| 序号 | 专利名 | 申请号 | 申请日 | 公开（公告）号 | 公开（公告）日 | 发明人 |
|---|---|---|---|---|---|---|
| 81 | Ship1 modulators | JP2004543854 | 2003-04-23 | JP2006506363A | 2006-02-23 | アリス・ムイ; クリストファー・オン; ジェラルド・クリスタル; デイビッド・イー・ウィリアムズ; レイモンド・アンダーセン |
| 本発明は、ＳＨＩＰ１活性のモデュレーターとしてのペロロール、その関連化合物およびその医薬組成物の使用を包含する。 本発明はまた、ＳＨＩＰ１活性をモデュレートすることのできる新規なテルペン化合物およびその合成法をも提供する。 | ||||||
| 82 | Hedgehog antagonist, methods and use for their | JP2002533901 | 2001-10-15 | JP2004529067A | 2004-09-24 | カラバノフ アイリーナ; ペピセリ カーメン; デュデック ヘンリック |
| 本願は、ヘッジホッグ経路を、例えばここに記載したようなヘッジホッグ経路のアンタゴニストを用いて阻害することにより、血管形成を阻止し及び腫瘍を含む望ましくない細胞増殖を治療し又は予防する組成物及び方法に向けられている。 | ||||||
| 83 | Regulator of hedgehog pathway, composition and use about them | JP2000593166 | 2000-01-13 | JP2003517279A | 2003-05-27 | ジー ベンシウ; デュデック ヘンリック |
| (57)【要約】 本願は、ヘッジホッグ機能増進、ｐｔｃ機能喪失又はスムースンド機能増進から生じる異常型の増殖状態を阻止するための利用可能な方法及び試薬であって、細胞を、異常型の増殖状態を制御する(例えば、正常なｐｔｃ経路を作動させ又はスムースンド若しくはヘッジホッグ活性に拮抗する)のに十分な量のポリペプチド又は小分子等の化合物と接触させることを含む、上記の方法及び試薬を作成する。 本発明は、更に、ヘッジホッグ機能喪失、ｐｔｃ機能増進又はスムースンド機能喪失の結果を改善するための利用可能な方法及び試薬であって、細胞を、を改善するのに十分な量のポリペプチド又は小分子等の化合物と接触させることを含む、上記の方法及び試薬を作成する。 ある具体例においては、主題の化合物例えばｃＡＭＰ類似体、アデニレートシクラーゼアゴニスト又はｃＡＭＰホスホジエステラーゼインヒビターは、ｃＡＭＰレベルを調節し、それは、更に、ヘッジホッグ経路の活性を調節する。 | ||||||
| 84 | JPS4818442B1 - | JP8637569 | 1969-10-28 | JPS4818442B1 | 1973-06-06 | |
| 85 | TREATING BRAIN CANCER USING AGELASTATIN A (AA) AND ANALOGUES THEREOF | EP13845901.1 | 2013-10-11 | EP2906564A1 | 2015-08-19 | TUN, Han W.; YOSHIMITSU, Takehiko; SHIGEOKA, Daisuke; KAMON, Takuma; LI, Zhimin; QIU, Yushi; CAULFIELD, Thomas, R. |
| This document relates to compounds and compositions useful for treating cancers, such as brain and nervous system cancers. | ||||||
| 86 | Methods of use for cyclopamine analogs | EP11165825.8 | 2007-12-27 | EP2368551B1 | 2013-09-18 | Matsui, William; Tremblay, Martin R.; Castro, Alfredo C.; Grogan, Michael J.; McGovern, Karen J. |
| The invention provides methods for treating various conditions using derivatives of cyclopamine having the following formula: | ||||||
| 87 | METHODS FOR STEREOSELECTIVE REDUCTION | EP08868213 | 2008-12-24 | EP2224807A4 | 2012-12-12 | AUSTAD BRIAN C; LESCARBEAU ANDRE; YU LIN-CHEN |
| 88 | Methods of use for cyclopamine analogs | EP11165825.8 | 2007-12-27 | EP2368551A3 | 2011-12-21 | Matsui, William; Tremblay, Martin R.; Castro, Alfredo C.; Grogan, Michael J.; McGovern, Karen J. |
The invention provides methods for treating various conditions using derivatives of cyclopamine having the following formula:
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| 89 | REGULATORS OF THE HEDGEHOG PATHWAY, COMPOSITIONS AND USES RELATED THERETO | EP00973544.0 | 2000-10-13 | EP1235851B1 | 2006-05-31 | BEACHY, Philip, A.; Taipale, Anssi Jussi; Chen, James K. |
| The present invention makes available, <i>inter alia</i>, methods and reagents for modulating <i>smoothened-dependent</i> pathway activation. In certain embodiments, the subject methods can be used to counteract the phenotypic effects of unwanted activation of a hedgehog pathway, such as resulting from <i>hedgehog</i> gain-of-function, <i>ptc</i> loss-of-function or smoothened gain-of-function mutations. | ||||||
| 90 | METHODS FOR OBTAINING CYCLOPAMINE | PCT/CA2009/000916 | 2009-07-03 | WO2010000070A1 | 2010-01-07 | SPLINTER, Steven; KADALI, Satyasagar |
