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1. 外观设计

USD910126S1 Body stretching bar 有权
公开(公告)号：USD910126S1
公开(公告)日：2021-02-09
申请号：US29651881
申请日：2019-05-29
申请人： John DiMarco
设计人： John DiMarco

2. 发明申请

US20060128726A1 Process for preparing novel crystalline forms of (2S)-1-[[(7R)-7-(3,4-dichlorophenyl)-4,7-dihydro-5-methylpyrazolo[1,5]pyrimidine-6-yl]carbonyl]-2-(4-fluorophenyl)pyrrolidine, novel stable forms produced therein and formulations 审中-公开
标题翻译：制备（2S）-1 - [[（7R）-7-（3,4-二氯苯基）-4,7-二氢-5-甲基吡唑并[1,5]嘧啶-6-基]羰基的新结晶形式的方法 ] -2-（4-氟苯基）吡咯烷，其中制备的新型稳定形式和制剂
公开(公告)号：US20060128726A1
公开(公告)日：2006-06-15
申请号：US11283651
申请日：2005-11-21
申请人： Xuebao Wang , Chiajen Lai , Nachimuthu Soundararajan , Nina Nguyen , Weiming Ying , Lori Burton , Rajesh Gandhi , Krishnaswamy Raghavan , Ronald West , Yuji Zhou , Lin Yan , Xiaotian Yin , John DiMarco , Jack Gougoutas
发明人： Xuebao Wang , Chiajen Lai , Nachimuthu Soundararajan , Nina Nguyen , Weiming Ying , Lori Burton , Rajesh Gandhi , Krishnaswamy Raghavan , Ronald West , Yuji Zhou , Lin Yan , Xiaotian Yin , John DiMarco , Jack Gougoutas
IPC分类号： A61K31/519 , C07D487/04
CPC分类号： C07D487/04
摘要： A process is provided for preparing novel crystalline forms, namely selectively and consistently preparing the H2-1 dihydrate crystalline form, the H2-2 dihydrate crystalline form, the N-3 anhydrate crystalline form and the MTBE solvate crystalline form of the IKur compound (2S)-1-[[(7R)-7-(3,4-dichlorophenyl)-4,7-dihydro-5-methylpyrazolo[1,5]pyrimidine-6-yl]carbonyl]-2-(4-fluorophenyl)pyrrolidine. The process includes preparation of the H2-1 and H2-2 forms which are used in preparing the N-3 anhydrate form which is particularly stable and has suitable flow properties and desired particle size. Novel H2-1 dihydrate and H2-2 dihydrate forms, the N-3 anhydrate form and the MTBE solvate form of the above IKur compound, pharmaceutical compositions containing such novel forms and a method for preventing or treating arrhythmias including atrial fibrillation and IKur related conditions employing such novel forms are also provided.
摘要翻译：提供了一种制备新型结晶形式的方法，即选择性和一致地制备H 2 - II二水合物结晶形式，H2-2二水合物结晶形式，N-3无水物结晶形式和IKEA化合物（2S ）-1 - [[（7R）-7-（3,4-二氯苯基）-4,7-二氢-5-甲基吡唑并[1,5]嘧啶-6-基]羰基] -2-（4-氟苯基）吡咯烷。该方法包括制备用于制备N-3无水物形式的H2-1和H2-2形式，其特别稳定并具有合适的流动性能和所需的粒度。新型H2-1二水合物和H2-2二水合物形成上述IKur化合物的N-3无水物形式和MTBE溶剂化物形式，含有这种新型形式的药物组合物和用于预防或治疗包括心房颤动和IKur相关病症的心律失常的方法也提供了这种新颖的形式。

