JPWO2020023191A5 - - Google Patents
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- JPWO2020023191A5 JPWO2020023191A5 JP2021500520A JP2021500520A JPWO2020023191A5 JP WO2020023191 A5 JPWO2020023191 A5 JP WO2020023191A5 JP 2021500520 A JP2021500520 A JP 2021500520A JP 2021500520 A JP2021500520 A JP 2021500520A JP WO2020023191 A5 JPWO2020023191 A5 JP WO2020023191A5
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- Prior art keywords
- pharmaceutical composition
- composition according
- acid
- tumor
- alcohol
- Prior art date
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- 239000008194 pharmaceutical composition Substances 0.000 claims description 40
- 239000000203 mixture Substances 0.000 claims description 28
- 206010028980 Neoplasm Diseases 0.000 claims description 18
- WVDDGKGOMKODPV-UHFFFAOYSA-N benzyl alcohol Chemical compound OCC1=CC=CC=C1 WVDDGKGOMKODPV-UHFFFAOYSA-N 0.000 claims description 18
- SECXISVLQFMRJM-UHFFFAOYSA-N n-methylpyrrolidone Chemical compound CN1CCCC1=O SECXISVLQFMRJM-UHFFFAOYSA-N 0.000 claims description 18
- KXGVEGMKQFWNSR-LLQZFEROSA-N Deoxycholic acid Chemical group C([C@H]1CC2)[C@H](O)CC[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H]([C@@H](CCC(O)=O)C)[C@@]2(C)[C@@H](O)C1 KXGVEGMKQFWNSR-LLQZFEROSA-N 0.000 claims description 9
- 239000002253 acid Substances 0.000 claims description 9
- 239000003795 chemical substances by application Substances 0.000 claims description 9
- 229960003964 deoxycholic acid Drugs 0.000 claims description 9
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 9
- 241000124008 Mammalia Species 0.000 claims description 8
- 230000000202 analgesic Effects 0.000 claims description 8
- 239000003613 bile acid Substances 0.000 claims description 8
- SFNALCNOMXIBKG-UHFFFAOYSA-N ethylene glycol monododecyl ether Chemical compound CCCCCCCCCCCCOCCO SFNALCNOMXIBKG-UHFFFAOYSA-N 0.000 claims description 8
- 230000003902 lesions Effects 0.000 claims description 7
- 235000019445 benzyl alcohol Nutrition 0.000 claims description 6
- 210000001519 tissues Anatomy 0.000 claims description 6
- 210000000988 Bone and Bones Anatomy 0.000 claims description 4
- 210000004556 Brain Anatomy 0.000 claims description 4
- 210000000481 Breast Anatomy 0.000 claims description 4
- 210000001072 Colon Anatomy 0.000 claims description 4
- 210000001035 Gastrointestinal Tract Anatomy 0.000 claims description 4
- 210000004185 Liver Anatomy 0.000 claims description 4
- 210000004072 Lung Anatomy 0.000 claims description 4
- 210000002751 Lymph Anatomy 0.000 claims description 4
- 210000001672 Ovary Anatomy 0.000 claims description 4
- 210000000496 Pancreas Anatomy 0.000 claims description 4
- 210000002307 Prostate Anatomy 0.000 claims description 4
- 210000003491 Skin Anatomy 0.000 claims description 4
- 210000002784 Stomach Anatomy 0.000 claims description 4
