JP2004519493A5 - - Google Patents
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- Publication number
- JP2004519493A5 JP2004519493A5 JP2002572770A JP2002572770A JP2004519493A5 JP 2004519493 A5 JP2004519493 A5 JP 2004519493A5 JP 2002572770 A JP2002572770 A JP 2002572770A JP 2002572770 A JP2002572770 A JP 2002572770A JP 2004519493 A5 JP2004519493 A5 JP 2004519493A5
- Authority
- JP
- Japan
- Prior art keywords
- hydrogen
- lower alkyl
- combination
- bond
- combination according
- 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.)
- Withdrawn
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- 125000000217 alkyl group Chemical group 0.000 claims 9
- 229910052739 hydrogen Inorganic materials 0.000 claims 9
- 239000001257 hydrogen Substances 0.000 claims 9
- 229940125714 antidiarrheal agent Drugs 0.000 claims 6
- 239000003793 antidiarrheal agent Substances 0.000 claims 6
- 201000010099 disease Diseases 0.000 claims 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 5
- 150000003883 epothilone derivatives Chemical class 0.000 claims 5
- 230000002062 proliferating effect Effects 0.000 claims 5
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 4
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 3
- -1 bapreotide Chemical compound 0.000 claims 2
- 239000002552 dosage form Substances 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- DEQANNDTNATYII-OULOTJBUSA-N (4r,7s,10s,13r,16s,19r)-10-(4-aminobutyl)-19-[[(2r)-2-amino-3-phenylpropanoyl]amino]-16-benzyl-n-[(2r,3r)-1,3-dihydroxybutan-2-yl]-7-[(1r)-1-hydroxyethyl]-13-(1h-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxa Chemical compound C([C@@H](N)C(=O)N[C@H]1CSSC[C@H](NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC=2C3=CC=CC=C3NC=2)NC(=O)[C@H](CC=2C=CC=CC=2)NC1=O)C(=O)N[C@H](CO)[C@H](O)C)C1=CC=CC=C1 DEQANNDTNATYII-OULOTJBUSA-N 0.000 claims 1
- PUDHBTGHUJUUFI-SCTWWAJVSA-N (4r,7s,10s,13r,16s,19r)-10-(4-aminobutyl)-n-[(2s,3r)-1-amino-3-hydroxy-1-oxobutan-2-yl]-19-[[(2r)-2-amino-3-naphthalen-2-ylpropanoyl]amino]-16-[(4-hydroxyphenyl)methyl]-13-(1h-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-7-propan-2-yl-1,2-dithia-5,8,11,14,17-p Chemical compound C([C@H]1C(=O)N[C@H](CC=2C3=CC=CC=C3NC=2)C(=O)N[C@@H](CCCCN)C(=O)N[C@H](C(N[C@@H](CSSC[C@@H](C(=O)N1)NC(=O)[C@H](N)CC=1C=C2C=CC=CC2=CC=1)C(=O)N[C@@H]([C@@H](C)O)C(N)=O)=O)C(C)C)C1=CC=C(O)C=C1 PUDHBTGHUJUUFI-SCTWWAJVSA-N 0.000 claims 1
- UEJJHQNACJXSKW-UHFFFAOYSA-N 2-(2,6-dioxopiperidin-3-yl)-1H-isoindole-1,3(2H)-dione Chemical compound O=C1C2=CC=CC=C2C(=O)N1C1CCC(=O)NC1=O UEJJHQNACJXSKW-UHFFFAOYSA-N 0.000 claims 1
- 239000005995 Aluminium silicate Substances 0.000 claims 1
- 108010067722 Dipeptidyl Peptidase 4 Proteins 0.000 claims 1
- 102100025012 Dipeptidyl peptidase 4 Human genes 0.000 claims 1
- ZDXPYRJPNDTMRX-VKHMYHEASA-N L-glutamine Chemical compound OC(=O)[C@@H](N)CCC(N)=O ZDXPYRJPNDTMRX-VKHMYHEASA-N 0.000 claims 1
- 229940116366 Motilin antagonist Drugs 0.000 claims 1
- 108010016076 Octreotide Proteins 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- 235000012211 aluminium silicate Nutrition 0.000 claims 1
