公开(公告)号：US20120302579A1

公开(公告)日：2012-11-29

申请号：US13487488

申请日：2012-06-04

Applicant: Connie Erickson-Miller

Inventor： Connie Erickson-Miller

IPC: A61K31/4152 ,  A61P35/00 ,  A61P7/06 ,  A61K31/4155 ,  A61K31/496

CPC classification number: A61K45/06 ,  A61K9/0019 ,  A61K9/2054 ,  A61K9/4858 ,  A61K31/167 ,  A61K31/19 ,  A61K31/4045 ,  A61K31/4152 ,  A61K31/496 ,  A61K31/506 ,  A61K38/15 ,  A61K47/10 ,  A61K2300/00

Abstract: Invented is a method of treating cancer and pre-cancerous syndromes in a mammal, including a human, in need thereof which comprises the administration of a therapeutically effective amount of a non-peptide TPO receptor agonist to such mammal.

Abstract translation: 发明的是一种在有需要的哺乳动物（包括人）中治疗癌症和癌前综合征的方法，其包括向这种哺乳动物施用治疗有效量的非肽TPO受体激动剂。

公开(公告)号：US20120213791A1

公开(公告)日：2012-08-23

申请号：US13289373

申请日：2011-11-04

Applicant: Valerio BERDINI ,  Michael Alistair O'BRIEN ,  Maria Grazia CARR ,  Theresa Rachel EARLY ,  Adrian Liam GILL ,  Gary TREWARTHA ,  Alison Jo-Anne WOOLFORD ,  Andrew James WOODHEAD ,  Paul Graham WYATT

Inventor： Valerio BERDINI ,  Michael Alistair O'BRIEN ,  Maria Grazia CARR ,  Theresa Rachel EARLY ,  Adrian Liam GILL ,  Gary TREWARTHA ,  Alison Jo-Anne WOOLFORD ,  Andrew James WOODHEAD ,  Paul Graham WYATT

IPC: A61K31/415 ,  A61K31/4439 ,  A61K31/4196 ,  A61K31/454 ,  A61K31/496 ,  A61K31/4178 ,  A61K31/5377 ,  A61K31/497 ,  A61K31/4709 ,  A61K31/541 ,  A61K39/395 ,  A61K33/24 ,  A61K31/513 ,  A61K31/664 ,  A61K31/704 ,  A61P35/00 ,  A61P37/06 ,  A61P31/14 ,  A61P31/18 ,  A61P31/20 ,  A61P3/10 ,  A61P25/08 ,  A61P9/10 ,  A61P25/28 ,  A61P29/00 ,  A61P9/00 ,  A61P13/12 ,  A61P1/16 ,  A61P11/00 ,  A61N5/00 ,  A61K31/4155

CPC classification number: C07D231/38 ,  A61K31/415 ,  A61K31/4152 ,  A61K31/4155 ,  A61K31/416 ,  A61K31/4178 ,  A61K31/4196 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/541 ,  A61K45/06 ,  C04B35/632 ,  C07D231/14 ,  C07D231/40 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D453/02 ,  C07D471/04

Abstract: The invention provides compounds of the formula (0) or salts or tautomers or N-oxides or solvates thereof, and combinations thereof with other anti-cancer agents, for use in the prophylaxis or treatment of disease states and conditions such as cancers mediated by cyclin-dependent kinase and glycogen synthase kinase-3.

