CA2990192A1 - Compositions and methods for inhibiting arginase activity - Google Patents
Compositions and methods for inhibiting arginase activity Download PDFInfo
- Publication number
- CA2990192A1 CA2990192A1 CA2990192A CA2990192A CA2990192A1 CA 2990192 A1 CA2990192 A1 CA 2990192A1 CA 2990192 A CA2990192 A CA 2990192A CA 2990192 A CA2990192 A CA 2990192A CA 2990192 A1 CA2990192 A1 CA 2990192A1
- Authority
- CA
- Canada
- Prior art keywords
- alkyl
- aryl
- cancer
- alkylene
- heterocycloalkyl
- 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.)
- Abandoned
Links
- 238000000034 method Methods 0.000 title claims abstract description 154
- 230000000694 effects Effects 0.000 title claims description 19
- 239000000203 mixture Substances 0.000 title description 54
- 102000004452 Arginase Human genes 0.000 title description 19
- 108700024123 Arginases Proteins 0.000 title description 19
- 230000002401 inhibitory effect Effects 0.000 title description 3
- 206010028980 Neoplasm Diseases 0.000 claims abstract description 172
- 239000004475 Arginine Substances 0.000 claims abstract description 164
- ODKSFYDXXFIFQN-UHFFFAOYSA-N arginine Natural products OC(=O)C(N)CCCNC(N)=N ODKSFYDXXFIFQN-UHFFFAOYSA-N 0.000 claims abstract description 164
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- 125000003118 aryl group Chemical group 0.000 claims description 160
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| WO2012058065A1 (en) | 2010-10-26 | 2012-05-03 | Mars Incorporated | Boronates as arginase inhibitors |
| CN107921051A (zh) | 2015-06-23 | 2018-04-17 | 卡里塞拉生物科学股份公司 | 抑制精氨酸酶活性的组合物和方法 |
| KR20220118559A (ko) | 2015-10-30 | 2022-08-25 | 칼리테라 바이오사이언시즈, 인코포레이티드 | 아르기닌 활성 억제용 조성물 및 방법 |
| PL417066A1 (pl) | 2016-05-04 | 2017-11-06 | Oncoarendi Therapeutics Spółka Z Ograniczoną Odpowiedzialnością | Inhibitory arginazy oraz ich zastosowania terapeutyczne |
| US11291674B2 (en) | 2016-11-08 | 2022-04-05 | Calithera Biosciences, Inc. | Arginase inhibitor combination therapies |
| AU2017382405B2 (en) | 2016-12-22 | 2021-12-16 | Calithera Biosciences, Inc. | Compositions and methods for inhibiting arginase activity |
| CN108794517B (zh) * | 2017-04-27 | 2021-03-30 | 南京谷睿生物科技有限公司 | 一种精氨酸酶抑制剂及其制备方法与用途 |
| CN110709383A (zh) | 2017-05-12 | 2020-01-17 | 卡里塞拉生物科学股份公司 | (3r,4s)-3-乙酰胺基-4-烯丙基-n-(叔丁基)吡咯烷-3-羧酰胺的制备方法 |
| WO2019000163A1 (zh) * | 2017-06-26 | 2019-01-03 | 余祖江 | 精氨酸在制备抗肿瘤药物中的用途 |
| CN111491937A (zh) * | 2017-12-22 | 2020-08-04 | 广东新契生物医药科技有限公司 | 作为精氨酸酶抑制剂的杂环化合物 |
| KR102657919B1 (ko) * | 2018-02-17 | 2024-04-15 | 아스트라제네카 아베 | 아르기나제 저해제 및 이의 사용 방법 |
| UA127897C2 (uk) * | 2018-03-05 | 2024-02-07 | Аркус Байосайєнсіз, Інк. | Інгібітори аргінази |
| US10851099B2 (en) | 2018-03-29 | 2020-12-01 | Oncoarendi Therapeutics S.A. | Dipeptide piperidine derivatives |
| CN111770756B (zh) * | 2018-04-27 | 2023-03-31 | 四川科伦博泰生物医药股份有限公司 | 非天然氨基酸类衍生物、包含其的药物组合物及其制备方法和用途 |
