High penetration compositions and their applications
High penetration compositions and their applications
 CN 102,307,857 A
 Filed: 12/04/2009
 Published: 01/04/2012
 Est. Priority Date: 12/04/2008
 Status: Active Application
First Claim
1. the highpenetrability composition of female medicine comprises the structural formula D51 that is selected from as among Fig. 6, structural formula D52, structural formula D53;
 Structural formula D54, structural formula D55, structural formula D56;
Structural formula D57, structural formula D58, structural formula D59;
Structural formula D510, structural formula D511, structural formula D512;
Structural formula D513, structural formula D514, structural formula D515;
Structural formula D516, structural formula D517, structural formula D518;
Structural formula D519, structural formula D520, structural formula D521;
Structural formula D522, structural formula D523, structural formula D524;
Structural formula D525, structural formula D526, structural formula D527;
Structural formula D528, structural formula D529, structural formula D530;
Structural formula D531, structural formula D532, structural formula D533;
Structural formula D534, structural formula D535, structural formula D536;
Structural formula D537, structural formula D538, structural formula D539;
Structural formula D540, structural formula D541, structural formula D542;
Structural formula D543, structural formula D544, structural formula D545;
Structural formula D546, structural formula D547, structural formula D548;
Structural formula D549, structural formula D550, structural formula D551;
Structural formula D552, structural formula D553, structural formula D554;
Structural formula D555, structural formula D556, structural formula D557;
Structural formula D558, structural formula D559, structural formula D560;
Structural formula D561, structural formula D562, structural formula D563;
Structural formula D564, structural formula D565, structural formula D566;
Structural formula D567, structural formula D568, structural formula D569;
Structural formula D570, structural formula D571, structural formula D572;
Structural formula D573, structural formula D574, structural formula D575;
Structural formula D576, structural formula D577, structural formula D578;
Structural formula D579, structural formula D580, structural formula D581;
Structural formula D582, structural formula D583, structural formula D584;
Structural formula D585, structural formula D586, structural formula D587;
Structural formula D588, structural formula D589, structural formula D590;
Structural formula D591, structural formula D592, structural formula D593;
Structural formula D594, structural formula D595, structural formula D596;
Structural formula D597, structural formula D598, structural formula D599;
Structural formula D5100, structural formula D5101, structural formula D5102;
Structural formula D5103, structural formula D5104, structural formula D5105;
Structural formula D5106, structural formula D5107, structural formula D5108;
Structural formula D5109, structural formula D5110, structural formula D5111;
Structural formula D5112, structural formula D5113, structural formula D5114;
Structural formula D5115, structural formula D5116, structural formula D5117;
Structural formula D5118, structural formula D5119, structural formula D5120;
Structural formula D5121, structural formula D5122, structural formula D5123;
Structural formula D5124, structural formula D5125, structural formula D5126;
Structural formula D5127, structural formula D5128, structural formula D5129;
Structural formula D5130, structural formula D5131, structural formula D5132;
Structural formula D5133, structural formula D5134, structural formula D5135;
Structural formula D5136, structural formula D5137, structural formula D5138;
Structural formula D5139;
Structural formula D5140, structural formula D5141, structural formula D5142;
Structural formula D5143;
Structural formula D5144, structural formula D5145, structural formula D5146;
Structural formula D5147;
Structural formula D5148, structural formula D5149, structural formula D5150;
Structural formula D5151;
Structural formula D5152, structural formula D5153, structural formula D5154;
Structural formula D5155;
Structural formula D5156, structural formula D5157, structural formula D5158;
Structural formula D5159;
Structural formula D5160, structural formula D5161, structural formula D5162;
Structural formula D5163;
Structural formula D5164, structural formula D5165, structural formula D5166;
Structural formula D5167;
Structural formula D5168, structural formula D5169, structural formula D5170;
Structural formula D5171;
Structural formula D5172, structural formula D5173, structural formula D5174;
Structural formula D5175;
Structural formula D5176, structural formula D5177, structural formula D5178;
Structural formula D5179;
Structural formula D5180, structural formula D5181, structural formula D5182;
Structural formula D5183;
Structural formula D5184, structural formula D5185, structural formula D5186;
Structural formula D5187;
Structural formula D5188, structural formula D5189, structural formula D5190;
Structural formula D5191;
Structural formula D5192, structural formula D5193, structural formula D5194;
Structural formula D5195;
Structural formula D5196, structural formula D5197, structural formula D5198;
Structural formula D5199;
Structural formula D5200, structural formula D5201, structural formula D5202;
Structural formula D5203;
Structural formula D5204, structural formula D5205, structural formula D5206;
Structural formula D5207;
Structural formula D5208, structural formula D5209, structural formula D5210;
Structural formula D5211;
Structural formula D5212, structural formula D5213, structural formula D5214;
Structural formula D5215;
Structural formula D5216, structural formula D5217, structural formula D5218;
Structural formula D5219;
Structural formula D5220, structural formula D5221, structural formula D5222;
Structural formula D5223;
Structural formula D5224, structural formula D5225, structural formula D5226;
Structural formula D5227;
Structural formula D5228, structural formula D5229, structural formula D5230;
Structural formula D5231;
Structural formula D5232, structural formula D5233, structural formula D5234;
Structural formula D5235;
Structural formula D5236, structural formula D5237, structural formula D5238;
Structural formula D5239;
Structural formula D5240, structural formula D5241, structural formula D5242;
Structural formula D5243;
Structural formula L, structural formula L3 and structural formula L4;
Chinese PRB Reexamination
Abstract
High penetration compositions (HPC) of a parent compound, which are capable of crossing biological barriers with high penetration efficiency. The HPCs are capable of being converted to parent drugs or parent drugrelated compounds such as metabolites after crossing one or more biological barriers and thus can render treatments for the conditions that the parent drugs or parent drugrelated compounds can. Additionally, the HPCs are capable of reaching areas that their parent drugs or parent drugrelated compounds may not be able to access or to render a sufficient concentration at the target areas HPCs of NSAIA, for example, have demonstrated indications such as treating hair loss. A HPC can be administered to a subject through various administration routes, e. g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.