- NNJVILVZKWQKPM-UHFFFAOYSA-N Xylocaine Chemical compound CCN(CC)CC(=O)NC1=C(C)C=CC=C1C NNJVILVZKWQKPM-UHFFFAOYSA-N 0.000 claims description 4
- 230000002601 intratumoral Effects 0.000 claims description 4
- 229960004194 lidocaine Drugs 0.000 claims description 4
- 210000004872 soft tissue Anatomy 0.000 claims description 4
- BHQCQFFYRZLCQQ-OELDTZBJSA-N Cholic acid Chemical compound C([C@H]1C[C@H]2O)[C@H](O)CC[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H]([C@@H](CCC(O)=O)C)[C@@]2(C)[C@@H](O)C1 BHQCQFFYRZLCQQ-OELDTZBJSA-N 0.000 claims description 2
- 239000004380 Cholic acid Substances 0.000 claims description 2
- 229940099347 Glycocholic Acid Drugs 0.000 claims description 2
- 108010007979 Glycocholic Acid Proteins 0.000 claims description 2
- RFDAIACWWDREDC-FRVQLJSFSA-N Glycocholic acid Chemical compound C([C@H]1C[C@H]2O)[C@H](O)CC[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H]([C@@H](CCC(=O)NCC(O)=O)C)[C@@]2(C)[C@@H](O)C1 RFDAIACWWDREDC-FRVQLJSFSA-N 0.000 claims description 2
- SMEROWZSTRWXGI-HVATVPOCSA-N Lithocholic acid Chemical compound C([C@H]1CC2)[C@H](O)CC[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H]([C@@H](CCC(O)=O)C)[C@@]2(C)CC1 SMEROWZSTRWXGI-HVATVPOCSA-N 0.000 claims description 2
- 230000003385 bacteriostatic Effects 0.000 claims description 2
- 239000003833 bile salt Substances 0.000 claims description 2
- 230000022534 cell killing Effects 0.000 claims description 2
- 229960002471 cholic acid Drugs 0.000 claims description 2
- 235000019416 cholic acid Nutrition 0.000 claims description 2
- 230000009089 cytolysis Effects 0.000 claims description 2
- 238000002347 injection Methods 0.000 claims description 2
- 239000007924 injection Substances 0.000 claims description 2
- 230000017074 necrotic cell death Effects 0.000 claims description 2
- 230000000149 penetrating Effects 0.000 claims description 2
- 239000004848 polyfunctional curative Substances 0.000 claims description 2
- JAJWGJBVLPIOOH-IZYKLYLVSA-M sodium taurocholate Chemical compound [Na+].C([C@H]1C[C@H]2O)[C@H](O)CC[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H]([C@@H](CCC(=O)NCCS([O-])(=O)=O)C)[C@@]2(C)[C@@H](O)C1 JAJWGJBVLPIOOH-IZYKLYLVSA-M 0.000 claims description 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 2
- OKKJLVBELUTLKV-UHFFFAOYSA-N methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 claims 1
- LTSWUFKUZPPYEG-UHFFFAOYSA-N 1-decoxydecane Chemical compound CCCCCCCCCCOCCCCCCCCCC LTSWUFKUZPPYEG-UHFFFAOYSA-N 0.000 description 1
- 229960001091 Chenodeoxycholic Acid Drugs 0.000 description 1
- RUDATBOHQWOJDD-BSWAIDMHSA-N Chenodeoxycholic acid Chemical compound C([C@H]1C[C@H]2O)[C@H](O)CC[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H]([C@@H](CCC(O)=O)C)[C@@]2(C)CC1 RUDATBOHQWOJDD-BSWAIDMHSA-N 0.000 description 1