Abstract translation: 本发明提供式（O）的化合物或其盐或互变异构体或其N-氧化物或溶剂合物，以及其与其它抗癌剂的组合，用于预防或治疗疾病状态和病症，例如由细胞周期蛋白介导的癌症 依赖性激酶和糖原合成酶激酶-3。

公开(公告)号：US20120149749A1

公开(公告)日：2012-06-14

申请号：US13124182

申请日：2009-10-14

Applicant: Michael Arning ,  Manuel Carlos Alves-Aivado ,  Roya Behbahani ,  Yanli Deng ,  Connie L. Erickson-Miller ,  Sophia M. Goodison ,  Julian Jenkins ,  Shivakumar G. Kapsi ,  Bhabita Mayer ,  Francis Xavier Muller ,  Bin Peng ,  Teresa S. Sellers ,  Nicole Lee Stone ,  Dickens Theodore ,  Dennis R. Williams ,  Mary Beth Wire

Inventor： Michael Arning ,  Manuel Carlos Alves-Aivado ,  Roya Behbahani ,  Yanli Deng ,  Connie L. Erickson-Miller ,  Sophia M. Goodison ,  Julian Jenkins ,  Shivakumar G. Kapsi ,  Bhabita Mayer ,  Francis Xavier Muller ,  Bin Peng ,  Teresa S. Sellers ,  Nicole Lee Stone ,  Dickens Theodore ,  Dennis R. Williams ,  Mary Beth Wire

IPC: A61K31/4152 ,  A61P7/02

CPC classification number: A61K31/415 ,  A61K31/4152

Abstract: Invented is a method of treating thrombocytopenia in a human in need thereof which comprises the administration of a therapeutically effective amount of a 3′-{N′-[1-(3,4-Dimethylphenyl)-3-methyl-5-oxo-1,5-dihydropyrazol-4-ylidene]hydrazino}-2′-hydroxybiphenyl-3-carboxylic acid to such human.

Abstract translation: 发明内容是一种在有需要的人中治疗血小板减少症的方法，其包括施用治疗有效量的3' - （N' - [1-（3,4-二甲基苯基）-3-甲基-5-氧代 - 1,5-二氢吡唑-4-亚基]肼基} -2'-羟基联苯-3-羧酸。

公开(公告)号：US08088813B2

公开(公告)日：2012-01-03

申请号：US12873565

申请日：2010-09-01

Applicant: Stephen Moore

Inventor： Stephen Moore

IPC: A61K31/4152 ,  C07D231/38

CPC classification number: C07D231/46 ,  A61K31/4152 ,  A61K38/193 ,  A61K45/06 ,  C07D231/08 ,  A61K2300/00

Abstract: An improved thrombopoietin mimetic, the bis-(monoethanolamine) salt of 3′-[(2Z)-[1-(3,4-dimethylphenyl)-1,5-dihydro-3-methyl-5-oxo-4H-pyrazol-4-ylidene]hydrazino]-2′-hydroxy-[1,1′-biphenyl]-3-carboxylic acid.

Abstract translation: 改进的血小板生成素模拟物，3' - [（2Z） - [1-（3,4-二甲基苯基）-1,5-二氢-3-甲基-5-氧代-4H-吡唑并[ -4-亚基]肼基] -2'-羟基 - [1,1'-联苯] -3-羧酸。

公开(公告)号：US08058264B2

公开(公告)日：2011-11-15

申请号：US11257056

申请日：2005-10-25

Applicant: Michael Firnges ,  Peter-Colin Gregory ,  Jochen Antel ,  Josephus Hubertus Maria Lange ,  Harald Waldeck

Inventor： Michael Firnges ,  Peter-Colin Gregory ,  Jochen Antel ,  Josephus Hubertus Maria Lange ,  Harald Waldeck

IPC: A01N33/26 ,  A61K31/535

CPC classification number: A61K31/00 ,  A61K31/40 ,  A61K31/415 ,  A61K31/4152 ,  A61K31/427 ,  A61K31/44 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/5377 ,  A61K31/54 ,  A61K31/655 ,  A61K45/06 ,  G01N33/6872 ,  G01N33/948 ,  G01N2500/00 ,  G01N2800/042 ,  G01N2800/044 ,  A61K2300/00

