JP2019531320A5 - - Google Patents
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- JP2019531320A5 JP2019531320A5 JP2019520691A JP2019520691A JP2019531320A5 JP 2019531320 A5 JP2019531320 A5 JP 2019531320A5 JP 2019520691 A JP2019520691 A JP 2019520691A JP 2019520691 A JP2019520691 A JP 2019520691A JP 2019531320 A5 JP2019531320 A5 JP 2019531320A5
- Authority
- JP
- Japan
- Prior art keywords
- fluoroallyloxy
- aminomethyl
- group
- pharmaceutical composition
- fibrosis
- 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.)
- Pending
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- 125000004202 aminomethyl group Chemical group [H]N([H])C([H])([H])* 0.000 claims 14
- 239000008194 pharmaceutical composition Substances 0.000 claims 9
- 208000008338 non-alcoholic fatty liver disease Diseases 0.000 claims 7
- 102100027159 Membrane primary amine oxidase Human genes 0.000 claims 6
- 101710132836 Membrane primary amine oxidase Proteins 0.000 claims 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 6
- 229910052739 hydrogen Inorganic materials 0.000 claims 5
- 239000001257 hydrogen Substances 0.000 claims 5
- 206010012601 diabetes mellitus Diseases 0.000 claims 4
- 208000019425 cirrhosis of liver Diseases 0.000 claims 3
- 201000010099 disease Diseases 0.000 claims 3
- 208000010706 fatty liver disease Diseases 0.000 claims 3
- 150000002431 hydrogen Chemical class 0.000 claims 3
- 239000003112 inhibitor Substances 0.000 claims 3
- 208000030159 metabolic disease Diseases 0.000 claims 3
- 206010053219 non-alcoholic steatohepatitis Diseases 0.000 claims 3
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 2
- KXDAEFPNCMNJSK-UHFFFAOYSA-N Benzamide Chemical compound NC(=O)C1=CC=CC=C1 KXDAEFPNCMNJSK-UHFFFAOYSA-N 0.000 claims 2
- 208000004930 Fatty Liver Diseases 0.000 claims 2
- 206010016654 Fibrosis Diseases 0.000 claims 2
- 206010018429 Glucose tolerance impaired Diseases 0.000 claims 2
- 206010019708 Hepatic steatosis Diseases 0.000 claims 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- 208000008589 Obesity Diseases 0.000 claims 2
- 206010033307 Overweight Diseases 0.000 claims 2
- 229940123518 Sodium/glucose cotransporter 2 inhibitor Drugs 0.000 claims 2
- 230000001476 alcoholic effect Effects 0.000 claims 2
- 125000000217 alkyl group Chemical group 0.000 claims 2
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 2
- 150000001875 compounds Chemical class 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- 208000027866 inflammatory disease Diseases 0.000 claims 2
- 235000020824 obesity Nutrition 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 239000001301 oxygen Substances 0.000 claims 2
- 125000000843 phenylene group Chemical group C1(=C(C=CC=C1)*)* 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 231100000240 steatosis hepatitis Toxicity 0.000 claims 2
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 2
- 208000004476 Acute Coronary Syndrome Diseases 0.000 claims 1
- 208000007082 Alcoholic Fatty Liver Diseases 0.000 claims 1
- 206010002388 Angina unstable Diseases 0.000 claims 1
- 208000031104 Arterial Occlusive disease Diseases 0.000 claims 1
- 206010003210 Arteriosclerosis Diseases 0.000 claims 1
- KHBQMWCZKVMBLN-UHFFFAOYSA-N Benzenesulfonamide Chemical compound NS(=O)(=O)C1=CC=CC=C1 KHBQMWCZKVMBLN-UHFFFAOYSA-N 0.000 claims 1
