物
AR076794A1 (es) 2009-05-22 2011-07-06 Incyte Corp Derivados de n-(hetero)aril-pirrolidina de pirazol-4-il-pirrolo [2,3-d]pirimidinas y pirrol-3-il-pirrolo [2,3-d ]pirimidinas como inhibidores de la quinasa janus y composiciones farmaceuticas que los contienen
SI2432472T1 (sl) * 2009-05-22 2019-11-29 Incyte Holdings Corp 3-(4-(7H-pirolo(2,3-d)pirimidin-4-il)-1H-pirazol-1-il)oktan- ali heptan-nitril kot inhibitorji JAK
TW201113285A (en) 2009-09-01 2011-04-16 Incyte Corp Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
EA021478B1 (ru) * 2009-10-09 2015-06-30 Инсайт Корпорейшн ГИДРОКСИЛЬНЫЕ, КЕТО И ГЛЮКУРОНИДНЫЕ ПРОИЗВОДНЫЕ 3-(4-(7Н-ПИРРОЛО[2,3-d]ПИРИМИДИН-4-ИЛ)-1Н-ПИРАЗОЛ-1-ИЛ)-3-ЦИКЛОПЕНТИЛПРОПАННИТРИЛА
JP5858434B2 (ja) * 2010-02-18 2016-02-10 インサイト・ホールディングス・コーポレイションＩｎｃｙｔｅ Ｈｏｌｄｉｎｇｓ Ｃｏｒｐｏｒａｔｉｏｎ Ｊａｎｕｓキナーゼ阻害薬としてのシクロブタンおよびメチルシクロブタン誘導体
EP3354652B1 (en) 2010-03-10 2020-05-06 Incyte Holdings Corporation Piperidin-4-yl azetidine derivatives as jak1 inhibitors
PE20130216A1 (es) 2010-05-21 2013-02-27 Incyte Corp Formulacion topica para un inhibidor de jak
PE20140146A1 (es) 2010-11-19 2014-02-06 Incyte Corp Derivados de pirrolopiridina y pirrolopirimidina sustituidos con ciclobutilo como inhibidores de jak
US9034884B2 (en) 2010-11-19 2015-05-19 Incyte Corporation Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as JAK inhibitors
ES2547916T3 (es) 2011-02-18 2015-10-09 Novartis Pharma Ag Terapia de combinación de inhibidores de mTOR/JAK
CN103797010B (zh) 2011-06-20 2016-02-24 因塞特控股公司 作为jak抑制剂的氮杂环丁烷基苯基、吡啶基或吡嗪基甲酰胺衍生物
EP2741747A1 (en) 2011-08-10 2014-06-18 Novartis Pharma AG JAK P13K/mTOR COMBINATION THERAPY
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
ES3018133T3 (en) 2011-11-30 2025-05-14 Univ Emory Jak inhibitors for use in the prevention or treatment of a viral disease caused by a coronaviridae
TW201406761A (zh) 2012-05-18 2014-02-16 Incyte Corp 做爲ｊａｋ抑制劑之哌啶基環丁基取代之吡咯并吡啶及吡咯并嘧啶衍生物
US20150246043A1 (en) 2012-07-27 2015-09-03 Ratiopharm Gmbh Oral dosage forms for modified release comprising ruxolitinib
TWI646099B (zh) 2012-11-01 2019-01-01 英塞特控股公司 作爲ｊａｋ抑制劑之三環稠合噻吩衍生物
PH12020551186B1 (en) 2012-11-15 2024-03-20 Incyte Holdings Corp Sustained-release dosage forms of ruxolitinib
US20160123982A1 (en) 2013-02-04 2016-05-05 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for assaying jak2 activity in red blood cells and uses thereof
RS62867B1 (sr) 2013-03-06 2022-02-28 Incyte Holdings Corp Postupci i intermedijeri za dobijanje inhibitora jak
HUE033587T2 (hu) 2013-05-17 2017-12-28 Incyte Corp Bipirazol-származékok mint JAK inhibitorok