3. 发明申请

US20060063815A1 Polymorphs of an epothilone analog 有权
标题翻译：埃坡霉素类似物的多晶型物
公开(公告)号：US20060063815A1
公开(公告)日：2006-03-23
申请号：US11271456
申请日：2005-11-10
申请人： John DiMarco , Jack Gougoutas , Imre Vitez , Martha Davidovich , Michael Galella , Timothy Malloy , Zhenrong Guo , Denis Favreau
发明人： John DiMarco , Jack Gougoutas , Imre Vitez , Martha Davidovich , Michael Galella , Timothy Malloy , Zhenrong Guo , Denis Favreau
IPC分类号： A61K31/427
CPC分类号： C07D491/04 , C07D417/06
摘要： There are provided in accordance with the present invention two crystalline polymorphs, designated Form A and Form B, respectively, as well as mixtures thereof, of an epothilone analog represented by the formula Also provided are methods of forming the novel polymorphs, therapeutic methods utilizing them and pharmaceutical dosage forms containing them.
摘要翻译：根据本发明，提供分别由式（I）和式（B）表示的两个结晶多晶型物及其混合物，其由式

4. 发明申请

US20060014741A1 Synthetic process, and crystalline forms of a pyrrolotriazine compound 审中-公开
标题翻译：合成方法和吡咯并三嗪化合物的结晶形式
公开(公告)号：US20060014741A1
公开(公告)日：2006-01-19
申请号：US11149525
申请日：2005-06-10
申请人： John DiMarco , Jack Gougoutas , Bharat Patel
发明人： John DiMarco , Jack Gougoutas , Bharat Patel
IPC分类号： A61K31/5377 , C07D487/04
CPC分类号： C07D487/04
摘要： The present invention provides a process for preparing pyrrolotriazine compounds of formula (I) or a pharmaceutically acceptable salt thereof. Also provided are crystalline forms of the pyrrolotriazine compound [4-[[1-(3-fluorophenyl)methyl]-1H-indazol-5-ylamino]-5-methyl-pyrrolo[2, 1-f][1,2,4]triazin-6-yl]-carbamic acid, (3S)-3-morpholinylmethyl ester and pharmaceutical compositions comprising at least one crystalline form, as well of methods of using the crystalline forms in the treatment of a proliferative disease, and methods for obtaining such crystalline forms. The compounds of formula (I), including [4-[[1-(3-fluorophenyl)methyl]-1H-indazol-5-ylamino]-5-methyl-pyrrolo[2,1-f][1,2,4]triazin-6-yl]-carbamic acid, (3S)-3-morpholinylmethyl ester, are useful for inhibiting tyrosine kinase activity of growth factor receptors such as HER1, HER2 and HER4 thereby making them useful as antiproliferative agents for the treatment of cancer and other diseases.
摘要翻译：本发明提供了制备式（I）的吡咯并三嗪化合物或其药学上可接受的盐的方法。还提供了吡咯并三嗪化合物[4 - [[1-（3-氟苯基）甲基] -1H-吲唑-5-基氨基] -5-甲基 - 吡咯并[2,1-f] [1,2， 4]三嗪-6-基] - 氨基甲酸，（3S）-3-吗啉基甲酯和包含至少一种结晶形式的药物组合物，以及使用结晶形式治疗增殖性疾病的方法，以及用于获得这样的结晶形式。式（I）化合物包括[4 - [[1-（3-氟苯基）甲基] -1H-吲唑-5-基氨基] -5-甲基 - 吡咯并[2,1-f] 4]三嗪-6-基] - 氨基甲酸，（3S）-3-吗啉基甲基酯可用于抑制生长因子受体如HER1，HER2和HER4的酪氨酸激酶活性，从而使其可用作抗增殖剂，用于治疗癌症等疾病。

5. 发明申请

US20060004067A1 Process for preparing 2-aminothiazole-5-aromatic carboxamides as kinase inhibitors 有权
标题翻译：制备2-氨基噻唑-5-芳族羧酰胺作为激酶抑制剂的方法
公开(公告)号：US20060004067A1
公开(公告)日：2006-01-05
申请号：US11192867
申请日：2005-07-29
申请人： Bang-Chi Chen , Roberto Droghini , Jean Lajeunesse , John DiMarco , Michael Galella , Ramakrishnan Chidambaram
发明人： Bang-Chi Chen , Roberto Droghini , Jean Lajeunesse , John DiMarco , Michael Galella , Ramakrishnan Chidambaram
IPC分类号： A61K31/427 , A61K31/426 , C07D417/02 , C07D277/46
CPC分类号： C07D403/12 , C07D277/56 , C07D417/12
摘要： The invention relates to processes for preparing compounds having the formula, and crystalline forms thereof, wherein Ar is aryl or heteroaryl, L is an optional alkylene linker, and R2, R3, R4, and R5, are as defined in the specification herein, which compounds are useful as kinase inhibitors, in particular, inhibitors of protein tyrosine kinase and p38 kinase.
摘要翻译：本发明涉及制备具有下式的化合物及其结晶形式的方法，其中Ar为芳基或杂芳基，L为任选的亚烷基连接基，R 2，R 3， R 4，R 5和R 5如本说明书中所定义，该化合物可用作激酶抑制剂，特别是蛋白酪氨酸激酶和p38激酶的抑制剂。

