PE20110164A1 - Nuevas fenilpirazinonas como inhibidores de quinasa - Google Patents
Nuevas fenilpirazinonas como inhibidores de quinasaInfo
- Publication number
- PE20110164A1 PE20110164A1 PE2010001208A PE2010001208A PE20110164A1 PE 20110164 A1 PE20110164 A1 PE 20110164A1 PE 2010001208 A PE2010001208 A PE 2010001208A PE 2010001208 A PE2010001208 A PE 2010001208A PE 20110164 A1 PE20110164 A1 PE 20110164A1
- Authority
- PE
- Peru
- Prior art keywords
- alkyl
- halogen
- dihydro
- phenyl
- amino
- Prior art date
Links
- 229940043355 kinase inhibitor Drugs 0.000 title 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 title 1
- 229910052736 halogen Inorganic materials 0.000 abstract 6
- 150000002367 halogens Chemical class 0.000 abstract 6
- -1 AMINO Chemical class 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 2
- UDEWPACGFVQRST-UHFFFAOYSA-N 5,5-difluorocyclohexa-1,3-diene Chemical compound FC1(F)CC=CC=C1 UDEWPACGFVQRST-UHFFFAOYSA-N 0.000 abstract 1
- 208000023275 Autoimmune disease Diseases 0.000 abstract 1
- 102000004022 Protein-Tyrosine Kinases Human genes 0.000 abstract 1
- 108090000412 Protein-Tyrosine Kinases Proteins 0.000 abstract 1
- CIUQDSCDWFSTQR-UHFFFAOYSA-N [C]1=CC=CC=C1 Chemical class [C]1=CC=CC=C1 CIUQDSCDWFSTQR-UHFFFAOYSA-N 0.000 abstract 1
- 206010003246 arthritis Diseases 0.000 abstract 1
- 230000001363 autoimmune Effects 0.000 abstract 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-M hydroxide Chemical class [OH-] XLYOFNOQVPJJNP-UHFFFAOYSA-M 0.000 abstract 1
- 208000027866 inflammatory disease Diseases 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 206010025135 lupus erythematosus Diseases 0.000 abstract 1
- 201000006417 multiple sclerosis Diseases 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
Classifications
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- 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
- C07D403/10—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 linked by a carbon chain containing aromatic 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
- A61K31/5377—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
- 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
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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
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
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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
- 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
- A61P17/00—Drugs for dermatological disorders
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- 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
- A61P17/04—Antipruritics
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- 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
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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
- 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
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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
- 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
- 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