- 229950001904 chenodiol Drugs 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 238000006011 modification reaction Methods 0.000 description 1
- YZUUTMGDONTGTN-UHFFFAOYSA-N nonaethylene glycol Chemical group OCCOCCOCCOCCOCCOCCOCCOCCOCCO YZUUTMGDONTGTN-UHFFFAOYSA-N 0.000 description 1
- 229920000847 nonoxynol Polymers 0.000 description 1
- 150000003839 salts Chemical class 0.000 description 1
- 239000003229 sclerosing agent Substances 0.000 description 1
- 239000011780 sodium chloride Substances 0.000 description 1
Description
[000124]本発明の好ましい実施形態を記載してきたが、本発明は厳格な実施形態に限定されず、さまざまな変更および変形が、添付の特許請求の範囲において定義される本発明の範囲または趣旨から逸脱することなく当業者によってその中で行われてもよいことを理解されたい。
以下に、出願時の特許請求の範囲の記載を示す。
［請求項１］
硬化剤および浸透剤の組合せを含む医薬組成物。
［請求項２］
硬化剤がノナエチレングリコールモノドデシルエーテルである、請求項１に記載の医薬組成物。
［請求項３］
浸透剤が無水１－メチル－２－ピロリジノンである、請求項１に記載の医薬組成物。
［請求項４］
硬化剤および浸透剤が、対象における腫瘍のサイズを減少させるのに有効な量の組合せで存在する、請求項１に記載の医薬組成物。
［請求項５］
対象が哺乳動物である、請求項４に記載の組成物。
［請求項６］
哺乳動物がヒトである、請求項５に記載の組成物。
［請求項７］
アルコールを更に含む、請求項１に記載の組成物。
［請求項８］
アルコールがベンジルアルコールである、請求項７に記載の組成物。
［請求項９］
酸またはその塩を更に含む、請求項１に記載の組成物。
［請求項１０］
酸が胆汁酸である、請求項９に記載の組成物。
［請求項１１］
胆汁酸塩がデオキシコール酸ナトリウムである、請求項１０に記載の組成物。
［請求項１２］
鎮痛剤を更に含む、請求項１に記載の組成物。
［請求項１３］
鎮痛剤がリドカインである、請求項１２に記載の組成物。
［請求項１４］
組合せが酸の存在下で組織に浸透する、請求項１に記載の組成物。
［請求項１５］
胆汁酸、ノナエチレングリコールモノドデシルエーテル、および無水１－メチル－２－ピロリジノンを含む、医薬組成物。
［請求項１６］
胆汁酸がデオキシコール酸ナトリウムである、請求項１５に記載の医薬組成物。
［請求項１７］
対象における腫瘍のサイズを減少させる方法であって、腫瘍を、治療有効量の硬化剤および浸透剤の組合せを含む組成物と接触させるステップを含む方法。
［請求項１８］
対象における腫瘍のサイズを減少させる方法であって、腫瘍を、治療有効量の硬化剤および浸透剤の組合せならびに胆汁酸を含む組成物と接触させるステップを含む方法。
［請求項１９］
接触させるステップが腫瘍内注射を含む、請求項１７～１８のいずれか一項に記載の方法。
［請求項２０］
腫瘍が、乳房、前立腺、肺、結腸、胃、膵臓、卵巣、脳、皮膚、骨、脂肪、リンパ、胃腸管、肝臓の組織、または軟組織に存在する、請求項１７～１８のいずれか一項に記載の方法。
［請求項２１］
硬化剤がノナエチレングリコールモノデシルエーテルである、請求項１７～１８のいずれか一項に記載の方法。
［請求項２２］
浸透剤が無水１－メチル－２－ピロリジノンである、請求項１７～１８のいずれか一項に記載の方法。
［請求項２３］
胆汁酸が、デオキシコール酸、コール酸、グリココール酸、タウロコール酸、ケノデオキシコール酸、グリコケノデオキシコール酸、タウロケノデオキシコール酸、またはリトコール酸である、請求項１８に記載の方法。
［請求項２４］
対象が哺乳動物である、請求項１７～１８のいずれか一項に記載の方法。
［請求項２５］
哺乳動物がヒトである、請求項２４に記載の方法。
［請求項２６］
組成物がアルコールを更に含む、請求項１７～１８のいずれか一項に記載の方法。
［請求項２７］
アルコールがベンジルアルコールである、請求項２６に記載の方法。
［請求項２８］
組成物が鎮痛剤を更に含む、請求項１７～１８のいずれか一項に記載の方法。
［請求項２９］
鎮痛剤がリドカインである、請求項２８に記載の方法。
［請求項３０］
組成物が、ベンジルアルコール、デオキシコール酸ナトリウム、ノナエチレングリコールモノドデシルエーテル、および無水１－メチル－２－ピロリジノンを含む、請求項１８に記載の方法。
［請求項３１］
組成物と接触させた腫瘍が、静菌水を含む対照と接触させた腫瘍と比較して腫瘍内壊死の増加を含む、請求項１７～３０のいずれか一項に記載の方法。
［請求項３２］
腫瘍が癌性である、請求項１７～３１のいずれか一項に記載の方法。
［請求項３３］
対象における病変部を処置する方法であって、病変部を、請求項１～１６のいずれか一項に記載の医薬組成物と接触させるステップを含む方法。
［請求項３４］
病変部が、乳房、前立腺、肺、結腸、胃、膵臓、卵巣、脳、皮膚、骨、脂肪、リンパ、胃腸管、肝臓の組織、または軟組織に存在する、請求項３３に記載の方法。
［請求項３５］
病変部が非癌性である、請求項３３～３４のいずれか一項に記載の方法。
[000124] Although preferred embodiments of the invention have been described, the invention is not limited to strict embodiments and various modifications and variations are defined within the scope of the appended claims or intent. It should be understood that it may be done within it by one of ordinary skill in the art without departing from.