The present invention relates to a process for extracting, purifying and isolating cyclopamine from cyclopamine-containing biomass comprising the steps of contacting cyclopamine-containing organic matter with an extractant (e.g., aqueous extractant) capable of extracting cyclopamine, separating the extracted organic matter from the cyclopamine/extract solution, concentrating the cyclopamine/extract solution leaving a concentrated aqueous solution, contacting the concentrated aqueous solution with an organic extractant capable of selectively extracting cyclopamine from the aqueous phase, concentrating the cyclopamine-containing organic phase, providing an enriched extract containing cyclopamine, separating cyclopamine from the enriched extract using column chromatography, providing at least one fraction containing cyclopamine, and crystallizing select chromatography fractions to provide purified cyclopamine. |
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| 91 | TETRAHYDROBENZFLUORENE DERIVATIVES | PCT/EP2002/014283 | 2002-12-16 | WO2003053994A1 | 2003-07-03 | LOOZEN, Hubert, Jan, Jozef |
A compound having formula (I), wherein the O-(CH2)n-N(R1,R2) substituent on the phenyl ring can be in meta or para position; n is 2-4, Re and 'Re are OH, optionally independently etherified or esterified; R1 and R2 are independently (1C-4C)alkyl, (2C-4C)alkenyl, hydroxy(2C-4C)alkyl, (1C-3C)alkoxy(2C-4C)alkyl, aryl or aryl(1C-2C)alkyl; or R1 and R2 together with the nitrogen form an aromatic or non-aromatic heterocyclic ring structure, optionally mono- or poly-substituted with (1C-4C)alkyl, (2C-4C)alkenyl, hydroxy(1C-2C)alkyl, (1C-2C)alkoxy(1C-3C)alkyl or aryl. These compounds can be used for estrogen receptor β selective medical treatments. |
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| 92 | USE OF CYCLOPAMINE IN THE TREATMENT OF BASAL CELL CARCINOMA AND OTHER TUMORS | PCT/TR0100027 | 2001-07-02 | WO02078703A8 | 2003-06-12 | TAS SINAN; AVCI OKTAY |
| This invention concerns the use of cyclopamine in vivo on basal cell carcinomas to achieve therapeutic effect by causing differentiation of the tumor cells and, at the same time, highly efficient apoptotic death and removal of these tumor cells while preserving the normal tissue cells, including the undifferentiated cells of the normal epidermal basal layer and hair follicles. Causation of apoptosis by cyclopamine is by a non-genotoxic mechanism. These effects make the use of cyclopamine highly desirable in the treatment of basal cell carcinomas and other tumors that use the hedgehog/smoothened signal transduction pathway for proliferation and prevention of apoptosis. | ||||||
| 93 | REGULATORS OF THE PCT OR SMOOTHENED PATHWAY, COMPOSITIONS AND USES RELATED THERETO | PCT/US0000873 | 2000-01-13 | WO0041545A3 | 2000-09-28 | DUDEK HENRYK; JI BENXIU |
| The present invention makes available methods and reagents for inhibiting aberrant growth states resulting from hedgehog gain-of-function, ptc loss-of-function or smoothened gain-of-function comprising contacting a cell with a compound, such as a polypeptide or small molecule in an amount sufficient to control the aberrant growth state, e.g., to agonize a normal ptc pathway or antagonize smoothened or hedgehog activity. The present invention further makes available methods and reagents for ameliorating the consequences of hedgehog loss-of-function, ptc gain-of-function, or smoothened loss-of-function comprising contacting a cell with a compound, such as a polypeptide or small molecule, in an amount sufficient for amelioration. In certain embodiments, the subject compounds, e.g., a cAMP analog, adenylate cyclase agonist, or cAMP phosphodiesterase inhibitor, regulate cAMP levels, which in turn modulates activity of the hedgehog pathway. | ||||||