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- 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
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- 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
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- 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
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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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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/06—Antianaemics
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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
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- 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
- 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
- C07D403/14—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 three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
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- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Diabetes (AREA)
- Dermatology (AREA)
- Hematology (AREA)
- Neurology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Pulmonology (AREA)
- Physical Education & Sports Medicine (AREA)
- Rheumatology (AREA)
- Transplantation (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Pain & Pain Management (AREA)
- Obesity (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Gastroenterology & Hepatology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
REFERIDA A UN DERIVADO DE FENILPIRAZINONA DE FORMULA (I), (II), (III), (IV) O (V), DONDE R ES H, R1, R1-R2-R3, ENTRE OTROS; R1 ES ARILO TAL COMO FENILO, NAFTILO, ENTRE OTROS, HETEROARILO DE 5 A 12 ATOMOS CON HETEROATOMOS DE N, S U O, CICLOALQUILO C3-C8, ENTRE OTROS; R2 ES C(=O), C(=O)O, ENTRE OTROS; R3 ES H O R4; R4 ES ALQUILO C1-C6, AMINO, ENTRE OTROS; Q ES CH2, CH(Y') O NH; Y' ES HALOGENO, HIDROXI O ALQUILO C1-C6; Y1 ES H O ALQUILO C1-C6; Y2 ES Y2a O Y2b; Y2a ES H O HALOGENO; Y2b ES ALQUILO C1-C6 OPCIONALMENTE SUSTITUIDO CON Y2b'; Y2b' ES OH, ALCOXI C1-C6 O HALOGENO; Y2' ES Y2'a O Y2'b; Y2'a ES HALOGENO; Y2'b ES ALQUILO C1-C6, ENTRE OTROS; n ES UN NUMERO ENTERO DE 0 A 3; Y3 ES HALOGENO, ALQUILO C1-C6, ENTRE OTROS; m ES 0 O 1; Y4 ES Y4a, Y4b, Y4c O Y4d; Y4a ES H O HALOGENO; Y4b ES ALQUILO C1-C6, ENTRE OTROS; Y4c ES CICLOALQUILO C1-C6, ENTRE OTROS; Y4d ES AMINO OPCIONALMENTE SUSTITUIDO CON ALQUILO C1-C6. SON COMPUESTOS PREFERIDOS: 6-CICLOPROPIL-2-(2-HIDROXIMETIL-3-{4-METIL-6-[4-(MORFOLINA-4-CARBONIL)-FENILAMINO]-5-OXO-4,5-DIHIDRO-PIRAZIN-2-IL}-FENIL-2H-ISOQUINOLIN-1-ONA, 2-{3-[6-(2,2-DIFLUOR-BENZOL[1,3]DIOXOL-5-IL-AMINO)-4-METIL-5-OXO-4,5-DIHIDRO-PIRAZIN-2-IL]-2-HIDROXIMETIL-FENIL}-6-DIMETILAMINO-3,4-DIHIDRO-2H-ISOQUINOLIN-1-ONA, ENTRE OTROS. DICHOS COMPUESTOS SON INHIBIDORES DE Btk (TIROSINA QUINASA BRUTON) Y SON UTILES EN EL TRATAMIENTO DE ENFERMEDADES AUTOINMUNES E INFLAMATORIAS TALES COMO ARTRITIS, LUPUS ERITEMATOSO, ESCLEROSIS MULTIPLE, ENTRE OTRAS
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US7751008P | 2008-07-02 | 2008-07-02 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20110164A1 true PE20110164A1 (es) | 2011-03-28 |
Family
ID=40940244