6. 发明申请

US20060116420A1 Crystalline forms of 3'-tert-Butyl-3'-N-tert-butyloxycarbonyl-4-deacetyl-3'-dephenyl-3'-N-debenzoyl-4-O-methoxycarbonyl-paclitaxel 审中-公开
标题翻译： 3'-叔丁基-3'-N-叔丁氧基羰基-4-脱乙酰基-3'-脱苯基-3'-N-脱苯甲酰基-4-O-甲氧基羰基 - 紫杉醇的结晶形式
公开(公告)号：US20060116420A1
公开(公告)日：2006-06-01
申请号：US11285463
申请日：2005-11-22
申请人： Ramakrishnan Chidambaram , Robert Perrone , Martha Davidovich , John DiMarco , Gary McGeorge , Imre Vitez
发明人： Ramakrishnan Chidambaram , Robert Perrone , Martha Davidovich , John DiMarco , Gary McGeorge , Imre Vitez
IPC分类号： A61K31/337 , C07D405/14
CPC分类号： C07D305/14
摘要： The present invention relates to crystalline forms of 3′-tert-Butyl-3′-N-tert-butyloxycarbonyl-4-deacetyl-3 ′-dephenyl-3′-N-debenzoyl-4-O-methoxycarbonyl-paclitaxel represented by formula I; processes for the production thereof; pharmaceutical compositions thereof; methods for preparing the pharmaceutical composition; and methods for inhibiting tumor growth therewith.
摘要翻译：本发明涉及由式（I）表示的3'-叔丁基-3'-N-叔丁氧基羰基-4-脱乙酰基-3'-二苯基-3'-N-脱苯甲酰基-4-O-甲氧基羰基 - 紫杉醇的结晶形式一世; 生产过程; 其药物组合物; 制备药物组合物的方法; 以及抑制肿瘤生长的方法。

7. 发明申请

US20070060599A1 Crystalline forms of [1S-(1alpha, 3alpha, 4beta)]-2-amino-1,9-dihydro-9-[4-hydroxy-3-(hydroxymethyl)-2-methylenecyclopentyl]-6H-purin-6-one 审中-公开
标题翻译： [1S-（1α，3α，4β）] - 2-氨基-1,9-二氢-9- [4-羟基-3-（羟甲基）-2-亚甲基环戊基] -6H-嘌呤-6-酮的结晶形式
公开(公告)号：US20070060599A1
公开(公告)日：2007-03-15
申请号：US11222597
申请日：2005-09-09
申请人： John DiMarco , Jack Gougoutas
发明人： John DiMarco , Jack Gougoutas
IPC分类号： A61K31/522 , C07D473/04
CPC分类号： C07D473/18
摘要： The present invention relates to crystalline forms containing [1S-(1α,3α,4β)]-2-amino-1,9-dihydro-9-[4-hydroxy-3-(hydroxymethyl)-2-methylenecyclopentyl]-6H-purin-6-one represented by formula I; processes for the production thereof; pharmaceutical compositions thereof; methods for preparing the pharmaceutical composition; and the use of these crystalline forms in the treatment of hepatitis B viral infections.
摘要翻译：本发明涉及含有[1S-（1α，3α，4beta）] - 2-氨基-1,9-二氢-9- [4-羟基-3-（羟甲基）-2-亚甲基环戊基] 由式I表示的嘌呤-6-酮; 生产过程; 其药物组合物; 制备药物组合物的方法; 以及这些结晶形式在治疗乙型肝炎病毒感染中的应用。