- 208000031229 Cardiomyopathies Diseases 0.000 claims 1
- 208000002177 Cataract Diseases 0.000 claims 1
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 1
- 201000003883 Cystic fibrosis Diseases 0.000 claims 1
- JVHXJTBJCFBINQ-ADAARDCZSA-N Dapagliflozin Chemical compound C1=CC(OCC)=CC=C1CC1=CC([C@H]2[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)O2)O)=CC=C1Cl JVHXJTBJCFBINQ-ADAARDCZSA-N 0.000 claims 1
- 208000007342 Diabetic Nephropathies Diseases 0.000 claims 1
- 208000032131 Diabetic Neuropathies Diseases 0.000 claims 1
- 206010012689 Diabetic retinopathy Diseases 0.000 claims 1
- 206010056340 Diabetic ulcer Diseases 0.000 claims 1
- 206010016262 Fatty liver alcoholic Diseases 0.000 claims 1
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 1
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 claims 1
- 206010019280 Heart failures Diseases 0.000 claims 1
- 201000009794 Idiopathic Pulmonary Fibrosis Diseases 0.000 claims 1
- 206010022489 Insulin Resistance Diseases 0.000 claims 1
- 208000029523 Interstitial Lung disease Diseases 0.000 claims 1
- WHSOLWOTCHFFBK-ZQGJOIPISA-N Luseogliflozin Chemical compound C1=CC(OCC)=CC=C1CC1=CC([C@H]2[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)S2)O)=C(OC)C=C1C WHSOLWOTCHFFBK-ZQGJOIPISA-N 0.000 claims 1
- 206010054805 Macroangiopathy Diseases 0.000 claims 1
- 208000001145 Metabolic Syndrome Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 208000002193 Pain Diseases 0.000 claims 1
- 208000001280 Prediabetic State Diseases 0.000 claims 1
- 208000032056 Radiation Fibrosis Syndrome Diseases 0.000 claims 1
- 206010067953 Radiation fibrosis Diseases 0.000 claims 1
- GSINGUMRKGRYJP-VZWAGXQNSA-N Remogliflozin Chemical compound C1=CC(OC(C)C)=CC=C1CC1=C(C)N(C(C)C)N=C1O[C@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 GSINGUMRKGRYJP-VZWAGXQNSA-N 0.000 claims 1
- 229910005965 SO 2 Inorganic materials 0.000 claims 1
- 208000034189 Sclerosis Diseases 0.000 claims 1
- 208000007718 Stable Angina Diseases 0.000 claims 1
- 208000006011 Stroke Diseases 0.000 claims 1
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 1
- ZXOCGDDVNPDRIW-NHFZGCSJSA-N Tofogliflozin Chemical compound O.C1=CC(CC)=CC=C1CC1=CC=C(CO[C@@]23[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)O3)O)C2=C1 ZXOCGDDVNPDRIW-NHFZGCSJSA-N 0.000 claims 1
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 1
- 208000007814 Unstable Angina Diseases 0.000 claims 1
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 claims 1
- 208000026594 alcoholic fatty liver disease Diseases 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 230000033115 angiogenesis Effects 0.000 claims 1
- 208000021328 arterial occlusion Diseases 0.000 claims 1
- 208000011775 arteriosclerosis disease Diseases 0.000 claims 1
- -1 athigliflozin Chemical compound 0.000 claims 1
- 239000008280 blood Substances 0.000 claims 1
- 210000004369 blood Anatomy 0.000 claims 1
- 229960001713 canagliflozin Drugs 0.000 claims 1
- VHOFTEAWFCUTOS-TUGBYPPCSA-N canagliflozin hydrate Chemical compound O.CC1=CC=C([C@H]2[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)O2)O)C=C1CC(S1)=CC=C1C1=CC=C(F)C=C1.CC1=CC=C([C@H]2[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)O2)O)C=C1CC(S1)=CC=C1C1=CC=C(F)C=C1 VHOFTEAWFCUTOS-TUGBYPPCSA-N 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 230000000747 cardiac effect Effects 0.000 claims 1
