KR910002432A - 국소투여용 약제학적 제제 - Google Patents

국소투여용 약제학적 제제 Download PDF

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KR910002432A
KR910002432A KR1019900010204A KR900010204A KR910002432A KR 910002432 A KR910002432 A KR 910002432A KR 1019900010204 A KR1019900010204 A KR 1019900010204A KR 900010204 A KR900010204 A KR 900010204A KR 910002432 A KR910002432 A KR 910002432A
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diphosphonic acid
amino
alkyl
substituted
hydroxy
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지오르지오 페리니 피에르
보엘미 카를로
하인리히 스탈 피터
그린 조나단
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베르너 발데그
시바-가이기 에이지
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Abstract

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Description

국소투여용 약제학적 제제
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (18)

  1. 약제학적으로 허용되는 일반식(I)의 메탄디포스폰산 유도체 및 이의 염을 함유하는 국소투여용 약제학적 제제.
    상기식에서, R1및 R2는 할로겐이거나, R1은 수소이고, R2는 Ar-S- 또는 Het1-NH-[여기에서, Ar은 비치환 되거나 치환된 페닐이며, Het1은 환탄소원자를 통하여 결합되는 비치환되거나 치환된 모노사이클릭 5- 또는 6-원 모노아자-, 디아자- 또는 티아자-아릴이다]이거나, R1은 수소 또는 하이드록시이고, R2는 -A-R3[여기에서, A는 알킬렌이고, R3은 Het2(이는 환 탄소원자 또는 환 질소원자를 통하여 결합된 Het1이다)이거나, R3은 수소, 또는 알킬, 사이클로알킬, Ar-알킬, Ar-O-알킬, Ar-S-알킬 및 Het1-알킬 중에서 선택된 동일하거나 상이한 치환체에 의해 일치환 또는 이치환되거나 비치환된 아미노 또는 Ar함유 알킬렌에 의해 임의로 이치환된 아미노이며, 여기서, 두 개의 알킬렌 탄소원자는 알킬렌을 통하여 추가로 서로 연결될 수 있고 Ar 및 Het1은 각각 상기에서 정의한 바와 같다]인데, 단 R2가 -A-R3이고 A가 에틸렌이며 R3이 비치환되거나 C1-C3알킬 치환된 아미노일 경우, R1은 하이드록시가 아니다.
  2. 제1항에 있어서, R1및 R2는 할로겐이거나, R1은 수소이고 R2가 Ar-S- 또는 Het1-NH(여기서, Ar은 비치환되거나 치환된 페닐이며, Het1은 환 탄소원자를 통하여 결합되는 비치환되거나 치환된 모노사이클릭 5- 또는 6-원 모노아자-, 디아자- 또는 티아자-아릴이다)이거나, R1은 수소 또는 하이드록시이며, R2가 -A-R3[여기에서, A는 알킬렌이고, R3은 Het2(이는 환 탄소원자 또는 환 질소원자를 통하여 결합된 Het1이다)이거나, R3은 수소, 또는 알킬, Ar-알킬, Ar-O-알킬 및 Het1-알킬 중에서 선택된 동일하거나 상이한 치환제에 의해 일치환 또는 이치환되거나 비치환된 아미노 또는 Ar함유 알킬렌에 의해 임의로 이치환된 아미노이며, (여기서, 두 개의 알킬렌 탄소원자는 알킬렌을 통하여 추가로 서로 연결될 수 있으며 Ar 및 Het1은 상기에서 정의한 바와 같다]인 일반식(I)의 화합물 또는 이의 염을 함유하는 제제.
