PE20151764A1 - Derivados de pirrolo[2,3-d]pirimidina - Google Patents
Derivados de pirrolo[2,3-d]pirimidinaInfo
- Publication number
- PE20151764A1 PE20151764A1 PE2015001766A PE2015001766A PE20151764A1 PE 20151764 A1 PE20151764 A1 PE 20151764A1 PE 2015001766 A PE2015001766 A PE 2015001766A PE 2015001766 A PE2015001766 A PE 2015001766A PE 20151764 A1 PE20151764 A1 PE 20151764A1
- Authority
- PE
- Peru
- Prior art keywords
- alkyl
- pirrolo
- pyrimidine
- derivatives
- pyrrolo
- Prior art date
Links
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 title abstract 2
- KAESVJOAVNADME-UHFFFAOYSA-N Pyrrole Chemical class C=1C=CNC=1 KAESVJOAVNADME-UHFFFAOYSA-N 0.000 title abstract 2
- 102000015617 Janus Kinases Human genes 0.000 abstract 2
- 108010024121 Janus Kinases Proteins 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- WCYWZMWISLQXQU-UHFFFAOYSA-N methyl Chemical class [CH3] WCYWZMWISLQXQU-UHFFFAOYSA-N 0.000 abstract 2
- 239000003112 inhibitor Substances 0.000 abstract 1
- 201000006417 multiple sclerosis Diseases 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 206010039073 rheumatoid arthritis Diseases 0.000 abstract 1
- 229940124530 sulfonamide Drugs 0.000 abstract 1
Classifications
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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
- A61K31/495—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
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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
- A61K31/535—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
- A61K31/5386—1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
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- 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
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- 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
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- 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
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P17/06—Antipsoriatics
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- 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
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- 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
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- 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
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- 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
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P37/00—Drugs for immunological or allergic disorders
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P37/08—Antiallergic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P5/00—Drugs for disorders of the endocrine system
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- A—HUMAN NECESSITIES
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- A61P9/00—Drugs for disorders of the cardiovascular system
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- 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
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- 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
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- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/18—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Epidemiology (AREA)