SMT202000315T1 (it) 2013-08-07 2020-07-08 Incyte Corp Forme di dosaggio a rilascio prolungato per un inibitore di jak1
MA39987A (fr) 2014-04-30 2017-03-08 Incyte Corp Procédés de préparation d'un inhibiteur de jak1 et nouvelles formes associées
US9498467B2 (en) 2014-05-30 2016-11-22 Incyte Corporation Treatment of chronic neutrophilic leukemia (CNL) and atypical chronic myeloid leukemia (aCML) by inhibitors of JAK1
JP6149810B2 (ja) * 2014-06-13 2017-06-21 株式会社島津製作所 代謝物解析システム及び代謝物解析方法
AR101504A1 (es) 2014-08-11 2016-12-21 Acerta Pharma Bv Combinaciones terapéuticas de un inhibidor de la btk, un inhibidor de la pi3k, un inhibidor de la jak-2, y/o un inhibidor de la cdk4/6
TW201618775A (zh) 2014-08-11 2016-06-01 艾森塔製藥公司 Ｂｔｋ抑制劑、ｐｉ３ｋ抑制劑、ｊａｋ－２抑制劑、ｐｄ－１抑制劑及／或ｐｄ－ｌ１抑制劑之治療組合物
PL3179991T3 (pl) 2014-08-11 2022-02-14 Acerta Pharma B.V. Kombinacje terapeutyczne inhibitora btk i inhibitora bcl-2
CN105777754B (zh) * 2014-12-16 2019-07-26 北京赛林泰医药技术有限公司 吡咯并嘧啶化合物
RS60237B1 (sr) 2015-11-24 2020-06-30 Theravance Biopharma R&D Ip Llc Prolekovi jak inhibitornih jedinjenja za lečenje gastorintestinalne inflamatorne bolesti
CN107513067A (zh) * 2016-06-16 2017-12-26 北京赛林泰医药技术有限公司 含有取代环戊基的吡咯并嘧啶化合物
CN107759623B (zh) * 2016-08-23 2020-08-14 苏州旺山旺水生物医药有限公司 Jak抑制剂的中间体及其制备方法
CN110418796A (zh) 2017-03-08 2019-11-05 施万生物制药研发Ip有限责任公司 托法替尼(tofacitinib)的葡萄糖苷酸前药
WO2018167283A1 (en) 2017-03-17 2018-09-20 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for the diagnosis and treatment of pancreatic ductal adenocarcinoma associated neural remodeling
EP3610264A1 (en) 2017-04-13 2020-02-19 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for the diagnosis and treatment of pancreatic ductal adenocarcinoma
CN108794480A (zh) * 2017-04-28 2018-11-13 天津药物研究院有限公司 吡咯并嘧啶类化合物、其制备方法和用途
EP3609903A1 (en) 2017-05-23 2020-02-19 Theravance Biopharma R&D IP, LLC Thiocarbamate prodrugs of tofacitinib
PH12019502605A1 (en) * 2017-05-23 2020-10-26 Theravance Biopharma R&D Ip Llc Glucuronide prodrugs of janus kinase inhibitors
WO2019113487A1 (en) 2017-12-08 2019-06-13 Incyte Corporation Low dose combination therapy for treatment of myeloproliferative neoplasms
SG11202007164UA (en) 2018-01-30 2020-08-28 Incyte Corp Processes for preparing (1 -(3-fluoro-2-(trifluoromethyl)isonicotinyl)piperidine-4-one)
KR102925957B1 (ko) 2018-02-16 2026-02-11 인사이트 코포레이션 사이토카인-관련 장애의 치료를 위한 jak1 경로 억제제
SMT202400306T1 (it) 2018-03-30 2024-09-16 Incyte Corp Trattamento dell'idrosadenite suppurativa utilizzando inibitori di jak.