  3. 제2항에 있어서, R1및 R2는 할로겐이거나, R1은 수소이고 R2가 Ar-S- 또는 Het1-NH-(여기에서, Ar은 저급알킬, 저급알콕시, 트리풀루오로메틸 및/또는 특히, 할로겐에 의해 치환되거나 비치환된 페닐이고, Het1은 비치환되거나 저급알킬 치환된 타아졸릴이다)이거나, R1은 수도 또는 하이드록시이고, R2가 -A-R3[여기에서, A는 저급 알킬렌이고, R3은 비치환되거나 환 탄소원자 또는 환 질소원자를 통하여 결합되는 저급 알킬 치환된 이미다졸릴, 또는 피리딜이거나 R3은 수소, 또는 저급 알킬, C3-C7-사이클로알킬, Ar-저급알킬, Ar-O-저급알킬 및 피리딜 저급 알킬 중에서 선택된 동일하거나 상기한 치환체에 의해 일치환 또는 이치환되거나 비치환된 아미노, 또는 Ar함유 저급 알킬렌에 의해 임의로 이치환되거나 저급 알킬렌에 의해 임의로 이치환되는 (이때, 인접하지 않은 두 개의 저급 알킬렌 탄소원자는 저급 알킬렌을 통하여 추가로 서로 연결된다)아미노이며, 각각의 경우에 Ar은 상기에서 정의한 바와 같다]인 일반식(I)의 화합물 또는 이의 염을 함유하는 제제.
  4. 제3항에 있어서, R1이 수소 또는 하이드록시이고 R2가 -A-R3[여기에서, A는 저급 알킬렌이고, R3은 저급 알킬, Ar-저급알킬, C3-C7-사이클로알킬, Ar-O-저급알킬, Ar-S-저급 알킬 및 피리딜-저급알킬중에서 선택된 동일하거나 상이한 치환체에 의해 일치환 또는 이치환된 아미노이다]인 일반식(I)의 화합물 또는 이의 염을 함유하는 제제.
  5. 제2항에 있어서, R1및 R2가 각각 할로겐, 특히 염소이거나, R1이 수소이고 R2가 할로겐(예 : 염소)에 의해 치환되거나 비치환된 페닐티오(예:4-클로로페닐티오) 또는 저급알킬, 특히 C1-C4알킬 (예:메틸)에 의해 치환되거나 비치환된 티아졸릴아미노 (예: 티아졸-2-일-, 5-n-부틸티아졸-2-일- 또는 5-메틸타아졸-2-일-아미노)이거나, R1이 수소 또는 아이드록시이며, R2가 -A-R3[여기에서, A는 C1-C7알킬렌(예: 메틸렌, 에틸렌, 프로필렌 또는 펜틸렌)이고 R3은 환 탄소원자 또는 환 질소원자를 통하여 결합되고 저급 알킬, 특히 C1-C1알킬(예: 메틸)에 의해 치환되거나 비치환된 이미다졸릴(예: 이미다졸-1-일, 이미다졸-5-일, 1-메틸이미다졸-2-일 또는 4-메틸이미다졸-5-일)또는 피리딜(예: 2- 또는 3-피리딜)이다]이거나, R1이 하이드록시이며 R2가 -A-R3[여기에서, A는 상기에서 정의한 바와 같고 R3은 아미노, 디-C1-C5-알킬아미노 (예: 디메틸아미노), N-메틸-N-n-프로필아미노 또는 N-메틸-N-n-펜탈아미노, N-C1-C4알킬-N-페닐-C1-C5알킬아미노(예 : N-메틸-N-(3-페닐프로필)아미노 또는 N-메틸-N-(5-페닐펜틸)-아미노), N-C1-C4알킬-N-피리딜-C1-C4알킬-아미노(예: N-메틸-N-[3-(2-피리딜)-프로필]-아미노), 할로겐(예: 염소)을 함유할 수 있는 페닐(예:4-클로로페닐)에 의해 치환되거나 비치환되는 C4-C6알킬렌아미노, 예를들면, 특히 4위치에서 페닐에 의해 치환되거나 비치환된 피페리딘-1-일 또는 특히 3위치에서 4-클로로페닐에 의해 치환되거나 비치환된 피롤리딘-1-일, 또는 1.5-디-C1-C4알킬-(예: 1.5-디메틸-3-아자비사이클로[3.1.1]헵트-3-일)이다]이거나 R1이 하이드록시이고 R2가 -A-R3(여기서, A는 C1-C4알킬렌, 특히 메틸렌이며, R3은 수소이다)인 일반식(I)의 화합물 또는 이의 염, 특히 알칼리 금속염(예: 나트륨염)을 함유하는 제제.
  6. 제5항에 있어서, R1이 수소 또는 하이드록시이고, R2가 -A-R3(여기에서, A는 C1-C7알킬렌(예: 메틸렌, 에틸렌, 프로필렌 또는 페틸렌)이고 R3은 N-C3-C7-사이클로알킬아미노(예: 사이클로헵틸아미노) 또는 N-C1-C1알킬-N-페닐티오-C1-C1알킬(예: N-메틸-N-(2-페닐티오에틸)-아미노)이다]인 일반식(I)의 화합물 또는 이의 염을 함유하는 제제.