- YBHILYKTIRIUTE-UHFFFAOYSA-N berberine Chemical compound C1=C2CC[N+]3=CC4=C(OC)C(OC)=CC=C4C=C3C2=CC2=C1OCO2 YBHILYKTIRIUTE-UHFFFAOYSA-N 0.000 claims 1
- 229940093265 berberine Drugs 0.000 claims 1
- QISXPYZVZJBNDM-UHFFFAOYSA-N berberine Natural products COc1ccc2C=C3N(Cc2c1OC)C=Cc4cc5OCOc5cc34 QISXPYZVZJBNDM-UHFFFAOYSA-N 0.000 claims 1
- ZREIPSZUJIFJNP-UHFFFAOYSA-K bismuth subsalicylate Chemical compound C1=CC=C2O[Bi](O)OC(=O)C2=C1 ZREIPSZUJIFJNP-UHFFFAOYSA-K 0.000 claims 1
- 229960000782 bismuth subsalicylate Drugs 0.000 claims 1
- 229940111134 coxibs Drugs 0.000 claims 1
- 239000003255 cyclooxygenase 2 inhibitor Substances 0.000 claims 1
- 229960002743 glutamine Drugs 0.000 claims 1
- ZDXPYRJPNDTMRX-UHFFFAOYSA-N glutamine Natural products OC(=O)C(N)CCC(N)=O ZDXPYRJPNDTMRX-UHFFFAOYSA-N 0.000 claims 1
- 150000002431 hydrogen Chemical class 0.000 claims 1
- 239000003112 inhibitor Substances 0.000 claims 1
- 229960000829 kaolin Drugs 0.000 claims 1
- NLYAJNPCOHFWQQ-UHFFFAOYSA-N kaolin Chemical compound O.O.O=[Al]O[Si](=O)O[Si](=O)O[Al]=O NLYAJNPCOHFWQQ-UHFFFAOYSA-N 0.000 claims 1
- 229960002437 lanreotide Drugs 0.000 claims 1
- 108010021336 lanreotide Proteins 0.000 claims 1
- 229960002700 octreotide Drugs 0.000 claims 1
- 229960000292 pectin Drugs 0.000 claims 1
- 235000010987 pectin Nutrition 0.000 claims 1
- 229920001277 pectin Polymers 0.000 claims 1
- 239000001814 pectin Substances 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 229960003433 thalidomide Drugs 0.000 claims 1
- 230000001225 therapeutic effect Effects 0.000 claims 1
Claims (10)
- 同時的、個別的または逐次的使用のための、(ａ)抗下痢剤および(ｂ)式Ｉ
のエポチロン誘導体を含む組合せ剤であって、
活性成分(ａ)および(ｂ)はそれぞれの場合において遊離の形態または薬学的に許容される塩の形態であり、そして所望により少なくとも１つの薬学的に許容される担体を含む組合せ剤。 - ＡがＯを表し、Ｒは低級アルキルまたは水素であり、そしてＺはＯまたは結合である、式Ｉのエポチロン誘導体を含む、請求項１に記載の組合せ剤。
- 抗下痢剤がＤＰＰ−ＩＶインヒビターである、請求項１または２に記載の組合せ剤。
- 抗下痢剤が、天然のオピオイド、合成オピオイド、次サリチル酸ビスマス、ランレオチド、バプレオチド、オクトレオチド、ＣＯＸ２インヒビター、モチリンアンタゴニスト、カオリン、グルタミン、サリドマイド、ペクチンもしくはベルベリン、または薬学的に許容されるその塩である、請求項１または２に記載の組合せ剤。
- 増殖性疾患に対して共同で治療有効性を示す量の請求項１〜３のいずれかに記載の組合せ剤と、少なくとも１つの薬学的に許容される担体とを含む医薬組成物。
- 増殖性疾患のための、請求項１〜４のいずれかに記載の組合せ剤の使用。
- 増殖性疾患処置用医薬の製造のための、請求項１〜４のいずれかに記載の組合せ剤の使用。
- 増殖性疾患処置用医薬の製造のための、式Ｉ
のエポチロン誘導体と組み合せた抗下痢剤の使用。 - 増殖性疾患の処置における同時的、個別的または逐次的使用のための指導書とともに、(ａ)抗下痢剤および(ｂ)式Ｉ
のエポチロン誘導体を含む商業用パッケージ。 - 遊離の形態または薬学的に許容される塩の形態の、(ａ)１またはそれ以上の単位投与形態の抗下痢剤および(ｂ)１またはそれ以上の単位投与形態の式Ｉ
のエポチロン誘導体を含む、組合せ製剤。
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US27715301P | 2001-03-19 | 2001-03-19 | |
| US27720701P | 2001-03-20 | 2001-03-20 | |
| PCT/EP2002/002977 WO2002074042A2 (en) | 2001-03-19 | 2002-03-18 | Combinations comprising an antidiarrheal agent and an epothilone or an epothilone derivative |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009196666A Division JP2010006830A (ja) | 2001-03-19 | 2009-08-27 | 抗下痢剤およびエポチロンまたはエポチロン誘導体を含む組合せ剤 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2004519493A JP2004519493A (ja) | 2004-07-02 |
| JP2004519493A5 true JP2004519493A5 (ja) | 2005-12-22 |
Family
ID=26958333
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2002572770A Withdrawn JP2004519493A (ja) | 2001-03-19 | 2002-03-18 | 抗下痢剤およびエポチロンまたはエポチロン誘導体を含む組合せ剤 |
