EA201391584A1 - Новое соединение, предназначенное для лечения дегенеративных и воспалительных заболеваний - Google Patents
Новое соединение, предназначенное для лечения дегенеративных и воспалительных заболеванийInfo
- Publication number
- EA201391584A1 EA201391584A1 EA201391584A EA201391584A EA201391584A1 EA 201391584 A1 EA201391584 A1 EA 201391584A1 EA 201391584 A EA201391584 A EA 201391584A EA 201391584 A EA201391584 A EA 201391584A EA 201391584 A1 EA201391584 A1 EA 201391584A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- degenerative
- treatment
- conditions
- inflammatory diseases
- diseases
- Prior art date
Links
- 230000003412 degenerative effect Effects 0.000 title 1
- 208000027866 inflammatory disease Diseases 0.000 title 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 4
- 201000010099 disease Diseases 0.000 abstract 3
- 210000000845 cartilage Anatomy 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 239000012453 solvate Substances 0.000 abstract 2
- 208000023275 Autoimmune disease Diseases 0.000 abstract 1
- 208000032170 Congenital Abnormalities Diseases 0.000 abstract 1
- 206010020751 Hypersensitivity Diseases 0.000 abstract 1
- 241000124008 Mammalia Species 0.000 abstract 1
- 206010052779 Transplant rejections Diseases 0.000 abstract 1
- 230000001594 aberrant effect Effects 0.000 abstract 1
- 230000007815 allergy Effects 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 230000004968 inflammatory condition Effects 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 239000002207 metabolite Substances 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 230000002062 proliferating effect Effects 0.000 abstract 1
- -1 pyrazolopyridine compound Chemical class 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
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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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
- A61K31/54—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 sulfur as the ring hetero atoms, e.g. sulthiame
- A61K31/541—Non-condensed thiazines containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- A—HUMAN NECESSITIES
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- 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
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- A—HUMAN NECESSITIES
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- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
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- A—HUMAN NECESSITIES
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- A61P17/06—Antipsoriatics
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- A—HUMAN NECESSITIES
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- A61P19/00—Drugs for skeletal disorders
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
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- A—HUMAN NECESSITIES
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- 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]
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- A—HUMAN NECESSITIES
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- A61P3/00—Drugs for disorders of the metabolism
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- 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
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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
- 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
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- A61P37/00—Drugs for immunological or allergic disorders
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/10—Spiro-condensed systems
- C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
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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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Immunology (AREA)