MA52655A (fr) 2018-03-30 2021-02-17 Incyte Corp Biomarqueurs pour maladie cutanée inflammatoire
CA3097025A1 (en) 2018-04-13 2019-10-17 Incyte Corporation Biomarkers for graft-versus-host disease
CN117285467A (zh) 2018-07-31 2023-12-26 罗索肿瘤学公司 喷雾干燥的分散体和制剂
CN112955431A (zh) * 2018-09-06 2021-06-11 艾尼纳制药公司 可用于治疗自身免疫性病症和炎性病症的化合物
CA3117969A1 (en) 2018-10-31 2020-05-07 Incyte Corporation Combination therapy for treatment of hematological diseases
WO2020092015A1 (en) 2018-11-02 2020-05-07 University Of Rochester Therapeutic mitigation of epithelial infection
US12351571B2 (en) 2018-12-19 2025-07-08 Array Biopharma Inc. Substituted quinoxaline compounds as inhibitors of FGFR tyrosine kinases
EP3898626A1 (en) 2018-12-19 2021-10-27 Array Biopharma, Inc. Substituted pyrazolo[1,5-a]pyridine compounds as inhibitors of fgfr tyrosine kinases
US20220372135A1 (en) 2019-09-27 2022-11-24 Disc Medicine, Inc. Methods for treating myelofibrosis and related conditions
CN110538183B (zh) * 2019-10-09 2021-05-04 吉林大学 一种预防和治疗小儿湿疹的组合物及其制备方法
WO2021072098A1 (en) 2019-10-10 2021-04-15 Incyte Corporation Biomarkers for graft-versus-host disease
EP4041204A1 (en) 2019-10-10 2022-08-17 Incyte Corporation Biomarkers for graft-versus-host disease
JP7717065B2 (ja) 2019-11-22 2025-08-01 インサイト コーポレーション Ａｌｋ２阻害剤及びｊａｋ２阻害剤を含む併用療法
KR20230012539A (ko) 2020-05-13 2023-01-26 디스크 메디슨, 인크. 골수섬유증을 치료하기 위한 항-헤모주벨린 (hjv) 항체
MX2022015221A (es) 2020-06-02 2023-03-08 Incyte Corp Procesos para preparar un inhibidor de cinasa jano 1 (jak1).
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
PE20231743A1 (es) 2020-08-18 2023-10-31 Incyte Corp Proceso e intermediarios para preparar un inhibidor de jak
IL300557A (en) 2020-08-18 2023-04-01 Incyte Corp Process and intermediates for preparing a JAK1 inhibitor
CA3204374A1 (en) 2020-12-08 2022-06-16 Incyte Corporation Jak1 pathway inhibitors for the treatment of vitiligo
UA129643C2 (uk) 2021-05-03 2025-06-18 Інсайт Корпорейшн Інгібітори шляху jak1 для лікування вузлуватого свербця
US12071439B2 (en) 2021-07-12 2024-08-27 Incyte Corporation Process and intermediates for preparing a JAK inhibitor

Family Cites Families (73)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3036390A1 (de) 1980-09-26 1982-05-13 Troponwerke GmbH & Co KG, 5000 Köln Neue pyrrolo-pyrimidine, verfahren zu ihrer herstellung und ihre verwendung bei der herstellung von biologischen wirkstoffen
US5521184A (en) 1992-04-03 1996-05-28 Ciba-Geigy Corporation Pyrimidine derivatives and processes for the preparation thereof
JP4010563B2 (ja) 1995-07-05 2007-11-21 イー・アイ・デユポン・ドウ・ヌムール・アンド・カンパニー 殺菌・殺カビ性のピリミジノン類
SI9620103A (sl) 1995-07-06 1998-10-31 Novartis Ag Pirolopirimidini in postopki za njihovo pripravo
US6232320B1 (en) 1998-06-04 2001-05-15 Abbott Laboratories Cell adhesion-inhibiting antiinflammatory compounds
AU4231299A (en) 1998-06-04 1999-12-20 Abbott Laboratories Cell adhesion-inhibiting antinflammatory compounds
PA8474101A1 (es) 1998-06-19 2000-09-29 Pfizer Prod Inc Compuestos de pirrolo [2,3-d] pirimidina
SK286640B6 (sk) 1998-06-19 2009-03-05 Pfizer Products Inc. Pyrol [2,3-d] pyrimidínová zlúčenina, jej použitie na výrobu liečiva, farmaceutická kompozícia s jej obsahom, použitie jej kombinácie s ďalšími činidlami a súpravy s jej obsahom na výrobu liečiva
PT1107964E (pt) 1998-08-11 2010-06-11 Novartis Ag Derivados de isoquinolina com actividade inibidora da angiogénese