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No References
25 Claims

1. the highpenetrability composition of female medicine comprises the structural formula D51 that is selected from as among Fig. 6, structural formula D52, structural formula D53;
 Structural formula D54, structural formula D55, structural formula D56;
Structural formula D57, structural formula D58, structural formula D59;
Structural formula D510, structural formula D511, structural formula D512;
Structural formula D513, structural formula D514, structural formula D515;
Structural formula D516, structural formula D517, structural formula D518;
Structural formula D519, structural formula D520, structural formula D521;
Structural formula D522, structural formula D523, structural formula D524;
Structural formula D525, structural formula D526, structural formula D527;
Structural formula D528, structural formula D529, structural formula D530;
Structural formula D531, structural formula D532, structural formula D533;
Structural formula D534, structural formula D535, structural formula D536;
Structural formula D537, structural formula D538, structural formula D539;
Structural formula D540, structural formula D541, structural formula D542;
Structural formula D543, structural formula D544, structural formula D545;
Structural formula D546, structural formula D547, structural formula D548;
Structural formula D549, structural formula D550, structural formula D551;
Structural formula D552, structural formula D553, structural formula D554;
Structural formula D555, structural formula D556, structural formula D557;
Structural formula D558, structural formula D559, structural formula D560;
Structural formula D561, structural formula D562, structural formula D563;
Structural formula D564, structural formula D565, structural formula D566;
Structural formula D567, structural formula D568, structural formula D569;
Structural formula D570, structural formula D571, structural formula D572;
Structural formula D573, structural formula D574, structural formula D575;
Structural formula D576, structural formula D577, structural formula D578;
Structural formula D579, structural formula D580, structural formula D581;
Structural formula D582, structural formula D583, structural formula D584;
Structural formula D585, structural formula D586, structural formula D587;
Structural formula D588, structural formula D589, structural formula D590;
Structural formula D591, structural formula D592, structural formula D593;
Structural formula D594, structural formula D595, structural formula D596;
Structural formula D597, structural formula D598, structural formula D599;
Structural formula D5100, structural formula D5101, structural formula D5102;
Structural formula D5103, structural formula D5104, structural formula D5105;
Structural formula D5106, structural formula D5107, structural formula D5108;
Structural formula D5109, structural formula D5110, structural formula D5111;
Structural formula D5112, structural formula D5113, structural formula D5114;
Structural formula D5115, structural formula D5116, structural formula D5117;
Structural formula D5118, structural formula D5119, structural formula D5120;
Structural formula D5121, structural formula D5122, structural formula D5123;
Structural formula D5124, structural formula D5125, structural formula D5126;
Structural formula D5127, structural formula D5128, structural formula D5129;
Structural formula D5130, structural formula D5131, structural formula D5132;
Structural formula D5133, structural formula D5134, structural formula D5135;
Structural formula D5136, structural formula D5137, structural formula D5138;
Structural formula D5139;
Structural formula D5140, structural formula D5141, structural formula D5142;
Structural formula D5143;
Structural formula D5144, structural formula D5145, structural formula D5146;
Structural formula D5147;
Structural formula D5148, structural formula D5149, structural formula D5150;
Structural formula D5151;
Structural formula D5152, structural formula D5153, structural formula D5154;
Structural formula D5155;
Structural formula D5156, structural formula D5157, structural formula D5158;
