公开(公告)号：US06828341B2

公开(公告)日：2004-12-07

申请号：US10108086

申请日：2002-03-27

Applicant: Russell Joseph DeOrazio ,  Sham Shridhar Nikam ,  Ian Leslie Scott ,  Brian Alan Sherer

Inventor： Russell Joseph DeOrazio ,  Sham Shridhar Nikam ,  Ian Leslie Scott ,  Brian Alan Sherer

IPC: C07D41304

CPC classification number: C07D413/04 ,  C07D263/58 ,  C07D413/12 ,  C07D417/12

Abstract: Described are cyclohexylamine derivatives of Formula I and pharmaceutically acceptable salts thereof, wherein R1, g, *, R, V, B, E, Y, G, H, X1, and d are as defined in the description. The compounds of Formulas I, VI, and VIa are antagonists of NMDA receptor channel complexes useful for treating cerebral vascular disorders such as, for example, stroke, cerebral ischemia, trauma, hypoglycemia, anxiety, migraine headache, convulsions, Parkinson's disease, aminoglycoside antibiotics-induced hearing loss, psychosis, glaucoma, CMV retinitis, opioid tolerance or withdrawal, chronic pain, or urinary incontinence.

Abstract translation: 描述了式I的环己胺衍生物及其药学上可接受的盐，其中R1，g，*，R，V，B，E，Y，G，H，X1和d如说明书中所定义。 式I，VI和VIa的化合物是可用于治疗脑血管病症例如中风，脑缺血，创伤，低血糖，焦虑，偏头痛，抽搐，帕金森病，氨基糖苷类抗生素的NMDA受体通道复合物的拮抗剂 引起的听力损失，精神病，青光眼，CMV视网膜炎，阿片样物质耐受或戒断，慢性疼痛或尿失禁。

公开(公告)号：US06919377B2

公开(公告)日：2005-07-19

申请号：US10258721

申请日：2001-04-24

Applicant: Russell Joseph Deorazio ,  Sham Shridhar Nikam ,  Ian Leslie Scott ,  Brian Alan Sherer ,  Lawrence David Wise

Inventor： Russell Joseph Deorazio ,  Sham Shridhar Nikam ,  Ian Leslie Scott ,  Brian Alan Sherer ,  Lawrence David Wise

IPC: C07D213/74 ,  A61K31/135 ,  A61K31/136 ,  A61K31/137 ,  A61K31/138 ,  A61K31/165 ,  A61K31/27 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/4409 ,  A61K45/00 ,  A61P3/00 ,  A61P9/10 ,  A61P13/02 ,  A61P17/02 ,  A61P25/00 ,  A61P25/02 ,  A61P25/04 ,  A61P25/06 ,  A61P25/08 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/36 ,  A61P27/02 ,  A61P27/06 ,  A61P27/16 ,  A61P29/00 ,  A61P43/00 ,  C07C215/54 ,  C07C215/56 ,  C07C215/64 ,  C07C217/16 ,  C07C217/60 ,  C07C217/62 ,  C07C233/23 ,  C07C235/14 ,  C07C235/22 ,  C07C271/24 ,  C07C323/25 ,  C07D213/38 ,  C07D213/02 ,  A61K31/44

CPC classification number: C07C323/25 ,  C07B2200/07 ,  C07C215/64 ,  C07C217/16 ,  C07C217/60 ,  C07C217/62 ,  C07C233/23 ,  C07C235/22 ,  C07C271/24 ,  C07C2601/14 ,  C07D213/38

Abstract: Described are compounds of Formula I and Formula II and their pharmaceutically acceptable salts. The compounds of Formulas I and II are antagonists of NMDA receptor channel complexes useful for treating cerebral vascular disorders such as, for example, cerebral ischemia, cardiac arrest, stroke, and Parkinson's disease.