| JP2009196666A Pending JP2010006830A (ja) | 2001-03-19 | 2009-08-27 | 抗下痢剤およびエポチロンまたはエポチロン誘導体を含む組合せ剤 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009196666A Pending JP2010006830A (ja) | 2001-03-19 | 2009-08-27 | 抗下痢剤およびエポチロンまたはエポチロン誘導体を含む組合せ剤 |
Country Status (27)
| Country | Link |
|---|---|
| US (1) | US7030147B2 (ja) |
| EP (1) | EP1372650B1 (ja) |
| JP (2) | JP2004519493A (ja) |
| KR (1) | KR100863089B1 (ja) |
| CN (1) | CN100540001C (ja) |
| AT (1) | ATE414514T1 (ja) |
| AU (1) | AU2002251067B2 (ja) |
| BR (1) | BR0208142A (ja) |
| CA (1) | CA2440111C (ja) |
| CY (1) | CY1108845T1 (ja) |
| CZ (1) | CZ302848B6 (ja) |
| DE (1) | DE60229922D1 (ja) |
| DK (1) | DK1372650T3 (ja) |
| ES (1) | ES2318001T3 (ja) |
| HK (1) | HK1061516A1 (ja) |
| HU (1) | HUP0303621A3 (ja) |
| IL (1) | IL157333A0 (ja) |
| MX (1) | MXPA03008462A (ja) |
| NO (1) | NO333106B1 (ja) |
| NZ (1) | NZ541703A (ja) |
| PT (1) | PT1372650E (ja) |
| RU (1) | RU2330661C2 (ja) |
| SI (1) | SI1372650T1 (ja) |
| SK (1) | SK287334B6 (ja) |
| TW (1) | TWI331525B (ja) |
| WO (1) | WO2002074042A2 (ja) |
| ZA (1) | ZA200306318B (ja) |
Families Citing this family (35)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6242469B1 (en) | 1996-12-03 | 2001-06-05 | Sloan-Kettering Institute For Cancer Research | Synthesis of epothilones, intermediates thereto, analogues and uses thereof |
| US20020058286A1 (en) * | 1999-02-24 | 2002-05-16 | Danishefsky Samuel J. | Synthesis of epothilones, intermediates thereto and analogues thereof |
| AU2001280120A1 (en) * | 2000-08-24 | 2002-03-04 | Chugai Seiyaku Kabushiki Kaisha | Cyclic peptide derivative |
| KR20040025904A (ko) | 2001-03-14 | 2004-03-26 | 브리스톨-마이어스 스큅 컴퍼니 | 증식성 질환의 치료를 위한 에포틸론 유사체 및화학치료제의 병용 |
| US6727261B2 (en) | 2001-12-27 | 2004-04-27 | Hoffman-La Roche Inc. | Pyrido[2,1-A]Isoquinoline derivatives |
| US7649006B2 (en) | 2002-08-23 | 2010-01-19 | Sloan-Kettering Institute For Cancer Research | Synthesis of epothilones, intermediates thereto and analogues thereof |
| WO2004018478A2 (en) | 2002-08-23 | 2004-03-04 | Sloan-Kettering Institute For Cancer Research | Synthesis of epothilones, intermediates thereto, analogues and uses thereof |
| US20040242566A1 (en) * | 2003-03-25 | 2004-12-02 | Syrrx, Inc. | Dipeptidyl peptidase inhibitors |
| ZA200602051B (en) * | 2003-08-13 | 2007-10-31 | Takeda Pharmaceutical | 4-pyrimidone derivatives and their use as peptidyl peptidase inhibitors |
| US7678909B1 (en) | 2003-08-13 | 2010-03-16 | Takeda Pharmaceutical Company Limited | Dipeptidyl peptidase inhibitors |
| US7169926B1 (en) | 2003-08-13 | 2007-01-30 | Takeda Pharmaceutical Company Limited | Dipeptidyl peptidase inhibitors |
| EP1697342A2 (en) * | 2003-09-08 | 2006-09-06 | Takeda Pharmaceutical Company Limited | Dipeptidyl peptidase inhibitors |
| US7790734B2 (en) * | 2003-09-08 | 2010-09-07 | Takeda Pharmaceutical Company Limited | Dipeptidyl peptidase inhibitors |
| US7732446B1 (en) | 2004-03-11 | 2010-06-08 | Takeda Pharmaceutical Company Limited | Dipeptidyl peptidase inhibitors |
| CN102134231B (zh) * | 2004-03-15 | 2020-08-04 | 武田药品工业株式会社 | 二肽基肽酶抑制剂 |