- Pulmonology (AREA)
- Diabetes (AREA)
- Physical Education & Sports Medicine (AREA)
- Rheumatology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Pain & Pain Management (AREA)
- Endocrinology (AREA)
- Dermatology (AREA)
- Emergency Medicine (AREA)
- Transplantation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
Раскрыто соединение пиразолопиридина в соответствии с формулой I, способное ингибировать JAK, а также его фармацевтически приемлемые соли, сольват, сольваты фармацевтически приемлемых солей и его биологически активный метаболит. Соединение может быть получено в виде фармацевтической композиции и может применяться для лечения или профилактики разнообразных состояний у млекопитающих, включающих людей, и, конкретно, таких состояний, которые могут быть ассоциированы с аберрантной активностью JAK, включающих посредством приведения неограничивающего примера аллергию, воспалительные состояния, аутоиммунные заболевания, пролиферативные заболевания, отторжение трансплантата, заболевания, включающие нарушения обновления хряща, врожденные дефекты хряща и/или заболевания, ассоциированные с гиперсекрецией IL6.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201161479956P | 2011-04-28 | 2011-04-28 | |
PCT/EP2012/057652 WO2012146657A1 (en) | 2011-04-28 | 2012-04-26 | Novel compound useful for the treatment of degenerative and inflammatory diseases |
Publications (2)
Publication Number | Publication Date |
---|---|
EA201391584A1 true EA201391584A1 (ru) | 2014-04-30 |
EA024743B1 EA024743B1 (ru) | 2016-10-31 |
Family
ID=46017860
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EA201391584A EA024743B1 (ru) | 2011-04-28 | 2012-04-26 | Соединение, предназначенное для лечения дегенеративных и воспалительных состояний |
Country Status (18)
Country | Link |
---|---|
US (5) | US8975406B2 (ru) |
EP (2) | EP2702059B1 (ru) |
JP (2) | JP5947372B2 (ru) |
KR (1) | KR101934707B1 (ru) |
CN (2) | CN103492385B (ru) |
AR (1) | AR086042A1 (ru) |
AU (2) | AU2012247484B2 (ru) |
BR (1) | BR112013027338A2 (ru) |
CA (2) | CA2833942A1 (ru) |
EA (1) | EA024743B1 (ru) |
HK (2) | HK1195312A1 (ru) |
IL (1) | IL228786A (ru) |
MX (2) | MX360697B (ru) |
SG (1) | SG194508A1 (ru) |
TW (1) | TWI536990B (ru) |
UY (1) | UY34037A (ru) |
WO (2) | WO2012146659A1 (ru) |
ZA (1) | ZA201307793B (ru) |
Families Citing this family (35)
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AR086042A1 (es) * | 2011-04-28 | 2013-11-13 | Galapagos Nv | Compuesto util para el tratamiento de enfermedades degenerativas e inflamatorias y composicion farmaceutica |
CN105338965A (zh) * | 2013-04-29 | 2016-02-17 | 赛诺菲股份有限公司 | 可吸入药用组合物和含有该药用组合物的吸入器装置 |
GB201321733D0 (en) * | 2013-12-09 | 2014-01-22 | Ucb Pharma Sa | Therapeutic agents |
KR101690760B1 (ko) * | 2014-11-05 | 2016-12-30 | 조길래 | 피부자극완화, 탈모방지 및 발모촉진 효과를 나타내는 카페오일펜타펩타이드 및 이를 함유하는 탈모방지 및 발모촉진용 화장료 조성물 |
TW201705961A (zh) * | 2015-06-11 | 2017-02-16 | 阿爾米雷爾有限公司 | 作為jak抑制劑的2-(吡唑并吡啶-3-基)嘧啶衍生物 |
WO2016205590A1 (en) | 2015-06-18 | 2016-12-22 | Cephalon, Inc. | Substituted 4-benzyl and 4-benzoyl piperidine derivatives |
JP6999424B2 (ja) | 2015-06-18 | 2022-01-18 | エイティナイン バイオ リミテッド | 1,4-置換ピペリジン誘導体 |
CA2992586A1 (en) | 2015-07-16 | 2017-01-19 | Array Biopharma, Inc. | Substituted pyrazolo[1,5-a]pyridine compounds as ret kinase inhibitors |
WO2017013270A1 (en) | 2015-07-23 | 2017-01-26 | Universite De Strasbourg | Use of leptin signaling inhibitor for protecting kidneys from patients having ciliopathy |
DE102015215820A1 (de) * | 2015-08-19 | 2017-02-23 | Siemens Healthcare Gmbh | Steuern eines medizintechnischen Geräts |
JP6978098B2 (ja) * | 2016-07-26 | 2021-12-08 | スーヂョウ ロングバイオテック ファーマシューティカルズ カンパニー リミテッドSuzhou Longbiotech Pharmaceuticals Co., Ltd. | 選択的jak阻害剤としての化合物、該化合物の塩類および治療への使用 |
JOP20190077A1 (ar) * | 2016-10-10 | 2019-04-09 | Array Biopharma Inc | مركبات بيرازولو [1، 5-a]بيريدين بها استبدال كمثبطات كيناز ret |