Abstract: Described is a novel combination therapy for diabetes mellitus type I and/or for obesity and its concomitant and/or secondary diseases or conditions, in particular the metabolic syndrome and/or syndrome X, and/or diabetes mellitus type II, by administering a combination of at least one KATP channel opener as a first active agent and at least one CB1 cannabinoid receptor antagonist as a second active agent. The invention is further directed to such novel combination therapy wherein a dually acting compound with combined KATP channel opening and CB1 antagonistic properties is used. The invention also relates to novel pharmaceutical compositions comprising KATP channel openers and CB1 antagonists and the use of said pharmaceutical compositions in the treatment, delayed progression, delayed onset of and/or inhibition of diabetes mellitus type 1, and the prophylaxis and treatment, of obesity as well as the prophylaxis, treatment, delayed onset and/or inhbition of its concomitant and/or secondary diseases or conditions, in particular the metabolic syndrome and/or syndrome X, and/or diabetes mellitus type II, in mammals and humans. The invention is further directed to such novel pharmaceutical compositions comprising a dually acting compound with combined KATP channel opening and CB1 antagonistic properties.

Abstract translation: 描述了通过施用组合来描述I型糖尿病和/或用于肥胖及其伴随和/或继发疾病或病症，特别是代谢综合征和/或综合征X和/或II型糖尿病的新型联合治疗 的至少一种KATP通道开放剂作为第一活性剂和至少一种CB1大麻素受体拮抗剂作为第二活性剂。 本发明进一步涉及这种新型联合治疗，其中使用具有组合的KATP通道开放和CB1拮抗性质的双作用化合物。 本发明还涉及包含KATP通道开放剂和CB1拮抗剂的新型药物组合物，以及所述药物组合物在治疗，延迟进展，延迟发作和/或抑制1型糖尿病以及预防和治疗肥胖症中的用途 以及其伴随和/或继发疾病或病症，特别是哺乳动物和人类的代谢综合征和/或综合征X和/或II型糖尿病的预防，治疗，延迟发作和/或吸收。 本发明还涉及这种新型药物组合物，其包含具有组合的KATP通道开口和CB1拮抗性质的双作用化合物。

公开(公告)号：US20110129550A1

公开(公告)日：2011-06-02

申请号：US12948159

申请日：2010-11-17

Applicant: Connie ERICKSON-MILLER

Inventor： Connie ERICKSON-MILLER

IPC: A61K33/24 ,  A61K38/17 ,  A61K31/4152 ,  A61K31/41 ,  A61P35/00

CPC classification number: A61K31/496 ,  A61K9/0053 ,  A61K31/41 ,  A61K31/4152 ,  A61K31/4155 ,  A61K31/497 ,  A61K31/655 ,  A61K33/24 ,  A61K38/17 ,  A61K45/06 ,  A61K2300/00

Abstract: Invented is a method of treating cancer or a pre-cancerous syndrome in a mammal, including a human, in need thereof which comprises the administration of an effective amount of a non-peptide thrombopoietin (TPO) receptor agonist or TPO cell cycle activator and a chemotherapeutic agent to such mammal, suitably a human.

Abstract translation: 本发明是一种在有需要的哺乳动物（包括人）中治疗癌症或癌前综合征的方法，其包括施用有效量的非肽血小板生成素（TPO）受体激动剂或TPO细胞周期激活剂和 这种哺乳动物，合适地是人的化学治疗剂。

公开(公告)号：US20110081312A1

公开(公告)日：2011-04-07

申请号：US12873565

申请日：2010-09-01

Applicant: Stephen MOORE

Inventor： Stephen MOORE

IPC: A61K38/20 ,  A61K39/395 ,  A61K35/12 ,  C12N5/02 ,  A61K38/16 ,  A61K38/18 ,  A61P7/00 ,  A61K31/4152

CPC classification number: C07D231/46 ,  A61K31/4152 ,  A61K38/193 ,  A61K45/06 ,  C07D231/08 ,  A61K2300/00

Abstract: An improved thrombopoietin mimetic, the bis-(monoethanolamine) salt of 3′-[(2Z)-[1-(3,4-dimethylphenyl)-1,5-dihydro-3-methyl-5-oxo-4H-pyrazol-4-ylidene]hydrazino]-2′-hydroxy-[1,1′-biphenyl]-3-carboxylic acid.

