AR096758A1 - Inhibidores cristalinos de bromodominios - Google Patents
Inhibidores cristalinos de bromodominiosInfo
- Publication number
- AR096758A1 AR096758A1 ARP140102431A ARP140102431A AR096758A1 AR 096758 A1 AR096758 A1 AR 096758A1 AR P140102431 A ARP140102431 A AR P140102431A AR P140102431 A ARP140102431 A AR P140102431A AR 096758 A1 AR096758 A1 AR 096758A1
- Authority
- AR
- Argentina
- Prior art keywords
- bromodominium
- ethanesulfonamide
- difluorophenoxy
- pyrrole
- dihydro
- Prior art date
Links
- 239000013078 crystal Substances 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- -1 2,4-Difluorophenoxy Chemical group 0.000 abstract 3
- ZCRZCMUDOWDGOB-UHFFFAOYSA-N ethanesulfonimidic acid Chemical compound CCS(N)(=O)=O ZCRZCMUDOWDGOB-UHFFFAOYSA-N 0.000 abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- 125000000339 4-pyridyl group Chemical group N1=C([H])C([H])=C([*])C([H])=C1[H] 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 239000004615 ingredient Substances 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 238000000634 powder X-ray diffraction Methods 0.000 abstract 1
Classifications
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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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- 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
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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
- 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
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
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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
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
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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
- A61P11/08—Bronchodilators
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A61P13/12—Drugs for disorders of the urinary system of the kidneys
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/16—Masculine contraceptives
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A—HUMAN NECESSITIES
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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
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- 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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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
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- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
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- 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
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
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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
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
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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
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- 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
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- A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
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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
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
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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
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Endocrinology (AREA)
- Oncology (AREA)
- Immunology (AREA)
- Diabetes (AREA)
- Virology (AREA)
- Cardiology (AREA)
- Pulmonology (AREA)
- Urology & Nephrology (AREA)
- Communicable Diseases (AREA)
- Physical Education & Sports Medicine (AREA)
- Hematology (AREA)
- Reproductive Health (AREA)
- Heart & Thoracic Surgery (AREA)
- Rheumatology (AREA)