  7. 제2항에 있어서, R1이 하이드록시이고, R2가 -A-R3[여기에서, A는 C1-C7알킬렌(예: 에틸렌, 프로필렌 또는 펜틸렌)이고 R3은 아니모, 디-C1-C4알킬아미노(예: 디메틸-또는N-메틸-N-n-프로필-아미노) 또는 N-C1-C1알킬-N-페닐-C1-C4알킬아미노 (예: N-메틸-N-(3-페닐프로필)-아미노)이다]인 일반식(I)의 화합물 또는 이의 염, 특히 알칼리 금속염(예: 나트륨 염)을 함유하는 제제.
  8. 제2항에 있어서, R1이 하이드록시이고, R2가 -A-R3[여기서, A는 C1-C7알킬렌, 특히 C1-C4알킬렌(예: 메틸렌)이고 R3은 환 탄소원자 또는 환 질소원자를 통하여 결합되고, C1-C4알킬(예: 메틸)에 의해 치환되거나 비치환된 이미다졸릴(예: 이미다졸-1-일, 이미다졸-5-일, 1-메틸이미다졸-2-일 또는 4-메틸이미다졸-5-일)이다]인 일반식(I)의 화합물 또는 이의 염, 특히 알칼리 금속염(예: 나트륨염)을 함유하는 제제.
  9. 제2항에 있어서, 하기 일반식(I)의 화합물중에서 선택된 약제학적으로 유효한 메탄디포스폰산 또는 약제학적으로 허용되는 이의 염을 함유하는 제제, 4-아미노-1-하이드록시부탄-1,1-디포스폰산, 6-아미노-1-하이드록시헥산-1,1-디포스폰산, 3-(N-메틸-N-n-펜탈아미노)-1-하이드록시프로판-1,1-디포스폰산, 3-[N-(3-페닐프로필)-N-메틸아미노]-1-하이드록시프로판-1,1-디포스폰산, 3-(N-메틸-N-5-페닐펜틸아미노)-1-하이드록시프로판-1,1-디프스폰산, 3-[N-메틸-N-3-(2-피리딜)-프로필아미노)-1-하이드록시프로판-1,1-디포스폰산, 1-하이드록시-3-[N-메틸-N-(3-펜옥시프로필)-아미노]-프로판-1,1-디포스폰산, 1-하이드록시-3-[N-메틸-N-(2-페옥시에틸)-아미노]-프로판-1,1-디포스폰산, 4-(4-페닐-피페리딘-1-일)-1-하이드록시부탄-1,1-디포스폰산, 1-하이드록시-3-(1-피페라디노)-프로판-1,1-디포스폰산, 1-하이드록시-3-[3-(4-클로로페닐)-피롤리딘-1-일]-프로판-1,1-디포스폰산, 1-하이드록시-2-(이미다졸-1-일)-에탄-1,1-디포스폰산, 2-(1-메틸이미다졸-2-일)-에탄-1,1-디포스폰산, 1-하이드록시-2-(4-메틸이미다졸-5-일)-에탄-1,1-디포스폰산, 1-하이드록시-2-(이미다졸-5-일)-에탄-1,1-디포스폰산, 1-하이드록시-2-(3-피리딜)-에탄-1,1-디포스폰산, 2-(2-피리딜)-에탄-1,1-디포스폰산, 1-[(5-n-부틸-2-티아졸릴)-아미노]-메탄-1,1-디포스폰산, 1-[(5-메틸-2-티아졸릴)-아미노]-메탄-1,1-디포스폰산, 1-[(2-타아졸릴)-아미노]-메탄-1,1-디포스폰산, 1-하이드록시에탄-1,1-디포스폰산, 1-(4-클로로페닐티오)-메탄-1,1-디포스폰산, 1,1-디클로로메탄-1,1-디포스폰산 또는 3-(1,5-디메틸-3-아자비사이클로[3,1,1]-헵트-3-일)-1-하이드록시프로판-1,1-디포스폰산, 및 또한 1[(5-에틸-2-티아졸릴)-아미노]-메탄-1,1-디포스폰산, 3-[N-(2-페닐에틸)-N-메틸아미노]-1-하이드록시프로판-1,1-디포스폰산, 3-[N-(2-페닐티오에틸)-N-메틸아미노]-1-하이드록시프로판-1,1-디포스폰산 또는 1-하이드록시-3-(피롤리딘-1-일)-프로판-1,1-디포스폰산2-(N-사이클로헵틸아미노)-에탄-1,1-디포스폰사.
