KR20180126619A - 3-(4-(7H-피롤로〔2,3-d〕피리미딘-4-일)-1H-피라졸-1-일)-3-사이클로펜틸프로판니트릴의 하이드록실, 케토 및 글루쿠로나이드 유도체 - Google Patents
3-(4-(7H-피롤로〔2,3-d〕피리미딘-4-일)-1H-피라졸-1-일)-3-사이클로펜틸프로판니트릴의 하이드록실, 케토 및 글루쿠로나이드 유도체 Download PDFInfo
- Publication number
- KR20180126619A KR20180126619A KR1020187033300A KR20187033300A KR20180126619A KR 20180126619 A KR20180126619 A KR 20180126619A KR 1020187033300 A KR1020187033300 A KR 1020187033300A KR 20187033300 A KR20187033300 A KR 20187033300A KR 20180126619 A KR20180126619 A KR 20180126619A
- Authority
- KR
- South Korea
- Prior art keywords
- pyrrolo
- pyrimidin
- pyrazol
- propanenitrile
- hydroxy
- Prior art date
- Legal status (The legal status 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 status listed.)
- Ceased
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- 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
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
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- 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
- 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
- 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
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- 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)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Immunology (AREA)
- Biochemistry (AREA)
- Biotechnology (AREA)
- Genetics & Genomics (AREA)
- Molecular Biology (AREA)
- Biomedical Technology (AREA)
- Diabetes (AREA)
- Neurology (AREA)
- Endocrinology (AREA)
- Physical Education & Sports Medicine (AREA)
- Neurosurgery (AREA)
- Hematology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Dermatology (AREA)
- Oncology (AREA)
- Rheumatology (AREA)
- Obesity (AREA)
- Cardiology (AREA)
- Urology & Nephrology (AREA)
- Hospice & Palliative Care (AREA)
- Reproductive Health (AREA)
- Pain & Pain Management (AREA)
- Heart & Thoracic Surgery (AREA)
- Psychiatry (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US25038709P | 2009-10-09 | 2009-10-09 | |
| US61/250,387 | 2009-10-09 | ||
| US31621810P | 2010-03-22 | 2010-03-22 | |
| US61/316,218 | 2010-03-22 | ||
| 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 |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020177023122A Division KR101921850B1 (ko) | 2009-10-09 | 2010-10-08 | 3-(4-(7H-피롤로〔2,3-d〕피리미딘-4-일)-1H-피라졸-1-일)-3-사이클로펜틸프로판니트릴의 하이드록실, 케토 및 글루쿠로나이드 유도체 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| KR20180126619A true KR20180126619A (ko) | 2018-11-27 |
Family
ID=43037845
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020187033300A Ceased KR20180126619A (ko) | 2009-10-09 | 2010-10-08 | 3-(4-(7H-피롤로〔2,3-d〕피리미딘-4-일)-1H-피라졸-1-일)-3-사이클로펜틸프로판니트릴의 하이드록실, 케토 및 글루쿠로나이드 유도체 |
| KR1020127009995A Active KR101805936B1 (ko) | 2009-10-09 | 2010-10-08 | 3-(4-(7H-피롤로〔2,3-d〕피리미딘-4-일)-1H-피라졸-1-일)-3-사이클로펜틸프로판니트릴의 하이드록실, 케토 및 글루쿠로나이드 유도체 |
| KR1020177023122A Active KR101921850B1 (ko) | 2009-10-09 | 2010-10-08 | 3-(4-(7H-피롤로〔2,3-d〕피리미딘-4-일)-1H-피라졸-1-일)-3-사이클로펜틸프로판니트릴의 하이드록실, 케토 및 글루쿠로나이드 유도체 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020127009995A Active KR101805936B1 (ko) | 2009-10-09 | 2010-10-08 | 3-(4-(7H-피롤로〔2,3-d〕피리미딘-4-일)-1H-피라졸-1-일)-3-사이클로펜틸프로판니트릴의 하이드록실, 케토 및 글루쿠로나이드 유도체 |
| KR1020177023122A Active KR101921850B1 (ko) | 2009-10-09 | 2010-10-08 | 3-(4-(7H-피롤로〔2,3-d〕피리미딘-4-일)-1H-피라졸-1-일)-3-사이클로펜틸프로판니트릴의 하이드록실, 케토 및 글루쿠로나이드 유도체 |
Country Status (13)
| Country | Link |
|---|---|
| US (3) | US8486902B2 (enExample) |
| EP (1) | EP2486041B1 (enExample) |
| JP (3) | JP5946768B2 (enExample) |
| KR (3) | KR20180126619A (enExample) |
| CN (2) | CN102596960B (enExample) |
| BR (1) | BR112012008267B1 (enExample) |
| CA (1) | CA2777114C (enExample) |
| EA (1) | EA021478B1 (enExample) |
| ES (1) | ES2435491T3 (enExample) |
| MX (1) | MX2012004180A (enExample) |
| PL (1) | PL2486041T3 (enExample) |
| PT (1) | PT2486041E (enExample) |
| WO (1) | WO2011044481A1 (enExample) |
