JP2001519842A - 生分解性テレフタレートポリエステル−ポリホスフェートポリマー、組成物、物品、並びにその製造及び使用方法 - Google Patents
生分解性テレフタレートポリエステル−ポリホスフェートポリマー、組成物、物品、並びにその製造及び使用方法Info
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- JP2001519842A JP2001519842A JP54194998A JP54194998A JP2001519842A JP 2001519842 A JP2001519842 A JP 2001519842A JP 54194998 A JP54194998 A JP 54194998A JP 54194998 A JP54194998 A JP 54194998A JP 2001519842 A JP2001519842 A JP 2001519842A
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- C08L85/02—Compositions of macromolecular compounds obtained by reactions forming a linkage in the main chain of the macromolecule containing atoms other than silicon, sulfur, nitrogen, oxygen and carbon; Compositions of derivatives of such polymers containing phosphorus
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Abstract
Description
Claims (1)
- 【特許請求の範囲】 1.式Iに示される繰返しモノマー単位からなる生分解性テレフタレートポリ マー 式中、Rは2価の有機部分であり、 R'は脂肪族、芳香族又は複素環式残基であり、xは≧1であり、 そしてnは0〜5,000であり、 この生分解性ポリマーは生分解前及び生分解の際に生体適合性を有している。 2.Rがアルキレン基、脂環式基、フェニレン基又は下記の式の2価の基であ る請求の範囲第1項のポリマー。 式中、Xは酸素、窒素又は硫黄であり、nは1ないし3である。 3.Rが1いないし7の炭素原子を有するアルキレン基である請求の範囲第1 項のポリマー。 4.Rがエチレン基である請求の範囲第1項のポリマー。 5.Rがn−プロピレン基である請求の範囲第1項のポリマー。 6.Rが2−メチルプロピレンである請求の範囲第1項のポリマー。 7.Rが2,2'−ジメチルプロピレンである請求の範囲第1項のポリマー。 8.R'がアルキル基又はフェニル基である請求の範囲第1項のポリマー。 9.R'が1ないし7の炭素原子を有するアルキル基である請求の範囲第1項 のポリマー。 10.R'がエチル基である請求の範囲第1項のポリマー。 11.xが約1から約30である請求の範囲第1項のポリマー。 12.xが約1から約20である請求の範囲第1項のポリマー。 13.xが約2から約20である請求の範囲第1項のポリマー。 14.前記のポリマーが溶液重合法で製造されたものである請求の範囲第1項の ポリマー。 15.前記のポリマーがさらに生体適合性モノマー単位を含んでいる請求の範囲 第1項のポリマー。 16.前記のポリマーが、アセトン、ジメチレンクロライド、クロロホルム、酢 酸エチル、DMAC、N−メチルピロリドン、ジメチルホルムアミド及びジメチ ルスルホキシドよりなる群から選ばれた溶媒の少なくとも1つに溶けるものであ る請求の範囲第1項のポリマー。 17.式Iの繰返しモノマー単位からなり、 式中、Rは2価の有機部分であり、 R'は脂肪族、芳香族又は複素環式残基であり、xは≧1であり、 そしてnは0〜5,000であり、 生分解前及び生分解の際に生物適応性を有している生分解性テレフタレートポリ マーの製造方法であって、 式IIを有するジオール化合物 式中、Rは前記の定義の通りである のpモルと、式IIIのホスホロジクロリデート 式中、R'は前記の定義の通りであり、p>qのqモルを重合させて下記に示 す式IVのホモポリマー 式中、R,R'及びxは前記定義の通りである のqモルを生成させる工程よりなることを特徴とする 前記生分解性テレフタレートポリマーの製造方法。 18.Rが1ないし7の炭素原子を有するアルキレン基である請求の範囲第17項 の方法。 19.Rがエチレン基である請求の範囲第17項の方法。 