公开(公告)号：US20070232664A1

公开(公告)日：2007-10-04

申请号：US11582846

申请日：2006-10-17

Applicant: Raymond Bergeron

Inventor： Raymond Bergeron

IPC: A61K31/4439 ,  A61K31/426

CPC classification number: C07D417/04 ,  A61K31/4164 ,  A61K31/426 ,  A61K31/4436 ,  A61K31/4439 ,  C07D207/22 ,  C07D233/28 ,  C07D277/10 ,  C07D277/12 ,  Y02A50/411

Abstract: Composition, article of manufacture for and method of treating malaria in a human having an infestation of Plasmodium protozoans are described. The method comprises administering a therapeutically-effective amount of a compound of formula (I) or (IV), i.e. sufficient quantity to reduce the population of Plasmodium. The composition of the invention is a compound of formula (I) or (IV) with a pharmaceutical excipient. The article of manufacture is the composition in combination with labeling for treating malaria. The substituents are detailed in the specification.

Abstract translation: 描述了具有侵染疟原虫原虫的人的组合物，制品和治疗疟疾的方法。 该方法包括施用治疗有效量的式（I）或（IV）的化合物，即足够的量以减少疟原虫的种群。 本发明的组合物是具有药物赋形剂的式（I）或（IV）的化合物。 该制品是与治疗疟疾标签相结合的组合物。 取代基在说明书中详细描述。

公开(公告)号：US20060094791A1

公开(公告)日：2006-05-04

申请号：US10979765

申请日：2004-11-03

Applicant: Raymond Bergeron

Inventor： Raymond Bergeron

IPC: A61K31/13 ,  C07C211/13

CPC classification number: C07C211/14

Abstract: An aminated polyamine having the formula: or its possible stereoisomers or a salt thereof with a pharmaceutically acceptable acid wherein: R1 and R4 may be the same or different and are alkyl, aryl, aryl alkyl or cycloalkyl, optionally having an alkyl chain interrupted by at least one etheric oxygen atom; R2 and R3 may be the same or different and are R1, R4 or H; N1, N2, N3 and N4 are nitrogen atoms capable of protonation at physiological pH's; ALK1, ALK2 AND ALK3 may be the same or different and are straight or branched chain alkylene bridging groups having 1 to 4 carbon atoms which effectively maintain the distance between the nitrogen atoms such that the polyamine: (i) is capable of uptake by a target cell upon administration of the polyamine to a human or non-human animal or is capable of binding to at least one polyamine site of a receptor located within or on the surface of a cell upon administration of the polyamine to a human or non-human animal; and (ii) upon uptake by the target cell, competitively binds via an electrostatic interaction between the positively charged nitrogen atoms to biological counter-anions; the polyamine, upon binding to the biological counter-anion in the cell, functions in a manner biologically different than the intracellular polyamines; and further wherein at least one of said bridging groups ALK1, ALK2 and ALK3 contains at least one —CH(NRH)— group which is not alpha- to either of the nitrogen atoms and R is H, alkyl, acyl or sulfonyl.

Abstract translation: 具有下式的胺化多胺或其可能的立体异构体或其盐与药学上可接受的酸，其中：R 1和R 4可以相同或不同，并且是烷基 ，芳基，芳基烷基或环烷基，任选地具有被至少一个醚性氧原子间隔的烷基链; R 2和R 3可以相同或不同，为R 1，R 4或H; N 1，N 2，N 3和N 4是在生理pH下能够质子化的氮原子; ALK 1，ALK 2和AL 3 3可以相同或不同，并且是具有1至4个碳原子的直链或支链亚烷基桥连基团 其有效地保持氮原子之间的距离，使得多胺：（i）在将多胺向人或非人动物施用时能够被靶细胞吸收或能够结合到至少一个多胺位点 将多胺施用于人或非人动物时位于细胞表面内或细胞表面的受体; 和（ii）被靶细胞吸收后，通过带正电的氮原子之间的静电相互作用与生物反阴离子竞争结合; 多胺在与细胞中的生物反阴离子结合时以与细胞内多胺生物学不同的方式起作用; 并且其中所述桥连基团ALK 1，ALK 2和ALK 3 3中的至少一个含有至少一个-CH（NRH） - 基团 其不是氮原子中的任一个，R是H，烷基，酰基或磺酰基。