The following is a description of the scope of claims at the time of filing.
[Claim 1]
A pharmaceutical composition comprising a combination of a curing agent and a penetrant.
[Claim 2]
The pharmaceutical composition according to claim 1, wherein the curing agent is nonaethylene glycol monododecyl ether.
[Claim 3]
The pharmaceutical composition according to claim 1, wherein the penetrant is anhydrous 1-methyl-2-pyrrolidinone.
[Claim 4]
The pharmaceutical composition according to claim 1, wherein the curing agent and the penetrating agent are present in a combination of effective amounts to reduce the size of the tumor in the subject.
[Claim 5]
The composition according to claim 4, wherein the subject is a mammal.
[Claim 6]
The composition according to claim 5, wherein the mammal is a human.
[Claim 7]
The composition according to claim 1, further comprising alcohol.
[Claim 8]
The composition according to claim 7, wherein the alcohol is benzyl alcohol.
[Claim 9]
The composition according to claim 1, further comprising an acid or a salt thereof.
[Claim 10]
The composition according to claim 9, wherein the acid is a bile acid.
[Claim 11]
The composition according to claim 10, wherein the bile salt is sodium deoxycholate.
[Claim 12]
The composition according to claim 1, further comprising an analgesic.
[Claim 13]
12. The composition of claim 12, wherein the analgesic is lidocaine.
[Claim 14]
The composition of claim 1, wherein the combination penetrates the tissue in the presence of acid.
[Claim 15]
A pharmaceutical composition comprising bile acids, nonaethylene glycol monododecyl ether, and anhydrous 1-methyl-2-pyrrolidinone.
[Claim 16]
The pharmaceutical composition according to claim 15, wherein the bile acid is sodium deoxycholate.
[Claim 17]
A method of reducing the size of a tumor in a subject, comprising contacting the tumor with a composition comprising a therapeutically effective amount of a combination of hardener and penetrant.
[Claim 18]
A method of reducing the size of a tumor in a subject, comprising contacting the tumor with a therapeutically effective combination of a sclerosing agent and a penetrant and a composition comprising a bile acid.
[Claim 19]
The method of any one of claims 17-18, wherein the contacting step comprises an intratumoral injection.
[Claim 20]
Any one of claims 17-18, wherein the tumor is present in the breast, prostate, lung, colon, stomach, pancreas, ovary, brain, skin, bone, fat, lymph, gastrointestinal tract, liver tissue, or soft tissue. The method described in.
[Claim 21]
The method according to any one of claims 17 to 18, wherein the curing agent is nonaethylene glycol monodecyl ether.
[Claim 22]
The method according to any one of claims 17 to 18, wherein the penetrant is anhydrous 1-methyl-2-pyrrolidinone.
[Claim 23]
18. The method of claim 18, wherein the bile acid is deoxycholic acid, cholic acid, glycocholic acid, taurocholic acid, chenodeoxycholic acid, glycokenodeoxycholic acid, taurokenodeoxycholic acid, or lithocholic acid.
[Claim 24]
The method according to any one of claims 17 to 18, wherein the subject is a mammal.
[Claim 25]
24. The method of claim 24, wherein the mammal is a human.
[Claim 26]
The method according to any one of claims 17 to 18, wherein the composition further comprises alcohol.
[Claim 27]
26. The method of claim 26, wherein the alcohol is benzyl alcohol.
[Claim 28]
The method of any one of claims 17-18, wherein the composition further comprises an analgesic.
[Claim 29]
28. The method of claim 28, wherein the analgesic is lidocaine.
[Claim 30]
18. The method of claim 18, wherein the composition comprises benzyl alcohol, sodium deoxycholate, nonaethylene glycol monododecyl ether, and anhydrous 1-methyl-2-pyrrolidinone.
[Claim 31]
The method of any one of claims 17-30, wherein the tumor contacted with the composition comprises an increase in intratumoral necrosis as compared to a tumor contacted with a control containing bacteriostatic water.
[Claim 32]
The method according to any one of claims 17 to 31, wherein the tumor is cancerous.
[Claim 33]
A method of treating a lesion in a subject, comprising contacting the lesion with the pharmaceutical composition according to any one of claims 1-16.