20.Rがn−プロピレン基である請求の範囲第17項の方法。 21.Rが2−メチルプロピレンである請求の範囲第17項の方法。 22.Rが2,2'−ジメチルプロピレンである請求の範囲第17項の方法。 23.R'が1ないし7の炭素原子を有するアルキル基である請求の範囲第17項 の方法。 24.R'がエチル基である請求の範囲第17項の方法。 25.xが約1から約40である請求の範囲第17項の方法。 26.前記の重合反応が約−40から約+160℃の温度で行なわれる請求の範囲第1 7項の方法。 27.重合温度が約0から65℃まで変化する請求の範囲第17項の方法。 28.前記の重合が約30分と24時間の間の時間で行なわれる請求の範囲第17項の 方法。 29.前記の重合が溶液重合反応である請求の範囲第17項の方法。 30.酸受容体が存在する請求の範囲第17項の方法。 31.酸受容体が第3アミンである請求の範囲第17項の方法。 32.式Iの繰返しモノマー単位からなり、 式中、Rは2価の有機部分であり、 R'は脂肪族、芳香族又は複素環式残基であり、xは≧1であり、 そしてnは0〜5,000であり、 生分解前及び生分解の際に生体適合性を有している生分解性テレフタレートポリ マーの製造方法であって、 この方法は、 (a) 式IIを有するジオール化合物 式中、R'は前記の定義の通りである のpモルと、式IVのホスホロジクロリデート 式中、R'は前記の定義の通りであり、p>qのqモルを重合させて下記に示 す式IVのホモポリマー 式中、R,R'及びxは前記定義の通りである のqモルを生成させ、そして (b) 式IVの前記ポリマーと式IIの過剰ジオールを、式V を有するテレフタロイルクロライドの(p−q)モルとさらに反応させて前記の 式Iのポリマーを生成させることを特徴とする前記生分解性テレフタレートポリ マーの製造方法。 33.Rが1ないし7の炭素原子を有するアルキレン基である請求の範囲第32項 の方法。 34.Rがエチレン基である請求の範囲第32項の方法。 35.Rがn−プロピレン基である請求の範囲第32項の方法。 36.Rが2−メチルプロピレンである請求の範囲第32項の方法。 37.Rが2,2'−ジメチルプロピレンである請求の範囲第32項の方法。 38.R'が1ないし7の炭素原子を有するアルキル基である請求の範囲第32項 の方法。 39.R'がエチル基である請求の範囲第32項の方法。 40.xが約1から約30である請求の範囲第32項の方法。 41.xが約2から約20である請求の範囲第32項の方法。 42.前記のステップ(a)の重合反応が約−40から約+160℃の温度で行なわ れる請求の範囲第32項の方法。 43.重合ステップ(a)の温度が約0から65℃まで変化する請求の範囲第32項 の方法。 44.前記の重合スッテプ(a)が約30分と24時間の間の時間で行なわれる請求 の範囲第32項の方法。 45.前記の重合ステップ(a)が溶液重合反応である請求の範囲第32項の方法 。 46.酸受容体が前記の重合ステップ(a)の間に存在する請求の範囲第32項の 方法。 47.酸受容体が第3アミンである請求の範囲第32項の方法。 48.前記のステップ(b)共重合が約−40と100℃の間の温度で行なわれる請 求の範囲第32項の方法。 49.前記ステップ(b)共重合が約30分と24時間の間に行なわれる請求の範囲 第32項の方法。 50.前記の式Iのポリマーがこのポリマーの溶液を非溶媒又は部分溶媒で急冷 することによって精製される請求の範囲第32項の方法。 51.請求の範囲第1項のポリマーよりなる生体吸収性縫合糸。 52.請求の範囲第1項のポリマーよりなる骨及び結合組織の損傷の修復用整形 外科用器具、骨セメント又は骨ワックス。 53.請求の範囲第1項のポリマーよりなる分解性又は非分解性布用積層物。 54.請求の範囲第1項のポリマーよりなる移植器具用コーティング。 55.次の成分よりなる生分解性テレフタレートポリマー組成物。 (a)少なくとも1つの生物学的に活性な物質及び (b)式Iに示される繰返しモノマー単位を有するポリマー 式中、Rは2価の有機部分であり、R'は脂肪族、芳香族又は複素乾式残基で あり、xは≧1であり、そしてnは0〜5,000であり、 このポリマーは生分解の前及び生分解の際に生体適合性を有している。 56.Rがアルキレン基、脂環式基、フェニレン基又は下記の式の2価の基である 請求の範囲第55項のポリマー組成物。 式中、Xは酸素、窒素又は硫黄であり、nは1ないし3である請求の範囲第55 項のポリマー組成物。 57.Rがエチレン基である請求の範囲第55項のポリマー組成物。 58.Rがn−プロピレン基である請求の範囲第55項のポリマー組成物。 