公开(公告)号：US20050113455A1

公开(公告)日：2005-05-26

申请号：US10970725

申请日：2004-10-22

Applicant: Raymond Bergeron

Inventor： Raymond Bergeron

IPC: A61K31/13 ,  A61K31/135 ,  A61K31/785

CPC classification number: A61K31/13 ,  A61K31/135 ,  A61K31/785

Abstract: A composition, method and article of manufacture for the amelioration of pain comprising: a polyamine having the formula: R1R2N1—A—[N2R3—B]a—[N3R4—C]b—N4R5R6wherein: R1-R6 may be the same or different and are alkyl, aryl, aryl alkyl, cycloalkyl, optionally having an alkyl chains interrupted by at least one etheric oxygen atom, or hydrogen; N1-N4 are nitrogen atoms capable of protonation at physiological pH's; a and b may be the same or different and are integers from 0 to 4; A, B and C may be the same or different and are bridging groups which effectively maintain the distance between the nitrogen atoms such that the polyamine: (i) is capable of uptake by a target cell upon administration of the polyamine to a human or non-human animal; and (ii) upon uptake by the target cell, competitively binds via an electrostatic interaction between the positively charged nitrogen atoms to substantially the same biological counter-anions as the intra-cellular natural polyamines in the target cell; the polyamine, upon binding to the biological counter-anion in the cell, functions to alleviate pain; a mixture of the amines; a derivative, salt or complex of the amine wherein the derivative, salt or complex former is physiologically acceptable and the formation of the salt, derivative or complex does not materially affect the pain amelioration properties of the amine; a mixture of the derivatives, salts and/or complexes, or a prodrug that provides the amine, mixture of the amines, the derivative, salt or complex or mixture of the derivatives, salts and/or complexes.

公开(公告)号：US20050113391A1

公开(公告)日：2005-05-26

申请号：US10973383

申请日：2004-10-27

Applicant: Raymond Bergeron

Inventor： Raymond Bergeron

IPC: A61K31/131 ,  A61K31/136 ,  A61K31/135 ,  A61K31/13

CPC classification number: A61K31/136 ,  A61K31/131

Abstract: Pharmaceutical compositions for the treatment of hypertension comprising an effective anti-hypertensive amount of at least one compound in association with a pharmaceutically acceptable, substantially non-toxic carrier or excipient, the compound having one of the formulae (I), (II), (III) or (IV), and methods for the treatment of hypertension or effecting anti-hypertensive action which comprises administering to a patient requiring anti-hypertensive therapy or effect at least one of the above-described compounds.

Abstract translation: 用于治疗高血压的药物组合物，其包含与药学上可接受的，基本上无毒的载体或赋形剂结合的有效抗高血压量的至少一种化合物，所述化合物具有式（I），（II），（II）， III）或（IV），以及治疗高血压或进行抗高血压作用的方法，其包括对需要抗高血压治疗或影响至少一种上述化合物的患者施用。

公开(公告)号：US20180339887A1

公开(公告)日：2018-11-29

申请号：US15606604

申请日：2017-05-26

Applicant: Raymond Bergeron

Inventor： Raymond Bergeron

IPC: B66C3/00 ,  B66C3/02 ,  E02F3/413 ,  E02F3/38

CPC classification number: B66C3/005 ,  B66C3/02 ,  B66C3/06 ,  E02F3/384 ,  E02F3/413

Abstract: A power bucket having a first and second bucket half pivotally secured together about a main axis by a pivot pin. The bucket halves are movable between an open and a closed position. A head is disposed above the bucket halves and at least one arm pivotally connects the head to one bucket half while at least one second arm is pivotally connected between the head and the other bucket half. A cylinder support is pivotally mounted to the pivot pin and one end of a hydraulic cylinder is attached to the pivot support. The other end of the cylinder is attached to the bucket. Upon actuation of the cylinders, the cylinders move the bucket halves so that a cutting edge of the bucket half moves in a substantially horizontal plane.