  10. 제1항에 있어서, 하기 일반식(I)의 화합물중에서 선택된 약제학적으로 유효한 메탄디포스폰산 또는 약제학적으로 허용되는 이의 염을 함유하는 제제, 1-[(5-에틸-2-티아졸릴)-아미노]-메탄-1, 1-디포스폰산, 3-[N-(2-페닐에틸)-N-메틸아미노]-1-하이드록시프로판-1,1-디포스폰산 및 3-[N-(2-페닐티오에틸)-N-메닐아미노]-1-하이드록시프로판-1,1-디포스폰산, 1-하이드록시-3-(피롤리딘-1-일)-프로판-1,1-디포스폰산 및 2-(N-사이클로헵틸아미노)-에탄-1,1-디포스폰산.
  11. 제2항에 있어서, 1-하이드록시-2-(이미다졸-1-일)-에탄-1,1-디포스폰산 또는 약제학적으로 허용되는 이의 염을 함유하는 제제.
  12. 크림, 겔, 연고, 로션, 페이스트, 발포체, 팅크제, 미세 유액 또는 용액의 형태로 존재하는 제1항 내지 제11항 중의 어느 한 항에 따르는 제제.
  13. 경피투여용 다층 치료학적 시스템 형태로 존재하는 제1항 내지 제11항중의 어느 한 항에 따르는 제제.
  14. 제13항에 있어서, 경피투여용 다층 치료학적 시스템이 하기 구성성분을 포함하는 제제. (1) 활성성분 제형의 구성성분의 연속 층을 투과할수 없는 밀폐된 이면(backing)호일, (2) 활성성분이 접착성 호일에 미리 존재하지 않을 경우, 이면 호일 다음에 존재하는 활성 성분 저장기, (3) 접착층 및 (4) 박리성 보호 호일.
  15. 매트릭스형 또는 막형의 경피투여용 다층 치료학적 시스템 형태로 존재하는 제1항 내지 제11항, 제13항 및 제14항 중의 어느 한 항에 따르는 제제.
  16. 실시예에서 기술된 약제학적 제제 및 이의 제조방법.
  17. 제1항 내지 제16항 중의 어느 한 항에 따르는 일반식(I)의 화합물 또는 이의 염을 국소투여용 약제학적 조성물에 혼입한 다음, 이를 사람을 포함한 온혈동물에게 적용시킴을 특징으로 하여 약제학적으로 허용되는 일반식(I)의 메탄디포스폰산 유도체의 흡수를 증가시키는 방법.