- 239000000460 chlorine Substances 0.000 claims 1
- 229910052801 chlorine Inorganic materials 0.000 claims 1
- 230000007882 cirrhosis Effects 0.000 claims 1
- 229960003834 dapagliflozin Drugs 0.000 claims 1
- 208000033679 diabetic kidney disease Diseases 0.000 claims 1
- 208000016097 disease of metabolism Diseases 0.000 claims 1
- 230000002526 effect on cardiovascular system Effects 0.000 claims 1
- 229960003345 empagliflozin Drugs 0.000 claims 1
- OBWASQILIWPZMG-QZMOQZSNSA-N empagliflozin Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@H]1C1=CC=C(Cl)C(CC=2C=CC(O[C@@H]3COCC3)=CC=2)=C1 OBWASQILIWPZMG-QZMOQZSNSA-N 0.000 claims 1
- 208000030533 eye disease Diseases 0.000 claims 1
- 230000004761 fibrosis Effects 0.000 claims 1
- 230000003176 fibrotic effect Effects 0.000 claims 1
- 229910052731 fluorine Inorganic materials 0.000 claims 1
- 239000011737 fluorine Substances 0.000 claims 1
- 206010061989 glomerulosclerosis Diseases 0.000 claims 1
- 239000008103 glucose Substances 0.000 claims 1
- 230000002641 glycemic effect Effects 0.000 claims 1
- 125000001188 haloalkyl group Chemical group 0.000 claims 1
- 125000001475 halogen functional group Chemical group 0.000 claims 1
- 208000006454 hepatitis Diseases 0.000 claims 1
- 231100000283 hepatitis Toxicity 0.000 claims 1
- 201000001421 hyperglycemia Diseases 0.000 claims 1
- 201000004332 intermediate coronary syndrome Diseases 0.000 claims 1
- 208000036971 interstitial lung disease 2 Diseases 0.000 claims 1
- 229950000991 ipragliflozin Drugs 0.000 claims 1
- AHFWIQIYAXSLBA-RQXATKFSSA-N ipragliflozin Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@H]1C1=CC=C(F)C(CC=2SC3=CC=CC=C3C=2)=C1 AHFWIQIYAXSLBA-RQXATKFSSA-N 0.000 claims 1
- 208000028867 ischemia Diseases 0.000 claims 1
- 229950004397 luseogliflozin Drugs 0.000 claims 1
- 206010062198 microangiopathy Diseases 0.000 claims 1
- 208000010125 myocardial infarction Diseases 0.000 claims 1
- 230000000926 neurological effect Effects 0.000 claims 1
- 230000002093 peripheral effect Effects 0.000 claims 1
- 201000009104 prediabetes syndrome Diseases 0.000 claims 1
- 229940126844 remogliflozin Drugs 0.000 claims 1
- 201000002793 renal fibrosis Diseases 0.000 claims 1
- 208000037803 restenosis Diseases 0.000 claims 1
- 230000033764 rhythmic process Effects 0.000 claims 1
- 125000005649 substituted arylene group Chemical group 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- 239000011593 sulfur Substances 0.000 claims 1
- 229950006667 tofogliflozin Drugs 0.000 claims 1
- 231100000331 toxic Toxicity 0.000 claims 1
- 230000002588 toxic effect Effects 0.000 claims 1
- 230000002792 vascular Effects 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP16194572 | 2016-10-19 | ||
| EP16194572.0 | 2016-10-19 | ||
| PCT/EP2017/076300 WO2018073154A1 (en) | 2016-10-19 | 2017-10-16 | Combinations comprising an ssao/vap-1 inhibitor and a sglt2 inhibitor, uses thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2019531320A JP2019531320A (ja) | 2019-10-31 |
| JP2019531320A5 true JP2019531320A5 (cg-RX-API-DMAC7.html) | 2020-11-26 |
Family
ID=57178303
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019520691A Pending JP2019531320A (ja) | 2016-10-19 | 2017-10-16 | Ｓｓａｏ／ｖａｐ−１阻害剤とｓｇｌｔ２阻害剤とを含む組合せ、その使用 |
Country Status (14)