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2010001208A PE20110164A1 (es) | 2008-07-02 | 2009-06-22 | Nuevas fenilpirazinonas como inhibidores de quinasa |
Country Status (24)
| Country | Link |
|---|---|
| US (1) | US8536166B2 (es) |
| EP (1) | EP2300459B1 (es) |
| JP (1) | JP5490789B2 (es) |
| KR (2) | KR101320763B1 (es) |
| CN (1) | CN102083819B (es) |
| AR (1) | AR072545A1 (es) |
| AU (1) | AU2009265813B2 (es) |
| BR (1) | BRPI0913879A2 (es) |
| CA (1) | CA2728683C (es) |
| CL (1) | CL2010001608A1 (es) |
| CY (1) | CY1114223T1 (es) |
| DK (1) | DK2300459T3 (es) |
| ES (1) | ES2420854T3 (es) |
| HR (1) | HRP20130698T1 (es) |
| IL (1) | IL209729A0 (es) |
| MX (1) | MX2010013478A (es) |
| PE (1) | PE20110164A1 (es) |
| PL (1) | PL2300459T3 (es) |
| PT (1) | PT2300459E (es) |
| RU (1) | RU2507202C2 (es) |
| SI (1) | SI2300459T1 (es) |
| TW (1) | TWI401083B (es) |
| WO (1) | WO2010000633A1 (es) |
| ZA (1) | ZA201008808B (es) |
Families Citing this family (45)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8299077B2 (en) | 2009-03-02 | 2012-10-30 | Roche Palo Alto Llc | Inhibitors of Bruton's tyrosine kinase |
| SG175287A1 (en) * | 2009-04-24 | 2011-11-28 | Hoffmann La Roche | Inhibitors of bruton's tyrosine kinase |
| EP2566869B1 (en) * | 2010-05-07 | 2016-03-02 | Gilead Connecticut, Inc. | Pyridone and aza-pyridone compounds and methods of use |
| AR082590A1 (es) | 2010-08-12 | 2012-12-19 | Hoffmann La Roche | Inhibidores de la tirosina-quinasa de bruton |
| CN106220614B (zh) * | 2010-09-01 | 2019-07-16 | 吉利德康涅狄格有限公司 | 吡啶酮/吡嗪酮、其制备方法及使用方法 |
| CN103732596B (zh) | 2011-07-08 | 2016-06-01 | 诺华股份有限公司 | 吡咯并嘧啶衍生物 |
| SG11201401993RA (en) * | 2011-11-03 | 2014-05-29 | Hoffmann La Roche | Alkylated piperazine compounds as inhibitors of btk activity |
| HK1205111A1 (en) | 2011-11-03 | 2015-12-11 | 霍夫曼-拉罗奇有限公司 | 8-fluorophthalazin-1 (2h) - one compounds as inhibitors of btk activity |
| ES2552514T3 (es) | 2011-11-03 | 2015-11-30 | Hoffmann-La Roche Ag | Compuestos bicíclicos de piperazina |
| UA111756C2 (uk) | 2011-11-03 | 2016-06-10 | Ф. Хоффманн-Ля Рош Аг | Сполуки гетероарилпіридону та азапіридону як інгібітори тирозинкінази брутона |
| WO2013148603A1 (en) | 2012-03-27 | 2013-10-03 | Takeda Pharmaceutical Company Limited | Cinnoline derivatives as as btk inhibitors |
| CA2869954C (en) | 2012-04-20 | 2023-01-03 | Advinus Therapeutics Limited | Substituted hetero-bicyclic compounds, compositions and medicinal applications thereof in medical conditions related to modulation of bruton's tyrosine kinase activity |
| EP2895473A1 (en) * | 2012-09-13 | 2015-07-22 | F. Hoffmann-La Roche AG | Inhibitors of bruton's tyrosine kinase |
| WO2014108820A1 (en) * | 2013-01-08 | 2014-07-17 | Aurigene Discovery Technologies Limited | Substituted 2-pyrazinone derivatives as kinase inhibitors |
| WO2014125410A1 (en) * | 2013-02-12 | 2014-08-21 | Aurigene Discovery Technologies Limited | N-substituted heterocyclic derivatives as kinase inhibitors |
| JP6089124B2 (ja) | 2013-03-05 | 2017-03-01 | エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ | ブルトン型チロシンキナーゼの阻害薬 |
| JO3377B1 (ar) | 2013-03-11 | 2019-03-13 | Takeda Pharmaceuticals Co | مشتقات بيريدينيل وبيريدينيل مندمج |