TWI704148B (zh) * | 2016-10-10 | 2020-09-11 | 美商亞雷生物製藥股份有限公司 | 作為ret激酶抑制劑之經取代吡唑并[1,5-a]吡啶化合物 |
US11168090B2 (en) | 2017-01-18 | 2021-11-09 | Array Biopharma Inc. | Substituted pyrazolo[1,5-a]pyrazines as RET kinase inhibitors |
WO2018163971A1 (ja) * | 2017-03-09 | 2018-09-13 | 富士フイルム株式会社 | 音響レンズ用樹脂材料、音響レンズ、音響波プローブ、音響波測定装置、超音波診断装置、光音響波測定装置および超音波内視鏡 |
EA037208B1 (ru) * | 2017-09-29 | 2021-02-19 | Эррей Биофарма Инк. | ЗАМЕЩЕННЫЕ ПИРАЗОЛО[1,5-а]ПИРИДИНОВЫЕ СОЕДИНЕНИЯ В КАЧЕСТВЕ ИНГИБИТОРОВ RET КИНАЗЫ |
EA035568B1 (ru) * | 2017-09-29 | 2020-07-08 | Эррей Биофарма Инк. | ЗАМЕЩЕННЫЕ ПИРАЗОЛО[1,5-а]ПИРИДИНОВЫЕ СОЕДИНЕНИЯ В КАЧЕСТВЕ ИНГИБИТОРОВ RET КИНАЗЫ |
TW202410896A (zh) | 2017-10-10 | 2024-03-16 | 美商絡速藥業公司 | 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之調配物 |
TWI783057B (zh) * | 2017-10-10 | 2022-11-11 | 美商絡速藥業公司 | 製備6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈的方法 |
JP6997876B2 (ja) | 2018-01-18 | 2022-02-04 | アレイ バイオファーマ インコーポレイテッド | Retキナーゼ阻害剤としての置換ピラゾリル[4,3-c]ピリジン化合物 |
US11524963B2 (en) | 2018-01-18 | 2022-12-13 | Array Biopharma Inc. | Substituted pyrazolo[3,4-d]pyrimidines as RET kinase inhibitors |
TWI802635B (zh) | 2018-01-18 | 2023-05-21 | 美商亞雷生物製藥股份有限公司 | 作為ret激酶抑制劑之經取代吡咯并[2,3-d]嘧啶化合物 |
EP3849986B1 (en) | 2018-09-10 | 2022-06-08 | Array Biopharma, Inc. | Fused heterocyclic compounds as ret kinase inhibitors |
CN112771043B (zh) * | 2018-09-30 | 2023-04-28 | 北京志健金瑞生物医药科技有限公司 | 取代吡唑稠环类衍生物及其制备方法和应用 |
SG11202104687SA (en) * | 2018-12-07 | 2021-06-29 | Sunshine Lake Pharma Co Ltd | Ret inhibitors, pharmaceutical compositions and uses thereof |
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EP4141003A4 (en) * | 2020-04-22 | 2024-05-15 | Shenzhen Zhongge Biological Tech Co Ltd | PYRAZOLO[1,5-A]PYRIDINE DERIVATIVE, PREPARATION METHOD THEREFOR AND ASSOCIATED COMPOSITION AND USE |
CN113713083A (zh) * | 2020-05-25 | 2021-11-30 | 南京帝昌医药科技有限公司 | 一种用于治疗脱发的药物组合 |
BR112023003835A2 (pt) | 2020-09-01 | 2023-04-04 | Syngenta Crop Protection Ag | Derivados heterocíclicos com substituintes contendo enxofre ativos em termos pesticidas |
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EP4284802A1 (en) * | 2021-02-01 | 2023-12-06 | Janssen Biotech, Inc. | Small molecule inhibitors of salt inducible kinases |
EP4284801A1 (en) * | 2021-02-01 | 2023-12-06 | Janssen Biotech, Inc. | Small molecule inhibitors of salt inducible kinases |
EP4384523A1 (en) | 2021-08-10 | 2024-06-19 | Syngenta Crop Protection AG | 2,2-difluoro-5h-[1,3]dioxolo[4,5-f]isoindol-7-one derivatives as pesticides |
CN114409675B (zh) * | 2022-01-07 | 2023-08-04 | 重庆医科大学 | 螺环异恶唑酮色满衍生物在制备用于治疗jak1介导的疾病药物中的用途 |
WO2023187191A1 (en) | 2022-04-01 | 2023-10-05 | Syngenta Crop Protection Ag | Pesticidally active heterocyclic derivatives with sulfur containing substituents |
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ES2427046T3 (es) | 2004-06-21 | 2013-10-28 | Galapagos N.V. | Métodos y medios para el tratamiento de la osteoartritis |
EP2057158B8 (en) * | 2006-08-30 | 2015-09-30 | Cellzome Limited | Triazole derivatives as kinase inhibitors |
WO2009017954A1 (en) * | 2007-08-01 | 2009-02-05 | Phenomix Corporation | Inhibitors of jak2 kinase |
SG178812A1 (en) | 2008-06-20 | 2012-03-29 | Genentech Inc | Triazolopyridine jak inhibitor compounds and methods |
WO2010010186A1 (en) * | 2008-07-25 | 2010-01-28 | Galapagos Nv | Novel compounds useful for the treatment of degenerative and inflammatory diseases |
JO3041B1 (ar) * | 2008-07-25 | 2016-09-05 | Galapagos Nv | مركبات جديدة مفيدة لمعالجة الأمراض التنكسية والالتهابية |
TWI462920B (zh) * | 2009-06-26 | 2014-12-01 | 葛萊伯格有限公司 | 用於治療退化性及發炎疾病之新穎化合物 |
AR086042A1 (es) * | 2011-04-28 | 2013-11-13 | Galapagos Nv | Compuesto util para el tratamiento de enfermedades degenerativas e inflamatorias y composicion farmaceutica |
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