59.Rが2−メチルプロピレンである請求の範囲第55項のポリマー組成物。 60.Rが2,2'−ジメチルプロピレンである請求の範囲第55項のポリマー組成 物。 61.R'がアルキル基又はフェニル基である請求の範囲第55項のポリマー組成 物。 62.R'がエチル基である請求の範囲第55項のポリマー組成物。 63.xが約1から約30である請求の範囲第55項のポリマー組成物。 64.前記のコポリマーが溶液重合法で製造されたものである請求の範囲第55項 のポリマー組成物。 65.前記のポリマーがさらに生体適合性モノマー単位を含んでいる請求の範囲 第1項のポリマー組成物。 66.前記のポリマーが、アセトン、ジメチレンクロライド、クロロホルム、酢 酸エチル、DMAC、N−メチルピロリドン、ジメチルホルムアミド及びジメチ ルスルホキシドよりなる群から選ばれた溶媒の少なくとも1つに溶けるものであ る請求の範囲第55項のポリマー組成物。 67.前記の生物学的に活性な物質がペプチド、ポリペプチド、蛋白、アミノ酸 、多糖類、成長因子、ホルモン、抗脈管形成因子、インターフェロン又はサイト カイニン、及びこれらの物質のプロ医薬よりなる群から選ばれたものである請求 の範囲第55項のポリマー組成物。 68.前記の生物学的に活性な物質が治療薬又はプロ医薬である請求の 範囲第55項のポリマー組成物。 69.前記の医薬が抗新生物剤、抗生物質、抗ウイルス剤、抗菌剤、抗炎症剤及 び抗凝固剤よりなる群から選ばれたものである請求の範囲第68項のポリマー組成 物。 70.前記の生物学的に活性な物質と前記のポリマーが物質なマトリックスを形 成している請求の範囲第55項のポリマー組成物。 71.前記のポリマーが、生分解中のこのポリマーのホスホエステル結合の加水 分解作用として少なくとも部分的にコントロールされているインビボでのこの生 物学的に活性な物質の放出速度によって特徴づけられている請求の範囲第55項の ポリマー組成物。 72.次の成分よりなる生分解性テレフタレートポリマー組成物よりなる、移植 、注入、又は体内に全体もしくは1部を設置する他の物に有用な物品。 (a)少なくとも1つの生物学的に活性な物質及び (b)式Iに示される繰返しモノマー単位を有するポリマー 式中、Rは2価の有機部分であり、 R'は脂肪族、芳香族又は複素環式残基であり、xは≧1であり、そして nは0〜5,000であり、 このポリマーは生分解の際に生体・適合性を有するこの生分解性組成物をつく るのに充分なほど純粋である。 73.Rがアルキレン基、脂環式基、フェニレン基又は下記の式の2価の基であ る請求の範囲第55項のポリマー組成物。 式中、Xは酸素、窒素又は硫黄であり、nは1ないし3である請求の範囲第72 項の物品。 74.Rがエチレン基である請求の範囲第72項の物品。 75.Rがn−プロピレン基である請求の範囲第72項の物品。 76.Rが2−メチルプロピレンである請求の範囲第72項の物品。 77.Rが2,2'−ジメチルプロピレンである請求の範囲第72項の物品。 78.R'がアルキル基又はフェニル基である請求の範囲第72項の物品。 79.R'がエチル基である請求の範囲第72項の物品。 80.xが約1から約30である請求の範囲第72項の物品。 81.xが約2から約20である請求の範囲第72項の物品。 82.前記のポリマーが溶液重合法で製造されたものである請求の範囲第72項の 物品。 83.前記のポリマーがさらに生体適合性モノマー単位を含んでいる請求の範囲 第72項の物品。 84.前記のポリマーが、アセトン、ジメチレンクロライド、クロロホルム、酢 酸エチル、DMAC、N−メチルピロリドン、ジメチルホルムアミド及びジメチ ルスルホキシドよりなる群から選ばれた溶媒の少なくとも1つに溶けるものであ る請求の範囲第72項の物品。 85.前記の生物学的に活性な物質がペプチド、ポリペプチド、蛋白、アミノ酸 、多糖類、成長因子、ホルモン、抗脈管形成因子、インターフェロン又はサイト カイニン、及びこれらの物質のプロ医薬よりなる群から選ばれたものである請求 の範囲第72項の物品。 86.前記の生物学的に活性な物質が治療薬又はプロ医薬である請求の 範囲第72項の物品。 87.前記の生物学的に活性な物質が抗新生物剤、抗生物質、抗ウイルス剤、抗 菌剤、抗炎症剤、抗凝固剤及びこれらの物質のプロ医薬よりなる群から選ばれた ものである請求の範囲第86項の物品。 88.前記の生物学的に活性な物質と前記のポリマーが物質なマトリックスを形 成している請求の範囲第72項の物品。 89.前記の生物学的に活性な物質が前記のポリマー内にカプセル化されている 請求の範囲第72項の物品。 90.