  18. 과칼슘혈증과 골연화성 골전이층 치료에 있어서의 제1항 내지 제16항중 어느 한항에 따른 국소투여용 약제학적 제제의 용도.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019900010204A 1989-07-07 1990-07-06 국소투여용 약제학적 제제 KR910002432A (ko)

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Families Citing this family (76)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH05194563A (ja) * 1991-07-12 1993-08-03 Hoechst Ag 置換アミノエタン−１，１−ビスホスホン酸およびアミノエタン−１，１−アルキルホスフィノホスホン酸
US5328696A (en) * 1991-07-22 1994-07-12 Dow Corning Corporation Devices using silicone pressure sensitive adhesives containing organic wax
EP0529437B1 (en) * 1991-08-14 1996-07-17 Kao Corporation Hair treatment composition
ATE165603T1 (de) * 1991-09-05 1998-05-15 Toray Industries Methandiphosphonsäurederivat, herstellung davon und verwendung davon als arzneimittel
US6096342A (en) * 1997-03-12 2000-08-01 The Procter & Gamble Company Dosage forms of risedronate
WO1993009785A1 (en) * 1991-11-22 1993-05-27 Procter & Gamble Pharmaceuticals, Inc. Risedronate delayed-release compositions
TW237386B (ko) * 1992-04-15 1995-01-01 Ciba Geigy
US5283057A (en) * 1992-04-24 1994-02-01 The Procter & Gamble Company Risedronate in oral compositions
GB9215433D0 (en) * 1992-07-21 1992-09-02 Cmb Foodcan Plc Apparatus for stripping a drawn article from a punch
AU670337B2 (en) 1992-11-30 1996-07-11 Novartis Ag Use of certain methanebisphosphonic acid derivatives in fracture healing
EP0676962B9 (en) * 1992-12-31 2002-04-03 Sunkyong Industries Co., Ltd. Enhanced pharmaceutical compositions for skin penetration for piroxicam
DE4308649C2 (de) * 1993-03-18 1995-11-16 Lohmann Gmbh & Co Kg Medizinisches Pflastermaterial sowie Verfahren zu seiner Herstellung und dessen Verwendung
US5728650A (en) * 1993-10-07 1998-03-17 Zeneca Limited Herbicidal aza bisphosphonic acids and compositions containing the same
HU221029B1 (hu) * 1994-11-09 2002-07-29 The Procter & Gamble Co. Perianális szennyeződések eltávolítására alkalmas víz a lipidben emulzióval kezelt tisztítókendő és eljárás az előállítására
US5948540A (en) * 1995-04-27 1999-09-07 The Procter & Gamble Company Carrier substrate treated with high internal phase inverse emulsions made with an organopolysiloxane-polyoxyalkylene emulsifier
ATE177450T1 (de) * 1995-04-27 1999-03-15 Procter & Gamble Trägersubstrat behandelt mit einer inversen emulsion mit hohem gehalt an diskontinuierlicher wasserphase, die mit einem polyoxyalkylenpolysiloxan-emulgator hergestellt wird
US5980922A (en) * 1996-04-30 1999-11-09 Procter & Gamble Company Cleaning articles treated with a high internal phase inverse emulsion
US5763332A (en) * 1996-04-30 1998-06-09 The Procter & Gamble Company Cleaning articles comprising a polarphobic region and a high internal phase inverse emulsion
US5908707A (en) * 1996-12-05 1999-06-01 The Procter & Gamble Company Cleaning articles comprising a high internal phase inverse emulsion and a carrier with controlled absorbency
US6018679A (en) * 1997-01-29 2000-01-25 Novartis Finance Corp. Iontophoretic transdermal delivery and control of adverse side-effects
US6133166A (en) * 1997-07-01 2000-10-17 The Procter & Gamble Company Cleaning articles comprising a cellulosic fibrous structure having discrete basis weight regions treated with a high internal phase inverse emulsion
JP2001512178A (ja) * 1997-07-31 2001-08-21 ザ、プロクター、エンド、ギャンブル、カンパニー 濡れ清浄製品
SE9703691D0 (sv) * 1997-10-10 1997-10-10 Astra Ab Pharmaceutical compositions
HUP0103143A3 (en) 1998-09-09 2003-01-28 Metabasis Therapeutics Inc San Novel heteroaromatic inhibitors of fructose 1,6-bisphosphatase, process for their preparation and their use
US6495229B1 (en) * 1999-09-17 2002-12-17 Avery Dennison Corporation Pattern coated adhesive article
CN100595204C (zh) * 1999-12-22 2010-03-24 症变治疗公司 双氨基化膦酸酯前药
PE20011061A1 (es) 2000-02-01 2001-11-20 Procter & Gamble Cristalizacion selectiva del acido 3-piridil-1-hidroxi-etiliden-1,1-bisfosfonico sodio como el hemipentahidrato o el monohidrato