Families Citing this family (69)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PT1966202E (pt) | 2005-12-13 | 2012-01-03 | Incyte Corp | Pirrolo[2,3-b] pirimidinas e pirrolo[2,3-b]piridinas substituídas com heteroarilo como inibidores de janus quinase |
| RS53245B2 (sr) | 2007-06-13 | 2022-10-31 | Incyte Holdings Corp | Soli inhibitora janus kinaze (r)-3-(4-(7h-pirolo(2,3-d) pirimidin-4-il)-1h-pirazol-1-il)-3-ciklopentilpropan-nitrila |
| 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. |
| 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. |
| JOP20190231A1 (ar) * | 2009-01-15 | 2017-06-16 | Incyte Corp | طرق لاصلاح مثبطات انزيم jak و المركبات الوسيطة المتعلقة به |
| PL2432472T3 (pl) | 2009-05-22 | 2020-03-31 | Incyte Holdings Corporation | 3-[4-(7H-Pirolo[2,3-d]pirymidyn-4-ylo)-1H-pirazol-1-ilo]oktano- lub heptano-nitryle jako inhibitory JAK |
| 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 |
| 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 |
| ES2435491T3 (es) * | 2009-10-09 | 2013-12-19 | Incyte Corporation | Derivados de hidroxilo, ceto y glucurónido de 3-(4-(7H-pirrolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il)-3-ciclopentilpropanonitrilo |
| CN102844317B (zh) * | 2010-02-18 | 2015-06-03 | 因西特公司 | 作为Janus激酶抑制剂的环丁烷和甲基环丁烷衍生物 |
| MX354212B (es) | 2010-03-10 | 2018-02-19 | Incyte Corp | Derivados de piperidin-4-il azetidina como inhibidores de janus cinasa 1 (jak1). |
| EA202091303A3 (ru) | 2010-05-21 | 2021-05-31 | Инсайт Холдингс Корпорейшн | Композиция ингибитора jak для местного применения |
| CA2818542A1 (en) | 2010-11-19 | 2012-05-24 | Incyte Corporation | Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors |
| WO2012068440A1 (en) | 2010-11-19 | 2012-05-24 | Incyte Corporation | Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as jak inhibitors |
| EP2675451B9 (en) | 2011-02-18 | 2017-07-26 | Novartis Pharma AG | mTOR/JAK INHIBITOR COMBINATION THERAPY |
| 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 |
| HK1198579A1 (en) | 2011-08-10 | 2015-04-30 | 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 |
| CA2856722C (en) | 2011-11-30 | 2022-11-22 | Emory University | Antiviral jak inhibitors useful in treating or preventing retroviral and other viral infections |
| US9193733B2 (en) | 2012-05-18 | 2015-11-24 | Incyte Holdings Corporation | Piperidinylcyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as JAK inhibitors |
| US20150246043A1 (en) | 2012-07-27 | 2015-09-03 | Ratiopharm Gmbh | Oral dosage forms for modified release comprising ruxolitinib |
| BR112015009942A2 (pt) | 2012-11-01 | 2017-07-11 | Incyte Corp | derivados de tiofeno fundidos tricíclicos como inibidores de jak |
| NZ708157A (en) | 2012-11-15 | 2019-07-26 | 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 |
| 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 |
| WO2014186706A1 (en) | 2013-05-17 | 2014-11-20 | Incyte Corporation | Bipyrazole derivatives as jak inhibitors |
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Patent event code: PX09011S01I Patent event date: 20190827 Comment text: Decision to Refuse Application Patent event code: PX09012R01I Patent event date: 20190411 Comment text: Amendment to Specification, etc. Patent event code: PX09012R01I Patent event date: 20181116 Comment text: Amendment to Specification, etc. |
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| PX0601 | Decision of rejection after re-examination |
Comment text: Decision to Refuse Application Patent event code: PX06014S01D Patent event date: 20191010 Comment text: Amendment to Specification, etc. Patent event code: PX06012R01I Patent event date: 20190925 Comment text: Decision to Refuse Application Patent event code: PX06011S01I Patent event date: 20190827 Comment text: Amendment to Specification, etc. Patent event code: PX06012R01I Patent event date: 20190411 Comment text: Notification of reason for refusal Patent event code: PX06013S01I Patent event date: 20190211 Comment text: Amendment to Specification, etc. Patent event code: PX06012R01I Patent event date: 20181116 |