| SMT201700160T1 (it) | 2013-04-25 | 2017-05-08 | Beigene Ltd | Composti eterociclici fusi come inibitori di protein chinasi |
| CN104177338B (zh) * | 2013-05-22 | 2018-04-03 | 南京勇山生物科技有限公司 | 一类布鲁顿激酶抑制剂 |
| CN104211703B (zh) * | 2013-05-30 | 2018-04-03 | 南京勇山生物科技有限公司 | 一类作为布鲁顿激酶抑制剂的稠杂环化合物 |
| CN110698481B (zh) * | 2013-07-03 | 2023-02-28 | 豪夫迈·罗氏有限公司 | 杂芳基吡啶酮和氮杂-吡啶酮酰胺化合物 |
| KR101742550B1 (ko) * | 2013-07-26 | 2017-06-01 | 카나 바이오사이언스, 인코포레이션 | 신규 트리아진 유도체 |
| MX2016001304A (es) | 2013-07-30 | 2016-04-07 | Gilead Connecticut Inc | Polimorfo de inhibidores de syk. |
| PT3027171T (pt) | 2013-07-30 | 2020-06-18 | Gilead Connecticut Inc | Formulação de inibidores da syk |
| ES2792183T3 (es) | 2013-09-13 | 2020-11-10 | Beigene Switzerland Gmbh | Anticuerpos anti-PD1 y su uso como productos terapéuticos y de diagnóstico |
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| TWI735853B (zh) | 2013-12-23 | 2021-08-11 | 美商克洛諾斯生技有限公司 | 脾酪胺酸激酶抑制劑 |
| CN106604742B (zh) | 2014-07-03 | 2019-01-11 | 百济神州有限公司 | 抗pd-l1抗体及其作为治疗剂及诊断剂的用途 |
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| ES2876974T3 (es) | 2015-04-07 | 2021-11-15 | Novartis Ag | Combinación de terapia con receptor de antígeno quimérico y derivados de amino pirimidina |
| AU2017240609B2 (en) | 2016-03-31 | 2021-07-15 | Takeda Pharmaceutical Company Limited | Isoquinolinyl triazolone complexes |
| CN109475536B (zh) | 2016-07-05 | 2022-05-27 | 百济神州有限公司 | 用于治疗癌症的PD-l拮抗剂和RAF抑制剂的组合 |
| WO2018033853A2 (en) | 2016-08-16 | 2018-02-22 | Beigene, Ltd. | Crystalline form of (s)-7-(1-acryloylpiperidin-4-yl)-2-(4-phenoxyphenyl)-4,5,6,7-tetra-hydropyrazolo[1,5-a]pyrimidine-3-carboxamide, preparation, and uses thereof |
| PT3500299T (pt) | 2016-08-19 | 2024-02-21 | Beigene Switzerland Gmbh | Combinação de zanubrutinib com um anticorpo anti-cd20 ou anti-pd-1 para utilização no tratamento do cancro |
| MA46285A (fr) | 2016-09-19 | 2019-07-31 | Mei Pharma Inc | Polythérapie |
| WO2018098275A1 (en) * | 2016-11-22 | 2018-05-31 | Dana-Farber Cancer Institute, Inc. | Degradation of bruton's tyrosine kinase (btk) by conjugation of btk inhibitors with e3 ligase ligand and methods of use |
| CN110461847B (zh) | 2017-01-25 | 2022-06-07 | 百济神州有限公司 | (S)-7-(1-(丁-2-炔酰基)哌啶-4-基)-2-(4-苯氧基苯基)-4,5,6,7-四氢吡唑并[1,5-a]嘧啶-3-甲酰胺的结晶形式、其制备及用途 |
| TW202515616A (zh) | 2017-06-26 | 2025-04-16 | 英屬開曼群島商百濟神州有限公司 | 抗pd-1抗體或其抗原結合片段在製備治療用於患有肝細胞癌(hcc)之藥物的用途 |
| CN110997677A (zh) | 2017-08-12 | 2020-04-10 | 百济神州有限公司 | 具有改进的双重选择性的Btk抑制剂 |
| CN115028640A (zh) | 2017-08-25 | 2022-09-09 | 吉利德科学公司 | Syk抑制剂的多晶型物 |
| WO2019108795A1 (en) | 2017-11-29 | 2019-06-06 | Beigene Switzerland Gmbh | Treatment of indolent or aggressive b-cell lymphomas using a combination comprising btk inhibitors |
| KR20210131372A (ko) | 2019-02-22 | 2021-11-02 | 크로노스 바이오, 인코포레이티드 | Syk 억제제로서의 축합된 피라진의 고체 형태 |
| WO2020249001A1 (zh) | 2019-06-10 | 2020-12-17 | 百济神州瑞士有限责任公司 | 一种含有布鲁顿氏酪氨酸激酶抑制剂的口服固体片剂及其制备方法 |
| US11786531B1 (en) | 2022-06-08 | 2023-10-17 | Beigene Switzerland Gmbh | Methods of treating B-cell proliferative disorder |
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| CA2323771A1 (en) * | 1998-03-14 | 1999-09-23 | Byk Gulden Lomberg Chemische Fabrik Gmbh | Phthalazinone pde iii/iv inhibitors |