- Pulmonology (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Diabetes (AREA)
- Psychiatry (AREA)
- Hematology (AREA)
- Dermatology (AREA)
- Oncology (AREA)
- Urology & Nephrology (AREA)
- Cardiology (AREA)
- Physical Education & Sports Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Heart & Thoracic Surgery (AREA)
- Hospice & Palliative Care (AREA)
- Endocrinology (AREA)
- Obesity (AREA)
- Emergency Medicine (AREA)
- Ophthalmology & Optometry (AREA)
- Transplantation (AREA)
- Communicable Diseases (AREA)
Abstract
SE REFIERE A DERIVADOS DE PIRROLO[2,3-d]PIRIMIDINA DONDE R1 ES H O ALQUILO C1-C4; R2 Y R3 SON H, ALQUILO C1-C6, ENTRE OTROS; R4 ES H, ARILO, ENTRE OTROS; X ES -NH-, ENTRE OTROS; Y ES -A-R5, EN DONDE A ES UN ENLACE, ENTRE OTROS; R5 ES ALQUILO C1-C6, CICLOALQUILO C3-C6, ENTRE OTROS; n ES 1 O 2; p ES DE 0 A 2. SON COMPUESTOS PREFERIDOS: 2,2,2-TRIFLUORO-N-{CIS-3-[METIL(7H-PIRROLO[2,3-d]PIRIMIDIN-4-IL)AMINO]CICLOBUTIL}-ETANSULFONAMIDA; N-{CIS-3-[METIL(7H-PIRROLO[2,3-d]PIRIMIDIN-4-IL)AMINO]CICLOBUTIL}-PROPAN-1-SULFONAMIDA; ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE LA QUINASA JANUS (JAK) SIENDO UTILES EN EL TRATAMIENTO DE ESCLEROSIS MULTIPLE, ARTRITIS REUMATOIDE
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361767947P | 2013-02-22 | 2013-02-22 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20151764A1 true PE20151764A1 (es) | 2015-12-03 |
Family
ID=50151346
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2015001766A PE20151764A1 (es) | 2013-02-22 | 2014-02-11 | Derivados de pirrolo[2,3-d]pirimidina |
Country Status (47)
Families Citing this family (39)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2011291989B2 (en) | 2010-08-18 | 2015-08-20 | Samumed, Llc | Diketones and hydroxyketones as catenin signaling pathway activators |
| ES2797376T3 (es) | 2013-01-24 | 2020-12-02 | Palvella Therapeutics Inc | Composiciones para la administración transdérmica de inhibidores de mTOR |
| HRP20190142T1 (hr) | 2013-02-22 | 2019-03-22 | Samumed, Llc | Gama-diketoni kao aktivatori signalizacijskog puta wnt/beta-katenina |
| PE20151764A1 (es) | 2013-02-22 | 2015-12-03 | Pfizer | Derivados de pirrolo[2,3-d]pirimidina |
| ES2750655T3 (es) * | 2014-08-12 | 2020-03-26 | Pfizer | Derivados de pirrolo[2,3-d]pirimidina útiles para inhibir la Janus cinasa |
| HRP20192161T1 (hr) | 2014-08-20 | 2020-02-21 | Samumed, Llc | Gama-diketoni za liječenje i prevenciju starenja kože i bora |
| KR102081272B1 (ko) * | 2015-05-29 | 2020-02-25 | 우시 포춘 파마슈티컬 컴퍼니 리미티드 | Janus 키나아제 억제제 |
| US10550126B2 (en) | 2015-10-16 | 2020-02-04 | Abbvie Inc. | Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-A]pyrrolo[2,3-e]-pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof |
| CN116270646A (zh) | 2015-10-16 | 2023-06-23 | 艾伯维公司 | 制备咪唑并[1,2-a]吡咯并[2,3-e]吡嗪类化合物及其固态形式的方法 |
| US12365689B2 (en) | 2015-10-16 | 2025-07-22 | Abbvie Inc. | Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-n-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof |
| US11773106B2 (en) | 2015-10-16 | 2023-10-03 | Abbvie Inc. | Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof |
| US11365198B2 (en) | 2015-10-16 | 2022-06-21 | Abbvie Inc. | Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof |
| CN106831779B (zh) * | 2015-11-28 | 2019-07-19 | 南昌弘益药业有限公司 | 一类jak激酶抑制剂的新化合物 |