Structural formula D5159;
Structural formula D5160, structural formula D5161, structural formula D5162;
Structural formula D5163;
Structural formula D5164, structural formula D5165, structural formula D5166;
Structural formula D5167;
Structural formula D5168, structural formula D5169, structural formula D5170;
Structural formula D5171;
Structural formula D5172, structural formula D5173, structural formula D5174;
Structural formula D5175;
Structural formula D5176, structural formula D5177, structural formula D5178;
Structural formula D5179;
Structural formula D5180, structural formula D5181, structural formula D5182;
Structural formula D5183;
Structural formula D5184, structural formula D5185, structural formula D5186;
Structural formula D5187;
Structural formula D5188, structural formula D5189, structural formula D5190;
Structural formula D5191;
Structural formula D5192, structural formula D5193, structural formula D5194;
Structural formula D5195;
Structural formula D5196, structural formula D5197, structural formula D5198;
Structural formula D5199;
Structural formula D5200, structural formula D5201, structural formula D5202;
Structural formula D5203;
Structural formula D5204, structural formula D5205, structural formula D5206;
Structural formula D5207;
Structural formula D5208, structural formula D5209, structural formula D5210;
Structural formula D5211;
Structural formula D5212, structural formula D5213, structural formula D5214;
Structural formula D5215;
Structural formula D5216, structural formula D5217, structural formula D5218;
Structural formula D5219;
Structural formula D5220, structural formula D5221, structural formula D5222;
Structural formula D5223;
Structural formula D5224, structural formula D5225, structural formula D5226;
Structural formula D5227;
Structural formula D5228, structural formula D5229, structural formula D5230;
Structural formula D5231;
Structural formula D5232, structural formula D5233, structural formula D5234;
Structural formula D5235;
Structural formula D5236, structural formula D5237, structural formula D5238;
Structural formula D5239;
Structural formula D5240, structural formula D5241, structural formula D5242;
Structural formula D5243;
Structural formula L, structural formula L3 and structural formula L4;
 Structural formula D54, structural formula D55, structural formula D56;

2. the purposes of highpenetrability composition is made the medicament that can penetrate biological barrier;
 The highpenetrability composition that the highpenetrability composition is selected from the said highpenetrability composition of claim 1 and comprises one of following structure;
structural formula L;
Structural formula L3 or structural formula L4;
Wherein T is selected from structural formula T1;
Fg is selected from structural formula F2;
Structural formula F79 is to structural formula F125;
Structural formula F132 is to structural formula F211;
Structural formula F2360 is to structural formula F2403;
Structural formula F2408 is to structural formula F2411;
Structural formula F2418 or structural formula F2419;
F3 is selected from structural formula F335 to structural formula F340, and F4 is structural formula F41.
 The highpenetrability composition that the highpenetrability composition is selected from the said highpenetrability composition of claim 1 and comprises one of following structure;

3. in the purposes of the described highpenetrability composition of claim 2, transparent biological barrier comprises blood brain barrier, blood cerebrospinal fluid barrier and bloodsynovia barrier.

4. the described highpenetrability composition of claim 1 is processed the treatable disease of female medicine that is used for treating them behind the medicament.

5. in the use of the said highpenetrability composition of claim 4, said highpenetrability composition reaches the female medicine of the needed dosage of curative effect less than them.

6. in the use of the said highpenetrability composition of claim 5, said highpenetrability composition reach the needed dosage of curative effect be they female pharmaceutical quantities 50% or lower.