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20190110736A (ko) | 2018-03-21 | 2019-10-01 | 주식회사유한양행 | 신규의 트라이아졸론 유도체 또는 이의 염 및 이를 포함하는 약학 조성물 |
| KR20190110740A (ko) | 2018-03-21 | 2019-10-01 | 주식회사유한양행 | 신규의 아릴 또는 헤테로아릴 트라이아졸론 유도체 또는 이의 염 및 이를 포함하는 약학 조성물 |
| AU2019351122A1 (en) * | 2018-09-28 | 2021-05-20 | Acucela Inc. | Inhibitors of VAP-1 |
| AU2019351124A1 (en) | 2018-09-28 | 2021-05-20 | Acucela Inc. | Inhibitors of VAP-1 |
| JP7414230B2 (ja) * | 2018-11-09 | 2024-01-16 | 国立大学法人 琉球大学 | 抗血液悪性腫瘍薬 |
| CN121081472A (zh) | 2018-12-13 | 2025-12-09 | 拓臻股份有限公司 | 一种THRβ受体激动剂化合物及其制备方法和用途 |
| TW202039486A (zh) | 2018-12-14 | 2020-11-01 | 南韓商柳韓洋行股份有限公司 | 三唑并吡啶-3-酮化物或其鹽及包含彼之醫藥組合物 |
| TWI835945B (zh) | 2018-12-14 | 2024-03-21 | 南韓商柳韓洋行股份有限公司 | 3,3-二氟烯丙胺化物或其鹽及包含彼的醫藥組合物 |
| WO2021050945A1 (en) | 2019-09-12 | 2021-03-18 | Terns, Inc. | Thyroid hormone receptor beta agonist compounds |
| AU2020377093A1 (en) | 2019-10-29 | 2022-05-12 | Eccogene Inc. | SSAO inhibitors and use thereof |
| US20230127498A1 (en) * | 2020-03-25 | 2023-04-27 | Terns, Inc. | Treatment of respiratory disorders |
| CA3183414A1 (en) * | 2020-05-13 | 2021-11-18 | Terns Pharmaceuticals, Inc. | Combination treatment of liver disorders |
| CN113893256A (zh) * | 2020-07-06 | 2022-01-07 | 诺未科技（北京）有限公司 | 化合物或其可药用盐、二聚体或三聚体在制备治疗癌症的药物中的应用 |
| KR20230058112A (ko) | 2020-08-25 | 2023-05-02 | 일라이 릴리 앤드 캄파니 | Ssao 억제제의 다형체 |
| US20240148767A1 (en) * | 2021-03-04 | 2024-05-09 | The Governors Of The University Of Alberta | The use of empagliflozin for the treatment of ulcerative colitis and crohn's disease |
| CN119013027A (zh) * | 2021-11-11 | 2024-11-22 | 拓臻制药公司 | 用于治疗肝脏病症的SSAO抑制剂和THR-β激动剂的组合 |
| JP2024543419A (ja) * | 2021-11-11 | 2024-11-21 | ターンズ・ファーマシューティカルズ・インコーポレイテッド | Ｓｓａｏ阻害剤による肝障害の治療 |
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| NZ517439A (en) | 1999-08-31 | 2003-03-28 | Kissei Pharmaceutical | Glucopyranosyloxypyrazole derivatives, medicinal compositions containing the same and intermediates in the production thereof |
| PH12000002657B1 (en) | 1999-10-12 | 2006-02-21 | Bristol Myers Squibb Co | C-aryl glucoside SGLT2 inhibitors |
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| WO2002044192A1 (en) | 2000-11-30 | 2002-06-06 | Kissei Pharmaceutical Co., Ltd. | Glucopyranosyloxybenzyl benzene derivatives, medicinal compositions containing the same and intermediates in the production thereof |
| DK1354888T3 (da) | 2000-12-28 | 2009-09-21 | Kissei Pharmaceutical | Glukopyranosyloxypyrazolderivater og anvendelse deraf i medikamenter |
| JP4490109B2 (ja) | 2002-03-22 | 2010-06-23 | キッセイ薬品工業株式会社 | グルコピラノシルオキシベンジルベンゼン誘導体の結晶 |
| DE10231370B4 (de) | 2002-07-11 | 2006-04-06 | Sanofi-Aventis Deutschland Gmbh | Thiophenglycosidderivate, diese Verbindungen enthaltende Arzneimittel und Verfahren zur Herstellung dieser Arzneimittel |
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| ES2649737T5 (es) | 2003-08-01 | 2021-07-07 | Mitsubishi Tanabe Pharma Corp | Compuestos novedosos que tienen actividad inhibidora frente a transportador de glucosa dependiente de sodio |
| CN103435581B (zh) | 2004-03-16 | 2015-08-19 | 贝林格尔.英格海姆国际有限公司 | 吡喃葡萄糖基取代的苯基衍生物、含该化合物的药物、其用途及其制造方法 |
| TW200637839A (en) | 2005-01-07 | 2006-11-01 | Taisho Pharmaceutical Co Ltd | 1-thio-d-glucitol derivatives |