8. 发明申请

US20060135474A1 Methods for the preparation, isolation and purification of epothilone B, and X-ray crystal structures of epothilone B 有权
标题翻译：埃坡霉素B的制备，分离和纯化方法以及埃坡霉素B的X射线晶体结构
公开(公告)号：US20060135474A1
公开(公告)日：2006-06-22
申请号：US10805724
申请日：2004-03-22
申请人： Daniel Benigni , Jack Gougoutas , John DiMarco
发明人： Daniel Benigni , Jack Gougoutas , John DiMarco
IPC分类号： C08B30/18 , A61K31/724
CPC分类号： C07D493/04 , C12N1/20 , C12N1/38 , C12P17/181 , C12R1/01
摘要： The present invention relates to improved methods for the production, isolation and purification of epothilone B. These methods include, for example, a fermentation process for the production of epothilone B, isolation via adsorption onto a resin, and subsequent purification.
摘要翻译：本发明涉及埃坡霉素B的生产，分离和纯化的改进方法。这些方法包括例如用于生产埃坡霉素B的发酵方法，通过吸附到树脂上进行分离和随后的纯化。

9. 发明申请

US20060069118A1 Crystalline forms of a factor Xa inhibitor 失效
标题翻译：晶体形式的因子Xa抑制剂
公开(公告)号：US20060069118A1
公开(公告)日：2006-03-30
申请号：US11235519
申请日：2005-09-26
申请人： Margaret Gleeson , Gary McGeorge , Bang-Chi Chen , Huiping Zhang , Mary Malley , John DiMarco , Denette Murphy , Xiaotian Yin , Steven Fabian , Jasmine Gupta
发明人： Margaret Gleeson , Gary McGeorge , Bang-Chi Chen , Huiping Zhang , Mary Malley , John DiMarco , Denette Murphy , Xiaotian Yin , Steven Fabian , Jasmine Gupta
IPC分类号： C07D471/02 , A61K31/4745
CPC分类号： C07D471/04
摘要： The instant invention provides crystalline forms of 1-(3-chlorophenyl)-7-oxo-6-[4-(2-oxo-1 (2H)pyridinyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide and its solvates thereof; processes for the production of such crystalline forms; pharmaceutical compositions comprising such crystalline forms; and methods of treating thromboembolic disorders with such crystalline forms or such pharmaceutical compositions.
摘要翻译：本发明提供1-（3-氯苯基）-7-氧代-6- [4-（2-氧代-1（2H）吡啶基）苯基] -4,5,6,7-四氢-1H- 吡唑并[3,4-c]吡啶-3-甲酰胺及其溶剂化物; 生产这种结晶形式的方法; 包含这种结晶形式的药物组合物; 以及用这种结晶形式或这种药物组合物治疗血栓栓塞障碍的方法。

10. 发明申请

US20050215795A1 Process for preparing 2-aminothiazole-5-aromatic carboxamides as kinase inhibitors 审中-公开
标题翻译：制备2-氨基噻唑-5-芳族羧酰胺作为激酶抑制剂的方法
公开(公告)号：US20050215795A1
公开(公告)日：2005-09-29
申请号：US11051208
申请日：2005-02-04
申请人： Bang-Chi Chen , Roberto Droghini , Jean Lajeunesse , John Dimarco , Michael Galella , Ramakrishnan Chidambaram
发明人： Bang-Chi Chen , Roberto Droghini , Jean Lajeunesse , John Dimarco , Michael Galella , Ramakrishnan Chidambaram
IPC分类号： A61K31/426 , C07D277/56 , C07D417/02 , C07D417/12
CPC分类号： C07D277/56 , C07D417/12
摘要： The invention relates to processes for preparing compounds having the formula, and crystalline forms thereof, wherein Ar is aryl or heteroaryl, L is an optional alkylene linker, and R2, R3, R4, and R5, are as defined in the specification herein, which compounds are useful as kinase inhibitors, in particular, inhibitors of protein tyrosine kinase and p38 kinase.
摘要翻译：本发明涉及制备具有下式的化合物及其结晶形式的方法，其中Ar为芳基或杂芳基，L为任选的亚烷基连接基，R 2，R 3， R 4，R 5和R 5如本说明书中所定义，该化合物可用作激酶抑制剂，特别是蛋白酪氨酸激酶和p38激酶的抑制剂。

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