| RU2253440C1 (ru) * | 2004-03-31 | 2005-06-10 | Открытое Акционерное Общество "Фаберлик" | Средство для устранения нарушений нейрогенной и эндокринной регуляции системы капиллярного кровотока |
| JP2008501714A (ja) * | 2004-06-04 | 2008-01-24 | 武田薬品工業株式会社 | ジペプチジルペプチダーゼインヒビター |
| WO2006019965A2 (en) | 2004-07-16 | 2006-02-23 | Takeda San Diego, Inc. | Dipeptidyl peptidase inhibitors |
| US20060121511A1 (en) | 2004-11-30 | 2006-06-08 | Hyerim Lee | Biomarkers and methods for determining sensitivity to microtubule-stabilizing agents |
| US7872124B2 (en) | 2004-12-21 | 2011-01-18 | Takeda Pharmaceutical Company Limited | Dipeptidyl peptidase inhibitors |
| EP1856255A4 (en) | 2005-02-11 | 2010-01-27 | Univ Southern California | METHODS OF EXPRESSING PROTEINS WITH DISULFIDE BRIDGES |
| CN101309689B (zh) * | 2005-09-14 | 2012-10-10 | 武田药品工业株式会社 | 用于治疗糖尿病的二肽基肽酶抑制剂 |
| EA015169B1 (ru) | 2005-09-14 | 2011-06-30 | Такеда Фармасьютикал Компани Лимитед | Применение ингибиторов дипептидилпептидазы |
| TW200745080A (en) * | 2005-09-16 | 2007-12-16 | Takeda Pharmaceuticals Co | Polymorphs of tartrate salt of 2-[2-(3-(R)-amino-piperidin-1-yl)-5-fluoro-6-oxo-6H-pyrimidin-1-ylmethyl]-benzonitrile and methods of use therefor |
| WO2007035629A2 (en) | 2005-09-16 | 2007-03-29 | Takeda Pharmaceutical Company Limited | Process for the preparation of pyrimidinedione derivatives |
| TW200745079A (en) * | 2005-09-16 | 2007-12-16 | Takeda Pharmaceuticals Co | Polymorphs of benzoate salt of 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]-benzonitrile and methods of use therefor |
| WO2007112347A1 (en) | 2006-03-28 | 2007-10-04 | Takeda Pharmaceutical Company Limited | Dipeptidyl peptidase inhibitors |
| US8008256B2 (en) * | 2006-05-01 | 2011-08-30 | University Of Southern California | Combination therapy for treatment of cancer |
| US8324383B2 (en) | 2006-09-13 | 2012-12-04 | Takeda Pharmaceutical Company Limited | Methods of making polymorphs of benzoate salt of 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]-benzonitrile |
| TW200838536A (en) | 2006-11-29 | 2008-10-01 | Takeda Pharmaceutical | Polymorphs of succinate salt of 2-[6-(3-amino-piperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-ylmethy]-4-fluor-benzonitrile and methods of use therefor |
| US8093236B2 (en) | 2007-03-13 | 2012-01-10 | Takeda Pharmaceuticals Company Limited | Weekly administration of dipeptidyl peptidase inhibitors |
| US20100267682A1 (en) * | 2007-11-09 | 2010-10-21 | Novartis Ag | Corticosteroids to treat epothilone or epothilone derivative induced diarrhea |
| WO2010056901A2 (en) | 2008-11-13 | 2010-05-20 | University Of Southern California | Method of expressing proteins with disulfide bridges with enhanced yields and activity |
| CN103037903A (zh) | 2010-05-18 | 2013-04-10 | 天蓝制药公司 | 用于治疗自身免疫性疾病或其它疾病的组合物和方法 |
| KR101478925B1 (ko) * | 2013-12-31 | 2015-01-08 | 아주대학교산학협력단 | 프로테아좀 저해제와 로페라마이드를 유효성분으로 함유하는 암질환 예방 또는 치료용 약학조성물 |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5919816A (en) * | 1994-11-14 | 1999-07-06 | Bionumerik Pharmaceuticals, Inc. | Formulations and methods of reducing toxicity of antineoplastic agents |
| WO1997033552A1 (en) * | 1996-03-12 | 1997-09-18 | Pg-Txl Company, L.P. | Water soluble paclitaxel prodrugs |