7. in the use of the said highpenetrability composition of claim 5, said highpenetrability composition reach the needed dosage of curative effect be they female pharmaceutical quantities 25% or lower.

8. in the use of the said highpenetrability composition of claim 5, said highpenetrability composition reach the needed dosage of curative effect be they female pharmaceutical quantities 10% or lower.

9. in the use of the said highpenetrability composition of claim 5, said highpenetrability composition reach the needed dosage of curative effect be they female pharmaceutical quantities 5% or lower.

10. in the use of the said highpenetrability composition of claim 5, said highpenetrability composition reach the needed dosage of curative effect be they female pharmaceutical quantities 2% or lower.

11. in the use of the said highpenetrability composition of claim 5, reach the needed dosage of curative effect and be they female pharmaceutical quantities 1% or lower.

12. in the use of the said highpenetrability composition of claim 5, said highpenetrability composition reach the needed dosage of curative effect be they female pharmaceutical quantities 0.1% or lower.

13. the purposes of the highpenetrability composition of nonsteroidal antiinflammatory drugs is made medicament, the treatment lupus erythematosus;
 Multiple sclerosis;
Prostate cancer;
Osteocarcinoma;
Type i diabetes;
Type ii diabetes;
Apoplexy;
Heart trouble;
Alopecia and bald;
Achromachia;
Vitiligo;
Parkinsonism;
Alzheimer'"'"'s disease;
Spinal injury;
Glaucoma;
Cataract;
Aging;
Amyotrophic lateral sclerosis (ALS);
Oculopharyngeal muscular dystrophy disease (OPMD);
Myotonic dystrophy (MD);
Duchenne muscular dystrophy (DMD);
Polymyositis (PM);
Dermatomyositis (DM);
Inclusion body myositis (IBM);
Hyperthyroidism;
Hepatic fibrosis;
Gallbladder;
Lung;
Pancreas;
Spleen;
Gi tract;
Cholelith;
The skin injury aberrant angiogenesis;
Birthmark;
Mole;
Skin is superfluous;
Senile plaque;
Acne;
Cystic acne;Acute and chronic cough, organ transplant rejection and osteoporosis of skin after running sore or redness, blackhead, papule, warts, tubercle, epidermoid cyst, keratosis pilaris, skin sagging, wrinkle, crow'"'"'s feet, yellowish pink skin speckle, rosacea, the treatment.
 Multiple sclerosis;

14. the highpenetrability composition of yperite can be processed medicament, treatment cancer of the stomach, multiple myeloma or brain tumor.

15. the purposes of the highpenetrability composition of polypeptide is made medicament, the treatment alzheimer disease.

16. the purposes of the highpenetrability composition of prostaglandin(PG) is made medicament, promotes the growth of hair and eyelashes.

17. the purposes of the highpenetrability composition of β
 Nei Xiananleikangshengsu is made medicament, treatment microorganism relative disease.

18. the purposes of the highpenetrability composition of steroid is made medicament, treatment cerebral trauma, apoplexy, embryo nidation, early pregnancy, discoid lupus erythematosus, systemic lupus erythematous, multiple sclerosis and female contraception.

19. the said highpenetrability composition of claim 18 on, steroid comprises progesterone, desogestrel and ethinylestradiol.

20. the purposes of the highpenetrability composition of glibornuride is made medicament, the treatment diabetes.

21. the purposes of the highpenetrability composition of atenolol USP 23 is made medicament, treatment hypertension.

22. in the purposes of the described highpenetrability composition of the arbitrary claim of claim 2 to claim 21;
 Highpenetrability composition or its pharmaceutical cpd can be applied to organism through transdermal, saturating mucous membrane, intranasal, transvaginal, transoral, perrectum mode.

23. in the purposes of the described highpenetrability composition of the arbitrary claim of claim 2 to claim 21, highpenetrability composition or its medical composition can be applied to organism through the mode of local application.

24. in the purposes of the described highpenetrability composition of the arbitrary claim of claim 2 to claim 21;
 Highpenetrability composition or its medical composition, can administered through oral or the mode that is used for nose, vagina, rectum, parenteral, subcutaneous injection, intramuscular injection, intravenous injection, suction or medicament for the eyes be applied to organism.

25. the purposes of the highpenetrability composition of nonsteroidal antiinflammatory drugs is used for treating the disease that plant is caused by virus, fungi, insect.
Specification(s)