| WO2017143014A1 (en) * | 2016-02-16 | 2017-08-24 | Brian Kim | Jak inhibitors and uses thereof |
| EP3565520A4 (en) | 2017-01-06 | 2020-08-19 | Palvella Therapeutics, Inc. | ANHYDROUS COMPOSITIONS OF MTOR INHIBITORS AND METHODS OF USE |
| 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 |
| SMT202200134T1 (it) | 2018-03-08 | 2022-05-12 | Incyte Corp | Composti di amminopirazindiolo come inibitori di pi3k-y |
| WO2020010003A1 (en) | 2018-07-02 | 2020-01-09 | Incyte Corporation | AMINOPYRAZINE DERIVATIVES AS PI3K-γ INHIBITORS |
| EP3817743A4 (en) | 2018-07-02 | 2022-07-06 | Palvella Therapeutics, Inc. | ANHYDROUS COMPOSITIONS OF MTOR INHIBITORS AND METHODS OF USE |
| IL279926B2 (en) | 2018-07-06 | 2023-12-01 | Pfizer | Manufacturing process and intermediates for a pyrrolo[2,3- d]pyrimidine compound and use thereof |
| US10744136B2 (en) | 2018-11-05 | 2020-08-18 | Avista Pharma Solutions, Inc. | Sulfonamide derivatives as JAK inhibitors |
| MX2021008984A (es) * | 2019-01-30 | 2021-09-08 | Felicamed Biotechnology Co Ltd | Inhibidor jak y metodo de preparacion del mismo. |
| KR102820235B1 (ko) | 2019-02-15 | 2025-06-16 | 화이자 인코포레이티드 | 결정질 피리미디닐-3,8-다이아자바이사이클로[3.2.1]옥타닐메타논 화합물 및 이의 용도 |
| JP7248256B2 (ja) | 2019-03-14 | 2023-03-29 | 上海華匯拓医薬科技有限公司 | Ｊａｋキナーゼ阻害剤及びその調製方法、並びにその医薬分野での使用 |
| WO2020261041A1 (en) * | 2019-06-27 | 2020-12-30 | Glenmark Life Sciences Limited | Process for preparation of abrocitinib |
| WO2021048736A1 (en) | 2019-09-11 | 2021-03-18 | Pfizer Inc. | Treatment of hidradenitis with jak inhibitors |
| CN114761013A (zh) | 2019-09-27 | 2022-07-15 | 迪斯克医药公司 | 治疗骨髓纤维化和相关病症的方法 |
| US20230149407A1 (en) | 2020-04-04 | 2023-05-18 | Pfizer Inc. | Methods of Treating Coronavirus Disease 2019 |
| CN113637018A (zh) | 2020-04-27 | 2021-11-12 | 苏州晶云药物科技股份有限公司 | 磺酰胺类化合物的晶型及其制备方法 |
| JP2023528223A (ja) | 2020-05-13 | 2023-07-04 | ディスク・メディシン・インコーポレイテッド | 骨髄線維症を処置するための抗ヘモジュベリン（ｈｊｖ）抗体 |
| EP4157845B1 (en) * | 2020-05-28 | 2025-08-13 | Pfizer Inc. | Pyrrolo[2,3-d]pyrimidine derivatives |
| CN116897156A (zh) * | 2020-09-08 | 2023-10-17 | 高德美控股有限公司 | 新型jak抑制剂化合物、其合成方法及其用途 |
| EP4210828A1 (en) * | 2020-09-11 | 2023-07-19 | Galderma Holding SA | Novel jak inhibitor compounds, method for synthesizing same and use thereof |
| US20250082638A1 (en) | 2021-02-02 | 2025-03-13 | Pfizer Inc. | Dosing Regime For Treatment of Chronic Hand Eczema |
| WO2023014049A1 (ko) * | 2021-08-02 | 2023-02-09 | 한국화학연구원 | 신규한 피롤로 피리미딘 유도체 화합물, 이의 제조방법, 및 이를 유효성분으로 포함하는 대사성 간질환의 예방 또는 치료용 약학적 조성물 |
| CN118255769A (zh) * | 2022-12-28 | 2024-06-28 | 格格巫（珠海）生物科技有限公司 | 一种立体异构体的制备方法及中间体 |
| ES2993658B2 (es) * | 2023-06-27 | 2025-07-02 | Moehs Iberica Sl | (3-(metil(7h-pirrolo[2,3-d]pirimidin-4-il)amino)ciclobutilo)carbamato de bencilo o una sal del mismo, procedimiento para su preparacion y su uso en la sintesis de abrocitinib |
| WO2025008772A2 (en) | 2023-07-06 | 2025-01-09 | Pfizer Ireland Pharmaceuticals | Improved manufacturing process and intermediates for a pyrrolo[2,3-d]pyrimidine compound and use thereof |
| ES3040374A1 (es) | 2024-04-30 | 2025-10-30 | Moehs Iberica Sl | Cocristales de N-{cis-3-[metil(7H-pirrolo[2,3-d]pirimidin-4-il)amino]ciclobutil}propano-1-sulfonamida |
Family Cites Families (53)
| Publication number | Priority date | Publication date | Assignee | Title |
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