| EA202190532A1 (ru) * | 2018-08-22 | 2021-07-08 | Астразенека Аб | Ингибиторы аргиназы и способы их применения |
| TWI828800B (zh) * | 2018-11-16 | 2024-01-11 | 美商阿克思生物科學有限公司 | Arg1及/或arg2之抑制劑 |
| US20220017541A1 (en) * | 2018-11-21 | 2022-01-20 | Black Belt Tx Ltd | Inhibitors of arginase |
| WO2020160707A1 (en) * | 2019-02-06 | 2020-08-13 | Guangdong Newopp Biopharmaceuticals Co., Ltd. | Alkylboronic acids as arginase inhibitors |
| SG11202108503PA (en) * | 2019-02-08 | 2021-09-29 | Astrazeneca Ab | Arginase inhibitors and methods of use thereof |
| US10967020B2 (en) * | 2019-04-05 | 2021-04-06 | King Saud University | Method of synthesizing custard apple peel nanoparticles |
| CN112110944B (zh) * | 2019-06-21 | 2022-02-11 | 南京谷睿生物科技有限公司 | 一种化合物及其制备方法和应用 |
| AU2020319132B2 (en) * | 2019-07-23 | 2023-09-07 | Astrazeneca Ab | Arginase inhibitors and methods of use thereof |
| CN110734456A (zh) * | 2019-11-06 | 2020-01-31 | 南京谷睿生物科技有限公司 | 一种化合物及其制备方法和医药上的应用 |
| TW202228720A (zh) | 2020-12-22 | 2022-08-01 | 波蘭商昂科艾倫迪治療法股份公司 | 精胺酸酶抑制劑及其使用方法 |
| US20250099408A1 (en) | 2022-01-21 | 2025-03-27 | Sammy Oyoo OPIYO | Improved suramin methods and compositions |
Family Cites Families (28)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4172896A (en) | 1978-06-05 | 1979-10-30 | Dainippon Pharmaceutical Co., Ltd. | Methane-sulfonamide derivatives, the preparation thereof and composition comprising the same |
| GB9217295D0 (en) | 1992-08-14 | 1992-09-30 | Wellcome Found | Controlled released tablets |
| GB9315856D0 (en) | 1993-07-30 | 1993-09-15 | Wellcome Found | Stabilized pharmaceutical |
| US5541231A (en) | 1993-07-30 | 1996-07-30 | Glaxo Wellcome Inc. | Stabilized Pharmaceutical |
| US5358970A (en) | 1993-08-12 | 1994-10-25 | Burroughs Wellcome Co. | Pharmaceutical composition containing bupropion hydrochloride and a stabilizer |
| ATE250923T1 (de) | 1997-07-29 | 2003-10-15 | Alcon Lab Inc | Galaktomannanpolymere und borat enthaltende augenarzneimittel |
| EP1049660A1 (en) | 1997-10-10 | 2000-11-08 | The Trustees Of The University Of Pennsylvania | Compositions and methods for inhibiting arginase activity |
| EP1051167A1 (en) | 1998-01-29 | 2000-11-15 | Sepracor, Inc. | Pharmaceutical uses of optically pure (-) -bupropion |
| US20040063666A1 (en) | 1998-10-09 | 2004-04-01 | David Christianson | Compositions for inhibiting arginase activity |
| US8889112B2 (en) | 1999-09-16 | 2014-11-18 | Ocularis Pharma, Llc | Ophthalmic formulations including selective alpha 1 antagonists |
| AU2001275870A1 (en) * | 2000-07-06 | 2002-01-21 | Fal Diagnostics | Methods and kits for the detection of arginine compounds |
| CA2431080A1 (en) | 2003-06-02 | 2004-12-02 | Catherine Adele O'brien | Enhancement of anticancer immunity through inhibition of arginase |
| US6933289B2 (en) | 2003-07-01 | 2005-08-23 | Allergan, Inc. | Inhibition of irritating side effects associated with use of a topical ophthalmic medication |