[Claim 34]
33. The method of claim 33, wherein the lesion is present in the breast, prostate, lung, colon, stomach, pancreas, ovary, brain, skin, bone, fat, lymph, gastrointestinal tract, liver tissue, or soft tissue.
[Claim 35]
The method according to any one of claims 33 to 34, wherein the lesion is non-cancerous.
Claims (26)
無水１－メチル－２－ピロリジノンである浸透剤、
アルコール、および、
胆汁酸、
の組合せを含む医薬組成物。 Hardener, which is nonaethylene glycol monododecyl ether,
Penetrant, anhydrous 1-methyl-2-pyrrolidinone,
Alcohol and
Bile acid,
A pharmaceutical composition comprising a combination of.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862695613P | 2018-07-09 | 2018-07-09 | |
| US62/695,613 | 2018-07-09 | ||
| PCT/US2019/040264 WO2020023191A1 (en) | 2018-07-09 | 2019-07-02 | Tumor reduction formulations and methods of use thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2021530482A JP2021530482A (en) | 2021-11-11 |
| JPWO2020023191A5 true JPWO2020023191A5 (en) | 2022-07-07 |
Family
ID=75267393
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021500520A Withdrawn JP2021530482A (en) | 2018-07-09 | 2019-07-02 | Tumor-reducing preparations and how to use them |
Country Status (11)
| Country | Link |
|---|---|
| EP (1) | EP3820482A4 (en) |
| JP (1) | JP2021530482A (en) |
| KR (1) | KR20220098082A (en) |
| CN (1) | CN112584841A (en) |
| AU (1) | AU2019309757A1 (en) |
| BR (1) | BR112021000279A8 (en) |
| CA (1) | CA3105717A1 (en) |
| EA (1) | EA202190201A1 (en) |
| IL (1) | IL280000A (en) |
| PH (1) | PH12021550033A1 (en) |
| WO (1) | WO2020023191A1 (en) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX2021013901A (en) | 2019-05-14 | 2022-04-12 | Tyme Inc | Compositions and methods for treating cancer. |
| CN114945374A (en) * | 2019-12-09 | 2022-08-26 | 迪美公司 | Pharmaceutical compositions and methods |
| US10905698B1 (en) | 2020-05-14 | 2021-02-02 | Tyme, Inc. | Methods of treating SARS-COV-2 infections |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1713443A2 (en) * | 2004-01-29 | 2006-10-25 | Baxter International Inc. | Nanosuspensions of anti-retroviral agents for increased central nervous system delivery |
| WO2006099685A1 (en) * | 2005-03-24 | 2006-09-28 | Medical Therapies Limited | Method for the prophylaxis or treatment of carcinomas |
| CN101023940A (en) * | 2006-02-20 | 2007-08-29 | 郝守祝 | Medicine composition of Taxane compounds, preparing method and use |
| AU2015287749B2 (en) * | 2014-07-11 | 2021-03-11 | The Regents Of The University Of California | Tumor selective macropinocytosis-dependent rapidly internalizing antibodies |
| US9687528B2 (en) * | 2014-12-23 | 2017-06-27 | Steven Hoffman | Transdermal formulations |
| US20190091252A1 (en) * | 2016-03-15 | 2019-03-28 | Tyme, Inc. | Pharmaceutical compositions for the treatment of cancer |
-
2019
- 2019-07-02 CA CA3105717A patent/CA3105717A1/en active Pending
- 2019-07-02 EA EA202190201A patent/EA202190201A1/en unknown
- 2019-07-02 CN CN201980054337.1A patent/CN112584841A/en active Pending
- 2019-07-02 KR KR1020217003523A patent/KR20220098082A/en active Search and Examination
- 2019-07-02 EP EP19841949.1A patent/EP3820482A4/en not_active Withdrawn
- 2019-07-02 WO PCT/US2019/040264 patent/WO2020023191A1/en unknown
- 2019-07-02 JP JP2021500520A patent/JP2021530482A/en not_active Withdrawn
- 2019-07-02 BR BR112021000279A patent/BR112021000279A8/en not_active Application Discontinuation
- 2019-07-02 AU AU2019309757A patent/AU2019309757A1/en not_active Abandoned
-
2021
- 2021-01-06 PH PH12021550033A patent/PH12021550033A1/en unknown
- 2021-01-07 IL IL280000A patent/IL280000A/en unknown
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