Abstract translation: 改进的血小板生成素模拟物，3' - [（2Z） - [1-（3,4-二甲基苯基）-1,5-二氢-3-甲基-5-氧代-4H-吡唑并[ -4-亚基]肼基] -2'-羟基 - [1,1'-联苯] -3-羧酸。

公开(公告)号：US20110034568A1

公开(公告)日：2011-02-10

申请号：US12883873

申请日：2010-09-16

Applicant: Lenard M. Lichtenberger

Inventor： Lenard M. Lichtenberger

IPC: A61K47/44 ,  A61K47/24 ,  A61P29/00 ,  A61P35/00 ,  A61P25/28 ,  A61P19/02 ,  A61P9/00 ,  A61K47/22 ,  A61K47/08

CPC classification number: A61K47/24 ,  A61K9/0053 ,  A61K9/107 ,  A61K9/1075 ,  A61K31/167 ,  A61K31/192 ,  A61K31/195 ,  A61K31/196 ,  A61K31/405 ,  A61K31/4152 ,  A61K31/5415 ,  A61K31/616 ,  A61K31/685 ,  A61K47/44 ,  A61K47/55

Abstract: A novel pharmaceutical composition is provided by which nonsteroidal anti-inflammatory drugs (NSAIDs) are added directly to phospholipid-containing oil such as lecithin oils or to a bio-compatible oil to which an phospholipid has been added to make a NSAID-containing formulation that possess low gastrointestinal (GI) toxicity and enhanced therapeutic activity to treat or prevent inflammation, pain, fever, platelet aggregation, tissue ulcerations and/or other tissue disorders. The composition of the invention are in the form of a non-aqueous solution, paste, suspension, dispersion, colloidal suspension or in the form of an aqueous emulsion or microemulstion for internal, oral, direct or topical administration.

Abstract translation: 提供了一种新的药物组合物，通过其将非甾体抗炎药（NSAID）直接加入到含磷脂的油例如卵磷脂油或已加入磷脂的生物相容性油中以制备含NSAID的制剂， 具有低胃肠道（GI）毒性和增强的治疗活性以治疗或预防炎症，疼痛，发热，血小板聚集，组织溃疡和/或其他组织疾病。 本发明的组合物是非水溶液，糊剂，悬浮液，分散体，胶体悬浮液或用于内部，口服，直接或局部给药的水性乳液或微乳液形式的形式。

公开(公告)号：US20110003799A1

公开(公告)日：2011-01-06

申请号：US12877499

申请日：2010-09-08

Applicant: Valerio BERDINI ,  Michael Alistair O'BRIEN ,  Maria Grazia CARR ,  Theresa Rachel EARLY ,  Adrian Liam GILL ,  Gary TREWARTHA ,  Alison Jo-Anne WOOLFORD ,  Andrew James WOODHEAD ,  Paul Graham WYATT

Inventor： Valerio BERDINI ,  Michael Alistair O'BRIEN ,  Maria Grazia CARR ,  Theresa Rachel EARLY ,  Adrian Liam GILL ,  Gary TREWARTHA ,  Alison Jo-Anne WOOLFORD ,  Andrew James WOODHEAD ,  Paul Graham WYATT

IPC: A61K31/415 ,  C07D231/38 ,  C07D231/40 ,  C07D403/12 ,  A61K31/4155 ,  C07D401/12 ,  A61K31/4439 ,  A61K31/4196 ,  A61K31/454 ,  A61K31/496 ,  C07D413/12 ,  A61K31/5377 ,  C07D417/12 ,  A61K31/541 ,  A61P35/00