| CA2534484A1 (en) | 2003-08-07 | 2005-02-17 | Allergan, Inc. | Compositions for delivery of therapeutics into the eyes and methods for making and using same |
| US20050059744A1 (en) | 2003-09-12 | 2005-03-17 | Allergan, Inc. | Methods and compositions for the treatment of pain and other alpha 2 adrenergic-mediated conditions |
| EP1915143A4 (en) | 2005-07-01 | 2009-11-11 | Univ Johns Hopkins | ARGINASE II: TARGET TREATMENT FOR THE AGING HEART AND HEART FAILURE |
| EP2172655B1 (en) | 2007-07-12 | 2018-10-24 | Sanyo Denki Co., Ltd. | Dual reversal-rotating type axial blower |
| JP2012515799A (ja) | 2009-01-26 | 2012-07-12 | ザ トラスティーズ オブ ザ ユニバーシティ オブ ペンシルバニア | アルギナーゼ阻害剤および使用方法 |
| CN104876955B (zh) | 2010-04-22 | 2018-11-23 | 马尔斯公司 | 精氨酸酶抑制剂及其治疗应用 |
| WO2012058065A1 (en) | 2010-10-26 | 2012-05-03 | Mars Incorporated | Boronates as arginase inhibitors |
| US8894970B2 (en) | 2010-12-31 | 2014-11-25 | Corridor Pharmaceuticals, Inc. | Arginase inhibitors and methods of use thereof |
| EP2768491B1 (en) | 2011-10-19 | 2016-12-21 | Mars, Incorporated | Inhibitors of arginase and their therapeutic applications |
| KR20140077963A (ko) | 2011-10-20 | 2014-06-24 | 글락소스미스클라인 엘엘씨 | 시르투인 조절제로서의 치환된 비시클릭 아자-헤테로사이클 및 유사체 |
| CN104540836B (zh) * | 2012-04-18 | 2016-11-09 | 马尔斯公司 | 作为精氨酸酶抑制剂的环约束类似物 |
| EA201690746A1 (ru) | 2013-10-25 | 2016-12-30 | Фармасайкликс Элэлси | Лечение с применением ингибиторов тирозинкиназы брутона и иммунотерапии |
| CN105879030A (zh) | 2014-09-30 | 2016-08-24 | 复旦大学 | 治疗肿瘤的增效药物复合物及其制备方法 |
| EP3270907A1 (en) | 2015-03-20 | 2018-01-24 | Sammy Oyoo OPIYO | Use of suramin and arginase inhibitors in malignant neoplasia |
| CN107921051A (zh) | 2015-06-23 | 2018-04-17 | 卡里塞拉生物科学股份公司 | 抑制精氨酸酶活性的组合物和方法 |
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2016
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- 2016-06-23 WO PCT/US2016/038983 patent/WO2016210106A1/en not_active Ceased
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| US20190343852A1 (en) | 2019-11-14 |
| US20210077510A1 (en) | 2021-03-18 |
| CN107921051A (zh) | 2018-04-17 |
| US10905701B2 (en) | 2021-02-02 |
| UA123700C2 (uk) | 2021-05-19 |
| MX385315B (es) | 2025-03-14 |
| AU2016281620A1 (en) | 2018-02-15 |
| MA42269A (fr) | 2018-05-02 |
| MX2017016868A (es) | 2018-09-06 |
| EP3313410A1 (en) | 2018-05-02 |
| EP3313410A4 (en) | 2019-01-02 |
| EA201890113A1 (ru) | 2018-07-31 |
| US20160375044A1 (en) | 2016-12-29 |
| IL256352A (en) | 2018-02-28 |
| PH12017502391A1 (en) | 2018-06-25 |
| JP2018520352A (ja) | 2018-07-26 |
| MY192605A (en) | 2022-08-29 |
| US10143699B2 (en) | 2018-12-04 |
| ZA201800328B (en) | 2018-12-19 |
| US20180360860A1 (en) | 2018-12-20 |
| US10398714B2 (en) | 2019-09-03 |
| WO2016210106A1 (en) | 2016-12-29 |
| AU2016281620B2 (en) | 2021-07-22 |
| KR20180021117A (ko) | 2018-02-28 |
| SG10202110144TA (en) | 2021-10-28 |
| JP2021185146A (ja) | 2021-12-09 |
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