| BR0113930A (pt) * | 2000-09-15 | 2003-06-24 | Anormed Inc | Compostos heterocìclicos de ligação aos receptores de quimiocina |
| DE602004005881T2 (de) * | 2003-10-14 | 2008-01-17 | Pharmacia Corp. | Substituierte pyrazinonverbindungen zur behandlung von entzündungen |
| CA2601628C (en) * | 2005-03-10 | 2014-05-13 | Cgi Pharmaceuticals, Inc. | Certain substituted amides, method of making, and method of use thereof |
| WO2006124731A2 (en) | 2005-05-12 | 2006-11-23 | Irm Llc | Compounds and compositions as protein kinase inhibitors |
| EP2099797B1 (en) | 2005-08-09 | 2010-09-29 | Irm Llc | Compounds and compositions as protein kinase inhibitors |
| WO2007027594A1 (en) | 2005-08-29 | 2007-03-08 | Vertex Pharmaceuticals Incorporated | 3,5-disubstituted pyrid-2-ones useful as inhibitors of tec family of non-receptor tyrosine kinases |
| AU2006285145A1 (en) | 2005-08-29 | 2007-03-08 | Vertex Pharmaceuticals Incorporated | 3,5-disubstituted pyrid-2-ones useful as inhibitors of Tec family of non-.receptor tyrosine kinases |
| ATE528302T1 (de) | 2005-08-29 | 2011-10-15 | Vertex Pharma | 3,5-disubstituierte pyrid-2-one, die als hemmer der tec-familie von nicht-rezeptor tyrosin- kinasen nützlich sind |
| CN101300253B (zh) * | 2005-09-09 | 2012-08-22 | 沃泰克斯药物股份有限公司 | 作为电压门控离子通道调控剂的二环衍生物 |
| CA2645583A1 (en) * | 2006-03-20 | 2007-09-27 | F. Hoffman-La Roche Ag | Methods of inhibiting btk and syk protein kinases |
| EP2018167A4 (en) | 2006-05-15 | 2010-07-14 | Irm Llc | COMPOSITIONS AND METHODS AS INHIBITORS OF FGF RECEPTOR KINASES |
| AR063707A1 (es) | 2006-09-11 | 2009-02-11 | Cgi Pharmaceuticals Inc | Determinadas amidas sustituidas, el uso de las mismas para el tratamiento de enfermedades mediadas por la inhibicion de la actividad de btk y composiciones farmacéuticas que las comprenden. |
| US7838523B2 (en) | 2006-09-11 | 2010-11-23 | Cgi Pharmaceuticals, Inc. | Certain substituted amides, method of making, and method of use thereof |
| EP2068849A2 (en) * | 2006-09-11 | 2009-06-17 | CGI Pharmaceuticals, Inc. | Kinase inhibitors, and methods of using and identifying kinase inhibitors |
| AR063706A1 (es) * | 2006-09-11 | 2009-02-11 | Cgi Pharmaceuticals Inc | Determinadas amidas sustituidas, el uso de las mismas para el tratamiento de enfermedades mediadas por la inhibicion de la actividad de btk y composiciones farmaceuticas que las comprenden. |
| CL2008002793A1 (es) | 2007-09-20 | 2009-09-04 | Cgi Pharmaceuticals Inc | Compuestos derivados de amidas sustituidas, inhibidores de la actividad de btk; composicion farmaceutica que los comprende; utiles en el tratamiento del cancer, trastornos oseos, enfermedades autoinmunes, entre otras |
| CA2701275C (en) | 2007-10-23 | 2016-06-21 | F. Hoffmann-La Roche Ag | Kinase inhibitors |
| NZ601700A (en) * | 2008-06-24 | 2013-02-22 | Hoffmann La Roche | 5-phenyl-1H-pyridin-2-one and 6-phenyl-2H-pyridazin-3-one derivatives as inhibitors of Bruton's Tyrosine Kinase (Btk) |
| JP5635535B2 (ja) * | 2009-01-08 | 2014-12-03 | レスバーロジックス コーポレイション | 心血管疾患の予防および治療のための化合物 |
| US8299077B2 (en) * | 2009-03-02 | 2012-10-30 | Roche Palo Alto Llc | Inhibitors of Bruton's tyrosine kinase |
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