CPC classification number: C07D231/38 ,  A61K31/415 ,  A61K31/4152 ,  A61K31/4155 ,  A61K31/416 ,  A61K31/4178 ,  A61K31/4196 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/541 ,  A61K45/06 ,  C04B35/632 ,  C07D231/14 ,  C07D231/40 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D453/02 ,  C07D471/04

Abstract: The invention provides compounds of the formula (0) or salts or tautomers or N-oxides or solvates thereof for use in the prophylaxis or treatment of disease states and conditions such as cancers mediated by cyclin-dependent kinase and glycogen synthase kinase-3. In formula (0): X is a group R1-A-NR4— or a 5- or 6-membered carbocyclic or heterocyclic ring; A is a bond, SO2, C═O, NRg(C═O) or O(C═O) wherein Rg is hydrogen or C1-4 hydrocarbyl optionally substituted by hydroxy or C1-4 alkoxy; Y is a bond or an alkylene chain of 1, 2 or 3 carbon atoms in length; R1 is hydrogen; a carbocyclic or heterocyclic group having from 3 to 12 ring members; or a C1-8 hydrocarbyl group optionally substituted by one or more substituents selected from halogen (e.g. fluorine), hydroxy, C1-4 hydrocarbyloxy, amino, mono- or di-C1-4 hydrocarbylamino, and carbocyclic or heterocyclic groups having from 3 to 12 ring members, and wherein 1 or 2 of the carbon atoms of the hydrocarbyl group may optionally be replaced by an atom or group selected from O, S, NH, SO, SO2; R2 is hydrogen; halogen; C1-4 alkoxy (e.g. methoxy); or a C1-4 hydrocarbyl group optionally substituted by halogen (e.g. fluorine), hydroxyl or C1-4 alkoxy (e.g. methoxy); R3 is selected from hydrogen and carbocyclic and heterocyclic groups having from 3 to 12 ring members; and R4 is hydrogen or a C1-4 hydrocarbyl group optionally substituted by halogen (e.g. fluorine), hydroxyl or C1-4 alkoxy (e.g. methoxy).

Abstract translation: 本发明提供式（O）的化合物或其盐或互变异构体或N-氧化物或溶剂合物，用于预防或治疗疾病状态和病症，例如由细胞周期蛋白依赖性激酶和糖原合酶激酶-3介导的癌症。 在式（0）中：X为基团R 1 -A-NR 4 - 或5或6元碳环或杂环; A是键，SO 2，C = O，NR g（C = O）或O（C = O），其中R g是氢或任选被羟基或C 1-4烷氧基取代的C 1-4烃基; Y是长度为1,2或3个碳原子的键或亚烷基链; R1是氢; 具有3至12个环成员的碳环或杂环基; 或任选被一个或多个选自卤素（例如氟），羟基，C 1-4烃氧基，氨基，单或二-C 1-4烃基氨基的取代基取代的C 1-8烃基，以及具有3至 12个环成员，并且其中烃基的1或2个碳原子可以任选地被选自O，S，NH，SO，SO 2的原子或基团取代; R2是氢; 卤素; C 1-4烷氧基（如甲氧基）; 或任选被卤素（例如氟），羟基或C 1-4烷氧基（例如甲氧基）取代的C 1-4烃基; R 3选自具有3至12个环成员的氢和碳环和杂环基; 和R 4是氢或任选被卤素（例如氟），羟基或C 1-4烷氧基（例如甲氧基）取代的C 1-4烃基。

公开(公告)号：US07745638B2

公开(公告)日：2010-06-29

申请号：US11875470

申请日：2007-10-19

Applicant: Valerio Berdini ,  Michael Alistair O'Brien ,  Maria Grazia Carr ,  Theresa Rachel Early ,  Adrian Liam Gill ,  Gary Trewartha ,  Alison Jo-Anne Woolford ,  Andrew James Woodhead ,  Paul Graham Wyatt