公开(公告)号：US20080108706A1

公开(公告)日：2008-05-08

申请号：US12003735

申请日：2007-12-31

Applicant: Raymond Bergeron

Inventor： Raymond Bergeron

IPC: A61K31/133 ,  A61P41/00

CPC classification number: A61K31/131

Abstract: A method of chemically resecting the exocrine portion of the pancreas of a patient in need thereof comprising administering to the patient an amount of a hydroxy polyamine or a salt thereof with a pharmaceutically acceptable acid sufficient to resect the exocrine portion of the pancreas thereof, but insufficient to substantially alter the endocrine portion thereof. The hydroxy polyamine has a structure according to the formula: wherein: R1 and R2 may be the same or different and are alkyl having 1 to 6 carbon atoms or aryl or aralkyl having up to 12 carbon atoms; a, b, d and e may be the same or different and are integers from 1 to 4; and c is an integer from 2 to 6. A pharmaceutical composition in unit dosage form comprising the hydroxy polyamine or a salt thereof with a pharmaceutically acceptable acid for use in the method of the invention is also disclosed.

Abstract translation: 一种化学切除有需要的患者胰腺的外分泌部分的方法，包括向患者施用一定量的羟基多胺或其盐与足以切除胰腺的外分泌部分的药学上可接受的酸，但不足 基本上改变其内分泌部分。 羟基多胺具有下式的结构：其中：R 1和R 2可以相同或不同，为具有1-6个碳原子的烷基或芳基或 具有至多12个碳原子的芳烷基; a，b，d和e可以相同或不同，为1〜4的整数; 并且c是2至6的整数。还公开了包含羟基多胺或其盐与用于本发明方法的药学上可接受的酸的单位剂型的药物组合物。

公开(公告)号：US20080096974A2

公开(公告)日：2008-04-24

申请号：US11368276

申请日：2006-03-03

Applicant: Raymond Bergeron

Inventor： Raymond Bergeron

IPC: A01N35/02

CPC classification number: A61K31/132 ,  A61K47/54 ,  A61K47/547 ,  A61K47/59

Abstract: Many metal chelators have polar or charged functional groups, which render them difficult to transport across a cell membrane. Polyamine-metal chelator conjugates of the invention are compounds comprising a first moiety which is a metal chelator and a second moiety which is a polyamine, where the polyamine moiety includes three or more nitrogen atoms which are capable of being positively charged at physiological pH. A spermine-L1 conjugate has been shown to accumulate in L1210 cells several hundred fold more than the unconjugated L1 chelator.

Abstract translation: 许多金属螯合剂具有极性或带电的官能团，这使得它们难以在细胞膜上运输。 本发明的多胺 - 金属螯合剂缀合物是包含金属螯合剂的第一部分和多胺的第二部分的化合物，其中多胺部分包括能够在生理pH下带正电荷的三个或更多个氮原子。 已经显示精胺-L1缀合物在L1210细胞中积累比未偶联的L1螯合剂多百倍。

公开(公告)号：US20060211773A1

公开(公告)日：2006-09-21

申请号：US11368276

申请日：2006-03-03

Applicant: Raymond Bergeron

Inventor： Raymond Bergeron

IPC: A01N35/02

CPC classification number: A61K31/132 ,  A61K47/54 ,  A61K47/547 ,  A61K47/59

Abstract: Many metal collators have polar or charged functional groups, which render them difficult to transport across a cell membrane. Polyimide-metal collator conjugates of the invention are compounds comprising a first moiety which is a metal collator and a second moiety which is a polyimide, where the polyimide moiety includes three or more nitrogen atoms which are capable of being positively charged at physiological pH. A sperms-L1 conjugate has been shown to accumulate in L1210 cells several hundred fold more than the unconjugated L1 chelator.