| US5969145A (en) * | 1996-08-30 | 1999-10-19 | Novartis Ag | Process for the production of epothilones and intermediate products within the process |
| US6441186B1 (en) * | 1996-12-13 | 2002-08-27 | The Scripps Research Institute | Epothilone analogs |
| US6103487A (en) * | 1997-08-27 | 2000-08-15 | Merck & Co., Inc. | Method of treating cancer |
| US6127390A (en) * | 1997-10-02 | 2000-10-03 | Merck & Co., Inc. | Inhibitors of prenyl-protein transferase |
| US6040321A (en) * | 1997-11-12 | 2000-03-21 | Bristol-Myers Squibb Company | Aminothiazole inhibitors of cyclin dependent kinases |
| EP1052974B1 (en) * | 1998-02-05 | 2009-05-20 | Novartis AG | Pharmaceutical formulation containing epothilone |
| US6302838B1 (en) * | 1998-02-25 | 2001-10-16 | Novartis Ag | Cancer treatment with epothilones |
| US20020045609A1 (en) | 2000-05-26 | 2002-04-18 | Gary Ashley | Epothilone derivatives and methods for making and using the same |
-
2002
- 2002-03-18 EP EP02719992A patent/EP1372650B1/en not_active Expired - Lifetime
- 2002-03-18 MX MXPA03008462A patent/MXPA03008462A/es active IP Right Grant
- 2002-03-18 SK SK1170-2003A patent/SK287334B6/sk not_active IP Right Cessation
- 2002-03-18 WO PCT/EP2002/002977 patent/WO2002074042A2/en active IP Right Grant
- 2002-03-18 IL IL15733302A patent/IL157333A0/xx not_active IP Right Cessation
- 2002-03-18 CZ CZ20032529A patent/CZ302848B6/cs not_active IP Right Cessation
- 2002-03-18 AT AT02719992T patent/ATE414514T1/de active
- 2002-03-18 DE DE60229922T patent/DE60229922D1/de not_active Expired - Lifetime
- 2002-03-18 ES ES02719992T patent/ES2318001T3/es not_active Expired - Lifetime
- 2002-03-18 US US10/471,904 patent/US7030147B2/en not_active Expired - Fee Related
- 2002-03-18 HU HU0303621A patent/HUP0303621A3/hu unknown
- 2002-03-18 KR KR1020037012154A patent/KR100863089B1/ko not_active IP Right Cessation
- 2002-03-18 CN CNB028068459A patent/CN100540001C/zh not_active Expired - Fee Related
- 2002-03-18 DK DK02719992T patent/DK1372650T3/da active
- 2002-03-18 JP JP2002572770A patent/JP2004519493A/ja not_active Withdrawn
- 2002-03-18 NZ NZ541703A patent/NZ541703A/en not_active IP Right Cessation
- 2002-03-18 AU AU2002251067A patent/AU2002251067B2/en not_active Ceased
- 2002-03-18 TW TW091105086A patent/TWI331525B/zh not_active IP Right Cessation
- 2002-03-18 PT PT02719992T patent/PT1372650E/pt unknown
- 2002-03-18 RU RU2003130058/15A patent/RU2330661C2/ru not_active IP Right Cessation
- 2002-03-18 CA CA2440111A patent/CA2440111C/en not_active Expired - Fee Related
- 2002-03-18 BR BR0208142-3A patent/BR0208142A/pt not_active Application Discontinuation
- 2002-03-18 SI SI200230793T patent/SI1372650T1/sl unknown
-
2003
- 2003-08-14 ZA ZA2003/06318A patent/ZA200306318B/en unknown
- 2003-09-15 NO NO20034094A patent/NO333106B1/no not_active IP Right Cessation
-
2004
- 2004-06-16 HK HK04104401.1A patent/HK1061516A1/xx not_active IP Right Cessation
-
2009
- 2009-02-19 CY CY20091100200T patent/CY1108845T1/el unknown
- 2009-08-27 JP JP2009196666A patent/JP2010006830A/ja active Pending
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