| 94 | USE OF STEROIDAL ALKALOID DERIVATIVES AS INHIBITORS OF HEDGEHOG SIGNALING PATHWAYS | PCT/US1999/007811 | 1999-04-09 | WO99052534A1 | 1999-10-21 | |
| The present invention makes available assays and reagents inhibiting paracrine and/or autocrine signals produced by a hedgehog protein or aberrant activation of a hedgehog signal transduction pathway, e.g., which involve the use of a steroidal alkaloid or other small molecule. | ||||||
| 95 | METHODS FOR STEREOSELECTIVE REDUCTION OF CYCLOPAMINE 4-EN-3-ONE DERIVATIVE | EP16197797.0 | 2008-12-24 | EP3190121B1 | 2019-02-20 | Austad, Brian C.; Lescarbeau, Andre; Yu, Lin-Chen |
| 96 | TETRACYCLIC COMPOUNDS AS ESTROGEN LIGANDS | EP05788764.8 | 2005-06-29 | EP1761513A1 | 2007-03-14 | MILLER, Christopher, P.; COLLINI, Michael, D.; MORRIS, Robert, L.; SINGHAUS, Robert, R., Jr. |
| This invention provides estrogen receptor modulators having the structure: (I) wherein R1, R2, R3, R4, Q, n, R8, R9, R10, and R11 have been defined in the specification; or a pharmaceutically acceptable salt thereof. The invention further provides methods for the preparation and use of the compounds. | ||||||
| 97 | Regulators of the hedgehog pathway, compositions and uses related thereto | EP06011086.3 | 2000-10-13 | EP1728797A2 | 2006-12-06 | Beachy, Philip, A.; Chen, James, K.; Taipale, Anssi Jussi |
The present invention makes available, inter alia, methods and reagents for modulating smoothened-dependent pathway activation. In certain embodiments, the subject methods can be used to counteract the phenotypic effects of unwanted activation of a hedgehog pathway, such as resulting from hedgehog gain-of-function, ptc loss-of-function or smoothened gain-of-function mutations. |
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| 98 | TETRAHYDROBENZFLUORENE DERIVATIVES | EP02793020.5 | 2002-12-16 | EP1458743A1 | 2004-09-22 | LOOZEN, Hubert Jan Jozef |
| A compound having formula (I), wherein the O-(CH2)n-N(R1,R2) substituent on the phenyl ring can be in meta or para position; n is 2-4, Re and 'Re are OH, optionally independently etherified or esterified; R1 and R2 are independently (1C-4C)alkyl, (2C-4C)alkenyl, hydroxy(2C-4C)alkyl, (1C-3C)alkoxy(2C-4C)alkyl, aryl or aryl(1C-2C)alkyl; or R1 and R2 together with the nitrogen form an aromatic or non-aromatic heterocyclic ring structure, optionally mono- or poly-substituted with (1C-4C)alkyl, (2C-4C)alkenyl, hydroxy(1C-2C)alkyl, (1C-2C)alkoxy(1C-3C)alkyl or aryl. These compounds can be used for estrogen receptor β selective medical treatments. | ||||||
| 99 | REGULATORS OF THE HEDGEHOG PATHWAY, COMPOSITIONS AND USES RELATED THERETO | EP00973544.0 | 2000-10-13 | EP1235851A2 | 2002-09-04 | BEACHY, Philip, A. |
| The present invention makes available, inter alia, methods and reagents for modulating smoothened-dependent pathway activation. In certain embodiments, the subject methods can be used to counteract the phenotypic effects of unwanted activation of a hedgehog pathway, such as resulting from hedgehog gain-of-function, ptc loss-of-function or smoothened gain-of-function mutations. | ||||||
| 100 | Benzo(a)fluorene compounds | EP92306221.0 | 1992-07-07 | EP0524742B1 | 1996-02-28 | Jones, Charles David |