Abstract translation: 许多金属整理机具有极性或带电的官能团，这使得它们难以在细胞膜上运输。 本发明的聚酰亚胺 - 金属整理剂共轭物是包含作为金属整理机的第一部分和作为聚酰亚胺的第二部分的化合物，其中聚酰亚胺部分包括能够在生理pH下带正电荷的三个或更多个氮原子。 已经显示精子-L1结合物在L1210细胞中积累比未偶联的L1螯合剂多几百倍。

公开(公告)号：US20060160905A1

公开(公告)日：2006-07-20

申请号：US11036130

申请日：2005-01-18

Applicant: Raymond Bergeron

Inventor： Raymond Bergeron

IPC: A61K31/137

CPC classification number: A61K31/137

Abstract: A method and pharmaceutical composition for ameliorating pain in a human or non-human mammal suffering therefrom based on an antinociceptive amine having the formula: wherein: Z is H or OH, is phenyl or cyclohexyl, R and R1 are the same or different and may be H or linear or branched chain alkyl having 1 to 8 carbon atoms, m is an integer from 0 to 10, inclusive and wherein the amine exhibits a mean reduction in abdominal writhings exhibited by mice in the standard acetic acid-induced visceral pain mouse model of at least 20%; a mixture of the amines; a derivative, salt or complex of the amine wherein the derivative, salt or complex former is physiologically acceptable and the formation of said salt, derivative or complex does not materially affect the pain amelioration properties of the amine; a mixture of the derivatives, salts and/or complexes or a prodrug that provides the amine, mixture of the amines, the derivative, salt or complex, or a mixture of the derivatives, salts and/or complexes.

Abstract translation: 基于具有下式的抗伤害感受性胺，其中：Z为H或OH，为苯基或环己基，R 1和R 2为一种用于改善患有其的人或非人哺乳动物疼痛的方法和药物组合物 >相同或不同，并且可以是H或具有1至8个碳原子的直链或支链烷基，m是0至10的整数，其中胺表现出标准中小鼠表现出的腹部扭体的平均降低 乙酸诱导的内脏痛小鼠模型至少20％; 胺的混合物; 衍生物，盐或络合物，其中衍生物，盐或络合物在生理上是可接受的，并且所述盐，衍生物或复合物的形成不会实质上影响胺的疼痛改善性质; 衍生物，盐和/或配合物的混合物或前体药物，其提供胺，胺，衍生物，盐或络合物的混合物，或衍生物，盐和/或配合物的混合物。

公开(公告)号：US20050234113A1

公开(公告)日：2005-10-20

申请号：US11034040

申请日：2005-01-12

Applicant: Raymond Bergeron

Inventor： Raymond Bergeron

IPC: A61K31/40 ,  A61K31/426 ,  A61K31/427 ,  A61K31/4439 ,  C07F15/02

CPC classification number: A61K31/426 ,  A61K31/40 ,  A61K31/427 ,  A61K31/4439

Abstract: Free radicals and reactive oxygen species have the potential to damage a wide variety of organic molecules, typically by oxidizing certain moieties. These damaging species can, for example, be produced by an organism as a by-product of cellular respiration or by the reaction of iron(II) and peroxide. The present invention includes methods of using aryl-substituted heterocyclic iron chelating compounds as antioxidants, as well as preventing the reduction of iron(III) to iron(II). In addition, the present invention provides methods of treating conditions such as inflammatory disease, neoplastic disease, and ischemic episodes.

Abstract translation: 自由基和活性氧具有损害多种有机分子的潜力，通常通过氧化某些部分。 这些有害物质可以例如由生物体作为细胞呼吸的副产物或通过铁（II）和过氧化物的反应产生。 本发明包括使用芳基取代的杂环铁螯合化合物作为抗氧化剂的方法，以及防止铁（III）还原成铁（II）的方法。 此外，本发明提供治疗诸如炎性疾病，肿瘤性疾病和缺血发作的病症的方法。