US7563774B2 (en) * 2000-06-29 2009-07-21 Metabasis Therapeutics, Inc. Combination of FBPase inhibitors and antidiabetic agents useful for the treatment of diabetes
GB2380526A (en) * 2000-06-30 2003-04-09 Phillip Roy Caskey Improvements in and relating to methods and apparatus for the application of honey to wounds
US8512718B2 (en) 2000-07-03 2013-08-20 Foamix Ltd. Pharmaceutical composition for topical application
US6613347B2 (en) * 2001-02-21 2003-09-02 Tolland Development Company, Llc PVA sponge with low durometer skin silicone
EP1435970A4 (en) * 2001-10-18 2005-05-04 Ilex Products Inc METHOD OF TREATING SKIN WITH DIPHOSPHONATE DERIVATIVES
US20030124174A1 (en) * 2001-10-25 2003-07-03 Endo Pharmaceuticals, Inc Method for treating non-neuropathic pain
AU2003211963A1 (en) 2002-02-14 2003-09-04 Kyukyu Pharmaceutical Co., Ltd. Percutaneous preparations
JP4546704B2 (ja) * 2002-02-14 2010-09-15 救急薬品工業株式会社 経皮投与製剤
IL152486A0 (en) 2002-10-25 2003-05-29 Meir Eini Alcohol-free cosmetic and pharmaceutical foam carrier
US7820145B2 (en) 2003-08-04 2010-10-26 Foamix Ltd. Oleaginous pharmaceutical and cosmetic foam
US9668972B2 (en) 2002-10-25 2017-06-06 Foamix Pharmaceuticals Ltd. Nonsteroidal immunomodulating kit and composition and uses thereof
US8486376B2 (en) 2002-10-25 2013-07-16 Foamix Ltd. Moisturizing foam containing lanolin
US20080138296A1 (en) 2002-10-25 2008-06-12 Foamix Ltd. Foam prepared from nanoemulsions and uses
US7700076B2 (en) 2002-10-25 2010-04-20 Foamix, Ltd. Penetrating pharmaceutical foam
US10117812B2 (en) 2002-10-25 2018-11-06 Foamix Pharmaceuticals Ltd. Foamable composition combining a polar solvent and a hydrophobic carrier
US8119150B2 (en) 2002-10-25 2012-02-21 Foamix Ltd. Non-flammable insecticide composition and uses thereof
US8900554B2 (en) 2002-10-25 2014-12-02 Foamix Pharmaceuticals Ltd. Foamable composition and uses thereof
US8119109B2 (en) 2002-10-25 2012-02-21 Foamix Ltd. Foamable compositions, kits and methods for hyperhidrosis
US9265725B2 (en) 2002-10-25 2016-02-23 Foamix Pharmaceuticals Ltd. Dicarboxylic acid foamable vehicle and pharmaceutical compositions thereof
MXPA05004278A (es) 2002-10-25 2005-10-05 Foamix Ltd Espuma cosmetica y farmaceutica.
US7704518B2 (en) 2003-08-04 2010-04-27 Foamix, Ltd. Foamable vehicle and pharmaceutical compositions thereof
US9211259B2 (en) * 2002-11-29 2015-12-15 Foamix Pharmaceuticals Ltd. Antibiotic kit and composition and uses thereof
CN1738623A (zh) * 2003-01-23 2006-02-22 夏尔控股公司 治疗血小板增多症的制剂和方法
US7575739B2 (en) 2003-04-28 2009-08-18 Foamix Ltd. Foamable iodine composition
US8486374B2 (en) 2003-08-04 2013-07-16 Foamix Ltd. Hydrophilic, non-aqueous pharmaceutical carriers and compositions and uses
US8795693B2 (en) 2003-08-04 2014-08-05 Foamix Ltd. Compositions with modulating agents
US20050112183A1 (en) * 2003-11-25 2005-05-26 Galer Bradley S. Compositions and methods for treating neuropathic sensory loss
US7700608B2 (en) 2004-08-04 2010-04-20 Shire Holdings Ag Quinazoline derivatives and their use in the treatment of thrombocythemia
US20060030574A1 (en) * 2004-08-04 2006-02-09 Shire Holdings Ag Quinazoline derivatives useful for the treatment of peripheral arterial disease and as phosphodiesterase inhibitors
EP1778250A2 (en) * 2004-08-18 2007-05-02 Metabasis Therapeutics, Inc. Novel thiazole inhibitors of fructose 1,6-bisphosphatase
JPWO2008032678A1 (ja) 2006-09-11 2010-01-28 救急薬品工業株式会社 貼付剤
US20080260655A1 (en) 2006-11-14 2008-10-23 Dov Tamarkin Substantially non-aqueous foamable petrolatum based pharmaceutical and cosmetic compositions and their uses
EP2088996A1 (en) * 2006-11-17 2009-08-19 Besins Healthcare Liquid pharmaceutical compositions comprising a bisphosphonate compound
US7910597B2 (en) * 2006-11-28 2011-03-22 Shire Llc Substituted quinazolines
US8304420B2 (en) 2006-11-28 2012-11-06 Shire Llc Substituted quinazolines for reducing platelet count