| TW200637869A (en) | 2005-01-28 | 2006-11-01 | Chugai Pharmaceutical Co Ltd | The spiroketal derivatives and the use as therapeutical agent for diabetes of the same |
| UA91546C2 (uk) | 2005-05-03 | 2010-08-10 | Бьорінгер Інгельхайм Інтернаціональ Гмбх | КРИСТАЛІЧНА ФОРМА 1-ХЛОР-4-(β-D-ГЛЮКОПІРАНОЗ-1-ИЛ)-2-[4-((S)-ТЕТРАГІДРОФУРАН-3-ІЛОКСИ)-БЕНЗИЛ]-БЕНЗОЛУ, СПОСІБ ЇЇ ОДЕРЖАННЯ ТА ЇЇ ЗАСТОСУВАННЯ ПРИ ПРИГОТУВАННІ ЛІКАРСЬКИХ ЗАСОБІВ |
| US7772191B2 (en) | 2005-05-10 | 2010-08-10 | Boehringer Ingelheim International Gmbh | Processes for preparing of glucopyranosyl-substituted benzyl-benzene derivatives and intermediates therein |
| ATE517099T1 (de) | 2006-02-15 | 2011-08-15 | Boehringer Ingelheim Int | Glucopyranosyl-substituierte benzonitril-derivate,pharmazeutische zusammensetzungen mit derartigen verbindungen, ihre verwendung und herstellungsverfahren dafür |
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| PL2200606T3 (pl) | 2007-09-10 | 2018-08-31 | Janssen Pharmaceutica, N.V. | Sposób wytwarzania związków użytecznych jako inhibitory SGLT2 |
| CN101917845A (zh) | 2007-11-21 | 2010-12-15 | 法马克西斯制药公司 | Ssao/vap-1的卤代烯丙胺抑制剂及其用途 |
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| TWI472521B (zh) | 2008-07-17 | 2015-02-11 | Lexicon Pharmaceuticals Inc | （２ｓ，３ｒ，４ｒ，５ｓ，６ｒ）－２－（４－氯－３－（４－乙氧苄基）苯基）－６－（甲硫）四氫－２ｈ－哌喃－３，４，５－三醇的固體形態與其使用方法 |
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| US20110014284A1 (en) | 2009-02-13 | 2011-01-20 | Boehringer Ingelheim International Gmbh | Pharmaceutical composition, pharmaceutical dosage form, process for their preparation, methods for treating and uses thereof |
| RS53761B1 (sr) | 2009-04-16 | 2015-06-30 | Taisho Pharmaceutical Co. Ltd. | Farmaceutski preparati sa (1s)-1,5-anhidro-1-[5-(4-etoksibenzil)-2-metoksi-4-metilfenil]-1-tio-d-glucitolom i sekretagogom insulina |
| DK2486029T3 (en) | 2009-09-30 | 2015-08-24 | Boehringer Ingelheim Int | Methods of making of glucopyranosyl-substituted benzyl-benzene derivatives. |
| CA2775961C (en) | 2009-09-30 | 2017-11-07 | Boehringer Ingelheim International Gmbh | Method for the preparation of a crystalline form of 1-chloro-4-(beta-d-glucopyranos-1-yl)-2-(4-((s)-tetrahydrofuran-3-yloxy)benzyl)benzene |
| MX377635B (es) * | 2012-05-02 | 2025-03-11 | Boehringer Ingelheim Int | Inhibidores de 3-haloalilamina sustituidos de ssao y uso de los mismos |
-
2017
- 2017-10-16 MX MX2019004549A patent/MX2019004549A/es unknown
- 2017-10-16 US US16/341,460 patent/US20210212968A1/en not_active Abandoned
- 2017-10-16 AU AU2017344882A patent/AU2017344882A1/en not_active Abandoned
- 2017-10-16 CN CN201780063937.5A patent/CN109843279A/zh active Pending
- 2017-10-16 EP EP17804068.9A patent/EP3528800A1/en not_active Withdrawn
- 2017-10-16 KR KR1020197014347A patent/KR20190070956A/ko not_active Withdrawn
- 2017-10-16 CA CA3041169A patent/CA3041169A1/en not_active Abandoned
- 2017-10-16 WO PCT/EP2017/076300 patent/WO2018073154A1/en not_active Ceased
- 2017-10-16 BR BR112019005930A patent/BR112019005930A2/pt not_active IP Right Cessation
- 2017-10-16 JP JP2019520691A patent/JP2019531320A/ja active Pending
- 2017-10-16 EA EA201990951A patent/EA201990951A1/ru unknown
-
2019
- 2019-04-08 CL CL2019000935A patent/CL2019000935A1/es unknown
- 2019-04-11 IL IL265989A patent/IL265989A/en unknown
- 2019-04-17 PH PH12019500845A patent/PH12019500845A1/en unknown