Abstract translation: 描述了式I和式II的化合物及其药学上可接受的盐。 式I和II的化合物是可用于治疗脑血管病症例如脑缺血，心脏骤停，中风和帕金森病的NMDA受体通道复合物的拮抗剂。

公开(公告)号：US08697697B2

公开(公告)日：2014-04-15

申请号：US13977948

申请日：2012-01-03

Applicant: David Fairfax ,  Russell Joseph Deorazio

Inventor： David Fairfax ,  Russell Joseph Deorazio

IPC: A01N43/66 ,  A61K31/53 ,  A01N43/58 ,  A01N43/60 ,  A61K31/50 ,  A01N43/42 ,  A61K31/44 ,  C07D491/02 ,  C07D498/02 ,  C07D251/00 ,  C07D239/70 ,  C07D241/36

CPC classification number: C07D471/04 ,  C07D487/04

Abstract: This invention describes substituted pyrazole derivatives of Formula I and methods of making and using the compounds. These compounds have utility in the treatment of conditions or diseases in which modification of the activity of ERK would have a positive therapeutic outcome, for instance various cancers, psoriasis and actinic keratosis.

Abstract translation: 本发明描述了式I的取代的吡唑衍生物及其制备和使用方法。 这些化合物可用于治疗其中ERK的活性修饰具有阳性治疗结果的病症或疾病，例如各种癌症，牛皮癣和光化性角化病。

公开(公告)号：US06683101B2

公开(公告)日：2004-01-27

申请号：US10297263

申请日：2002-12-03

Applicant: Russell Joseph Deorazio ,  Sham Shridhar Nikam ,  Ian Leslie Scott ,  Brian Alan Sherer ,  Lawrence David Wise

Inventor： Russell Joseph Deorazio ,  Sham Shridhar Nikam ,  Ian Leslie Scott ,  Brian Alan Sherer ,  Lawrence David Wise

IPC: A61K314184

CPC classification number: C07D263/58 ,  C07D235/26

Abstract: Described are heterocycle-substituted cyclohexylamines of formula (I), and their pharmaceutically acceptable salts thereof. The compounds of the formula (I) are antagonists of NMDA receptor channel complexes useful for treating cerebral vascular disorders such as, for example, cerebral ischemia, cardiac arrest, stroke, and Parkinson's disease,

Abstract translation: 描述了式（I）的杂环取代的环己胺及其药学上可接受的盐。 式（I）的化合物是可用于治疗脑血管病症例如脑缺血，心脏骤停，中风和帕金森病的NMDA受体通道复合物的拮抗剂，

公开(公告)号：US20140011806A1

公开(公告)日：2014-01-09

申请号：US13977948

申请日：2012-01-03

Applicant: David Fairfax ,  Russell Joseph Deorazio

Inventor： David Fairfax ,  Russell Joseph Deorazio

IPC: C07D471/04

CPC classification number: C07D471/04 ,  C07D487/04

Abstract: This invention describes substituted pyrazole derivatives of Formula I and methods of making and using the compounds. These compounds have utility in the treatment of conditions or diseases in which modification of the activity of ERK would have a positive therapeutic outcome, for instance various cancers, psoriasis and actinic keratosis.

Abstract translation: 本发明描述了式I的取代的吡唑衍生物及其制备和使用方法。 这些化合物可用于治疗其中ERK的活性修饰具有阳性治疗结果的病症或疾病，例如各种癌症，牛皮癣和光化性角化病。

公开(公告)号：US06765022B2

公开(公告)日：2004-07-20

申请号：US10297055

申请日：2002-12-02

Applicant: Russell Joseph Deorazio ,  Sham Shridhar Nikam ,  Ian Leslie Scott ,  Brian Alan Sherer ,  Lawrence David Wise

Inventor： Russell Joseph Deorazio ,  Sham Shridhar Nikam ,  Ian Leslie Scott ,  Brian Alan Sherer ,  Lawrence David Wise

IPC: A61K31137

CPC classification number: C07C215/60 ,  C07C215/52 ,  C07C215/54 ,  C07C2601/14

Abstract: Described are cyclobexylamine derivatives of Formula I, Formula II, or Formula III and their pharmaceutically acceptable salts thereof: The compounds are antagonists of NMDA receptor channel complexes useful for treating cerebral vascular disorders such as, for example, cerebral ischemia, cardiac arrest, stroke, and Parkinson's disease. The substituents are described in the specification.

Abstract translation: 描述了式I，式II或式III的环丁胺衍生物及其药学上可接受的盐：该化合物是可用于治疗脑血管病症的NMDA受体通道复合物的拮抗剂，例如脑缺血，心脏骤停，中风， 和帕金森病。 取代基在说明书中描述。