US8636982B2 (en) 2007-08-07 2014-01-28 Foamix Ltd. Wax foamable vehicle and pharmaceutical compositions thereof
WO2009069006A2 (en) 2007-11-30 2009-06-04 Foamix Ltd. Foam containing benzoyl peroxide
WO2010041141A2 (en) 2008-10-07 2010-04-15 Foamix Ltd. Oil-based foamable carriers and formulations
WO2009072007A2 (en) 2007-12-07 2009-06-11 Foamix Ltd. Carriers, formulations, methods for formulating unstable active agents for external application and uses thereof
FR2926081B1 (fr) * 2008-01-03 2010-02-19 Univ Nantes Derives d'acide hydroxy-bisphosphonique comme vecteur ciblant le tissu osseux
CA2712120A1 (en) 2008-01-14 2009-07-23 Foamix Ltd. Poloxamer foamable pharmaceutical compositions with active agents and/or therapeutic cells and uses
EP2266578A4 (de) * 2008-03-18 2011-08-17 Dikovskiy Aleksander Vladimirovich Pharmazeutische zusammensetzung zur prävention und behandlung von knochenresorption unterschiedlicher ätiologie
US20120087872A1 (en) 2009-04-28 2012-04-12 Foamix Ltd. Foamable Vehicles and Pharmaceutical Compositions Comprising Aprotic Polar Solvents and Uses Thereof
CA2769677A1 (en) 2009-07-29 2011-02-03 Foamix Ltd. Non surface active agent non polymeric agent hydro-alcoholic foamable compositions, breakable foams and their uses
WO2011013009A2 (en) 2009-07-29 2011-02-03 Foamix Ltd. Non surfactant hydro-alcoholic foamable compositions, breakable foams and their uses
BR112012007473A2 (pt) 2009-10-02 2019-05-07 Foamix Ltd composições tópicas de tetraciclina e respectivo método de uso
US9849142B2 (en) 2009-10-02 2017-12-26 Foamix Pharmaceuticals Ltd. Methods for accelerated return of skin integrity and for the treatment of impetigo
US20140243727A1 (en) * 2011-10-12 2014-08-28 Dow Corning Corporation High-viscosity silicone gel adhesive compositions
US10398641B2 (en) 2016-09-08 2019-09-03 Foamix Pharmaceuticals Ltd. Compositions and methods for treating rosacea and acne

Family Cites Families (27)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3683080A (en) * 1970-08-28 1972-08-08 Procter & Gamble Compositions for inhibiting anomalous deposition and mobilization of calcium phosphate in animal tissue
DE2405254C2 (de) * 1974-02-04 1982-05-27 Henkel KGaA, 4000 Düsseldorf Verwendung von 3-Amino-1-Hydroxypropan-1, 1-diphosphonsäure oder ihrer wasserlöslichen Salze bei der Beeinflußung von Calciumstoffwechselstörungen im menschlichen oder tierischen Körper
US4134969A (en) * 1974-02-04 1979-01-16 Henkel Kommanditgesellschaft Auf Aktien (Henkel Kgaa) Method of treatment of calcium disorders using aminoalkane-diphosphonic acids
DE2534391C2 (de) * 1975-08-01 1983-01-13 Henkel KGaA, 4000 Düsseldorf 1-Hydroxy-3-aminoalkan-1,1-diphosphonsäuren
SE7612534L (sv) * 1975-12-01 1977-06-02 Henkel & Cie Gmbh Forfarande for framstellning av farmaceutiska preparat for behandling av storningar i kalciumemnesomsettning
AU2649977A (en) * 1976-07-15 1979-01-04 Procter & Gamble Pharmaceutical composition
DE2813121A1 (de) * 1977-03-29 1978-10-12 Procter & Gamble Verwendung von dichlormethan-diphosphonatverbindungen bei der bekaempfung von collagen-erkrankungen und zur wundheilung
DE2943498C2 (de) * 1979-10-27 1983-01-27 Henkel KGaA, 4000 Düsseldorf Verfahren zur Herstellung von 3-Amino-1-hydroxypropan-1,1-diphosphonsäure
US4634691A (en) * 1980-10-07 1987-01-06 The Procter & Gamble Company Method for inhibiting tumor metastasis
BE890453A (fr) * 1980-10-07 1982-03-22 Procter & Gamble Procede d'inhibition des metastases de cellules tumorales
US4304734A (en) * 1980-10-16 1981-12-08 Vysoka Skola Chemicko-Technologicka 6-Amino-1-hydroxyhexylidene diphosphonic acid, salts and a process for production thereof
DK154260C (da) * 1981-02-20 1989-05-22 Mundipharma Gmbh Fremgangsmaade til fremstilling af et knogleimplantat af braendt tricalciumphosphat, specielt til udfyldning af hulrum eller til sammensaetning af knogledele efter fraktur.