US6133031A (en) 1999-08-19 2000-10-17 Isis Pharmaceuticals Inc. Antisense inhibition of focal adhesion kinase expression
GB9905075D0 (en) 1999-03-06 1999-04-28 Zeneca Ltd Chemical compounds
DE60037345T2 (de) * 1999-12-10 2008-11-13 Pfizer Products Inc., Groton Pyrrolo(2,3-d)pyrimidin-Verbindungen
WO2001047922A2 (en) 1999-12-24 2001-07-05 Aventis Pharma Limited Azaindoles
GB0004890D0 (en) 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
US6335342B1 (en) 2000-06-19 2002-01-01 Pharmacia & Upjohn S.P.A. Azaindole derivatives, process for their preparation, and their use as antitumor agents
CN100548375C (zh) 2000-06-23 2009-10-14 田边三菱制药株式会社 抗肿瘤作用增效剂
ATE423120T1 (de) 2000-06-26 2009-03-15 Pfizer Prod Inc Pyrroloä2,3-düpyrimidin verbindungen als immunosuppressive wirkstoffe
KR100786927B1 (ko) 2000-06-28 2007-12-17 스미스클라인비이참피이엘시이 습식 분쇄방법
GB0100622D0 (en) 2001-01-10 2001-02-21 Vernalis Res Ltd Chemical compounds V111
US20040102455A1 (en) 2001-01-30 2004-05-27 Burns Christopher John Method of inhibiting kinases
US7301023B2 (en) 2001-05-31 2007-11-27 Pfizer Inc. Chiral salt resolution
EP1414443B1 (en) 2001-08-01 2006-11-15 Merck & Co., Inc. BENZIMIDAZO 4,5-f|ISOQUINOLINONE DERIVATIVES
BR0212760A (pt) 2001-09-19 2004-12-07 Aventis Pharma Sa Compostos quìmicos
DE60213842T2 (de) 2001-10-30 2007-09-06 Novartis Ag Staurosporin-derivate als hemmer der flt3-rezeptor-tyrosinkinase-wirkung
PY0228255A (es) 2001-12-06 2004-06-01 Pfizer Prod Inc Compuestos cristalinos novedosos
TW200403058A (en) 2002-04-19 2004-03-01 Bristol Myers Squibb Co Heterocyclo inhibitors of potassium channel function
PE20040522A1 (es) 2002-05-29 2004-09-28 Novartis Ag Derivados de diarilurea dependientes de la cinasa de proteina
GB0215676D0 (en) 2002-07-05 2002-08-14 Novartis Ag Organic compounds
US7259161B2 (en) 2002-11-04 2007-08-21 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of JAK and other protein kinases
TWI335913B (en) 2002-11-15 2011-01-11 Vertex Pharma Diaminotriazoles useful as inhibitors of protein kinases
NZ539901A (en) 2002-11-26 2007-09-28 Pfizer Prod Inc Method of treatment of transplant rejection
UA80767C2 (en) 2002-12-20 2007-10-25 Pfizer Prod Inc Pyrimidine derivatives for the treatment of abnormal cell growth
JP2006518381A (ja) 2003-02-07 2006-08-10 バーテックス　ファーマシューティカルズ　インコーポレイテッド プロテインキナーゼのインヒビターとして有用なヘテロアリール置換ピロール
GB0305929D0 (en) 2003-03-14 2003-04-23 Novartis Ag Organic compounds
SE0301373D0 (sv) 2003-05-09 2003-05-09 Astrazeneca Ab Novel compounds
SE0301372D0 (sv) 2003-05-09 2003-05-09 Astrazeneca Ab Novel compounds
US20050043346A1 (en) 2003-08-08 2005-02-24 Pharmacia Italia S.P.A. Pyridylpyrrole derivatives active as kinase inhibitors
AR045944A1 (es) 2003-09-24 2005-11-16 Novartis Ag Derivados de isoquinolina 1.4-disustituidas
EP1689407A1 (en) 2003-11-25 2006-08-16 Pfizer Products Inc. Method of treatment of atherosclerosis
SG133602A1 (en) 2003-12-17 2007-07-30 Pfizer Prod Inc Pyrrolo [2,3-d] pyrimidine compounds for treating transplant rejection
US20050239806A1 (en) 2004-01-13 2005-10-27 Ambit Biosciences Corporation Pyrrolopyrimidine derivatives and analogs and their use in the treatment and prevention of diseases
ES2364340T3 (es) 2004-03-30 2011-08-31 Vertex Pharmaceuticals Incorporated Azaindoles útiles como inhibidores de jak y otras proteína quinasas.