前記のポリマーが、生分解中のこのポリマーのホスホエステル結合の加水 分解作用として少なくとも部分的にコントロールされているインビボでのこの生 物学的に活性な物質の放出速度によって特徴づけられている請求の範囲第72項の 物品。 91.前記の物品が動物の体内への移植又は注入用のものである請求の範囲第72 項の物品。 92.前記の物品が血管の多い組織に移植され又は注入されたときの組織への刺 激が最小化されている請求の範囲第72項の物品。 93.前記の物品が分解性布用の積層物の形をしている請求の範囲第72項の物品 。 94.前記の物品が生体吸収可能な縫合糸、骨の損傷修復用材料又は移植器具の コーティングである請求の範囲第72項の物品。 95.次のステップよりなる生物学的に活性な物質のコントロールされた放出方 法。 (a)生物学的に活性な物質に式Iに示される繰返しモノマー単位を有する生分 解性テレフタレートポリマーを組み合わせて混合物をつくり、 式中、Rは2価の有機部分であり、R'は脂肪族、芳香族又は複素環式残基であ り、xは≧1であり、そしてnは0〜5,000であり、 前記のポリマーは生分解の前及び生分解の際に生体適合性である。 (b)前記の混合物を成形して固形物品にし、そして、 (c)前記の固形物品を、予め選定した部位に、この固形の移植又は注入されたマ トリックスが生物学的液と少なくとも1部が接触するように、インビボで移植又 は注入する。 96.Rがエチレン基である請求の範囲第95項の方法。 97.Rがn−プロピレン基である請求の範囲第96項の方法。 98.Rが2−メチルプロピレンである請求の範囲第96項の方法。 99.Rが2,2'−ジメチルプロピレンである請求の範囲第96項の方法。 100.R'がエチル基である請求の範囲第96項の方法。 101.xが約1から約30である請求の範囲第96の項方法。 102.比率が約10:1から約1:1である請求の範囲第96項の方法。 103.前記ポリマーがさらに生体適合性基を含んでいる請求の範囲第96項の方 法。 104.前記の生物学的に活性な物質がペプチド、ポリペプチド、蛋白、アミノ 酸、多糖類、成長因子、ホルモン、抗脈管形成因子と他の抗新生物剤、インター フェロン又はサイトカイニン、及びこれらの物質のプロ医薬よりなる群から選ば れたものである請求の範囲第96項の方法。 105.前記の生物学的に活性な物質が治療薬又はプロ医薬である請求の範囲第9 6項の方法。 106.前記の医薬が化学療法剤、抗生物質、抗ウイルス剤、抗菌剤、抗炎症剤 及び抗凝固剤よりなる群から選ばれたものである請求の範囲第96項の方法。 107.前記の生物学的に活性な物質と前記のポリマーが均質なマトリックスを 形成している請求の範囲第96項の方法。 108.前記の生物学的に活性な物質が前記のポリマー内にカプセル化されてい る請求の範囲第96項の方法。 109.前記のポリマーが、生分解中のこのポリマーのホスホエステル結合の加 水分解作用として少なくとも部分的にコントロールされているインビボでのこの 生物学的に活性な物質の放出速度によって特徴づけられている請求の範囲第96項 の方法。 110.前記の物品が無毒であり、血管の多い組織に移植され又は注入されたと きの組織への刺激が最小化されている請求の範囲第96項の方法。 111.前記の物品が分解性布用の積層物である請求の範囲第96項の方法。 112.前記のポリマー組成物が移植物用のコーティングである請求の範囲第96項 の方法。 113.このポリマー組成物が癒着防止用のバリヤーとして使用されるものであ る請求の範囲第96項の方法。 114.前記のポリマー組成物が神経発生用チューブとして成形されている請求 の範囲第96項の方法。
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- 1998-04-02 US US09/053,648 patent/US6322797B1/en not_active Expired - Lifetime
- 1998-04-02 WO PCT/US1998/006381 patent/WO1998044021A1/en active IP Right Grant
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- 1998-04-02 CA CA 2285903 patent/CA2285903A1/en not_active Abandoned
- 1998-04-02 CN CN98805193A patent/CN1256700A/zh active Pending
- 1998-04-02 AU AU69450/98A patent/AU741145B2/en not_active Ceased