Inventor： Valerio Berdini ,  Michael Alistair O'Brien ,  Maria Grazia Carr ,  Theresa Rachel Early ,  Adrian Liam Gill ,  Gary Trewartha ,  Alison Jo-Anne Woolford ,  Andrew James Woodhead ,  Paul Graham Wyatt

IPC: C07D231/10

CPC classification number: C07D231/38 ,  A61K31/415 ,  A61K31/4152 ,  A61K31/4155 ,  A61K31/416 ,  A61K31/4178 ,  A61K31/4196 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/541 ,  A61K45/06 ,  C04B35/632 ,  C07D231/14 ,  C07D231/40 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D453/02 ,  C07D471/04

Abstract: The invention provides compounds of the formula (0) or salts or tautomers or N-oxides or solvates thereof for use in the prophylaxis or treatment of disease states and conditions such as cancers mediated by cyclin-dependent kinase and glycogen synthase kinase-3. In formula (0): X is a group R1—A—NR4— or a 5- or 6-membered carbocyclic or heterocyclic ring; A is a bond, SO2, C═O, NRg(C═O) or O(C═O) wherein Rg is hydrogen or C1-4 hydrocarbyl optionally substituted by hydroxy or C1-4 alkoxy; Y is a bond or an alkylene chain of 1, 2 or 3 carbon atoms in length; R1 is hydrogen; a carbocyclic or heterocyclic group having from 3 to 12 ring members; or a C1-8 hydrocarbyl group optionally substituted by one or more substituents selected from halogen (e.g. fluorine), hydroxy, C1-4 hydrocarbyloxy, amino, mono- or di-C1-4 hydrocarbylamino, and carbocyclic or heterocyclic groups having from 3 to 12 ring members, and wherein 1 or 2 of the carbon atoms of the hydrocarbyl group may optionally be replaced by an atom or group selected from O, S, NH, SO, SO2; R2 is hydrogen; halogen; C1-4 alkoxy (e.g. methoxy); or a C1-4 hydrocarbyl group optionally substituted by halogen (e.g. fluorine), hydroxyl or C1-4 alkoxy (e.g. methoxy); R3 is selected from hydrogen and carbocyclic and heterocyclic groups having from 3 to 12 ring members; and R4 is hydrogen or a C1-4 hydrocarbyl group optionally substituted by halogen (e.g. fluorine), hydroxyl or C1-4 alkoxy (e.g. methoxy).

Abstract translation: 本发明提供式（O）的化合物或其盐或互变异构体或N-氧化物或溶剂合物，用于预防或治疗疾病状态和病症，例如由细胞周期蛋白依赖性激酶和糖原合酶激酶-3介导的癌症。 在式（0）中：X为基团R 1 -A-NR 4 - 或5或6元碳环或杂环; A是键，SO 2，C = O，NR g（C = O）或O（C = O），其中R g是氢或任选被羟基或C 1-4烷氧基取代的C 1-4烃基; Y是长度为1,2或3个碳原子的键或亚烷基链; R1是氢; 具有3至12个环成员的碳环或杂环基; 或任选被一个或多个选自卤素（例如氟），羟基，C 1-4烃氧基，氨基，单或二-C 1-4烃基氨基的取代基取代的C 1-8烃基，以及具有3至 12个环成员，并且其中烃基的1或2个碳原子可以任选地被选自O，S，NH，SO，SO 2的原子或基团取代; R2是氢; 卤素; C 1-4烷氧基（如甲氧基）; 或任选被卤素（例如氟），羟基或C 1-4烷氧基（例如甲氧基）取代的C 1-4烃基; R 3选自具有3至12个环成员的氢和碳环和杂环基; 和R 4是氢或任选被卤素（例如氟），羟基或C 1-4烷氧基（例如甲氧基）取代的C 1-4烃基。