WO2005105988A2 (en) 2004-04-28 2005-11-10 Vertex Pharmaceuticals Incorporated Crystal structure of human jak3 kinase domain complex and binding pockets thereof
US20060106020A1 (en) 2004-04-28 2006-05-18 Rodgers James D Tetracyclic inhibitors of Janus kinases
AU2005237254B2 (en) 2004-05-03 2010-02-04 Novartis Ag Combinations comprising a S1P receptor agonist and a JAK3 kinase inhibitor
WO2005110410A2 (en) 2004-05-14 2005-11-24 Abbott Laboratories Kinase inhibitors as therapeutic agents
PE20060426A1 (es) 2004-06-02 2006-06-28 Schering Corp DERIVADOS DE ACIDO TARTARICO COMO INHIBIDORES DE MMPs, ADAMs, TACE Y TNF-alfa
WO2006013114A1 (en) 2004-08-06 2006-02-09 Develogen Aktiengesellschaft Use of a timp-2 secreted protein product for preventing and treating pancreatic diseases and/or obesity and/or metabolic syndrome
MY179032A (en) 2004-10-25 2020-10-26 Cancer Research Tech Ltd Ortho-condensed pyridine and pyrimidine derivatives (e.g.purines) as protein kinase inhibitors
UY29177A1 (es) 2004-10-25 2006-05-31 Astex Therapeutics Ltd Derivados sustituidos de purina, purinona y deazapurina, composiciones que los contienen métodos para su preparación y sus usos
AU2005309019A1 (en) 2004-11-24 2006-06-01 Novartis Ag Combinations of JAK inhibitors and at least one of Bcr-Abl, Flt-3, FAK or RAF kinase inhibitors
AR054416A1 (es) 2004-12-22 2007-06-27 Incyte Corp Pirrolo [2,3-b]piridin-4-il-aminas y pirrolo [2,3-b]pirimidin-4-il-aminas como inhibidores de las quinasas janus. composiciones farmaceuticas.