CA1248450A (en) * 1984-04-05 1989-01-10 Kazuo Kigasawa Soft patch
DE3428524A1 (de) * 1984-08-02 1986-02-13 Boehringer Mannheim Gmbh, 6800 Mannheim Neue diphosphonsaeurederivate, verfahren zu deren herstellung und diese verbindungen enthaltende arzneimittel
IL77243A (en) * 1984-12-21 1996-11-14 Procter & Gamble Pharmaceutical compositions containing geminal diphosphonic acid compounds and certain such novel compounds
US4687768A (en) * 1984-12-21 1987-08-18 The Procter & Gamble Company Certain hexahydroindan-2,2-diphosphonic acids useful in treating diseases associated with abnormal calcium and phosphate metabolism
US4597961A (en) * 1985-01-23 1986-07-01 Etscorn Frank T Transcutaneous application of nicotine
DE3512536A1 (de) * 1985-04-06 1986-10-16 Boehringer Mannheim Gmbh, 6800 Mannheim Neue diphosphonsaeure-derivate, verfahren zu deren herstellung und diese verbindungen enthaltende arzneimittel
US4761406A (en) * 1985-06-06 1988-08-02 The Procter & Gamble Company Regimen for treating osteoporosis
DE3623397A1 (de) * 1986-07-11 1988-01-14 Boehringer Mannheim Gmbh Neue diphosphonsaeurederivate, verfahren zu deren herstellung und diese verbindungen enthaltende arzneimittel
GB8618259D0 (en) * 1986-07-25 1986-09-03 Leo Pharm Prod Ltd Pharmaceutical compositions
DE3626058A1 (de) * 1986-08-01 1988-02-11 Boehringer Mannheim Gmbh Neue diphosphonsaeurederivate, verfahren zu deren herstellung und diese verbindungen enthaltende arzneimittel
ATE64397T1 (de) * 1986-11-21 1991-06-15 Ciba Geigy Ag Aromatisch substituierte azacycloalkylalkandiphosphons|uren.
DE3776880D1 (de) * 1986-11-21 1992-04-02 Ciba Geigy Ag Neue substituierte alkandiphosphonsaeuren.
DE3640938A1 (de) * 1986-11-29 1988-06-01 Boehringer Mannheim Gmbh Neue diphosphonsaeurederivate, verfahren zu deren herstellung und diese verbindung enthaltende arzneimittel
EP0317505A1 (de) * 1987-11-13 1989-05-24 Ciba-Geigy Ag Neue Azacycloalkylalkandiphosphonsäuren
US4877618A (en) * 1988-03-18 1989-10-31 Reed Jr Fred D Transdermal drug delivery device

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MX21452A (es) 1994-01-31
IE902481A1 (en) 1991-02-13
EP0407344A2 (de) 1991-01-09
EP0407344A3 (en) 1991-06-12
JPH0344328A (ja) 1991-02-26
NZ234377A (en) 1992-12-23
FI903382A0 (fi) 1990-07-04
PT94611A (pt) 1991-04-18
HU904122D0 (en) 1990-12-28
HUT54502A (en) 1991-03-28
US5133972A (en) 1992-07-28
IL94926A (en) 1994-10-21
ZA905306B (en) 1991-02-27
AU5869890A (en) 1991-01-10
CA2020557A1 (en) 1991-01-08
DD296418A5 (de) 1991-12-05
AU633598B2 (en) 1993-02-04
PT94611B (pt) 1997-02-28

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