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- 1998-04-02 HU HU0001256A patent/HUP0001256A3/hu unknown
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- 1998-04-02 JP JP54194998A patent/JP4496316B2/ja not_active Expired - Fee Related
- 1998-04-02 BR BR9809064A patent/BR9809064A/pt not_active Application Discontinuation
- 1998-07-02 TW TW87105028A patent/TW534915B/zh active
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1999
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Cited By (4)
Publication number | Priority date | Publication date | Assignee | Title |
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JP2007517902A (ja) * | 2004-01-12 | 2007-07-05 | 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 | 長期間送達製剤及びその使用方法 |
JP2011173930A (ja) * | 2004-01-12 | 2011-09-08 | Trustees Of The Univ Of Pennsylvania | 長期間送達製剤及びその使用方法 |
JP2007535368A (ja) * | 2004-04-30 | 2007-12-06 | アドヴァンスド カーディオヴァスキュラー システムズ, インコーポレイテッド | 埋め込み型用具上のコーティングの熱特性及び機械的特性を調節する方法 |
US8815274B2 (en) | 2004-04-30 | 2014-08-26 | Advanced Cardiovascular Systems, Inc. | Poly(ester amides) for the control of agent-release from polymeric compositions |
Also Published As
Publication number | Publication date |
---|---|
US6600010B2 (en) | 2003-07-29 |
CN1256700A (zh) | 2000-06-14 |
EP0973818A1 (en) | 2000-01-26 |
NO994802L (no) | 1999-12-03 |
ATE279461T1 (de) | 2004-10-15 |
NO994802D0 (no) | 1999-10-01 |
AU6945098A (en) | 1998-10-22 |
CA2285903A1 (en) | 1998-10-08 |
AU741145B2 (en) | 2001-11-22 |
IL132120A0 (en) | 2001-03-19 |
DE69826994D1 (de) | 2004-11-18 |
WO1998044021A9 (en) | 1999-04-22 |
DE69826994T2 (de) | 2005-12-08 |
KR20010006026A (ko) | 2001-01-15 |
NZ500649A (en) | 2001-05-25 |
HUP0001256A3 (en) | 2002-12-28 |
WO1998044021A1 (en) | 1998-10-08 |
BR9809064A (pt) | 2002-01-02 |
EP0973818B1 (en) | 2004-10-13 |
JP4496316B2 (ja) | 2010-07-07 |
US6322797B1 (en) | 2001-11-27 |
HUP0001256A2 (hu) | 2002-01-28 |
US20020091230A1 (en) | 2002-07-11 |
TW534915B (en) | 2003-06-01 |
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