- Epidemiology (AREA)
- Tropical Medicine & Parasitology (AREA)
- Obesity (AREA)
- AIDS & HIV (AREA)
- Pain & Pain Management (AREA)
- Molecular Biology (AREA)
- Dermatology (AREA)
- Gastroenterology & Hepatology (AREA)
- Emergency Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Transplantation (AREA)
Abstract
N-[4-(2,4-difluorofenoxi)-3-(6-metil-7-oxo-6,7-dihidro-1H-pirrol[2,3-c]piridin-4-il)fenil]etansulfonamida y formas cristalinas de la misma como ingrediente farmacéutico adecuado para composiciones farmacéuticas de utilidad en el tratamiento de enfermedades, por ejemplo, cáncer. Reivindicación 2: Una forma cristalina aislada de N-[4-(2,4-difluorofenoxi)-3-(6-metil-7-oxo-6,7-dihidro-1H-pirrol[2,3-c]piridin-4-il)fenil]etansulfonamida, caracterizada porque la forma cristalina tiene un patrón de difracción de rayos X en polvo que comprende los siguientes valores pico 2q ± 0,2: 6,2º, 9,0º, 11,0º, 12,3º, 12,6º, 13,1º, 14,1º, 15,6º, 16,4º, 16,5º, 16,9º, 17,8º, 18,1º, 18,3º, 18,9º, 20,4º, 21,1º, 21,6º, 21,8º, 22,1º, 22,9º, 23,2º, 24,4º, 24,7º, 25,6º, 26,3º, 27,0º y 27,3º.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361840777P | 2013-06-28 | 2013-06-28 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR096758A1 true AR096758A1 (es) | 2016-02-03 |
Family
ID=51261220
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP140102431A AR096758A1 (es) | 2013-06-28 | 2014-06-26 | Inhibidores cristalinos de bromodominios |
Country Status (33)
| Country | Link |
|---|---|
| US (3) | US9321765B2 (es) |
| EP (1) | EP3013826B1 (es) |
| JP (1) | JP6423425B2 (es) |
| KR (1) | KR102323829B1 (es) |
| CN (1) | CN105473586B (es) |
| AR (1) | AR096758A1 (es) |
| AU (2) | AU2014302252B2 (es) |
| BR (1) | BR112015032736A2 (es) |
| CA (1) | CA2916221C (es) |
| CL (1) | CL2015003722A1 (es) |
| CR (1) | CR20160036A (es) |
| CY (1) | CY1119066T1 (es) |
| DK (1) | DK3013826T3 (es) |
| DO (1) | DOP2015000304A (es) |
| ES (1) | ES2636939T3 (es) |
| HR (1) | HRP20171154T1 (es) |
| IL (1) | IL243202B (es) |
| LT (1) | LT3013826T (es) |
| ME (1) | ME02801B (es) |
| MX (1) | MX360065B (es) |
| NZ (1) | NZ631112A (es) |
| PE (1) | PE20160287A1 (es) |
| PH (1) | PH12015502792A1 (es) |
| PL (1) | PL3013826T3 (es) |
| PT (1) | PT3013826T (es) |
| RS (1) | RS56318B1 (es) |
| RU (1) | RU2675268C2 (es) |
| SG (1) | SG11201510692TA (es) |
| SI (1) | SI3013826T1 (es) |
| SM (1) | SMT201700363T1 (es) |
| TW (1) | TWI639594B (es) |
| UY (1) | UY35632A (es) |
| WO (1) | WO2014210425A1 (es) |
Families Citing this family (32)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2013365926B9 (en) | 2012-12-21 | 2019-01-17 | Zenith Epigenetics Ltd. | Novel heterocyclic compounds as bromodomain inhibitors |
| TWI719464B (zh) | 2013-03-15 | 2021-02-21 | 美商英塞特控股公司 | 作為bet蛋白抑制劑之三環雜環 |
| ES2661437T3 (es) | 2013-06-21 | 2018-04-02 | Zenith Epigenetics Corp. | Nuevos compuestos bicíclicos sustituidos como inhibidores de bromodominio |
| SI3010503T1 (sl) | 2013-06-21 | 2020-07-31 | Zenith Epigenetics Ltd. | Novi biciklični inhibitorji bromodomene |
| JP2016523964A (ja) | 2013-07-08 | 2016-08-12 | インサイト・ホールディングス・コーポレイションIncyte Holdings Corporation | Betタンパク質阻害剤としての三環式複素環 |
| CN105593224B (zh) | 2013-07-31 | 2021-05-25 | 恒元生物医药科技(苏州)有限公司 | 作为溴结构域抑制剂的新型喹唑啉酮类化合物 |
| PE20161065A1 (es) | 2013-10-18 | 2016-11-19 | Celgene Quanticel Res Inc | Inhibidores de bromodominio |
| WO2015081203A1 (en) | 2013-11-26 | 2015-06-04 | Incyte Corporation | Bicyclic heterocycles as bet protein inhibitors |
| WO2015081189A1 (en) | 2013-11-26 | 2015-06-04 | Incyte Corporation | Bicyclic heterocycles as bet protein inhibitors |
| US9309246B2 (en) | 2013-12-19 | 2016-04-12 | Incyte Corporation | Tricyclic heterocycles as BET protein inhibitors |
| KR20240134245A (ko) | 2014-04-23 | 2024-09-06 | 인사이트 홀딩스 코포레이션 | BET 단백질의 저해제로서의 1H-피롤로[2,3-c]피리딘-7(6H)-온 및 피라졸로[3,4-c]피리딘-7(6H)-온 |