KR101390563B1 (ko) * 2005-01-31 2014-04-30 밀란 인크. 글루쿠로니드화된 네비볼롤
KR20070104641A (ko) 2005-02-03 2007-10-26 버텍스 파마슈티칼스 인코포레이티드 단백질 키나제의 억제제로 유용한 피롤로피리미딘
US7019626B1 (en) * 2005-03-03 2006-03-28 Omnitek Engineering, Inc. Multi-fuel engine conversion system and method
EP2354140A1 (en) 2005-05-20 2011-08-10 Vertex Pharmaceuticals Incorporated Pyrrolopyridines useful as inhibitors of protein kinase
US20070049591A1 (en) 2005-08-25 2007-03-01 Kalypsys, Inc. Inhibitors of MAPK/Erk Kinase
CA2621261C (en) 2005-09-22 2014-05-20 Incyte Corporation Azepine inhibitors of janus kinases
ZA200802685B (en) 2005-09-30 2009-10-28 Vertex Pharma Deazapurines useful as inhibitors of janus kinases
SG10202003901UA (en) 2005-12-13 2020-05-28 Incyte Holdings Corp Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as janus kinase inhibitors
WO2007076423A2 (en) 2005-12-22 2007-07-05 Smithkline Beecham Corporation INHIBITORS OF Akt ACTIVITY
UA95940C2 (uk) 2006-01-17 2011-09-26 Вертекс Фармасьютикалс Інкорпорейтед Азаіндоли як інгібітори кіназ януса
SG170828A1 (en) * 2006-04-05 2011-05-30 Vertex Pharmaceuticals Inc Us Deazapurines useful as inhibitors of janus kinases
CA2673038C (en) 2006-12-22 2015-12-15 Incyte Corporation Substituted tricyclic heteroaryl compounds as janus kinase inhibitors
KR20150036210A (ko) 2007-06-13 2015-04-07 인사이트 코포레이션 야누스 키나제 억제제（Ｒ）―３―（４―（７Ｈ―피롤로［２，３－ｄ］피리미딘―4―일）―1Ｈ―피라졸―1―일）―３―사이클로펜틸프로판니트릴의 염
CL2008001709A1 (es) * 2007-06-13 2008-11-03 Incyte Corp Compuestos derivados de pirrolo [2,3-b]pirimidina, moduladores de quinasas jak; composicion farmaceutica; y uso en el tratamiento de enfermedades tales como cancer, psoriasis, artritis reumatoide, entre otras.
HUE029767T2 (en) * 2008-03-11 2017-04-28 Incyte Holdings Corp JAK inhibitor azetidine and cyclobutane derivatives
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.
TWI720517B (zh) * 2009-01-15 2021-03-01 美商英塞特公司 製造ｊａｋ抑制劑之方法及相關中間化合物
AR076794A1 (es) * 2009-05-22 2011-07-06 Incyte Corp Derivados de n-(hetero)aril-pirrolidina de pirazol-4-il-pirrolo [2,3-d]pirimidinas y pirrol-3-il-pirrolo [2,3-d ]pirimidinas como inhibidores de la quinasa janus y composiciones farmaceuticas que los contienen
TW201113285A (en) * 2009-09-01 2011-04-16 Incyte Corp Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
EA021478B1 (ru) * 2009-10-09 2015-06-30 Инсайт Корпорейшн ГИДРОКСИЛЬНЫЕ, КЕТО И ГЛЮКУРОНИДНЫЕ ПРОИЗВОДНЫЕ 3-(4-(7Н-ПИРРОЛО[2,3-d]ПИРИМИДИН-4-ИЛ)-1Н-ПИРАЗОЛ-1-ИЛ)-3-ЦИКЛОПЕНТИЛПРОПАННИТРИЛА
JP5858434B2 (ja) * 2010-02-18 2016-02-10 インサイト・ホールディングス・コーポレイションＩｎｃｙｔｅ Ｈｏｌｄｉｎｇｓ Ｃｏｒｐｏｒａｔｉｏｎ Ｊａｎｕｓキナーゼ阻害薬としてのシクロブタンおよびメチルシクロブタン誘導体

Also Published As

Publication number Publication date
JP2017226695A (ja) 2017-12-28
KR20120102604A (ko) 2012-09-18
CN102596960B (zh) 2016-01-20
EP2486041B1 (en) 2013-08-14
BR112012008267B1 (pt) 2022-10-04
EA021478B1 (ru) 2015-06-30
KR20170098334A (ko) 2017-08-29
WO2011044481A1 (en) 2011-04-14
JP6251232B2 (ja) 2017-12-20
CA2777114A1 (en) 2011-04-14
PT2486041E (pt) 2013-11-14
KR101805936B1 (ko) 2017-12-07
BR112012008267A2 (2) 2021-11-03
US20110086810A1 (en) 2011-04-14
JP2016056183A (ja) 2016-04-21