| US9527864B2 (en) | 2014-09-15 | 2016-12-27 | Incyte Corporation | Tricyclic heterocycles as BET protein inhibitors |
| EP3227280B1 (en) | 2014-12-01 | 2019-04-24 | Zenith Epigenetics Ltd. | Substituted pyridines as bromodomain inhibitors |
| US10710992B2 (en) | 2014-12-01 | 2020-07-14 | Zenith Epigenetics Ltd. | Substituted pyridinones as bromodomain inhibitors |
| US10292968B2 (en) | 2014-12-11 | 2019-05-21 | Zenith Epigenetics Ltd. | Substituted heterocycles as bromodomain inhibitors |
| CA2966450A1 (en) | 2014-12-17 | 2016-06-23 | Olesya KHARENKO | Inhibitors of bromodomains |
| US20180200261A1 (en) * | 2015-07-20 | 2018-07-19 | Mayo Foundation For Medical Education And Research | Methods and materials for treating cancer |
| US20170121347A1 (en) | 2015-10-29 | 2017-05-04 | Incyte Corporation | Amorphous solid form of a bet protein inhibitor |
| WO2017177955A1 (en) | 2016-04-15 | 2017-10-19 | Abbvie Inc. | Bromodomain inhibitors |
| EP4234554A3 (en) | 2016-06-20 | 2023-12-27 | Incyte Corporation | Crystalline solid forms of a bet inhibitor |
| WO2018106988A1 (en) * | 2016-12-09 | 2018-06-14 | Smet Pharmaceutical Inc. | Biologically active compositions containing two different classes of chemical compounds for treating solid tumors |
| CN109384784B (zh) * | 2017-08-10 | 2021-01-12 | 浙江海正药业股份有限公司 | 磺酰胺类衍生物、其制备方法及其在医药上的用途 |
| WO2019222331A1 (en) | 2018-05-15 | 2019-11-21 | Abbvie Inc. | Treating solid tumors with bromodomain inhibitors |
| US11633399B2 (en) | 2018-12-25 | 2023-04-25 | Sol-Gel Technologies Ltd. | Treatment of skin disorders with compositions comprising an EGFR inhibitor |
| WO2020232214A1 (en) | 2019-05-14 | 2020-11-19 | Abbvie Inc. | Treating acute myeloid leukemia (aml) with mivebresib, a bromodomain inhibitor |
| TW202132303A (zh) * | 2019-11-13 | 2021-09-01 | 美商瑞佩特治療公司 | C-c趨化介素受體第四型拮抗劑之晶形及其用途 |
| CN110964691B (zh) * | 2019-12-31 | 2020-10-30 | 深圳新赛尔生物科技有限公司 | 子宫内膜干细胞的定向成脂分化培养 |
| US20240101551A1 (en) * | 2020-01-19 | 2024-03-28 | Chia Tai Tianqing Pharmaceutical Group Co., Ltd. | Crystal form and salt form of bromine domain protein inhibitor and preparation method therefor |
| US11833155B2 (en) | 2020-06-03 | 2023-12-05 | Incyte Corporation | Combination therapy for treatment of myeloproliferative neoplasms |
| US11746932B2 (en) | 2020-07-02 | 2023-09-05 | Hempvana, Llc | Expandable and retractable hose reinforced with hemp |
| CN117337293A (zh) * | 2020-12-22 | 2024-01-02 | 弗埃塞股份有限公司 | 固体形式的eif4e抑制剂 |
| US11583602B2 (en) | 2021-06-23 | 2023-02-21 | Kimtron, Inc. | System and method for ultra-close proximity irradiation of rotating biomass |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6271380B1 (en) * | 1998-12-30 | 2001-08-07 | Dupont Pharmaceuticals Company | 1H-imidazo[4,5-d]pyridazin-7-ones, 3H-imidazo-[4,5-c]pyridin-4-ones and corresponding thiones as corticotropin releasing factor (CRF) receptor ligands |
| CN100348599C (zh) * | 2002-06-06 | 2007-11-14 | 卫材R&D管理有限公司 | 新的稠合咪唑衍生物 |
| TWI339206B (en) * | 2003-09-04 | 2011-03-21 | Vertex Pharma | Compositions useful as inhibitors of protein kinases |
| GB0919434D0 (en) * | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
| ES2652304T3 (es) * | 2009-11-05 | 2018-02-01 | Glaxosmithkline Llc | Compuesto de benzodiacepina novedoso |
| HUE031073T2 (en) * | 2010-05-14 | 2017-06-28 | Dana Farber Cancer Inst Inc | Thieno triazolo-diazepine compounds for the treatment of neoplasia |
| CN103119160B (zh) | 2010-05-14 | 2016-06-01 | 达那-法伯癌症研究所 | 用于调节代谢的组合物和方法 |
| AT510136B1 (de) * | 2010-07-12 | 2016-11-15 | Primetals Technologies Austria GmbH | Verfahren zur herstellung von kohlepartikeln enthaltenden presslingen |
| WO2013097052A1 (en) * | 2011-12-30 | 2013-07-04 | Abbott Laboratories | Bromodomain inhibitors |
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2014
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