US20130345157A1 (en) 2013-12-26
CA2777114C (en) 2018-10-23
US20140378400A1 (en) 2014-12-25
MX2012004180A (es) 2012-07-17
AU2010303245A1 (en) 2012-05-10
CN102596960A (zh) 2012-07-18
EP2486041A1 (en) 2012-08-15
KR101921850B1 (ko) 2018-11-23
JP2013507390A (ja) 2013-03-04
US9512161B2 (en) 2016-12-06
CN105541847A (zh) 2016-05-04
ES2435491T3 (es) 2013-12-19
JP5946768B2 (ja) 2016-07-06
KR20180126619A (ko) 2018-11-27
US8486902B2 (en) 2013-07-16
US8748401B2 (en) 2014-06-10
CN105541847B (zh) 2019-08-16
EA201200565A1 (ru) 2012-09-28
HK1174899A1 (en) 2013-06-21

Similar Documents

Publication Publication Date Title
PL2486041T3 (pl) Pochodne hydroksylowe, keto i glukuronidowe 3-(4-(7H-pirolo[2,3-d]pirymidyn-4-ylo)-1H-pirazol-1-ilo)-3-cyklopentylopropanonitrylu
IL216609A0 (en) Preparation and uses of 1,2,4-triazolo [1,5a] pyridine derivatives
EP2346837B8 (en) Methods of preparing quinazolinone derivatives
IL208023A (en) Acetonitriles of {1 – modified-3– [4– (h7 – pyrrolo [3,2– d] pyrimidin – 4 – il) - h1– pyrazole – 1 – il] azetidine – 3 – il} and pharmaceutical preparations containing them
SI2432472T1 (sl) 3-(4-(7H-pirolo(2,3-d)pirimidin-4-il)-1H-pirazol-1-il)oktan- ali heptan-nitril kot inhibitorji JAK
IL210176A0 (en) Substituted pyrimidone derivatives
IL209840A0 (en) Azacarboline derivatives, preparation thereof, and therapeutic use thereof as kinase inhibitors
IL216226A0 (en) Cyclopenta [c] pyrrole-2-carboxylate derivatives, preparation thereof, and therapeutic use thereof
IL211584A (en) Macrocyclic pyrimidine compounds, their preparation and use
EP2089392A4 (en) 3- (DIHYDRO-1H-PYRAZOLO Ý4,3-D¨PYRIMIDIN-5-YL) -4-PROPOXYBENZENESULFONAMIDE DERIVATIVES AND METHODS OF USE
IL210514A0 (en) Pyridino-pyridinone derivatives, preparation thereof, and therapeutic use thereof
EP2411009B8 (fr) Applications thérapeutiques de dérivés de quinazolinedione
ZA201104100B (en) Dimeric avermectin and milbemycin derivatives
IL213790A (en) 2-Pyridine-2-Ill-Pyrazole-3 (2 h) History - On, Preparation and Medical Use
IL215609A0 (en) Quinazolinedione derivatives, preparation thereof and various therapeutic uses thereof
ZA201100759B (en) Process for the preparation of substituted pyrimidine derivatives
EP2418330B8 (en) Foaming ceramic sanitary
IL209903A0 (en) Derivatives of 2-oxo-alkyl-1-piperazin-2-one, preparation method thereof and therapeutic use of same
IL212170A0 (en) Atropisomers of (hydroxyalkyl) pyrrole derivatives
ZA201100251B (en) Substituted 1-benzyl-cinnolin-4(1h)-one derivatives,preparation thereof,and therapeutic use thereof
IL214544A0 (en) Substituted 3-benzofuranyl-indol-2-one-3-acetamidopiperazine derivatives, preparation thereof, and therapeutic use thereof
IL215512A0 (en) Substituted 1-alkylcinnolin-4(1h)-one derivatives, preparation thereof and therapeutic application of same
HK1134493A (en) 3-(dihydro-1h-pyrazolo ü4,3-d¨pyrimidin-5-yl)-4-propoxybenzenesulfonamide derivatives and methods of use
HK1156857B (en) Process for the preparation of substituted pyrimidine derivatives
HK1166066A (en) Substituted 1-alkylcinnolin-4(1h)-one derivatives, preparation thereof and therapeutic application of same